Zanmbeel

Monday, August 2, 2010

Amoxicillin and clavulanate potassium

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Augmentin® may be confused with Azulfidine®

U.S. BRAND NAMES — Amoclan; Augmentin ES-600®; Augmentin XR®; Augmentin®

PHARMACOLOGIC CATEGORY
Antibiotic, Penicillin

DOSING: ADULTS — Note: Dose is based on the amoxicillin component; see "Augmentin® Product-Specific Considerations" table.

Susceptible infections: Children >40 kg and Adults: Oral: 250-500 mg every 8 hours or 875 mg every 12 hours

Augmentin® Product-Specific Considerations

125 mg: Chewable tablet: q8h dosing Suspension:

" q8h dosing
" For adults having difficulty swallowing tablets, 125 mg/5 mL suspension may be substituted for 500 mg tablet.

200 mg: Chewable tablet:

" q12h dosing
" Contains phenylalanine Suspension:

" q12h dosing
" For adults having difficulty swallowing tablets, 200 mg/5 mL suspension may be substituted for 875 mg tablet.

250 mg: Chewable tablet:

" q8h dosing
" Contains phenylalanine
" Tablet and chewable tablet are not interchangeable due to differences in clavulanic acid. Suspension:

" q8h dosing
" For adults having difficulty swallowing tablets, 250 mg/5 mL suspension may be substituted for 500 mg tablet. Tablet:

" q8h dosing
" Not for use in patients <40 kg
" Tablet and chewable tablet are not interchangeable due to differences in clavulanic acid.

400 mg: Chewable tablet:

" q12h dosing
" Contains phenylalanine Suspension:

" q12h dosing
" For adults having difficulty swallowing tablets, 400 mg/5 mL suspension may be substituted for 875 mg tablet.

500 mg: Tablet: q8h or q12h dosing

600 mg: Suspension:

" q12h dosing
" Not for use in adults or children ≥ 40 kg
" 600 mg/5 mL suspension is not equivalent to or interchangeable with 200 mg/5 mL or 400 mg/5 mL due to differences in clavulanic acid.

875 mg: Tablet:

" q12h dosing
" Not for use in Clcr <30 mL/minute

1000 mg: Extended release tablet:

" q12h dosing
" Not for use in children <16 years of age
" Not interchangeable with two 500 mg tablets
" Not for use if Clcr <30 mL/minute or hemodialysis

Acute bacterial sinusitis: Oral: Extended release tablet: Two 1000 mg tablets every 12 hours for 10 days

Bite wounds (animal/human): Oral: 875 mg every 12 hours or 500 mg every 8 hours

Chronic obstructive pulmonary disease: Oral: 875 mg every 12 hours or 500 mg every 8 hours

Diabetic foot: Oral: Extended release tablet: Two 1000 mg tablets every 12 hours for 7-14 days

Diverticulitis, perirectal abscess: Oral: Extended release tablet: Two 1000 mg tablets every 12 hours for 7-10 days

Erysipelas: Oral: 875 mg every 12 hours or 500 mg every 8 hours

Febrile neutropenia: Oral: 875 mg every 12 hours

Pneumonia:
Aspiration: Oral: 875 mg every 12 hours
Community-acquired: Oral: Extended release tablet: Two 1000 mg tablets every 12 hours for 7-10 days

Pyelonephritis (acute, uncomplicated): Oral: 875 mg every 12 hours or 500 mg every 8 hours

Skin abscess: Oral: 875 mg every 12 hours

DOSING: PEDIATRIC — Note: Dose is based on the amoxicillin component; see "Augmentin® Product-Specific Considerations" table.

(For additional information see "Amoxicillin and clavulanate potassium: Pediatric drug information")

Susceptible infections: Infants <3 months: Oral: 30 mg/kg/day divided every 12 hours using the 125 mg/5 mL suspension

Lower respiratory tract infections, severe infections, sinusitis: Children ≥ 3 months and <40 kg: Oral: 45 mg/kg/day divided every 12 hours or 40 mg/kg/day divided every 8 hours

Mild-to-moderate infections: Children ≥ 3 months and <40 kg: Oral: 25 mg/kg/day divided every 12 hours or 20 mg/kg/day divided every 8 hours

Otitis media (Augmentin ES-600®): Children ≥ 3 months and <40 kg: Oral: 90 mg/kg/day divided every 12 hours for 10 days in children with severe illness and when coverage for ß-lactamase positive H. influenzae and M. catarrhalis is needed.

Children >40 kg: Refer to adult dosing.

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT
Clcr <30 mL/minute: Do not use 875 mg tablet or extended release tablets.

Clcr 10-30 mL/minute: 250-500 mg every 12 hours

Clcr <10 mL/minute: 250-500 every 24 hours

Hemodialysis: Moderately dialyzable (20% to 50%)
250-500 mg every 24 hours; administer dose during and after dialysis. Do not use extended release tablets.

Peritoneal dialysis: Moderately dialyzable (20% to 50%)
Amoxicillin: Administer 250 mg every 12 hours
Clavulanic acid: Dose for Clcr <10 mL/minute

Continuous arteriovenous or venovenous hemofiltration effects:
Amoxicillin: ~50 mg of amoxicillin/L of filtrate is removed
Clavulanic acid: Dose for Clcr <10 mL/minute

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Powder for oral suspension: 200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine]; 400: Amoxicillin 400 mg and clavulanate potassium 57 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine]; 600: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL (75 mL, 125 mL, 200 mL)
Amoclan:
200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine 7 mg/5 mL and potassium 0.14 mEq/5 mL; fruit flavor]
400: Amoxicillin 400 mg and clavulanate potassium 57 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine 7 mg/5 mL and potassium 0.29 mEq/5 mL; fruit flavor]
600: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL (75 mL, 125 mL) [contains phenylalanine 7 mg/5 mL, potassium 0.248 mEq/5 mL; orange flavor]
Augmentin®:
125: Amoxicillin 125 mg and clavulanate potassium 31.25 mg per 5 mL (75 mL, 100 mL, 150 mL) [contains potassium 0.16 mEq/5 mL; banana flavor]
200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine 7 mg/5 mL and potassium 0.14 mEq/5 mL; orange flavor] [DSC]
250: Amoxicillin 250 mg and clavulanate potassium 62.5 mg per 5 mL (75 mL, 100 mL, 150 mL) [contains potassium 0.32 mEq/5 mL; orange flavor]
400: Amoxicillin 400 mg and clavulanate potassium 57 mg per 5 mL (50 mL, 75 mL, 100 mL) [contains phenylalanine 7 mg/5 mL and potassium 0.29 mEq/5 mL; orange flavor] [DSC]
Augmentin ES-600®: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL (75 mL, 125 mL, 200 mL) [contains phenylalanine 7 mg/5 mL and potassium 0.23 mEq/5 mL; strawberry cream flavor]

Tablet: 250: Amoxicillin 250 mg and clavulanate potassium 125 mg; 500: Amoxicillin 500 mg and clavulanate potassium 125 mg; 875: Amoxicillin 875 mg and clavulanate potassium 125 mg
Augmentin®:
250: Amoxicillin 250 mg and clavulanate potassium 125 mg [contains potassium 0.63 mEq/tablet]
500: Amoxicillin 500 mg and clavulanate potassium 125 mg [contains potassium 0.63 mEq/tablet]
875: Amoxicillin 875 mg and clavulanate potassium 125 mg [contains potassium 0.63 mEq/tablet]

Tablet, chewable: 200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg [contains phenylalanine]; 400: Amoxicillin 400 mg and clavulanate potassium 57 mg [contains phenylalanine]

Tablet, extended release:
Augmentin XR®: 1000: Amoxicillin 1000 mg and clavulanate acid 62.5 mg [contains potassium 12.6 mg (0.32 mEq) and sodium 29.3 mg (1.27 mEq) per tablet; packaged in either a 7-day or 10-day package]

