U.S. BRAND NAMES — Albenza®
PHARMACOLOGIC CATEGORY Anthelmintic
DOSING: ADULTS Neurocysticercosis: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) for 8-30 days 60 kg: 400 mg twice daily for 8-30 days Note: Give concurrent anticonvulsant and steroid therapy during first week.
Hydatid: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) 60 kg: 400 mg twice daily Note: Administer dose for three 28-day cycles with a 14-day drug-free interval in between.
Ancylostoma caninum, Ascaris lumbricoides(roundworm), Ancylostoma duodenale, and Necator americanus(hookworms) (unlabeled use): Oral: 400 mg as a single dose
Clonorchis sinensis(Chinese liver fluke) (unlabeled use): Oral: 10 mg/kg for 7 days
Cutaneous larva migrans (unlabeled use): Oral: 400 mg once daily for 3 days
Enterobius vermicularis(pinworm) (unlabeled use): Oral: 400 mg as a single dose; may repeat in 2 weeks
Gnathostoma spinigerum (unlabeled use): Oral: 400 mg twice daily for 21 days
Gongylonemiasis (unlabeled use): Oral: 10 mg/kg/day for 3 days
Mansonella perstans(unlabeled use): Oral: 400 mg twice daily for 10 days
Visceral larva migrans (toxocariasis) (unlabeled use): Oral: 400 mg twice daily for 5 days
Cysticercus cellulosae(unlabeled use): Oral: 400 mg twice daily for 8-30 days; may be repeated as necessary
Disseminated microsporidiosis (unlabeled use): Oral: 400 mg twice daily
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 400 mg twice daily for 1-6 months
Intestinal microsporidiosis (unlabeled use): Oral: 400 mg twice daily for 21 days
Ocular microsporidiosis (unlabeled use): Oral: 400 mg twice daily, in combination with fumagillin
DOSING: PEDIATRIC
(For additional information see "Albendazole: Pediatric drug information")Neurocysticercosis: Oral: Refer to adult dosing.
Hydatid: Oral: Refer to adult dosing.
Cysticercus cellulosae(unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg/day) in 2 divided doses for 8-30 days; may be repeated as necessary
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg) divided twice daily for 1-6 months
For the following unlabeled uses, refer to adult dosing: Ancylostoma caninum, Ascaris lumbricoides (roundworm), Ancylostoma duodenale, Clonorchis sinensis, (Chinese liver fluke), cutaneous larva migrans, Enterobius vermicularis (pinworm), Gnathostoma spinigerum, gongylonemiasis, Mansonella perstans, Necator americanus (hookworms), visceral larva migrans (toxocariasis)
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 200 mg
DOSAGE FORMS: CONCISE Tablet: Albenza®: 200 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer with meals. Administer anticonvulsant and steroid therapy during first week of neurocysticercosis therapy.
USE — Treatment of parenchymal neurocysticercosis caused by Taenia solium and cystic hydatid disease of the liver, lung, and peritoneum caused by Echinococcus granulosus
USE - UNLABELED / INVESTIGATIONAL — Albendazole has activity against Ascaris lumbricoides (roundworm); Ancylostoma caninum; Ancylostoma duodenale and Necator americanus (hookworms); cutaneous larva migrans; Enterobius vermicularis (pinworm); Gnathostoma spinigerum; Gongylonema sp; Hymenolepis nana sp (tapeworms); Mansonella perstans (filariasis); Opisthorchis sinensis and Opisthorchis viverrini (liver flukes); Strongyloides stercoralis and Trichuris trichiura (whipworm); visceral larva migrans (toxocariasis); activity has also been shown against the liver fluke Clonorchis sinensis, Giardia lamblia, Cysticercus cellulosae, and Echinococcus multilocularis. Albendazole has also been used for the treatment of intestinal microsporidiosis (Encephalitozoon intestinalis), disseminated microsporidiosis (E. hellem, E. cuniculi, E. intestinalis, Pleistophora sp, Trachipleistophora sp, Brachiola vesicularum), and ocular microsporidiosis (E. hellem, E. cuniculi, Vittaforma corneae).
ADVERSE REACTIONS SIGNIFICANT N = Neurocysticercosis; H = Hydatid disease
>10%: Central nervous system: Headache (11% - N; 1% - H) Hepatic: LFTs increased (~15% - H; <1% - N)
1% to 10%: Central nervous system: Dizziness, vertigo, fever (1%), intracranial pressure increased (1% - N), meningeal signs (1% - N) Dermatologic: Alopecia (2% - H; <1% - N) Gastrointestinal: Abdominal pain (6% - H; 0% - N), nausea/vomiting (3% to 6%) Hematologic: Leukopenia (reversible) (<1%) Miscellaneous: Allergic reactions (<1%)
<1% (Limited to important or life-threatening): Acute renal failure, agranulocytopenia, allergic reaction, granulocytopenia, pancytopenia, rash, thrombocytopenia, urticaria
CONTRAINDICATIONS — Hypersensitivity to albendazole or any component of the formulation
WARNINGS / PRECAUTIONS — Discontinue therapy if LFT elevations are significant; may restart treatment when decreased to pretreatment values. Becoming pregnant within 1 month following therapy is not advised.
Neurocysticercosis: Corticosteroids should be administered 1-2 days before albendazole therapy to minimize inflammatory reactions. Steroid and anticonvulsant therapy should be used concurrently during the first week of therapy to prevent cerebral hypertension. If retinal lesions exist, weigh risk of further retinal damage due to albendazole-induced changes to the retinal lesion vs benefit of disease treatment.
DRUG INTERACTIONS — Substrate (minor) of CYP1A2, 3A4; Inhibits CYP1A2 (weak)
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Albendazole serum levels may be increased if taken with a fatty meal (increases the oral bioavailability by 4-5 times).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Albendazole has been shown to be teratogenic in laboratory animals and should not be used during pregnancy, if at all possible. Women should be advised to avoid pregnancy for at least 1 month following therapy. Discontinue if pregnancy occurs during treatment.
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — Should be taken with a high-fat meal.
PRICING — (data from drugstore.com)Tablets (Albenza) 200 mg (12): $23.59
MONITORING PARAMETERS — Monitor fecal specimens for ova and parasites for 3 weeks after treatment; if positive, retreat; monitor LFTs and clinical signs of hepatotoxicity; CBC at start of each 28-day cycle and every 2 weeks during therapy
INTERNATIONAL BRAND NAMES — Abentel (CN); ABZ (IN); Acure (PK); Adazol (EC); Albatel (TH); Alben (BR); Albendol (MY); Albenzol (EC); Albex (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Albezole (IN); Alfuca (TH); Alminth (IN); Alzental (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SG, SY, YE); Alzol (TH); Bendapar (MX); Bendex-400 (ZA); Borotel (PE); Ceprazol (CL, PE); Champs D-Worm 6 (MY); Ciclopar (CO); Dalben (HR); Emanthal (IN); Eskazole (AT, AU, DE, GB, IL, JP, MX, NL); Fintel (PE); Gascop (MX); Getzol (CO); Helmiben (UY); Labenda (TH); Loveral (MX); Mebenix (BR); Monodox (CO); Mycotel (TH); Nemozole (IN); Pantex (PY); Paranthil (ZA); Rotopar (EC); Sioban (IN); Vastus (AR); Vemizol (MY); Vermin Plus (MX); Xadem (CO); Zeben (TH); Zela (TH); Zentab (TH); Zentel (AE, AN, AU, BB, BF, BG, BH, BJ, BM, BR, BS, BZ, CI, CL, CO, CR, CY, CZ, DO, EC, EG, ET, FR, GH, GM, GN, GR, GT, GY, HN, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, OM, PA, PE, PH, PL, QA, SA, SC, SD, SL, SN, SR, SV, SY, TH, TT, TZ, UG, VE, YE, ZA, ZM, ZW)
MECHANISM OF ACTION — Active metabolite, albendazole, causes selective degeneration of cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae; glycogen is depleted, glucose uptake and cholinesterase secretion are impaired, and desecratory substances accumulate intracellulary. ATP production decreases causing energy depletion, immobilization, and worm death.
PHARMACODYNAMICS / KINETICS Absorption: <5%; may increase up to 4-5 times when administered with a fatty meal
Distribution: Well inside hydatid cysts and CSF
Protein binding: 70%
Metabolism: Hepatic; extensive first-pass effect; pathways include rapid sulfoxidation (major), hydrolysis, and oxidation
Half-life elimination: 8-12 hours
Time to peak, serum: 2-2.4 hours
Excretion: Urine (<1% as active metabolite); feces
Wednesday, January 23, 2008
Albendazole
U.S. BRAND NAMES — Albenza®
PHARMACOLOGIC CATEGORY Anthelmintic
DOSING: ADULTS Neurocysticercosis: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) for 8-30 days 60 kg: 400 mg twice daily for 8-30 days Note: Give concurrent anticonvulsant and steroid therapy during first week.
Hydatid: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) 60 kg: 400 mg twice daily Note: Administer dose for three 28-day cycles with a 14-day drug-free interval in between.
Ancylostoma caninum, Ascaris lumbricoides(roundworm), Ancylostoma duodenale, and Necator americanus(hookworms) (unlabeled use): Oral: 400 mg as a single dose
Clonorchis sinensis(Chinese liver fluke) (unlabeled use): Oral: 10 mg/kg for 7 days
Cutaneous larva migrans (unlabeled use): Oral: 400 mg once daily for 3 days
Enterobius vermicularis(pinworm) (unlabeled use): Oral: 400 mg as a single dose; may repeat in 2 weeks
Gnathostoma spinigerum (unlabeled use): Oral: 400 mg twice daily for 21 days
Gongylonemiasis (unlabeled use): Oral: 10 mg/kg/day for 3 days
Mansonella perstans(unlabeled use): Oral: 400 mg twice daily for 10 days
Visceral larva migrans (toxocariasis) (unlabeled use): Oral: 400 mg twice daily for 5 days
Cysticercus cellulosae(unlabeled use): Oral: 400 mg twice daily for 8-30 days; may be repeated as necessary
Disseminated microsporidiosis (unlabeled use): Oral: 400 mg twice daily
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 400 mg twice daily for 1-6 months
Intestinal microsporidiosis (unlabeled use): Oral: 400 mg twice daily for 21 days
Ocular microsporidiosis (unlabeled use): Oral: 400 mg twice daily, in combination with fumagillin
DOSING: PEDIATRIC
(For additional information see "Albendazole: Pediatric drug information")Neurocysticercosis: Oral: Refer to adult dosing.
