View source for Metaproterenol

{{DrugProjectFormSinglePage
|authorTag={{AV}}
|genericName=Metaproterenol sulfate 
|aOrAn=a
|indicationType=treatment
|indication=[[bronchial asthma]] and for reversible [[bronchospasm]] which may occur in association with [[bronchitis]] and [[emphysema]].
|adverseReactions=[[hypertension]], [[palpitations]], [[tachyarrhythmia]], [[flushing]], [[nausea]], [[tremor]]
Psychiatric: Feeling nervous<!--Black Box Warning-->
|blackBoxWarningTitle=Title
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>

* Content

<!--Adult Indications and Dosage-->

<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult=
=====Bronchial asthma=====
*Metaproterenol sulfate tablets are indicated as a [[bronchodilator]] for [[bronchial asthma]] and for reversible [[bronchospasm]] which may occur in association with [[bronchitis]] and [[emphysema]].
======Dosing Information======
*Adults: The usual dose is 20 mg three or four times a day.

<!--Off-Label Use and Dosage (Adult)-->

<!--Guideline-Supported Use (Adult)-->
|offLabelAdultGuideSupport=
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.

<!--Non–Guideline-Supported Use (Adult)-->
|offLabelAdultNoGuideSupport=
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.

<!--Pediatric Indications and Dosage-->

<!--FDA-Labeled Indications and Dosage (Pediatric)-->
|fdaLIADPed=
=====Bronchial asthma=====
*Metaproterenol sulfate tablets are indicated as a [[bronchodilator]] for [[bronchial asthma]] and for reversible [[bronchospasm]] which may occur in association with [[bronchitis]] and [[emphysema]].
======Dosing Information======

*Children: Aged six to nine years or weight under 60 lbs - 10 mg three or four times a day. Over nine years or weight over 60 lbs - 20 mg three or four times a day. Metaproterenol sulfate tablets are not recommended for use in children under six years at this time. 

*It is recommended that the physician titrate the dosage according to each individual patient's response to therapy.
<!--Off-Label Use and Dosage (Pediatric)-->

<!--Guideline-Supported Use (Pediatric)-->
|offLabelPedGuideSupport=
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.

<!--Non–Guideline-Supported Use (Pediatric)-->
|offLabelPedNoGuideSupport=

There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.

<!--Contraindications-->
|contraindications=* Use in patients with cardiac [[arrhythmias]] associated with [[tachycardia]] is contraindicated.

*Although rare, immediate [[hypersensitivity]] reactions can occur. Therefore, metaproterenol sulfate tablets are contraindicated in patients with a history of [[hypersensitivity]] to any of its components.

<!--Warnings-->
|warnings=

====Precautions====

* 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]].

<!--Adverse Reactions-->

<!--Clinical Trials Experience-->
|clinicalTrials=Adverse reactions are similar to those noted with other [[sympathomimetic agents]].

The following table of adverse experiences is derived from 26 controlled clinical trials with 496 patients treated with metaproterenol sulfate tablets:

: [[File:{{PAGENAME}}02.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]


<!--Postmarketing Experience-->
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.


<!--Drug Interactions-->
|drugInteractions=* [[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.
<!--Use in Specific Populations-->
|FDAPregCat=C
|useInPregnancyFDA=*Teratogenic Effects: Metaproterenol sulfate has been shown to be [[teratogenic]] and embryotoxic in rabbits when given orally at doses of 100 mg/kg or 62 times the maximum recommended human oral dose. These effects included skeletal abnormalities, hydrocephalus and skull bone separation. [[Embryotoxicity]] has also been shown in mice when given orally at doses of 50 mg/kg or 31 times the maximum recommended human oral dose. Results of other oral reproduction studies in rats (40 mg/kg) and rabbits (50 mg/kg) 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.
|useInPregnancyAUS=There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=*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.
|useInPed=*Metaproterenol sulfate tablets are not recommended for use in children under six years of age because of insufficient clinical data to establish safety and effectiveness.
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with [[renal impairment]].
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with [[hepatic impairment]].
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are [[immunocompromised]].

<!--Administration and Monitoring-->
|administration=* Oral
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.



<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.

