ALBUTEROL SULFATE

Albuterol Sulfate Syrup contains albuterol sulfate, USP, the racemic form of albuterol and a relatively selective beta 2 -adrenergic bronchodilator. Albuterol sulfate has the chemical name α 1 -[( tert -butylamino)methyl]-4-hydroxy- m -xylene-α,α'-diolsulfate (2:1) (salt) and the following chemical structure: (C 13 H 21 NO 3 ) 2 •H 2 SO 4 M.W. 576.7 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 base is salbutamol. Albuterol Sulfate Syrup for oral administration contains 2 mg of albuterol as 2.4 mg of albuterol sulfate in each teaspoonful (5 mL). Albuterol Sulfate Syrup also contains the inactive ingredients purified water, hypromellose, citric acid anhydrous, sodium citrate dihydrate, sodium benzoate, sorbitol solution, strawberry flavor, and FD&C Yellow # 6. The pH of the syrup is 3.2 to 4.2. Albuterol Sulphate Chemical Structure

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.

The following dosages of albuterol sulfate syrup are expressed in terms of albuterol base. Usual Dosage Adults and Children Over 14 Years of Age: 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. Children Over 6 Years to 14 Years of Age: 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. Children 2 to 5 Years of Age: 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 Adults and Children Over 14 Years of Age: 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. 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: 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). Children 2 to 5 Years of Age Who Do Not Respond Satisfactorily to the Initial Dosage: 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. Elderly Patients and Those Sensitive to Beta-adrenergic Stimulators: The initial dosage should be restricted to 2 mg three or four times a day and individually adjusted thereafter.

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

In clinical trials, the most frequent adverse reactions to albuterol sulfate syrup in adults and older children were: Percent Incidence of Adverse Reactions in Adults and Children (6-14 Years of Age) Reaction Percent Incidence Central nervous system Tremor 10% Nervousness 9% Shakiness 9% Headache 4% Dizziness 3% Hyperactivity 2% Excitement 2% Sleeplessness 1% Disturbed sleep <1% Irritable behavior <1% Dilated pupils <1% Weakness <1% Cardiovascular Tachycardia 1% Palpitations <1% Sweating <1% Chest pain <1% Ear, nose, and throat Epistaxis 1% Gastrointestinal Increased appetite 3% Epigastric pain <1% Stomachache <1% Musculoskeletal Muscle spasm <1% Respiratory Cough <1% In clinical trials, the following adverse reactions to albuterol sulfate syrup were noted more frequently in young children 2 to 6 years of age than in older children and adults: Percent Incidence of Adverse Reactions Noted More Frequently in Children 2 to 6 Years of Age Than in Older Children and Adults Reaction Percent Incidence Central nervous system Excitement 20% Nervousness 15% Hyperkinesia 4% Sleeplessness 2% Emotional lability 1% Fatigue 1% Cardiovascular Tachycardia 2% Pallor 1% Gastrointestinal Gastrointestinal symptoms 2% Loss of Appetite 1% Ophthalmologic Conjunctivitis 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 sulfate syrup. In addition, 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 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.