DOSAGE FORMS: CONCISE
Powder for oral suspension: 200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg per 5 mL; 400: Amoxicillin 400 mg and clavulanate potassium 57 mg per 5 mL; 600: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL
Amoclan:
200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg per 5 mL
400: Amoxicillin 400 mg and clavulanate potassium 57 mg per 5 mL
600: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL
Augmentin®:
125: Amoxicillin 125 mg and clavulanate potassium 31.25 mg per 5 mL
250: Amoxicillin 250 mg and clavulanate potassium 62.5 mg per 5 mL
Augmentin ES-600®: Amoxicillin 600 mg and clavulanate potassium 42.9 mg per 5 mL

Tablet: 500: Amoxicillin 500 mg and clavulanate potassium 125 mg; 875: Amoxicillin 875 mg and clavulanate potassium 125 mg
Augmentin®:
250: Amoxicillin 250 mg and clavulanate potassium 125 mg
500: Amoxicillin 500 mg and clavulanate potassium 125 mg
875: Amoxicillin 875 mg and clavulanate potassium 125 mg

Tablet, chewable: 200: Amoxicillin 200 mg and clavulanate potassium 28.5 mg; 400: Amoxicillin 400 mg and clavulanate potassium 57 mg

Tablet, extended release:
Augmentin XR®: 1000: Amoxicillin 1000 mg and clavulanate acid 62.5 mg

GENERIC EQUIVALENT AVAILABLE — Yes: Excludes extended release

ADMINISTRATION — Administer around-the-clock to promote less variation in peak and trough serum levels. Administer with food to decrease stomach upset; shake suspension well before use. Extended release tablets should be administered with food.

Some penicillins (eg, carbenicillin, ticarcillin, and piperacillin) have been shown to inactivate aminoglycosides in vitro. This has been observed to a greater extent with tobramycin and gentamicin, while amikacin has shown greater stability against inactivation. Concurrent use of these agents may pose a risk of reduced antibacterial efficacy in vivo, particularly in the setting of profound renal impairment. However, definitive clinical evidence is lacking. If combination penicillin/aminoglycoside therapy is desired in a patient with renal dysfunction, separation of doses (if feasible), and routine monitoring of aminoglycoside levels, CBC, and clinical response should be considered.

USE — Treatment of otitis media, sinusitis, and infections caused by susceptible organisms involving the lower respiratory tract, skin and skin structure, and urinary tract; spectrum same as amoxicillin with additional coverage of beta-lactamase producing B. catarrhalis, H. influenzae, N. gonorrhoeae, and S. aureus (not MRSA). The expanded coverage of this combination makes it a useful alternative when amoxicillin resistance is present and patients cannot tolerate alternative treatments.

ADVERSE REACTIONS SIGNIFICANT
>10%: Gastrointestinal: Diarrhea (3% to 34%; incidence varies upon dose and regimen used)

1% to 10%:
Dermatologic: Diaper rash, skin rash, urticaria
Gastrointestinal: Abdominal discomfort, loose stools, nausea, vomiting
Genitourinary: Vaginitis, vaginal mycosis
Miscellaneous: Moniliasis

<1% (Limited to important or life-threatening): Alkaline phosphatase increased, cholestatic jaundice, flatulence, headache, hepatic dysfunction, hepatitis, liver function tests increased, prothrombin time increased, thrombocytosis, vasculitis (hypersensitivity)

Additional adverse reactions seen with ampicillin-class antibiotics: Agitation, agranulocytosis, alkaline phosphatase increased, anaphylaxis, anemia, angioedema, anxiety, behavioral changes, bilirubin increased, black "hairy" tongue, confusion, convulsions, crystalluria, dizziness, enterocolitis, eosinophilia, erythema multiforme, exanthematous pustulosis, exfoliative dermatitis, gastritis, glossitis, hematuria, hemolytic anemia, hemorrhagic colitis, indigestion, insomnia, hyperactivity, interstitial nephritis, leukopenia, mucocutaneous candidiasis, pruritus, pseudomembranous colitis, serum sickness-like reaction, Stevens-Johnson syndrome, stomatitis, transaminases increased, thrombocytopenia, thrombocytopenic purpura, tooth discoloration, toxic epidermal necrolysis

CONTRAINDICATIONS — Hypersensitivity to amoxicillin, clavulanic acid, penicillin, or any component of the formulation; history of cholestatic jaundice or hepatic dysfunction with amoxicillin/clavulanate potassium therapy; Augmentin XR™ : severe renal impairment (Clcr <30 mL/minute) and hemodialysis patients

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Use with caution in asthmatic patients. Low incidence of cross-allergy with cephalosporins exists. Diarrhea: Incidence of diarrhea is higher than with amoxicillin alone. Hepatic effects: Although rare, hepatic dysfunction is more common in elderly and/or males, and occurs more frequently with prolonged treatment, and may occur after therapy is complete. Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment. Infectious mononucleosis: A high percentage of patients with infectious mononucleosis have developed rash during therapy; ampicillin-class antibiotics not recommended in these patients. Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.

Dosage form specific issues: Clavulanic acid content: Due to differing content of clavulanic acid, not all formulations are interchangeable. Phenylalanine: Some products contain phenylalanine.

DRUG INTERACTIONS
Allopurinol: May enhance the potential for allergic or hypersensitivity reactions to Amoxicillin. Risk C: Monitor therapy

Fusidic Acid: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Methotrexate: Penicillins may decrease the excretion of Methotrexate. Risk C: Monitor therapy

Mycophenolate: Penicillins may decrease serum concentrations of the active metabolite(s) of Mycophenolate. This effect appears to be the result of impaired enterohepatic recirculation. Risk C: Monitor therapy

Tetracycline Derivatives: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Risk D: Consider therapy modification

Uricosuric Agents: May decrease the excretion of Penicillins. Risk C: Monitor therapy

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Adverse events have not been observed in animal studies; therefore, amoxicillin/clavulanate is classified as pregnancy category B. Both amoxicillin and clavulanic acid cross the placenta. There is no documented increased risk of teratogenic effects caused by amoxicillin/clavulanate. A potential increased risk of necrotizing enterocolitis in the newborn has been noted after maternal use of amoxicillin/clavulanate for preterm labor or premature prolonged rupture of membranes. When used during pregnancy, pharmacokinetic changes have been observed with amoxicillin alone (refer to the Amoxicillin monograph for details).

LACTATION — Enters breast milk/use caution

BREAST-FEEDING CONSIDERATIONS — Amoxicillin is found in breast milk. The manufacturer recommends that caution be used if administered to breast-feeding women. The use of amoxicillin/clavulanate may be safe while breast-feeding; however, the risk of adverse events in the infant may be increased when compared to the use of amoxicillin alone. The risk of adverse events may be related to maternal dose. Nondose-related effects could include modification of bowel flora and allergic sensitization of the infant.

DIETARY CONSIDERATIONS — May be taken with meals or on an empty stomach; take with meals to increase absorption and decrease GI intolerance; may mix with milk, formula, or juice. Extended release tablets should be taken with food. Some products contain phenylalanine. If you have phenylketonuria or PKU, avoid use. All dosage forms contain potassium.

PRICING — (data from drugstore.com)
Chewable (Amoxicillin-Pot Clavulanate)
400-57 mg (20): $63.79

Suspension (reconstituted) (Amoxicillin-Pot Clavulanate)
600-42.9 mg/5 mL (75): $35.99

Tablet, 12-hour (Augmentin XR)
1000-62.5 mg (28): $116.70

Tablets (Amoxicillin-Pot Clavulanate)
250-125 mg (30): $116.54
500-125 mg (20): $45.99
875-125 mg (20): $31.99

Tablets (Augmentin)
250-125 mg (30): $118.99
500-125 mg (30): $166.71
875-125 mg (20): $145.99

MONITORING PARAMETERS — Assess patient at beginning and throughout therapy for infection; with prolonged therapy, monitor renal, hepatic, and hematologic function periodically; monitor for signs of anaphylaxis during first dose

CANADIAN BRAND NAMES — Alti-Amoxi-Clav; Apo-Amoxi-Clav®; Augmentin®; Clavulin®; Novo-Clavamoxin; ratio-Aclavulanate

