Drugs that have glucuronidation listed as a clearance mechanism, including those in the top 200 U.S. prescribed drugs in 2002
Drug | Listed UGT | Rank in Top 200 | In Vitro Kma | Reference | Total (Unbound) [Plasma]b | Reference |
|---|---|---|---|---|---|---|
| μM | μM | |||||
| Amitriptyline | 1A4c | >200 | 10 | Dehal et al. (1992) | 0.76 | Franke et al. (2003) |
| Carvedilol | 1A1, 2B4, 2B7 | 174 | 27 | Ohno et al. (2004) | 0.6 (0.003) | Therapeutic Drugs (A), 1994 |
| Clofibric acid | 2B7 | >200 | N/A | Jin et al. (1993) | 532710 | Sallustio et al. (1991) |
| Codeine | >200 | 2600 | Court et al. (2003) | 0.83 (0.66) | Therapeutic Drugs (B), 1994 | |
| Cyclobenzaprine | 1A4d | 61 | N/A | Hawes (1998) | 0.16 | Hucker and Stauffer (1976) |
| Diclofenac | 2B7 | 197 | 18 | Kumar et al. 2002 | 0.94 (0.005) | Therapeutic Drugs (C), 1994 |
| DMXAA | N/A | >200 | 100 | Miners et al. (1997) | 787 (32) | Zhou et al. (2002) |
| Etoposide | >200 | 440 | Watanabe et al., 2003 | 5.4 (0.27) | Therapeutic Drugs (C), 1994 | |
| Fenofibrate | 1A9c | 130 | N/A | Barbier et al. (2003) | 34 (0.68) | Doser et al. (1996) (Mogi et al., 1995) |
| Flavopiridol | >200 | 125 | Hagenauer (2001) | 0.25 (0.015) | Rudek et al. (2003) | |
| Flurbiprofen | >200 | 520 | Hamdoune et al. (1995) | 10.6 (0.02) | Knadler et al. (1989) | |
| Furosemide | 1A8, 1A10d | 7 | N/A | Cheng et al. (1999) | 3.3 (0.08) | Najib et al. (2003) (Pacifici et al., 1987) |
| Gemfibrozil | >200 | 82 | Prueksaritanont et al. (2002) | 132 (1.32) | Therapeutic Drugs (D), 1994 | |
| Glipizide | N/A | 150 | N/A | N/A | 0.35 | Niemi et al. (2001) |
| Irbesartan | N/A | 149 | N/A | N/A | 3.5 | Gu et al. (2002) |
| Lamotrigine | 1A4c | >200 | 5500 | Furlan et al. (1999) | 37 (15) | Ramsay et al. (1991) [Therapeutic Drugs (E), 1994] |
| Levothyroxine | 1A1d | 4 | N/A | N/A | 0.003 | www.fda.gov/cder/guidance/3645fnl.htm |
| Metoclopromide | N/A | 138 | N/A | N/A | 0.27 (0.16) | Hasan et al. (2003) [Therapeutic Drugs (F), 1994] |
| Metronidazole | N/A | 147 | N/A | N/A | 6.8 (6.8) | Hoffman et al. 1995 [Therapeutic Drugs (G), 1994] |
| Morphine | >200 | 2400-4300 | Court et al. (2003) | 0.16 (0.1) | Therapeutic Drugs (H), 1994 | |
| Naloxone | 2B7c | >200 | N/A | Coffman et al. (2001) | 11.5 | Groeger and Inturrisi (1987) |
| Naproxen | 1A3 | >200 | N/A | Green et al. (1998) | 240 (0.26) | Toothaker et al. (2000) (Bertin et al. 1994) |
| Olanzapine | 1A4d | 109 | 227 (UGT1A4)e | Linnet (2002) | 0.67 | Bergeman et al. (2004) |
| Oxazepam | >200 | 43-303 | Court et al. (2002) | 1.7 (0.005) | Therapeutic Drugs (I), 1994 | |
| Paracetamol | 1A1, 1A6, 1A9d | 6000-55000 | Court et al. (2001) | 23 (18) | Therapeutic Drugs (J), 1994 | |
| Propofol | 1A9c | >200 | 190-280 | Soars et al. (2003) | 14 (0.03) | Hiraoka et al. (2004) [Therapeutic Drugs (K), 1994] |
| Raloxifene | 1A1, 1A8, 1A10d | 97 | 8-58 | Kemp et al. (2002) | 0.003 | www.rxlist.com |
| Tramadol | N/A | N/A | N/A | 0.82 (0.65) | Dyderksi et al. (2001) (Raffa et al. 1995) | |
| Valdecoxib | N/A | 148 | N/A | N/A | 2.29 | Yuan et al. (2002) |
| Valproic acid | 2B7d | 121 | 2300-5200 | Ethell et al. (2003) | 805 (113) | Dutta et al. (2002) (Hussain et al. 1994) |
| Zidovudine | 2B7c | >200 | 510-1400 | Court et al. (2003) | 3 (1.08) | Pereira et al. (2002) [Therapeutic Drugs (L), 1994] |
N/A, information not available on www.rxlist.com or in the literature.
↵ a In Human Liver Microsomes unless specified
↵ b Total (unbound + bound) Cmax concentrations reported
↵ c Data from literature sources
↵ d Data from www.rxlist.com
↵ e Vmax not reached in human liver microsomes