U.S. BRAND NAMES — Differin®
CANADIAN BRAND NAMES — Differin® XP; Differin®
SYNONYMS — CD271
THERAPEUTIC CATEGORY Acne Products
DOSING — Topical: Children >12 years and Adults: Apply topically once daily in the evening
(For additional information see "Adapalene: Drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, topical: 0.1% (15 g, 45 g)
Gel, topical: 0.1% (15 g, 45 g) [alcohol free]
Pledget, topical: 0.1% (60s) [DSC]
Solution, topical: 0.1% (30 mL) [DSC]
GENERIC AVAILABLE — No
ADMINISTRATION — Topical: After cleansing the affected area with mild or soapless cleanser, using gloves, apply a thin film of medication (cream or gel) before retiring in the evening. Avoid contact with eyes, angles of the nose, lips and mucous membranes.
USE — Topical treatment of acne vulgaris
ADVERSE REACTIONS Dermatologic: Erythema, scaling, dry skin, skin irritation, pruritus, acne flares, photosensitivity, sunburn, skin discoloration
Local: Pruritus or burning immediately after application
Ophthalmic: Eyelid edema, conjunctivitis
CONTRAINDICATIONS — Hypersensitivity to adapalene or any component; sunburn
PRECAUTIONS — Use with caution in patients with eczema
WARNINGS — Avoid excessive exposure to sunlight and sunlamps; avoid contact with abraded skin, mucous membranes, eyes, mouth, or angles of the nose
DRUG INTERACTIONS — Topical sulfur, benzoyl peroxide, salicylic acid, and resorcinol potentiate adverse reactions seen with adapalene; other topical products containing alcohol, astringents, or lime may increase drying effects
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Reduction in lesion size and/or inflammation; reduction in the number of lesions
STABILITY — Store at controlled room temperature
MECHANISM OF ACTION — Retinoid-like compound which is a modulator of cellular differentiation, keratinization, and inflammatory processes, all of which represent important features in the pathology of acne vulgaris
PHARMACODYNAMICS — Onset of action: 8-12 weeks
PHARMACOKINETICS Absorption: Absorption through the skin is very low; only trace amounts have been measured in serum after chronic application
Elimination: Primarily in bile
PATIENT INFORMATION — For external use only; apply using gloves; avoid contact with eyes, mouth, mucous membranes, or open wounds. Do not apply occlusive dressing. Moisturizers may be used if necessary; however, products containing alpha hydroxy or glycolic acids should be avoided. Wax epilation should not be performed on treated skin due to the potential for skin erosions. Transient burning or stinging immediately after applying may occur. Mild to moderate redness, dryness, scaling, burning or itching are likely to occur during the first 2-4 weeks and will usually lessen with continued use; report worsening of condition or skin redness, dryness, peeling, or burning that persists between applications to the healthcare provider. May cause photosensitivity reactions (eg, exposure to sunlight may cause severe sunburn, skin rash, redness, or itching); avoid exposure to sunlight and artificial light sources (sunlamps, tanning booth/bed); wear protective clothing, wide-brimmed hats, sunglasses, and lip sunscreen (SPF 15); use a sunscreen [broad-spectrum sunscreen or physical sunscreen(preferred) or sunblock with SPF 15]; contact physician if reaction occurs.
Thursday, January 31, 2008
Adapalene
U.S. BRAND NAMES — Differin®
CANADIAN BRAND NAMES — Differin® XP; Differin®
SYNONYMS — CD271
THERAPEUTIC CATEGORY Acne Products
DOSING — Topical: Children >12 years and Adults: Apply topically once daily in the evening
(For additional information see "Adapalene: Drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, topical: 0.1% (15 g, 45 g)
Gel, topical: 0.1% (15 g, 45 g) [alcohol free]
Pledget, topical: 0.1% (60s) [DSC]
Solution, topical: 0.1% (30 mL) [DSC]
GENERIC AVAILABLE — No
ADMINISTRATION — Topical: After cleansing the affected area with mild or soapless cleanser, using gloves, apply a thin film of medication (cream or gel) before retiring in the evening. Avoid contact with eyes, angles of the nose, lips and mucous membranes.
USE — Topical treatment of acne vulgaris
ADVERSE REACTIONS Dermatologic: Erythema, scaling, dry skin, skin irritation, pruritus, acne flares, photosensitivity, sunburn, skin discoloration
Local: Pruritus or burning immediately after application
Ophthalmic: Eyelid edema, conjunctivitis
CONTRAINDICATIONS — Hypersensitivity to adapalene or any component; sunburn
PRECAUTIONS — Use with caution in patients with eczema
WARNINGS — Avoid excessive exposure to sunlight and sunlamps; avoid contact with abraded skin, mucous membranes, eyes, mouth, or angles of the nose
DRUG INTERACTIONS — Topical sulfur, benzoyl peroxide, salicylic acid, and resorcinol potentiate adverse reactions seen with adapalene; other topical products containing alcohol, astringents, or lime may increase drying effects
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Reduction in lesion size and/or inflammation; reduction in the number of lesions
STABILITY — Store at controlled room temperature
MECHANISM OF ACTION — Retinoid-like compound which is a modulator of cellular differentiation, keratinization, and inflammatory processes, all of which represent important features in the pathology of acne vulgaris
PHARMACODYNAMICS — Onset of action: 8-12 weeks
PHARMACOKINETICS Absorption: Absorption through the skin is very low; only trace amounts have been measured in serum after chronic application
Elimination: Primarily in bile
PATIENT INFORMATION — For external use only; apply using gloves; avoid contact with eyes, mouth, mucous membranes, or open wounds. Do not apply occlusive dressing. Moisturizers may be used if necessary; however, products containing alpha hydroxy or glycolic acids should be avoided. Wax epilation should not be performed on treated skin due to the potential for skin erosions. Transient burning or stinging immediately after applying may occur. Mild to moderate redness, dryness, scaling, burning or itching are likely to occur during the first 2-4 weeks and will usually lessen with continued use; report worsening of condition or skin redness, dryness, peeling, or burning that persists between applications to the healthcare provider. May cause photosensitivity reactions (eg, exposure to sunlight may cause severe sunburn, skin rash, redness, or itching); avoid exposure to sunlight and artificial light sources (sunlamps, tanning booth/bed); wear protective clothing, wide-brimmed hats, sunglasses, and lip sunscreen (SPF 15); use a sunscreen [broad-spectrum sunscreen or physical sunscreen(preferred) or sunblock with SPF 15]; contact physician if reaction occurs.
CANADIAN BRAND NAMES — Differin® XP; Differin®
SYNONYMS — CD271
THERAPEUTIC CATEGORY Acne Products
DOSING — Topical: Children >12 years and Adults: Apply topically once daily in the evening
(For additional information see "Adapalene: Drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, topical: 0.1% (15 g, 45 g)
Gel, topical: 0.1% (15 g, 45 g) [alcohol free]
Pledget, topical: 0.1% (60s) [DSC]
Solution, topical: 0.1% (30 mL) [DSC]
GENERIC AVAILABLE — No
ADMINISTRATION — Topical: After cleansing the affected area with mild or soapless cleanser, using gloves, apply a thin film of medication (cream or gel) before retiring in the evening. Avoid contact with eyes, angles of the nose, lips and mucous membranes.
USE — Topical treatment of acne vulgaris
ADVERSE REACTIONS Dermatologic: Erythema, scaling, dry skin, skin irritation, pruritus, acne flares, photosensitivity, sunburn, skin discoloration
Local: Pruritus or burning immediately after application
Ophthalmic: Eyelid edema, conjunctivitis
CONTRAINDICATIONS — Hypersensitivity to adapalene or any component; sunburn
PRECAUTIONS — Use with caution in patients with eczema
WARNINGS — Avoid excessive exposure to sunlight and sunlamps; avoid contact with abraded skin, mucous membranes, eyes, mouth, or angles of the nose
DRUG INTERACTIONS — Topical sulfur, benzoyl peroxide, salicylic acid, and resorcinol potentiate adverse reactions seen with adapalene; other topical products containing alcohol, astringents, or lime may increase drying effects
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Reduction in lesion size and/or inflammation; reduction in the number of lesions
STABILITY — Store at controlled room temperature
MECHANISM OF ACTION — Retinoid-like compound which is a modulator of cellular differentiation, keratinization, and inflammatory processes, all of which represent important features in the pathology of acne vulgaris
PHARMACODYNAMICS — Onset of action: 8-12 weeks
PHARMACOKINETICS Absorption: Absorption through the skin is very low; only trace amounts have been measured in serum after chronic application
Elimination: Primarily in bile
PATIENT INFORMATION — For external use only; apply using gloves; avoid contact with eyes, mouth, mucous membranes, or open wounds. Do not apply occlusive dressing. Moisturizers may be used if necessary; however, products containing alpha hydroxy or glycolic acids should be avoided. Wax epilation should not be performed on treated skin due to the potential for skin erosions. Transient burning or stinging immediately after applying may occur. Mild to moderate redness, dryness, scaling, burning or itching are likely to occur during the first 2-4 weeks and will usually lessen with continued use; report worsening of condition or skin redness, dryness, peeling, or burning that persists between applications to the healthcare provider. May cause photosensitivity reactions (eg, exposure to sunlight may cause severe sunburn, skin rash, redness, or itching); avoid exposure to sunlight and artificial light sources (sunlamps, tanning booth/bed); wear protective clothing, wide-brimmed hats, sunglasses, and lip sunscreen (SPF 15); use a sunscreen [broad-spectrum sunscreen or physical sunscreen(preferred) or sunblock with SPF 15]; contact physician if reaction occurs.
