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{{drugbox
__NOTOC__
| IUPAC_name = 1-(2,6-dimethylphenoxy)propan-2-amine
| image = Mexiletine_svg.png
| CAS_number = 31828-71-4
| ATC_prefix = C01
| ATC_suffix = BB02
| PubChem = 4178
| DrugBank = APRD00242
| C = 11 | H = 17 | N = 1 | O = 1
| molecular_weight = 179.259 g/mol
| bioavailability = 90%
| protein_bound = 50-60%
| metabolism = [[Liver|Hepatic]] ([[CYP2D6]] and [[CYP1A2|1A2]]- mediated)
| elimination_half-life = 10-12 hours
| excretion = [[Kidney|Renal]] (10%)
| pregnancy_AU = B1
| pregnancy_US = C
| legal_UK = POM
| legal_US = Rx-only
| routes_of_administration = Oral, [[Intravenous therapy|IV]]
}}


{{SI}}
{{Mexiletine}}
{{CMG}}


{{CMG}}; {{AE}} {{SS}]


'''''For patient information about Mexiletine, click [[Mexiletine (patient information)|here]].'''''
{{SB}} MEXILETINE HYDROCHLORIDE<sup>®</sup>
==Overview==


==Overview==
'''Mexiletine''' ([[International Nonproprietary Name|INN]], sold under the trade name '''Mexitil®''') belongs to the [[Class IB anti-arrhythmic]] group of medicines. It is used to treat [[arrhythmia]]s within the [[heart]] - or seriously irregular heartbeats. It slows nerve impulses in the heart and makes the heart tissue less sensitive. Dizziness, heartburn, nausea, nervousness, trembling, unsteadiness are common side effects. It is available in injection and capsule form.
'''Mexiletine''' ([[International Nonproprietary Name|INN]], sold under the trade name '''Mexitil®''') belongs to the [[Class IB anti-arrhythmic]] group of medicines. It is used to treat [[arrhythmia]]s within the [[heart]] - or seriously irregular heartbeats. It slows nerve impulses in the heart and makes the heart tissue less sensitive. Dizziness, heartburn, nausea, nervousness, trembling, unsteadiness are common side effects. It is available in injection and capsule form.


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Mexiletine may also be of use in patients experiencing refractory pain. (Sweetman, 2002) and is also effective for treating muscle stiffness resulting from [[myotonia congenita]] ([[Thomsen disease]])
Mexiletine may also be of use in patients experiencing refractory pain. (Sweetman, 2002) and is also effective for treating muscle stiffness resulting from [[myotonia congenita]] ([[Thomsen disease]])


==External links==
==Category==
* [http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202369.html MedlinePlus Drug Information: Mexiletine]
 
[[Sodium channel blockers]];[[Phenol ethers]];[[Cardiovascular Drugs]]
==FDA Package Insert==
 
====MEXILETINE HYDROCHLORIDE capsule====
 
'''  [[Mexiletine indications and usage|Indications and Usage]]'''
'''| [[Mexiletine dosage and administration|Dosage and Administration]]'''
'''| [[Mexiletine dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Mexiletine contraindications|Contraindications]]'''
'''| [[Mexiletine warnings and precautions|Warnings and Precautions]]'''
'''| [[Mexiletine adverse reactions|Adverse Reactions]]'''
'''| [[Mexiletine drug interactions|Drug Interactions]]'''
'''| [[Mexiletine use in specific populations|Use in Specific Populations]]'''
'''| [[Mexiletine overdosage|Overdosage]]'''
'''| [[Mexiletine description|Description]]'''
'''| [[Mexiletine clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Mexiletine nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Mexiletine clinical studies|Clinical Studies]]'''
'''| [[Mexiletine how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Mexiletine patient counseling information|Patient Counseling Information]]'''
'''| [[Mexiletine labels and packages|Labels and Packages]]'''
 
==Mechanism of Action==
 
Mexiletine hydrochloride is a local anesthetic, antiarrhythmic agent, structurally similar to lidocaine, but orally active. In animal studies, mexiletine has been shown to be effective in the suppression of induced ventricular arrhythmias, including those induced by glycoside toxicity and coronary artery ligation. Mexiletine, like lidocaine, inhibits the inward sodium current, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine decreased the effective refractory period (ERP) in Purkinje fibers. The decrease in ERP was of lesser magnitude than the decrease in action potential duration (APD), with a resulting increase in the ERP/APD ratio.


==References==
==References==
*{{cite book | author = Peck T | coauthors = Hill S, Williams M (eds.) | title = Pharmacology for Anaesthesia and Intensive Care | edition = 2nd ed. | publisher = Cambridge University Press | year = 2004 | id = ISBN 0-521-68794-2}}
*{{cite book | author = Sweetman S (ed.) | title = [[Martindale: The complete drug reference]] | edition = 33rd ed. | location = London | publisher = Pharmaceutical Press | year = 2002 | id = ISBN 0-85369-499-0}}


{{Antiarrhythmic agents}}
{{Reflist|2}}




{{Antiarrhythmic agents}}


[[Category:Antiarrhythmic agents]]
[[Category:Sodium channel blockers]]
[[Category:Phenol ethers]]
[[Category:Cardiovascular Drugs]]
[[Category:Drugs]]
[[Category:Drugs]]
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{{WikiDoc Sources}}

Revision as of 05:38, 3 March 2014


Mexiletine
MEXILETINE HYDROCHLORIDE® FDA Package Insert
Indications and Usage
Dosage and Administration
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
How Supplied/Storage and Handling
Labels and Packages
Clinical Trials on Mexiletine
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: {{SS}]

For patient information about Mexiletine, click here. Synonyms / Brand Names: MEXILETINE HYDROCHLORIDE®

Overview

Mexiletine (INN, sold under the trade name Mexitil®) belongs to the Class IB anti-arrhythmic group of medicines. It is used to treat arrhythmias within the heart - or seriously irregular heartbeats. It slows nerve impulses in the heart and makes the heart tissue less sensitive. Dizziness, heartburn, nausea, nervousness, trembling, unsteadiness are common side effects. It is available in injection and capsule form.

Class IB antiarrhythmics decrease action potential duration by shortening the repolarization phase. This is achieved by blocking sodium channels[2].

Mexiletine may also be of use in patients experiencing refractory pain. (Sweetman, 2002) and is also effective for treating muscle stiffness resulting from myotonia congenita (Thomsen disease)

Category

Sodium channel blockers;Phenol ethers;Cardiovascular Drugs

FDA Package Insert

MEXILETINE HYDROCHLORIDE capsule

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of Action

Mexiletine hydrochloride is a local anesthetic, antiarrhythmic agent, structurally similar to lidocaine, but orally active. In animal studies, mexiletine has been shown to be effective in the suppression of induced ventricular arrhythmias, including those induced by glycoside toxicity and coronary artery ligation. Mexiletine, like lidocaine, inhibits the inward sodium current, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine decreased the effective refractory period (ERP) in Purkinje fibers. The decrease in ERP was of lesser magnitude than the decrease in action potential duration (APD), with a resulting increase in the ERP/APD ratio.

References


Template:Antiarrhythmic agents

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