Hydatid: Oral: Refer to adult dosing.
Cysticercus cellulosae(unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg/day) in 2 divided doses for 8-30 days; may be repeated as necessary
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg) divided twice daily for 1-6 months
For the following unlabeled uses, refer to adult dosing: Ancylostoma caninum, Ascaris lumbricoides (roundworm), Ancylostoma duodenale, Clonorchis sinensis, (Chinese liver fluke), cutaneous larva migrans, Enterobius vermicularis (pinworm), Gnathostoma spinigerum, gongylonemiasis, Mansonella perstans, Necator americanus (hookworms), visceral larva migrans (toxocariasis)
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 200 mg
DOSAGE FORMS: CONCISE Tablet: Albenza®: 200 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer with meals. Administer anticonvulsant and steroid therapy during first week of neurocysticercosis therapy.
USE — Treatment of parenchymal neurocysticercosis caused by Taenia solium and cystic hydatid disease of the liver, lung, and peritoneum caused by Echinococcus granulosus
USE - UNLABELED / INVESTIGATIONAL — Albendazole has activity against Ascaris lumbricoides (roundworm); Ancylostoma caninum; Ancylostoma duodenale and Necator americanus (hookworms); cutaneous larva migrans; Enterobius vermicularis (pinworm); Gnathostoma spinigerum; Gongylonema sp; Hymenolepis nana sp (tapeworms); Mansonella perstans (filariasis); Opisthorchis sinensis and Opisthorchis viverrini (liver flukes); Strongyloides stercoralis and Trichuris trichiura (whipworm); visceral larva migrans (toxocariasis); activity has also been shown against the liver fluke Clonorchis sinensis, Giardia lamblia, Cysticercus cellulosae, and Echinococcus multilocularis. Albendazole has also been used for the treatment of intestinal microsporidiosis (Encephalitozoon intestinalis), disseminated microsporidiosis (E. hellem, E. cuniculi, E. intestinalis, Pleistophora sp, Trachipleistophora sp, Brachiola vesicularum), and ocular microsporidiosis (E. hellem, E. cuniculi, Vittaforma corneae).
ADVERSE REACTIONS SIGNIFICANT N = Neurocysticercosis; H = Hydatid disease
>10%: Central nervous system: Headache (11% - N; 1% - H) Hepatic: LFTs increased (~15% - H; <1% - N)
1% to 10%: Central nervous system: Dizziness, vertigo, fever (1%), intracranial pressure increased (1% - N), meningeal signs (1% - N) Dermatologic: Alopecia (2% - H; <1% - N) Gastrointestinal: Abdominal pain (6% - H; 0% - N), nausea/vomiting (3% to 6%) Hematologic: Leukopenia (reversible) (<1%) Miscellaneous: Allergic reactions (<1%)
<1% (Limited to important or life-threatening): Acute renal failure, agranulocytopenia, allergic reaction, granulocytopenia, pancytopenia, rash, thrombocytopenia, urticaria
CONTRAINDICATIONS — Hypersensitivity to albendazole or any component of the formulation
WARNINGS / PRECAUTIONS — Discontinue therapy if LFT elevations are significant; may restart treatment when decreased to pretreatment values. Becoming pregnant within 1 month following therapy is not advised.
Neurocysticercosis: Corticosteroids should be administered 1-2 days before albendazole therapy to minimize inflammatory reactions. Steroid and anticonvulsant therapy should be used concurrently during the first week of therapy to prevent cerebral hypertension. If retinal lesions exist, weigh risk of further retinal damage due to albendazole-induced changes to the retinal lesion vs benefit of disease treatment.
DRUG INTERACTIONS — Substrate (minor) of CYP1A2, 3A4; Inhibits CYP1A2 (weak)
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Albendazole serum levels may be increased if taken with a fatty meal (increases the oral bioavailability by 4-5 times).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Albendazole has been shown to be teratogenic in laboratory animals and should not be used during pregnancy, if at all possible. Women should be advised to avoid pregnancy for at least 1 month following therapy. Discontinue if pregnancy occurs during treatment.
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — Should be taken with a high-fat meal.
PRICING — (data from drugstore.com)Tablets (Albenza) 200 mg (12): $23.59
MONITORING PARAMETERS — Monitor fecal specimens for ova and parasites for 3 weeks after treatment; if positive, retreat; monitor LFTs and clinical signs of hepatotoxicity; CBC at start of each 28-day cycle and every 2 weeks during therapy
INTERNATIONAL BRAND NAMES — Abentel (CN); ABZ (IN); Acure (PK); Adazol (EC); Albatel (TH); Alben (BR); Albendol (MY); Albenzol (EC); Albex (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Albezole (IN); Alfuca (TH); Alminth (IN); Alzental (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SG, SY, YE); Alzol (TH); Bendapar (MX); Bendex-400 (ZA); Borotel (PE); Ceprazol (CL, PE); Champs D-Worm 6 (MY); Ciclopar (CO); Dalben (HR); Emanthal (IN); Eskazole (AT, AU, DE, GB, IL, JP, MX, NL); Fintel (PE); Gascop (MX); Getzol (CO); Helmiben (UY); Labenda (TH); Loveral (MX); Mebenix (BR); Monodox (CO); Mycotel (TH); Nemozole (IN); Pantex (PY); Paranthil (ZA); Rotopar (EC); Sioban (IN); Vastus (AR); Vemizol (MY); Vermin Plus (MX); Xadem (CO); Zeben (TH); Zela (TH); Zentab (TH); Zentel (AE, AN, AU, BB, BF, BG, BH, BJ, BM, BR, BS, BZ, CI, CL, CO, CR, CY, CZ, DO, EC, EG, ET, FR, GH, GM, GN, GR, GT, GY, HN, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, OM, PA, PE, PH, PL, QA, SA, SC, SD, SL, SN, SR, SV, SY, TH, TT, TZ, UG, VE, YE, ZA, ZM, ZW)
MECHANISM OF ACTION — Active metabolite, albendazole, causes selective degeneration of cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae; glycogen is depleted, glucose uptake and cholinesterase secretion are impaired, and desecratory substances accumulate intracellulary. ATP production decreases causing energy depletion, immobilization, and worm death.
PHARMACODYNAMICS / KINETICS Absorption: <5%; may increase up to 4-5 times when administered with a fatty meal
Distribution: Well inside hydatid cysts and CSF
Protein binding: 70%
Metabolism: Hepatic; extensive first-pass effect; pathways include rapid sulfoxidation (major), hydrolysis, and oxidation
Half-life elimination: 8-12 hours
Time to peak, serum: 2-2.4 hours
Excretion: Urine (<1% as active metabolite); feces
PHARMACOLOGIC CATEGORY Anthelmintic
DOSING: ADULTS Neurocysticercosis: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) for 8-30 days 60 kg: 400 mg twice daily for 8-30 days Note: Give concurrent anticonvulsant and steroid therapy during first week.
Hydatid: Oral: <60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) 60 kg: 400 mg twice daily Note: Administer dose for three 28-day cycles with a 14-day drug-free interval in between.
Ancylostoma caninum, Ascaris lumbricoides(roundworm), Ancylostoma duodenale, and Necator americanus(hookworms) (unlabeled use): Oral: 400 mg as a single dose
Clonorchis sinensis(Chinese liver fluke) (unlabeled use): Oral: 10 mg/kg for 7 days
Cutaneous larva migrans (unlabeled use): Oral: 400 mg once daily for 3 days
Enterobius vermicularis(pinworm) (unlabeled use): Oral: 400 mg as a single dose; may repeat in 2 weeks
Gnathostoma spinigerum (unlabeled use): Oral: 400 mg twice daily for 21 days
Gongylonemiasis (unlabeled use): Oral: 10 mg/kg/day for 3 days
Mansonella perstans(unlabeled use): Oral: 400 mg twice daily for 10 days
Visceral larva migrans (toxocariasis) (unlabeled use): Oral: 400 mg twice daily for 5 days
Cysticercus cellulosae(unlabeled use): Oral: 400 mg twice daily for 8-30 days; may be repeated as necessary
Disseminated microsporidiosis (unlabeled use): Oral: 400 mg twice daily
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 400 mg twice daily for 1-6 months
Intestinal microsporidiosis (unlabeled use): Oral: 400 mg twice daily for 21 days
Ocular microsporidiosis (unlabeled use): Oral: 400 mg twice daily, in combination with fumagillin
DOSING: PEDIATRIC
(For additional information see "Albendazole: Pediatric drug information")Neurocysticercosis: Oral: Refer to adult dosing.
Hydatid: Oral: Refer to adult dosing.
Cysticercus cellulosae(unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg/day) in 2 divided doses for 8-30 days; may be repeated as necessary
Echinococcus granulosus(tapeworm) (unlabeled use): Oral: 15 mg/kg/day (maximum: 800 mg) divided twice daily for 1-6 months
For the following unlabeled uses, refer to adult dosing: Ancylostoma caninum, Ascaris lumbricoides (roundworm), Ancylostoma duodenale, Clonorchis sinensis, (Chinese liver fluke), cutaneous larva migrans, Enterobius vermicularis (pinworm), Gnathostoma spinigerum, gongylonemiasis, Mansonella perstans, Necator americanus (hookworms), visceral larva migrans (toxocariasis)
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet: 200 mg
DOSAGE FORMS: CONCISE Tablet: Albenza®: 200 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Administer with meals. Administer anticonvulsant and steroid therapy during first week of neurocysticercosis therapy.
