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
Table 1: Pharmacologically active metabolites of currently marketed drugs [2].