U.S. BRAND NAMES — AccuNeb®; ProAir™ HFA; Proventil® HFA; Proventil®; Ventolin® HFA; VoSpire ER®
PHARMACOLOGIC CATEGORY Beta2 Agonist
DOSING: ADULTS Acute treatment of bronchospasm: Inhalation: MDI 90 mcg/puff: 4-8 puffs every 20 minutes for up to 4 hours, then every 1-4 hours as needed Nebulization: 2.5 mg, diluted to a total of 3 mL, 3-4 times/day over 5-15 minutes NIH guidelines: 1.25-5 mg every 4-8 hours
Bronchospasm in ICU patients (acute): Nebulization: 2.5-5 mg every 20 minutes for 3 doses, then 2.5-10 mg every 1-4 hours as needed, or 10-15 mg/hour continuously
Chronic treatment of bronchospasm: Inhalation: MDI 90 mcg/puff: 1-2 inhalations every 4-6 hours; maximum: 12 inhalations/day NIH guidelines: 2 puffs 3-4 times a day as needed; may double dose for mild exacerbations Oral: Regular release: 2-4 mg/dose 3-4 times/day; maximum dose not to exceed 32 mg/day (divided doses) Extended release: 8 mg every 12 hours; maximum dose not to exceed 32 mg/day (divided doses). A 4 mg dose every 12 hours may be sufficient in some patients, such as adults of low body weight.
Prophylaxis of exercise-induced bronchospasm: Inhalation: MDI 90 mcg/puff: 2 puffs 5-30 minutes prior to exercise
DOSING: PEDIATRIC
(For additional information see "Albuterol: Pediatric drug information")Bronchospasm (acute): Inhalation: MDI 90 mcg/puff: Children 12 years: 4-8 puffs every 20 minutes for 3 doses, then every 1-4 hours; spacer/holding-chamber device should be used Children >12 years: Refer to adult dosing. Nebulization: Children 12 years: Solution 0.5%: 0.15 mg/kg (minimum dose: 2.5 mg) every 20 minutes for 3 doses, then 0.15-0.3 mg/kg (up to 10 mg) every 1-4 hours as needed; may also use 0.5 mg/kg/hour by continuous infusion. Continuous nebulized albuterol at 0.3 mg/kg/hour has been used safely in the treatment of severe status asthmaticus in children; continuous nebulized doses of 3 mg/kg/hour +/- 2.2 mg/kg/hour in children whose mean age was 20.7 months resulted in no cardiac toxicity; the optimal dosage for continuous nebulization remains to be determined. Children >12 years: Refer to adult dosing.
Prophylaxis of exercise-induced bronchospasm: Inhalation: MDI 90 mcg/puff: Children 12 years: 1-2 puffs 5 minutes prior to exercise Children >12 years: Refer to adult dosing.
Chronic treatment of bronchospasm: Inhalation: MDI 90 mcg/puff: Children 4 years: Refer to adult dosing. Oral: Children: 2-6 years: 0.1-0.2 mg/kg/dose 3 times/day; maximum dose not to exceed 12 mg/day (divided doses) Children: 6-12 years: 2 mg/dose 3-4 times/day; maximum dose not to exceed 24 mg/day (divided doses) Extended release: 4 mg every 12 hours; maximum dose not to exceed 24 mg/day (divided doses) Children >12 years: Refer to adult dosing. Nebulization: Children 12 years: 0.05 mg/kg every 4-6 hours; minimum dose: 1.25 mg, maximum dose: 2.5 mg 2-12 years: AccuNeb®: 0.63 mg or 1.25 mg 3-4 times/day, as needed, delivered over 5-15 minutes Note: Use of the 0.5% solution should be used for bronchospasm (acute or treatment) in children <15>40 kg, patients with more severe asthma, or children 11-12 years: May respond better with a 1.25 mg dose Children >12 years: Refer to adult dosing.
DOSING: ELDERLY Inhalation: Refer to adult dosing.