USE — Treatment of parenchymal neurocysticercosis caused by Taenia solium and cystic hydatid disease of the liver, lung, and peritoneum caused by Echinococcus granulosus
USE - UNLABELED / INVESTIGATIONAL — Albendazole has activity against Ascaris lumbricoides (roundworm); Ancylostoma caninum; Ancylostoma duodenale and Necator americanus (hookworms); cutaneous larva migrans; Enterobius vermicularis (pinworm); Gnathostoma spinigerum; Gongylonema sp; Hymenolepis nana sp (tapeworms); Mansonella perstans (filariasis); Opisthorchis sinensis and Opisthorchis viverrini (liver flukes); Strongyloides stercoralis and Trichuris trichiura (whipworm); visceral larva migrans (toxocariasis); activity has also been shown against the liver fluke Clonorchis sinensis, Giardia lamblia, Cysticercus cellulosae, and Echinococcus multilocularis. Albendazole has also been used for the treatment of intestinal microsporidiosis (Encephalitozoon intestinalis), disseminated microsporidiosis (E. hellem, E. cuniculi, E. intestinalis, Pleistophora sp, Trachipleistophora sp, Brachiola vesicularum), and ocular microsporidiosis (E. hellem, E. cuniculi, Vittaforma corneae).
ADVERSE REACTIONS SIGNIFICANT N = Neurocysticercosis; H = Hydatid disease
>10%: Central nervous system: Headache (11% - N; 1% - H) Hepatic: LFTs increased (~15% - H; <1% - N)
1% to 10%: Central nervous system: Dizziness, vertigo, fever (1%), intracranial pressure increased (1% - N), meningeal signs (1% - N) Dermatologic: Alopecia (2% - H; <1% - N) Gastrointestinal: Abdominal pain (6% - H; 0% - N), nausea/vomiting (3% to 6%) Hematologic: Leukopenia (reversible) (<1%) Miscellaneous: Allergic reactions (<1%)
<1% (Limited to important or life-threatening): Acute renal failure, agranulocytopenia, allergic reaction, granulocytopenia, pancytopenia, rash, thrombocytopenia, urticaria
CONTRAINDICATIONS — Hypersensitivity to albendazole or any component of the formulation
WARNINGS / PRECAUTIONS — Discontinue therapy if LFT elevations are significant; may restart treatment when decreased to pretreatment values. Becoming pregnant within 1 month following therapy is not advised.
Neurocysticercosis: Corticosteroids should be administered 1-2 days before albendazole therapy to minimize inflammatory reactions. Steroid and anticonvulsant therapy should be used concurrently during the first week of therapy to prevent cerebral hypertension. If retinal lesions exist, weigh risk of further retinal damage due to albendazole-induced changes to the retinal lesion vs benefit of disease treatment.
DRUG INTERACTIONS — Substrate (minor) of CYP1A2, 3A4; Inhibits CYP1A2 (weak)
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Albendazole serum levels may be increased if taken with a fatty meal (increases the oral bioavailability by 4-5 times).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Albendazole has been shown to be teratogenic in laboratory animals and should not be used during pregnancy, if at all possible. Women should be advised to avoid pregnancy for at least 1 month following therapy. Discontinue if pregnancy occurs during treatment.
LACTATION — Excretion in breast milk unknown/not recommended
DIETARY CONSIDERATIONS — Should be taken with a high-fat meal.
PRICING — (data from drugstore.com)Tablets (Albenza) 200 mg (12): $23.59
MONITORING PARAMETERS — Monitor fecal specimens for ova and parasites for 3 weeks after treatment; if positive, retreat; monitor LFTs and clinical signs of hepatotoxicity; CBC at start of each 28-day cycle and every 2 weeks during therapy
INTERNATIONAL BRAND NAMES — Abentel (CN); ABZ (IN); Acure (PK); Adazol (EC); Albatel (TH); Alben (BR); Albendol (MY); Albenzol (EC); Albex (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Albezole (IN); Alfuca (TH); Alminth (IN); Alzental (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SG, SY, YE); Alzol (TH); Bendapar (MX); Bendex-400 (ZA); Borotel (PE); Ceprazol (CL, PE); Champs D-Worm 6 (MY); Ciclopar (CO); Dalben (HR); Emanthal (IN); Eskazole (AT, AU, DE, GB, IL, JP, MX, NL); Fintel (PE); Gascop (MX); Getzol (CO); Helmiben (UY); Labenda (TH); Loveral (MX); Mebenix (BR); Monodox (CO); Mycotel (TH); Nemozole (IN); Pantex (PY); Paranthil (ZA); Rotopar (EC); Sioban (IN); Vastus (AR); Vemizol (MY); Vermin Plus (MX); Xadem (CO); Zeben (TH); Zela (TH); Zentab (TH); Zentel (AE, AN, AU, BB, BF, BG, BH, BJ, BM, BR, BS, BZ, CI, CL, CO, CR, CY, CZ, DO, EC, EG, ET, FR, GH, GM, GN, GR, GT, GY, HN, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, OM, PA, PE, PH, PL, QA, SA, SC, SD, SL, SN, SR, SV, SY, TH, TT, TZ, UG, VE, YE, ZA, ZM, ZW)
MECHANISM OF ACTION — Active metabolite, albendazole, causes selective degeneration of cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae; glycogen is depleted, glucose uptake and cholinesterase secretion are impaired, and desecratory substances accumulate intracellulary. ATP production decreases causing energy depletion, immobilization, and worm death.
PHARMACODYNAMICS / KINETICS Absorption: <5%; may increase up to 4-5 times when administered with a fatty meal
Distribution: Well inside hydatid cysts and CSF
Protein binding: 70%
Metabolism: Hepatic; extensive first-pass effect; pathways include rapid sulfoxidation (major), hydrolysis, and oxidation
Half-life elimination: 8-12 hours
Time to peak, serum: 2-2.4 hours
Excretion: Urine (<1% as active metabolite); feces
Agalsidase beta
U.S. BRAND NAMES — Fabrazyme®
PHARMACOLOGIC CATEGORY Enzyme
DOSING: ADULTS — Fabry disease: I.V.: 1 mg/kg every 2 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No dosage adjustment required.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution: 5 mg [contains mannitol 33 mg; derived from Chinese hamster cells]; 35 mg [contains mannitol 222 mg/vial; derived from Chinese hamster cells]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution: Fabrazyme®: 5 mg, 35 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Antipyretics should be administered prior to infusion. Initial infusion rate should not exceed 0.25 mg/minute (15 mg/hour). Decrease rate in the event of an infusion reaction. After patient tolerance to the infusion is established, rate may be increased in increments of 0.05-0.08 mg/minute (3-5 mg/hour) with each subsequent infusion. A 0.2 micron low protein-binding filter may be used.
COMPATIBILITY — Stable in NS.
Compatibility when admixed: Do not mix with other products.
USE — Replacement therapy for Fabry disease
ADVERSE REACTIONS SIGNIFICANT — Note: The most common and serious adverse reactions are infusion reactions (symptoms may include fever, tachycardia, hypertension, throat tightness, dyspnea, chills, abdominal pain, pruritus, urticaria, vomiting).
>10%: Cardiovascular: Edema (21%), chest pain (17%), hypotension (14%) Central nervous system: Fever (48%), headache (45%), anxiety (28%), pain (21%), dizziness (14%), paresthesia (14%) Dermatologic: Pallor (14%) Gastrointestinal: Nausea (28%) Neuromuscular & skeletal: Rigors (52%), skeletal pain (21%) Respiratory: Rhinitis (38%), pharyngitis (28%) Miscellaneous: Infusion reactions (alteration of temperature sensation 17%)
1% to 10%: Cardiovascular: Cardiomegaly (10%), hypertension (10%) Central nervous system: Depression (10%) Gastrointestinal: Dyspepsia (10%) Genitourinary: Testicular pain (7%) Neuromuscular & skeletal: Arthrosis (10%) Respiratory: Bronchitis (10%), bronchospasm (7%), laryngitis (7%), sinusitis (7%)
Other reported severe reactions (frequency not established): Arrhythmia, ataxia, bradycardia, cardiac arrest, cardiac output decreased, nephritic syndrome, stroke, vertigo
CONTRAINDICATIONS — No known contraindications
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Infusion reactions: Are common, and may be severe; pretreatment with antipyretics is advised.
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease; risk related infusion reactions may be increased.
Special populations: Pediatrics: Safety and efficacy have not been established in children (studies limited to patients 16 years of age).
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.fabryregistry.com or 1-800-745-4447).
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential are encouraged to enroll in Fabry registry.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Nursing mothers are encouraged to enroll in Fabry registry.
MONITORING PARAMETERS — Development of IgG or IgE antibodies in patients with suspected allergic reactions (test available from manufacturer).
CANADIAN BRAND NAMES — Fabrazyme®
INTERNATIONAL BRAND NAMES — Fabrazyme (AT, BE, BG, CA, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IL, IT, NL, NO, PL, PT, RU, SE, TR)
MECHANISM OF ACTION — Agalsidase beta is a recombinant form of the enzyme alpha-galactosidase-A, which is required for the hydrolysis of GL-3 and other glycosphingolipids. The compounds may accumulate (over many years) within the tissues of patients with Fabry disease, leading to renal and cardiovascular complications. In clinical trials of limited duration, agalsidase been noted to reduce tissue inclusions of a key sphingolipid (GL-3). It is believed that long-term enzyme replacement may reduce clinical manifestations of renal failure, cardiomyopathy, and stroke. However, the relationship to a reduction in clinical manifestations has not been established.
PHARMACODYNAMICS / KINETICS — Half-life elimination: 42-102 minutes (nonlinear)
PHARMACOLOGIC CATEGORY Enzyme
DOSING: ADULTS — Fabry disease: I.V.: 1 mg/kg every 2 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No dosage adjustment required.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution: 5 mg [contains mannitol 33 mg; derived from Chinese hamster cells]; 35 mg [contains mannitol 222 mg/vial; derived from Chinese hamster cells]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution: Fabrazyme®: 5 mg, 35 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Antipyretics should be administered prior to infusion. Initial infusion rate should not exceed 0.25 mg/minute (15 mg/hour). Decrease rate in the event of an infusion reaction. After patient tolerance to the infusion is established, rate may be increased in increments of 0.05-0.08 mg/minute (3-5 mg/hour) with each subsequent infusion. A 0.2 micron low protein-binding filter may be used.
COMPATIBILITY — Stable in NS.
Compatibility when admixed: Do not mix with other products.
USE — Replacement therapy for Fabry disease
ADVERSE REACTIONS SIGNIFICANT — Note: The most common and serious adverse reactions are infusion reactions (symptoms may include fever, tachycardia, hypertension, throat tightness, dyspnea, chills, abdominal pain, pruritus, urticaria, vomiting).
