DESCRIPTION
id: 564137A9-7382-CA33-4850-D8EF6E308CAA
displayName: DESCRIPTION SECTION
FDA Article Code: 34089-3
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: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.
CLINICAL PHARMACOLOGY
id: 8991A291-1CFC-831D-B17F-FDD17355FE8D
displayName: CLINICAL PHARMACOLOGY SECTION
FDA Article Code: 34090-1
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.
INDICATIONS AND USAGE
id: A1F7DABF-382E-A82E-9591-27156FC4EC05
displayName: INDICATIONS & USAGE SECTION
FDA Article Code: 34067-9
Albuterol Inhalation Aerosol is indicated for the prevention and relief of bronchospasm in patients 4 years of age and older with reversible obstructive airway disease, and for the prevention of exercise induced bronchospasm in patients 4 years of age and older.Albuterol Inhalation Aerosol can be used with or without concomitant steroid therapy.
CONTRAINDICATIONS
id: 8F0DFD0B-B5C8-9A78-C99A-2637451B9073
displayName: CONTRAINDICATIONS SECTION
FDA Article Code: 34070-3
Albuterol Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.
ADVERSE REACTIONS
id: 9D5BF50F-DF89-DB65-555D-D932580ACC29
displayName: ADVERSE REACTIONS SECTION
FDA Article Code: 34084-4
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.
Percent Incidence of Adverse Reactions in Patients ≥ 12 Years of Age in a 13-Week Clinical TrialA 13-week double-blind study compared albuterol and isoproterenol inhalation aerosols in 147 asthmatic patients.
|
Percent Incidence |
| Reaction |
Albuterol |
Isoproterenol |
| Tremor |
<15% |
<15% |
| Nausea |
<15% |
<15% |
| Tachycardia |
10% |
10% |
| Palpitations |
<10% |
<15% |
| Nervousness |
<10% |
<15% |
| Increased Blood Pressure |
<5% |
<5% |
| Dizziness |
<5% |
<5% |
| Heartburn |
<5% |
<5% |
Percent Incidence of Adverse Reactions in Children 4 to 11 Years of Age in a 12-Week TrialA 12-week double-blind trial in 104 patients aged 4 to 11 years.
| Reaction |
Percent Incidence |
| Central Nervous System |
|
| Headache |
3% |
| Nervousness |
1% |
| Lightheadedness |
<1% |
| Tremor |
<1% |
| Agitation |
1% |
| Nightmares |
1% |
| Hyperactivity |
1% |
| Aggressive Behavior |
1% |
| Gastrointestinal |
|
| Nausea and/or Vomiting |
6% |
| Stomachache |
3% |
| Diarrhea |
1% |
| Oropharyngeal |
|
| Throat Irritation |
6% |
| Discoloration of Teeth |
1% |
| Respiratory |
|
| Epistaxis |
3% |
| Cough |
2% |
| Musculoskeletal |
|
| Muscle Cramp |
1% |
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.
OVERDOSAGE
id: 95B0F124-B7F8-1E77-E2F7-17E1C8C0CC4B
displayName: OVERDOSAGE SECTION
FDA Article Code: 34088-5
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.
DOSAGE AND ADMINISTRATION
id: ABD1510C-AA9A-1A78-A98A-F86DCE2994E8
displayName: DOSAGE & ADMINISTRATION SECTION
FDA Article Code: 34068-7
For treatment of acute episodes of bronchospasm or prevention of asthmatic symptoms, the usual dosage for adults and pediatric patients 4 years and older is 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.
HOW SUPPLIED
id: 8FA8E51F-EEC0-8E22-480A-BDAAC5A8086E
displayName: HOW SUPPLIED SECTION
FDA Article Code: 34069-5
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.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.Shake well before using.Note: The indented statement below is required by the Federal government Clean Air Act for all products containing chlorofluorocarbons (CFC’s).
WARNING: This product contains trichloromonofluoro-methane and dichlorodifluoromethane (CFC’s), substances which harm public health and environment by destroying ozone in the upper atmosphere.A notice similar to the above warning has been placed in the patient instruction leaflet of this package insert pursuant to the regulations of the U.S. Environmental Protection Agency (EPA). The patient’s warning states that the patient should consult his or her physician if there are questions about alternatives.
