Albuterol

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Albuterol
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]

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Black Box Warning

WARNINGS
See full prescribing information for complete Boxed Warning.
  • The action of Albuterol Inhalation Aerosol may last up to 6 hours or longer. Albuterol Inhalation Aerosol should not be used more frequently than recommended. Do not increase the dose or frequency of Albuterol Inhalation Aerosol without consulting your doctor. If you find that treatment with Albuterol Inhalation Aerosol becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While you are using Albuterol Inhalation Aerosol, other inhaled drugs and asthma medicines should be used only as directed by your doctor.

Overview

Albuterol is a beta-2 adrenergic agonist that is FDA approved for the prophylaxis of exercise-induced bronchospasm and bronchospasm in patients with reversible obstructive airway disease. There is a Black Box Warning for this drug as shown here. Common adverse reactions include tachyarrhythmia, hypokalemia, nausea, pharyngitis, throat irritation, feeling nervous, headache, tremor, cough, rhinitis, upper respiratory infection, and viral lower respiratory infection.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Acute Episodes of Bronchospasm

  • Dosing information (Aerosol,Inhalant)
  • Usual dosage: two inhalations repeated every four to six hours
  • In some patients, one inhalation every four hours may be sufficient. More frequent administration or a larger number of inhalations are not recommended.
  • It is recommended to "test spray" Albuterol Inhalation Aerosol into the air before using for the first time and in cases where the aerosol has not been used for a prolonged period of time.
  • The use of Albuterol Inhalation Aerosol can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the inhaler. Safe usage for periods extending over several years has been documented.
  • If a previously effective dosage regimen fails to provide the usual response, this may be a marker of destabilization of asthma and requires reevaluation of the patient and the treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids.
  • Exercise-Induced Bronchospasm Prevention
  • Usual dosage for adults and pediatric patients 4 years and older is two inhalations 15 minutes before exercise.

For treatment, see above.

  • Dosing information (Tablet)
  • Usual starting dosage: 2 or 4 mg PO tid or aid
  • Dosage Adjustment
  • A dosage above 4 mg four times a day should be used only when the patient fails to respond. If a favorable response does not occur with the 4 mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.
  • Elderly Patients and Those Sensitive to Beta-adrenergic Stimulators
  • An initial dosage: 2 mg PO tid or qid. If adequate bronchodilation is not obtained, dosage may be increased gradually to as much as 8 mg three or four times a day.
  • The total daily dose should not exceed 32 mg in adults.
  • Dosing information (Syrup)
  • Usual starting dosage: 2 mg (1 teaspoonful) or 4 mg (2 teaspoonfuls) three or four times a day.
  • Dosage Adjustment
  • A dosage above 4 mg four times a day should be used only when the patient fails to respond. If a favorable response does not occur with the 4-mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.
  • Dosing information (Solution)
  • Usual dosage for adults: 2.5 mg three to four times daily by nebulization. More frequent administration or higher doses are not recommended. To administer 2.5 mg of albuterol, dilute 0.5 mL of the 0.5% inhalation solution with 2.5 mL of sterile normal saline solution. The flow rate is regulated to suit the particular nebulizer so that albuterol sulfate inhalation solution will be delivered over approximately 5 to 15 minutes.
  • The use of albuterol sulfate inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the inhalation solution.
  • If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately as this is often a sign of seriously worsening asthma that would require reassessment of therapy.
  • Drug compatibility (physical and chemical), efficacy, and safety of albuterol sulfate inhalation solution when mixed with other drugs in a nebulizer have not been established.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Albuterol in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Albuterol in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Bronchospasm