INTERNATIONAL BRAND NAMES — Acarbixin (MX); Aclam (ID); Ambilan (PE); AMK (TH); Amobay Cl (MX); Amocla (KP); Amocla Duo (KP); Amoclan (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Amoclav (DE); Amoksiclav (TH); Amoksiklav (CL, PL); Amolanic (KP); Amolanic Duo (KP); Amoxa (KP); Amoxi Plus (PY); Amoxiclav (MX); Amoxiclav-BID (MX); Amoxiclav-Teva (IL); Amoxsiklav Forte (TH); Amoxxlin (KP); Amoxyclav (IL); Augamox (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); AugMaxcil (ZA); Augmentan (DE); Augmentin (AE, AT, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CH, CI, CR, CY, CZ, DE, DK, DO, EG, ES, ET, FI, FR, GB, GH, GM, GN, GR, GT, GY, HK, HN, IE, IL, IN, IQ, IR, IT, JM, JO, JP, KE, KP, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NO, OM, PA, PE, PK, PL, PT, QA, RU, SA, SC, SD, SE, SL, SN, SR, SV, SY, TH, TN, TR, TT, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Augmentine (ES); Augmex (PH); Augpen (TH); Augurcin (PH); Bactiv (PH); Bactoclav (PH); Bioclavid (AE, BH, CY, DE, DK, EG, IL, IQ, IR, JO, KW, LB, LY, OM, PH, QA, SA, SE, SY, YE); Bioclavid Forte (PH); Cavumox (MY, TH); Cax (PH); Clacillin Duo Dry Syrup (KP); Clamax (KP); Clamentin (ZA); Clamohexal (AU); Clamohexal Duo (AU); Clamovid (HK, MY, SG); Clamoxin (MX); Clamoxyl (AU); Clamoxyl Duo 400 (AU); Clamoxyl DuoForte (AU); Clavamox (DE, ID, IN); Clavant (MX); Clavar (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Claventin (IL); Clavinex (CN, EC); Clavipen (MX); Clavmex (PH); Clavodar (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Clavoxil (BR); Clavoxine (EC); Clavucyd (MX); Clavulin (BF, BJ, CI, CO, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, MX, NE, NG, SC, SD, SL, SN, TN, TZ, UG, ZA, ZM, ZW); Clavulin Duo Forte (AU); Clavulox Duo (AR, PY); Clavumox (DE, PE, ZA); Clavuser (MX); Cramon Duo (KP); Curam (AU, CO, CR, DO, GT, HK, MY, NI, PA, PE, PL, SG, SV, TH, TW); Danoclav (ID); Darzitil Plus (AR); E-Moxclav (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Enhancin (SG); Exten (PH); Fleming (HK); Forcid (PL); Fugentin (SG); Fullicilina Plus (AR); Gimaclav (MX); Hibiotic (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Klamonex (KP); Klavic (PH); Klavocin (PL); Kmoxilin (KP); Lansiclav (ID); Moxiclav (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SG, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW); Moxicle (KP, TH); Moxlin (MX); Natravox (PH); Novamox (BR); Nufaclav (ID); Penhance (PH); Quali-Mentin (HK); Ramoclav (PL); Ranclav (TH, ZA); Riclasip (MX); Servamox (MX); Sinufin (MX); Spektramox (SE); Sullivan (PH); Suplentin (PH); Synermox (NZ); Taromentin (PL); Velamox CL (PE); Vestaclav (MY); Viaclav (ID); Vulamox (CO, ID)

MECHANISM OF ACTION — Clavulanic acid binds and inhibits beta-lactamases that inactivate amoxicillin resulting in amoxicillin having an expanded spectrum of activity. Amoxicillin inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

PHARMACODYNAMICS / KINETICS — Amoxicillin pharmacokinetics are not affected by clavulanic acid.

Amoxicillin: See Amoxicillin monograph.

Clavulanic acid:
Protein binding: ~25%
Metabolism: Hepatic
Half-life elimination: 1 hour
Time to peak: 1 hour
Excretion: Urine (30% to 40% as unchanged drug)

PATIENT INFORMATION — Take entire course of medication. Take extended release tablets with food. Report diarrhea promptly. Females should report onset of symptoms of candidal vaginitis

Amoxicillin

EDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Amoxicillin may be confused with amoxapine, Amoxil®, Atarax®
Amoxil® may be confused with amoxapine, amoxicillin

International issues:
Fisamox® [Australia] may be confused with Fosamax® which is a brand name for alendronate in the U.S.
Fisamox® [Australia] may be confused with Vigamox® which is a brand name for moxifloxacin in the U.S.

U.S. BRAND NAMES — Amoxil®; Moxatag™

PHARMACOLOGIC CATEGORY
Antibiotic, Penicillin

DOSING: ADULTS
Usual dosage range: Oral: 250-500 mg every 8 hours or 500-875 mg twice daily or extended-release tablet 775 mg once daily

Anthrax exposure (CDC guidelines): Oral: Note: Postexposure prophylaxis in pregnant or nursing women only with documented susceptible organisms: 500 mg every 8 hours

Ear, nose, throat, genitourinary tract, or skin/skin structure infections:
Mild-to-moderate: Oral: 500 mg every 12 hours or 250 mg every 8 hours
Severe: Oral: 875 mg every 12 hours or 500 mg every 8 hours
Tonsillitis and/or pharyngitis: Oral: Extended release tablet: 775 mg once daily

Helicobacter pylorieradication: Oral: 1000 mg twice daily; requires combination therapy with at least one other antibiotic and an acid-suppressing agent (proton pump inhibitor or H2 blocker)

Lower respiratory tract infections: Oral: 875 mg every 12 hours or 500 mg every 8 hours

Lyme disease: Oral: 500 mg every 6-8 hours (depending on size of patient) for 21-30 days

Prophylaxis against infective endocarditis: Oral: 2 g 30-60 minutes before procedure. Note: American Heart Association (AHA) guidelines now recommend prophylaxis only in patients undergoing invasive procedures and in whom underlying cardiac conditions may predispose to a higher risk of adverse outcomes should infection occur. As of April 2007, routine prophylaxis for GI/GU procedures is no longer recommended by the AHA.

Prophylaxis in total joint replacement patients undergoing dental procedures which produce bacteremia: 2 g 1 hour prior to procedure

DOSING: PEDIATRIC

(For additional information see "Amoxicillin: Pediatric drug information")
Usual dosage range:
Children ≤ 3 months: Oral: 20-30 mg/kg/day divided every 12 hours
Children >3 months and <40 kg: Oral: 20-50 mg/kg/day in divided doses every 8-12 hours
Children ≥ 12 years: Oral: Extended-release tablet: 775 mg once daily

Acute otitis media: Children >3 months and <40 kg: Oral: 80-90 mg/kg/day divided every 12 hours

Anthrax exposure (CDC guidelines): Children >3 months and <40 kg: Oral: Note: Postexposure prophylaxis only with documented susceptible organisms: 80 mg/kg/day in divided doses every 8 hours (maximum: 500 mg/dose)

Community-acquired pneumonia:
4 months to <5 years: 80-100 mg/kg/day divided every 8 hours
5-15 years: 100 mg/kg/day divided every 8 hours; Note: Treatment with a macrolide or doxycycline (if age >8 years) is preferred due to higher prevalence of atypical pathogens in this age group

Ear, nose, throat, genitourinary tract, or skin/skin structure infections: Children >3 months and <40 kg: Oral:
Mild-to-moderate: 25 mg/kg/day in divided doses every 12 hours or 20 mg/kg/day in divided doses every 8 hours
Severe: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours
Tonsillitis and/or pharyngitis: Children ≥ 12 years: Extended release tablet: 775 mg once daily

Lower respiratory tract infections: Children >3 months and <40 kg: Oral: 45 mg/kg/day in divided doses every 12 hours or 40 mg/kg/day in divided doses every 8 hours

Lyme disease: Children >3 months and <40 kg: Oral: 25-50 mg/kg/day divided every 8 hours (maximum: 500 mg)

Prophylaxis against infective endocarditis: Children >3 months and <40 kg: Oral: 50 mg/kg 1 hour before procedure. Note: American Heart Association (AHA) guidelines now recommend prophylaxis only in patients undergoing invasive procedures and in whom underlying cardiac conditions may predispose to a higher risk of adverse outcomes should infection occur. As of April 2007, routine prophylaxis for GI/GU procedures is no longer recommended by the AHA.

