albuterol, Accuneb, Airomir, Proair HFA, Proair Respiclick, Proventil HFA, Salbutamol, Ventolin HFA, Ventolin Diskus, Ventolin Nebules, VoSpire ER

 Indications

Treatment or prevention of bronchospasm in asthma or

chronic obstructive pulmonary disease (COPD). Inhaln:

Prevention of exercise-induced bronchospasm.

PO: Used as a long-term control agent in patients with

chronic/persistent bronchospasm.

Action

Binds to beta2-adrenergic receptors in airway smooth

muscle, leading to activation of adenyl cyclase and increased

levels of cyclic-3, 5-adenosine monophosphate

(cAMP). Increases in cAMP activate kinases,

which inhibit the phosphorylation of myosin and decrease

intracellular calcium. Decreased intracellular

calcium relaxes smooth muscle airways. Relaxation of

airway smooth muscle with subsequent bronchodilation.

Relatively selective for beta2 (pulmonary) receptors.

Therapeutic Effects: Bronchodilation.

Pharmacokinetics

Absorption: Well absorbed after oral administration

but rapidly undergoes extensive metabolism.

Distribution: Small amounts appear in breast milk.

Metabolism and Excretion: Extensively metabolized

by the liver and other tissues.

Half-life: Oral 2.7–5 hr; Inhalation: 3.8 hr.

TIME/ACTION PROFILE (bronchodilation)

ROUTE ONSET PEAK DURATION

PO 15–30 min 2–3 hr 4–6 hr or

more

PO–ER 30 min 2–3 hr 12 hr

Inhaln 5–15 min 60–90 min 3–6 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity to adrenergic

amines.

Use Cautiously in: Cardiac disease; Hypertension;

Hyperthyroidism; Diabetes; Glaucoma; Seizure disorders;

Excess inhaler use may lead to tolerance and paradoxical

bronchospasm; OB, Lactation, Pedi: Safety not

established for pregnant women near term, breast-feeding

women, and children 2 yr; Geri:qrisk of adverse

reactions; may require dosep.

Adverse Reactions/Side Effects

CNS: nervousness, restlessness, tremor, headache, insomnia

(Pedi: occurs more frequently in young children

than adults), hyperactivity in children. Resp:

PARADOXICAL BRONCHOSPASM (excessive use of inhalers).

CV: chest pain, palpitations, angina, arrhythmias,

hypertension. GI: nausea, vomiting. Endo: hyperglycemia.

F and E: hypokalemia. Neuro: tremor.

Interactions

Drug-Drug: Concurrent use with other adrenergic

agents will haveqadrenergic side effects. Use with

MAO inhibitors may lead to hypertensive crisis. Beta

blockers may negate therapeutic effect. Maypserum

digoxin levels. Cardiovascular effects are potentiated

in patients receiving tricyclic antidepressants. Risk

of hypokalemiaqconcurrent use of potassium-losing

diuretics. Hypokalemiaqthe risk of digoxin toxicity.

Drug-Natural Products: Use with caffeine-containing

herbs (cola nut, guarana, tea, coffee)q

stimulant effect.

Route/Dosage

PO (Adults and Children 12 yr): 2–4 mg 3–4

times daily (not to exceed 32 mg/day) or 4–8 mg of

extended-release tablets twice daily.

PO (Geriatric Patients): Initial dose should not exceed

2 mg 3–4 times daily, may beqcarefully (up to

32 mg/day).

PO (Children 6–12 yr): 2 mg 3–4 times daily or

0.3–0.6 mg/kg/day as extended-release tablets divided

twice daily; may be carefullyqas needed (not to exceed

8 mg/day). 

PO (Children 2–6 yr): 0.1 mg/kg 3 times daily (not A

to exceed 2 mg 3 times daily initially); may be carefully

qto 0.2 mg/kg 3 times daily (not to exceed 4 mg 3

times daily).

Inhaln (Adults and Children 4 yr): Via metereddose

inhaler or dry powder inhaler—2 inhalations

every 4–6 hr (some patients may respond to 1 inhalation)

or 2 inhalations 15 min before exercise; NIH

Guidelines for acute asthma exacerbation: Children—

4–8 puffs every 20 min for 3 doses then every

1–4 hr; Adults—4–8 puffs every 20 min for up to 4

hr then every 1–4 hr as needed.

Inhaln (Adults and Children 12 yr): NIH Guidelines

for acute asthma exacerbation via nebulization

or IPPB—2.5–5 mg every 20 min for 3 doses

then 2.5–10 mg every 1–4 hr as needed; Continuous

nebulization—10–15 mg/hr.

Inhaln (Children 2–12 yr): NIH Guidelines for

acute asthma exacerbation via nebulization or

IPPB—0.15 mg/kg/dose (minimum dose 2.5 mg)

every 20 min for 3 doses then 0.15–0.3 mg/kg (not to

exceed 10 mg) every 1–4 hr as needed or 1.25 mg 3–

4 times daily for children 10–15 kg or 2.5 mg 3–4

times daily for children 15 kg; Continuous nebulization—

0.5–3 mg/kg/hr.

Inhaln (Neonates): 1.25 mg/dose every 8 hr via nebulization

or 1–2 puffs via MDI into the ventilator circuit

every 6 hrs.

Availability (generic available)

Tablets: 2 mg, 4 mg. Cost: Generic—4 mg $565.87/

100. Extended-release tablets: 4 mg, 8 mg. Oral

syrup (strawberry-flavored): 2 mg/5mL. Metereddose

aerosol: 90 mcg/inhalation in 6.7-g, 8-g, 8.5-g,

and 18-g canisters (200 metered inhalations), 100

mcg/spray. Cost: Proair HFA—$52.53/8.5-g canister;

Proventil HFA—$62.62/6.7-g canister; Ventolin

HFA—$19.08/8-g canister. Inhalation solution:

0.63 mg/3 mL (0.021%), 1.25 mg/3 mL (0.042%), 2.5

mg/3 mL (0.083%), 1 mg/mL, 2 mg/mL, 5 mg/mL

(0.5%). Cost: Generic—2.5 mg/3 mL $40.82/90 mL,

5 mg/mL $51.02/60 mL. Powder for inhalation

(Proair Respiclick): 90 mcg/inhalation (200 metered

inhalations). Powder for inhalation (Ventolin

Diskus): 200 mcg. In combination with: ipratropium

(Combivent). See Appendix B.