  • Dosing information (Tablet)
  • Usual starting dosage: 2 or 4 mg PO tid or aid
  • Dosage Adjustment
  • Children Over 12 Years of Age
  • For adults and children 12 years and older, a dosage above 4 mg four times a day should be used only when the patient fails to respond. If a favorable response does not occur with the 4 mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.
  • Children 6 to 12 Years of Age Who Fail to Respond to the Initial Starting Dosage of 2 mg Four Times a Day
  • For children from 6 to 12 years of age who fail to respond to the initial starting dosage of 2 mg four times a day, the dosage may be cautiously increased stepwise, but not to exceed 24 mg/day (given in divided doses).
  • Dosing information (Syrup)
  • The usual starting dosage for adults and children over 14 years of age is 2 mg (1 teaspoonful) or 4 mg (2 teaspoonfuls) three or four times a day.
  • The usual starting dosage for children over 6 years to 14 years of age is 2 mg (1 teaspoonful) three or four times a day.
  • Dosing in children 2 to 5 years of age should be initiated at 0.1 mg/kg of body weight three times a day. This starting dosage should not exceed 2 mg (1 teaspoonful) three times a day.
  • Dosage Adjustment
  • For adults and children over 14 years of age, a dosage above 4 mg four times a day should be used only when the patient fails to respond. If a favorable response does not occur with the 4-mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.
  • For children over 6 years to 14 years of age who fail to respond to the initial starting dosage of 2 mg four times a day, the dosage may be cautiously increased stepwise, but not to exceed 24 mg/day (given in divided doses).
  • For children from 2 to 5 years of age who do not respond satisfactorily to the initial starting dosage, the dosage may be increased stepwise to 0.2 mg/kg of body weight three times a day, but not to exceed a maximum of 4 mg (2 teaspoonfuls) given three times a day.
  • Dosing information (Solution)
  • The usual dosage for children 12 years of age and older : 2.5 mg three to four times daily by nebulization. More frequent administration or higher doses are not recommended. To administer 2.5 mg of albuterol, dilute 0.5 mL of the 0.5% inhalation solution with 2.5 mL of sterile normal saline solution. The flow rate is regulated to suit the particular nebulizer so that albuterol sulfate inhalation solution will be delivered over approximately 5 to 15 minutes.
  • The use of albuterol sulfate inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the inhalation solution.
  • If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately as this is often a sign of seriously worsening asthma that would require reassessment of therapy.
  • Drug compatibility (physical and chemical), efficacy, and safety of albuterol sulfate inhalation solution when mixed with other drugs in a nebulizer have not been established.
  • For children 2 to 12 years of age, initial dosing should be based upon body weight (0.1 to 0.15 mg/kg per dose), with subsequent dosing titrated to achieve the desired clinical response. Dosing should not exceed 2.5 mg three to four times daily by nebulization. The following table outlines approximate dosing according to body weight.
This image is provided by the National Library of Medicine.

The appropriate volume of the 0.5% inhalation solution should be diluted in sterile normal saline solution to a total volume of 3 mL prior to administration via nebulization.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Albuterol in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Albuterol in pediatric patients.

Contraindications

Albuterol is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.

Warnings

WARNINGS
See full prescribing information for complete Boxed Warning.
  • The action of Albuterol Inhalation Aerosol may last up to 6 hours or longer. Albuterol Inhalation Aerosol should not be used more frequently than recommended. Do not increase the dose or frequency of Albuterol Inhalation Aerosol without consulting your doctor. If you find that treatment with Albuterol Inhalation Aerosol becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While you are using Albuterol Inhalation Aerosol, other inhaled drugs and asthma medicines should be used only as directed by your doctor.

Paradoxical bronchospasm

Albuterol can produce paradoxical bronchospasm, which may be life threatening. If paradoxical bronchospasm occurs, Albuterol Inhalation Aerosol should be discontinued immediately and alternative therapy instituted. It should be recognized that paradoxical bronchospasm, when associated with inhaled formulations, frequently occurs with the first use of a new canister or vial.

Cardiovascular Effects

Albuterol, like all other beta-adrenergic agonists, can produce a clinically significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, and/or symptoms. Although such effects are uncommon after administration of Albuterol Inhalation Aerosol at recommended doses, if they occur, the drug may need to be discontinued. In addition, beta-agonists have been reported to produce electrocardiogram (ECG) changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression. The clinical significance of these findings is unknown. Therefore, albuterol, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.

Deterioration of Asthma

Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. If the patient needs more doses of Albuterol Inhalation Aerosol than usual, this may be a marker of destabilization of asthma and requires reevaluation of the patient and treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids.

Use of Anti-Inflammatory Agents

The use of beta-adrenergic agonist bronchodilators alone may not be adequate to control asthma in many patients. Early consideration should be given to adding anti-inflammatory agents, e.g., corticosteroids.

