J05AR08 - Emtricitabine, Tenofovir Disoproxil and Rilpivirine |
Propably not porphyrinogenic |
PNP |
Important Information
Side effects like diarrhoea, nausea and vomiting may potentially be porphyrinogenic through reduction in carbohydrate intake.
Side effects
Very common side effects of this combination product are diarrhoea, vomiting, nausea and insomnia. Other common side effects are abdominal pains and decreased appetite. These side effects can be confused with an acute porphyric attack and may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake or sleep deprivation.
Rationale
This combination product contains three substances: Emtricitabine (ATC-code: J05AF09), tenofovir disoproxil (ATC-code J05AF07) and rilpivirine (ATC-code: J05AF07). All of them are safety classified as probably not porphyrinogenic. The combination is therefore classified as probably not porphyrinogenic. For more details please refer to the monographs of the three substances.
Chemical description
Emtricitabine belongs to a class known as 3’-thia pyrimidine nucleosides
Tenofovir belongs to the class 6-aminopurines
Rilpivirine is a diaryldyrimidine
Therapeutic characteristics
This combination product is indicated for the treatment of HIV-1 infection in adults.
It is administered orally.
Metabolism and pharmacokinetics
Emtricitabine is not metabolized by CYP450 enzymes and is not an inducer or an inhibitor of CYP450 enzymes (SPC). Emtricitabine is classified as probably not porphyrinogenic (see monograph, ATC-code: J05AF09).
Tenofovir disoproxil is not metabolized by CYP450 enzymes and is not an inducer or an inhibitor of CYP450 enzymes (SPC). Tenofovir disoproxil is classified as probably not porphyrinogenic (see monograph, ATC-code: J05AF07).
Rilpivirine is metabolized by CYP3A4 (SPC). It has been found to be an activator of hPXR and an inducer of CYP3A4 (Weiss 2013). However, this is unlikely to be clinically relevant as free plasma-concentration is very low and there are no drug-drug interactions with rilpivirine as perpetrator. Rilpivirine is classified as probably not porphyrinogenic (see monograph, ATC-code: J05AG05).
References
- Scientific articles
- Weiss J, Haefeli WE. Potential of the novel antiretroviral drug rilpivirine to modulate the expression and function of drug transporters and drug-metabolising enzymes in vitro. Int J Antimicrob Agents. 2013 May;41(5):484-7. PMID 23428312. #3137
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Eviplera). #3168
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