Bronchospasm (treatment): Oral: 2 mg 3-4 times/day; maximum: 8 mg 4 times/day
DOSING: RENAL IMPAIRMENT — Not removed by hemodialysis
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Aerosol, for oral inhalation: 90 mcg/metered inhalation (17 g) [200 metered inhalations; contains chlorofluorocarbons] Proventil®: 90 mcg/metered inhalation (17 g) [200 metered inhalations; contains chlorofluorocarbons]
Aerosol, for oral inhalation: ProAir™ HFA: 90 mcg/metered inhalation (8.5 g) [200 metered inhalations; chlorofluorocarbon free] Proventil® HFA: 90 mcg/metered inhalation (6.7 g) [200 metered inhalations; chlorofluorocarbon free] Ventolin® HFA: 90 mcg/metered inhalation (18 g) [200 metered inhalations; chlorofluorocarbon free]
Solution for nebulization: 0.042% (3 mL); 0.083% (3 mL); 0.5% (0.5 mL, 20 mL) AccuNeb® [preservative free]: 0.63 mg/3 mL (3 mL) [0.021%]; 1.25 mg/3 mL (3 mL) [0.042%] Proventil®: 0.083% (3 mL) [preservative free]; 0.5% (20 mL) [contains benzalkonium chloride]
Syrup, as sulfate: 2 mg/5 mL (480 mL)
Tablet: 2 mg, 4 mg
Tablet, extended release: 4 mg, 8 mg VoSpire ER®: 4 mg, 8 mg
DOSAGE FORMS: CONCISE Aerosol, for oral inhalation [contains chlorofluorocarbon]: 90 mcg/metered inhalation (17 g) Proventil®: 90 mcg/metered inhalation (17 g)
Aerosol, for oral inhalation [chlorofluorocarbon free]: 90 mcg/metered inhalation (8.5 g) ProAir™ HFA: 90 mcg/metered inhalation (8.5 g) Proventil® HFA: 90 mcg/metered inhalation (6.7 g) Ventolin® HFA: 90 mcg/metered inhalation (18 g)
Solution for nebulization: 0.042% (3 mL); 0.083% (3 mL); 0.5% (0.5 mL, 20 mL) AccuNeb® [preservative free]: 0.63 mg/3 mL (3 mL) [0.021%]; 1.25 mg/3 mL (3 mL) [0.042%] Proventil®: 0.083% (3 mL) [preservative free]; 0.5% (20 mL) [contains benzalkonium chloride]
Syrup: 2 mg/5 mL
Tablet: 2 mg, 4 mg
Tablet, extended release: 4 mg, 8 mg VoSpire ER™: 4 mg, 8 mg
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION Inhalation: MDI: Shake well before use; prime prior to first use, and whenever inhaler has not been used for >2 weeks or when it has been dropped, by releasing 4 test sprays into the air (away from face)
Oral: Do not crush or chew extended release tablets.
USE — Bronchodilator in reversible airway obstruction due to asthma or COPD; prevention of exercise-induced bronchospasm
ADVERSE REACTIONS SIGNIFICANT — Incidence of adverse effects is dependent upon age of patient, dose, and route of administration.
Cardiovascular: Angina, atrial fibrillation, chest discomfort, extrasystoles, flushing, hypertension, palpitation, tachycardia
Central nervous system: CNS stimulation, dizziness, drowsiness, headache, insomnia, irritability, lightheadedness, migraine, nervousness, nightmares, restlessness, sleeplessness, tremor
Dermatologic: Angioedema, erythema multiforme, rash, Stevens-Johnson syndrome, urticaria
Endocrine & metabolic: Hypokalemia, serum glucose increased, serum potassium decreased
Gastrointestinal: Diarrhea, dry mouth, gastroenteritis, nausea, unusual taste, vomiting, tooth discoloration
Genitourinary: Micturition difficulty
Neuromuscular & skeletal: Muscle cramps, weakness
Otic: Otitis media, vertigo
Respiratory: Asthma exacerbation, bronchospasm, cough, epistaxis, laryngitis, oropharyngeal drying/irritation, oropharyngeal edema
Miscellaneous: Allergic reaction, lymphadenopathy
CONTRAINDICATIONS — Hypersensitivity to albuterol, adrenergic amines, or any component of the formulation
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Bronchospasm: Rarely, paradoxical bronchospasm may occur with use of inhaled bronchodilating agents; this should be distinguished from inadequate response. Hypersensitivity reactions: Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm) have been reported. Serious effects/fatalities: Do not exceed recommended dose; serious adverse events, including fatalities, have been associated with excessive use of inhaled sympathomimetics.