Acyclovir
U.S. BRAND NAMES — Zovirax®
CANADIAN BRAND NAMES — Apo-Acyclovir®; Gen-Acyclovir; Nu-Acyclovir; ratio-Acyclovir; Zovirax®
SYNONYMS — Aciclovir; ACV; Acycloguanosine
THERAPEUTIC CATEGORY Antiviral Agent, OralAntiviral Agent, ParenteralAntiviral Agent, Topical
DOSING
(For additional information see "Acyclovir: Drug information")Genital herpes simplex virus (HSV): First infection: Oral: Children: 40-80 mg/kg/day in 3-4 divided doses for 5-10 days; maximum dose: 1 g/day Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5-10 days I.V.: Children and Adults: 5 mg/kg/dose every 8 hours for 5-7 days
Genital HSV infection: Recurrence: Oral: Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5 days
Recurrent genital and cutaneous (ocular) HSV episodes in a patient with frequent recurrences, chronic suppressive therapy: Oral: Children: 40-80 mg/kg/day in 3 divided doses for up to 12 months; maximum dose: 1 g/day; re-evaluate after 12 months of treatment Adolescents and Adults: 400 mg twice daily or 400 mg 3 times/day or 200 mg 3 times/day for as long as 12 continuous months; re-evaluate after 12 months of treatment
HSV in immunocompromised host: Oral: Children:1000 mg/day in 3-5 divided doses for 7-14 days; maximum dose: 80 mg/kg/day not to exceed 1 g/day Adults: 400 mg 5 times/day for 7-14 days I.V.: Children <12 years: 10 mg/kg/dose every 8 hours for 7-14 days Children 12 years and Adults: 5 mg/kg/dose every 8 hours for 7-14 days
Prophylaxis of HSV in immunocompromised host: Oral: Children and Adults: 600-1000 mg/day in 3-5 divided doses during period of risk; maximum dose in children: 80 mg/kg/day not to exceed 1 g/day
HSV encephalitis: I.V.: Children 3 months to 12 years: 20 mg/kg/dose every 8 hours; some clinicians recommend 500 mg/m2/dose every 8 hours for 14-21 days Children >12 years and Adults: 10-15 mg/kg/dose every 8 hours for 14-21 days
Neonatal HSV: I.V.: 20 mg/kg/dose every 8 hours for 14-21 days
Varicella-zoster in immunocompromised host: I.V.: Infants <1 year: 10 mg/kg/dose every 8 hours for 7-10 days Children 1 year: 500 mg/m2/dose every 8 hours for 7-10 days or 10 mg/kg/dose every 8 hours for 7-10 days
Varicella in immunocompetent host: Oral (initiate treatment within the first 24 hours of rash onset): Children 2 years and 40 kg: 20 mg/kg/dose 4 times/day for 5 days; maximum dose: 3200 mg/day Children >40 kg and Adults: 800 mg 4 times/day for 5 days
Zoster in immunocompetent host: Oral (initiate treatment within 48 hours of rash onset): Children 12 years and Adults: 800 mg 5 times/day for 7-10 days
Prophylaxis in bone marrow transplant recipients: I.V.: Autologous patients who are HSV-seropositive: 250 mg/m2/dose every 8 hours Autologous patients who are CMV seropositive: 500 mg/m2/dose every 8 hours; for clinically symptomatic CMV infection, consider replacing acyclovir with ganciclovir
Children and Adults: Topical: Apply 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Dosing interval in renal impairment: Neonates: I.V.: Scr 0.8-1.1 mg/dL: Administer 20 mg/kg/dose every 12 hours Scr 1.2-1.5 mg/dL: Administer 20 mg/kg/dose every 24 hours Scr >1.5 mg/dL: Administer 10 mg/kg/dose every 24 hours Children 6 months and Adults: Oral:
Usual dose: 200 mg 5 times/day: Adjusted dose for Clcr <10 mL/minute: 200 mg every 12 hours Usual dose: 800 mg 5 times/day: Adjusted dose for Clcr 10-25 mL/minute: 800 mg every 8 hours Adjusted dose for Clcr <10 mL/minute: 800 mg every 12 hours I.V.: Clcr 25-50 mL/minute: Administer normal dose every 12 hours Clcr 10-25 mL/minute: Administer normal dose every 24 hours Clcr <10 mL/minute: 50% decrease in dose, administer every 24 hours Hemodialysis: Administer dose after dialysis CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg Zovirax®: 500 mg [DSC]
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) Zovirax®: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
GENERIC AVAILABLE — Yes: Excludes cream, ointment
ADMINISTRATION Oral: May administer with food; shake suspension well before use
Parenteral: Reconstitute vial for injection with paraben-free SWI; administer by slow I.V. infusion over at least 1 hour at a final concentration not to exceed 7 mg/mL since rapid infusions can cause nephrotoxicity with crystalluria and renal tubular damage; in patients who require fluid restriction, a concentration of up to 10 mg/mL has been infused; concentration >10 mg/mL increases the risk of phlebitis
USE — Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV 1 and HSV 2) infections; herpes simplex encephalitis; herpes zoster infections; varicella-zoster infections in healthy, nonpregnant persons >13 years of age, children >12 months of age who have a chronic skin or lung disorder or are receiving long-term aspirin therapy, and immunocompromised patients
ADVERSE REACTIONS Central nervous system: Headache, lethargy, delirium, coma, dizziness, seizures, pain, insomnia, fever, hallucinations, aggressive behavior, ataxia
Dermatologic: Skin rash, pruritus, alopecia, erythema multiforme, urticaria, photosensitivity, Stevens-Johnson syndrome, angioedema
Gastrointestinal: Nausea, vomiting, diarrhea
Hematologic: Bone marrow suppression, neutropenia, thrombotic thrombocytopenic purpura/hemolytic uremic syndrome
Hepatic: Elevated liver enzymes, hepatitis, jaundice, hyperbilirubinemia
Local: Phlebitis at injection site, tissue necrosis upon extravasation, local pain and stinging with topical use
Neuromuscular & skeletal: Tremulousness, myalgia, paresthesia
Renal: Nephrotoxicity, hematuria, elevated BUN and serum creatinine
Respiratory: Sore throat
Miscellaneous: Diaphoresis, anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acyclovir, valacyclovir, or any component
PRECAUTIONS — Use with caution in patients with renal disease, dehydration, underlying neurologic disease, and in patients with hypoxia, hepatic, or electrolyte abnormalities; dosage should be reduced in patients with renal impairment
WARNINGS — HSV and VZV with reduced susceptibility to acyclovir have been isolated from immunocompromised patients, especially with advanced HIV infection; renal failure, in some cases resulting in death, has occurred with acyclovir
DRUG INTERACTIONS — Zidovudine (neurotoxicity); probenecid decreases renal clearance of acyclovir
FOOD INTERACTIONS — Food does not appear to affect absorption
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Urinalysis, BUN, serum creatinine, I & O; liver enzymes, CBC; neutrophil count at least twice weekly in neonates receiving acyclovir 60 mg/kg/day I.V.
STABILITY — Incompatible with blood products and protein-containing solutions; reconstituted 50 mg/mL solution should be used within 12 hours; do not refrigerate reconstituted solutions as they may precipitate
MECHANISM OF ACTION — Inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and by incorporation into viral DNA
PHARMACOKINETICS Absorption: Oral: 15% to 30%
Distribution: Widely distributed throughout the body including brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, and the CSF; CSF acyclovir concentration is 50% of serum concentration; crosses the placenta; excreted into breast milk; Vd: Neonates to 3 months of age: 28.8 L/1.73 m2 Children 1-2 years: 31.6 L/1.73 m2 Children 2-7 years: 42 L/1.73 m2
Protein binding: <30%
Half-life, terminal phase: Neonates: 4 hours Children 1-12 years: 2-3 hours Adults: 2-3.5 hours (with normal renal function)
Time to peak serum concentration: Oral: Within 1.5-2 hours
Elimination: Primary route is the kidney with 30% to 90% of a dose excreted unchanged in the urine; requires dosage adjustment with renal impairment; hemodialysis removes ~60% of a dose while removal by peritoneal dialysis is to a much lesser extent; supplemental dose recommended after hemodialysis
NURSING IMPLICATIONS — Maintain adequate hydration and urine output the first 2 hours after I.V. infusion to decrease the risk of nephrotoxicity; check infusion site for phlebitis; avoid extravasation
ADDITIONAL INFORMATION — Sodium content of 1 g: 4.2 mEq
CANADIAN BRAND NAMES — Apo-Acyclovir®; Gen-Acyclovir; Nu-Acyclovir; ratio-Acyclovir; Zovirax®
SYNONYMS — Aciclovir; ACV; Acycloguanosine
THERAPEUTIC CATEGORY Antiviral Agent, OralAntiviral Agent, ParenteralAntiviral Agent, Topical
DOSING
(For additional information see "Acyclovir: Drug information")Genital herpes simplex virus (HSV): First infection: Oral: Children: 40-80 mg/kg/day in 3-4 divided doses for 5-10 days; maximum dose: 1 g/day Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5-10 days I.V.: Children and Adults: 5 mg/kg/dose every 8 hours for 5-7 days
Genital HSV infection: Recurrence: Oral: Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5 days
Recurrent genital and cutaneous (ocular) HSV episodes in a patient with frequent recurrences, chronic suppressive therapy: Oral: Children: 40-80 mg/kg/day in 3 divided doses for up to 12 months; maximum dose: 1 g/day; re-evaluate after 12 months of treatment Adolescents and Adults: 400 mg twice daily or 400 mg 3 times/day or 200 mg 3 times/day for as long as 12 continuous months; re-evaluate after 12 months of treatment
HSV in immunocompromised host: Oral: Children:1000 mg/day in 3-5 divided doses for 7-14 days; maximum dose: 80 mg/kg/day not to exceed 1 g/day Adults: 400 mg 5 times/day for 7-14 days I.V.: Children <12 years: 10 mg/kg/dose every 8 hours for 7-14 days Children 12 years and Adults: 5 mg/kg/dose every 8 hours for 7-14 days
Prophylaxis of HSV in immunocompromised host: Oral: Children and Adults: 600-1000 mg/day in 3-5 divided doses during period of risk; maximum dose in children: 80 mg/kg/day not to exceed 1 g/day
HSV encephalitis: I.V.: Children 3 months to 12 years: 20 mg/kg/dose every 8 hours; some clinicians recommend 500 mg/m2/dose every 8 hours for 14-21 days Children >12 years and Adults: 10-15 mg/kg/dose every 8 hours for 14-21 days
Neonatal HSV: I.V.: 20 mg/kg/dose every 8 hours for 14-21 days
Varicella-zoster in immunocompromised host: I.V.: Infants <1 year: 10 mg/kg/dose every 8 hours for 7-10 days Children 1 year: 500 mg/m2/dose every 8 hours for 7-10 days or 10 mg/kg/dose every 8 hours for 7-10 days
Varicella in immunocompetent host: Oral (initiate treatment within the first 24 hours of rash onset): Children 2 years and 40 kg: 20 mg/kg/dose 4 times/day for 5 days; maximum dose: 3200 mg/day Children >40 kg and Adults: 800 mg 4 times/day for 5 days
Zoster in immunocompetent host: Oral (initiate treatment within 48 hours of rash onset): Children 12 years and Adults: 800 mg 5 times/day for 7-10 days
Prophylaxis in bone marrow transplant recipients: I.V.: Autologous patients who are HSV-seropositive: 250 mg/m2/dose every 8 hours Autologous patients who are CMV seropositive: 500 mg/m2/dose every 8 hours; for clinically symptomatic CMV infection, consider replacing acyclovir with ganciclovir
Children and Adults: Topical: Apply 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Dosing interval in renal impairment: Neonates: I.V.: Scr 0.8-1.1 mg/dL: Administer 20 mg/kg/dose every 12 hours Scr 1.2-1.5 mg/dL: Administer 20 mg/kg/dose every 24 hours Scr >1.5 mg/dL: Administer 10 mg/kg/dose every 24 hours Children 6 months and Adults: Oral:
