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albuterol sulfate Proventil, Proventil HFA, Proventil Repetabs, Proventil Syrup, Ventolin, Ventolin HFA, Ventolin Syrup, Volmax
Pharmacologic classification: adrenergic Therapeutic classification: bronchodilator Pregnancy risk category C
Available forms Available by prescription only Aerosol inhaler: 90 mcg/metered spray Capsules for inhalation: 200 mcg microfine Solution for nebulization: 0.083%, 0.5% Syrup: 2 mg/5 ml Tablets: 2 mg, 4 mg Tablets (sustained-release): 4 mg, 8 mg
Indications and dosages
Bronchospasm in patients with reversible obstructive airway disease. Adults and children age 12 and older: 2 to 4 mg (immediate-release tablets) P.O. t.i.d. or q.i.d.; maximum dose, 8 mg q.i.d. Or, use sustained-release tablets.
Usual starting dose is 4 mg q 12 hours. Increase to 8 mg q 12 hours if patient fails to respond. Cautiously increase in stepwise
manner as needed and tolerated to 16 mg q 12 hours. Don’t exceed 32 mg daily. Oral solution Children ages 6 to 14: 2 mg P.O. t.i.d. to q.i.d.; may increase to 24 mg daily in divided doses. Aerosol solution Adults and children age 4 and older: One to two inhalations q 4 to 6 hours. More frequent administration or a greater number of inhalations isn’t usually recommended.
However, because deposition of inhaled medications is variable, higher doses are occasionally used, especially in patients
with acute bronchospasm. Solution for inhalation Adults: 2.5 mg t.i.d. or q.i.d. by nebulizer. Children ages 2 to 12: 0.1 mg/kg to 0.15 mg/kg to maximum of 2.5 mg t.i.d. to q.i.d. Capsules for inhalation Adults and children age 4 and older: 200 mcg inhaled q 4 to 6 hours using a Rotahaler inhalation device. Children ages 6 to 11: Administer 2 mg P.O. t.i.d. or q.i.d. or 4 mg extended-release preparation q 12 hours. Children ages 2 to 5: Administer 0.1 mg/kg P.O. t.i.d., not to exceed 2 mg t.i.d. ≡ Dosage adjustment. For adults older than age 65, give 2 mg P.O. t.i.d. or q.i.d.
To prevent exercise-induced bronchospasm. Adults and children age 4 and older: Two inhalations 15 minutes before exercise or 200 mcg (1 capsule) inhaled via the Rotahaler delivery device 15 minutes before
exercise.
Pharmacodynamics Bronchodilator action: Selectively stimulates beta-adrenergic receptors of the lungs, uterus, and vascular smooth muscle. Bronchodilation results
from relaxation of bronchial smooth muscles, which relieves bronchospasm and reduces airway resistance.
Pharmacokinetics Absorption: After oral inhalation, appears to be absorbed gradually, over several hours, from the respiratory tract; however, dose is
mostly swallowed and absorbed through the GI tract. Distribution: Doesn’t cross the blood-brain barrier. Metabolism: Extensively metabolized in the liver to inactive compounds. Excretion: Rapidly excreted in urine and feces. After oral inhalation, 70% of dose is excreted in urine unchanged and as metabolites
within 24 hours; 10% in feces. Elimination half-life is about 4 hours. After oral administration, 75% of dose is excreted
in urine within 72 hours as metabolites; 4% in feces.
| Route |
Onset |
Peak |
Duration |
| P.O. |
15-30 min |
2-3 hr |
6-12 hr
|
| Inhalation |
5-15 min |
1/2-2 hr |
2-6 hr
|
|
Contraindications and precautions Contraindicated in patients hypersensitive to drug or any component of its formulation. Use cautiously in patients with CV
disorders, including coronary insufficiency and hypertension; in patients with hyperthyroidism or diabetes mellitus; and in
those who are unusually responsive to adrenergics.
Interactions Drug-drug. Epinephrin, other orally inhaled sympathomimetic amines: May increase sympathomimetic effects and risk of toxicity. Avoid use together. MAO inhibitors, tricyclic antidepressants: Serious CV effects may follow use. Avoid use together. Propranolol, other beta blockers: May antagonize effects of albuterol. Use together cautiously.