Disease-related concerns: Asthma: Appropriate use: Optimize anti-inflammatory treatment before initiating maintenance treatment with albuterol. Do not use as a component of chronic therapy without an anti-inflammatory agent. Only the mildest forms of asthma (Step 1 and/or exercise-induced) would not require concurrent use based upon asthma guidelines. Cardiovascular disease: Use with caution in patients with cardiovascular disease (arrhythmia or hypertension or CHF); beta-agonists may cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation. Beta2-agonists may also increase risk of arrhythmias. Diabetes: Use with caution in patients with diabetes mellitus; beta2-agonists may increase serum glucose. Glaucoma: Use with caution in patients with glaucoma; may elevate intraocular pressure. Hyperthyroidism: Use with caution in hyperthyroidism; may stimulate thyroid activity. Hypokalemia: Use with caution in patients with hypokalemia; beta2-agonists may decrease serum potassium. Seizures: Use with caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation.
Special populations: Elderly: Because of its minimal effect on beta1-receptors and its relatively long duration of action, albuterol is a rational choice in the elderly when an inhaled beta-agonist is indicated; oral use should be avoided in the elderly due to adverse effects. Pediatrics: Face masks should be used in children <4 years of age.
Dosage form specific issues: Chlorofluorocarbons: Patient response may vary between inhalers that contain chlorofluorocarbons and those which are chlorofluorocarbon-free.
Other warnings/precautions: Patient information: Patients must be instructed to seek medical attention in cases where acute symptoms are not relieved or a previous level of response is diminished. The need to increase frequency of use may indicate deterioration of asthma, and treatment must not be delayed. All patients should utilize a spacer device when using a metered-dose inhaler.
DRUG INTERACTIONS — Substrate of CYP3A4 (major)
Beta-adrenergic blockers (eg, propranolol) antagonize albuterol's effects; avoid concurrent use.
CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of albuterol. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
Halothane may increase risk of malignant arrhythmias; avoid concurrent use.
Inhaled ipratropium may increase duration of bronchodilation.
MAO inhibitors may increase side effects; monitor heart rate and blood pressure.
TCAs may increase side effects; monitor heart rate and blood pressure.
Sympathomimetics may increase side effects; monitor heart rate and blood pressure.
ETHANOL / NUTRITION / HERB INTERACTIONS Food: Avoid or limit caffeine (may cause CNS stimulation).
Herb/Nutraceutical: Avoid ephedra, yohimbe (may cause CNS stimulation).
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Albuterol crosses the placenta; tocolytic effects, fetal tachycardia, fetal hypoglycemia secondary to maternal hyperglycemia with oral or intravenous routes reported. Available evidence suggests safe use during pregnancy.
LACTATION — Excretion in breast milk unknown/use caution
DIETARY CONSIDERATIONS — Oral forms should be administered with water 1 hour before or 2 hours after meals.
PRICING — (data from drugstore.com)Aerosol solution (ProAir HFA) 108 mcg/ACT (8.5): $34.99
Aerosol solution (Proventil) 90 mcg/ACT (17): $38.10
Aerosol solution (Proventil HFA) 108 mcg/ACT (6.7): $39.61
Nebulization (AccuNeb) 0.63 mg/3 mL (75): $44.99 1.25 mg/3 mL (75): $44.99
Nebulization (Albuterol Sulfate) (2.5 MG/3ML) 0.083% (75): $18.99 (5 MG/ML) 0.5% (20): $15.99
Tablet, 12-hour (VoSpire ER) 4 mg (30): $40.39 8 mg (60): $148.22
Tablets (Albuterol Sulfate) 2 mg (60): $15.99 4 mg (60): $11.99
MONITORING PARAMETERS — FEV1, peak flow, and/or other pulmonary function tests; blood pressure, heart rate; CNS stimulation; serum glucose, serum potassium; asthma symptoms; arterial or capillary blood gases (if patients condition warrants)
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include tachycardia, tremor, hypertension, angina, and seizures. Hypokalemia also may occur. Cardiac arrest and death may be associated with abuse of beta-agonist bronchodilators. Treatment includes immediate discontinuation and symptomatic and supportive therapies. Cautious use of beta-adrenergic blocking agents may be considered in severe cases.