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT
Use of certain dosage forms (eg, extended-release 775 mg tablet and immediate-release 875 mg tablet) should be avoided in patients with Clcr <30 mL/minute or patients requiring hemodialysis
Clcr 10-30 mL/minute: 250-500 mg every 12 hours
Clcr <10 mL/minute: 250-500 mg every 24 hours

Moderately dialyzable (20% to 50%) by hemodialysis or peritoneal dialysis; approximately 50 mg of amoxicillin per liter of filtrate is removed by continuous arteriovenous or venovenous hemofiltration. Dose as per Clcr <10 mL/minute guidelines.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule: 250 mg, 500 mg
Amoxil®: 500 mg [DSC]

Powder for suspension, oral: 125 mg/5 mL (80 mL, 100 mL, 150 mL); 200 mg/5 mL (50 mL, 75 mL, 100 mL); 250 mg/5 mL (80 mL, 100 mL, 150 mL); 400 mg/5 mL (50 mL, 75 mL, 100 mL)
Amoxil®: 250 mg/5 mL (100 mL, 150 mL) [contains sodium benzoate; bubble gum flavor] [DSC]; 400 mg/5 mL (100 mL) [contains sodium benzoate; bubble gum flavor] [DSC]

Powder for suspension, oral [drops]:
Amoxil®: 50 mg/mL (30 mL) [contains sodium benzoate; bubble gum flavor] [DSC]

Tablet: 500 mg, 875 mg

Tablet, chewable: 125 mg, 200 mg, 250 mg, 400 mg

Tablet, extended release:
Moxatag™ : 775 mg

DOSAGE FORMS: CONCISE
Capsule: 250 mg, 500 mg

Powder for suspension, oral: 125 mg/5 mL, 200 mg/5 mL, 250 mg/5 mL, 400 mg/5 mL

Tablet: 500 mg, 875 mg

Tablet, chewable: 125 mg, 200 mg, 250 mg, 400 mg

Tablet, extended release:
Moxatag™ : 775 mg

GENERIC EQUIVALENT AVAILABLE — Yes: Excludes drops and extended-release formulation

ADMINISTRATION — Administer around-the-clock to promote less variation in peak and trough serum levels. The appropriate amount of suspension may be mixed with formula, milk, fruit juice, water, ginger ale, or cold drinks; administer dose immediately after mixing.

Moxatag™ extended release tablet: Administer within 1 hour of finishing a meal.

Some penicillins (eg, carbenicillin, ticarcillin, and piperacillin) have been shown to inactivate aminoglycosides in vitro. This has been observed to a greater extent with tobramycin and gentamicin, while amikacin has shown greater stability against inactivation. Concurrent use of these agents may pose a risk of reduced antibacterial efficacy in vivo, particularly in the setting of profound renal impairment. However, definitive clinical evidence is lacking. If combination penicillin/aminoglycoside therapy is desired in a patient with renal dysfunction, separation of doses (if feasible), and routine monitoring of aminoglycoside levels, CBC, and clinical response should be considered.

USE — Treatment of otitis media, sinusitis, and infections caused by susceptible organisms involving the upper and lower respiratory tract, skin, and urinary tract; prophylaxis of infective endocarditis in patients undergoing surgical or dental procedures; as part of a multidrug regimen for H. pylori eradication

USE - UNLABELED / INVESTIGATIONAL — Postexposure prophylaxis for anthrax exposure with documented susceptible organisms

ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.

Central nervous system: Agitation, anxiety, behavioral changes, confusion, dizziness, headache, hyperactivity (reversible), insomnia, seizure

Dermatologic: Acute exanthematous pustulosis, erythematous maculopapular rash, erythema multiforme, exfoliative dermatitis, hypersensitivity vasculitis, mucocutaneous candidiasis, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria

Gastrointestinal: Black hairy tongue, diarrhea, hemorrhagic colitis, nausea, pseudomembranous colitis, tooth discoloration (brown, yellow, or gray; rare), vomiting

Hematologic: Agranulocytosis, anemia, eosinophilia, hemolytic anemia, leukopenia,thrombocytopenia, thrombocytopenia purpura

Hepatic: Acute cytolytic hepatitis, ALT increased, AST increased, cholestatic jaundice, hepatic cholestasis

Renal: Crystalluria

Miscellaneous: Anaphylaxis, serum sickness-like reaction

CONTRAINDICATIONS — Hypersensitivity to amoxicillin, penicillin, other beta-lactams, or any component of the formulation

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Anaphylactoid/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Use with caution in asthmatic patients. Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns: Infectious mononucleosis: A high percentage of patients with infectious mononucleosis have developed rash during therapy; ampicillin-class antibiotics not recommended in these patients. Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended. In addition, use of certain dosage forms (eg, extended-release 775 mg tablet and immediate-release 875 mg tablet) should be avoided in patients with Clcr <30 mL/minute or patients requiring hemodialysis.

Dosage form specific issues: Phenylalanine: Chewable tablets contain phenylalanine.

DRUG INTERACTIONS
Allopurinol: May enhance the potential for allergic or hypersensitivity reactions to Amoxicillin. Risk C: Monitor therapy

Fusidic Acid: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Methotrexate: Penicillins may decrease the excretion of Methotrexate. Risk C: Monitor therapy

Mycophenolate: Penicillins may decrease serum concentrations of the active metabolite(s) of Mycophenolate. This effect appears to be the result of impaired enterohepatic recirculation. Risk C: Monitor therapy

Tetracycline Derivatives: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Risk D: Consider therapy modification

Uricosuric Agents: May decrease the excretion of Penicillins. Risk C: Monitor therapy

PREGNANCY RISK FACTOR — B (show table)

PREGNANCY IMPLICATIONS — Adverse events have not been observed in animal studies; therefore, amoxicillin is classified as pregnancy category B. There is no documented increased risk of adverse pregnancy outcome or teratogenic effects caused by amoxicillin. It is the drug of choice for the treatment of chlamydial infections in pregnancy and for anthrax prophylaxis when penicillin susceptibility is documented.

Due to pregnancy-induced physiologic changes, amoxicillin clearance is increased during pregnancy resulting in lower concentrations and smaller AUCs. Oral ampicillin-class antibiotics are poorly-absorbed during labor.

LACTATION — Enters breast milk/compatible

BREAST-FEEDING CONSIDERATIONS — Very small amounts of amoxicillin are excreted in breast milk. The manufacturer recommends that caution be exercised when administering amoxicillin to nursing women. The AAP considers amoxicillin to be "usually compatible with breastfeeding." Nondose-related effects could include modification of bowel flora and allergic sensitization of the infant.

DIETARY CONSIDERATIONS — May be taken with food. Amoxil® chewable contains phenylalanine 1.82 mg per 200 mg tablet, phenylalanine 3.64 mg per 400 mg tablet.

Moxatag™ : Take within 1 hour of finishing a meal.

PRICING — (data from drugstore.com)
Capsules (Amoxicillin)
250 mg (90): $17.99
500 mg (30): $13.99

Capsules (Amoxil)
500 mg (30): $15.99

Chewable (Amoxicillin)
125 mg (21): $11.99
250 mg (30): $13.99

Chewable (Amoxil)
400 mg (20): $13.99

Suspension (reconstituted) (Amoxicillin)
250 mg/5 mL (150): $14.00
400 mg/5 mL (100): $16.99

Suspension (reconstituted) (Amoxil)
50 mg/mL (30): $8.99
200 mg/5 mL (100): $11.99
250 mg/5 mL (100): $8.99
250 mg/5 mL (150): $8.99
400 mg/5 mL (50): $8.99
400 mg/5 mL (75): $9.99
400 mg/5 mL (100): $11.99

Suspension (reconstituted) (Trimox)
125 mg/5 mL (100): $11.99
250 mg/5 mL (80): $11.99

Tablet, 24-hour (Moxatag)
775 mg (30): $249.98

Tablets (Amoxicillin)
500 mg (100): $49.99
875 mg (30): $26.99

Tablets (Amoxil)
500 mg (21): $12.99
875 mg (21): $27.99

MONITORING PARAMETERS — With prolonged therapy, monitor renal, hepatic, and hematologic function periodically; assess patient at beginning and throughout therapy for infection; monitor for signs of anaphylaxis during first dose