Usual dose: 200 mg 5 times/day: Adjusted dose for Clcr <10 mL/minute: 200 mg every 12 hours Usual dose: 800 mg 5 times/day: Adjusted dose for Clcr 10-25 mL/minute: 800 mg every 8 hours Adjusted dose for Clcr <10 mL/minute: 800 mg every 12 hours I.V.: Clcr 25-50 mL/minute: Administer normal dose every 12 hours Clcr 10-25 mL/minute: Administer normal dose every 24 hours Clcr <10 mL/minute: 50% decrease in dose, administer every 24 hours Hemodialysis: Administer dose after dialysis CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg Zovirax®: 500 mg [DSC]
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) Zovirax®: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
GENERIC AVAILABLE — Yes: Excludes cream, ointment
ADMINISTRATION Oral: May administer with food; shake suspension well before use
Parenteral: Reconstitute vial for injection with paraben-free SWI; administer by slow I.V. infusion over at least 1 hour at a final concentration not to exceed 7 mg/mL since rapid infusions can cause nephrotoxicity with crystalluria and renal tubular damage; in patients who require fluid restriction, a concentration of up to 10 mg/mL has been infused; concentration >10 mg/mL increases the risk of phlebitis
USE — Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV 1 and HSV 2) infections; herpes simplex encephalitis; herpes zoster infections; varicella-zoster infections in healthy, nonpregnant persons >13 years of age, children >12 months of age who have a chronic skin or lung disorder or are receiving long-term aspirin therapy, and immunocompromised patients
ADVERSE REACTIONS Central nervous system: Headache, lethargy, delirium, coma, dizziness, seizures, pain, insomnia, fever, hallucinations, aggressive behavior, ataxia
Dermatologic: Skin rash, pruritus, alopecia, erythema multiforme, urticaria, photosensitivity, Stevens-Johnson syndrome, angioedema
Gastrointestinal: Nausea, vomiting, diarrhea
Hematologic: Bone marrow suppression, neutropenia, thrombotic thrombocytopenic purpura/hemolytic uremic syndrome
Hepatic: Elevated liver enzymes, hepatitis, jaundice, hyperbilirubinemia
Local: Phlebitis at injection site, tissue necrosis upon extravasation, local pain and stinging with topical use
Neuromuscular & skeletal: Tremulousness, myalgia, paresthesia
Renal: Nephrotoxicity, hematuria, elevated BUN and serum creatinine
Respiratory: Sore throat
Miscellaneous: Diaphoresis, anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acyclovir, valacyclovir, or any component
PRECAUTIONS — Use with caution in patients with renal disease, dehydration, underlying neurologic disease, and in patients with hypoxia, hepatic, or electrolyte abnormalities; dosage should be reduced in patients with renal impairment
WARNINGS — HSV and VZV with reduced susceptibility to acyclovir have been isolated from immunocompromised patients, especially with advanced HIV infection; renal failure, in some cases resulting in death, has occurred with acyclovir
DRUG INTERACTIONS — Zidovudine (neurotoxicity); probenecid decreases renal clearance of acyclovir
FOOD INTERACTIONS — Food does not appear to affect absorption
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Urinalysis, BUN, serum creatinine, I & O; liver enzymes, CBC; neutrophil count at least twice weekly in neonates receiving acyclovir 60 mg/kg/day I.V.
STABILITY — Incompatible with blood products and protein-containing solutions; reconstituted 50 mg/mL solution should be used within 12 hours; do not refrigerate reconstituted solutions as they may precipitate
MECHANISM OF ACTION — Inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and by incorporation into viral DNA
PHARMACOKINETICS Absorption: Oral: 15% to 30%
Distribution: Widely distributed throughout the body including brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, and the CSF; CSF acyclovir concentration is 50% of serum concentration; crosses the placenta; excreted into breast milk; Vd: Neonates to 3 months of age: 28.8 L/1.73 m2 Children 1-2 years: 31.6 L/1.73 m2 Children 2-7 years: 42 L/1.73 m2
Protein binding: <30%
Half-life, terminal phase: Neonates: 4 hours Children 1-12 years: 2-3 hours Adults: 2-3.5 hours (with normal renal function)
Time to peak serum concentration: Oral: Within 1.5-2 hours
Elimination: Primary route is the kidney with 30% to 90% of a dose excreted unchanged in the urine; requires dosage adjustment with renal impairment; hemodialysis removes ~60% of a dose while removal by peritoneal dialysis is to a much lesser extent; supplemental dose recommended after hemodialysis
NURSING IMPLICATIONS — Maintain adequate hydration and urine output the first 2 hours after I.V. infusion to decrease the risk of nephrotoxicity; check infusion site for phlebitis; avoid extravasation
ADDITIONAL INFORMATION — Sodium content of 1 g: 4.2 mEq
Acyclovir
U.S. BRAND NAMES — Zovirax®
CANADIAN BRAND NAMES — Apo-Acyclovir®; Gen-Acyclovir; Nu-Acyclovir; ratio-Acyclovir; Zovirax®
SYNONYMS — Aciclovir; ACV; Acycloguanosine
THERAPEUTIC CATEGORY Antiviral Agent, OralAntiviral Agent, ParenteralAntiviral Agent, Topical
DOSING
(For additional information see "Acyclovir: Drug information")Genital herpes simplex virus (HSV): First infection: Oral: Children: 40-80 mg/kg/day in 3-4 divided doses for 5-10 days; maximum dose: 1 g/day Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5-10 days I.V.: Children and Adults: 5 mg/kg/dose every 8 hours for 5-7 days
Genital HSV infection: Recurrence: Oral: Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5 days
Recurrent genital and cutaneous (ocular) HSV episodes in a patient with frequent recurrences, chronic suppressive therapy: Oral: Children: 40-80 mg/kg/day in 3 divided doses for up to 12 months; maximum dose: 1 g/day; re-evaluate after 12 months of treatment Adolescents and Adults: 400 mg twice daily or 400 mg 3 times/day or 200 mg 3 times/day for as long as 12 continuous months; re-evaluate after 12 months of treatment
HSV in immunocompromised host: Oral: Children:1000 mg/day in 3-5 divided doses for 7-14 days; maximum dose: 80 mg/kg/day not to exceed 1 g/day Adults: 400 mg 5 times/day for 7-14 days I.V.: Children <12 years: 10 mg/kg/dose every 8 hours for 7-14 days Children 12 years and Adults: 5 mg/kg/dose every 8 hours for 7-14 days
Prophylaxis of HSV in immunocompromised host: Oral: Children and Adults: 600-1000 mg/day in 3-5 divided doses during period of risk; maximum dose in children: 80 mg/kg/day not to exceed 1 g/day
HSV encephalitis: I.V.: Children 3 months to 12 years: 20 mg/kg/dose every 8 hours; some clinicians recommend 500 mg/m2/dose every 8 hours for 14-21 days Children >12 years and Adults: 10-15 mg/kg/dose every 8 hours for 14-21 days
Neonatal HSV: I.V.: 20 mg/kg/dose every 8 hours for 14-21 days
Varicella-zoster in immunocompromised host: I.V.: Infants <1 year: 10 mg/kg/dose every 8 hours for 7-10 days Children 1 year: 500 mg/m2/dose every 8 hours for 7-10 days or 10 mg/kg/dose every 8 hours for 7-10 days
Varicella in immunocompetent host: Oral (initiate treatment within the first 24 hours of rash onset): Children 2 years and 40 kg: 20 mg/kg/dose 4 times/day for 5 days; maximum dose: 3200 mg/day Children >40 kg and Adults: 800 mg 4 times/day for 5 days
Zoster in immunocompetent host: Oral (initiate treatment within 48 hours of rash onset): Children 12 years and Adults: 800 mg 5 times/day for 7-10 days
Prophylaxis in bone marrow transplant recipients: I.V.: Autologous patients who are HSV-seropositive: 250 mg/m2/dose every 8 hours Autologous patients who are CMV seropositive: 500 mg/m2/dose every 8 hours; for clinically symptomatic CMV infection, consider replacing acyclovir with ganciclovir
Children and Adults: Topical: Apply 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Dosing interval in renal impairment: Neonates: I.V.: Scr 0.8-1.1 mg/dL: Administer 20 mg/kg/dose every 12 hours Scr 1.2-1.5 mg/dL: Administer 20 mg/kg/dose every 24 hours Scr >1.5 mg/dL: Administer 10 mg/kg/dose every 24 hours Children 6 months and Adults: Oral:
Usual dose: 200 mg 5 times/day: Adjusted dose for Clcr <10 mL/minute: 200 mg every 12 hours Usual dose: 800 mg 5 times/day: Adjusted dose for Clcr 10-25 mL/minute: 800 mg every 8 hours Adjusted dose for Clcr <10 mL/minute: 800 mg every 12 hours I.V.: Clcr 25-50 mL/minute: Administer normal dose every 12 hours Clcr 10-25 mL/minute: Administer normal dose every 24 hours Clcr <10 mL/minute: 50% decrease in dose, administer every 24 hours Hemodialysis: Administer dose after dialysis CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg Zovirax®: 500 mg [DSC]
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) Zovirax®: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
GENERIC AVAILABLE — Yes: Excludes cream, ointment
ADMINISTRATION Oral: May administer with food; shake suspension well before use
Parenteral: Reconstitute vial for injection with paraben-free SWI; administer by slow I.V. infusion over at least 1 hour at a final concentration not to exceed 7 mg/mL since rapid infusions can cause nephrotoxicity with crystalluria and renal tubular damage; in patients who require fluid restriction, a concentration of up to 10 mg/mL has been infused; concentration >10 mg/mL increases the risk of phlebitis
USE — Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV 1 and HSV 2) infections; herpes simplex encephalitis; herpes zoster infections; varicella-zoster infections in healthy, nonpregnant persons >13 years of age, children >12 months of age who have a chronic skin or lung disorder or are receiving long-term aspirin therapy, and immunocompromised patients
ADVERSE REACTIONS Central nervous system: Headache, lethargy, delirium, coma, dizziness, seizures, pain, insomnia, fever, hallucinations, aggressive behavior, ataxia
Dermatologic: Skin rash, pruritus, alopecia, erythema multiforme, urticaria, photosensitivity, Stevens-Johnson syndrome, angioedema
Gastrointestinal: Nausea, vomiting, diarrhea
Hematologic: Bone marrow suppression, neutropenia, thrombotic thrombocytopenic purpura/hemolytic uremic syndrome
Hepatic: Elevated liver enzymes, hepatitis, jaundice, hyperbilirubinemia
Local: Phlebitis at injection site, tissue necrosis upon extravasation, local pain and stinging with topical use
Neuromuscular & skeletal: Tremulousness, myalgia, paresthesia
Renal: Nephrotoxicity, hematuria, elevated BUN and serum creatinine
Respiratory: Sore throat
Miscellaneous: Diaphoresis, anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acyclovir, valacyclovir, or any component
PRECAUTIONS — Use with caution in patients with renal disease, dehydration, underlying neurologic disease, and in patients with hypoxia, hepatic, or electrolyte abnormalities; dosage should be reduced in patients with renal impairment
WARNINGS — HSV and VZV with reduced susceptibility to acyclovir have been isolated from immunocompromised patients, especially with advanced HIV infection; renal failure, in some cases resulting in death, has occurred with acyclovir
DRUG INTERACTIONS — Zidovudine (neurotoxicity); probenecid decreases renal clearance of acyclovir
FOOD INTERACTIONS — Food does not appear to affect absorption
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Urinalysis, BUN, serum creatinine, I & O; liver enzymes, CBC; neutrophil count at least twice weekly in neonates receiving acyclovir 60 mg/kg/day I.V.
