Monograph
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
# | Citation details | PMID |
---|---|---|
* | Scientific articles | |
1. | Dolutegravir - a review of the pharmacology, efficacy, and safety in the treatment of HIV.
Kandel CE, Walmsley SL. Drug Des Devel Ther. 2015 Jul 7;9:3547-55. |
|
2. | Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol.
Song IH, Borland J, et al. Ann Pharmacother. 2015 Jul;49(7):784-9. |
25862012 |
* | Summary of Product Characteristics | |
3. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Tivicay).
|
Similar drugs
Tradenames and packages
From some sources, we get a list of packages (United Kingdom, Ireland, Estonia).
Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway).
What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names
are the searchable terms. The gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors.
We strive to improve it continuously.
Netherlands
Tivicay · Tivicay 10 mg, filmomhulde tablet · Tivicay 25 mg, filmomhulde tablet · Tivicay 5 mg oplosbare tabletten · Tivicay 50 mg, filmomhulde tabletBelgium
Tivicay · Tivicay 10 mg compr. pellic. · Tivicay 25 mg compr. pellic. · Tivicay 5 mg compr. disp. · Tivicay 50 mg compr. pellic.United Kingdom
Tivicay · Tivicay 10mg tablets · Tivicay 25mg tablets · Tivicay 50mg tablets · Tivicay 5mg dispersible tabletsDenmark
TivicayNorway
TivicayPoland
TivicayLuxembourg
TivicayIceland
TivicayFinland
TivicayLatvia
Tivicay
© NAPOS 2024