>10%: Cardiovascular: Edema (21%), chest pain (17%), hypotension (14%) Central nervous system: Fever (48%), headache (45%), anxiety (28%), pain (21%), dizziness (14%), paresthesia (14%) Dermatologic: Pallor (14%) Gastrointestinal: Nausea (28%) Neuromuscular & skeletal: Rigors (52%), skeletal pain (21%) Respiratory: Rhinitis (38%), pharyngitis (28%) Miscellaneous: Infusion reactions (alteration of temperature sensation 17%)
1% to 10%: Cardiovascular: Cardiomegaly (10%), hypertension (10%) Central nervous system: Depression (10%) Gastrointestinal: Dyspepsia (10%) Genitourinary: Testicular pain (7%) Neuromuscular & skeletal: Arthrosis (10%) Respiratory: Bronchitis (10%), bronchospasm (7%), laryngitis (7%), sinusitis (7%)
Other reported severe reactions (frequency not established): Arrhythmia, ataxia, bradycardia, cardiac arrest, cardiac output decreased, nephritic syndrome, stroke, vertigo
CONTRAINDICATIONS — No known contraindications
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Infusion reactions: Are common, and may be severe; pretreatment with antipyretics is advised.
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease; risk related infusion reactions may be increased.
Special populations: Pediatrics: Safety and efficacy have not been established in children (studies limited to patients 16 years of age).
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.fabryregistry.com or 1-800-745-4447).
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential are encouraged to enroll in Fabry registry.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Nursing mothers are encouraged to enroll in Fabry registry.
MONITORING PARAMETERS — Development of IgG or IgE antibodies in patients with suspected allergic reactions (test available from manufacturer).
CANADIAN BRAND NAMES — Fabrazyme®
INTERNATIONAL BRAND NAMES — Fabrazyme (AT, BE, BG, CA, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IL, IT, NL, NO, PL, PT, RU, SE, TR)
MECHANISM OF ACTION — Agalsidase beta is a recombinant form of the enzyme alpha-galactosidase-A, which is required for the hydrolysis of GL-3 and other glycosphingolipids. The compounds may accumulate (over many years) within the tissues of patients with Fabry disease, leading to renal and cardiovascular complications. In clinical trials of limited duration, agalsidase been noted to reduce tissue inclusions of a key sphingolipid (GL-3). It is believed that long-term enzyme replacement may reduce clinical manifestations of renal failure, cardiomyopathy, and stroke. However, the relationship to a reduction in clinical manifestations has not been established.
PHARMACODYNAMICS / KINETICS — Half-life elimination: 42-102 minutes (nonlinear)
Agalsidase beta
U.S. BRAND NAMES — Fabrazyme®
PHARMACOLOGIC CATEGORY Enzyme
DOSING: ADULTS — Fabry disease: I.V.: 1 mg/kg every 2 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No dosage adjustment required.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution: 5 mg [contains mannitol 33 mg; derived from Chinese hamster cells]; 35 mg [contains mannitol 222 mg/vial; derived from Chinese hamster cells]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution: Fabrazyme®: 5 mg, 35 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Antipyretics should be administered prior to infusion. Initial infusion rate should not exceed 0.25 mg/minute (15 mg/hour). Decrease rate in the event of an infusion reaction. After patient tolerance to the infusion is established, rate may be increased in increments of 0.05-0.08 mg/minute (3-5 mg/hour) with each subsequent infusion. A 0.2 micron low protein-binding filter may be used.
COMPATIBILITY — Stable in NS.
Compatibility when admixed: Do not mix with other products.
USE — Replacement therapy for Fabry disease
ADVERSE REACTIONS SIGNIFICANT — Note: The most common and serious adverse reactions are infusion reactions (symptoms may include fever, tachycardia, hypertension, throat tightness, dyspnea, chills, abdominal pain, pruritus, urticaria, vomiting).
>10%: Cardiovascular: Edema (21%), chest pain (17%), hypotension (14%) Central nervous system: Fever (48%), headache (45%), anxiety (28%), pain (21%), dizziness (14%), paresthesia (14%) Dermatologic: Pallor (14%) Gastrointestinal: Nausea (28%) Neuromuscular & skeletal: Rigors (52%), skeletal pain (21%) Respiratory: Rhinitis (38%), pharyngitis (28%) Miscellaneous: Infusion reactions (alteration of temperature sensation 17%)
1% to 10%: Cardiovascular: Cardiomegaly (10%), hypertension (10%) Central nervous system: Depression (10%) Gastrointestinal: Dyspepsia (10%) Genitourinary: Testicular pain (7%) Neuromuscular & skeletal: Arthrosis (10%) Respiratory: Bronchitis (10%), bronchospasm (7%), laryngitis (7%), sinusitis (7%)
Other reported severe reactions (frequency not established): Arrhythmia, ataxia, bradycardia, cardiac arrest, cardiac output decreased, nephritic syndrome, stroke, vertigo
CONTRAINDICATIONS — No known contraindications
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Infusion reactions: Are common, and may be severe; pretreatment with antipyretics is advised.
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease; risk related infusion reactions may be increased.
Special populations: Pediatrics: Safety and efficacy have not been established in children (studies limited to patients 16 years of age).
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.fabryregistry.com or 1-800-745-4447).
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential are encouraged to enroll in Fabry registry.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Nursing mothers are encouraged to enroll in Fabry registry.
MONITORING PARAMETERS — Development of IgG or IgE antibodies in patients with suspected allergic reactions (test available from manufacturer).
CANADIAN BRAND NAMES — Fabrazyme®
INTERNATIONAL BRAND NAMES — Fabrazyme (AT, BE, BG, CA, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IL, IT, NL, NO, PL, PT, RU, SE, TR)
MECHANISM OF ACTION — Agalsidase beta is a recombinant form of the enzyme alpha-galactosidase-A, which is required for the hydrolysis of GL-3 and other glycosphingolipids. The compounds may accumulate (over many years) within the tissues of patients with Fabry disease, leading to renal and cardiovascular complications. In clinical trials of limited duration, agalsidase been noted to reduce tissue inclusions of a key sphingolipid (GL-3). It is believed that long-term enzyme replacement may reduce clinical manifestations of renal failure, cardiomyopathy, and stroke. However, the relationship to a reduction in clinical manifestations has not been established.
PHARMACODYNAMICS / KINETICS — Half-life elimination: 42-102 minutes (nonlinear)
PHARMACOLOGIC CATEGORY Enzyme
DOSING: ADULTS — Fabry disease: I.V.: 1 mg/kg every 2 weeks
DOSING: ELDERLY — Refer to adult dosing.
DOSING: RENAL IMPAIRMENT — No dosage adjustment required.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution: 5 mg [contains mannitol 33 mg; derived from Chinese hamster cells]; 35 mg [contains mannitol 222 mg/vial; derived from Chinese hamster cells]
DOSAGE FORMS: CONCISE Injection, powder for reconstitution: Fabrazyme®: 5 mg, 35 mg
GENERIC EQUIVALENT AVAILABLE — No
ADMINISTRATION — Antipyretics should be administered prior to infusion. Initial infusion rate should not exceed 0.25 mg/minute (15 mg/hour). Decrease rate in the event of an infusion reaction. After patient tolerance to the infusion is established, rate may be increased in increments of 0.05-0.08 mg/minute (3-5 mg/hour) with each subsequent infusion. A 0.2 micron low protein-binding filter may be used.
COMPATIBILITY — Stable in NS.
Compatibility when admixed: Do not mix with other products.
USE — Replacement therapy for Fabry disease
ADVERSE REACTIONS SIGNIFICANT — Note: The most common and serious adverse reactions are infusion reactions (symptoms may include fever, tachycardia, hypertension, throat tightness, dyspnea, chills, abdominal pain, pruritus, urticaria, vomiting).
>10%: Cardiovascular: Edema (21%), chest pain (17%), hypotension (14%) Central nervous system: Fever (48%), headache (45%), anxiety (28%), pain (21%), dizziness (14%), paresthesia (14%) Dermatologic: Pallor (14%) Gastrointestinal: Nausea (28%) Neuromuscular & skeletal: Rigors (52%), skeletal pain (21%) Respiratory: Rhinitis (38%), pharyngitis (28%) Miscellaneous: Infusion reactions (alteration of temperature sensation 17%)
1% to 10%: Cardiovascular: Cardiomegaly (10%), hypertension (10%) Central nervous system: Depression (10%) Gastrointestinal: Dyspepsia (10%) Genitourinary: Testicular pain (7%) Neuromuscular & skeletal: Arthrosis (10%) Respiratory: Bronchitis (10%), bronchospasm (7%), laryngitis (7%), sinusitis (7%)
Other reported severe reactions (frequency not established): Arrhythmia, ataxia, bradycardia, cardiac arrest, cardiac output decreased, nephritic syndrome, stroke, vertigo
CONTRAINDICATIONS — No known contraindications
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Infusion reactions: Are common, and may be severe; pretreatment with antipyretics is advised.
Disease-related concerns: Cardiovascular disease: Use with caution in patients with cardiovascular disease; risk related infusion reactions may be increased.
Special populations: Pediatrics: Safety and efficacy have not been established in children (studies limited to patients 16 years of age).
Other warnings/precautions: Registry: A registry has been created to monitor therapeutic responses and adverse effects during long-term treatment; patients should be encouraged to register (www.fabryregistry.com or 1-800-745-4447).
DRUG INTERACTIONS — No formal drug interaction studies have been conducted.
PREGNANCY RISK FACTOR — B (show table)
PREGNANCY IMPLICATIONS — There are no adequate and well-controlled studies in pregnant women. Women of childbearing potential are encouraged to enroll in Fabry registry.
LACTATION — Excretion in breast milk unknown/use caution
BREAST-FEEDING CONSIDERATIONS — Nursing mothers are encouraged to enroll in Fabry registry.
MONITORING PARAMETERS — Development of IgG or IgE antibodies in patients with suspected allergic reactions (test available from manufacturer).