Immediate Hypersensitivity Reactions

Immediate hypersensitivity reactions may occur after administration of Albuterol Inhalation Aerosol, as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema. The contents of Albuterol Inhalation Aerosol are under pressure. Do not puncture. Do not use or store near heat or open flame. Exposure to temperatures above 120°F may cause bursting. Never throw container into fire or incinerator. Avoid spraying in eyes. Keep out of reach of children.

Microbial Contamination (only in solution): To avoid microbial contamination, proper aseptic technique should be used each time the bottle is opened. Precautions should be taken to prevent contact of the dropper tip of the bottle with any surface, including the nebulizer reservoir and associated ventilatory equipment. In addition, if the solution changes color or becomes cloudy, it should not be used.

PRECAUTIONS

General

Albuterol, as with all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension; in patients with convulsive disorders, hyperthyroidism, or diabetes mellitus; and in patients who are unusually responsive to sympathomimetic amines. Clinically significant changes in systolic and diastolic blood pressure have been seen in individual patients and could be expected to occur in some patients after use of any beta-adrenergic bronchodilator. Large doses of intravenous albuterol have been reported to aggravate preexisting diabetes mellitus and ketoacidosis. As with other beta-agonists, albuterol may produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse cardiovascular effects. The decrease is usually transient, not requiring supplementation. Although there have been no reports concerning the use of Albuterol Inhalation Aerosol during labor and delivery, it has been reported that high doses of albuterol administered intravenously inhibit uterine contractions. Although this effect is extremely unlikely as a consequence of aerosol use, it should be kept in mind.

Adverse Reactions

Clinical Trials Experience

The adverse reactions to albuterol are similar in nature to reactions to other sympathomimetic agents, although the incidence of certain cardiovascular effects is lower with albuterol.

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

Cases of urticaria, angioedema, rash, bronchospasm, hoarseness, oropharyngeal edema, and arrhythmias (including atrial fibrillation, supraventricular tachycardia, extrasystoles) have been reported after the use of albuterol inhalation aerosol. In addition, albuterol, like other sympathomimetic agents, can cause adverse reactions such as hypertension, angina, vertigo, central nervous system stimulation, sleeplessness, and unusual taste.

Postmarketing Experience

There is limited information regarding Albuterol Postmarketing Experience in the drug label.

Drug Interactions

Other short-acting sympathomimetic aerosol bronchodilators should not be used concomitantly with albuterol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.

Monoamine Oxidase Inhibitors or Tricyclic Antidepressants

Albuterol should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within two weeks of discontinuation of such agents, because the action of albuterol on the vascular system may be potentiated.

Beta-Blockers

Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-agonists, such as albuterol, but may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers should be considered, although they should be administered with caution.

Diuretics

The ECG changes and/or hypokalemia that may result from the administration of nonpotassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is not known, caution is advised in the coadministration of beta-agonists with nonpotassium-sparing diuretics.

Digoxin

Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of albuterol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are receiving albuterol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully evaluate the serum digoxin levels in patients who are currently receiving digoxin and albuterol.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Albuterol sulfate has been shown to be teratogenic in mice. A study in CD-1 mice at subcutaneous (sc) doses of 0.025, 0.25, and 2.5 mg/kg (approximately 2/25, 1.0, and 8.0 times, respectively, the maximum recommended daily inhalation dose for adults on a mg/m2 basis), showed cleft palate formation in 5 of 111 (4.5%) fetuses at 0.25 mg/kg and in 10 of 108 (9.3%) fetuses at 2.5 mg/kg. The drug did not induce cleft palate formation at the lowest dose, 0.025 mg/kg. Cleft palate also occurred in 22 of 72 (30.5%) fetuses from females treated with 2.5 mg/kg of isoproterenol (positive control) sc (approximately 8 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis). A reproduction study in Stride Dutch rabbits revealed cranioschisis in 7 of 19 (37%) fetuses when albuterol sulfate was administered orally at a 50 mg/kg dose (approximately 680 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis). There are no adequate and well-controlled studies in pregnant women. Albuterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. During worldwide marketing experience, various congenital anomalies, including cleft palate and limb defects, have been rarely reported in the offspring of patients being treated with albuterol. Some of the mothers were taking multiple medications during their pregnancies. No consistent pattern of defects can be discerned, and a relationship between albuterol use and congenital anomalies has not been established.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Albuterol in women who are pregnant.

