albuterol

General

Pronunciation:
al-byoo-ter-ole


albuterol

albuterol

Trade Name(s)

  • Accuneb
  • Airomir Canadian Tradename
  • Proair Digihaler
  • Proair HFA
  • Proair Respiclick
  • Proventil HFA
  • Salbutamol Canadian Tradename
  • Ventolin HFA
  • Ventolin Diskus Canadian Tradename
  • Ventolin Nebules Canadian Tradename
  • VoSpire ER

Ther. Class.
bronchodilators

Pharm. Class.
adrenergics

Indications

  • Treatment or prevention of bronchospasm in asthma or chronic obstructive pulmonary disease (COPD).
  • Inhaln Prevention of exercise-induced bronchospasm.
  • PO Treatment of bronchospasm in asthma or COPD.

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
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:   Use during pregnancy only if potential maternal benefit justifies potential fetal risk
  • Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
  • Pedi:   Children <2 yr (safety and effectiveness not established)
  • Geri:  ↑ risk of adverse reactions in older adults; may require dose ↓.

Adverse Reactions/Side Effects

CV: chest pain, palpitations, angina, arrhythmias, hypertension

Endo: hyperglycemia

F and E: hypokalemia

GI: nausea, vomiting

Neuro: nervousness, restlessness, tremor, headache, hyperactivity (children), insomnia

Resp: PARADOXICAL BRONCHOSPASM (EXCESSIVE USE OF INHALERS)

* CAPITALS indicate life-threatening.
Underline 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).

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; 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 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)

Immediate-release tablets: 2 mg, 4 mg

Cost:

Generic: 4 mg $565.87/100

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

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 Canadian Tradename, 2 mg/mL Canadian Tradename, 5 mg/mL (0.5%)

Cost:

Generic: 2.5 mg/3 mL $40.82/90 mL, 5 mg/mL $51.02/60 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 Canadian Tradename

Cost:

Proair HFA: $52.53/8.5-g canister

Proventil HFA: $62.62/6.7-g canister

Ventolin HFA: $19.08/8-g canister

Powder for inhalation (Proair Digihaler and Proair Respiclick): 90 mcg/inhalation (200 metered inhalations)

Powder for inhalation (Ventolin Diskus): 200 mcg Canadian Tradename

In Combination with: ipratropium (Combivent). 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.

Implementation

  • PO Administer oral medication with meals to minimize gastric irritation.
  • 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.  Proair Respiclick  does not require priming. 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 canister after 200 sprays. Actuators should not be changed among products.
    • Inform patient that these products contain hydrofluoroalkane (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.
  • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage patients who become pregnant during therapy to enroll in the pregnancy registry that monitors pregnancy outcomes in women exposed to asthma medications during pregnancy. For more information, contact the MothersToBaby Pregnancy Studies conducted by the Organization of Teratology Information Specialists at 1-877-311-8972 or visit http://mothertobaby.org/pregnancy-studies/.
  • 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 wk.
    • 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 re-evaluate patient's therapy.

Evaluation/Desired Outcomes

Prevention or relief of bronchospasm.

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