CANADIAN BRAND NAMES — Fabrazyme®
INTERNATIONAL BRAND NAMES — Fabrazyme (AT, BE, BG, CA, CH, CZ, DE, DK, ES, FI, FR, GB, GR, HU, IE, IL, IT, NL, NO, PL, PT, RU, SE, TR)
MECHANISM OF ACTION — Agalsidase beta is a recombinant form of the enzyme alpha-galactosidase-A, which is required for the hydrolysis of GL-3 and other glycosphingolipids. The compounds may accumulate (over many years) within the tissues of patients with Fabry disease, leading to renal and cardiovascular complications. In clinical trials of limited duration, agalsidase been noted to reduce tissue inclusions of a key sphingolipid (GL-3). It is believed that long-term enzyme replacement may reduce clinical manifestations of renal failure, cardiomyopathy, and stroke. However, the relationship to a reduction in clinical manifestations has not been established.
PHARMACODYNAMICS / KINETICS — Half-life elimination: 42-102 minutes (nonlinear)
Adenosine
U.S. BRAND NAMES — Adenocard®; Adenoscan®
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IVDiagnostic Agent
DOSING: ADULTS Paroxysmal supraventricular tachycardia (Adenocard®): I.V. (rapid - over 1-2 seconds, via peripheral line): 6 mg; if not effective within 1-2 minutes, 12 mg may be given; may repeat 12 mg bolus if needed; maximum single dose: 12 mg. Follow each I.V. bolus of adenosine with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via a central line at lower doses (ie, initial adult dose: 3 mg).
Pharmacologic stress agent (Adenoscan®): I.V.: Continuous I.V. infusion via peripheral line: 140 mcg/kg/minute for 6 minutes using syringe or columetric infusion pump; total dose: 0.84 mg/kg. Thallium-201 is injected at midpoint (3 minutes) of infusion.
Acute vasodilator testing (unlabeled use) (Adenoscan®): I.V.: Initial: 50 mcg/kg/minute increased by 50 mcg/kg/minute every 2 minutes to a maximum dose of 500 mcg/kg/minute; acutely assess vasodilator response
DOSING: PEDIATRIC
(For additional information see "Adenosine: Pediatric drug information")Paroxysmal supraventricular tachycardia (Adenocard®): Rapid I.V. push (over 1-2 seconds) via peripheral line: Infants and Children (manufacturer's recommendation): Children <50 kg: 0.05-0.1 mg/kg. If conversion of PSVT does not occur within 1-2 minutes, may increase dose by 0.05-0.1 mg/kg. May repeat until sinus rhythm is established or to a maximum single dose of 0.3 mg/kg or 12 mg. Follow each dose with normal saline flush. Children 50 kg: Refer to adult dosing.
Pediatric advanced life support (PALS): Treatment of SVT: I.V., I.O.: 0.1 mg/kg; if not effective, administer 0.2 mg/kg; maximum single dose: 12 mg. Follow each dose with normal saline flush.
DOSING: ELDERLY — Refer to adult dosing. Elderly may be more sensitive to effects of adenosine.
DOSING: RENAL IMPAIRMENT Hemodialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Peritoneal dialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Note: Higher doses may be needed for administration via peripheral versus central vein.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For rapid bolus I.V. use only; administer I.V. push over 1-2 seconds at a peripheral I.V. site as proximal as possible to trunk (not in lower arm, hand, lower leg, or foot); follow each bolus with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via central line at lower doses (eg, adults initial dose: 3 mg)
COMPATIBILITY — Stable in D5LR, D5W, LR, NS.
USE Adenocard®: Treatment of paroxysmal supraventricular tachycardia (PSVT) including that associated with accessory bypass tracts (Wolff-Parkinson-White syndrome); when clinically advisable, appropriate vagal maneuvers should be attempted prior to adenosine administration; not effective in atrial flutter, atrial fibrillation, or ventricular tachycardia
Adenoscan®: Pharmacologic stress agent used in myocardial perfusion thallium-201 scintigraphy
USE - UNLABELED / INVESTIGATIONAL — Adenoscan®: Acute vasodilator testing in pulmonary artery hypertension
ADVERSE REACTIONS SIGNIFICANT — Note: Frequency varies based on use; higher frequency of infusion-related effects, such as flushing and lightheadedness, were reported with continuous infusion (Adenoscan®).
>10%: Cardiovascular: Facial flushing (18% to 44%) Central nervous system: Headache (2% to 18%), lightheadedness (2% to 12%) Neuromuscular & skeletal: Discomfort of neck, throat, jaw (<1% to 15%) Respiratory: Dyspnea (12% to 28%), chest pressure/discomfort (7% to 40%)
1% to 10%: Cardiovascular: Hypotension (<1% to 2%), AV block (infusion 6%; third degree <1%), ST segment depression (3%), palpitation, chest pain Central nervous system: Dizziness, nervousness (2%), apprehension Gastrointestinal: Nausea (3%) Neuromuscular & skeletal: Upper extremity discomfort (up to 4%), numbness (up to 2%), paresthesia (up to 2%) Respiratory: Hyperventilation Miscellaneous: Diaphoresis
<1% (Limited to important or life-threatening): Asystole (prolonged), atrial fibrillation, back discomfort, bradycardia, bronchospasm, blurred vision, burning sensation, hypertension (transient), injection site reaction, intracranial pressure increased, metallic taste, pressure in groin, respiratory arrest, seizure, torsade de pointes, ventricular fibrillation, ventricular tachycardia
CONTRAINDICATIONS — Hypersensitivity to adenosine or any component of the formulation; second- or third-degree AV block or sick sinus syndrome (except in patients with a functioning artificial pacemaker), atrial flutter, atrial fibrillation, and ventricular tachycardia (this drug is not effective in converting these arrhythmias to sinus rhythm). The manufacturer states that Adenoscan® should be avoided in patients with known or suspected bronchoconstrictive or bronchospastic lung disease.
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Atrial fibrillation/flutter: There have been reports of atrial fibrillation/flutter in patients with paroxysmal supraventricular tachycardia (PSVT) associated with accessory conduction pathways after adenosine. Does not convert afib/flutter to normal sinus rhythm; risk of serious arrhythmias/hypotension. Not for use in patients with afib/flutter associated with Wolff-Parkinson-White Syndrome. Conduction disturbances: Adenosine decreases conduction through the AV node and may produce first-, second-, or third-degree heart block. Patients with pre-existing S-A nodal dysfunction may experience prolonged sinus pauses after adenosine; use caution in patients with first-degree AV block or bundle branch block; avoid use of adenosine for pharmacologic stress testing in patients with high-grade AV block or sinus node dysfunction (unless a functional pacemaker is in place). Rare, prolonged episodes of asystole have been reported, with fatal outcomes in some cases. Hypotension: May produce profound vasodilation with subsequent hypotension. When used as a bolus dose (PSVT), effects are generally self-limiting (due to the short half-life of adenosine). However, when used as a continuous infusion (pharmacologic stress testing), effects may be more pronounced and persistent, corresponding to continued exposure. Use infusions with caution in patients with autonomic dysfunction, carotid stenosis (with cerebrovascular insufficiency), uncorrected hypovolemia, pericarditis, pleural effusion and/or stenotic valvular heart disease. Proarrhythmic effects: Watch for proarrhythmic effects; monitor and adjust dose to prevent QTc prolongation.
Disease-related concerns: Asthma: A limited number of patients with asthma have received adenosine and have not experienced exacerbation of their asthma. Adenosine may cause bronchoconstriction in patients with asthma; should be used cautiously in patients with obstructive lung disease not associated with bronchoconstriction (eg, emphysema, bronchitis). Electrolyte imbalance: Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy.
Concurrent drug therapy issues: Caffeine: Pharmacologic stress testing: Withhold for five half-lives prior to adenosine use; avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing. Drugs which slow AV conduction: Use with caution in patients receiving other drugs which slow AV conduction (eg, digoxin, verapamil). Theophylline: Withhold for five half-lives prior to adenosine use whenever possible (eg, pharmacological stress testing).
Special populations: Elderly: Use with caution in the elderly; may be at increased risk of hemodynamic effects, bradycardia, and/or AV block.
Dosage form specific issues: Adenocard®: Transient AV block is expected. When used in PSVT, at the time of conversion to normal sinus rhythm, a variety of new rhythms may appear on the ECG. Administer as a rapid bolus, either directly into a vein or (if administered into an I.V. line), as close to the patient as possible (followed by saline flush).
Other warnings/precautions: CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, nonlife-threatening ventricular arrhythmias did not benefit and may have been harmed by attempts to suppress the arrhythmia with flecainide or encainide. An increased mortality or nonfatal cardiac arrest rate (7.7%) was seen in the active treatment group compared with patients in the placebo group (3%). The applicability of the CAST results to other populations is unknown. Antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmias.
DRUG INTERACTIONS Carbamazepine may increase heart block.
Dipyridamole potentiates effects of adenosine; reduce dose of adenosine.
Theophylline and caffeine (methylxanthines) antagonize adenosine's effects; may require increased dose of adenosine.
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Avoid food or drugs with caffeine. Adenosine's therapeutic effect may be decreased if used concurrently with caffeine. Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reports of administration during pregnancy have indicated no adverse effects on fetus or newborn attributable to adenosine.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
MONITORING PARAMETERS — ECG monitoring, heart rate, blood pressure
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Since the half-life of adenosine is <10 seconds, any adverse effects are rapidly self-limiting. Intoxication is usually short-lived since the half-life of the drug is very short. Treatment of prolonged effects requires individualization. Theophylline and other methylxanthines are competitive inhibitors of adenosine and may have a role in reversing its toxic effects. To reverse the effects of Adenoscan®, administer theophylline 50-125 mg slow I.V. push.
CANADIAN BRAND NAMES — Adenocard®; Adenoscan®; Adenosine Injection, USP
INTERNATIONAL BRAND NAMES — Adenocard (BR, CA); Adenocor (AU, BE, BG, CN, CZ, DK, EC, EE, EG, ES, FI, GB, HU, IE, IL, KR, MY, NO, NZ, PE, PL, TH, TW, UY, VE, ZA); Adenocur (NL); Adenoject (IN); Adenoscan (CA, HK); Adenosin Ebewe (PL); Adenosina Biol (AR, PY); Adenosine Injection, USP (CA); Adrekar (AT, DE); Cardiovert (PH); Fosfobion (PL); Krenosin (FR, IT, MX); Krenosine (CH); Soladen (PL)
MECHANISM OF ACTION — Slows conduction time through the AV node, interrupting the re-entry pathways through the AV node, restoring normal sinus rhythm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: Very brief
Metabolism: Blood and tissue to inosine then to adenosine monophosphate (AMP) and hypoxanthine
Half-life elimination: <10 seconds
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IVDiagnostic Agent
DOSING: ADULTS Paroxysmal supraventricular tachycardia (Adenocard®): I.V. (rapid - over 1-2 seconds, via peripheral line): 6 mg; if not effective within 1-2 minutes, 12 mg may be given; may repeat 12 mg bolus if needed; maximum single dose: 12 mg. Follow each I.V. bolus of adenosine with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via a central line at lower doses (ie, initial adult dose: 3 mg).