CANADIAN BRAND NAMES — Apo-Amoxi®; Gen-Amoxicillin; Lin-Amox; Mylan-Amoxicillin; Novamoxin®; Nu-Amoxi; PHL-Amoxicillin; PMS-Amoxicillin

INTERNATIONAL BRAND NAMES — Acilina (PY); Acimox (MX); Adbiotin (CO); Alfamox (IT); Almodan (GB); Almorsan (AR); Alphamox (AU); Amagesen Solutab (DE); Amicil (MX); Amimox (SE); Amobay (MX); Amoclave (ES); Amoclen (CZ); Amodex (FR); Amoflux (BR); Amohexal (AU); Amolin (JP, TW); Amosine (ID); Amotaks (PL); Amox (AE, BH, CY, EG, IL, IQ, IR, IT, JO, KW, LB, LY, OM, QA, SA, SY, YE); Amoxa (HK); Amoxal (VE); Amoxapen (BB, BM, BS, BZ, GY, JM, NL, SG, SR, TT); Amoxcil (CL); Amoxcillin (TH); Amoxcin (TW); Amoxi (IL); Amoxi TO (TH); Amoxi-basan (DE); Amoxicap (PK); Amoxicilina (CO, EC); Amoxicilline (PL); Amoxiclin (PE); Amoxico (PH); Amoxidal (AR, UY); Amoxidin (AE, BB, BF, BH, BJ, BM, BS, BZ, CI, CY, EG, ET, GH, GM, GN, GY, IL, IQ, IR, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, NL, OM, QA, SA, SC, SD, SL, SN, SR, SY, TN, TT, TZ, UG, YE, ZA, ZM, ZW); Amoxifur (MX); Amoxihexal (DE); Amoxil (AE, AU, BB, BF, BH, BJ, BM, BR, BS, BZ, CI, CY, EG, ET, GB, GH, GM, GN, GR, GY, ID, IE, IL, IQ, IR, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, NE, NG, NL, NZ, OM, PE, PL, QA, SA, SC, SD, SL, SN, SR, SY, TN, TT, TZ, UG, YE, ZA, ZM, ZW); Amoxil Duo (AU); Amoxillin (IL, IT); Amoxin (FI); Amoxinova (MX); Amoxipen (IT); Amoxipenil (CN); Amoxisol (MX); Amoxivan (IN); Amoxivet (MX); Amoxsan (ID); Amoxsan Forte (ID); Amoxy-diolan (DE); Amoxycillin (PL); Amoxypen (DE, PE); Apo-Amoxi (MY, PL); Aroxin (SG); Azillin (CH); Bacihexal (PH); Bactamox (VE); Bactox (EE); Bactox Ge (FR); Baymox (HN); Beamoxy (MY); Bimxan (MX); Biotamoxal (AR); Bristamox (EC, FR); Bufamoxy (ID); Cilamox (AU, PH); Clamoxyl (AT, AU, BB, BE, BM, BS, BZ, CH, FR, GY, JM, JP, NL, PE, PT, SR, TT); Dimopen (MX); Duomox (BG, HN, PL); Dymoxin (TH); Efpinex (JP); Ethimox (ID); Farconcil (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Fisamox (AU); Flemoxin (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Flubiotic (ES); Foxolin (KP); Fullcilina (AR); Gexcil (PH); Gimalxina (MX); Gomcillin (KP); Grinsul (AR); Grunamox (EC, PL); Hiconcil (BE, FR, ID, NL, PL); Hidramox (MX); Hipen (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TN, TZ, UG, ZA, ZM, ZW); Ibiamox (AE, AU, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, TH, YE); Ikamoxil (ID); Imacillin (DK, NO, SE); Imadrax (DK); Imaxilin (CO); Isimoxin (IT); Izoltil (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW); Jutamox (DE); Lamoxy (IN); Magnimox (PE); Manmox (TH); Maxamox (AU, NZ); Maxcil (ZA); Meixil (TH); Milamox-BIG (TH); Mopen (IT); Mox (IN); Moxacin (AU, NZ); Moxarin (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Moxilen (BF, BJ, CI, ET, GH, GM, GN, HK, KE, LR, MA, ML, MR, MU, MW, MY, NE, NG, SC, SD, SG, SL, SN, TN, TW, TZ, UG, ZA, ZM, ZW); Moxitab (TH); Moxtid (ID); Moxylin (EC); Moxypen (IL, ZA); Moxyvit (IL); Novabritine (BE); Novamox (PH, PL); Novax (ID); Novoxil (BR); Ospamox (AE, AT, BG, BH, CY, DE, EG, HK, ID, IL, IQ, IR, JO, KW, LB, LY, NZ, OM, PE, PL, PT, QA, SA, SY, UY, YE); Pamocil (IT); Pamoxicillin (TW); Pamoxin (KP); Pasetocin (JP); Penamox (MX, NZ, PE); Penbiosyn (PH); Piramox (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW); Polymox (MX); Pondnoxcill (TH); Rancil (TH); Ranmoxy (AU, ZA); Ranoxyl (MY, TH); Robamox (ID); Sawacillin (JP); Sawamezin (JP); Servamox (TW); Setmoxil (HK); Shamoxil (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Sia-mox (TH); Simoxil (IT); Solciclina (MX); Solpenox (ID); Sterimox (PH); Supercillin (TW); Teramoxyl (PH); Trifamox (AR, PY); Trimox (TH); Vastamox (PH); Velamox (PE); Widecillin (ID); Winpen (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TN, TZ, UG, ZA, ZM, ZW); Xalyn-Or (MX); Xazexy (PH); Yusimox (ID); Zamoxil (MY); Zerrsox (PH); Zimox (IT)

MECHANISM OF ACTION — Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

PHARMACODYNAMICS / KINETICS
Absorption: Oral: Rapid and nearly complete; food does not interfere
Extended-release tablet: Rate of absorption is slower compared to immediate-release formulations; food decreases the rate but not extent of absorption

Distribution: Widely to most body fluids and bone; poor penetration into cells, eyes, and across normal meninges
Pleural fluids, lungs, and peritoneal fluid; high urine concentrations are attained; also into synovial fluid, liver, prostate, muscle, and gallbladder; penetrates into middle ear effusions, maxillary sinus secretions, tonsils, sputum, and bronchial secretions
CSF:blood level ratio: Normal meninges: <1%; Inflamed meninges: 8% to 90%

Protein binding: 17% to 20%

Metabolism: Partially hepatic

Half-life elimination:
Neonates, full-term: 3.7 hours
Infants and Children: 1-2 hours
Adults: Normal renal function: 0.7-1.4 hours
Clcr <10 mL/minute: 7-21 hours

Time to peak: Capsule: 2 hours; Extended-release tablet: 3.1 hours; Suspension: 1 hour

Excretion: Urine (60% as unchanged drug); lower in neonatesNote: Extended-release tablets: In healthy volunteers, serum drug concentrations were below 0.25 mcg/mL and undetectable at 16 hours following dosing.

PATIENT INFORMATION — Take entire course of medication. Report diarrhea promptly. females should report symptoms of vaginitis. Pediatric drops may be placed on child's tongue or added to formula, milk, etc.

(For additional information see "Amoxicillin: Patient drug information")

PRODUCT AVAILABILITY
Moxatag™ : FDA approved January 2009; availability anticipated in March 2009

Moxatag™ is an extended-release tablet of amoxicillin intended for once-daily administration

Amoxapine

MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Amoxapine may be confused with amoxicillin, Amoxil®
Asendin may be confused with aspirin

MEDICATION GUIDE — An FDA-approved patient medication guide, which is available with the product information and at http://www.fda.gov/downloads/Drugs/DrugSafety/ucm088622.pdf, must be dispensed with this medication for each new outpatient prescription and refill.

PHARMACOLOGIC CATEGORY
Antidepressant, Tricyclic (Secondary Amine)

DOSING: ADULTS — Once symptoms are controlled, decrease gradually to lowest effective dose. Maintenance dose is usually given at bedtime to reduce daytime sedation.