STABILITY — Incompatible with blood products and protein-containing solutions; reconstituted 50 mg/mL solution should be used within 12 hours; do not refrigerate reconstituted solutions as they may precipitate
MECHANISM OF ACTION — Inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and by incorporation into viral DNA
PHARMACOKINETICS Absorption: Oral: 15% to 30%
Distribution: Widely distributed throughout the body including brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, and the CSF; CSF acyclovir concentration is 50% of serum concentration; crosses the placenta; excreted into breast milk; Vd: Neonates to 3 months of age: 28.8 L/1.73 m2 Children 1-2 years: 31.6 L/1.73 m2 Children 2-7 years: 42 L/1.73 m2
Protein binding: <30%
Half-life, terminal phase: Neonates: 4 hours Children 1-12 years: 2-3 hours Adults: 2-3.5 hours (with normal renal function)
Time to peak serum concentration: Oral: Within 1.5-2 hours
Elimination: Primary route is the kidney with 30% to 90% of a dose excreted unchanged in the urine; requires dosage adjustment with renal impairment; hemodialysis removes ~60% of a dose while removal by peritoneal dialysis is to a much lesser extent; supplemental dose recommended after hemodialysis
NURSING IMPLICATIONS — Maintain adequate hydration and urine output the first 2 hours after I.V. infusion to decrease the risk of nephrotoxicity; check infusion site for phlebitis; avoid extravasation
ADDITIONAL INFORMATION — Sodium content of 1 g: 4.2 mEq
CANADIAN BRAND NAMES — Apo-Acyclovir®; Gen-Acyclovir; Nu-Acyclovir; ratio-Acyclovir; Zovirax®
SYNONYMS — Aciclovir; ACV; Acycloguanosine
THERAPEUTIC CATEGORY Antiviral Agent, OralAntiviral Agent, ParenteralAntiviral Agent, Topical
DOSING
(For additional information see "Acyclovir: Drug information")Genital herpes simplex virus (HSV): First infection: Oral: Children: 40-80 mg/kg/day in 3-4 divided doses for 5-10 days; maximum dose: 1 g/day Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5-10 days I.V.: Children and Adults: 5 mg/kg/dose every 8 hours for 5-7 days
Genital HSV infection: Recurrence: Oral: Adolescents and Adults: 200 mg 5 times/day or 400 mg 3 times/day for 5 days
Recurrent genital and cutaneous (ocular) HSV episodes in a patient with frequent recurrences, chronic suppressive therapy: Oral: Children: 40-80 mg/kg/day in 3 divided doses for up to 12 months; maximum dose: 1 g/day; re-evaluate after 12 months of treatment Adolescents and Adults: 400 mg twice daily or 400 mg 3 times/day or 200 mg 3 times/day for as long as 12 continuous months; re-evaluate after 12 months of treatment
HSV in immunocompromised host: Oral: Children:1000 mg/day in 3-5 divided doses for 7-14 days; maximum dose: 80 mg/kg/day not to exceed 1 g/day Adults: 400 mg 5 times/day for 7-14 days I.V.: Children <12 years: 10 mg/kg/dose every 8 hours for 7-14 days Children 12 years and Adults: 5 mg/kg/dose every 8 hours for 7-14 days
Prophylaxis of HSV in immunocompromised host: Oral: Children and Adults: 600-1000 mg/day in 3-5 divided doses during period of risk; maximum dose in children: 80 mg/kg/day not to exceed 1 g/day
HSV encephalitis: I.V.: Children 3 months to 12 years: 20 mg/kg/dose every 8 hours; some clinicians recommend 500 mg/m2/dose every 8 hours for 14-21 days Children >12 years and Adults: 10-15 mg/kg/dose every 8 hours for 14-21 days
Neonatal HSV: I.V.: 20 mg/kg/dose every 8 hours for 14-21 days
Varicella-zoster in immunocompromised host: I.V.: Infants <1 year: 10 mg/kg/dose every 8 hours for 7-10 days Children 1 year: 500 mg/m2/dose every 8 hours for 7-10 days or 10 mg/kg/dose every 8 hours for 7-10 days
Varicella in immunocompetent host: Oral (initiate treatment within the first 24 hours of rash onset): Children 2 years and 40 kg: 20 mg/kg/dose 4 times/day for 5 days; maximum dose: 3200 mg/day Children >40 kg and Adults: 800 mg 4 times/day for 5 days
Zoster in immunocompetent host: Oral (initiate treatment within 48 hours of rash onset): Children 12 years and Adults: 800 mg 5 times/day for 7-10 days
Prophylaxis in bone marrow transplant recipients: I.V.: Autologous patients who are HSV-seropositive: 250 mg/m2/dose every 8 hours Autologous patients who are CMV seropositive: 500 mg/m2/dose every 8 hours; for clinically symptomatic CMV infection, consider replacing acyclovir with ganciclovir
Children and Adults: Topical: Apply 1/2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Dosing interval in renal impairment: Neonates: I.V.: Scr 0.8-1.1 mg/dL: Administer 20 mg/kg/dose every 12 hours Scr 1.2-1.5 mg/dL: Administer 20 mg/kg/dose every 24 hours Scr >1.5 mg/dL: Administer 10 mg/kg/dose every 24 hours Children 6 months and Adults: Oral:
Usual dose: 200 mg 5 times/day: Adjusted dose for Clcr <10 mL/minute: 200 mg every 12 hours Usual dose: 800 mg 5 times/day: Adjusted dose for Clcr 10-25 mL/minute: 800 mg every 8 hours Adjusted dose for Clcr <10 mL/minute: 800 mg every 12 hours I.V.: Clcr 25-50 mL/minute: Administer normal dose every 12 hours Clcr 10-25 mL/minute: Administer normal dose every 24 hours Clcr <10 mL/minute: 50% decrease in dose, administer every 24 hours Hemodialysis: Administer dose after dialysis CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule: 200 mg Zovirax®: 200 mg
Cream, topical: Zovirax®: 5% (2 g, 5 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg Zovirax®: 500 mg [DSC]
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: Zovirax®: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) Zovirax®: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg Zovirax®: 400 mg, 800 mg
GENERIC AVAILABLE — Yes: Excludes cream, ointment
ADMINISTRATION Oral: May administer with food; shake suspension well before use
Parenteral: Reconstitute vial for injection with paraben-free SWI; administer by slow I.V. infusion over at least 1 hour at a final concentration not to exceed 7 mg/mL since rapid infusions can cause nephrotoxicity with crystalluria and renal tubular damage; in patients who require fluid restriction, a concentration of up to 10 mg/mL has been infused; concentration >10 mg/mL increases the risk of phlebitis
USE — Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV 1 and HSV 2) infections; herpes simplex encephalitis; herpes zoster infections; varicella-zoster infections in healthy, nonpregnant persons >13 years of age, children >12 months of age who have a chronic skin or lung disorder or are receiving long-term aspirin therapy, and immunocompromised patients
ADVERSE REACTIONS Central nervous system: Headache, lethargy, delirium, coma, dizziness, seizures, pain, insomnia, fever, hallucinations, aggressive behavior, ataxia
Dermatologic: Skin rash, pruritus, alopecia, erythema multiforme, urticaria, photosensitivity, Stevens-Johnson syndrome, angioedema
Gastrointestinal: Nausea, vomiting, diarrhea
Hematologic: Bone marrow suppression, neutropenia, thrombotic thrombocytopenic purpura/hemolytic uremic syndrome
Hepatic: Elevated liver enzymes, hepatitis, jaundice, hyperbilirubinemia
Local: Phlebitis at injection site, tissue necrosis upon extravasation, local pain and stinging with topical use
Neuromuscular & skeletal: Tremulousness, myalgia, paresthesia
Renal: Nephrotoxicity, hematuria, elevated BUN and serum creatinine
Respiratory: Sore throat
Miscellaneous: Diaphoresis, anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to acyclovir, valacyclovir, or any component
PRECAUTIONS — Use with caution in patients with renal disease, dehydration, underlying neurologic disease, and in patients with hypoxia, hepatic, or electrolyte abnormalities; dosage should be reduced in patients with renal impairment
WARNINGS — HSV and VZV with reduced susceptibility to acyclovir have been isolated from immunocompromised patients, especially with advanced HIV infection; renal failure, in some cases resulting in death, has occurred with acyclovir
DRUG INTERACTIONS — Zidovudine (neurotoxicity); probenecid decreases renal clearance of acyclovir
FOOD INTERACTIONS — Food does not appear to affect absorption
PREGNANCY RISK FACTOR — C (show table)
MONITORING PARAMETERS — Urinalysis, BUN, serum creatinine, I & O; liver enzymes, CBC; neutrophil count at least twice weekly in neonates receiving acyclovir 60 mg/kg/day I.V.
