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Albuterol

Pronunciation

Pronunciation: al-BUE-ter-ol
Class: Sympathomimetic, bronchodilator

Trade Names

AccuNeb
- Solution, inhalation 0.021% (0.63 mg per 3 mL)

Albuterol
- Aerosol, inhalation 90 mcg per actuation
- Solution, inhalation, oral 0.083% (2.5 mg per 3 mL)
- Solution, inhalation, oral 0.5% (2.5 mg per 0.5 mL)
- Syrup, oral 2 mg per 5 mL
- Tablets, oral 2 mg
- Tablets, oral 4 mg

ProAir HFA
- Aerosol, inhalation 90 mcg per actuation

Proventil HFA
- Aerosol, inhalation 90 mcg per actuation

Ventolin HFA
- Aerosol, inhalation 90 mcg per actuation

VoSpire
- Tablets, ER, oral 4 mg
- Tablets, ER, oral 8 mg

Airomir (Canada)
Apo-Salvent (Canada)
Apo-Salvent CFC Free (Canada)
Gen-Salbutamol Respirator Solution (Canada)
Gen-Salbutamol Sterinebs P.F. (Canada)
ratio-Salbutamol HFA (Canada)
Sandoz Salbutamol (Canada)
Ventolin Diskus (Canada)
Ventolin Oral Liquid (Canada)

Pharmacology

Produces bronchodilation by relaxing bronchial smooth muscle through beta-2 receptor stimulation.

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Pharmacokinetics

Absorption

Tablets

Rapidly absorbed; T max is 2 h; C max is approximately 18 ng/mL. Food reduces the rate of absorption of the ER tablets.

Aerosol

T max is 0.17 (chlorofluorocarbon [CFC]–propelled); 0.42 h (hydrofluoroalkane [HFA]).

Inhalation solution

Less than 20% absorbed; T max is 0.5 h; C max is 2.1 ng/mL.

Metabolism

Metabolized in the GI tract by SULTIA3 (sulfotransferase).

Elimination

Half-life is 4.6 to 6 h. 76% is recovered in the urine over 3 days with 60% as metabolites (oral); 80% to 100% is renally excreted (inhalation); 4% and less than 20% is excreted in feces (oral and inhalation, respectively).

Duration

6 h (syrup); 8 h (immediate-release tablets); 12 h (ER tablets).

Special Populations

Renal Function Impairment

67% decline in albuterol Cl in patients with CrCl 7 to 53 mL/min.

Hepatic Function Impairment

No studies have been conducted.

Elderly

No studies have been conducted.

Children

Reduced bioavailability after single-dose ER oral administration; no studies have been conducted in neonates.

Indications and Usage

Prevention and treatment of reversible bronchospasm associated with asthma and other obstructive pulmonary diseases; acute attacks of bronchospasm (0.5% and 0.083% inhalation solution only); prevention of exercise-induced bronchospasm (aerosol only).

Unlabeled Uses

Adjunctive treatment of hyperkalemia in patients undergoing dialysis.

Contraindications

Hypersensitivity to albuterol or any of its components.

Dosage and Administration

Aerosol
Asthma/Bronchospasm Adults and Children 4 y of age and older

Inhalation 1 to 2 inhalations every 4 to 6 h (max, 12 inhalations per 24 h).

Prevention of exercise-induced bronchospasm Adults and Children 4 y of age and older

Inhalation 2 inhalations 15 to 30 min before exercise.

Inhalation Solution
Asthma/Bronchospasm Adults and Children older than 13 y of age

Inhalation 1 vial (2.5 mg per 3 mL or 2.5 mg per 0.5 mL) 3 to 4 times daily by nebulization over 5 to 15 min (max, 4 vials [10 mg] per 24 h).

Children 2 to 12 y of age (15 kg or more)

Inhalation 1 vial (2.5 mg per 3 mL) 3 to 4 times daily by nebulization over 5 to 15 min (max, 4 vials [10 mg] per 24 h).