<!--Overdosage-->
|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.
<!--Pharmacology-->

<!--Drug box 2-->
|drugBox={{Drugbox
| Verifiedfields = changed
| verifiedrevid = 408782146
| IUPAC_name = (''RS'')-5-[1-hydroxy-2-(isopropylamino)ethyl]benzene-1,3-diol
| image = Orciprenaline skeletal.png
| width = 200px
| imagename = 1 : 1 mixture (racemate)
| drug_name = Orciprenaline
| image2 = Orciprenaline ball-and-stick.png

<!--Clinical data-->
| tradename =  
| Drugs.com = [http://www.drugs.com/monograph/metaproterenol-sulfate.html monograph]
| MedlinePlus = a682084
| pregnancy_AU = A
| pregnancy_US = C
| legal_US = Rx-only
| routes_of_administration = Inhalation / tablets

<!--Pharmacokinetic data-->
| bioavailability = 3% if inhaled, 40% if taken orally
| protein_bound =  
| metabolism = [[Gastrointestinal tract|Gastrointestinal]] and [[liver|hepatic]]
| elimination_half-life = 6 hours

<!--Identifiers-->
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 586-06-1
| ATC_prefix = R03
| ATC_suffix = AB03
| ATC_supplemental =  {{ATC|R03|CB03}}<br>{{ATC|R03|CB53}}
| PubChem = 4086
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = DB00816
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 3944
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 53QOG569E0
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08300
| ChEBI_Ref = {{ebicite|changed|EBI}} 
| ChEBI = 82719
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 776

<!--Chemical data-->
| C=11 | H=17 | N=1 | O=3 
| molecular_weight = 211.258 g/mol
| smiles = Oc1cc(cc(O)c1)C(O)CNC(C)C
| InChI = 1/C11H17NO3/c1-7(2)12-6-11(15)8-3-9(13)5-10(14)4-8/h3-5,7,11-15H,6H2,1-2H3
| InChIKey = LMOINURANNBYCM-UHFFFAOYAL
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C11H17NO3/c1-7(2)12-6-11(15)8-3-9(13)5-10(14)4-8/h3-5,7,11-15H,6H2,1-2H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = LMOINURANNBYCM-UHFFFAOYSA-N
| solubility = 9.7
}}<!--Mechanism of Action-->
|mechAction=* Metaproterenol sulfate is a beta adrenergic agonist [[bronchodilator]].

*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 mediators of immediate [[hypersensitivity]] from cells, especially from mast cells.
<!--Structure-->
|structure=*Metaproterenol sulfate in tablet form is an oral [[bronchodilator]].

*Each tablet, for oral administration, contains 10 mg or 20 mg of metaproterenol sulfate. In addition, each tablet contains the following inactive ingredients: colloidal silicon dioxide, corn starch, lactose anhydrous, magnesium stearate, microcrystalline cellulose and pregelatinized starch.
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: 

: [[File:{{PAGENAME}}01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]

<!--Pharmacodynamics-->
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.

<!--Pharmacokinetics-->
|PK=*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-O-methyltransferase]] nor converted to [[glucuronide]] conjugates but is excreted primarily as the polar sulfate conjugate, metaproterenol-3-O-sulfate, 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]] (FEV1), 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]].

*In controlled single- and multiple-dose studies in which 319 patients were treated with metaproterenol sulfate tablets (89 patients with 10 mg and 230 patients with 20 mg), a majority (65%) demonstrated improvements in pulmonary function defined as an increase of at least 15% in the one-second [[forced expiratory volume]] (FEV1). For 54% the onset was within 30 minutes. The duration of effect persisted for at least four hours in 51% of those patients who demonstrated a response.

*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.

<!--Nonclinical Toxicology-->
|nonClinToxic======Carcinogenesis and Mutagenesis and Impairment of Fertility=====

*In an 18-month study in mice, metaproterenol produced a significant increase in benign [[hepatic adenomas]] in males and benign ovarian tumors in females at doses corresponding to 31 and 62 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 62 times the maximum recommended dose. The relevance of these findings to man is not known. [[Mutagenicity]] studies with metaproterenol have not been conducted. Reproduction studies in rats revealed no evidence of impaired fertility.
<!--Clinical Studies-->
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.

<!--How Supplied-->
|howSupplied=* Metaproterenol sulfate tablets are supplied as follows:

:*10 mg: white, compressed, round, scored tablets, debossed "PAR 258" available in bottles of 100 (NDC #49884-258-01).

:*20 mg: white, compressed, round, scored tablets, debossed "PAR 259" available in bottles of 100 (NDC #49884-259-01).

<!--Patient Counseling Information-->
|storage=*Store at controlled room temperature 15°-30°C (59°-86°F). Protect from light and moisture
|fdaPatientInfo=*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.

<!--Precautions with Alcohol-->
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

<!--Brand Names-->
|brandNames=* Alupent
<!--Look-Alike Drug Names-->
|lookAlike=<!--Drug Shortage Status-->
|drugShortage=
}}
<!--Pill Image-->


<!--Label Display Image-->

{{LabelImage
|fileName={{PAGENAME}}03.png|This image is provided by the National Library of Medicine.
}}

{{LabelImage
|fileName={{PAGENAME}}04.png|This image is provided by the National Library of Medicine.
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{{LabelImage
|fileName={{PAGENAME}}05.png|This image is provided by the National Library of Medicine.
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<!--Category-->

[[Category:Drug]]