STABILITY — Incompatible with blood products and protein-containing solutions; reconstituted 50 mg/mL solution should be used within 12 hours; do not refrigerate reconstituted solutions as they may precipitate
MECHANISM OF ACTION — Inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and by incorporation into viral DNA
PHARMACOKINETICS Absorption: Oral: 15% to 30%
Distribution: Widely distributed throughout the body including brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, and the CSF; CSF acyclovir concentration is 50% of serum concentration; crosses the placenta; excreted into breast milk; Vd: Neonates to 3 months of age: 28.8 L/1.73 m2 Children 1-2 years: 31.6 L/1.73 m2 Children 2-7 years: 42 L/1.73 m2
Protein binding: <30%
Half-life, terminal phase: Neonates: 4 hours Children 1-12 years: 2-3 hours Adults: 2-3.5 hours (with normal renal function)
Time to peak serum concentration: Oral: Within 1.5-2 hours
Elimination: Primary route is the kidney with 30% to 90% of a dose excreted unchanged in the urine; requires dosage adjustment with renal impairment; hemodialysis removes ~60% of a dose while removal by peritoneal dialysis is to a much lesser extent; supplemental dose recommended after hemodialysis
NURSING IMPLICATIONS — Maintain adequate hydration and urine output the first 2 hours after I.V. infusion to decrease the risk of nephrotoxicity; check infusion site for phlebitis; avoid extravasation
ADDITIONAL INFORMATION — Sodium content of 1 g: 4.2 mEq
Acetylcysteine
U.S. BRAND NAMES — Acetadote®
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
SYNONYMS — N-Acetyl-L-Cysteine; N-Acetylcysteine; Mercapturic Acid; NAC
THERAPEUTIC CATEGORY Antidote, AcetaminophenMucolytic Agent
DOSING
(For additional information see "Acetylcysteine: Drug information")Acetaminophen poisoning: Children and Adults: Begin treatment within 8 hours of ingestion to optimize therapy in patients whose serum acetaminophen levels fall above the "possible" toxicity line on the Rumack-Matthew nomogram Treatment is also indicated in patients with a history of known or suspected acute acetaminophen ingestion of >150 mg/kg (child) or >7.5 g (adolescent or adult) total dose when plasma levels are not available within 8-10 hours of ingestion or in patients presenting >24 hours after acute ingestion who have a measurable acetaminophen level. See Warnings. I.V.: 150 mg/kg infused over 60 minutes; followed by a 4-hour infusion of 50 mg/kg; followed by a 16-hour infusion of 100 mg/kg; equivalent to a total dose of 300 mg/kg infused over 21 hours Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until all doses are administered even though the acetaminophen plasma level has dropped below the toxic range
Nebulized inhalation: Infants: 1-2 mL of 20% solution or 2-4 mL of 10% solution until nebulized, given 3-4 times/day Children: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized, given 3-4 times/day Adolescents: 5-10 mL of 10% to 20% solution until nebulized, given 3-4 times/day Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine
Intratracheal: Children and Adults: 1-2 mL of 10% to 20% solution every 1-4 hours as needed
Distal intestinal obstruction syndrome (previously known as meconium ileus equivalent): Varying regimens have been reported (polyethylene glycol has become more widely used for this indication): Oral: Children <10 years: 30 mL of 10% solution diluted in 30 mL juice or soda 3 times/day for 24 hours Children 10 years and Adults: 60 mL of 10% solution diluted in 60 mL juice or soda 3 times/day for 24 hours Note: Prior to treatment, administer a phosphosoda enema. A clear liquid diet should be used during the 24-hour acetylcysteine treatment Rectal enema: Children: Varying dosages; 100-300 mL of 4% to 6% solution 2-4 times/day; 50 mL of 20% solution 1-4 times/day and 5-30 mL of 10% to 20% solution 3-4 times/day have been used; rectal enemas appear to have less favorable results than oral administration (Mascarenhas, 2003) Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Adults: Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); hydrate patient concurrently
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
GENERIC AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Parenteral: I.V.: Three infusions (See Usual Dosage) of different lengths: Dilute first dose (150 mg/kg) in 200 mL D5W and infuse over 60 minutes; dilute second dose (50 mg/kg) in 500 mL D5W and infuse over 4 hours; dilute third dose (100 mg/kg) in 1000 mL D5W and infuse over 16 hours; for children <40 kg and patients who are fluid restricted, the manufacturer recommends reducing the diluent to a "proportional" amount. See table for manufacturer's recommended infusion guideline for patients <40 kg. Or as an alternative to proportionally lower the diluent volume, a reasonable approach might be to utilize the concentrations resulting from using the recommended dilution for the dosage in a 50 kg patient. The calculated concentration would range between 5 mg/mL (maintenance infusion) to 37.5 mg/mL (loading dose).
Infusion Guide by Weight for Patients <40 kg Body Weight = 10 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 30 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 500 mg (2.5 mL) 5% dextrose: 70 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL Body Weight = 15 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 2250 mg (11.25 mL) 5% dextrose: 45 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 750 mg (3.75 mL) 5% dextrose: 105 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 210 mL Body Weight = 20 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 60 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2000 mg (10 mL) 5% dextrose: 280 mL Body Weight = 25 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3750 mg (18.75 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1250 mg (6.25 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2500 mg (12.5 mL) 5% dextrose: 500 mL Body Weight = 30 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 4500 mg (22.5 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 500 mL
Oral: For treatment of acetaminophen overdosage, administer as a 5% solution; dilute the 20% solution (inhalation formulation) 1:3 with a cola, orange juice, or other soft drink; use within 1 hour of preparation
Oral inhalation: May be administered by nebulization either undiluted (both 10% and 20%) or diluted in NS
Rectal: Dilute the inhalation solution in NS to the desired final concentration and administer rectally
USE Inhalation: Adjunctive therapy in patients with abnormal or viscid mucous secretions in bronchopulmonary diseases, pulmonary complications of surgery, and cystic fibrosis; diagnostic bronchial studies
Injection, Oral: Antidote for acute acetaminophen toxicity; prevention of radiocontrast-induced renal dysfunction
Oral, rectal: Treatment of distal intestinal obstruction syndrome (previously known as "meconium ileus or its equivalent")
ADVERSE REACTIONS Cardiovascular: Tachycardia, hypotension, syncope, chest tightness, vasodilation, hypertension (after large oral doses)
Central nervous system: Drowsiness, chills, dysphoria
Dermatologic: Generalized urticaria, rash, pruritus, erythema, angioedema
Gastrointestinal: Stomatitis, nausea, vomiting, dyspepsia, hemoptysis
Hepatic: Mild elevations in liver function tests have occurred after oral therapy
Ocular: Eye pain
Respiratory: Bronchospasm, rhinorrhea, cough
Miscellaneous: Anaphylactoid reactions (I.V. use; 17% in an open label study; 1% reported as severe or moderate in 10% of patients within 15 minutes of the first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after the 60 minute infusion); diaphoresis, unpleasant odor during administration
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component
PRECAUTIONS — Use with caution in patients with asthma or previous history of bronchospasm
WARNINGS — Serious anaphylactoid reactions including death in a patient with asthma have been reported after I.V. use; acute flushing and erythema may occur 30-60 minutes into an I.V. infusion, resolving spontaneously; the infusion may be interrupted until treatment of allergic symptoms is initiated; if acute hypersensitivity reactions occur which do not respond to medical management (eg, antihistamines, H2 blockers) or temporarily halting infusion, discontinue use and pursue alternative management. Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow.
Acetaminophen overdose: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients) or individuals ingesting higher than recommended acetaminophen doses for extended periods of time (repeated supratherapeutic ingestion).
DRUG INTERACTIONS — May potentiate the hemodynamic effects of nitroglycerin; acetylcysteine is adsorbed by activated charcoal
PREGNANCY RISK FACTOR — B (show table)
MONITORING PARAMETERS — When used in acetaminophen overdose, determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion of immediate release formulations or 2 hours after ingestion of liquid formulations (to ensure peak levels have been obtained); coingestion of acetaminophen with other medications which may delay GI peristalsis eg, antihistamines, opioids, may require repeated serum levels to determine the peak serum level; liver function tests
STABILITY — Store at room temperature; I.V. formulation is preservative free and stable 24 hours after dilution at room temperature; opened inhalation solution vials may be stored in the refrigerator; use within 96 hours; contact with rubber, copper, iron, and cork may inactivate the drug; the light purple color of solution does not affect its activity. I.V. acetylcysteine is hyperosmolar (2600 mOsm/L) and is compatible with 5% dextrose, 0.45% sodium chloride, and SWI.
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering the viscosity. The exact mechanism of action in acetaminophen toxicity is unknown. It may act by maintaining or restoring glutathione levels or by acting as an alternative substrate for conjugation with the acetaminophen's toxic metabolite.
