Depression Symptoms Treatment

November 9th, 2009 by admin

Drug interactions: cytochrome P450. Part 5

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CYP2D6 Isoenzyme Metabolism

About 25% of all drugs used today are substrates for the CYP2D6 isozyme. This isozyme has been studied extensively. It greatly exhibits genetic polymorphism; certain individuals will lack this enzyme from birth as a result of an autosomal recessive defect in its expression. Individuals lacking CYP2D6 will have a much larger pharmacologic response to usual doses of drugs metabolized by this enzyme and will have a greater risk of adverse drug effects and/or toxicity. Conversely, prodrugs are usually inactive until enzymatic metabolism converts them to an active metabolite. Individuals will have little or no pharmacologic response to these drugs. CYP2D6 substrates include some tricyclic antidepressants, neuroleptics, antiarrhythmics, and b-adrenergic blockers. Inhibitors of CYP2D6 include tricyclics and SSRIs, and antiarrhythmics (particularly quinidine) and fluoxetine. CYP2D6 inducers include only a few drugs, primarily anticonvulsant agents. A more extensive listing of drugs involved with the CYP2D6 isoenzyme is shown in Table 2.

Table 2

Cytochrome P450 2D6 Enzyme
Substrates   Inducers Inhibitors
Amitripyline Methadone Carbamazepine Amiodarone
Bisoprolol Methamphetamine Phenobarbital Cimetidine
Captopril Metoprolol Phenytoin Citalopram
Cilostazol Mexiletine Rifampin Clomipramine
Chlorpheniramine Morphine Ritonavir Desipramine
Chlorpromazine Nefazodone   Fluoxetine
Citalopram Nelfinavir   Fluphenzine
Clomipramine Nortriptyline   Fluvoxamine
Clozapine Ondansetron   Haloperidol
Codeine Omeprazole   Methadone
Cyclobenzaprine Oxycodone   Mibefradil
Desipramine Paclitaxel   Moclobemide
Dexfenfluramine Paroxetine   Norfluoxetine
Dextromethorphan Perphenazine   Paroxetine
Donepezil Phenformin   Perphenazine
Doxepin Propafenone   Propafenone
Encainide Propranolol   Quinidine
Ethylmorphine Retinoic acid   Ritonavir
Fenfluramine Quinidine   Sertraline
Flecainide Risperidone   Thioridazine
Fluoxetine Ritonavir     
Fluphenazine RU486     
Haloperidol Tamoxifen     
Hydrocodone Testosterone     
Imipramine Timolol     
Indoramin Tramadol     
Labetalol Trazodone     
Lidocaine Trifluperidol     
Loratadine Trimipramine     
Maprotiline Venlafaxine     
(R)-methadone Vinblastine     
Meperidine        

Synonyms of Carbamazepine:

carbamazepine, Carbamezepine

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Therapeutic classes of Carbamazepine:

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Dosage forms of Carbamazepine:

Form Route Strength
Suspension Oral
Tablet Oral
Tablet, extended release Oral

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