DESCRIPTION
id: BDA57A2A-FD57-88E6-5F98-6F3FDB3D99A0
displayName: DESCRIPTION SECTION
FDA Article Code: 34089-3
The active component of Albuterol Inhalation Aerosol is albuterol, USP racemic α1-[(tert-butylamino)methyl]-4-hydroxy-m-xylene-α,α’-diol), a relatively selective beta2-adrenergic bronchodilator, having the chemical structure:The molecular weight of albuterol is 239.3, and the empirical 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. The World Health Organization recommended name for albuterol base is salbutamol.Albuterol Inhalation Aerosol is a pressurized metered-dose aerosol unit for oral inhalation. It contains a microcrystalline suspension of albuterol in propellants (trichloromonofluoromethane and dichlorodifluoromethane) with oleic acid. Each actuation delivers 100 mcg albuterol, USP from the valve and 90 mcg of albuterol, USP from the mouthpiece. Each 17.0 g canister provides 200 oral inhalations. Each 6.8 g canister provides 80 oral inhalations.Albuterol Inhalation Aerosol should be primed by actuating into air, away from the eyes and face, four times before using for the first time and two times when the aerosol has not been used for a period of at least four days.
CLINICAL PHARMACOLOGY
id: C85A4392-3FA1-FB81-B5C9-E65C480E171E
displayName: CLINICAL PHARMACOLOGY SECTION
FDA Article Code: 34090-1
The primary action of beta-adrenergic drugs, including albuterol, is to stimulate adenyl cyclase, the enzyme which catalyzes the formation of cyclic-3′,5′-adenosine monophosphate (cyclic AMP) from adenosine triphosphate (ATP) in beta-adrenergic cells. The cyclic AMP thus formed mediates the cellular responses. 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.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.In controlled clinical trials, albuterol has been shown 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 ECG 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 the propensity for increase in heart rate for albuterol is ½ to ¼ that of isoproterenol. In asthmatic patients similar cardiovascular differentiation between the two drugs was also seen.
INDICATIONS AND USAGE
id: AD0926D5-2AAB-12BB-DFE0-6E01C9D56C98
displayName: INDICATIONS & USAGE SECTION
FDA Article Code: 34067-9
Albuterol Inhalation Aerosol is indicated in patients 12 years of age and older, for the prevention and relief of bronchospasm in patients with reversible obstructive airway disease, and for the prevention of exercise-induced bronchospasm.
CONTRAINDICATIONS
id: 55F62E53-BF85-85D7-1036-A6419C2EBFD8
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: 8ACC45AB-952B-F8A6-CF7E-71DF35ACB215
displayName: ADVERSE REACTIONS SECTION
FDA Article Code: 34084-4
The adverse reactions of albuterol are similar in nature to those of other sympathomimetic agents, although the incidence of certain cardiovascular effects is less 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 aerosols in 147 asthmatic patients. (n=147)
| Adverse Event |
Albuterol Inhalation Aerosol |
Isoproterenol Inhaler |
| 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 |
Cases of urticaria, angioedema, rash, bronchospasm, hoarseness, oropharyngeal edema, and arrhythmias (including atrial fibrillation, supraventricular tachycardia, and extrasystoles) have also been reported after the use of inhaled albuterol. In addition, albuterol, like other sympathomimetic agents, can cause adverse reactions such as hypertension, angina, vomiting, vertigo, central nervous system stimulation, insomnia, headache, unusual taste, and drying or irritation of the oropharynx.
OVERDOSAGE
id: 3194AF94-7DEE-DC69-A637-5E3D93C70FCD
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, eg, angina, hypertension, tachycardia with rates up to 200 beats per minute, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, and insomnia. In addition, seizures, hypotension, arrhythmias, fatigue, malaise, and 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). In mature rats, the subcutaneous 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). In small young rats, the subcutaneous median lethal dose is approximately 2000 mg/kg (approximately 14,000 times the maximum recommended daily inhalation dose for adults and children on a mg/m2 basis). The inhalation median lethal dose has not been determined in animals.
HOW SUPPLIED
id: 6D1B2017-5A06-851D-FDD3-CA3AEC6BB551
displayName: HOW SUPPLIED SECTION
FDA Article Code: 34069-5
Albuterol Inhalation Aerosol, 17.0 g canister contains 200 metered inhalations, box of one (NDC 59930-1560-1). Each actuation delivers 100 mcg of albuterol from the valve and 90 mcg of albuterol from the mouthpiece. Each canister is supplied with a white plastic actuator with white dust cap, and Patient’s Instructions.Albuterol Inhalation Aerosol REFILL canister, 17.0 g, contains 200 metered inhalations, with Patient’s Instructions; box of one (NDC 59930-1560-2).The correct amount of medication in each inhalation cannot be assured after 200 actuations from the 17.0 g canister or 80 actuations from the 6.8 g canister even though the canister is not completely empty. The canister should be discarded when the labeled number of actuations have been used.Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F) [see USP Controlled Room Temperature]. Failure to use the product within this temperature range may result in improper dosing. For optimal results, the canister should be at room temperature before use. Shake well before using.Albuterol Inhalation Aerosol canister should be used only with the actuator provided. The white actuator should not be used with other aerosol medication canisters.Note: The indented statement below is required by the Federal government’s Clean Air Act for all products containing or manufactured with chlorofluorocarbons (CFCs).
WARNING: Contains dichlorodifluoromethane (CFC-12) and trichloromonofluoromethane (CFC-11), substances which harm public health and the environment by destroying ozone in the upper atmosphere.A notice similar to the above WARNING has been placed in the “Patient’s Instructions for Use” portion of this package insert under the Environmental Protection Agency’s (EPA’s) regulations. The patient’s warning states that the patient should consult his or her physician if there are questions about alternatives.
