Metaproterenol: Difference between revisions

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


* Content
* Content
Line 42: Line 16:


<!--FDA-Labeled Indications and Dosage (Adult)-->
<!--FDA-Labeled Indications and Dosage (Adult)-->
 
|fdaLIADAdult======Bronchial asthma=====
|fdaLIADAdult=
*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======
=====Condition1=====
*Adults: The usual dose is 20 mg three or four times a day.
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
* Dosing Information
 
:* Dosage
 
=====Condition3=====
 
* Dosing Information
 
:* Dosage
 
=====Condition4=====
 
* Dosing Information
 
:* Dosage


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


<!--Guideline-Supported Use (Adult)-->
<!--Guideline-Supported Use (Adult)-->
 
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.


<!--Non–Guideline-Supported Use (Adult)-->
<!--Non–Guideline-Supported Use (Adult)-->
 
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultNoGuideSupport=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.


<!--Pediatric Indications and Dosage-->
<!--Pediatric Indications and Dosage-->


<!--FDA-Labeled Indications and Dosage (Pediatric)-->
<!--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======


|fdaLIADPed=
*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.  
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.


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


<!--Guideline-Supported Use (Pediatric)-->
<!--Guideline-Supported Use (Pediatric)-->
 
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.


<!--Non–Guideline-Supported Use (Pediatric)-->
<!--Non–Guideline-Supported Use (Pediatric)-->
 
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedNoGuideSupport=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.


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


|contraindications=
*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.
 
* 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-->
|warnings=====Precautions====


|warnings=
* Extreme care must be exercised with respect to the administration of additional [[sympathomimetic agents]].
 
* Description
 
====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.
*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-->
<!--Adverse Reactions-->


<!--Clinical Trials Experience-->
<!--Clinical Trials Experience-->
 
|clinicalTrials=Adverse reactions are similar to those noted with other [[sympathomimetic agents]].
|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:
The following table of adverse experiences is derived from 26 controlled clinical trials with 496 patients treated with metaproterenol sulfate tablets:


table02
: [[File:{{PAGENAME}}02.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]


=====Dosage=====
*Adults: The usual dose is 20 mg three or four times a day.
*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. (Please refer to the CLINICAL PHARMACOLOGY section for further information on clinical experience with this product.)


*It is recommended that the physician titrate the dosage according to each individual patient's response to therapy.
<!--Postmarketing Experience-->
<!--Postmarketing Experience-->
 
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|postmarketing=
 
There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.




<!--Drug Interactions-->
<!--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.
|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-->
<!--Use in Specific Populations-->
 
|FDAPregCat=C
|useInPregnancyFDA=
|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.
*Teratogenic Effects: Pregnancy Category C: 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.
|useInPregnancyAUS=
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|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.
|useInLaborDelivery=
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|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.
|useInNursing=
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with [[renal impairment]].
*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.
|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.
|useInPed=
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are [[immunocompromised]].
*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 and Monitoring-->
|administration=* Oral
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.


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


* Description


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


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


<!--Drug box 2-->
<!--Drug box 2-->
|drugBox={{Drugbox2
| 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


|drugBox=
<!--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


<!--Mechanism of Action-->
<!--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


|mechAction=
<!--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]].


* 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.
 
*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-->
 
|structure=*Metaproterenol sulfate in tablet form is an oral [[bronchodilator]].
|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.
*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:  
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|600px|This image is provided by the National Library of Medicine.]]
: [[File:{{PAGENAME}}01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]


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


<!--Pharmacokinetics-->
<!--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.


|PK=
*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]].
*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.
*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.
*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-->
<!--Nonclinical Toxicology-->
|nonClinToxic======Carcinogenesis and Mutagenesis and Impairment of Fertility=====


|nonClinToxic=
*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.
=====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-->
<!--Clinical Studies-->
|clinicalStudies=
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
 
There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.