PHARMACODYNAMICS Onset of action: Upon inhalation, mucus liquefaction occurs maximally within 5-10 minutes
Duration of mucus liquefaction: More than 1 hour
PHARMACOKINETICS Distribution: Vd: 0.47 L/kg
Protein binding: 83%
Half-life: Reduced acetylcysteine: 2 hours Total acetylcysteine: Newborns: 11 hours Adults: 5.6 hours
Time to peak serum concentration: Oral: 1-2 hours
Elimination: Clearance: Adults: 0.11 L/hour/kg
PATIENT INFORMATION — Clear airway by coughing deeply before aerosol treatment
(For additional information see "Acetylcysteine: Patient drug information")
NURSING IMPLICATIONS — Anaphylactoid reactions following I.V. administration have been reported; have emergency treatments such as antihistamines and H2 blockers readily available for potential adverse effects; assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning; intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
SYNONYMS — N-Acetyl-L-Cysteine; N-Acetylcysteine; Mercapturic Acid; NAC
THERAPEUTIC CATEGORY Antidote, AcetaminophenMucolytic Agent
DOSING
(For additional information see "Acetylcysteine: Drug information")Acetaminophen poisoning: Children and Adults: Begin treatment within 8 hours of ingestion to optimize therapy in patients whose serum acetaminophen levels fall above the "possible" toxicity line on the Rumack-Matthew nomogram Treatment is also indicated in patients with a history of known or suspected acute acetaminophen ingestion of >150 mg/kg (child) or >7.5 g (adolescent or adult) total dose when plasma levels are not available within 8-10 hours of ingestion or in patients presenting >24 hours after acute ingestion who have a measurable acetaminophen level. See Warnings. I.V.: 150 mg/kg infused over 60 minutes; followed by a 4-hour infusion of 50 mg/kg; followed by a 16-hour infusion of 100 mg/kg; equivalent to a total dose of 300 mg/kg infused over 21 hours Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until all doses are administered even though the acetaminophen plasma level has dropped below the toxic range
Nebulized inhalation: Infants: 1-2 mL of 20% solution or 2-4 mL of 10% solution until nebulized, given 3-4 times/day Children: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized, given 3-4 times/day Adolescents: 5-10 mL of 10% to 20% solution until nebulized, given 3-4 times/day Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine
Intratracheal: Children and Adults: 1-2 mL of 10% to 20% solution every 1-4 hours as needed
Distal intestinal obstruction syndrome (previously known as meconium ileus equivalent): Varying regimens have been reported (polyethylene glycol has become more widely used for this indication): Oral: Children <10 years: 30 mL of 10% solution diluted in 30 mL juice or soda 3 times/day for 24 hours Children 10 years and Adults: 60 mL of 10% solution diluted in 60 mL juice or soda 3 times/day for 24 hours Note: Prior to treatment, administer a phosphosoda enema. A clear liquid diet should be used during the 24-hour acetylcysteine treatment Rectal enema: Children: Varying dosages; 100-300 mL of 4% to 6% solution 2-4 times/day; 50 mL of 20% solution 1-4 times/day and 5-30 mL of 10% to 20% solution 3-4 times/day have been used; rectal enemas appear to have less favorable results than oral administration (Mascarenhas, 2003) Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Adults: Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); hydrate patient concurrently
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
GENERIC AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Parenteral: I.V.: Three infusions (See Usual Dosage) of different lengths: Dilute first dose (150 mg/kg) in 200 mL D5W and infuse over 60 minutes; dilute second dose (50 mg/kg) in 500 mL D5W and infuse over 4 hours; dilute third dose (100 mg/kg) in 1000 mL D5W and infuse over 16 hours; for children <40 kg and patients who are fluid restricted, the manufacturer recommends reducing the diluent to a "proportional" amount. See table for manufacturer's recommended infusion guideline for patients <40 kg. Or as an alternative to proportionally lower the diluent volume, a reasonable approach might be to utilize the concentrations resulting from using the recommended dilution for the dosage in a 50 kg patient. The calculated concentration would range between 5 mg/mL (maintenance infusion) to 37.5 mg/mL (loading dose).
Infusion Guide by Weight for Patients <40 kg Body Weight = 10 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 30 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 500 mg (2.5 mL) 5% dextrose: 70 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL Body Weight = 15 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 2250 mg (11.25 mL) 5% dextrose: 45 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 750 mg (3.75 mL) 5% dextrose: 105 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 210 mL Body Weight = 20 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 60 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2000 mg (10 mL) 5% dextrose: 280 mL Body Weight = 25 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3750 mg (18.75 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1250 mg (6.25 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2500 mg (12.5 mL) 5% dextrose: 500 mL Body Weight = 30 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 4500 mg (22.5 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 500 mL
Oral: For treatment of acetaminophen overdosage, administer as a 5% solution; dilute the 20% solution (inhalation formulation) 1:3 with a cola, orange juice, or other soft drink; use within 1 hour of preparation
Oral inhalation: May be administered by nebulization either undiluted (both 10% and 20%) or diluted in NS
Rectal: Dilute the inhalation solution in NS to the desired final concentration and administer rectally
USE Inhalation: Adjunctive therapy in patients with abnormal or viscid mucous secretions in bronchopulmonary diseases, pulmonary complications of surgery, and cystic fibrosis; diagnostic bronchial studies
Injection, Oral: Antidote for acute acetaminophen toxicity; prevention of radiocontrast-induced renal dysfunction
Oral, rectal: Treatment of distal intestinal obstruction syndrome (previously known as "meconium ileus or its equivalent")
ADVERSE REACTIONS Cardiovascular: Tachycardia, hypotension, syncope, chest tightness, vasodilation, hypertension (after large oral doses)
Central nervous system: Drowsiness, chills, dysphoria
Dermatologic: Generalized urticaria, rash, pruritus, erythema, angioedema
Gastrointestinal: Stomatitis, nausea, vomiting, dyspepsia, hemoptysis
Hepatic: Mild elevations in liver function tests have occurred after oral therapy
Ocular: Eye pain
Respiratory: Bronchospasm, rhinorrhea, cough
Miscellaneous: Anaphylactoid reactions (I.V. use; 17% in an open label study; 1% reported as severe or moderate in 10% of patients within 15 minutes of the first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after the 60 minute infusion); diaphoresis, unpleasant odor during administration
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component
PRECAUTIONS — Use with caution in patients with asthma or previous history of bronchospasm
WARNINGS — Serious anaphylactoid reactions including death in a patient with asthma have been reported after I.V. use; acute flushing and erythema may occur 30-60 minutes into an I.V. infusion, resolving spontaneously; the infusion may be interrupted until treatment of allergic symptoms is initiated; if acute hypersensitivity reactions occur which do not respond to medical management (eg, antihistamines, H2 blockers) or temporarily halting infusion, discontinue use and pursue alternative management. Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow.
Acetaminophen overdose: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients) or individuals ingesting higher than recommended acetaminophen doses for extended periods of time (repeated supratherapeutic ingestion).
DRUG INTERACTIONS — May potentiate the hemodynamic effects of nitroglycerin; acetylcysteine is adsorbed by activated charcoal
PREGNANCY RISK FACTOR — B (show table)
MONITORING PARAMETERS — When used in acetaminophen overdose, determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion of immediate release formulations or 2 hours after ingestion of liquid formulations (to ensure peak levels have been obtained); coingestion of acetaminophen with other medications which may delay GI peristalsis eg, antihistamines, opioids, may require repeated serum levels to determine the peak serum level; liver function tests
STABILITY — Store at room temperature; I.V. formulation is preservative free and stable 24 hours after dilution at room temperature; opened inhalation solution vials may be stored in the refrigerator; use within 96 hours; contact with rubber, copper, iron, and cork may inactivate the drug; the light purple color of solution does not affect its activity. I.V. acetylcysteine is hyperosmolar (2600 mOsm/L) and is compatible with 5% dextrose, 0.45% sodium chloride, and SWI.
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering the viscosity. The exact mechanism of action in acetaminophen toxicity is unknown. It may act by maintaining or restoring glutathione levels or by acting as an alternative substrate for conjugation with the acetaminophen's toxic metabolite.
PHARMACODYNAMICS Onset of action: Upon inhalation, mucus liquefaction occurs maximally within 5-10 minutes
Duration of mucus liquefaction: More than 1 hour
PHARMACOKINETICS Distribution: Vd: 0.47 L/kg
Protein binding: 83%
Half-life: Reduced acetylcysteine: 2 hours Total acetylcysteine: Newborns: 11 hours Adults: 5.6 hours
Time to peak serum concentration: Oral: 1-2 hours
Elimination: Clearance: Adults: 0.11 L/hour/kg
PATIENT INFORMATION — Clear airway by coughing deeply before aerosol treatment
(For additional information see "Acetylcysteine: Patient drug information")
NURSING IMPLICATIONS — Anaphylactoid reactions following I.V. administration have been reported; have emergency treatments such as antihistamines and H2 blockers readily available for potential adverse effects; assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning; intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime
Acetylcysteine
U.S. BRAND NAMES — Acetadote®
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
SYNONYMS — N-Acetyl-L-Cysteine; N-Acetylcysteine; Mercapturic Acid; NAC
THERAPEUTIC CATEGORY Antidote, AcetaminophenMucolytic Agent
DOSING
(For additional information see "Acetylcysteine: Drug information")Acetaminophen poisoning: Children and Adults: Begin treatment within 8 hours of ingestion to optimize therapy in patients whose serum acetaminophen levels fall above the "possible" toxicity line on the Rumack-Matthew nomogram Treatment is also indicated in patients with a history of known or suspected acute acetaminophen ingestion of >150 mg/kg (child) or >7.5 g (adolescent or adult) total dose when plasma levels are not available within 8-10 hours of ingestion or in patients presenting >24 hours after acute ingestion who have a measurable acetaminophen level. See Warnings. I.V.: 150 mg/kg infused over 60 minutes; followed by a 4-hour infusion of 50 mg/kg; followed by a 16-hour infusion of 100 mg/kg; equivalent to a total dose of 300 mg/kg infused over 21 hours Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until all doses are administered even though the acetaminophen plasma level has dropped below the toxic range
Nebulized inhalation: Infants: 1-2 mL of 20% solution or 2-4 mL of 10% solution until nebulized, given 3-4 times/day Children: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized, given 3-4 times/day Adolescents: 5-10 mL of 10% to 20% solution until nebulized, given 3-4 times/day Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine
Intratracheal: Children and Adults: 1-2 mL of 10% to 20% solution every 1-4 hours as needed
Distal intestinal obstruction syndrome (previously known as meconium ileus equivalent): Varying regimens have been reported (polyethylene glycol has become more widely used for this indication): Oral: Children <10 years: 30 mL of 10% solution diluted in 30 mL juice or soda 3 times/day for 24 hours Children 10 years and Adults: 60 mL of 10% solution diluted in 60 mL juice or soda 3 times/day for 24 hours Note: Prior to treatment, administer a phosphosoda enema. A clear liquid diet should be used during the 24-hour acetylcysteine treatment Rectal enema: Children: Varying dosages; 100-300 mL of 4% to 6% solution 2-4 times/day; 50 mL of 20% solution 1-4 times/day and 5-30 mL of 10% to 20% solution 3-4 times/day have been used; rectal enemas appear to have less favorable results than oral administration (Mascarenhas, 2003) Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Adults: Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); hydrate patient concurrently
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
GENERIC AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Parenteral: I.V.: Three infusions (See Usual Dosage) of different lengths: Dilute first dose (150 mg/kg) in 200 mL D5W and infuse over 60 minutes; dilute second dose (50 mg/kg) in 500 mL D5W and infuse over 4 hours; dilute third dose (100 mg/kg) in 1000 mL D5W and infuse over 16 hours; for children <40 kg and patients who are fluid restricted, the manufacturer recommends reducing the diluent to a "proportional" amount. See table for manufacturer's recommended infusion guideline for patients <40 kg. Or as an alternative to proportionally lower the diluent volume, a reasonable approach might be to utilize the concentrations resulting from using the recommended dilution for the dosage in a 50 kg patient. The calculated concentration would range between 5 mg/mL (maintenance infusion) to 37.5 mg/mL (loading dose).
