Alupent

Alupent information, interactions and side effects, Alupent (metaproterenol sulfate USP) Inhalation Aerosol is a bronchodilator administered by oral inhalation. The Alupent Inhalation Aerosol containing 75 mg of metaproterenol sulfate as micronized powder is sufficient medication for 100 inhalations. The Alupent (metaproterenol sulfate) Inhalation Aerosol containing 150 mg of metaproterenol sulfate as micronized powder is sufficient medication for 200 inhalations. Each metered dose delivers through the mouthpiece 0.65 mg of metaproterenol sulfate (each ml contains 15 mg). The inert ingredients are dichlorodifluoromethane, dichlorotetrafluoroethane and trichloromonofluoromethane as propellants, and sorbitan trioleate. Alupent (metaproterenol sulfate) , 1-(3,5-dihydroxyphenyl)-2-isopropylaminoethanol sulfate, is a white, crystalline, racemic mixture of two optically active isomers. It has the following chemical structure:

Alupent

INDICATIONS

Alupent® (metaproterenol sulfate USP) is indicated as a bronchodilator for bronchial asthma and for reversible bronchospasm which may occur in association with bronchitis and emphysema.

DOSAGE AND ADMINISTRATION

The usual single dose is two to three inhalations. With repetitive dosing, inhalation should usually not be repeated more often than about every three to four hours. Total dosage per day should not exceed 12 inhalations.

Alupent (metaproterenol sulfate USP) Inhalation Aerosol is not recommended for children under 12 years of age. It is recommended that the physician titrate dosage according to each individual patient’s response to therapy.

HOW SUPPLIED

Each 100 inhalations of Alupent (metaproterenol sulfate USP) Inhalation Aerosol contains 75 mg of metaproterenol sulfate as a micronized powder in inert propellants. Each metered dose delivers through the mouthpiece 0.65 mg metaproterenol sulfate (each ml contains 15 mg). Alupent (metaproterenol sulfate) Inhalation Aerosol with Mouthpiece (NDC 0597-0070-08), net contents 7g (5 ml). The mouthpiece is white with a clear, colorless sleeve and a blue protective cap.

Each 200 inhalations of Alupent (metaproterenol sulfate) Inhalation Aerosol contains 150 mg of metaproterenol sulfate as a micronized powder in inert propellants. Each metered dose delivers through the mouthpiece 0.65 mg metaproterenol sulfate (each ml contains 15 mg). Alupent (metaproterenol sulfate) Inhalation Aerosol with Mouthpiece (NDC 0597-0070-17), net contents 14g (10ml). The mouthpiece is white with a clear, colorless sleeve and a blue protective cap. Alupent (metaproterenol sulfate) Inhalation Aerosol Refill (NDC 0597-0070-18), net contents 14g (10 ml). 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 trichloromonofluoromethane (CFC-11), dichlorodifluoromethane (CFC-12) and dichlorotetrafluoroethane (CFC-114), 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 information for the patient of this product 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.

Store between 59°F (15°C) and 77°F (25°C). Avoid excessive humidity.

SIDE EFFECTS

Adverse reactions are similar to those noted with other sympathomimetic agents. The most frequent adverse reaction to Alupent( (metaproterenol sulfate USP) administered by metered-dose inhaler among 251 patients in 90-day controlled clinical trials was nervousness. This was reported in 6.8% of patients. Less frequent adverse experiences, occurring in 1-4% of patients were headache, dizziness, palpitations, gastrointestinal distress, tremor, throat irritation, nausea, vomiting, cough and asthma exacerbation. Tachycardia occurred in less than 1% of patients.

DRUG INTERACTIONS

Other beta adrenergic aerosol bronchodilators should not be used concomitantly with Alupent( (metaproterenol sulfate USP) because they may have additive effects. Beta adrenergic agonists should be administered with caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, since the action of beta adrenergic agonists on the vascular system may be potentiated.

WARNINGS

Fatalities have been reported following excessive use of Alupent (metaproterenol sulfate USP) as with other sympathomimetic inhalation preparations, and the exact cause is unknown. Cardiac arrest was noted in several cases.

Alupent (metaproterenol sulfate) , like other beta adrenergic agonists, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or ECG changes. As with other beta adrenergic aerosols, Alupent (metaproterenol sulfate) can produce paradoxical bronchospasm (which can be life threatening). If it occurs, the preparation should be discontinued immediately and alternative therapy instituted.

Alupent (metaproterenol sulfate) should not be used more often than prescribed. Patients should be advised to contact their physician in the event that they do not respond to their usual dose of a sympathomimetic amine aerosol.

PRECAUTIONS

General

Extreme care must be exercised with respect to the administration of additional sympathomimetic agents.

Since metaproterenol is a sympathomimetic amine, it should be used with caution in patients with cardiovascular disorders, including ischemic heart disease, hypertension or cardiac arrhythmias, in patients with hyperthyroidism or diabetes mellitus, and in patients who are unusually responsive to sympathomimetic amines or who have convulsive disorders. Significant changes in systolic and diastolic blood pressure could be expected to occur in some patients after use of any beta adrenergic bronchodilator.

Information for Patients

Appropriate care should be exercised when considering the administration of additional sympathomimetic agents. A sufficient interval of time should elapse prior to administration of another sympathomimetic agent.

Carcinogenesis/Mutagenesis/Impairment of Fertility

In an 18-month study in mice, Alupent (metaproterenol sulfate) produced an increase in benign ovarian tumors in females at doses corresponding to 320 and 640 times the maximum recommended dose (based on a 50 kg individual). In a two-year study in rats, a non-significant incidence of benign leiomyomata of the mesovarium was noted at 640 times the maximum recommended dose. The relevance of the findings to man is not known. Mutagenic studies with Alupent (metaproterenol sulfate) have not been conducted. Reproduction studies in rats revealed no evidence of impaired fertility.

Pregnancy

Teratogenic Effects

PREGNANCY CATEGORY C:

Alupent (metaproterenol sulfate) has been shown to be teratogenic and embryotoxic in rabbits when given in doses corresponding to 640 times the maximum recommended dose. These effects included skeletal abnormalities, hydrocephalus and skull bone separation. Results of other studies in rabbits, rats or mice have not revealed any teratogenic, embryocidal or fetotoxic effects. There are no adequate and well-controlled studies in pregnant women. Alupent (metaproterenol sulfate) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether Alupent (metaproterenol sulfate) is excreted in human milk; therefore, Alupent (metaproterenol sulfate) should be used during nursing only if the potential benefit justifies the possible risk to the newborn.

Pediatric Use

Safety and effectiveness in the pediatric population below the age of 12 have not been established. Studies are currently under way in this age group.

OVERDOSE

The expected symptoms with overdosage are those of excessive beta-stimulation and/or any of the symptoms listed under adverse reactions, e.g. angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia.

Treatment consists of discontinuation of metaproterenol together with appropriate symptomatic therapy.

CONTRAINDICATIONS

Use in patients with cardiac arrhythmias associated with tachycardia is contraindicated.

Although rare, immediate hypersensitivity reactions can occur. Therefore, Alupent (metaproterenol sulfate USP) Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to any of its components.

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