Labor and Delivery

Because of the potential for beta-agonist interference with uterine contractility, use of albuterol for relief of bronchospasm during labor should be restricted to those patients in whom the benefits clearly outweigh the risk.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because of the potential for tumorigenicity shown for albuterol in some animal studies, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in pediatric patients below 4 years of age have not been established.

Geriatic Use

There is no FDA guidance on the use of Albuterol in geriatric settings.

Gender

There is no FDA guidance on the use of Albuterol with respect to specific gender populations.

Race

There is no FDA guidance on the use of Albuterol with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Albuterol in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Albuterol in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Albuterol in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Albuterol in patients who are immunocompromised.

Tocolysis

Albuterol has not been approved for the management of preterm labor. The benefit:risk ratio when albuterol is administered for tocolysis has not been established. Serious adverse reactions, including maternal pulmonary edema, have been reported during or following treatment of premature labor with beta2-agonists, including albuterol.

Administration and Monitoring

Administration

Inhale and oral

Monitoring

FDA Package Insert for Albuterol contains no information regarding Drug Monitoring.

IV Compatibility

There is limited information about the IV Compatibility.

Overdosage

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under ADVERSE REACTIONS, e.g., seizures, angina, hypertension, hypotension, tachycardia with rates up to 200 beats/minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and sleeplessness. hypokalemia may also occur. As with all sympathomimetic aerosol medications, cardiac arrest and even death may be associated with abuse of Albuterol Inhalation Aerosol. Treatment consists of discontinuation of Albuterol Inhalation Aerosol together with appropriate symptomatic therapy. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. There is insufficient evidence to determine if dialysis is beneficial for overdosage of Albuterol Inhalation Aerosol. The oral median lethal dose of albuterol sulfate in mice is greater than 2000 mg/kg (approximately 6800 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 3200 times the maximum recommended daily inhalation dose for children on a mg/m2 basis). In mature rats, the sc median lethal dose of albuterol sulfate is approximately 450 mg/kg (approximately 3000 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 1400 times the maximum recommended daily inhalation dose for children on a mg/m2 basis). In small young rats, the sc median lethal dose of albuterol sulfate is approximately 2000 mg/kg (approximately 14,000 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 6400 times the maximum recommended daily inhalation dose for children on a mg/m2 basis). The inhalation median lethal dose has not been determined in animals.

Pharmacology

Salbutamol.png
Salbutamol-S-enantiomer-3D-balls.png
1 : 1 mixture (racemate)Salbutamol
Systematic (IUPAC) name
(RS)-4-2-(tert-butylamino)-1-hydroxyethyl-2-(hydroxymethyl)phenol
Identifiers
CAS number 18559-94-9
ATC code R03AC02 R03CC02 (WHO)
PubChem 2083
DrugBank DB01001
Chemical data
Formula C13H21NO3 
Mol. mass 239.311
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Half life 1.6 hours
Excretion Renal
Therapeutic considerations
Licence data

US

Pregnancy cat.

A(AU) C(US)

Legal status

Pharmacist Only (S3)(AU) ?(CA) POM(UK) -only(US)

Routes Oral, inhalational, IV

Mechanism of Action

Albuterol is typically used to treat bronchospasm (due to any cause, allergen asthma or exercise-induced), as well as chronic obstructive pulmonary disease. Emergency medical practice commonly treats people presenting with asthma who report taking their Albuterol inhaler as prescribed with Albuterol. In general, people tolerate large doses well.

Other uses include in cystic fibrosis, along with ipratropium bromide, acetylcysteine, and pulmozyme and subtypes of congenital myasthenic syndromes associated to mutations in Dok-7.

As a β2-agonist, Albuterol also finds use in obstetrics. Intravenous Albuterol can be used as a tocolytic to relax the uterine smooth muscle to delay premature labor. While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine, which is more effective, better tolerated and orally administered.[1]

Albuterol is used to treat acute hyperkalemia as it stimulates potassium to flow in cells thus lowering the level in the blood.

Albuterol has also been trialled in spinal muscular atrophy where it appears to show modest benefits. The drug is speculated to modulate the alternative splicing of the SMN2 gene, increasing the amount of the SMN protein whose deficiency is regarded as the root cause of the disease.

Structure

The active component of Albuterol Inhalation Aerosol is albuterol (α1-(tert-butylamino)methyl-4-hydroxy-m-xylene-α,α'-diol), a relatively selective beta2-adrenergic bronchodilator, having the following structural formula:

This image is provided by the National Library of Medicine.