Infusion Guide by Weight for Patients <40 kg Body Weight = 10 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 30 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 500 mg (2.5 mL) 5% dextrose: 70 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL Body Weight = 15 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 2250 mg (11.25 mL) 5% dextrose: 45 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 750 mg (3.75 mL) 5% dextrose: 105 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 210 mL Body Weight = 20 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 60 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2000 mg (10 mL) 5% dextrose: 280 mL Body Weight = 25 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3750 mg (18.75 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1250 mg (6.25 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2500 mg (12.5 mL) 5% dextrose: 500 mL Body Weight = 30 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 4500 mg (22.5 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 500 mL
Oral: For treatment of acetaminophen overdosage, administer as a 5% solution; dilute the 20% solution (inhalation formulation) 1:3 with a cola, orange juice, or other soft drink; use within 1 hour of preparation
Oral inhalation: May be administered by nebulization either undiluted (both 10% and 20%) or diluted in NS
Rectal: Dilute the inhalation solution in NS to the desired final concentration and administer rectally
USE Inhalation: Adjunctive therapy in patients with abnormal or viscid mucous secretions in bronchopulmonary diseases, pulmonary complications of surgery, and cystic fibrosis; diagnostic bronchial studies
Injection, Oral: Antidote for acute acetaminophen toxicity; prevention of radiocontrast-induced renal dysfunction
Oral, rectal: Treatment of distal intestinal obstruction syndrome (previously known as "meconium ileus or its equivalent")
ADVERSE REACTIONS Cardiovascular: Tachycardia, hypotension, syncope, chest tightness, vasodilation, hypertension (after large oral doses)
Central nervous system: Drowsiness, chills, dysphoria
Dermatologic: Generalized urticaria, rash, pruritus, erythema, angioedema
Gastrointestinal: Stomatitis, nausea, vomiting, dyspepsia, hemoptysis
Hepatic: Mild elevations in liver function tests have occurred after oral therapy
Ocular: Eye pain
Respiratory: Bronchospasm, rhinorrhea, cough
Miscellaneous: Anaphylactoid reactions (I.V. use; 17% in an open label study; 1% reported as severe or moderate in 10% of patients within 15 minutes of the first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after the 60 minute infusion); diaphoresis, unpleasant odor during administration
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component
PRECAUTIONS — Use with caution in patients with asthma or previous history of bronchospasm
WARNINGS — Serious anaphylactoid reactions including death in a patient with asthma have been reported after I.V. use; acute flushing and erythema may occur 30-60 minutes into an I.V. infusion, resolving spontaneously; the infusion may be interrupted until treatment of allergic symptoms is initiated; if acute hypersensitivity reactions occur which do not respond to medical management (eg, antihistamines, H2 blockers) or temporarily halting infusion, discontinue use and pursue alternative management. Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow.
Acetaminophen overdose: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients) or individuals ingesting higher than recommended acetaminophen doses for extended periods of time (repeated supratherapeutic ingestion).
DRUG INTERACTIONS — May potentiate the hemodynamic effects of nitroglycerin; acetylcysteine is adsorbed by activated charcoal
PREGNANCY RISK FACTOR — B (show table)
MONITORING PARAMETERS — When used in acetaminophen overdose, determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion of immediate release formulations or 2 hours after ingestion of liquid formulations (to ensure peak levels have been obtained); coingestion of acetaminophen with other medications which may delay GI peristalsis eg, antihistamines, opioids, may require repeated serum levels to determine the peak serum level; liver function tests
STABILITY — Store at room temperature; I.V. formulation is preservative free and stable 24 hours after dilution at room temperature; opened inhalation solution vials may be stored in the refrigerator; use within 96 hours; contact with rubber, copper, iron, and cork may inactivate the drug; the light purple color of solution does not affect its activity. I.V. acetylcysteine is hyperosmolar (2600 mOsm/L) and is compatible with 5% dextrose, 0.45% sodium chloride, and SWI.
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering the viscosity. The exact mechanism of action in acetaminophen toxicity is unknown. It may act by maintaining or restoring glutathione levels or by acting as an alternative substrate for conjugation with the acetaminophen's toxic metabolite.
PHARMACODYNAMICS Onset of action: Upon inhalation, mucus liquefaction occurs maximally within 5-10 minutes
Duration of mucus liquefaction: More than 1 hour
PHARMACOKINETICS Distribution: Vd: 0.47 L/kg
Protein binding: 83%
Half-life: Reduced acetylcysteine: 2 hours Total acetylcysteine: Newborns: 11 hours Adults: 5.6 hours
Time to peak serum concentration: Oral: 1-2 hours
Elimination: Clearance: Adults: 0.11 L/hour/kg
PATIENT INFORMATION — Clear airway by coughing deeply before aerosol treatment
(For additional information see "Acetylcysteine: Patient drug information")
NURSING IMPLICATIONS — Anaphylactoid reactions following I.V. administration have been reported; have emergency treatments such as antihistamines and H2 blockers readily available for potential adverse effects; assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning; intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime
CANADIAN BRAND NAMES — Acetylcysteine Solution; Mucomyst®; Parvolex®
SYNONYMS — N-Acetyl-L-Cysteine; N-Acetylcysteine; Mercapturic Acid; NAC
THERAPEUTIC CATEGORY Antidote, AcetaminophenMucolytic Agent
DOSING
(For additional information see "Acetylcysteine: Drug information")Acetaminophen poisoning: Children and Adults: Begin treatment within 8 hours of ingestion to optimize therapy in patients whose serum acetaminophen levels fall above the "possible" toxicity line on the Rumack-Matthew nomogram Treatment is also indicated in patients with a history of known or suspected acute acetaminophen ingestion of >150 mg/kg (child) or >7.5 g (adolescent or adult) total dose when plasma levels are not available within 8-10 hours of ingestion or in patients presenting >24 hours after acute ingestion who have a measurable acetaminophen level. See Warnings. I.V.: 150 mg/kg infused over 60 minutes; followed by a 4-hour infusion of 50 mg/kg; followed by a 16-hour infusion of 100 mg/kg; equivalent to a total dose of 300 mg/kg infused over 21 hours Oral: 140 mg/kg; followed by 17 doses of 70 mg/kg every 4 hours; repeat dose if emesis occurs within 1 hour of administration; therapy should continue until all doses are administered even though the acetaminophen plasma level has dropped below the toxic range
Nebulized inhalation: Infants: 1-2 mL of 20% solution or 2-4 mL of 10% solution until nebulized, given 3-4 times/day Children: 3-5 mL of 20% solution or 6-10 mL of 10% solution until nebulized, given 3-4 times/day Adolescents: 5-10 mL of 10% to 20% solution until nebulized, given 3-4 times/day Note: Patients should receive an aerosolized bronchodilator 10-15 minutes prior to acetylcysteine
Intratracheal: Children and Adults: 1-2 mL of 10% to 20% solution every 1-4 hours as needed
Distal intestinal obstruction syndrome (previously known as meconium ileus equivalent): Varying regimens have been reported (polyethylene glycol has become more widely used for this indication): Oral: Children <10 years: 30 mL of 10% solution diluted in 30 mL juice or soda 3 times/day for 24 hours Children 10 years and Adults: 60 mL of 10% solution diluted in 60 mL juice or soda 3 times/day for 24 hours Note: Prior to treatment, administer a phosphosoda enema. A clear liquid diet should be used during the 24-hour acetylcysteine treatment Rectal enema: Children: Varying dosages; 100-300 mL of 4% to 6% solution 2-4 times/day; 50 mL of 20% solution 1-4 times/day and 5-30 mL of 10% to 20% solution 3-4 times/day have been used; rectal enemas appear to have less favorable results than oral administration (Mascarenhas, 2003) Prevention of radiocontrast-induced renal dysfunction (unlabeled use): Adults: Oral: 600 mg twice daily for 2 days (beginning the day before the procedure); hydrate patient concurrently
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution: Acetadote®: 20% [200 mg/mL] (30 mL) [contains disodium edetate]
Solution, inhalation/oral: 10% [100 mg/mL] (4 mL, 10 mL, 30 mL); 20% [200 mg/mL] (4 mL, 10 mL, 30 mL)
GENERIC AVAILABLE — Yes: Solution for inhalation
ADMINISTRATION Parenteral: I.V.: Three infusions (See Usual Dosage) of different lengths: Dilute first dose (150 mg/kg) in 200 mL D5W and infuse over 60 minutes; dilute second dose (50 mg/kg) in 500 mL D5W and infuse over 4 hours; dilute third dose (100 mg/kg) in 1000 mL D5W and infuse over 16 hours; for children <40 kg and patients who are fluid restricted, the manufacturer recommends reducing the diluent to a "proportional" amount. See table for manufacturer's recommended infusion guideline for patients <40 kg. Or as an alternative to proportionally lower the diluent volume, a reasonable approach might be to utilize the concentrations resulting from using the recommended dilution for the dosage in a 50 kg patient. The calculated concentration would range between 5 mg/mL (maintenance infusion) to 37.5 mg/mL (loading dose).
