DrugindexOnline^{2nd edition}

Pronouncation: (al-BYOO-ter-ahl)
Class: Sympathomimetic

Trade Names:
Airet
- Solution for inhalation 0.083% (as sulfate)

Trade Names:
Proventil
- Tablets 2 mg (as sulfate)
- Tablets 4 mg (as sulfate)
- Syrup 2 mg (as sulfate) per 5 mL
- Aerosol Each actuation delivers 90 mcg albuterol
- Solution for inhalation 0.083% (as sulfate)
- Solution for inhalation 0.5% (as sulfate)

Trade Names:
Proventil HFA
- Aerosol Each actuation delivers 90 mcg albuterol (as sulfate)

Trade Names:
Ventolin
- Tablets 2 mg (as sulfate)
- Tablets 4 mg (as sulfate)
- Syrup 2 mg (as sulfate) per 5 mL
- Solution for inhalation 0.5% (as sulfate)

Trade Names:
Ventolin Nebules
- Solution for inhalation 0.083% (as sulfate)

Trade Names:
Ventolin Rotacaps
- Capsules for inhalation 200 mcg microfine (as sulfate)

Airomir (Canada)
Alti-Salbutamol Sulfate (Canada)
Apo-Salvent (Canada)
Gen-Salbutamol Respirator Solution (Canada)
Gen-Salbutamol Sterinebs P.F. (Canada)
Novo-Salmol (Canada)
Nu-Salbutamol Solution (Canada)
PMS-Salbutamol Respirator Solution (Canada)
ratio-Salbutamol (Canada)
Rho-Salbutamol (Canada)
Rhoxal-salbutamol (Canada)
Ventodisk Disk (Canada)
Ventolin Diskus (Canada)
Ventolin Oral Liquid (Canada)

Mechanism of Action

Pharmacology

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

Pharmacokinetics

Absorption

Tablets

Rapidly absorbed; T _max is 2 h; C _max is about 18 ng/mL.

Inhalation

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

Elimination

T _½ is 5 to 6 h. 76% recovered in urine over 3 days with 60% as metabolites; 4% excreted in feces.

Onset

Oral

Within 30 min.

Inhalation

Within 5 min.

Duration

Oral

4 to 8 h.

Inhalation

3 to 6 h.

Indications and Usage

Prevention and treatment of reversible bronchospasm associated with asthma and other obstructive pulmonary diseases.

Unlabeled Uses

Adjunctive treatment of hyperkalemia in patients undergoing dialysis.

Contraindications

Cardiac tachyarrhythmias.

Dosage and Administration

Inhalation Aerosol
Adults and Children at least 4 yr of age (at least 12 yr for Proventil )

1 to 2 inhalations every 4 to 6 h.

Prevention of exercise-induced bronchospasm

2 inhalations 15 min before exercise.

Inhalation Solution
Adults and children older than 2 yr of age

2.5 mg/dose 3 to 4 times/day by nebulization.

Children 2 to 12 yr of age ( AccuNeb )

1.25 mg or 0.63 mg 3 to 4 times/day by nebulization.

Oral
Adults and Children older than 12 yr of age

PO 2 to 4 mg/dose 3 to 4 times/day. Do not exceed 32 mg/day.

Children 6 to 12 yr of age

PO 2 mg/dose 3 to 4 times/day. Do not exceed 24 mg/day.

Children 2 to 6 yr of age

PO 0.1 to 0.2 mg/kg/dose 3 times/day. Do not exceed 12 mg/day.

Adults and Children older than 12 yr of age, extended-release ( Proventil Repetabs )

PO 4 to 8 mg every 12 h. May be cautiously increased stepwise to a max of 16 mg twice daily (max, 32 mg/day).

Children 6 to 12 yr of age, extended-release ( Proventil Repetabs )

PO 4 every 12 h. May be cautiously increased stepwise to a max of 12 mg twice daily.

Syrup
Adults and Children alder than 12 yr of age

2 or 4 mg (1 to 2 tsp) 3 or 4 times/day. Doses of above 4 mg 4 times/day may be appropriate when patient fails to respond.

Children 6 to 12 yr of age

2 mg (1 tsp) 3 or 4 times/day. Doses of 2 mg 4 times/day may be cautiously increased. Do not exceed 24 mg/day in divided doses.

Children 2 to 6 yr of age

Initiate at 0.1 mg/kg 3 times/day. Dose may be increased 2 mg 3 times/day. Do not exceed 2 mg 3 times/day. Dose may be increased to 0.2 mg/kg 3 times/day, but not to exceed 4 mg 3 times/day.

Elderly and those sensitive to beta-adrenergic stimulation

Restrict initial dose to 2 mg (1 tsp) 3 or 4 times/day. Individualize dosage thereafter.

Storage/Stability

Store at room temperature. Refrigeration of syrup improves palatability.

Drug Interactions

Beta-blockers

Severe bronchospasms may be produced in asthmatic patients taking albuterol.

Digoxin

Albuterol may decrease serum digoxin levels.

Diuretics

ECG changes and hypokalemia associated with these diuretics may worsen with albuterol coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations; tachycardia; elevated BP; chest tightness; angina.

CNS

Tremor; dizziness; hyperactivity; nervousness; headache; insomnia; weakness; drowsiness; restlessness.

EENT

Dry mouth; throat irritation.

GI

Nausea; vomiting; heartburn; diarrhea.

Genitourinary

Urinary retention.

Respiratory

Cough; bronchospasm; wheezing; dyspnea.

Miscellaneous

Flushing; sweating; anorexia; unusual sensory changes.

Precautions

Pregnancy

Category C .

Lactation

Unknown.

Children

Albuterol aerosol and inhalation powder in children younger than 4 yr of age and albuterol solution for inhalation in children younger than 2 yr of age not established.

Labor and Delivery

May inhibit uterine contractions.

CV effects

Toxic symptoms may occur in patients with CV disorders.

CNS effects

CNS stimulation may occur; use cautiously in patients with history of seizures or hyperthyroidism.

Diabetes

Dosage adjustment of insulin or oral hypoglycemic agent may be required.

Excessive use

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

Hypokalemia

Decreases in potassium levels have occurred.

Tolerance

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

Overdosage

Symptoms

Tremor, palpitations, tachycardia, elevated BP, seizures.

Patient Information

• Tell patient not to chew or crush capsules.
• Teach patient correct method for using metered-dose inhaler. Have patient demonstrate proper technique, including timing between inhalations.
• Instruct patient in home monitoring of pulse and BP.
• Advise patient to maintain fluid intake of 2,000 mL/day and to rinse mouth after each complete dose.
• Instruct patient not to use OTC inhalers without consulting health care provider.
• Instruct patient to contact health care provider if symptoms are not relieved by normal dose.
• Tell patient to report adverse reactions or side effects.