B01AF02 - Apixaban |
Propably not porphyrinogenic |
PNP |
Side effects
One common adverse reaction of apixaban that can be confused with an acute porphyric attack is nausea. This side effect may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Apixiban is not reported to be an inducer or a mechanism-based inhibitor of CYP enzymes, and is not observed to alter the metabolism of other CYP metabolized drugs. No pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Phenylpiperidines
Therapeutic characteristics
Apixaban is an antithrombotic agent, a direct inhibitor of factor Xa, used in the prevention and treatment of thromboembolic diseases. It is administered orally.
Hepatic exposure
Cmax of apixiban is reported to be 80.5 ng/mL (Frost 2014). This is equivalent to 175 nM and hepatic exposure is therefore significant.
Metabolism and pharmakokinetics
Apixaban mainly undergoes O-demethylation and hydroxylation to its metabolites. It is metabolized mainly via CYP3A4/5 with minor contributions from CYP1A2, 2C8, 2C9, 2C19, and 2J2 (SPC).
Apixaban is neither an inducer of CYP1A2, 2B6 or 3A4/5, nor an inhibitor of CYP1A2, 2A6, 2B6, 2C8, 2C9, 2D6 or 3A4 in vitro. It has been reported to be a weak inhibitor of CYP2C19 in vitro, but this was at concentrations significantly higher than peak plasma concentrations (SPC).
Apixaban is not observed to alter the metabolism of other CYP metabolized drugs (interaksjonsdatabasen.dk, SPC).
References
- Scientific articles
- Frost C, Song Y, et al. A randomized direct comparison of the pharmacokinetics and pharmacodynamics of apixaban and rivaroxaban. Clin Pharmacol. 2014 Nov 13;6:179-87. #3158
- Wang L, Zhang D, et al. In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies. Drug Metab Dispos. 2010 Mar;38(3):448-58 PMID 19940026. #4762
- Drug interaction databases
- Interaktionsdatabasen.dk. Apixaban. Accessible from www.interaktionsdatabasen.dk #3159
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Eliquis). #3160
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