Drug |
Metabolite |
Biotransformation |
Therapeutic action |
Atomoxetine |
4-Hydroxyatomoxetine |
Aromatic hydroxylation |
Treatment of attention-deficit
hyperactivity disorder |
Atorvastatin |
2- or 4-Hydroxyatorvastatin |
Anti-hypercholesterolemia |
Chlorpromazine |
7-Hydroxychlorpromazine |
Anti-depressive |
Clomiphene |
4-Hydroxyclomiphene |
Anti-uterotrophic |
Granisetron |
7-Hydroxygranisetron |
Anti-nausea |
Indapamide |
5-Hydroxyindapamide |
Anti-hypertensive |
Levamisole |
4-Hydroxylevamisole |
Anthelmintic |
Propafenone |
5-Hydroxypropafenone |
Anti-arrhythmic |
Propranolol |
4-Hydroxypropranolol |
Anti-arrhythmic |
Alprazolam |
4-Hydroxyalprazolam |
Aliphatic hydroxylation |
Anti-depressant |
Bupropion |
Hydroxybupropion |
Anti-mental depression |
Clarithromycin |
14-Hydroxyclarithromycin |
Anti-biotic |
Cyclosporin A |
Hydroxycyclosporin A |
Immunosuppressive |
Ibuprofen |
Hydroxyibuprofen |
Anti-inflammatory |
Itraconazole |
Hydroxyitraconazole |
Anti-mycotic |
Metronidazole |
Hydroxymetronidazole |
Anti-biotic |
Midazolam |
1′-Hydroxymidazolam |
Anxiolytic eŠect |
Nebivolol |
4- or 4′-Hydroxynebivolol |
Vasodilation |
Nefazodone |
Hydroxynefazodone |
Anti-depressant |
Praziquantel |
4-Hydroxypraziquantel |
Anti-neurocysticercosis |
Quinidine |
3-Hydroxyquinidine |
Anti-arrhythmic |
Risperidone |
9-Hydroxyrisperidone |
Anti-psychotic |
Simavastatin |
Simavastatinhydroxylic acid |
Anti-hypercholesterolemia |
Amiodarone |
Desethylamiodarone |
N-Dealkylation |
Anti-arrhythmic |
Azonafade |
N-Desmethylazonaˆde |
Anti-tumoral |
Chlordiazepoxide |
Desmethylchlordiazepoxide |
Anxiolytic |
Citalopram |
Desmethylcitalopram |
Anti-depressant |
Clobazam |
N-Desmethylclobazam |
Anti-epileptic |
Clomipramine |
N-Desmethylclomipramine |
Anti-depressant |
Clozapine |
Norclozapine |
Anti-psychotic |
Ferroquine |
N-Demethylferroquine |
Anti-malarial |
N,N-Didemethylferroquine |
Fluoxetine |
Nor‰uoxetine |
Anti-depressant |
Ivabradine |
N-Desmethylivabradine |
Bradycardia |
Lumefantrine |
Desbutyllumefantrine |
Anti-malarial |
Mianserin |
N-Desmethylmiaserin |
Anti-depressant |
Verapamil |
Norverapamil |
Anti-arrhythmic |
Oxybutynin |
N-Desethyloxybutynin |
Smooth muscle relaxant |
Rosuvastatin |
N-Desmethylrosuvastatin |
Anti-hypercholesterolemia |
Sertraline |
N-Desmethylsertraline |
Anti-depressant |
Sibutramine |
N-Desmethylsibutramine |
Treatment of obesity |
N,N-Didesmethylsibutramine |
Zolmitriptan |
N-Demethylzolmitriptan |
Treatment of migraine |
Zopiclone |
(S)-Desmethylzopiclone |
Treatment of insomnia |
Artemether |
Dihydroartemisinin |
O-Dealkylation |
Anti-malarial |
Ivabradine |
O-Demethylivabradine |
Bradycardia |
Tramadol |
O-Demethyltramadol |
Centrally acting analgesic |
Venlafaxine |
O-Desmethylvenlafaxine |
Anti-depressant |
Acebutol |
Diacetolol |
N-Acetylation |
Anti-hypertensive |
Albendazole |
Albendazolesulfoxide |
Sulfoxidation |
Anti-parasitic |
Aripiprazole |
Dehydroaripiprazole |
Dehydrogenation |
Anti-psychotic |
Bupropion |
Threo/erythro-hydrobupropion |
Carbonyl
reduction |
Anti-depressant |
Carbamazepine |
Carbamazepine-10,11 epoxide |
Epoxidation |
Anti-epilepsy |
|
Diacerein |
Rhein |
Deacetylation |
Treatment of osteoarthritis |
Isosorbide
Dinitrate |
5- or 2-Isosorbide mononitrate |
Denitration |
Treatment of angina pectoris |
Losartan |
Carboxylosartan |
Carboxylation |
Anti-hypertensive |
Minoxidil |
Minoxidil sulfate |
Sulfation |
Stimulating hair growth |
Oxcarbazepine |
10-Hydroxy-10,11-dihydrocarbamazepine |
Hydroxylation & Dehydrogenation |
Anti-epileptic |
Procainamide |
N-Acetyl procainamide |
N-Acetylation |
Anti-arrhythmic |
Rifampicin |
25-Desacetylrifampicin |
Deacetylation |
Treatment of tuberculosis |
Thiocolchicoside |
3-O-Glucuronidated-Thiocolchicoside |
Glucuronidation |
Muscle relaxant |
Tramadol |
O-Demethyl-N demethyltramadol |
N,O-Dealkylation |
Centrally acting analgesic |
Triamterene |
Hydroxytriamterene sulfate |
Sulfation |
Diuretic |