Pharmacologic stress agent (Adenoscan®): I.V.: Continuous I.V. infusion via peripheral line: 140 mcg/kg/minute for 6 minutes using syringe or columetric infusion pump; total dose: 0.84 mg/kg. Thallium-201 is injected at midpoint (3 minutes) of infusion.
Acute vasodilator testing (unlabeled use) (Adenoscan®): I.V.: Initial: 50 mcg/kg/minute increased by 50 mcg/kg/minute every 2 minutes to a maximum dose of 500 mcg/kg/minute; acutely assess vasodilator response
DOSING: PEDIATRIC
(For additional information see "Adenosine: Pediatric drug information")Paroxysmal supraventricular tachycardia (Adenocard®): Rapid I.V. push (over 1-2 seconds) via peripheral line: Infants and Children (manufacturer's recommendation): Children <50 kg: 0.05-0.1 mg/kg. If conversion of PSVT does not occur within 1-2 minutes, may increase dose by 0.05-0.1 mg/kg. May repeat until sinus rhythm is established or to a maximum single dose of 0.3 mg/kg or 12 mg. Follow each dose with normal saline flush. Children 50 kg: Refer to adult dosing.
Pediatric advanced life support (PALS): Treatment of SVT: I.V., I.O.: 0.1 mg/kg; if not effective, administer 0.2 mg/kg; maximum single dose: 12 mg. Follow each dose with normal saline flush.
DOSING: ELDERLY — Refer to adult dosing. Elderly may be more sensitive to effects of adenosine.
DOSING: RENAL IMPAIRMENT Hemodialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Peritoneal dialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Note: Higher doses may be needed for administration via peripheral versus central vein.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For rapid bolus I.V. use only; administer I.V. push over 1-2 seconds at a peripheral I.V. site as proximal as possible to trunk (not in lower arm, hand, lower leg, or foot); follow each bolus with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via central line at lower doses (eg, adults initial dose: 3 mg)
COMPATIBILITY — Stable in D5LR, D5W, LR, NS.
USE Adenocard®: Treatment of paroxysmal supraventricular tachycardia (PSVT) including that associated with accessory bypass tracts (Wolff-Parkinson-White syndrome); when clinically advisable, appropriate vagal maneuvers should be attempted prior to adenosine administration; not effective in atrial flutter, atrial fibrillation, or ventricular tachycardia
Adenoscan®: Pharmacologic stress agent used in myocardial perfusion thallium-201 scintigraphy
USE - UNLABELED / INVESTIGATIONAL — Adenoscan®: Acute vasodilator testing in pulmonary artery hypertension
ADVERSE REACTIONS SIGNIFICANT — Note: Frequency varies based on use; higher frequency of infusion-related effects, such as flushing and lightheadedness, were reported with continuous infusion (Adenoscan®).
>10%: Cardiovascular: Facial flushing (18% to 44%) Central nervous system: Headache (2% to 18%), lightheadedness (2% to 12%) Neuromuscular & skeletal: Discomfort of neck, throat, jaw (<1% to 15%) Respiratory: Dyspnea (12% to 28%), chest pressure/discomfort (7% to 40%)
1% to 10%: Cardiovascular: Hypotension (<1% to 2%), AV block (infusion 6%; third degree <1%), ST segment depression (3%), palpitation, chest pain Central nervous system: Dizziness, nervousness (2%), apprehension Gastrointestinal: Nausea (3%) Neuromuscular & skeletal: Upper extremity discomfort (up to 4%), numbness (up to 2%), paresthesia (up to 2%) Respiratory: Hyperventilation Miscellaneous: Diaphoresis
<1% (Limited to important or life-threatening): Asystole (prolonged), atrial fibrillation, back discomfort, bradycardia, bronchospasm, blurred vision, burning sensation, hypertension (transient), injection site reaction, intracranial pressure increased, metallic taste, pressure in groin, respiratory arrest, seizure, torsade de pointes, ventricular fibrillation, ventricular tachycardia
CONTRAINDICATIONS — Hypersensitivity to adenosine or any component of the formulation; second- or third-degree AV block or sick sinus syndrome (except in patients with a functioning artificial pacemaker), atrial flutter, atrial fibrillation, and ventricular tachycardia (this drug is not effective in converting these arrhythmias to sinus rhythm). The manufacturer states that Adenoscan® should be avoided in patients with known or suspected bronchoconstrictive or bronchospastic lung disease.
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Atrial fibrillation/flutter: There have been reports of atrial fibrillation/flutter in patients with paroxysmal supraventricular tachycardia (PSVT) associated with accessory conduction pathways after adenosine. Does not convert afib/flutter to normal sinus rhythm; risk of serious arrhythmias/hypotension. Not for use in patients with afib/flutter associated with Wolff-Parkinson-White Syndrome. Conduction disturbances: Adenosine decreases conduction through the AV node and may produce first-, second-, or third-degree heart block. Patients with pre-existing S-A nodal dysfunction may experience prolonged sinus pauses after adenosine; use caution in patients with first-degree AV block or bundle branch block; avoid use of adenosine for pharmacologic stress testing in patients with high-grade AV block or sinus node dysfunction (unless a functional pacemaker is in place). Rare, prolonged episodes of asystole have been reported, with fatal outcomes in some cases. Hypotension: May produce profound vasodilation with subsequent hypotension. When used as a bolus dose (PSVT), effects are generally self-limiting (due to the short half-life of adenosine). However, when used as a continuous infusion (pharmacologic stress testing), effects may be more pronounced and persistent, corresponding to continued exposure. Use infusions with caution in patients with autonomic dysfunction, carotid stenosis (with cerebrovascular insufficiency), uncorrected hypovolemia, pericarditis, pleural effusion and/or stenotic valvular heart disease. Proarrhythmic effects: Watch for proarrhythmic effects; monitor and adjust dose to prevent QTc prolongation.
Disease-related concerns: Asthma: A limited number of patients with asthma have received adenosine and have not experienced exacerbation of their asthma. Adenosine may cause bronchoconstriction in patients with asthma; should be used cautiously in patients with obstructive lung disease not associated with bronchoconstriction (eg, emphysema, bronchitis). Electrolyte imbalance: Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy.
Concurrent drug therapy issues: Caffeine: Pharmacologic stress testing: Withhold for five half-lives prior to adenosine use; avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing. Drugs which slow AV conduction: Use with caution in patients receiving other drugs which slow AV conduction (eg, digoxin, verapamil). Theophylline: Withhold for five half-lives prior to adenosine use whenever possible (eg, pharmacological stress testing).
Special populations: Elderly: Use with caution in the elderly; may be at increased risk of hemodynamic effects, bradycardia, and/or AV block.
Dosage form specific issues: Adenocard®: Transient AV block is expected. When used in PSVT, at the time of conversion to normal sinus rhythm, a variety of new rhythms may appear on the ECG. Administer as a rapid bolus, either directly into a vein or (if administered into an I.V. line), as close to the patient as possible (followed by saline flush).
Other warnings/precautions: CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, nonlife-threatening ventricular arrhythmias did not benefit and may have been harmed by attempts to suppress the arrhythmia with flecainide or encainide. An increased mortality or nonfatal cardiac arrest rate (7.7%) was seen in the active treatment group compared with patients in the placebo group (3%). The applicability of the CAST results to other populations is unknown. Antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmias.
DRUG INTERACTIONS Carbamazepine may increase heart block.
Dipyridamole potentiates effects of adenosine; reduce dose of adenosine.
Theophylline and caffeine (methylxanthines) antagonize adenosine's effects; may require increased dose of adenosine.
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Avoid food or drugs with caffeine. Adenosine's therapeutic effect may be decreased if used concurrently with caffeine. Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reports of administration during pregnancy have indicated no adverse effects on fetus or newborn attributable to adenosine.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
MONITORING PARAMETERS — ECG monitoring, heart rate, blood pressure
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Since the half-life of adenosine is <10 seconds, any adverse effects are rapidly self-limiting. Intoxication is usually short-lived since the half-life of the drug is very short. Treatment of prolonged effects requires individualization. Theophylline and other methylxanthines are competitive inhibitors of adenosine and may have a role in reversing its toxic effects. To reverse the effects of Adenoscan®, administer theophylline 50-125 mg slow I.V. push.
CANADIAN BRAND NAMES — Adenocard®; Adenoscan®; Adenosine Injection, USP
INTERNATIONAL BRAND NAMES — Adenocard (BR, CA); Adenocor (AU, BE, BG, CN, CZ, DK, EC, EE, EG, ES, FI, GB, HU, IE, IL, KR, MY, NO, NZ, PE, PL, TH, TW, UY, VE, ZA); Adenocur (NL); Adenoject (IN); Adenoscan (CA, HK); Adenosin Ebewe (PL); Adenosina Biol (AR, PY); Adenosine Injection, USP (CA); Adrekar (AT, DE); Cardiovert (PH); Fosfobion (PL); Krenosin (FR, IT, MX); Krenosine (CH); Soladen (PL)
MECHANISM OF ACTION — Slows conduction time through the AV node, interrupting the re-entry pathways through the AV node, restoring normal sinus rhythm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: Very brief
Metabolism: Blood and tissue to inosine then to adenosine monophosphate (AMP) and hypoxanthine
Half-life elimination: <10 seconds
Adenosine
U.S. BRAND NAMES — Adenocard®; Adenoscan®
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IVDiagnostic Agent
DOSING: ADULTS Paroxysmal supraventricular tachycardia (Adenocard®): I.V. (rapid - over 1-2 seconds, via peripheral line): 6 mg; if not effective within 1-2 minutes, 12 mg may be given; may repeat 12 mg bolus if needed; maximum single dose: 12 mg. Follow each I.V. bolus of adenosine with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via a central line at lower doses (ie, initial adult dose: 3 mg).
