Monograph
C09CA07 - Telmisartan |
Propably not porphyrinogenic |
PNP |
Rationale
Telmisartan is not metabolized by CYP450 enzymes. Telmisartan has been found to be an inhibitor of CYP2C19 and CYP2C9 in vitro, but this has not been observed in vivo.
Chemical description
Angiotensin II receptor antagonist
Therapeutic characteristics
Telmisartan is used in the treatment of essential hypertension. It is administered orally.
Hepatic exposure
Oral administration of 40 mg telmisartan gave a Cmax of 44.7 ng/ml (Wienen 2000), which is equivalent to 87 nM.
Metabolism and pharmacokinetics
Telmisartan is metabolized by glucuronidation and no CYP450 enzymes are thought to be involved (SPC).
Telmisartan was found to be an in vitro inhibitor of CYP2C9, however such inhibition is unlikely to be clinically relevant due to the low free plasma concentration obtained at therapeutic doses (Kamiyama 2007). An in vivo study with co-administration of telmisartan and the CYP2C9 substrate, warfarin, did not demonstrate a clinically relevant drug-drug interaction (Stangier 2000).
In vitro testing showed that telmisartan inhibited CYP2C19, but this was not clinically relevant (Wienen 2000).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
# | Citation details | PMID |
---|---|---|
* | Scientific articles | |
1. | Inhibitory effects of angiotensin receptor blockers on CYP2C9 activity in human liver microsomes.
Kamiyama E, Yoshigae Y, et al. Drug Metab Pharmacokinet. 2007 Aug;22(4):267-75. |
|
2. | Steady-state pharmacodynamics and pharmacokinetics of warfarin in the presence and absence of telmisartan in healthy male volunteers.
Stangier J, Su CA, et al. J Clin Pharmacol. 2000 Dec;40(12 Pt 1):1331-7. |
11185631 |
3. | A Review on Telmisartan: A Novel, Long-Acting Angiotensin II-Receptor Antagonist.
Wienen W, Entzeroth M, et al. Cardiovascular Drug Reviews. 2000. Vol. 18, No. 2, pp. 127–154 |
|
* | Summary of Product Characteristics | |
4. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Micardis).
|
Similar drugs
Tradenames and packages
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Netherlands
Kinzalmono · Kinzalmono 20 mg, tabletten · Kinzalmono 40 mg, tabletten · Kinzalmono 80 mg, tabletten · Micardis · Micardis 20 mg, tabletten · Micardis 40 mg, tabletten · Micardis 80 mg, tabletten · Pritor · Pritor 20 mg, tabletten · Pritor 40 mg, tabletten · Pritor 80 mg, tabletten · Telmisartan · Telmisartan Actavis 20 mg tabletten · Telmisartan Actavis 40 mg tabletten · Telmisartan Actavis 80 mg tabletten · Telmisartan Aurobindo 20mg tabletten · Telmisartan Aurobindo 40mg tabletten · Telmisartan Aurobindo 80mg tabletten · Telmisartan Fair-Med 20 mg tabletten · Telmisartan Fair-Med 40 mg tabletten · Telmisartan Fair-Med 80 mg tabletten · Telmisartan Glenmark 20 mg, Filmomhulde Tabletten · Telmisartan Glenmark 40 mg, Filmomhulde Tabletten · Telmisartan Glenmark 80 mg, Filmomhulde Tabletten · Telmisartan HEXAL 20 mg, tabletten · Telmisartan HEXAL 40 mg, tabletten · Telmisartan HEXAL 80 mg, tabletten · Telmisartan Lek 20 mg, tabletten · Telmisartan Lek 40 mg, tabletten · Telmisartan Lek 80 mg, tabletten · Telmisartan Sandoz 20 mg, tabletten · Telmisartan Sandoz 40 mg, tabletten · Telmisartan Sandoz 80 mg, tabletten · Telmisartan Teva 20 mg tabletten · Telmisartan Teva 40 mg tabletten · Telmisartan Teva 80 mg tabletten · Telmisartan Viatris 20 mg, tabletten · Telmisartan Viatris 40 mg, tabletten · Telmisartan Viatris 80 mg, tabletten · Telmisartan Xiromed 20 mg tabletten · Telmisartan Xiromed 40 mg tabletten · Telmisartan Xiromed 80 mg tabletten · Telmisartan-1A Pharma 20 mg, tabletten · Telmisartan-1A Pharma 40 mg, tabletten · Telmisartan-1A Pharma 80 mg, tabletten · Tolura · Tolura 20 mg tabletten · Tolura 40 mg tabletten · Tolura 80 mg tablettenBelgium
