Trade Name: Alupent

Generic Name: Metaproterenol sulfate

Dosage Form: Inhalation Solution

Classification: Spympathomimetic

 

 

Metaproterenol Sulfate Inhalation Solution is a bronchodilator administered by oral inhalation. It contains 0.4% or 0.6% Metaproterenol sulfate in a sterile, acidic, aqueous solution containing edetate disodium, sodium chloride, hydrochloric acid and/or sodium hydroxide for pH adjustment.

 

 

Metaproterenol Sulfate is a potent beta-adrenergic stimulator with a rapid onset of action. It is claimed that beta-adrenergic stimulants produce many of their pharmacological effects by activation of adenyl cyclase, the enzyme which catalyzes the conversion of adrenosine triphosphate to cyclic adenosine monosphosphate. Following oral administration in humans, an average of 40% of the drug is absorbed; it is not metabolized by catechol-O-methyltransferase but is excreted primarily as glucuronic acid conjugates.

 

 

Metaproterenol Sulfate Inhalation Solution is indicated as a bronchodilator for bronchial asthma and for reversible bronchospasm which may occur in association with bronchitis and emphysema.

Following controlled single dose studies by hand bulb nebulizers, significant improvement occurred within 5 to 30 minutes and persisted for periods varying from 2 to 6 hours.

 

 

Use in patients with cardiac arrhythmias associated with tachycardia is contraindicated. Although rare, immediate hypersensitivity reactions can occur. Therefore, Metaproterenol Sulfate Inhalation Solution is contraindicated in patients with a history of hypersensitivity to any of its components.

 

 

Adverse reactions are similar to those noted with other sympathomimetic agents.

The most frequent adverse reactions to Metaproterenol sulfate are nervousness, tremors, and nausea. Less frequent adverse reactions are hypertension, palpitations, vomiting and bad taste. Adverse reactions would be present with an overdose. Overdose reactions usually do not require treatment other than reduction of dosage and/or frequency of administration. Excessive use of adrenergic aerosols is potentially dangerous. Fatalities have been reported following excessive use of Metaproterenol sulfate as with other sympathomimetic inhalation preparations, and the exact cause is unknown. Cardiac arrest occurred in several cases.

 

 

Because Metaproterenol Sulfate Inhalation Solution is a sympathomimetic drug, it should be used with caution in patients with hypertension, coronary artery disease, congestive heart failure, hyperthyroidism or diabetes, or when there is sensitivity to sympathomimetic amines.

There are no adequate and well-controlled studies in pregnant women. Metaproterenol Sulfate Inhalation Solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Metaproterenol Sulfate Inhalation Solution is administered to a nursing woman.

Safety and effectiveness in children below the age of 12 have not been established.

 

 

A beta-blocker such as atenolol (Tenormin), metoprolol (Lopressor, Toprol XL), propranolol (Inderal), and others;

 

A tricyclic antidepressant such as amitriptyline (Elavil), doxepin (Sinequan), imipramine (Tofranil), nortriptyline (Pamelor), and others;

 

A monoamine oxidase inhibitor (MAOI) such as isocarboxazid (Marplan), phenelzine (Nardil), or tranylcypromine (Parnate);

 

Another inhaled oral bronchodilator, caffeine, diet pills, or decongestants.

 

 

Metaproterenol Sulfate Inhalation Solution is for administration with the aid of an air driven nebulizer. The usual adult dose is one vial per nebulization treatment. Usually, treatment need not be repeated more often than every four hours to relieve acute attacks of bronchospasm. As part of a total treatment program in chronic bronchospastic pulmonary diseases, Metaproterenol Sulfate Inhalation Solution may be administered three or four times a day.

 

 

0.6% Metaproterenol Sulfate Inhalation Solution, 2.5 mL vials. Equivalent to 0.3 mL Metaproterenol Sulfate Inhalation Solution 5% diluted to 2.5 mL Normal Saline. Total contents 15 mg of Metaproterenol Sulfate.

0.4% Metaproterenol Sulfate Inhalation Solution, 2.5 mL vials. Equivalent to 0.2 mL Metaproterenol Sulfate Inhalation Solution 5% diluted to 2.5 mL with Normal Saline. Total contents 10 mg of Metaproterenol Sulfate.