Pharmacologic stress agent (Adenoscan®): I.V.: Continuous I.V. infusion via peripheral line: 140 mcg/kg/minute for 6 minutes using syringe or columetric infusion pump; total dose: 0.84 mg/kg. Thallium-201 is injected at midpoint (3 minutes) of infusion.
Acute vasodilator testing (unlabeled use) (Adenoscan®): I.V.: Initial: 50 mcg/kg/minute increased by 50 mcg/kg/minute every 2 minutes to a maximum dose of 500 mcg/kg/minute; acutely assess vasodilator response
DOSING: PEDIATRIC
(For additional information see "Adenosine: Pediatric drug information")Paroxysmal supraventricular tachycardia (Adenocard®): Rapid I.V. push (over 1-2 seconds) via peripheral line: Infants and Children (manufacturer's recommendation): Children <50 kg: 0.05-0.1 mg/kg. If conversion of PSVT does not occur within 1-2 minutes, may increase dose by 0.05-0.1 mg/kg. May repeat until sinus rhythm is established or to a maximum single dose of 0.3 mg/kg or 12 mg. Follow each dose with normal saline flush. Children 50 kg: Refer to adult dosing.
Pediatric advanced life support (PALS): Treatment of SVT: I.V., I.O.: 0.1 mg/kg; if not effective, administer 0.2 mg/kg; maximum single dose: 12 mg. Follow each dose with normal saline flush.
DOSING: ELDERLY — Refer to adult dosing. Elderly may be more sensitive to effects of adenosine.
DOSING: RENAL IMPAIRMENT Hemodialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Peritoneal dialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Note: Higher doses may be needed for administration via peripheral versus central vein.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For rapid bolus I.V. use only; administer I.V. push over 1-2 seconds at a peripheral I.V. site as proximal as possible to trunk (not in lower arm, hand, lower leg, or foot); follow each bolus with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via central line at lower doses (eg, adults initial dose: 3 mg)
COMPATIBILITY — Stable in D5LR, D5W, LR, NS.
USE Adenocard®: Treatment of paroxysmal supraventricular tachycardia (PSVT) including that associated with accessory bypass tracts (Wolff-Parkinson-White syndrome); when clinically advisable, appropriate vagal maneuvers should be attempted prior to adenosine administration; not effective in atrial flutter, atrial fibrillation, or ventricular tachycardia
Adenoscan®: Pharmacologic stress agent used in myocardial perfusion thallium-201 scintigraphy
USE - UNLABELED / INVESTIGATIONAL — Adenoscan®: Acute vasodilator testing in pulmonary artery hypertension
ADVERSE REACTIONS SIGNIFICANT — Note: Frequency varies based on use; higher frequency of infusion-related effects, such as flushing and lightheadedness, were reported with continuous infusion (Adenoscan®).
>10%: Cardiovascular: Facial flushing (18% to 44%) Central nervous system: Headache (2% to 18%), lightheadedness (2% to 12%) Neuromuscular & skeletal: Discomfort of neck, throat, jaw (<1% to 15%) Respiratory: Dyspnea (12% to 28%), chest pressure/discomfort (7% to 40%)
1% to 10%: Cardiovascular: Hypotension (<1% to 2%), AV block (infusion 6%; third degree <1%), ST segment depression (3%), palpitation, chest pain Central nervous system: Dizziness, nervousness (2%), apprehension Gastrointestinal: Nausea (3%) Neuromuscular & skeletal: Upper extremity discomfort (up to 4%), numbness (up to 2%), paresthesia (up to 2%) Respiratory: Hyperventilation Miscellaneous: Diaphoresis
<1% (Limited to important or life-threatening): Asystole (prolonged), atrial fibrillation, back discomfort, bradycardia, bronchospasm, blurred vision, burning sensation, hypertension (transient), injection site reaction, intracranial pressure increased, metallic taste, pressure in groin, respiratory arrest, seizure, torsade de pointes, ventricular fibrillation, ventricular tachycardia
CONTRAINDICATIONS — Hypersensitivity to adenosine or any component of the formulation; second- or third-degree AV block or sick sinus syndrome (except in patients with a functioning artificial pacemaker), atrial flutter, atrial fibrillation, and ventricular tachycardia (this drug is not effective in converting these arrhythmias to sinus rhythm). The manufacturer states that Adenoscan® should be avoided in patients with known or suspected bronchoconstrictive or bronchospastic lung disease.
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Atrial fibrillation/flutter: There have been reports of atrial fibrillation/flutter in patients with paroxysmal supraventricular tachycardia (PSVT) associated with accessory conduction pathways after adenosine. Does not convert afib/flutter to normal sinus rhythm; risk of serious arrhythmias/hypotension. Not for use in patients with afib/flutter associated with Wolff-Parkinson-White Syndrome. Conduction disturbances: Adenosine decreases conduction through the AV node and may produce first-, second-, or third-degree heart block. Patients with pre-existing S-A nodal dysfunction may experience prolonged sinus pauses after adenosine; use caution in patients with first-degree AV block or bundle branch block; avoid use of adenosine for pharmacologic stress testing in patients with high-grade AV block or sinus node dysfunction (unless a functional pacemaker is in place). Rare, prolonged episodes of asystole have been reported, with fatal outcomes in some cases. Hypotension: May produce profound vasodilation with subsequent hypotension. When used as a bolus dose (PSVT), effects are generally self-limiting (due to the short half-life of adenosine). However, when used as a continuous infusion (pharmacologic stress testing), effects may be more pronounced and persistent, corresponding to continued exposure. Use infusions with caution in patients with autonomic dysfunction, carotid stenosis (with cerebrovascular insufficiency), uncorrected hypovolemia, pericarditis, pleural effusion and/or stenotic valvular heart disease. Proarrhythmic effects: Watch for proarrhythmic effects; monitor and adjust dose to prevent QTc prolongation.
Disease-related concerns: Asthma: A limited number of patients with asthma have received adenosine and have not experienced exacerbation of their asthma. Adenosine may cause bronchoconstriction in patients with asthma; should be used cautiously in patients with obstructive lung disease not associated with bronchoconstriction (eg, emphysema, bronchitis). Electrolyte imbalance: Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy.
Concurrent drug therapy issues: Caffeine: Pharmacologic stress testing: Withhold for five half-lives prior to adenosine use; avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing. Drugs which slow AV conduction: Use with caution in patients receiving other drugs which slow AV conduction (eg, digoxin, verapamil). Theophylline: Withhold for five half-lives prior to adenosine use whenever possible (eg, pharmacological stress testing).
Special populations: Elderly: Use with caution in the elderly; may be at increased risk of hemodynamic effects, bradycardia, and/or AV block.
Dosage form specific issues: Adenocard®: Transient AV block is expected. When used in PSVT, at the time of conversion to normal sinus rhythm, a variety of new rhythms may appear on the ECG. Administer as a rapid bolus, either directly into a vein or (if administered into an I.V. line), as close to the patient as possible (followed by saline flush).
Other warnings/precautions: CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, nonlife-threatening ventricular arrhythmias did not benefit and may have been harmed by attempts to suppress the arrhythmia with flecainide or encainide. An increased mortality or nonfatal cardiac arrest rate (7.7%) was seen in the active treatment group compared with patients in the placebo group (3%). The applicability of the CAST results to other populations is unknown. Antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmias.
DRUG INTERACTIONS Carbamazepine may increase heart block.
Dipyridamole potentiates effects of adenosine; reduce dose of adenosine.
Theophylline and caffeine (methylxanthines) antagonize adenosine's effects; may require increased dose of adenosine.
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Avoid food or drugs with caffeine. Adenosine's therapeutic effect may be decreased if used concurrently with caffeine. Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reports of administration during pregnancy have indicated no adverse effects on fetus or newborn attributable to adenosine.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
MONITORING PARAMETERS — ECG monitoring, heart rate, blood pressure
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Since the half-life of adenosine is <10 seconds, any adverse effects are rapidly self-limiting. Intoxication is usually short-lived since the half-life of the drug is very short. Treatment of prolonged effects requires individualization. Theophylline and other methylxanthines are competitive inhibitors of adenosine and may have a role in reversing its toxic effects. To reverse the effects of Adenoscan®, administer theophylline 50-125 mg slow I.V. push.
CANADIAN BRAND NAMES — Adenocard®; Adenoscan®; Adenosine Injection, USP
INTERNATIONAL BRAND NAMES — Adenocard (BR, CA); Adenocor (AU, BE, BG, CN, CZ, DK, EC, EE, EG, ES, FI, GB, HU, IE, IL, KR, MY, NO, NZ, PE, PL, TH, TW, UY, VE, ZA); Adenocur (NL); Adenoject (IN); Adenoscan (CA, HK); Adenosin Ebewe (PL); Adenosina Biol (AR, PY); Adenosine Injection, USP (CA); Adrekar (AT, DE); Cardiovert (PH); Fosfobion (PL); Krenosin (FR, IT, MX); Krenosine (CH); Soladen (PL)
MECHANISM OF ACTION — Slows conduction time through the AV node, interrupting the re-entry pathways through the AV node, restoring normal sinus rhythm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: Very brief
Metabolism: Blood and tissue to inosine then to adenosine monophosphate (AMP) and hypoxanthine
Half-life elimination: <10 seconds
PHARMACOLOGIC CATEGORY Antiarrhythmic Agent, Class IVDiagnostic Agent
DOSING: ADULTS Paroxysmal supraventricular tachycardia (Adenocard®): I.V. (rapid - over 1-2 seconds, via peripheral line): 6 mg; if not effective within 1-2 minutes, 12 mg may be given; may repeat 12 mg bolus if needed; maximum single dose: 12 mg. Follow each I.V. bolus of adenosine with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via a central line at lower doses (ie, initial adult dose: 3 mg).
Pharmacologic stress agent (Adenoscan®): I.V.: Continuous I.V. infusion via peripheral line: 140 mcg/kg/minute for 6 minutes using syringe or columetric infusion pump; total dose: 0.84 mg/kg. Thallium-201 is injected at midpoint (3 minutes) of infusion.
