Monograph
A10BG03 - Pioglitazone |
Propably not porphyrinogenic |
PNP |
Rationale
Pioglitazone is a substrate of CYP2C8, CYP2C9 and CYP3A4, but is not an inducer of them or CYP1A. Pioglitazone does not inhibit CYP2C8 or CYP3A4.
Chemical description
Pyridyl ethoxybenzyl thiazolidindione
Therapeutic characteristics
Common side effects are back pain and upper respiratory tract infections.
Hepatic exposure
Irrelevant
Metabolism and pharmacokinetics
Pioglitazone is listed to be metabolized by CYP2C8, CYP2C9 and CYP3A4 (Kajosaari 2006, Norsk legemiddelhåndbok, Scheen 2007). The elimination half-life is 5-6 hours.
Clinical studies showed no induction of CYP1A, CYP2C8, CYP2C9 (SPC) or CYP3A4 (Nowak 2002, Scheen 2007, SPC).
Pioglitazone inhibits CYP2C8 and CYP3A4 (Kajosaari 2006, Scheen 2007), and has also been shown to be a mechanism-based inhibitor of CYP3A4 in vitro (Lim 2005, Sinz 2006). In vivo studies have however, shown that pioglitazone does not increase the plasma concentration of repaglinide, a CYP2C8 and CYP3A4 substrate, which indicates that pioglitazone does not significantly inhibit these enzymes (Kajosaari 2006, Scheen 2007).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Pioglitazone, an in vitro inhibitor of CYP2C8 and CYP3A4, does not increase the plasma concentrations of the CYP2C8 and CYP3A4 substrate repaglinide.
Kajosaari LI, Jaakkola T, et al. Eur J Clin Pharmacol. 2006 Mar;62(3):217-23. |
|
| 2. | Pioglitazone: effect on CYP3A4 activity.
Nowak SN, Edwards DJ, et al. J Clin Pharmacol. 2002 Dec;42(12):1299-302. |
12463723 |
| 3. | Pharmacokinetic interactions with thiazolidinediones.
Scheen AJ. Clin Pharmacokinet. 2007;46(1):1-12. |
17201456 |
| 4. | Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions.
Sinz M, Kim S, et al. Curr Drug Metab. 2006 May;7(4):375-88. |
16724927 |
| * | Drug reference publications | |
| 5. | Norsk legemiddelhåndbok. Pioglitazone
|
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| * | Summary of Product Characteristics | |
| 6. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Pioglitazone.
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