Albuterol is the official generic name in the United States. The World Health Organization recommended name for the drug is salbutamol. The molecular weight of albuterol is 239.2, and the molecular formula is C13H21NO3. Albuterol is a white to off-white crystalline solid. It is soluble in ethanol, sparingly soluble in water, and very soluble in chloroform. Albuterol Inhalation Aerosol is a pressurized metered-dose aerosol unit for oral inhalation. It contains a microcrystalline (95% ≤ 10 µm) suspension of albuterol in propellants (trichloromonofluoromethane and dichlorodifluoromethane) with oleic acid. Each actuation delivers 100 mcg of albuterol from the valve and 90 mcg of albuterol from the mouthpiece. Each canister provides 200 inhalations.

Pharmacodynamics

In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established. The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'- adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Albuterol has been shown in most controlled clinical trials to have more effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, than isoproterenol at comparable doses while producing fewer cardiovascular effects. Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes. Albuterol is longer acting than isoproterenol in most patients by any route of administration because it is not a substrate for the cellular uptake processes for catecholamines nor for catechol-O-methyl transferase. The effects of rising doses of albuterol and isoproterenol aerosols were studied in volunteers and asthmatic patients. Results in normal volunteers indicated that albuterol is one half to one quarter as active as isoproterenol in producing increases in heart rate. In asthmatic patients similar cardiovascular differentiation between the two drugs was also seen.

Preclinical

Intravenous studies in rats with albuterol sulfate have demonstrated that albuterol crosses the blood brain barrier and reaches brain concentrations amounting to approximately 5.0% of the plasma concentrations. In structures outside the brain barrier (pineal and pituitary glands), albuterol concentrations were found to be 100 times those in the whole brain. Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta-agonists and methylxanthines are administered concurrently. The clinical significance of these findings is unknown.

Pharmacokinetics

Because of its gradual absorption from the bronchi, systemic levels of albuterol are low after inhalation of recommended doses. Studies undertaken with four subjects administered tritiated albuterol resulted in maximum plasma concentrations occurring within two to four hours. Due to the sensitivity of the assay method, the metabolic rate and half-life of elimination of albuterol in plasma could not be determined. However, urinary excretion provided data indicating that albuterol has an elimination half-life of 3.8 hours. Approximately 72% of the inhaled dose is excreted within 24 hours in the urine, and consists of 28% as unchanged drug and 44% as metabolite.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In a two-year study in Sprague-Dawley rats, albuterol sulfate caused a significant dose-related increase in the incidence of benign leiomyomas of the mesovarium at dietary doses of 2.0, 10, and 50 mg/kg (approximately 15, 70, and 340 times, respectively, the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 6, 30, and 160 times, respectively, the maximum recommended daily inhalation dose in children on a mg/m2 basis). In another study this effect was blocked by the coadministration of propranolol, a non-selective beta-adrenergic antagonist. In an 18-month study in CD-1 mice, albuterol sulfate showed no evidence of tumorigenicity at dietary doses of up to 500 mg/kg (approximately 1700 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 800 times the maximum recommended daily inhalation dose for children on a mg/m2 basis). In a 22-month study in the Golden hamster, albuterol sulfate showed no evidence of tumorigenicity at dietary doses of up to 50 mg/kg (approximately 225 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis, or, approximately 110 times the maximum recommended daily inhalation dose for children on a mg/m2 basis). Albuterol sulfate was not mutagenic in the Ames test with or without metabolic activation using tester strains S. typhimurium TA1537, TA1538, and TA98 or E. Coli WP2, WP2uvrA, and WP67. No forward mutation was seen in yeast strain S. cerevisiae S9 nor any mitotic gene conversion in yeast strain S. cerevisiae JD1 with or without metabolic activation. Fluctuation assays in S. typhimurium TA98 and E.Coli WP2, both with metabolic activation, were negative. Albuterol sulfate was not clastogenic in a human peripheral lymphocyte assay or in an AH1 strain mouse micronucleus assay at intraperitoneal doses of up to 200 mg/kg. Reproduction studies in rats demonstrated no evidence of impaired fertility at oral doses of up to 50 mg/kg (approximately 340 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis).

