Metaproterenol Sulfate

It is very important that you use the metaproterenol inhaler or nebulizer properly, so that the medicine gets into the lungs. Your doctor may want you to use a spacer with the inhaler. Talk to your doctor about proper inhaler and nebulizer use.

Seek medical attention if you notice that you require more than your usual or more than the maximum amount of any asthma medication in a 24-hour period. An increased need for medication could be an early sign of a serious asthma attack.

Your pharmacist has additional information about metaproterenol written for health professionals that you may read.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Bronchodilator; less selective than relatively selective β2-adrenergic agonists (e.g., albuterol).b c f h i j k

General

• Adjust dosage carefully according to individual requirements and response.146 c f g

Administration

Administer orally146 f or by oral inhalation via metered-dose inhaler or nebulizer.145 c

Oral Inhalation

Oral inhalation aerosol delivers approximately 0.65 mg from mouthpiece per metered spray; 7-g or 14-g canister delivers 100 or 200 metered sprays, respectively.c

Administer inhalation aerosol only with actuator provided by manufacturer.d

Shake the inhaler well before use.d

Avoid spraying aerosol into eyes.d

Place the mouthpiece of the inhaler well into the mouth with lips closed around it.d Exhale through nose as completely as possible.d Inhale slowly and deeply through mouth.d Actuate aerosol inhaler, hold breath for few seconds, withdraw mouthpiece, and exhale slowly.d

Allow ≥2 minutes to elapse between inhalations from aerosol inhaler.d

Clean inhalation aerosol inhaler by removing metal canister and running warm water through plastic mouthpiece.d If soap used, rinse thoroughly with plain water.d

Dosage

Available as metaproterenol sulfate; dosage expressed in terms of metaproterenol sulfate.145 c f

Pediatric Patients

Oral solution in children <6 years of age (limited experience): 1.3–2.6 mg/kg daily.f

Oral solution in children 6–9 years of age or those weighing <27.3 kg: Usually, 10 mg 3 or 4 times daily.f

Conventional tablets in children 6–9 years of age or those weighing <27.3 kg: Usually, 10 mg 3 or 4 times daily.146

Oral solution in children >9 years of age or those weighing >27.3 kg: Usually, 20 mg 3 or 4 times daily.f

Conventional tablets in children >9 years of age or those weighing >27.3 kg: Usually, 20 mg 3 or 4 times daily.146

Inhalation aerosol in children ≥12 years of age: 1.3 or 1.95 mg (2 or 3 inhalations).c Usually no need to repeat dosing more often than every 3–4 hours.c d If necessary, additional inhalations may be used, with dosage not exceeding 7.8 mg (12 inhalations) in any 24-hour period.c d

0.4 or 0.6% inhalation solution for nebulization in children ≥12 years of age: 10 or 15 mg (contents of 1 vial of 0.4 or 0.6% solution for nebulization, respectively) 3 or 4 times daily.145 Usually no need to repeat dosing more often than every 4 hours.145 g

Adults

Usually, 20 mg 3 or 4 times daily.146 f

Inhalation aerosol: 1.3 or 1.95 mg (2 or 3 inhalations).c Usually no need to repeat dosing more often than every 3–4 hours.d If necessary, additional inhalations may be used, with dosage not exceeding 7.8 mg (12 inhalations) in any 24-hour period.c d

0.4 or 0.6% inhalation solution for nebulization: 10 or 15 mg (contents of 1 vial of 0.4 or 0.6% solution for nebulization, respectively) 3 or 4 times daily.145 Usually no need to repeat dosing more often than every 4 hours.145 g

Inhalation aerosol: 1.3 or 1.95 mg (2 or 3 inhalations).c Usually no need to repeat dosing more often than every 3–4 hours.d If necessary, additional inhalations may be used, with dosage not exceeding 7.8 mg (12 inhalations) in any 24-hour period.c d

0.4 or 0.6% inhalation solution for nebulization: 10 or 15 mg (contents of 1 vial of 0.4 or 0.6% solution for nebulization, respectively) 3 or 4 times daily.145 Usually no need to repeat dosing more often than every 4 hours.145 g

Prescribing Limits

Pediatric Patients

Inhalation aerosol in children ≥12 years of age: Maximum ≤7.8 mg (≤12 inhalations) total daily dosage.c

Adults

Inhalation aerosol: Maximum ≤7.8 mg (≤12 inhalations) total daily dosage.d

Inhalation aerosol: Maximum ≤7.8 mg (≤12 inhalations) total daily dosage.d

Absorption

Bioavailability

Oral bioavailability about 10%.f h

Onset

Oral inhalation aerosol: ≤1 minute.b

Oral: ≤15–30 minutes.146 b

Oral inhalation solution: ≤5–30 minutes.b g

Oral or oral inhalation: Peak effect ≤1 hour.b

Duration

Oral: ≤4 hours for oral solution and ≥4 hours for tablets.146 f

Oral inhalation aerosol: About 1–2.5 hours.c

Oral inhalation solution: 4–6 hours.g

Bronchodilating effect of metaproterenol persists for ≥1 hour longer than that of equipotent doses of isoproterenol.b

Distribution

Extent

Not known if metaproterenol is distributed into milk.c

Plasma Protein Binding

Approximately 10–15%.i

Elimination

Metabolism

Following oral administration, extensively metabolized in GI tract to sulfate conjugate.c i Following oral inhalation, may be excreted as glucuronic acid conjugates.145 147

Elimination Route

Oral: Excreted in urine (approximately 40%) mostly as sulfate metabolite.147 f i

Half-life

Biphasic: Terminal half-life 1.5–6 hours.h i

Storage

Oral

Tight, light-resistant containers at 15–30°C.146 f Protect from moisture.146

Oral Inhalation

Oral inhalation aerosol: 15–25°C; avoid excessive humidity.c

Oral inhalation solution: ≤25°C.145 Discard solution if pinkish or darker than slightly yellow in color or if it contains a precipitate.g

• Importance of adherence to dosing schedules of metaproterenol and concomitant therapy, including not exceeding recommended dosage or frequency of use unless otherwise instructed by a clinician.b f

• Importance of using extreme care when considering administration of additional sympathomimetic agents.f Importance of allowing a sufficient interval of time to elapse before administering another sympathomimetic agent.f (See Specific Drugs under Interactions.)

• Importance of contacting clinician if asthmatic symptoms worsen or adverse reactions or diminished response occurs with usual dosage;b f g do not increase dose or frequency of administration.c f

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.c

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.c

• Importance of advising patients of other important precautionary information.146 c f g (See Cautions.)

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name