METAPROTERENOL SULFATE- metaproterenol sulfate syrup

United States - English - NLM (National Library of Medicine)

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Active ingredient:
METAPROTERENOL SULFATE (UNII: GJ20H50YF0) (METAPROTERENOL - UNII:53QOG569E0)
Available from:
Lannett Company, Inc.
INN (International Name):
METAPROTERENOL SULFATE
Composition:
METAPROTERENOL SULFATE 10 mg in 5 mL
Administration route:
ORAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
Metaproterenol sulfate syrup is indicated as a bronchodilator for bronchial asthma and for reversible bronchospasm which may occur in association with bronchitis and emphysema. Use in patients with cardiac arrhythmias associated with tachycardia is contraindicated. Although rare, immediate hypersensitivity reactions can occur. Therefore, metaproterenol sulfate syrup is contraindicated in patients with a history of hypersensitivity to any of its components.
Product summary:
Metaproterenol Sulfate Syrup, USP is available as a red, cherry-flavored syrup containing 10 mg of metaproterenol sulfate per teaspoonful (5 mL) in 473 mL (one pint) bottles. Store below 86°F (30°C). Protect from light. Manufactured by: Silarx Pharmaceuticals, Inc. 1033 Stoneleigh Ave Carmel, NY 10512
Authorization status:
Abbreviated New Drug Application
Authorization number:
54838-507-80

METAPROTERENOL SULFATE- metaproterenol sulfate syrup

Lannett Company, Inc.

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Metaproterenol Sulfate Syrup, USP

DESCRIPTION

Metaproterenol sulfate syrup is an oral bronchodilator.

Each teaspoonful (5 mL), for oral administration, contains metaproterenol sulfate 10 mg. In addition,

each teaspoonful (5 mL) contains the following inactive ingredients:

citric acid, edetate disodium, FD&C Red No. 40, glycerin, hydroxyethyl cellulose, black cherry flavor,

propylene glycol, saccharin sodium, sodium benzoate, sorbitol solution, sodium citrate and purified

water.

Metaproterenol sulfate, 1- (3, 5 dihydroxyphenyl) -2-isopropyl - aminoethanol sulfate, is a white,

crystalline, racemic mixture of two optically active isomers. It has the following structural formula:

CLINICAL PHARMACOLOGY

In vitro studies and in vivo pharmacologic studies have demonstrated that metaproterenol sulfate 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, recent data

indicate that there is a population of beta receptors in the human heart existing in a concentration

between 10 to 50%. The precise function of these, however, is not yet established (see WARNINGS

section).

The pharmacologic effects of beta adrenergic agonist drugs, including metaproterenol, are at least in

part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the

enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’ -adenosine

monophosphate (c-AMP). Increased c-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.

PHARMACOKINETICS: Absorption, biotransformation and excretion studies in humans following

oral administration have indicated that an average of less than 10% of the drug is absorbed intact; it is

not metabolized by catechol-0-methyltransferase nor converted to glucuronide conjugates but is

excreted primarily as the sulfate conjugate formed in the gut.

Pulmonary function tests performed after the administration of metaproterenol usually show

improvement, e.g., an increase in the one-second forced expiratory volume (FEV ), maximum expiratory

flow rate, peak expiratory flow rate, forced vital capacity, and/or a decrease in airway resistance. The

resultant decrease in airway obstruction may relieve the dyspnea associated with bronchospasm.

Pulmonary function has been monitored in controlled single- and multiple-dose studies. The duration of

effect of a single dose of metaproterenol sulfate syrup (that is, the period of time during which there is

a 15% or greater increase in mean FEV ) was up to 4 hours. Recent studies in laboratory animals

(minipigs, rodents and dogs) recorded the occurrence of cardiac arrhythmias and sudden death (with

histologic evidence of myocardial necrosis) when beta agonists and methylxanthines were administered

concurrently. The significance of these findings when applied to humans is currently unknown.

INDICATIONS AND USAGE

Metaproterenol sulfate syrup is indicated as a bronchodilator for bronchial asthma and for reversible

bronchospasm which may occur in association with bronchitis and emphysema.

CONTRAINDICATIONS

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

Although rare, immediate hypersensitivity reactions can occur. Therefore, metaproterenol sulfate syrup

is contraindicated in patients with a history of hypersensitivity to any of its components.

WARNINGS

Metaproterenol, 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.

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. Metaproterenol should not be used more often than prescribed. If

symptoms persist, patients should consult a physician promptly.

