Acute Porphyria Drug Database

J05AJ03 - Dolutegravir
Propably not porphyrinogenic
PNP

Important Information
Side effects like nausea and diarrhoea may potentially be porphyrinogenic through reduction in carbohydrate intake.
Side effects
Very common side effects of dolutegravir are nausea and diarrhoea. Other common side effects are vomiting and abdominal pains. These adverse reactions can be confused with an acute porphyric attack and may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Dolutegravir is not an inducer or an inhibitor of CYP450 enzymes and no pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Pyridinecarboxylic acid
Therapeutic characteristics
Dolutegravir is an integrase strand transfer inhibitor (INSTI) indicated in combination with other anti-retroviral medicinal products for the treatment of HIV-1 infection. It is administered orally.
Metabolism and pharmacokinetics
Dolutegravir is mainly metabolized through glucuronidation, with minor contribution from CYP3A4 (SPC). About 50 % of the dose is excreted in unchanged form in feaces and about 30 % is excreted in the urine as glucuronide conjugate. In vitro, dolutegravir is not found to be an inhibitor of CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6 or 3A4, and is not found to be an inducer of CYP1A2, 2B6 or 3A4 (SPC). Dolutegravir does not alter drug-metabolizing enzymes and there are no CYP-dependent drug-drug interactions with dolutegravir as perpetrator (Kandel 2015). A drug-drug interaction study found that dolutegravir had no effect on the pharmacokinetics of an oral contraceptive containing norgestimate and ethinyl estradiol (Song 2015).

References

  1. Scientific articles
  2. Kandel CE, Walmsley SL. Dolutegravir - a review of the pharmacology, efficacy, and safety in the treatment of HIV. Drug Des Devel Ther. 2015 Jul 7;9:3547-55. #3104
  3. Song IH, Borland J, et al. Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol. Ann Pharmacother. 2015 Jul;49(7):784-9. PMID 25862012. #4751
  4. Summary of Product Characteristics
  5. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Tivicay). #3106

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