CANADIAN BRAND NAMES — Airomir; Alti-Salbutamol; Apo-Salvent® CFC Free; Apo-Salvent® Respirator Solution; Apo-Salvent® Sterules; Apo-Salvent®; Gen-Salbutamol; PMS-Salbutamol; ratio-Inspra-Sal; ratio-Salbutamol; Rhoxal-salbutamol; Salbu-2; Salbu-4; Ventolin® Diskus; Ventolin® HFA; Ventolin®; Ventrodisk
INTERNATIONAL BRAND NAMES — Aerolin (BR, CL, GR); Airomir (AU, CA, FR, HK, MY, PL, TH, TW, UY); Almotex (PH); Alti-Salbutamol (CA); Apo-Salvent (CA); Apo-Salvent CFC Free (CA); Apo-Salvent Respirator Solution (CA); Apo-Salvent Sterules (CA); Asmacaire (PH); Asmadil (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, SC, SD, SL, SN, TZ, UG, ZM, ZW); Asmalin Pulmoneb (PH); Asmatol (AR); Asmidon (JP); Asmol CFC-Free (AU); Asmol Uni-Dose (NZ); Asmovent (MY); Assal (MX); Asthalin (IN); Azmasol (SG); Bronchosol (TH); Broncovaleas (IT); Bronter (CO); Brytolin (PH); Butahale (SG); Butamol (AU); Buto-Asma (ES, SG, TH); Butotal (CL); Buventol (SG, TW); Buventol Easyhaler (FR, ID, TH); Cletal (PH); Cybutol (HK, ID); Easyhaler Salbutamol (GB, IE); Emplusal (PH); Epaq Inhaler (AU); Farcolin (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Gen-Salbutamol (CA); Glisend (ID); Hivent DS (PH); Krosalburol (EC); Libretin (PH); Medolin (SG); Mozal (TW); PMS-Salbutamol (CA); Provexel NS (PH); Pulmol-S (PE); ratio-Inspra-Sal (CA); ratio-Salbutamol (CA); Respax (NZ); Rhoxal-salbutamol (CA); Salamol (PL); Salbetol (IN); Salbron (ID); Salbu-2 (CA); Salbu-4 (CA); Salbumed (PH); Salbutalan (MX); Salbutamol (PL); Salbutan (VE); Salbutin (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Salbutol (KR, PE); Salbutron SR (KR); Salbuven (ID); Salbuvent (NO); Salbuvent® (PL); Salda (TH); Salden (EC); Salmaplon (IN); Salmol (CN); Salmundin Retard (DE); Salomol (TW); Sedalin (PH); Solia (TH); Steri-Neb Salamol (PL); Sultanol (AT, DE, JP); Suprasma (ID); Teoden (BR); Tobybron (ID); Venalax (PH); Venetlin (JP); Ventilan (CO, PT); Ventilastin Novolizer (DE, FR); Ventimax (ZA); Ventodisk (PL); Ventodisks (CN); Ventol (AE, BH, CY, EG, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Ventolin [tabs./sol./sir.] (PL); Ventolin (AE, AN, AR, AU, BB, BE, BF, BG, BH, BJ, BM, BS, BZ, CA, CH, CI, CN, CR, CY, CZ, EC, EE, EG, ES, ET, GH, GM, GN, GT, GY, HK, HN, HR, HU, ID, IE, IL, IQ, IR, IT, JM, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, MY, NE, NG, NI, NL, NZ, OM, PA, PE, PH, PK, PL, PY, QA, SA, SC, SD, SL, SN, SR, SV, SY, TH, TT, TW, TZ, UG, UY, VE, YE, ZA, ZM, ZW); Ventolin CFC-Free (AU); Ventolin Diskus (CA); Ventolin HFA (CA); Ventoline (DK, FI, FR, NO, SE); Ventrodisk (CA); Volmax (AE, BH, CN, CY, EC, EG, HK, IQ, IR, JO, KW, LB, LY, NZ, OM, QA, SA, SY, YE); Zenmolin (AE, BH, CY, EG, HK, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE); Zibil (MX)
MECHANISM OF ACTION — Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate
PHARMACODYNAMICS / KINETICS Onset of action: Peak effect: Nebulization/oral inhalation: 0.5-2 hours CFC-propelled albuterol: 10 minutes Ventolin® HFA: 25 minutes Oral: 2-3 hours
Duration: Nebulization/oral inhalation: 3-4 hours; Oral: 4-6 hours
Metabolism: Hepatic to an inactive sulfate
Half-life elimination: Inhalation: 3.8 hours; Oral: 3.7-5 hours
Excretion: Urine (30% as unchanged drug)
PATIENT INFORMATION — Do not exceed recommended dosage. Rinse mouth with water following each inhalation to help with dry throat and mouth. Follow specific instructions accompanying inhaler; if more than one inhalation is necessary, wait at least 1 full minute between inhalations. May cause nervousness, restlessness, insomnia; if these effects continue after dosage reduction, notify prescriber. Also report palpitations, tachycardia, chest pain, muscle tremors, dizziness, headache, flushing, or if breathing difficulty persists.