Adverse reactions CNS: tremor, nervousness, dizziness, insomnia, headache, hyperactivity, weakness, CNS stimulation, malaise, hypesthesia, migraine, hypertonia. CV: tachycardia, palpitations, hypertension. EENT: dry and irritated nose and throat (with inhaled form), nasal congestion, epistaxis, hoarseness. GI: increased appetite, heartburn, nausea, vomiting, anorexia, taste perversion. Metabolic: hypokalemia with large doses. Musculoskeletal: muscle cramps. Respiratory: bronchospasm, cough, wheezing, dyspnea, bronchitis, increased sputum. Other: hypersensitivity reactions.
Effects on lab test results May decrease potassium level.
Overdose and treatment Signs and symptoms of overdose include exaggeration of common adverse reactions, particularly angina, hypertension, hypokalemia,
and seizures. Cardiac arrest may occur. To treat, use selective beta blockers (such as metoprolol) with extreme caution; they may induce asthmatic attack. Dialysis
isn’t appropriate. Monitor vital signs and electrolyte levels closely.
Special considerations Orally inhaled albuterol has been used investigationally to prevent or alleviate episodes of muscle paralysis in the treatment
of some patients with hyperkalemic familial periodic paralysis. Small, transient increases in blood glucose level may occur after oral inhalation. Serum potassium level may decrease after I.V. and inhalation therapy administration, but potassium supplementation is usually
unnecessary. Effectiveness of treatment is measured by periodic monitoring of patient’s pulmonary function. Monitor patient for worsening
symptoms or loss of control.
ALERT Don’t confuse Flomax (tamsulosin) 0.4 mg with Volmax (albuterol) 4 mg. These drugs sound and look alike. Pregnant patients Cleft palate and limb defects can occur; however, there’s no consistent pattern of congenital abnormalities. Breast-feeding patients Because it’s unknown if albuterol appears in breast milk, alternative feeding methods are recommended. Pediatric patients Safety and efficacy of extended-release tablets or immediate-release tablets in children younger than age 6 haven’t been established.
Geriatric patients Lower doses may be required because geriatric patients are more sensitive to sympathomimetic amines.
Patient education Instruct patient in proper use of inhaler. Tell him to read directions before use, that dryness of mouth and throat may occur,
and that rinsing with water after each dose may help. To administer by metered-dose nebulizer, give patient these instructions: Shake canister thoroughly to activate it, and place
the mouthpiece well into mouth, aimed at back of throat. Close lips and teeth around mouthpiece, exhale through nose as completely
as possible, and then inhale through mouth slowly and deeply while actuating the nebulizer to release a dose. Hold breath
10 seconds (count "1-100, 2-100, 3-100," until reaching "10-100"). Remove the mouthpiece and exhale slowly. To administer by metered powder inhaler, caution patient not to take forced deep breath, but to breathe with normal force
and depth. Observe patient closely for exaggerated systemic drug action. To administer by oxygen aerosolization, give over 15 to 20 minutes with oxygen flow rate adjusted to 4 L/minute. Turn on oxygen
supply before patient places nebulizer in mouth. Lips don’t have to be closed tightly around nebulizer opening. Placement
of Y tube in rubber tubing permits patient to control administration. Advise patient to rinse mouth immediately after inhalation
therapy to help prevent dryness and throat irritation. Rinse mouthpiece thoroughly with warm running water at least once daily
to prevent clogging (it isn’t dishwasher-safe.) After cleaning, wait until mouthpiece is completely dry before storing. Don’t
place near artificial heat, such as a dishwasher or oven. Replace reservoir bag every 2 to 3 weeks or as needed; replace mouthpiece
every 6 to 9 months or as needed. Note: Replacement of bags or mouthpieces may require a prescription. Advise patient that repeated use may result in paradoxical bronchospasm. In such a case, patient should discontinue drug and
call immediately. Tell patient to report if troubled breathing persists 1 hour after using medication, if symptoms return within 4 hours, if
condition worsens, or if new (refill) canister is needed within 2 weeks. Advise patient to wait 15 minutes after using inhaled albuterol before using adrenocorticoids (beclomethasone, dexamethasone,
flunisolide, or triamcinolone). Warn patient to use only as directed and not to use more than prescribed amount or more often than prescribed.
Reactions may be common, uncommon, life-threatening, or
COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use
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