Acute vasodilator testing (unlabeled use) (Adenoscan®): I.V.: Initial: 50 mcg/kg/minute increased by 50 mcg/kg/minute every 2 minutes to a maximum dose of 500 mcg/kg/minute; acutely assess vasodilator response
DOSING: PEDIATRIC
(For additional information see "Adenosine: Pediatric drug information")Paroxysmal supraventricular tachycardia (Adenocard®): Rapid I.V. push (over 1-2 seconds) via peripheral line: Infants and Children (manufacturer's recommendation): Children <50 kg: 0.05-0.1 mg/kg. If conversion of PSVT does not occur within 1-2 minutes, may increase dose by 0.05-0.1 mg/kg. May repeat until sinus rhythm is established or to a maximum single dose of 0.3 mg/kg or 12 mg. Follow each dose with normal saline flush. Children 50 kg: Refer to adult dosing.
Pediatric advanced life support (PALS): Treatment of SVT: I.V., I.O.: 0.1 mg/kg; if not effective, administer 0.2 mg/kg; maximum single dose: 12 mg. Follow each dose with normal saline flush.
DOSING: ELDERLY — Refer to adult dosing. Elderly may be more sensitive to effects of adenosine.
DOSING: RENAL IMPAIRMENT Hemodialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Peritoneal dialysis: Significant drug removal is unlikely based on physiochemical characteristics.
Note: Higher doses may be needed for administration via peripheral versus central vein.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
DOSAGE FORMS: CONCISE Injection, solution [preservative free]: 3 mg/mL (2 mL, 4 mL) Adenocard®: 3 mg/mL (2 mL, 4 mL) Adenoscan®: 3 mg/mL (20 mL, 30 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For rapid bolus I.V. use only; administer I.V. push over 1-2 seconds at a peripheral I.V. site as proximal as possible to trunk (not in lower arm, hand, lower leg, or foot); follow each bolus with normal saline flush. Note: Preliminary results in adults suggest adenosine may be administered via central line at lower doses (eg, adults initial dose: 3 mg)
COMPATIBILITY — Stable in D5LR, D5W, LR, NS.
USE Adenocard®: Treatment of paroxysmal supraventricular tachycardia (PSVT) including that associated with accessory bypass tracts (Wolff-Parkinson-White syndrome); when clinically advisable, appropriate vagal maneuvers should be attempted prior to adenosine administration; not effective in atrial flutter, atrial fibrillation, or ventricular tachycardia
Adenoscan®: Pharmacologic stress agent used in myocardial perfusion thallium-201 scintigraphy
USE - UNLABELED / INVESTIGATIONAL — Adenoscan®: Acute vasodilator testing in pulmonary artery hypertension
ADVERSE REACTIONS SIGNIFICANT — Note: Frequency varies based on use; higher frequency of infusion-related effects, such as flushing and lightheadedness, were reported with continuous infusion (Adenoscan®).
>10%: Cardiovascular: Facial flushing (18% to 44%) Central nervous system: Headache (2% to 18%), lightheadedness (2% to 12%) Neuromuscular & skeletal: Discomfort of neck, throat, jaw (<1% to 15%) Respiratory: Dyspnea (12% to 28%), chest pressure/discomfort (7% to 40%)
1% to 10%: Cardiovascular: Hypotension (<1% to 2%), AV block (infusion 6%; third degree <1%), ST segment depression (3%), palpitation, chest pain Central nervous system: Dizziness, nervousness (2%), apprehension Gastrointestinal: Nausea (3%) Neuromuscular & skeletal: Upper extremity discomfort (up to 4%), numbness (up to 2%), paresthesia (up to 2%) Respiratory: Hyperventilation Miscellaneous: Diaphoresis
<1% (Limited to important or life-threatening): Asystole (prolonged), atrial fibrillation, back discomfort, bradycardia, bronchospasm, blurred vision, burning sensation, hypertension (transient), injection site reaction, intracranial pressure increased, metallic taste, pressure in groin, respiratory arrest, seizure, torsade de pointes, ventricular fibrillation, ventricular tachycardia
CONTRAINDICATIONS — Hypersensitivity to adenosine or any component of the formulation; second- or third-degree AV block or sick sinus syndrome (except in patients with a functioning artificial pacemaker), atrial flutter, atrial fibrillation, and ventricular tachycardia (this drug is not effective in converting these arrhythmias to sinus rhythm). The manufacturer states that Adenoscan® should be avoided in patients with known or suspected bronchoconstrictive or bronchospastic lung disease.
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Atrial fibrillation/flutter: There have been reports of atrial fibrillation/flutter in patients with paroxysmal supraventricular tachycardia (PSVT) associated with accessory conduction pathways after adenosine. Does not convert afib/flutter to normal sinus rhythm; risk of serious arrhythmias/hypotension. Not for use in patients with afib/flutter associated with Wolff-Parkinson-White Syndrome. Conduction disturbances: Adenosine decreases conduction through the AV node and may produce first-, second-, or third-degree heart block. Patients with pre-existing S-A nodal dysfunction may experience prolonged sinus pauses after adenosine; use caution in patients with first-degree AV block or bundle branch block; avoid use of adenosine for pharmacologic stress testing in patients with high-grade AV block or sinus node dysfunction (unless a functional pacemaker is in place). Rare, prolonged episodes of asystole have been reported, with fatal outcomes in some cases. Hypotension: May produce profound vasodilation with subsequent hypotension. When used as a bolus dose (PSVT), effects are generally self-limiting (due to the short half-life of adenosine). However, when used as a continuous infusion (pharmacologic stress testing), effects may be more pronounced and persistent, corresponding to continued exposure. Use infusions with caution in patients with autonomic dysfunction, carotid stenosis (with cerebrovascular insufficiency), uncorrected hypovolemia, pericarditis, pleural effusion and/or stenotic valvular heart disease. Proarrhythmic effects: Watch for proarrhythmic effects; monitor and adjust dose to prevent QTc prolongation.
Disease-related concerns: Asthma: A limited number of patients with asthma have received adenosine and have not experienced exacerbation of their asthma. Adenosine may cause bronchoconstriction in patients with asthma; should be used cautiously in patients with obstructive lung disease not associated with bronchoconstriction (eg, emphysema, bronchitis). Electrolyte imbalance: Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy.
Concurrent drug therapy issues: Caffeine: Pharmacologic stress testing: Withhold for five half-lives prior to adenosine use; avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing. Drugs which slow AV conduction: Use with caution in patients receiving other drugs which slow AV conduction (eg, digoxin, verapamil). Theophylline: Withhold for five half-lives prior to adenosine use whenever possible (eg, pharmacological stress testing).
Special populations: Elderly: Use with caution in the elderly; may be at increased risk of hemodynamic effects, bradycardia, and/or AV block.
Dosage form specific issues: Adenocard®: Transient AV block is expected. When used in PSVT, at the time of conversion to normal sinus rhythm, a variety of new rhythms may appear on the ECG. Administer as a rapid bolus, either directly into a vein or (if administered into an I.V. line), as close to the patient as possible (followed by saline flush).
Other warnings/precautions: CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, nonlife-threatening ventricular arrhythmias did not benefit and may have been harmed by attempts to suppress the arrhythmia with flecainide or encainide. An increased mortality or nonfatal cardiac arrest rate (7.7%) was seen in the active treatment group compared with patients in the placebo group (3%). The applicability of the CAST results to other populations is unknown. Antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmias.
DRUG INTERACTIONS Carbamazepine may increase heart block.
Dipyridamole potentiates effects of adenosine; reduce dose of adenosine.
Theophylline and caffeine (methylxanthines) antagonize adenosine's effects; may require increased dose of adenosine.
ETHANOL / NUTRITION / HERB INTERACTIONS — Food: Avoid food or drugs with caffeine. Adenosine's therapeutic effect may be decreased if used concurrently with caffeine. Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reports of administration during pregnancy have indicated no adverse effects on fetus or newborn attributable to adenosine.
LACTATION — Excretion in breast milk unknown
DIETARY CONSIDERATIONS — Avoid dietary caffeine for 12-24 hours prior to pharmacologic stress testing.
MONITORING PARAMETERS — ECG monitoring, heart rate, blood pressure
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Since the half-life of adenosine is <10 seconds, any adverse effects are rapidly self-limiting. Intoxication is usually short-lived since the half-life of the drug is very short. Treatment of prolonged effects requires individualization. Theophylline and other methylxanthines are competitive inhibitors of adenosine and may have a role in reversing its toxic effects. To reverse the effects of Adenoscan®, administer theophylline 50-125 mg slow I.V. push.
CANADIAN BRAND NAMES — Adenocard®; Adenoscan®; Adenosine Injection, USP
INTERNATIONAL BRAND NAMES — Adenocard (BR, CA); Adenocor (AU, BE, BG, CN, CZ, DK, EC, EE, EG, ES, FI, GB, HU, IE, IL, KR, MY, NO, NZ, PE, PL, TH, TW, UY, VE, ZA); Adenocur (NL); Adenoject (IN); Adenoscan (CA, HK); Adenosin Ebewe (PL); Adenosina Biol (AR, PY); Adenosine Injection, USP (CA); Adrekar (AT, DE); Cardiovert (PH); Fosfobion (PL); Krenosin (FR, IT, MX); Krenosine (CH); Soladen (PL)
MECHANISM OF ACTION — Slows conduction time through the AV node, interrupting the re-entry pathways through the AV node, restoring normal sinus rhythm
PHARMACODYNAMICS / KINETICS Onset of action: Rapid
Duration: Very brief
Metabolism: Blood and tissue to inosine then to adenosine monophosphate (AMP) and hypoxanthine
Half-life elimination: <10 seconds
Monday, January 21, 2008
RADI ENEMA Lisko
RADI ENEMA Lisko
Contents: Liq: Per 120ml: Sodium biphosphate 19.2gm, sodium phosphate 7.2gm, sodium contents in 120ml 4.5gm.
Regn.No:Pack:Trade Prices:Retail Prices:
Enema(010012): 120ml: 18.70:22.00.
Contents: Liq: Per 120ml: Sodium biphosphate 19.2gm, sodium phosphate 7.2gm, sodium contents in 120ml 4.5gm.
Regn.No:Pack:Trade Prices:Retail Prices:
Enema(010012): 120ml: 18.70:22.00.
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