(For additional information see "Albuterol: Patient drug information")
Sunday, March 2, 2008
Albumin,Albumarc,Albuminar,AlbuRx,Albutein,Buminate,Flexbumin,Plasbumin
U.S. BRAND NAMES — Albumarc®; Albuminar®; AlbuRx™; Albutein®; Buminate®; Flexbumin; Plasbumin®
PHARMACOLOGIC CATEGORY Blood Product DerivativePlasma Volume Expander, Colloid
DOSING: ADULTS Note: Use 5% solution in hypovolemic patients or intravascularly-depleted patients. Use 25% solution in patients in whom fluid and sodium intake is restricted.
Usual dose: 25 g; initial dose may be repeated in 15-30 minutes if response is inadequate; no more than 250 g should be administered within 48 hours.
Hypoproteinemia: I.V.: 0.5-1 g/kg/dose; repeat every 1-2 days as calculated to replace ongoing losses.
Hypovolemia: 5% albumin: 0.5-1 g/kg/dose; repeat as needed. Note: May be considered after inadequate response to crystalloid therapy and when nonprotein colloids are contraindicated. The volume administered and the speed of infusion should be adapted to individual response.
DOSING: PEDIATRIC
(For additional information see "Albumin: Pediatric drug information")Note:5% should be used in hypovolemic patients or intravascularly-depleted patients. 25% should be used in patients in whom fluid and sodium intake must be minimized.
Dose depends on condition of patient: Hypovolemia: I.V.: 0.5-1 g/kg/dose (10-20 mL/kg/dose of albumin 5%); maximum dose: 6 g/kg/day
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free; human]: Albuminar®: 5% [50 mg/mL] (50 mL, 250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 1 mEq/L; packaging contains dry natural rubber]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 1 mEq/L; packaging contains dry natural rubber] AlbuRx™: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Albutein®: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Buminate®: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L; packaging contains dry natural rubber]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L; packaging contains dry natural rubber] Flexbumin: 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 and potassium 2 mEq/L] Human Albumin Grifols®: 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Plasbumin®: 5% [50 mg/mL] (50 mL, 250 mL) [contains sodium ~145 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium ~145 mEq/L and potassium 2 mEq/L]
DOSAGE FORMS: CONCISE Injection, solution [preservative free; human]: Albuminar®: 5% [50 mg/mL] (50 mL, 250 mL, 500 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) AlbuRx™: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (50 mL, 100 mL) Albutein®: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (50 mL, 100 mL) Buminate®: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) Flexbumin: 25% [250 mg/mL] (50 mL, 100 mL) Human Albumin Grifols®: 25% [250 mg/mL] (50 mL, 100 mL) Plasbumin®: 5% [50 mg/mL] (50 mL, 250 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For I.V. administration only. Use within 4 hours after opening vial; discard unused portion. In emergencies, may administer as rapidly as necessary to improve clinical condition. After initial volume replacement: 5%: Do not exceed 2-4 mL/minute in patients with normal plasma volume; 5-10 mL/minute in patients with hypoproteinemia 25%: Do not exceed 1 mL/minute in patients with normal plasma volume; 2-3 mL/minute in patients with hypoproteinemia
Do not dilute 5% solution. Rapid infusion may cause vascular overload. Albumin 25% may be given undiluted or diluted in normal saline. May give in combination or through the same administration set as saline or carbohydrates. Do not use with ethanol or protein hydrolysates, precipitation may form.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS; incompatible with sterile water.
