Albuterol (Albuterol) Sulfate Syrup contains Albuterol (Albuterol) sulfate, USP, the racemic form of Albuterol (Albuterol) and a relatively selective beta-adrenergic bronchodilator. Albuterol (Albuterol) sulfate has the chemical name (±)α-[(-butylamino) methyl]-4-hydroxy--xylene-a,a'-diol sulfate (2:1) (salt), and the following chemical structure:

Albuterol (Albuterol) sulfate has a molecular weight of 576.70 and the molecular formula (CHNO) o HSO. Albuterol (Albuterol) sulfate is a white or practically white powder freely soluble in water and slightly soluble in alcohol, in chloroform, and in ether per USP definition.

The World Health Organization recommended name for Albuterol (Albuterol) base is salbutamol.

Each 5 mL (teaspoonful), for oral administration contains 2.4 mg of Albuterol (Albuterol) sulfate equivalent to 2 mg of Albuterol (Albuterol) . Albuterol (Albuterol) Sulfate Syrup also contains the inactive ingredients citric acid anhydrous, FD & C Yellow No. 6, hydroxypropyl methylcellulose, orange flavor, purified water, saccharin, sodium benzoate, and sodium citrate.

The pH of the syrup is 3.5 to 4.5.

The pharmacologic effects of beta-adrenergic agonist drugs, including Albuterol (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 (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.

Albuterol (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--methyl transferase.

Albuterol (Albuterol) Sulfate Syrup is indicated for the relief of bronchospasm in adults and children 2 years of age and older with reversible obstructive airway disease.

Albuterol (Albuterol) Sulfate Syrup is contraindicated in patients with a history of hypersensitivity to Albuterol (Albuterol) or any of its components.

Immediate hypersensitivity reactions may occur after administration of Albuterol (Albuterol) , as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema. Albuterol (Albuterol) , like other beta-adrenergic agonists, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes.

Rarely, erythema multiforme and Stevens-Johnson syndrome have been associated with the administration of Albuterol (Albuterol) sulfate in children.

Albuterol (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 (Albuterol) have been reported to aggravate preexisting diabetes mellitus and ketoacidosis. As with other beta-agonists, Albuterol (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.

In a 2-year study in Sprague-Dawley rats, Albuterol (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 ½, 2, and 10 times, respectively, the maximum recommended daily oral dose for adults and children, on a mg/m 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 (Albuterol) sulfate showed no evidence of tumorigenicity at dietary doses of up to 500 mg/kg (approximately 60 times the maximum recommended daily oral dose for adults and children on a mg/m basis). In a 22-month study in the Golden hamster Albuterol (Albuterol) sulfate showed no evidence of tumorigenicity at dietary doses of up to 50 mg/kg (approximately 8 times the maximum recommended daily oral dose for adults and children on a mg/m basis).

Albuterol (Albuterol) sulfate was not mutagenic in the Ames test with or without metabolic activation using tester strains TA1537, TA1538, and TA98 or WP2, WP2uvrA, and WP67. No forward mutation was seen in yeast strain S9 nor any mitotic gene conversion in yeast strain JD1 with or without metabolic activation. Fluctuation assays in TA98 and E. coli WP2, both with metabolic activation, were negative. Albuterol (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 up to 50 mg/kg (approximately 15 times the maximum recommended daily oral dose for adults on a mg/m2 basis).

In clinical trials, the most frequent adverse reactions to Albuterol (Albuterol) sulfate syrup in adults and older children were:

In clinical trials, the following adverse reactions to Albuterol (Albuterol) sulfate syrup were noted more frequently in young children 2 to 6 years of age than in older children and adults:

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 (Albuterol) sulfate syrup.

In addition, Albuterol (Albuterol) , like other sympathomimetic agents, can cause adverse reactions such as hypertension, angina, vomiting, vertigo, central nervous system stimulation, unusual taste, and drying or irritation of the oropharynx.

The reactions are generally transient in nature, and it is usually not necessary to discontinue treatment with Albuterol (Albuterol) Sulfate Syrup. In selected cases, however, dosage may be reduced temporarily; after the reaction has subsided, dosage should be increased in small increments to the optimal dosage.

To report SUSPECTED ADVERSE REACTIONS, contact Hi-Tech Pharmacal Co., Inc. at 1-800-262-9010 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under , e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and sleeplessness. Hypokalemia may also occur. As with all sympathomimetic medications, cardiac arrest and even death may be associated with abuse of Albuterol (Albuterol) sulfate syrup. Treatment consists of discontinuation of Albuterol (Albuterol) sulfate syrup 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 (Albuterol) sulfate syrup.

The oral median lethal dose of Albuterol (Albuterol) sulfate in mice is greater than 2000 mg/kg (approximately 240 times the maximum recommended daily oral dose for adults and children on a mg/m basis). In mature rats the subcutaneous (sc) median lethal dose of Albuterol (Albuterol) sulfate is approximately 450 mg/kg (approximately 110 times the maximum recommended daily oral dose for adults and children on a mg/m basis). In small young rats the oral median lethal dose is approximately 2000 mg/kg (approximately 480 times the maximum recommended daily oral dose for adults and children on a mg/m basis).

The following dosages of Albuterol (Albuterol) Sulfate Syrup are expressed in terms of Albuterol (Albuterol) base.

Albuterol (Albuterol) Sulfate Syrup, a yellow-orange liquid with an orange flavor, contains 2 mg Albuterol (Albuterol) NDC 21695-350-16 as the sulfate per 5 mL; bottles of 16 fluid ounces.

HI-TECH PHARMACAL CO., INC.

Amityville, NY 11701

Rev. 740:03 4/09

Repackaged by:

REBEL DISTRIBUTORS CORP

Thousand Oaks, CA 91320