Children 2 to 12 y of age (14 kg or less)

Inhalation Use the 0.5% solution 3 to 4 times daily by nebulization over 5 to 15 min (max, 4 vials [10mg] per 24 h).

Children 2 to 12 y of age ( AccuNeb )

Inhalation 1 vial (1.25 or 0.63 mg/vial) 3 to 4 times daily by nebulization over 5 to 15 min (max, 4 vials [5 mg] per 24 h).

Immediate-release tablets
Asthma/Bronchospasm Adults and Children older than 12 y of age

PO 2 to 4 mg 3 to 4 times daily. May be cautiously increased stepwise. Dosages of above 4 mg 4 times daily may be appropriate when patient fails to respond (max, 32 mg/day).

Children 6 to 12 y of age

PO 2 mg 3 to 4 times daily May be cautiously increased stepwise (max, 24 mg/day).

Elderly and those sensitive to beta-adrenergic stimulation

Restrict initial dose to 2 mg 3 or 4 times/day. Individualize dosage thereafter.

ER Tablets
Adults and Children older than 12 y of age

PO 4 to 8 mg every 12 h. May be cautiously increased stepwise (max, 32 mg/day).

Children 6 to 12 y of age

PO 4 mg every 12 h. May be cautiously increased stepwise (max, 24 mg/day).

Syrup
Adults and Children older than 14 y of age

PO 2 or 4 mg (5 to 10 mL) 3 or 4 times daily. May be cautiously increased stepwise (max, 32 mg/day). Dosages of above 4 mg 4 times daily may be appropriate when patient fails to respond.

Children 6 to 14 y of age

PO 2 mg (5 mL) 3 or 4 times daily. May be cautiously increased stepwise (max, 24 mg/day).

Children 2 to 5 y of age

PO Initiate at 0.1 mg/kg 3 times daily. Do not exceed 2 mg 3 times daily initially. Dosage may be increased stepwise to 0.2 mg/kg 3 times daily (max, 12 mg/day).

Elderly and those sensitive to beta-adrenergic stimulation

PO Restrict initial dosage to 2 mg (5 mL) 3 or 4 times/day. Individualize dosage thereafter.

General Advice

  • Aerosol
  • For oral inhalation via meted dose inhaler.
  • Shake well before each spray.
  • Prime the inhaler before using for the first time, when the inhaler has not been used for more than 2 wk, or when the inhaler has been dropped. To prime, release 3 to 4 sprays into the air away from the face, shaking well before each spray.
  • Wash the actuator with warm running water for 30 seconds and dry thoroughly at least once a week. If the actuator becomes blocked with drug, washing the actuator will remove the blockage.
  • The actuator supplied with the aerosol should not be used with any other product canisters, and actuators from other products should not be used with the supplied canister.
  • The correct amount of medication in each canister cannot be ensured after 60 or 200 actuations, depending on the canister size, even though the canister is not completely empty. The canister should be discarded when 60 or 200 actuations have been used or 12 months after removal from the moisture-protective foil pouch, whichever comes first.
  • Ventolin HFA has a dose counter attached to the canister that starts at 64 or 204, depending on the canister size, and counts down each time a spray is released. When the counter reads 000, discard.
  • Continue therapy as medically necessary to control recurring bouts of bronchospasm.
  • Inhalation solution
  • For oral inhalation use via nebulizer. Do not swallow solution.
  • The 0.083% solution and AccuNeb do not require dilution before use.
  • The 0.5% solution (0.5 mL) requires dilution to a total volume of 3 mL of sterile normal saline before use.
  • Deliver via jet nebulizer connected to an air compressor with adequate air flow, equipped with a mouthpiece or suitable face mask, over 5 to 15 min.
  • Compatibility of inhalation solution mixed with other drugs has not been established.
  • The safety and efficacy of AccuNeb have been established using the Pari-LC Plus nebulizer and Pari-PRONEB compressor. The safety and efficacy when administering with other nebulizers have not been established.
  • Continue therapy as medically necessary to control recurring bouts of bronchospasm.
  • Immediate-release and ER tablets
  • ER tablets must be swallowed whole with the aid of liquids. Patients should not crush or chew.
  • Patients currently maintained on immediate-release tablets or syrup can be switched to ER tablets.