Y-site administration: Compatible: Diltiazem, lorazepam. Incompatible: Midazolam, vancomycin, verapamil.
Compatibility when admixed: Compatible: TPN. Incompatible: Verapamil.
USE — Plasma volume expansion and maintenance of cardiac output in the treatment of certain types of shock or impending shock; may be useful for burn patients, ARDS, and cardiopulmonary bypass; other uses considered by some investigators (but not proven) are retroperitoneal surgery, peritonitis, and ascites; unless the condition responsible for hypoproteinemia can be corrected, albumin can provide only symptomatic relief or supportive treatment
USE - UNLABELED / INVESTIGATIONAL — In cirrhotics, administered with diuretics to help facilitate diuresis; large volume paracentesis; volume expansion in dehydrated, mildly-hypotensive cirrhotics
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: CHF precipitation, edema, hyper-/hypotension, hypervolemia, tachycardia
Central nervous system: Chills, fever, headache
Dermatologic: Pruritus, rash, urticaria
Gastrointestinal: Nausea, vomiting
Respiratory: Bronchospasm, pulmonary edema
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to albumin or any component of the formulation; patients with severe anemia or cardiac failure
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Hypervolemia: All patients should be observed for signs of hypervolemia such as pulmonary edema; monitor closely with rapid infusions.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment; protein load may exacerbate or precipitate encephalopathy. Renal impairment: Use with caution in patients with renal impairment; protein load may precipitate azotemia.
Special populations: Preterm infants: Avoid 25% concentration in preterm infants due to risk of intraventricular hemorrhage. Sodium restricted patients: Use with caution in those patients for whom sodium restriction is necessary.
Other warnings/precautions: Nutritional supplementation: Is not an appropriate indication for albumin.
DRUG INTERACTIONS — ACE inhibitors: May have increased risk of atypical reactions; withhold ACEIs for at least 24 hours prior to plasma exchanges using large volumes of albumin
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Excretion in breast milk unknown/compatible
DIETARY CONSIDERATIONS Albumarc®, Albuminar®, Albutein®, Buminate®, Flexbumin: 5% [50 mg/mL] and 25% [250 mg/mL] contain sodium 130-160 mEq/L
Plasbumin®: 5% [50 mg/mL] and 25% [250 mg/mL] contain sodium ~145 mEq/L
MONITORING PARAMETERS — Blood pressure, pulmonary edema, hematocrit
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include hypervolemia, congestive heart failure, and pulmonary edema.
CANADIAN BRAND NAMES — Plasbumin®-25; Plasbumin®-5
INTERNATIONAL BRAND NAMES — Albapure (ID, TW); Albital (EC); Albotein (IT); Albuman (PE); Albumer (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, PH, SC, SD, SL, SN, TH, TZ, UG, ZM, ZW); Albumex (AU, NZ); Albumin 5% (CH); Albumin 5% Human (DE); Albumin Human Salzarm 25% (DE); Albumina Humana (BR); Albuminar (BR, IL); Albuminar-25 (TW); Albuminar-5 (TW); Albuminate (ID); Alburaas (TH); Albutein 25% (BR, HK); Biseko 5% (CH); Buminate 25% (HK); Human Albumin "SSI" (DK); Human Albumin (AT, PL); Human Albumin 25% (DE); Human Albumin 5% (CZ, DE); Humanalbumin 5% (AT); Makroalbumina (PL); Octalbin (FI, ID); Plasbumin (ID); Plasbumin-25 (CA); Plasbumin-5 (CA); Probialbumin (MX); Seralbumin (CO, CR, DO, GT, HN, NI, PA, SV); SRK (CH); Taninal (PL); Tanninum albuminatum (PL); Vialebex (FR)
MECHANISM OF ACTION — Provides increase in intravascular oncotic pressure and causes mobilization of fluids from interstitial into intravascular space
PHARMACOLOGIC CATEGORY Blood Product DerivativePlasma Volume Expander, Colloid
DOSING: ADULTS Note: Use 5% solution in hypovolemic patients or intravascularly-depleted patients. Use 25% solution in patients in whom fluid and sodium intake is restricted.