Depression: Oral: Initial: 25 mg 2-3 times/day. If tolerated, dosage may be increased to 100 mg 2-3 times/day. May be given in a single bedtime dose when dosage <300 mg/day.
Maximum daily dose: 600 mg (inpatients); 400 mg (outpatients)

DOSING: PEDIATRIC
Depression: Oral:
Children: Not established in children <16 years of age.
Adolescents: Initial: 25-50 mg/day; increase gradually to 100 mg/day. May administer as divided doses or as a single dose at bedtime.

Note: Once symptoms are controlled, decrease gradually to lowest effective dose. Maintenance dose is usually given at bedtime to reduce daytime sedation.

DOSING: ELDERLY — Oral: Initial: 25 mg at bedtime increased by 25 mg weekly for outpatients and every 3 days for inpatients if tolerated; usual dose: 50-150 mg/day, but doses up to 300 mg may be necessary. Note: Once symptoms are controlled, decrease gradually to lowest effective dose. See Geriatric Considerations.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet: 25 mg, 50 mg, 100 mg, 150 mg

DOSAGE FORMS: CONCISE
Tablet: 25 mg, 50 mg, 100 mg, 150 mg

GENERIC EQUIVALENT AVAILABLE — Yes

ADMINISTRATION — May be administered with food to decrease GI distress.

USE — Treatment of depression, psychotic depression, depression accompanied by anxiety or agitation

ADVERSE REACTIONS SIGNIFICANT
>10%:
Central nervous system: Drowsiness
Gastrointestinal: Xerostomia, constipation

1% to 10%:
Central nervous system: Anxiety, ataxia, confusion, dizziness, excitement, headache, insomnia, nervousness, restlessness
Dermatologic: Edema, skin rash
Endocrine: Prolactin levels increased
Gastrointestinal: Nausea
Neuromuscular & skeletal: Tremor, weakness
Ocular: Blurred vision
Miscellaneous: Diaphoresis

<1% (Limited to important or life-threatening): Agranulocytosis, allergic reactions, diarrhea, extrapyramidal symptoms, galactorrhea, hypertension, impotence, incoordination, intraocular pressure increased, leukopenia, menstrual irregularity, mydriasis, neuroleptic malignant syndrome, numbness, painful ejaculation, paresthesia, photosensitivity, seizure, SIADH, syncope, tardive dyskinesia, testicular edema, tinnitus, urinary retention, vomiting

CONTRAINDICATIONS — Hypersensitivity to amoxapine or any component of the formulation; use of MAO inhibitors within past 14 days; acute recovery phase following myocardial infarction

WARNINGS / PRECAUTIONS
Boxed warnings: Suicidal thinking/behavior: See "Major psychiatric warnings" below.

Major psychiatric warnings:
• [U.S. Boxed Warning]: Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (18-24 years of age) with major depressive disorder (MDD) and other psychiatric disorders; consider risk prior to prescribing. Short-term studies did not show an increased risk in patients >24 years of age and showed a decreased risk in patients ≥ 65 years. Closely monitor patients for clinical worsening, suicidality, or unusual changes in behavior, particularly during the initial 1-2 months of therapy or during periods of dosage adjustments (increases or decreases); the patient's family or caregiver should be instructed to closely observe the patient and communicate condition with healthcare provider. A medication guide concerning the use of antidepressants should be dispensed with each prescription. Amoxapine is not FDA approved for use in patients <16 years of age. The possibility of a suicide attempt is inherent in major depression and may persist until remission occurs. Patients treated with antidepressants should be observed for clinical worsening and suicidality, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases. Worsening depression and severe abrupt suicidality that are not part of the presenting symptoms may require discontinuation or modification of drug therapy. Use caution in high-risk patients during initiation of therapy. Prescriptions should be written for the smallest quantity consistent with good patient care. The patient's family or caregiver should be alerted to monitor patients for the emergence of suicidality and associated behaviors such as anxiety, agitation, panic attacks, insomnia, irritability, hostility, impulsivity, akathisia, hypomania, and mania; patients should be instructed to notify their healthcare provider if any of these symptoms or worsening depression or psychosis occur. May worsen psychosis in some patients or precipitate a shift to mania or hypomania in patients with bipolar disorder. Monotherapy in patients with bipolar disorder should be avoided. Patients presenting with depressive symptoms should be screened for bipolar disorder. Amoxapine is not FDA approved for the treatment of bipolar depression.

Concerns related to adverse effects: Anticholinergic effects: May cause anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention); use with caution in patients with decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems. The degree of anticholinergic blockade produced by this agent is moderate relative to other antidepressants. Extrapyramidal symptoms: May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is low). Neuroleptic malignant syndrome (NMS): Use may be associated with NMS; monitor for mental status changes, fever, muscle rigidity, and/or autonomic instability (risk may be increased in patients with Parkinson's disease or Lewy body dementia). Orthostatic hypotension: May cause orthostatic hypotension (risk is moderate relative to other antidepressants); use with caution in patients at risk of this effect or in those who would not tolerate transient hypotensive episodes (cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). Sedation: May cause sedation, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). The degree of sedation is moderate relative to other antidepressants.

Disease-related concerns: Cardiovascular disease: Use with caution in patients with a history of cardiovascular disease (including previous MI, stroke, tachycardia, or conduction abnormalities); the risk conduction abnormalities with this agent is moderate relative to other antidepressants. Hepatic impairment: Use with caution in patients with hepatic impairment. Renal impairment: Use with caution in patients with renal impairment. Seizure disorder: Use with caution in patients at risk of seizures, including those with a history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Thyroid dysfunction: Use with caution in patients with hyperthyroidism or those receiving thyroid supplementation.

Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations: Elderly: Use with caution in the elderly.

Other warnings/precautions: Discontinuation of therapy: Therapy should not be abruptly discontinued in patients receiving high doses for prolonged periods. Electroconvulsive therapy: May increase the risks associated with electroconvulsive therapy; consider discontinuing, when possible, prior to ECT treatment.

METABOLISM / TRANSPORT EFFECTS — Substrate of CYP2D6 (major)

DRUG INTERACTIONS
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alfuzosin: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy

Alpha-/Beta-Agonists (Direct-Acting): Tricyclic Antidepressants may enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Exceptions: Dipivefrin. Risk D: Consider therapy modification

Alpha1-Agonists: Tricyclic Antidepressants may enhance the vasopressor effect of Alpha1-Agonists. Risk D: Consider therapy modification

Alpha2-Agonists: Tricyclic Antidepressants may diminish the antihypertensive effect of Alpha2-Agonists. Exceptions: Apraclonidine; Brimonidine. Risk D: Consider therapy modification

Altretamine: May enhance the orthostatic effect of Tricyclic Antidepressants. Risk C: Monitor therapy

Amphetamines: Tricyclic Antidepressants may enhance the stimulatory effect of Amphetamines. Tricyclic Antidepressants may also potentiate the cardiovascular effects of Amphetamines. Risk C: Monitor therapy

Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy

Artemether: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination

Barbiturates: May increase the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification

Beta2-Agonists: Tricyclic Antidepressants may enhance the adverse/toxic effect of Beta2-Agonists. Risk C: Monitor therapy

CarBAMazepine: May increase the metabolism of Tricyclic Antidepressants. Risk C: Monitor therapy

Chloroquine: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy

Cimetidine: May decrease the metabolism of Tricyclic Antidepressants. Risk C: Monitor therapy

Cinacalcet: May increase the serum concentration of Tricyclic Antidepressants. Risk C: Monitor therapy

Ciprofloxacin: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk C: Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

CYP2D6 Inhibitors (Moderate): May decrease the metabolism of CYP2D6 Substrates. Risk C: Monitor therapy

CYP2D6 Inhibitors (Strong): May decrease the metabolism of CYP2D6 Substrates. Risk D: Consider therapy modification

Desmopressin: Tricyclic Antidepressants may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy

Dexmethylphenidate: May decrease the metabolism of Tricyclic Antidepressants. Risk C: Monitor therapy

Dronedarone: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Dronedarone. Risk X: Avoid combination

DULoxetine: May decrease the metabolism of Tricyclic Antidepressants. Risk C: Monitor therapy

Gadobutrol: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk D: Consider therapy modification

Iobenguane I 123: Tricyclic Antidepressants may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination

Lithium: May enhance the neurotoxic effect of Tricyclic Antidepressants. Risk C: Monitor therapy

