Proguanil Omeprazole

CYP 2C19 Poor and extensive hydroxylators Mephenytoin Hexobarbital Omeprazole Proguanil, etc. Poor increased toxicity Extensive drug resistance... 

CYP2C19 CYP2D6 diazepam, imipramine, 5-mephenytoin, omeprazol, proguanil, propranolol codeine, debrisoquine, dextromethorphan, flecainide, paroxetine, perphenazine, thioridazine carbamazepine, rifampicin cimetidine, felbamate fluoxetine, paroxetine, quinidine... 

C19. V-Mcphenyloin, diazepam, phenytoin, omeprazole, indomethacin, impramine, propanolol, proguanil [S-Mephentoin (4 -OH)]... 

Substrates other than mephenytoin which have caused clinical disturbances in people with deficient CYP2C19 alleles include omeprazol (41), proguanil (42), and citalopram (43). Additional substrates listed (8) include clomipramine, imipramine, diazepam, and propanolol. 

Substrates for this enzyme include (R)-mephobarbital, moclobemide, proguanil, diazepam, omeprazole, and imipramine, which do not show obvious structural or... 

Probe drugs used for CYP2C19 phenotyping are mephenytoin, omeprazole and proguanil. The most currently used probe drug is omeprazole. 

CYP2C19 Benzodiazepines diazepam Antidepressants imipramine, amitriptyline, clomipramine, citalopram Others propranolol, hexobarbital, mephobarbital, proguanil, omeprazole, S-mephenytoin 2 no activity 23%-39% in Asians 13% in Caucasians 25% in African Americans 3 no activity 6%-10% in Asians 0% in others... 

Acetaminophen, aldrin, alfentanil, amiodarone, aminopyrine, amitriptyline, amprenavir, androstenedione,antipyrine, astemizole, benzphetamine, budesonide, carbamazepine, celecoxib, chlorpromazine, chlorzoxazone, cisapride, clarithromycin, clozapine, cocaine, codeine, cortisol, cyclophosphamide,cyclosporin, dapsone, delavirdine, dextromethorphan, digitoxin, diltiazem, diazepam, erythromycin, 17j3-estradiol, ethinylestradiol, etoposide, felbamate, fentanyl, flutamide, hydroxyarginine, ifosphamide, imipramine, indinavir, ketoconazole, lansoprazole, loratidine, losartan, lovastatin, (iS)"mephen3d in, methadone, mianserin, miconazole, mifepristone, nelfinavir, nevirapine, nicardipine, nifedipine, odansetron, omeprazole, orphenadrine, proguanil, propafenone, quinidine, quinine, rapamycin, retinoic acid, ritonavir, saquinavir, selegiline, serindole, sufentanil, sulfinpyrazone, tacrolimus, tamoxifen, tamsulosin, taxol, teniposide, terfenadine, tetrahydrocannabinol, theophylline, toremifene, triazolam, trimethadone, trimethoprim, troleandomycin, verapamil, warfarin, zatosetron, Zolpidem, zonisamide... 

A number of drags, for example proguanil (33.6.1) and omeprazole (33.4.1), are not active in their own right, but undergo activation in vivo. Sometimes, however, an active drug is deliberately converted into a protected, possibly inactive, form - a prodrug (esters are quite common), so as to give better absorption or protection from breakdown, for example in the stomach. It does, of course, require a mechanism for re-activation, possibly an enzymatic conversion, at the site of action. 

CYP2C19 Mephenytoin, omeprazole, hexobarbital, mephobarbital, propranolol, proguanil, phenytoin Peptic ulcer response to omeprazole... 

Cimetidine and omeprazole increase the gastric pH, which may lead to an increase in the absorption of proguanil. Cimetidine and omeprazole are also thought to inhibit the metabolism of proguanil, due to their inhibitory effects on cytochrome P450 isoenzyme CYP2C19. 

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