Clinical Studies

In controlled clinical trials involving adults with asthma, the onset of improvement in pulmonary function was within 15 minutes, as determined by both MMEF (maximum midexpiratory flow rate) and FEV1 (forced expiratory volume in one second). MMEF measurements also showed that near maximum improvement in pulmonary function generally occurs within 60 to 90 minutes following two inhalations of albuterol and that clinically significant improvement generally continues for three to four hours in most patients. Some patients showed a therapeutic response (defined by maintaining FEV1 values 15% or more above baseline) that was still apparent at 6 hours. Continued effectiveness of albuterol was demonstrated over a 13-week period in these same trials. In controlled clinical trials involving children 4 to 12 years of age, FEV1 measurements showed that maximum improvement in pulmonary function occurs within 30 to 60 minutes. The onset of clinically significant (≥15%) improvement in FEV1 was observed as soon as five minutes following 180 mcg of albuterol in 18 of 30 (60%) children in a controlled dose-ranging study. Clinically significant improvement in FEV1 continued in the majority of patients for two hours and in 33% to 47% for four hours among 56 patients receiving inhalation aerosol in one pediatric study. In a second study among 48 patients receiving inhalation aerosol, clinically significant improvement continued in the majority for up to one hour and in 23% to 40% for four hours. In addition, at least 50% of the patients in both studies achieved an improvement in FEF25%–75% (forced expiratory flow rate between 25% and 75% of the forced vital capacity) of at least 20% for 2 to 5 hours. Continued effectiveness of albuterol was demonstrated over the 12-week study period. In other clinical studies in adults and children, two inhalations of albuterol aerosol taken approximately 15 minutes before exercise prevented exercise-induced bronchospasm, as demonstrated by the maintenance of FEV1 within 80% of baseline values in the majority of patients. One study in adults also evaluated the duration of the prophylactic effect to repeated exercise challenges, which was evident at 4 hours in a majority of the patients and at 6 hours in approximately one third of the patients.

How Supplied

Albuterol Inhalation Aerosol

Albuterol Inhalation Aerosol is supplied in 17 g canisters containing 200 metered inhalations (NDC 17270-721-01) in boxes of one. Each actuation delivers 100 mcg of albuterol from the valve and 90 mcg of albuterol from the mouthpiece. Each canister is supplied with a blue oral adapter and patient's instructions. Also available, Albuterol Inhalation Aerosol Refill with patient's instructions (NDC 17270-721-02). The blue adapter supplied with Albuterol Inhalation Aerosol should not be used with any other product canisters, and the adapters from other products should not be used with an Albuterol Inhalation Aerosol canister. The correct amount of medication in each canister cannot be assured after 200 actuations, even though the canister is not completely empty. The canister should be discarded when the labeled number of actuations have been used.

Albuterol Tablet

Albuterol tablets, USP; 2 mg of albuterol as the sulfate, are white, round, scored, debossed MP 47

This image is provided by the National Library of Medicine.

Albuterol tablets, USP; 4 mg of albuterol as the sulfate, are white, round, scored, debossed MP 88

This image is provided by the National Library of Medicine.

ALBUTEROL SULFATE syrup

Albuterol Sulfate Syrup, a clear, yellow liquid with a strawberry flavor, contains 2 mg of albuterol (present as the sulfate) per 5 mL in bottles of 16 fluid ounces (one pint).

ALBUTEROL SULFATE inhalation solution

Albuterol sulfate inhalation solution, 0.5% is supplied in amber glass bottles, with a calibrated dropper and with patient instructions in the following size: 20 mL bottles - NDC 24208-347-20

Storage

Albuterol Inhalation Aerosol

Store between 15°–30°C (59°–86°F). As with most inhaled medications in aerosol canisters, the therapeutic effect of this medication may decrease when the canister is cold; for best results, the canister should be at room temperature before use.

Albuterol Tablet

Store at 20° to 25°C (68° to 77°F). DISPENSE IN TIGHT, LIGHT-RESISTANT CONTAINER.

ALBUTEROL SULFATE syrup

Store at 20° to 25°C (68° to 77°F).

ALBUTEROL SULFATE inhalation solution

Storage: Store between 2°-25°C (36°-77°F).