<!--How Supplied-->
<!--How Supplied-->
 
|howSupplied=* Metaproterenol sulfate tablets are supplied as follows:
|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).
:*10 mg: white, compressed, round, scored tablets, debossed "PAR 258" available in bottles of 100 (NDC #49884-258-01).
Line 332: Line 199:
:*20 mg: white, compressed, round, scored tablets, debossed "PAR 259" available in bottles of 100 (NDC #49884-259-01).
:*20 mg: white, compressed, round, scored tablets, debossed "PAR 259" available in bottles of 100 (NDC #49884-259-01).


*Store at controlled room temperature 15°-30°C (59°-86°F). Protect from light and moisture.
<!--Patient Counseling Information-->
<!--Patient Counseling Information-->
 
|storage=*Store at controlled room temperature 15°-30°C (59°-86°F). Protect from light and moisture
|fdaPatientInfo=
|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.
*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-->
<!--Precautions with Alcohol-->
 
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|alcohol=
 
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.


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


Latest revision as of 16:41, 20 August 2015

Metaproterenol
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Aparna Vuppala, M.B.B.S. [2]

Disclaimer

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Overview

Metaproterenol is a brochodilator that is FDA approved for the treatment of bronchial asthma and for reversible bronchospasm which may occur in association with bronchitis and emphysema. Common adverse reactions include hypertension, palpitations, tachyarrhythmia, flushing, nausea, tremor feeling nervous.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Bronchial asthma
Dosing Information
  • Adults: The usual dose is 20 mg three or four times a day.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Metaproterenol in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Metaproterenol in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Bronchial asthma
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

There is limited information regarding Off-Label Guideline-Supported Use of Metaproterenol in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Metaproterenol in pediatric patients.

Contraindications

  • 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

Precautions

Adverse Reactions

Clinical Trials Experience

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:

This image is provided by the National Library of Medicine.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Metaproterenol in the drug label.

Drug Interactions

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

  • 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.


Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Metaproterenol in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Metaproterenol during labor and delivery.

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

  • 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.

Geriatic Use

There is no FDA guidance on the use of Metaproterenol with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Metaproterenol with respect to specific gender populations.

Race

There is no FDA guidance on the use of Metaproterenol with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Metaproterenol in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Metaproterenol in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Metaproterenol in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Metaproterenol in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

There is limited information regarding Monitoring of Metaproterenol in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Metaproterenol in the drug label.

Overdosage

Pharmacology

Template:Px
Template:Px
1 : 1 mixture (racemate)Orciprenaline
Systematic (IUPAC) name
(RS)-5-[1-hydroxy-2-(isopropylamino)ethyl]benzene-1,3-diol
Identifiers
CAS number 586-06-1
ATC code R03AB03 R03CB03 (WHO)
R03CB53 (WHO)
PubChem 4086
DrugBank DB00816
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 211.258 g/mol
SMILES eMolecules & PubChem
Physical data
Solubility in water 9.7 mg/mL (20 °C)
Pharmacokinetic data
Bioavailability 3% if inhaled, 40% if taken orally
Metabolism Gastrointestinal and hepatic
Half life 6 hours
Excretion ?
Therapeutic considerations
Pregnancy cat.

A(AU) C(US)

Legal status

[[Prescription drug|Template:Unicode-only]](US)

Routes Inhalation / tablets

Mechanism of Action

  • 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

  • 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:

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Metaproterenol in the drug label.

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-O-methyltransferase nor converted to glucuronide conjugates but is excreted primarily as the polar sulfate conjugate, metaproterenol-3-O-sulfate, formed in the gut.
  • 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

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

There is limited information regarding Clinical Studies of Metaproterenol in the drug label.

How Supplied

  • 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).

Storage

  • Store at controlled room temperature 15°-30°C (59°-86°F). Protect from light and moisture

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

  • 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-Metaproterenol interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

  • Alupent

Look-Alike Drug Names

There is limited information regarding Metaproterenol Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.



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