Storage/Stability

Syrup/Tablets

Store between 68° and 77°F. Protect from light.

Aerosol

Store between 15° and 25°C (59° and 77°F). Protect from freezing temperatures. Store canister with mouthpiece down. For best results, the canister should be at room temperature before use. Contents under pressure; do not puncture. Do not use or store near heat or open flame. Exposure to temperatures above 48.8°C (120°F) may cause bursting. Never throw container into fire or incinerator.

Inhalation solution

Store between 2° and 25°C (36° and 77°F). Protect from light and excessive heat. Store unit dose vials in protective foil pouch at all times. Once removed from the foil pouch, use within 1 wk. Discard the vial if the solution is not colorless.

Drug Interactions

Beta-blockers

Beta-blockers block the pulmonary effect of albuterol and may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances (eg, as prophylaxis after MI), there may be no acceptable alternatives to the use of beta-blockers in patients with asthma. In this setting, cardioselective beta-blockers (eg, atenolol) could be considered, although they should be administered with caution.

Digoxin

Albuterol may decrease serum digoxin levels. Carefully evaluate the serum digoxin levels and adjust the digoxin dose as needed.

Diuretics (eg, loop diuretics [eg, furosemide], thiazide diuretics [eg, chlorothiazide])

ECG changes and hypokalemia associated with these diuretics may worsen with albuterol coadministration. Caution is advised during coadministration. Monitor potassium levels.

Linezolid, MAOIs (eg, phenelzine), tricyclic antidepressants (amitriptyline)

Administer with extreme caution to patients being treated with these agents or within 2 wk of discontinuation of one of these agents because the action of albuterol on the vascular system may be potentiated. Consider alternative therapy.

Sympathomimetic amines (eg, terbutaline)

Concomitant use is not recommended, since combined use may lead to deleterious cardiovascular effects. This recommendation does not preclude the judicious use of an aerosol bronchodilator of the adrenergic stimulant type in patients receiving albuterol. However, concomitant use should be individualized and not given on a routine basis. If regular coadministration is required, consider alternative therapy.

Theophyllines

Coadministration may produce an augmented bronchodilating response. In addition, theophylline plasma concentrations may be reduced, decreasing the efficacy. Measure theophylline concentrations and monitor the response of the patient. Adjust the theophylline dose as needed.

Adverse Reactions

Cardiovascular

Tachycardia (7%); palpitations (5%); hypertension (1%); arrhythmia (including atrial fibrillation, supraventricular tachycardia, extrasystoles); angina

CNS

Tremor (24%); excitement, nervousness (20%); headache (19%); shakiness (9%); dizziness (7%); hyperkinesia (4%); accidental injury (nervous system), anxiety (less than 3%); hyperactivity, insomnia, migraine, weakness (2%); emotional liability, fatigue (1%); restlessness.

Dermatologic

Skin/appendage infection, urticaria (2%); pallor (1%).

EENT

Rhinitis (22%); inhalation taste sensation, otitis media (4%); ear disorder, ear pain, laryngitis, lung disorder, oropharyngeal edema (less than 3%); conjunctivitis, nasal congestion (1%); dry mouth or oropharynx; oropharynx or throat irritation; vertigo.

GI

Nausea (10%); vomiting (7%); nausea/vomiting (4%); gastroenteritis (3%); diarrhea, glossitis (less than 3%); GI symptoms (2%); dyspepsia (1%); unusual taste.

Hypersensitivity

Allergic reaction (6%); angioedema; bronchospasm; hoarseness; oropharyngeal edema; rash; urticaria.

Musculoskeletal

Musculoskeletal pain (5%); back pain (4%); muscle cramps (3%).

Respiratory

Upper respiratory tract infection (21%); asthma exacerbations (13%); throat irritation (10%); bronchospasm (8%); viral respiratory infection (7%); inhalation site sensation, respiratory disorder unspecified (6%); cough, upper respiratory inflammation (5%); bronchitis (4%); dyspnea (less than 3%); epistaxis, wheezing (1%); paradoxical bronchospasm (postmarketing).

