J05AF07 - Tenofovir Disoproxil |
Propably not porphyrinogenic |
PNP |
Important Information
Side effects like diarrhoea, vomiting and nausea may potentially be porphyrinogenic through reduction in carbohydrate intake.
Side effects
Very common side effects of tenofovir disoproxil are diarrhoea, vomiting and nausea. These side effects can be confused with an acute porphyric attack and may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Tenofovir is not a substrate, inhibitor or inducer of CYP450 enzymes. No pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Tenofovir belongs to the class 6-aminopurines
Therapeutic characteristics
Tenofovir is a nucleotide reverse transcriptase inhibitor indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric. It is also indicated for the treatment of chronic hepatitis B.
It is administered orally.
Metabolism and pharmakokinetics
Tenofovir disoproxil is first converted to tenofovir monophosphate and then converted to the active metabolite tenofovir diphosphate by cellular enzymes (SPC). Tenofovir is excreted by the kidney by both glomerular filtration and active tubular secretion.
Tenofovir is not a substrate, inhibitor or inducer of CYP450 enzymes (Kearney 2004). Although, tenofovir has been reported to be a weak inhibitor of CYP1A2 (Lexi-interact, SPC) it is unlikely that this is clinically relevant.
IPNet drug reports
Uneventful use of the emtricitabine and tenofovir disoproxil combination (ATC-code: J05AR03) is reported in 1 patient with acute intermittent porphyria.
References
- Scientific articles
- Kearney BP, Flaherty JF, et al. Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics. Clin Pharmacokinet. 2004;43(9):595-612. #1815
- Government bodies
- #1302
- Drug interaction databases
- Lexi-Interact in UpToDate. tenofovir: Drug interaction program. #1816
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). (Tenofovir disoproxil). #1817
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