Acute Porphyria Drug Database

J05AJ01 - Raltegravir
Propably not porphyrinogenic
PNP

Rationale
Raltegravir does not inhibit or induce CYP enzymes. Side effects such as nausea, vomiting and diarrhoea may be potentially porphyrinogenic through reduction in carbohydrate intake.
Therapeutic characteristics
Raltegravir is indicated in combination with other anti-retroviral medicinial products for the treatment of human immunodeficiency virus (HIV-1) infection in adults. Common reported side effects that can be confused with an acute porphyria attack are abdominal pain, diarrhoea, nausea and vomiting. Other common side effects are insomnia.
Metabolism and pharmacokinetics
In vitro and in vivo studies have shown that raltregravir is mainly metabolised via a UGT1A1 mediated glucuronidation pathway (SPC, Zhang 2010). The elimination half-life is 9 hours. In vitro-studies indicates that raltegravir is not a substrate of CYP450 enzymes. It does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 nor does it induce CYP3A4 (SPC). An in vivo study has shown that raltegravir does not affect the plasma level of midazolam, a sensitive probe CYP3A4 substrate. This indicates that it does not induce or inhibit CYP3A4 (Iwamoto 2008).

References

  1. Scientific articles
  2. Zhang L, Reynolds KS, et al. Drug interactions evaluation: an integrated part of risk assessment of therapeutics. Toxicol Appl Pharmacol. 2010 Mar 1;243(2):134-45. PMID 20045016. #4553
  3. Summary of Product Characteristics
  4. Norwegian medicines agency. Summary of Product Characteristics (SPC). Raltegravir. #1849
  5. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Raltegravir. Last edition: February 2013. #1850

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