Miscellaneous

Fever (6%); cold symptoms, flu syndrome, increased appetite, lymphadenopathy, UTI (3%); chest pain, infection (less than 3%); anorexia (1%).

Precautions

Pregnancy

Category C .

Lactation

Unknown. Other drugs in the class (eg, terbutaline) are considered compatible with breast-feeding, and albuterol most likely is compatible.

Children

Safety and efficacy not established in children younger than 12 y of age (0.5% inhalation solution); younger than 6 y of age (ER and immediate-release tablets); younger than 4 y of age (aerosol); younger than 2 y of age ( AccuNeb , 0.083% inhalation solution, syrup).

Elderly

Use caution in dose selection and monitor renal function.

Labor and Delivery

May inhibit uterine contractions.

Hypersensitivity

Immediate hypersensitivity reactions may occur (eg, angioedema, bronchospasm, oropharyngeal edema, rash, urticaria). Rarely, erythema multiforme and Steven-Johnson syndrome has occurred in children.

Renal Function

Use caution when administering high doses of albuterol.

Special Risk Patients

Use with caution in convulsive disorders, hyperthyroidism, or diabetes, and in patients unusually unresponsive to sympathicomimetic amines.

CV effects

Clinically significant CV effects may occur. Use with caution in patients with CV disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.

Excessive use

Paradoxical bronchospasm and cardiac arrest have been associated with excessive inhalant use. Fatalities have been reported.

Metabolic effects

May aggravate preexisting diabetes and ketoacidosis and may produce significant hypokalemia.

Tolerance

If previously effective dose fails to provide relief, therapy may need to be reassessed.

Overdosage

Symptoms

Angina, arrhythmias, cardiac arrest, dizziness, dry mouth, fatigue, headache, hypertension or hypotension, hypokalemia, malaise, nausea, nervousness, palpitations, seizures, sleeplessness, tachycardia with rates up to 200 bpm, tremor.

Patient Information

  • Advise patients or their caregivers to not use albuterol more frequently than recommended. Do not increase the dose or frequency of albuterol without consulting a health care provider. If patients find that treatment with albuterol becomes less effective for symptomatic relief, symptoms become worse, and/or they need to use the product more frequently than usual, advise them to seek medical attention immediately.
  • Inform patients that common adverse reactions include chest pain, palpitations, rapid heart rate, and tremor or nervousness.
  • Advise patient to not to chew or crush the ER capsules.
  • Teach patient correct method for using metered-dose inhaler. Have patient demonstrate proper technique, including timing between inhalations.
  • Inform patients to take other inhaled drugs and asthma medications only as directed by their health care provider while using albuterol aerosol.
  • Instruct patients or their caregivers to prime the aerosol inhaler before using the first time and in cases where the inhaler has not been used for more than 2 wk by releasing 3 to 4 test sprays into the air, away from the face.
  • Advise patients or their caregivers to keep the plastic actuator clean to prevent medication build-up and blockage. The actuator should be cleaned (with the canister removed) by running warm water through the top and bottom for 30 sec at least once a week. The actuator must be shaken to remove excess water, then air-dried thoroughly (such as overnight).
  • Advise patients or their caregivers that if the actuator should become blocked (little or no medication coming out of the mouthpiece), the blockage may be removed by washing the actuator.
  • Advise patients or their caregivers to use albuterol aerosol only with the actuator supplied with the product.
  • Advise patients or their caregivers using albuterol via nebulizer that AccuNeb and the 0.083% solution require no dilution before use; the 0.5% solution requires dilution with sterile normal saline solution prior to use.
  • The safety and efficacy of albuterol solution have not been determined when 1 or more drugs are mixed with it in a nebulizer. Advise patients or their caregivers to check with their health care provider before mixing any medications in the nebulizer.

Copyright © 2009 Wolters Kluwer Health.

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