Lumefantrine: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination

MAO Inhibitors: May enhance the serotonergic effect of Tricyclic Antidepressants. This may cause serotonin syndrome. Risk X: Avoid combination

MAO Inhibitors: May enhance the orthostatic effect of Orthostasis Producing Agents. Risk C: Monitor therapy

Methylphenidate: May decrease the metabolism of Tricyclic Antidepressants. Risk C: Monitor therapy

Nilotinib: May enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination

Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy

Pimozide: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Pimozide. Risk X: Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification

Propoxyphene: May enhance the CNS depressant effect of Tricyclic Antidepressants. Risk C: Monitor therapy

Protease Inhibitors: May increase the serum concentration of Tricyclic Antidepressants. Risk C: Monitor therapy

QTc-Prolonging Agents: May enhance the adverse/toxic effect of other QTc-Prolonging Agents. Their effects can be additive, causing life-threatening ventricular arrhythmias. Risk D: Consider therapy modification

QuiNIDine: Tricyclic Antidepressants may enhance the QTc-prolonging effect of QuiNIDine. QuiNIDine may decrease the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification

QuiNINE: QTc-Prolonging Agents may enhance the QTc-prolonging effect of QuiNINE. QuiNINE may enhance the QTc-prolonging effect of QTc-Prolonging Agents. Risk X: Avoid combination

Selective Serotonin Reuptake Inhibitors: May decrease the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification

Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination

St Johns Wort: May increase the metabolism of Tricyclic Antidepressants. The risk of serotonin syndrome may theoretically be increased. Risk D: Consider therapy modification

Sulfonylureas: Cyclic Antidepressants may enhance the hypoglycemic effect of Sulfonylureas. Risk C: Monitor therapy

Terbinafine: May decrease the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification

Tetrabenazine: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Tetrabenazine. Risk X: Avoid combination

Thioridazine: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Thioridazine. Risk X: Avoid combination

TraMADol: Tricyclic Antidepressants may enhance the neuroexcitatory and/or seizure-potentiating effect of TraMADol. Risk C: Monitor therapy

Valproic Acid: May increase the serum concentration of Tricyclic Antidepressants. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Tricyclic Antidepressants may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy

Yohimbine: Tricyclic Antidepressants may increase the serum concentration of Yohimbine. Risk C: Monitor therapy

Ziprasidone: QTc-Prolonging Agents may enhance the QTc-prolonging effect of Ziprasidone. The risk of a severe arrhythmia may be increased. Risk X: Avoid combination

ETHANOL / NUTRITION / HERB INTERACTIONS
Ethanol: Avoid ethanol (may increase CNS depression).

Food: Grapefruit juice may inhibit the metabolism of some TCAs and clinical toxicity may result.

Herb/Nutraceutical: Avoid valerian, St John's wort, SAMe, kava kava.

PREGNANCY RISK FACTOR — C (show table)

LACTATION — Enters breast milk/contraindicated (AAP rates "of concern")

PRICING — (data from drugstore.com)
Tablets (Amoxapine)
25 mg (60): $25.99
50 mg (60): $28.99
100 mg (30): $35.99
150 mg (30): $38.99

MONITORING PARAMETERS — Monitor blood pressure and pulse rate prior to and during initial therapy evaluate mental status, suicidal ideation (especially at the beginning of therapy or when doses are increased or decreased); monitor weight; ECG in older adults

REFERENCE RANGE — Therapeutic: Amoxapine: 20-100 ng/mL (SI: 64-319 nmol/L); 8-OH amoxapine: 150-400 ng/mL (SI: 478-1275 nmol/L); both: 200-500 ng/mL (SI: 637-1594 nmol/L)

INTERNATIONAL BRAND NAMES — Asendin (ID); Defanyl (FR); Demolox (DK, IN)

MECHANISM OF ACTION — Reduces the reuptake of serotonin and norepinephrine. The metabolite, 7-OH-amoxapine has significant dopamine receptor blocking activity similar to haloperidol.

PHARMACODYNAMICS / KINETICS
Onset of antidepressant effect: Usually occurs after 1-2 weeks, but may require 4-6 weeks

Absorption: Rapid and well absorbed

Distribution: Vd: 0.9-1.2 L/kg; enters breast milk

Protein binding: 80%

Metabolism: Primarily hepatic

Half-life elimination: Parent drug: 11-16 hours; Active metabolite (8-hydroxy): Adults: 30 hours

Time to peak, serum: 1-2 hours

Excretion: Urine (as unchanged drug and metabolites)

PATIENT INFORMATION — Dry mouth may be helped by sips of water, sugarless gum, or hard candy; avoid alcohol; very important to maintain established dosage regimen; photosensitivity to sunlight can occur, do not discontinue abruptly; full effect may not occur for 3-4 weeks; full dosage may be taken at bedtime to avoid daytime sedation

Amoxicillin

Amoxapine

Amobarbital

U.S. BRAND NAMES — Amytal®

PHARMACOLOGIC CATEGORY
Barbiturate

DOSING: ADULTS
Hypnotic: I.M., I.V.: 65-200 mg at bedtime (maximum single dose: 1000 mg)

Sedative: I.M., I.V.: 30-50 mg 2-3 times/day (maximum single dose: 1000 mg)

"Amytal® interview" (unlabeled use): I.V.: 50-100 mg/minute for total dose of 200-1000 mg or until patient experiences drowsiness, impaired attention, slurred speech, or nystagmus

Wada test (unlabeled use): Intra-arterial: 100 mg over 4-5 seconds via percutaneous transfemoral catheter

DOSING: PEDIATRIC

(For additional information see "Amobarbital: Pediatric drug information")
Sedative: I.M., I.V.: 6-12 years: Manufacturer's dosing range: 65-500 mg

Hypnotic (unlabeled use): I.M.: 2-3 mg/kg (maximum: 500 mg)

DOSING: ELDERLY — Refer to adult dosing.

DOSING: RENAL IMPAIRMENT — Dosing should be reduced; specific recommendations not available.

DOSING: HEPATIC IMPAIRMENT — Dosing should be reduced; specific recommendations not available.

DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Injection, powder for reconstitution, as sodium:
Amytal®: 500 mg

DOSAGE FORMS: CONCISE
Injection, powder for reconstitution:
Amytal®: 500 mg

GENERIC EQUIVALENT AVAILABLE — No

ADMINISTRATION
I.M.: Administer deeply into a large muscle. Do not use more than 5 mL at any single site (may cause tissue damage). I.M. dosages should not exceed 500 mg. Use 20% solution to facilitate larger doses.

I.V.: Use only when I.M. administration is not feasible. Administer by slow I.V. injection (maximum: 50 mg/minute in adults).

COMPATIBILITY — Stable in D5LR, D5NS, D5W, D10W, D20W, LR, NS.

Compatibility when admixed: Compatible: Amikacin, aminophylline, sodium bicarbonate. Incompatible: Cefazolin, cimetidine, clindamycin, diphenhydramine, droperidol, hydroxyzine, insulin (regular), levorphanol, meperidine, morphine, norepinephrine, pancuronium, pentazocine, penicillin G potassium, procaine, streptomycin, vancomycin. Variable (consult detailed reference): Atracurium, dimenhydrinate, hydrocortisone sodium succinate, isoproterenol, metaraminol, methyldopate, norepinephrine, succinylcholine.

USE — Hypnotic in short-term treatment of insomnia; reduce anxiety and provide sedation preoperatively

USE - UNLABELED / INVESTIGATIONAL — Therapeutic or diagnostic "Amytal® Interviewing"; Wada test

ADVERSE REACTIONS SIGNIFICANT — Frequency not defined and is reported as barbiturate use (not specifically amobarbital).