Kinzalmono · Kinzalmono 20 mg comp. · Kinzalmono 40 mg comp. · Kinzalmono 80 mg comp. · Micardis · Micardis 20 mg comp. · Micardis 40 mg comp. · Micardis 80 mg comp. · Pritor · Pritor 20 mg comp. · Pritor 20 mg compr. pellic. · Pritor 40 mg comp. · Pritor 80 mg comp. · PritorPlus · PritorPlus 40 mg - 12.5 mg comp. · PritorPlus 80 mg - 12.5 mg comp. · PritorPlus 80 mg - 25 mg comp. · Telmisartan · Telmisartan Actavis 20 mg comp. · Telmisartan Actavis 40 mg comp. · Telmisartan Actavis 80 mg comp. · Telmisartan EG 40 mg compr. pellic. · Telmisartan EG 80 mg compr. pellic. · Telmisartan Fair-Med 20 mg comp. · Telmisartan Fair-Med 40 mg comp. · Telmisartan Fair-Med 80 mg comp. · Telmisartan Teva 20 mg comp. · Telmisartan Teva 40 mg comp. · Telmisartan Teva 80 mg comp. · Telmisartan Teva Generics 40 mg comp. · Telmisartan Teva Generics 80 mg comp. · Telmisartan Viatris 20 mg comp. · Telmisartan Viatris 40 mg comp. · Telmisartan Viatris 80 mg comp. · Tolura · Tolura 40 mg comp. · Tolura 80 mg comp.United Kingdom
Micardis · Micardis 20mg tablets · Micardis 40mg tablets · Micardis 80mg tablets · Telmisartan · Telmisartan 20mg tablets · Telmisartan 40mg tablets · Telmisartan 40mg/5ml oral suspension · Telmisartan 80mg tablets · Tolura · Tolura 20mg tablets · Tolura 40mg tablets · Tolura 80mg tabletsDenmark
Kinzalmono · Micardis · Pritor · Telmisartan · Telmisartan "Actavis" · Telmisartan "Nordic Prime" · Telmisartan "Stada" · Telmisartan "Teva Pharma" · Tolura · ZanacodarNorway
Micardis · Telmisartan ActavisPoland
Actelsar · Kinzalmono · Micardis · Polsart · Pritor · Telmabax · Telmisartan Actavis · Telmisartan Aurovitas · Telmisartan Bluefish · Telmisartan EGIS · Telmisartan Genoptim · Telmisartan Medical Valley · Telmisartan Orion · Telmisartan Teva Pharma · Telmisartan Viatris · Telmisartanum Teva B.V. · Telmix · Telmizek · Tezeo · Tolura · Toptelmi · ZanacodarLuxembourg
KINZALMONO · KINZALMONO-20 · KINZALMONO-40 · KINZALMONO-80 · MICARDIS · MICARDIS-20 · MICARDIS-40 · MICARDIS-80 · PRITOR · PRITOR-20 · PRITOR-40 · PRITOR-80 · TELMISARTAN · TELMISARTAN ACTAVIS-20 · TELMISARTAN ACTAVIS-40 · Telmisartan EG · Telmisartan Micro Labs · TELMISARTAN RATIOPHARM-20 · TELMISARTAN RATIOPHARM-40 · TELMISARTAN RATIOPHARM-80 · Telmisartan Viatris · TELMISARTAN-80 · TOLURA · TOLURA-20 · TOLURA-40 · TOLURA-80Iceland
Kinzalmono · Micardis · Pritor · Telmisartan · Telmisartan Actavis · Telmisartan Teva Pharma · ToluraFinland
Kinzalmono · Micardis · Pritor · Telmark · Telmisartan Actavis · Telmisartan Orion · Telmisartan ratiopharm · Telmisartan Sandoz · Telmisartan Stada · ToluraLatvia
Kinzalmono · Micardis · Pritor · Telmisartan · Telmisartan Actavis · Telmisartan-ratiopharm · Tezeo · ToluraSerbia
Micardis · Micardis® · Telisar · Telisar® · TELMIKOR · TELMIKOR® · Telmipres · Telmipres® · Tolura · Tolura®
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