DESCRIPTION
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displayName: DESCRIPTION SECTION
FDA Article Code: 34089-3
Albuterol Sulfate Syrup contains albuterol sulfate, USP, the racemic form of albuterol and a relatively selective beta -adrenergic bronchodilator. Albuterol sulfate has the chemical name (±)α -[( -butylamino) methyl]-4-hydroxy- -xylene-a,a’-diol sulfate (2:1) (salt), and the following chemical structure:
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1
tert
m
Albuterol sulfate has a molecular weight of 576.70 and the molecular formula (C H NO ) o H SO . 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.
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The World Health Organization recommended name for albuterol base is salbutamol.
Each 5 mL (teaspoonful), for oral administration contains 2.4 mg of albuterol sulfate equivalent to 2 mg of 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.
CLINICAL PHARMACOLOGY
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displayName: CLINICAL PHARMACOLOGY SECTION
FDA Article Code: 34090-1
studies and pharmacologic studies have demonstrated that albuterol has a preferential effect on beta -adrenergic receptors compared with isoproterenol. While it is recognized that beta -adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta -receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established (see ).
In vitro
in vivo
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WARNINGS
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.
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.
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INDICATIONS AND USAGE
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displayName: INDICATIONS & USAGE SECTION
FDA Article Code: 34067-9
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.
CONTRAINDICATIONS
id: 7f28b474-75d8-4d8c-9339-290112670773
displayName: CONTRAINDICATIONS SECTION
FDA Article Code: 34070-3
Albuterol Sulfate Syrup is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.
ADVERSE REACTIONS
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displayName: ADVERSE REACTIONS SECTION
FDA Article Code: 34084-4
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.
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.
OVERDOSAGE
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displayName: SPL UNCLASSIFIED SECTION
FDA Article Code: 42229-5
The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under , 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 sulfate syrup. Treatment consists of discontinuation of 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 sulfate syrup.
ADVERSE REACTIONS
The oral median lethal dose of 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 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).
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DOSAGE AND ADMINISTRATION
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displayName: DOSAGE & ADMINISTRATION SECTION
FDA Article Code: 34068-7
The following dosages of Albuterol Sulfate Syrup are expressed in terms of albuterol base.
HOW SUPPLIED
id: 0e084235-dd8f-4bb1-b143-f0877d1f8d09
displayName: HOW SUPPLIED SECTION
FDA Article Code: 34069-5
NDC:17856-0740-3 in a CUP of 5 SYRUPS
ALBUTEROL SULFATE SYRUP
id: 310b9b50-e9e9-4592-969c-1738a4683181
displayName: PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
FDA Article Code: 51945-4
