Monograph
A10BH03 - Saxagliptin |
Propably not porphyrinogenic |
PNP |
Rationale
No capacity for significant Cyp-interaction, and thus not for pharmacokinetic porphyrinogenicity. Urinary and upper respiratory tract infections are common side effects and potentially porphyrinogenic. The pharmacodynamic effects on glucose homeostasis with inhibition of pancreatic glucagon release are probably anti-porphyrinogenic.
Chemical description
Aminoazabiocyclohexan carbonitrile.
Therapeutic characteristics
Saxagliptin is used in diabetes type 2 in combination with other orally administered anti-diabetics. Urinary and respiratory tract infections are common side effects and potentially porphyrinogenic. The very common hypoglycemic side effect noted in combination therapy with sulfonylureas is probably explained by enhanced effects on pancreatic insulin release and subsequent increase in tissue glucose uptake. It is thus not porphyrinogenic.
Metabolism and pharmacokinetics
The metabolism of saxagliptin is primarily mediated by CYP 3A4/5. In in vitro studies, saxagliptin and its major metabolite neither inhibited CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, or 3A4, nor induced CYP1A2, 2B6, 2C9, or 3A4.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors.
Golightly LK, Drayna CC, et al. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. |
|
| 2. | Pharmacokinetics of dipeptidylpeptidase-4 inhibitors.
Scheen AJ. Diabetes Obes Metab. 2010 Aug; 12(8):648-58. |
20590741 |
| 3. | Drug interactions with oral antidiabetic agents: pharmacokinetic mechanisms and clinical implications.
Tornio A, Niemi M, et al. Trends Pharmacol Sci. 2012 Jun;33(6):312-22. |
22475684 |
| * | Summary of Product Characteristics | |
| 4. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Onglyza.
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