Drug Interactions: Other beta adrenergic bronchodilators should not be used concomitantly with

metaproterenol because they may have additive effects. Beta adrenergic agonist 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.

Pregnancy: Teratogenic Effects: PREGNANCY CATEGORY C: Metaproterenol sulfate has been

shown to be teratogenic and embryotoxic in rabbits when given in doses corresponding to 62 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,

embryotoxic or fetotoxic effects. There are no adequate and well-controlled studies in pregnant

women. 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 metaproterenol is excreted in human milk; therefore,

metaproterenol should be used during nursing only if the potential benefit justifies the possible risk to

the newborn.

Pediatric Use: Safety and effectiveness in children below the age of 6 have been demonstrated in a

limited number of patients. See DOSAGE AND ADMINISTRATION section.

ADVERSE REACTIONS

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

The following table of adverse experiences is derived from 44 clinical trials involving 1,120 patients

treated with metaproterenol sulfate syrup:

Metaproterenol Sulfate Syrup Incidence of Adverse

Events Occurring in at least 1% of Patients

Adverse Experience

Incidence

Number of Patients %

Cardiovascular

Tachycardia

Central Nervous System

Headache

Nervousness

Gastrointestinal

Nausea

Musculoskeletal

Tremor

OVERDOSAGE

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.

The treatment consists of discontinuation of metaproterenol together with appropriate symptomatic

therapy.

DOSAGE AND ADMINISTRATION

Metaproterenol sulfate syrup contains 10 mg of metaproterenol sulfate per teaspoonful (5 mL).

Children: Aged six to nine years or weight under 60 lb - one teaspoonful (5 mL) three or four times a

day. Children over nine years or weight over 60 lb - two teaspoonfuls (10 mL) three or four times a

day. Clinical trial experience in children under the age of six is limited. Of 40 children treated with

metaproterenol sulfate syrup for at least one month, daily doses of approximately 1.3 to 2.6 mg/kg were

well tolerated.

Adults: Two teaspoonfuls (10 mL) three or four times a day.

It is recommended that the physician titrate the dosage according to each individual patient’s response to

therapy.

HOW SUPPLIED

Metaproterenol Sulfate Syrup, USP is available as a red, cherry-flavored syrup containing 10 mg of

metaproterenol sulfate per teaspoonful (5 mL) in 473 mL (one pint) bottles.

Store below 86°F (30°C). Protect from light.

Manufactured by:

Silarx Pharmaceuticals, Inc.

1033 Stoneleigh Ave

Carmel, NY 10512

METAPROTERENOL SULFATE

metaproterenol sulfate syrup

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:548 38 -50 7

Lannett Company, Inc.

Route of Administration

ORAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

METAPRO TERENO L SULFATE (UNII: GJ20 H50 YF0 ) (METAPROTERENOL -

UNII:53QOG56 9 E0 )

METAPROTERENOL

SULFATE

10 mg

in 5 mL

Inactive Ingredients

Ingredient Name

Stre ng th

ANHYDRO US CITRIC ACID (UNII: XF417D3PSL)

EDETATE DISO DIUM (UNII: 7FLD9 1C8 6 K)

GLYCERIN (UNII: PDC6 A3C0 OX)

HYDRO XYETHYL CELLULO SE ( 2 0 0 0 CPS AT 1%) (UNII: S38 J6 RZN16 )

PRO PYLENE GLYCO L (UNII: 6 DC9 Q16 7V3)

SACCHARIN SO DIUM (UNII: SB8 ZUX40 TY)

SO DIUM BENZO ATE (UNII: OJ245FE5EU)

SO RBITO L (UNII: 50 6 T6 0 A25R)

SO DIUM CITRATE (UNII: 1Q73Q2JULR)

WATER (UNII: 0 59 QF0 KO0 R)

FD&C RED NO . 4 0 (UNII: WZB9 127XOA)

Product Characteristics

Color

S core

S hap e

S iz e

Flavor

CHERRY (Black Cherry)

Imprint Code

Contains

Packag ing

#

Item Code

Package Description

Marketing Start

Date

Marketing End

Date

1

NDC:548 38 -50 7-

473 mL in 1 BOTTLE, PLASTIC; Type 0 : No t a Co mbinatio n

Pro duc t

0 9 /0 8 /20 0 9

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA0 736 32

0 9 /0 8 /20 0 9

Labeler -

Lannett Company, Inc. (161630033)

Revised: 6/2014

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