| 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 |