Usual dose: 25 g; initial dose may be repeated in 15-30 minutes if response is inadequate; no more than 250 g should be administered within 48 hours.
Hypoproteinemia: I.V.: 0.5-1 g/kg/dose; repeat every 1-2 days as calculated to replace ongoing losses.
Hypovolemia: 5% albumin: 0.5-1 g/kg/dose; repeat as needed. Note: May be considered after inadequate response to crystalloid therapy and when nonprotein colloids are contraindicated. The volume administered and the speed of infusion should be adapted to individual response.
DOSING: PEDIATRIC
(For additional information see "Albumin: Pediatric drug information")Note:5% should be used in hypovolemic patients or intravascularly-depleted patients. 25% should be used in patients in whom fluid and sodium intake must be minimized.
Dose depends on condition of patient: Hypovolemia: I.V.: 0.5-1 g/kg/dose (10-20 mL/kg/dose of albumin 5%); maximum dose: 6 g/kg/day
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, solution [preservative free; human]: Albuminar®: 5% [50 mg/mL] (50 mL, 250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 1 mEq/L; packaging contains dry natural rubber]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 1 mEq/L; packaging contains dry natural rubber] AlbuRx™: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Albutein®: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Buminate®: 5% [50 mg/mL] (250 mL, 500 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L; packaging contains dry natural rubber]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L; packaging contains dry natural rubber] Flexbumin: 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 and potassium 2 mEq/L] Human Albumin Grifols®: 25% [250 mg/mL] (50 mL, 100 mL) [contains sodium 130-160 mEq/L and potassium 2 mEq/L] Plasbumin®: 5% [50 mg/mL] (50 mL, 250 mL) [contains sodium ~145 mEq/L and potassium 2 mEq/L]; 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) [contains sodium ~145 mEq/L and potassium 2 mEq/L]
DOSAGE FORMS: CONCISE Injection, solution [preservative free; human]: Albuminar®: 5% [50 mg/mL] (50 mL, 250 mL, 500 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) AlbuRx™: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (50 mL, 100 mL) Albutein®: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (50 mL, 100 mL) Buminate®: 5% [50 mg/mL] (250 mL, 500 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL) Flexbumin: 25% [250 mg/mL] (50 mL, 100 mL) Human Albumin Grifols®: 25% [250 mg/mL] (50 mL, 100 mL) Plasbumin®: 5% [50 mg/mL] (50 mL, 250 mL); 25% [250 mg/mL] (20 mL, 50 mL, 100 mL)
GENERIC EQUIVALENT AVAILABLE — Yes
ADMINISTRATION — For I.V. administration only. Use within 4 hours after opening vial; discard unused portion. In emergencies, may administer as rapidly as necessary to improve clinical condition. After initial volume replacement: 5%: Do not exceed 2-4 mL/minute in patients with normal plasma volume; 5-10 mL/minute in patients with hypoproteinemia 25%: Do not exceed 1 mL/minute in patients with normal plasma volume; 2-3 mL/minute in patients with hypoproteinemia
Do not dilute 5% solution. Rapid infusion may cause vascular overload. Albumin 25% may be given undiluted or diluted in normal saline. May give in combination or through the same administration set as saline or carbohydrates. Do not use with ethanol or protein hydrolysates, precipitation may form.
COMPATIBILITY — Stable in dextran 6% in D5W, dextran 6% in NS, D5LR, D5NS, D51/2NS, D51/4NS, D5W, D10W, LR, NS, 1/2NS; incompatible with sterile water.
Y-site administration: Compatible: Diltiazem, lorazepam. Incompatible: Midazolam, vancomycin, verapamil.
Compatibility when admixed: Compatible: TPN. Incompatible: Verapamil.