Infusion Guide by Weight for Patients <40 kg Body Weight = 10 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 30 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 500 mg (2.5 mL) 5% dextrose: 70 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL Body Weight = 15 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 2250 mg (11.25 mL) 5% dextrose: 45 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 750 mg (3.75 mL) 5% dextrose: 105 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 210 mL Body Weight = 20 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 60 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1000 mg (5 mL) 5% dextrose: 140 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2000 mg (10 mL) 5% dextrose: 280 mL Body Weight = 25 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 3750 mg (18.75 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1250 mg (6.25 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 2500 mg (12.5 mL) 5% dextrose: 500 mL Body Weight = 30 kg: LOADING Dose 150 mg/kg over 60 minutes: Acetylcysteine dose: 4500 mg (22.5 mL) 5% dextrose: 100 mL SECOND Dose 50 mg/kg over 4 hours: Acetylcysteine dose: 1500 mg (7.5 mL) 5% dextrose: 250 mL THIRD Dose 100 mg/kg over 16 hours: Acetylcysteine dose: 3000 mg (15 mL) 5% dextrose: 500 mL
Oral: For treatment of acetaminophen overdosage, administer as a 5% solution; dilute the 20% solution (inhalation formulation) 1:3 with a cola, orange juice, or other soft drink; use within 1 hour of preparation
Oral inhalation: May be administered by nebulization either undiluted (both 10% and 20%) or diluted in NS
Rectal: Dilute the inhalation solution in NS to the desired final concentration and administer rectally
USE Inhalation: Adjunctive therapy in patients with abnormal or viscid mucous secretions in bronchopulmonary diseases, pulmonary complications of surgery, and cystic fibrosis; diagnostic bronchial studies
Injection, Oral: Antidote for acute acetaminophen toxicity; prevention of radiocontrast-induced renal dysfunction
Oral, rectal: Treatment of distal intestinal obstruction syndrome (previously known as "meconium ileus or its equivalent")
ADVERSE REACTIONS Cardiovascular: Tachycardia, hypotension, syncope, chest tightness, vasodilation, hypertension (after large oral doses)
Central nervous system: Drowsiness, chills, dysphoria
Dermatologic: Generalized urticaria, rash, pruritus, erythema, angioedema
Gastrointestinal: Stomatitis, nausea, vomiting, dyspepsia, hemoptysis
Hepatic: Mild elevations in liver function tests have occurred after oral therapy
Ocular: Eye pain
Respiratory: Bronchospasm, rhinorrhea, cough
Miscellaneous: Anaphylactoid reactions (I.V. use; 17% in an open label study; 1% reported as severe or moderate in 10% of patients within 15 minutes of the first infusion; severe in 1% or mild to moderate in 6% to 7% of patients after the 60 minute infusion); diaphoresis, unpleasant odor during administration
CONTRAINDICATIONS — Hypersensitivity to acetylcysteine or any component
PRECAUTIONS — Use with caution in patients with asthma or previous history of bronchospasm
WARNINGS — Serious anaphylactoid reactions including death in a patient with asthma have been reported after I.V. use; acute flushing and erythema may occur 30-60 minutes into an I.V. infusion, resolving spontaneously; the infusion may be interrupted until treatment of allergic symptoms is initiated; if acute hypersensitivity reactions occur which do not respond to medical management (eg, antihistamines, H2 blockers) or temporarily halting infusion, discontinue use and pursue alternative management. Since increased bronchial secretions may develop after inhalation, percussion, postural drainage, and suctioning should follow.
Acetaminophen overdose: The modified Rumack-Matthew nomogram allows for stratification of patients into risk categories based on the relationship between the serum acetaminophen level and time after ingestion. There are several situations where the nomogram is of limited use. Serum acetaminophen levels obtained prior to 4-hour postingestion are not interpretable; patients presenting late may have undetectable serum concentrations, but have received a lethal dose. The nomogram is less predictive in a chronic ingestion or in an overdose with an extended release product. Acetylcysteine should be administered for any signs of hepatotoxicity even if acetaminophen serum level is low or undetectable. The nomogram also does not take into account patients at higher risk of acetaminophen toxicity (eg, alcoholics, malnourished patients) or individuals ingesting higher than recommended acetaminophen doses for extended periods of time (repeated supratherapeutic ingestion).
DRUG INTERACTIONS — May potentiate the hemodynamic effects of nitroglycerin; acetylcysteine is adsorbed by activated charcoal
PREGNANCY RISK FACTOR — B (show table)
MONITORING PARAMETERS — When used in acetaminophen overdose, determine acetaminophen level as soon as possible, but no sooner than 4 hours after ingestion of immediate release formulations or 2 hours after ingestion of liquid formulations (to ensure peak levels have been obtained); coingestion of acetaminophen with other medications which may delay GI peristalsis eg, antihistamines, opioids, may require repeated serum levels to determine the peak serum level; liver function tests
STABILITY — Store at room temperature; I.V. formulation is preservative free and stable 24 hours after dilution at room temperature; opened inhalation solution vials may be stored in the refrigerator; use within 96 hours; contact with rubber, copper, iron, and cork may inactivate the drug; the light purple color of solution does not affect its activity. I.V. acetylcysteine is hyperosmolar (2600 mOsm/L) and is compatible with 5% dextrose, 0.45% sodium chloride, and SWI.
MECHANISM OF ACTION — Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins thus lowering the viscosity. The exact mechanism of action in acetaminophen toxicity is unknown. It may act by maintaining or restoring glutathione levels or by acting as an alternative substrate for conjugation with the acetaminophen's toxic metabolite.
PHARMACODYNAMICS Onset of action: Upon inhalation, mucus liquefaction occurs maximally within 5-10 minutes
Duration of mucus liquefaction: More than 1 hour
PHARMACOKINETICS Distribution: Vd: 0.47 L/kg
Protein binding: 83%
Half-life: Reduced acetylcysteine: 2 hours Total acetylcysteine: Newborns: 11 hours Adults: 5.6 hours
Time to peak serum concentration: Oral: 1-2 hours
Elimination: Clearance: Adults: 0.11 L/hour/kg
PATIENT INFORMATION — Clear airway by coughing deeply before aerosol treatment
(For additional information see "Acetylcysteine: Patient drug information")
NURSING IMPLICATIONS — Anaphylactoid reactions following I.V. administration have been reported; have emergency treatments such as antihistamines and H2 blockers readily available for potential adverse effects; assess patient for nausea, vomiting, and skin rash following oral administration for treatment of acetaminophen poisoning; intermittent aerosol treatments are commonly given when patient arises, before meals, and just before retiring at bedtime
Acetylcholine
U.S. BRAND NAMES — Miochol®-E
CANADIAN BRAND NAMES — Miochol®-E
THERAPEUTIC CATEGORY Cholinergic Agent, OphthalmicOphthalmic Agent, Miotic
DOSING — Ophthalmic: Adults: Instill 0.5-2 mL of 1% injection (5-20 mg)
(For additional information see "Acetylcholine: Drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for solution, intraocular, as chloride: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
GENERIC AVAILABLE — No
ADMINISTRATION — Ophthalmic: Instill into anterior chamber before or after securing one or more sutures; instillation should be gentle and parallel to the iris face and tangential to the pupil border; in cataract surgery, acetylcholine should be used only after delivery of the lens
USE — Produces complete miosis in cataract surgery, keratoplasty, iridectomy and other anterior segment surgery where rapid miosis is required
ADVERSE REACTIONS Cardiovascular: Transient bradycardia and hypotension
Central nervous system: Headache
Ocular: Iris atrophy, temporary lens opacities (attributed to osmotic effect of 5% mannitol present in preparation)
Respiratory: Dyspnea
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to acetylcholine chloride or any component; acute iritis and acute inflammatory disease of the anterior chamber
PRECAUTIONS — Systemic effects rarely occur, but can cause problems for patients with acute CHF, bronchial asthma, peptic ulcer, hyperthyroidism, GI spasm, and urinary tract obstruction
WARNINGS — Open under aseptic conditions only
DRUG INTERACTIONS — Flurbiprofen decreases effectiveness; sodium nitrate antagonizes acetylcholine's effects
PREGNANCY RISK FACTOR — C (show table)
STABILITY — Prepare solution immediately before use; do not use solution which is not clear and colorless
MECHANISM OF ACTION — Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle, leading to accommodation
PHARMACODYNAMICS Onset of action: Miosis occurs promptly
Duration: ~10-20 minutes
CANADIAN BRAND NAMES — Miochol®-E
THERAPEUTIC CATEGORY Cholinergic Agent, OphthalmicOphthalmic Agent, Miotic
DOSING — Ophthalmic: Adults: Instill 0.5-2 mL of 1% injection (5-20 mg)
(For additional information see "Acetylcholine: Drug information")
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for solution, intraocular, as chloride: Miochol®-E: 1:100 [20 mg; packaged with diluent (2 mL)]
GENERIC AVAILABLE — No
ADMINISTRATION — Ophthalmic: Instill into anterior chamber before or after securing one or more sutures; instillation should be gentle and parallel to the iris face and tangential to the pupil border; in cataract surgery, acetylcholine should be used only after delivery of the lens
USE — Produces complete miosis in cataract surgery, keratoplasty, iridectomy and other anterior segment surgery where rapid miosis is required
ADVERSE REACTIONS Cardiovascular: Transient bradycardia and hypotension
Central nervous system: Headache
Ocular: Iris atrophy, temporary lens opacities (attributed to osmotic effect of 5% mannitol present in preparation)
Respiratory: Dyspnea
Miscellaneous: Diaphoresis
CONTRAINDICATIONS — Hypersensitivity to acetylcholine chloride or any component; acute iritis and acute inflammatory disease of the anterior chamber
PRECAUTIONS — Systemic effects rarely occur, but can cause problems for patients with acute CHF, bronchial asthma, peptic ulcer, hyperthyroidism, GI spasm, and urinary tract obstruction
WARNINGS — Open under aseptic conditions only
DRUG INTERACTIONS — Flurbiprofen decreases effectiveness; sodium nitrate antagonizes acetylcholine's effects
PREGNANCY RISK FACTOR — C (show table)
STABILITY — Prepare solution immediately before use; do not use solution which is not clear and colorless
MECHANISM OF ACTION — Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle, leading to accommodation
PHARMACODYNAMICS Onset of action: Miosis occurs promptly
Duration: ~10-20 minutes
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