Images

Drug Images

Albuterol NDC 03780255.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: M;255
Dosage: 2 mg
Color(s): White
Shape: Round
Size (mm): 6
Score: 2
NDC:03780255

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol NDC 03780572.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: M;572
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 9
Score: 2
NDC:03780572

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol NDC 510790658.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: M;572
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 9
Score: 2
NDC:510790658

Drug Label Author: UDL Laboratories, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol Sulfate NDC 03784122.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: M;22
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 6
Score: 1
NDC:03784122

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol Sulfate NDC 03784124.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: M;24
Dosage: 8 mg
Color(s): Blue
Shape: Round
Size (mm): 6
Score: 1
NDC:03784124

Drug Label Author: Mylan Pharmaceuticals Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol Sulfate NDC 687740400.jpg

Drug Name: Albuterol
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: V;4
Dosage: 4 mg
Color(s): Green
Shape: Round
Size (mm): 6
Score: 1
NDC:687740400

Drug Label Author: DAVA Pharmaceuticals, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
VoSpire NDC 687740600.jpg

Drug Name: VoSpire
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: V;4
Dosage: 4 mg
Color(s): Green
Shape: Round
Size (mm): 6
Score: 1
NDC:687740600

Drug Label Author: DAVA Pharmaceuticals, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
VoSpire NDC 687740601.jpg

Drug Name: VoSpire
Ingredient(s): ALBUTEROL SULFATE[ALBUTEROL]
Imprint: V;8
Dosage: 8 mg
Color(s): White
Shape: Round
Size (mm): 6
Score: 1
NDC:687740601

Drug Label Author: DAVA Pharmaceuticals, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol sulfate NDC 534890176.jpg

Drug Name: Albuterol sulfate
Ingredient(s): albuterol sulfate[albuterol]
Imprint: MP;47
Dosage: 2 mg
Color(s): White
Shape: Round
Size (mm): 6
Score: 2
NDC:534890176

Drug Label Author: Mutual Pharmaceutical Company, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Albuterol sulfate NDC 534890177.jpg

Drug Name: Albuterol sulfate
Ingredient(s): albuterol sulfate[albuterol]
Imprint: MP;88
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 8
Score: 2
NDC:534890177

Drug Label Author: Mutual Pharmaceutical Company, Inc.

This pill image is provided by the National Library of Medicine's PillBox.

Package and Label Display Panel

Albuterol label 01.jpg
This image of the FDA label is provided by the National Library of Medicine.
Albuterol label 02.jpg
This image of the FDA label is provided by the National Library of Medicine.
Albuterol label 03.jpg
This image of the FDA label is provided by the National Library of Medicine.
Albuterol label 04.jpg
This image of the FDA label is provided by the National Library of Medicine.
Albuterol panel 01.png
This image of the FDA label is provided by the National Library of Medicine.
Albuterol panel 02.png
This image of the FDA label is provided by the National Library of Medicine.
Albuterol panel 03.png
This image of the FDA label is provided by the National Library of Medicine.
Albuterol panel 04.png
This image of the FDA label is provided by the National Library of Medicine.

Patient Counseling Information

The action of Albuterol Inhalation Aerosol may last up to six hours or longer. Albuterol Inhalation Aerosol should not be used more frequently than recommended. Do not increase the dose or frequency of Albuterol Inhalation Aerosol without consulting your physician. If you find that treatment with Albuterol Inhalation Aerosol becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While you are using Albuterol Inhalation Aerosol, other inhaled drugs and asthma medications should be taken only as directed by your physician. Common adverse effects include palpitations, chest pain, rapid heart rate, and tremor or nervousness. If you are pregnant or nursing, contact your physician about use of Albuterol Inhalation Aerosol. Effective and safe use of Albuterol Inhalation Aerosol includes an understanding of the way that it should be administered. In general, the technique for administering Albuterol Inhalation Aerosol to children is similar to that for adults, since children's smaller ventilatory exchange capacity automatically provides proportionally smaller aerosol intake. Children should use Albuterol Inhalation Aerosol under adult supervision, as instructed by the patient's physician.

Precautions with Alcohol

Alcohol-Albuterol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

  • Accuneb
  • Proventil
  • Proventil HFA
  • Proventil Repetabs
  • Ventolin
  • Ventolin HFA
  • VoSpire ER
  • ProAir HFA

Look-Alike Drug Names

There is limited information about the look-alike drug names.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Rossi, S (2004). Australian Medicines Handbook. AMH. ISBN 0-9578521-4-2.





















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