USE — Plasma volume expansion and maintenance of cardiac output in the treatment of certain types of shock or impending shock; may be useful for burn patients, ARDS, and cardiopulmonary bypass; other uses considered by some investigators (but not proven) are retroperitoneal surgery, peritonitis, and ascites; unless the condition responsible for hypoproteinemia can be corrected, albumin can provide only symptomatic relief or supportive treatment
USE - UNLABELED / INVESTIGATIONAL — In cirrhotics, administered with diuretics to help facilitate diuresis; large volume paracentesis; volume expansion in dehydrated, mildly-hypotensive cirrhotics
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: CHF precipitation, edema, hyper-/hypotension, hypervolemia, tachycardia
Central nervous system: Chills, fever, headache
Dermatologic: Pruritus, rash, urticaria
Gastrointestinal: Nausea, vomiting
Respiratory: Bronchospasm, pulmonary edema
Miscellaneous: Anaphylaxis
CONTRAINDICATIONS — Hypersensitivity to albumin or any component of the formulation; patients with severe anemia or cardiac failure
WARNINGS / PRECAUTIONS Concerns related to adverse effects: Hypervolemia: All patients should be observed for signs of hypervolemia such as pulmonary edema; monitor closely with rapid infusions.
Disease-related concerns: Hepatic impairment: Use with caution in patients with hepatic impairment; protein load may exacerbate or precipitate encephalopathy. Renal impairment: Use with caution in patients with renal impairment; protein load may precipitate azotemia.
Special populations: Preterm infants: Avoid 25% concentration in preterm infants due to risk of intraventricular hemorrhage. Sodium restricted patients: Use with caution in those patients for whom sodium restriction is necessary.
Other warnings/precautions: Nutritional supplementation: Is not an appropriate indication for albumin.
DRUG INTERACTIONS — ACE inhibitors: May have increased risk of atypical reactions; withhold ACEIs for at least 24 hours prior to plasma exchanges using large volumes of albumin
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Excretion in breast milk unknown/compatible
DIETARY CONSIDERATIONS Albumarc®, Albuminar®, Albutein®, Buminate®, Flexbumin: 5% [50 mg/mL] and 25% [250 mg/mL] contain sodium 130-160 mEq/L
Plasbumin®: 5% [50 mg/mL] and 25% [250 mg/mL] contain sodium ~145 mEq/L
MONITORING PARAMETERS — Blood pressure, pulmonary edema, hematocrit
TOXICOLOGY / OVERDOSE COMPREHENSIVE — Symptoms include hypervolemia, congestive heart failure, and pulmonary edema.
CANADIAN BRAND NAMES — Plasbumin®-25; Plasbumin®-5
INTERNATIONAL BRAND NAMES — Albapure (ID, TW); Albital (EC); Albotein (IT); Albuman (PE); Albumer (BF, BJ, CI, ET, GH, GM, GN, KE, LR, MA, ML, MR, MU, MW, NE, NG, PH, SC, SD, SL, SN, TH, TZ, UG, ZM, ZW); Albumex (AU, NZ); Albumin 5% (CH); Albumin 5% Human (DE); Albumin Human Salzarm 25% (DE); Albumina Humana (BR); Albuminar (BR, IL); Albuminar-25 (TW); Albuminar-5 (TW); Albuminate (ID); Alburaas (TH); Albutein 25% (BR, HK); Biseko 5% (CH); Buminate 25% (HK); Human Albumin "SSI" (DK); Human Albumin (AT, PL); Human Albumin 25% (DE); Human Albumin 5% (CZ, DE); Humanalbumin 5% (AT); Makroalbumina (PL); Octalbin (FI, ID); Plasbumin (ID); Plasbumin-25 (CA); Plasbumin-5 (CA); Probialbumin (MX); Seralbumin (CO, CR, DO, GT, HN, NI, PA, SV); SRK (CH); Taninal (PL); Tanninum albuminatum (PL); Vialebex (FR)
MECHANISM OF ACTION — Provides increase in intravascular oncotic pressure and causes mobilization of fluids from interstitial into intravascular space
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)
Use of UpToDate is subje
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)
Use of UpToDate is subje
Adenosine,Adenocard,Adenoscan
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
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