Albuterol, AccuNeb,ProAir HFA,Proventil HFA,Proventil,Ventolin HF, VoSpire ER

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")