DrugindexOnline^{2nd edition}

Pronouncation: (MEH-tuh-pro-TEHR-uh-nahl SULL-fate)
Class: Sympathomimetic

Trade Names:
Alupent
- Aerosol 75 mg as micronized powder in inert propellant (100 inhalations). Each dose delivers 0.65 mg
- Aerosol 150 mg as micronized powder in inert propellant (200 inhalations). Each dose delivers 0.65 mg
- Solution for inhalation 0.4%
- Solution for inhalation 0.6%
- Solution for inhalation 5%

Mechanism of Action

Pharmacology

Relaxes bronchial smooth muscle through beta-2 receptor stimulation.

Pharmacokinetics

Absorption

Less than 10% is absorbed intact.

Metabolism

Metaproterenol sulfate is metabolized through sulfate conjugation in the GI tract. The major metabolite is metaproterenol-o-sulfate.

Elimination

Metaproterenol sulfate is excreted fecally.

Onset

Onset is approximately 30 min (oral) and 5 to 30 min (inhalation).

Peak

Time to peak effect is 30 to 90 min.

Duration

Duration is 3 to 6 h.

Indications and Usage

Treatment of bronchial asthma and reversible bronchospasm associated with bronchitis and emphysema; control of acute asthma attacks in children 6 yr of age and older (inhalation solution only).

Contraindications

Cardiac arrhythmias associated with tachycardia.

Dosage and Administration

Aerosol
Adults and Children (12 yr of age and older)

Inhalation 2 to 3 inhalations every 3 to 4 h, not to exceed 12 inhalations/day.

Hand Nebulizer
Adults and Children (12 yr of age and older)

Inhalation 5 to 15 inhalations every 4 h as needed.

Intermittent Positive Pressure Breathing Apparatus
Adults and Children (12 yr of age and older)

Inhalation 0.2 to 0.3 mL of 5% solution in 2.5 mL of diluent every 4 h as needed.

Nebulizer
Adults and Children (12 yr of age and older)

Inhalation 0.1 to 0.2 mL in saline to a total volume of 3 mL.

Storage/Stability

Store metered-dose inhaler in pressurized container at room temperature (59° to 86°F); do not freeze. Keep away from extreme heat. Do not use near open flame or discard in incinerator. Store solution for inhalation below 77°F.

Drug Interactions

MAOIs, tricyclic antidepressants

Pressor effects may be potentiated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations; hypertension; tachycardia; cardiac arrest; palpitations; tachycardia; BP changes/hypertension.

CNS

Tremor; dizziness; nervousness; weakness; headache; shakiness/nervousness/tension; drowsiness; insomnia.

Dermatologic

Rash.

EENT

Throat irritation; bad taste; taste/smell change.

GI

GI distress; nausea; vomiting; dry mouth.

Respiratory

Cough; asthma exacerbation; throat dryness/irritation; pharyngitis; asthma exacerbation; hoarseness; nasal congestion.

Miscellaneous

Fatigue; skin reaction.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

May be used in children 6 yr of age and older.

Elderly

Lower doses may be required.

Labor and Delivery

May inhibit uterine contractions and delay preterm labor.

Hypersensitivity

Hypersensitivity (allergic) reactions can occur after administration.

CNS effects

CNS stimulation may occur; use drug with caution in patients with history of seizures or hypothyroidism.

CV disorders

Toxic symptoms may occur.

Diabetes mellitus

Dosage adjustment of insulin or oral hypoglycemic agent may be required.

Excessive use

Paradoxical bronchospasm and cardiac arrest have been associated with excessive inhalant use.

Tolerance

May occur.

Overdosage

Symptoms

Tremor, palpitations, angina, arrhythmias, tachycardia, elevated or decreased BP, seizures, nervousness, headache, dry mouth, nausea, dizziness, fatigue, malaise, insomnia.

Patient Information

• Ask patient to demonstrate correct use of inhaler. It may be necessary to repeat instructions and demonstrations more than once.
• Instruct patient that if more than 1 inhalation is necessary, to wait at least 2 min between doses.
• Instruct patient to wash and dry inhaler every day in warm water.
• Explain that tolerance may occur with prolonged use, but temporary cessation of drug usually restores its original effectiveness. Instruct patient to notify health care provider if medication is ineffective.
• Warn patient to avoid excessive use (no more than every 4 h), which can lead to adverse reactions or loss of effectiveness.
• Advise patient to increase fluid intake to liquefy secretions.
• Instruct patient to report the following symptoms to health care provider: palpitations, nervousness, dizziness, shortness of breath, rash, asthma exacerbation.
• Caution patient to avoid getting aerosol medication in eyes.
• Advise patient to avoid smoke-filled rooms and smoking.
• Instruct patient to rinse mouth with water after each use.