albuterol (Rx)

>10%

Tremor (20%)

Nervousness in children aged 2-6 years (20%)

Insomnia in children aged 6-12 years receiving 4-12 mg q12hr (11%)

1-10%

Nausea (10%)

Fever (1.6-9%)

Bronchospasm (8%)

Vomiting (7%)

Headache (4-7%)

Dizziness (1-7%)

Cough (5%)

Allergic reactions (4%)

Otitis media (3.3%)

Epistaxis in children (3%)

Increased appetite (3%)

Urinary tract infection (3%)

Dry mouth (<3%)

Eructation or flatulence (<3%)

Increased sweating (<3%)

Pain (2.7%)

Dyspepsia (1-2%)

Hyperactivity (1-2%)

Chills (<2%)

Lymphadenopathy (<2%)

Ocular pruritus (<2%)

Sweating (<2%)

Conjunctivitis in children aged 2-6 years (1%)

Dysphonia (>1%)

Flu syndrome

Nervousness

<1%

Epigastric pain

Epistaxis in adults

Hyperactivity in children

Frequency Not Defined

Adverse reactions such as hypertension, angina, vertigo, central nervous system stimulation, insomnia, headache, metabolic acidosis, and drying or irritation of oropharynx

Hypersensitivity

Hypokalemia

Increased blood glucose levels

Prolonged QT interval and ST-segment depression

Sleeplessness

Tachycardia (incidence varies with formulation)

Urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema (rare)

Contraindications

Hypersensitivity to albuterol

Severe hypersensitivity to milk proteins

Cautions

Some inhalers use hydrofluoroalkane (HFA) as propellant instead of chlorofluorocarbons (CFCs); otherwise, devices are equivalent

Immediate hypersensitivity reactions may occur after administration of albuterol sulfate, as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema

Paradoxical bronchospasm may occur

Need for more doses than usual may be a sign of deterioration of asthma and requires reevaluation of treatment

Use with caution in patients with cardiovascular disease, asthma, glaucoma, diabetes, hypokalemia, hyperthyroidism, or seizures

Use face mask in children <4 years

Excessive use may be fatal; do not exceed recommended dose; serious adverse effects occur when administered dose exceeds recommended dose

May exacerbate heart failure in patients with reduced ejection fraction (dose related increased risk for hospital admission)

Use of beta-adrenergic-agonist bronchodilators alone may not be adequate to control asthma; consider adding anti-inflammatory agents (eg, corticosteroids) to therapy

May produce significant hypokalemia, possibly through intracellular shunting, which potentially produces adverse cardiovascular effects

Drug interactions overview

• Do not use other short-acting sympathomimetic bronchodilators concomitantly with an albuterol inhaler
• Additional adrenergic drugs by any route should be used with caution to avoid deleterious cardiovascular effects
• ECG changes and/or hypokalemia which may result from coadministration of non-potassium sparing diuretics (eg, loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when recommended dose of beta-agonist is exceeded
• Mean decreases of 16% and 22% in serum digoxin levels were demonstrated after single dose IV and oral administration of albuterol, respectively, to normal volunteers who had received digoxin for 10 days; clinical significance is unclear; carefully evaluate serum digoxin levels in patients who are concurrently receiving digoxin and albuterol inhaler
• Use extreme caution in patients being treated with monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants (TCAs), or within 2 weeks of discontinuation of such agents, because coadministration may potentiate cardiovascular effects of albuterol; consider alternative therapy in patients taking MAOIs or TCAs

Pregnancy

There are no randomized clinical studies of use during pregnancy

Available data from published epidemiological studies and postmarketing case reports of pregnancy outcomes following inhaled albuterol use do not consistently demonstrate a risk of major birth defects or miscarriage

In animal reproduction studies, when administered SC to pregnant mice there was evidence of cleft palate at ≤9x the maximum recommended human daily inhalation dose (MRHDID)

Clinical considerations

• Disease-associated maternal and/or embryo/fetal risk

  • In women with poorly or moderately controlled asthma, there is an increased risk of preeclampsia in the mother and prematurity, low birth weight, and small for gestational age in the neonate
  • Closely monitor pregnant women and adjust medications as necessary to maintain optimal control

• Labor or delivery

  • Because of potential for beta-agonist interference with uterine contractility, restrict use for relief of bronchospasm during labor to those patients in whom the benefits clearly outweigh the risk

Lactation

There are no available data on the presence of albuterol in human milk, the effects on the breastfed child, or the effects on milk production

Consider developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Beta2 receptor agonist with some beta1 activity; relaxes bronchial smooth muscle with little effect on heart rate

Absorption

Onset: 25 min (Ventolin HFA); 0.5-2 hr (nebulization); 2-3 hr (PO)

Duration: 4-6 hr (PO);

Peak plasma time: Inhalation, 2-5 hr; PO, 2-2.5 hr

Distribution

Protein bound: 10%

Metabolism

Metabolized in liver

Elimination

Half-life: 3-8 hr (inhalation); 3.7-5 hr (PO)

Excretion: Urine

Oral Inhalation Administration

For oral inhalation only

Nebulizer solution

• Remove one vial from foil pouch
• Twist cap off vial and squeeze contents into nebulizer reservoir
• Attach mouthpiece/face mask and compressor to nebulizer
• Sit in a comfortable, upright position; place the mouthpiece in your mouth or put on mask, and turn on compressor
• Calmly breathe and evenly as possible through your mouth until no more mist is formed in the nebulizer chamber (~5-15 minutes)
• Clean nebulizer according to manufacturer instructions

Aerosol metered-dose inhaler

• Prime inhaler (before first-time use or when inhaler has not been used for >2 weeks): Release 4 test sprays into the air, away from the face
• Shake well before each use
• Breathe out fully through the mouth; place mouthpiece fully into mouth, holding inhaler in its upright position and close lips around it
• While breathing in deeply and slowly through the mouth, fully depress the top of the metal canister with your index finger
• Hold your breath for ≤10 sec; before breathing out
• For additional puffs, wait 1 minute, shake inhaler again, and repeat steps listed above; replace cap after use
• Cleaning: To maintain proper use of this product, wash and dry mouthpiece thoroughly ≥1/week

Powder metered-dose inhaler

• Does NOT require priming
• Do not use with a spacer or volume holding chamber

• Cleaning

  • Keep clean and dry at all times
  • Never wash or put any part of inhaler in water
  • Routine maintenance not required

Oral Administration

Extended-release tablets: Do not chew, crush, or mix with food

Storage

Nebulizer solution

• Store between 2-25°C (36-77°F)
• Protect from light before use, therefore, keep unused vials in the foil pouch

Aerosol metered-dose inhaler

• Store at room temperature (15-25°C [59-77°F])

Powder metered-dose inhaler

• Store at room temperature (15-25°C [59-77°F])
• Avoid exposure to extreme heat, cold, or humidity
• Discard 13 months after opening the foil pouch, when the dose counter displays zero, or after the expiration date on the product, whichever comes first