General

Pronunciation:
al-byoo-ter-ole


Trade Name(s)

  • Accuneb
  • Airomir [Canada]
  • Apo-Salvent [Canada]
  • Proair HFA
  • Proventil HFA
  • Salbutamol [Canada]
  • Ventolin HFA
  • Ventolin Diskus [Canada]
  • Ventolin Nebules [Canada]
  • VoSpire ER

Pregnancy Category
Category C

Ther. Class.
bronchodilators

Pharm. Class.
adrenergics

Indications

  • Used as a bronchodilator to control and prevent reversible airway obstruction caused by asthma or COPD.
  • Inhaln: Used as a quick-relief agent for acute bronchospasm and for 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 Effect(s):

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)

ROUTEONSETPEAKDURATION
PO15–30 min2–3 hr4–6 hr or more
PO–ER30 min2–3 hr12 hr
Inhaln5–15 min60–90 min3–6 hr

Contraindication/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: ↑ risk of adverse reactions; may require dose ↓.

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

* CAPITALS indicate life-threatening.
Italics indicate most frequent.

Interactions

Drug-Drug

  • Concurrent use with other adrenergic agents will have ↑ adrenergic side effects.
  • Use with MAO inhibitors may lead to hypertensive crisis.
  • Beta blockers may negate therapeutic effect.
  • May ↓ serum digoxin levels.
  • Cardiovascular effects are potentiated in patients receiving tricyclic antidepressants .
  • Risk of hypokalemia ↑ concurrent use of potassium-losing diuretics .
  • Hypokalemia ↑ the risk of digoxin toxicity.

Drug-Natural Products:

Use with caffeine-containing herbs ( cola nut, guarana , tea, coffee) ↑ 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 be ↑ carefully (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 carefully ↑ as needed (not to exceed 8 mg/day).

PO: (Children 2–6 yr): 0.1 mg/kg 3 times daily (not to exceed 2 mg 3 times daily initially); may be carefully ↑ to 0.2 mg/kg 3 times daily (not to exceed 4 mg 3 times daily).

Inhaln: (Adults and Children ≥4 yr): Via metered-dose inhaler– 2 inhalations q 4–6 hr or 2 inhalations 15 min before exercise (90 mcg/spray); some patients may respond to 1 inhalation. NIH Guidelines for acute asthma exacerbation: Children– 4–8 puffs q 20 min for 3 doses then q 1–4 hr; Adults– 4–8 puffs q 20 min for up to 4 hr then q 1–4 hr prn.

Inhaln: (Adults and Children >12 yr): NIH Guidelines for acute asthma exacerbation via nebulization or IPPB– 2.5–5 mg q 20 min for 3 doses then 2.5–10 mg q 1–4 hr prn; 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) q 20 min for 3 doses then 0.15–0.3 mg/kg (not to exceed 10 mg) q 1–4 hr prn or 1.25 mg 3–4 times daily for children 10–15 kg or 2.5 mg 3–4 times daily for children >15 k g; Continuous nebulization– 0.5–3 mg/kg/hr.

Inhaln: Neonates 1.25 mg/dose q 8 hr via nebulization or 1–2 puffs via MDI into the ventilator circuit q 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/5 mL

Metered-dose aerosol: 90 mcg/inhalation in 6.7-g, 8-g, 8.5-g, and 18-g canisters (200 metered inhalations), 100 mcg/spray [Canada]

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 [Canada], 2 mg/mL [Canada], 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 (Ventolin Diskus): 200 mcg [Canada]

In Combination with: ipratropium (Combivent, DuoNeb). See combination drugs.

Assessment

  • Assess lung sounds, pulse, and BP before administration and during peak of medication. Note amount, color, and character of sputum produced.
  • Monitor pulmonary function tests before initiating therapy and periodically during therapy.
  • Observe for paradoxical bronchospasm (wheezing). If condition occurs, withhold medication and notify health care professional immediately.

Lab Test Considerations:

May cause transient ↓ in serum potassium concentrations with nebulization or higher-than-recommended doses.

Potential Diagnoses

Implementation

  • PO: Administer oral medication with meals to minimize gastric irritation.
    • Extended-release tablets should be swallowed whole; do not break, crush, or chew.
  • Inhaln: Shake inhaler well, and allow at least 1 min between inhalations of aerosol medication. Prime the inhaler before first use by releasing 4 test sprays into the air away from the face. Pedi: Use spacer for children < 8 yr of age.
    • For nebulization or IPPB, the 0.5-, 0.83-, 1-, and 2-mg/mL solutions do not require dilution before administration. The 5 mg/mL (0.5%) solution must be diluted with 1–2.5 mL of 0.9% NaCl for inhalation. Diluted solutions are stable for 24 hr at room temperature or 48 hr if refrigerated.
    • For nebulizer, compressed air or oxygen flow should be 6–10 L/min; a single treatment of 3 mL lasts about 10 min.
    • IPPB usually lasts 5–20 min.

Patient/Family Teaching

  • Instruct patient to take albuterol as directed. If on a scheduled dosing regimen, take missed dose as soon as remembered, spacing remaining doses at regular intervals. Do not double doses or increase the dose or frequency of doses. Caution patient not to exceed recommended dose; may cause adverse effects, paradoxical bronchospasm (more likely with first dose from new canister), or loss of effectiveness of medication.
    • Instruct patient to contact health care professional immediately if shortness of breath is not relieved by medication or is accompanied by diaphoresis, dizziness, palpitations, or chest pain.
    • Instruct patient to prime unit with 4 sprays before using and to discard cannister after 200 sprays. Actuators should not be changed among products.
    • Inform patient that these products contain hydrofluoralkane (HFA) and the propellant and are described as non-CFC or CFC-free (contain no chlorofluorocarbons).
    • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any OTC medications or alcoholic beverages concurrently with this therapy. Caution patient also to avoid smoking and other respiratory irritants.
    • Inform patient that albuterol may cause an unusual or bad taste.
  • Inhaln: Instruct patient in the proper use of the metered-dose inhaler or nebulizer (see medication administration techniques).
    • Advise patients to use albuterol first if using other inhalation medications and allow 5 min to elapse before administering other inhalant medications unless otherwise directed.
    • Advise patient to rinse mouth with water after each inhalation dose to minimize dry mouth and clean the mouthpiece with water at least once a week.
    • Instruct patient to notify health care professional if there is no response to the usual dose or if contents of one canister are used in less than 2 wk. Asthma and treatment regimen should be re-evaluated and corticosteroids should be considered. Need for increased use to treat symptoms indicates decrease in asthma control and need to reevaluate patient's therapy.
  • Pedi: Caution adolescents and their parents about overuse of inhalers, which can cause heart damage and life-threatening arrhythmias.

Evaluation/Desired Outcomes

Prevention or relief of bronchospasm.