Cardiovascular: Bradycardia, hypotension, syncope

Central nervous system: Agitation, anxiety, ataxia, confusion, CNS depression, dizziness, fever, hallucinations, headache, insomnia, nightmares, nervousness, psychiatric disturbances, somnolence, thinking abnormal

Gastrointestinal: Constipation, nausea, vomiting

Hematologic: Megaloblastic anemia (following chronic phenobarbital use)

Hepatic: Liver damage

Local: Injection site reaction

Neuromuscular & skeletal: Hyperkinesia

Respiratory: Apnea, atelectasis (postoperative), hypoventilation

Miscellaneous: Hypersensitivity reaction (including angioedema, rash, and exfoliative dermatitis)

CONTRAINDICATIONS — Hypersensitivity to barbiturates or any component of the formulation; marked hepatic impairment; dyspnea or airway obstruction; porphyria

WARNINGS / PRECAUTIONS
Concerns related to adverse effects: CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Hypersensitivity reactions: Postmarketing studies have indicated that the use of hypnotic/sedative agents for sleep has been associated with hypersensitivity reactions including anaphylaxis as well as angioedema. Paradoxical responses: May cause paradoxical responses, including agitation and hyperactivity, particularly in acute pain, chronic pain and pediatric patients. Sleep-related activities: An increased risk for hazardous sleep-related activities such as sleep-driving; cooking and eating food, and making phone calls while asleep has been noted with sedative-hypnotic medications. Discontinue treatment in patients who report a sleep-driving episode.

Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease; may cause hypotension. Depression: Use with caution in patients with depression or suicidal tendencies. Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use. Hepatic impairment: Use with caution in patients with hepatic impairment, decreased dosage may be needed; contraindicated in severe impairment. Insomnia: Appropriate use: When used as a hypnotic for the treatment of insomnia, effectiveness is limited to ≤ 2 weeks. Renal impairment: Use with caution in patients with renal impairment; decreased dosage may be needed.

Concurrent drug therapy issues: Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations: Elderly: Use with caution in the elderly; not recommended for use. Closely monitor elderly or debilitated patients for impaired cognitive or motor performance. Pediatrics: Safety and efficacy have not been established in children <6 years of age; use with caution in children ≥ 6 years of age.

Dosage form specific issues: Alkaline solution: Solution for injection is highly alkaline and extravasation may cause local tissue damage.

Other warnings/precautions: Rapid administration: Rapid I.V. administration may cause respiratory depression, apnea, and hypotension. Withdrawal: Gradual withdrawal is recommended if used over extended periods of time.

RESTRICTIONS — C-II

METABOLISM / TRANSPORT EFFECTS — Induces CYP2A6 (strong)

DRUG INTERACTIONS
Acetaminophen: Barbiturates may increase the metabolism of Acetaminophen. This may 1) diminish the effect of acetaminophen; and 2) increase the risk of liver damage. Risk C: Monitor therapy

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Beta-Blockers: Barbiturates may decrease the serum concentration of Beta-Blockers. Exceptions: Atenolol; Levobunolol; Metipranolol; Nadolol. Risk C: Monitor therapy

Calcium Channel Blockers: Barbiturates may increase the metabolism of Calcium Channel Blockers. Exceptions: Clevidipine. Risk D: Consider therapy modification

Chloramphenicol: May decrease the metabolism of Barbiturates. Barbiturates may increase the metabolism of Chloramphenicol. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Contraceptive (Progestins): Barbiturates may diminish the therapeutic effect of Contraceptive (Progestins). Contraceptive failure is possible. Risk D: Consider therapy modification

Corticosteroids (Systemic): Barbiturates may increase the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy

CycloSPORINE: Barbiturates may increase the metabolism of CycloSPORINE. Risk D: Consider therapy modification

CYP2A6 Substrates: CYP2A6 Inducers (Strong) may increase the metabolism of CYP2A6 Substrates. Risk C: Monitor therapy

Disopyramide: Barbiturates may increase the metabolism of Disopyramide. Risk D: Consider therapy modification

Doxycycline: Barbiturates may decrease the serum concentration of Doxycycline. Risk D: Consider therapy modification

Etoposide: Barbiturates may increase the metabolism of Etoposide. Risk C: Monitor therapy

Etoposide Phosphate: Barbiturates may decrease the serum concentration of Etoposide Phosphate. Barbiturates may increase the metabolism, via CYP isoenzymes, of etoposide phosphate. Risk C: Monitor therapy

Felbamate: May increase the serum concentration of Barbiturates. Risk C: Monitor therapy

Griseofulvin: Barbiturates may decrease the absorption of Griseofulvin. Risk D: Consider therapy modification

LamoTRIgine: Barbiturates may increase the metabolism of LamoTRIgine. Risk D: Consider therapy modification

Meperidine: Barbiturates may enhance the CNS depressant effect of Meperidine. Risk C: Monitor therapy

Methadone: Barbiturates may increase the metabolism of Methadone. Risk D: Consider therapy modification

Oral Contraceptive (Estrogens): Barbiturates may diminish the therapeutic effect of Oral Contraceptive (Estrogens). Contraceptive failure is possible. Risk D: Consider therapy modification

Primidone: May enhance the adverse/toxic effect of Barbiturates. Primidone is converted to phenobarbital, and thus becomes additive with existing barbiturate therapy. Risk C: Monitor therapy

Propafenone: Barbiturates may increase the metabolism of Propafenone. Risk D: Consider therapy modification

Pyridoxine: May increase the metabolism of Barbiturates. Apparent in high pyridoxine doses (eg, 200 mg/day) Risk C: Monitor therapy

QuiNIDine: Barbiturates may increase the metabolism of QuiNIDine. Risk D: Consider therapy modification

Rifamycin Derivatives: May increase the metabolism of Barbiturates. Risk C: Monitor therapy

Teniposide: Barbiturates may increase the metabolism of Teniposide. Risk C: Monitor therapy

Theophylline Derivatives: Barbiturates may increase the metabolism of Theophylline Derivatives. Exceptions: Dyphylline. Risk C: Monitor therapy

Thiazide Diuretics: Barbiturates may enhance the orthostatic effect of Thiazide Diuretics. Risk C: Monitor therapy

Tricyclic Antidepressants: Barbiturates may increase the metabolism of Tricyclic Antidepressants. Risk D: Consider therapy modification

Valproic Acid: May decrease the metabolism of Barbiturates. Barbiturates may decrease the serum concentration of Valproic Acid. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Barbiturates may increase the metabolism of Vitamin K Antagonists. Risk D: Consider therapy modification

Voriconazole: Barbiturates may decrease the serum concentration of Voriconazole. Risk X: Avoid combination

ETHANOL / NUTRITION / HERB INTERACTIONS — Ethanol: Avoid ethanol (may increase CNS depression).

PREGNANCY RISK FACTOR — D (show table)

PREGNANCY IMPLICATIONS — Barbiturates cross the placenta and distribute in fetal tissue. Teratogenic effects have been reported with 1st trimester exposure. Exposure during the 3rd trimester may lead to symptoms of acute withdrawal following delivery; symptoms may be delayed up to 14 days.

LACTATION — Excretion in breast milk unknown/use caution

BREAST-FEEDING CONSIDERATIONS — Small amounts of barbiturates are excreted in breast milk; information specific for amobarbital is not available.

MONITORING PARAMETERS — Vital signs should be monitored during injection and for several hours after administration.

REFERENCE RANGE
Therapeutic: 1-5 mcg/mL (SI: 4-22 µmol/L)

Toxic: >10 mcg/mL (SI: >44 µmol/L)

Lethal: >50 mcg/mL

CANADIAN BRAND NAMES — Amytal®

INTERNATIONAL BRAND NAMES — Amybital (TW); Amycal (NO); Amytal Sodium (AU); Barbamyl (IL); Dorlotin (HU); Dorlotyn (HU); Eunoctal (FR); Isoamitil Sedante (ES); Isomytal (JP); Neur-Amyl (AU); Placidel (ES); Sodium Amytal (GB); Transital (ES)

MECHANISM OF ACTION — Interferes with transmission of impulses from the thalamus to the cortex of the brain resulting in an imbalance in central inhibitory and facilitatory mechanisms

PHARMACODYNAMICS / KINETICS
Onset of action: I.V.: Within 5 minutes

Distribution: Readily crosses placenta; small amounts enter breast milk

Metabolism: Primarily hepatic via microsomal enzymes

Half-life elimination: 15-40 hours (mean: 25 hours)

Excretion: Urine, feces

Pages

Monday, August 2, 2010

Amoxicillin and clavulanate potassium

Amoxicillin

Amoxapine

Amoxicillin

Amoxapine

Amobarbital