Telmisartan, pharmacokinetics

Structural differences of ARBs influence the variation in pharmacological (pharmacokinetic /pharmacodynamic) properties of these drugs. Affinity for the ATj receptor is highest with candesartan, followed by irbesartan, losartan, valsartan, and telmisartan. Differences and affinities at the ATj receptor are also involved in... 

Slangier J, Su CA, Hendriks MG, van Lier JJ, Sollie FA, Oosterhuis B, Jonkman JH. The effect of telmisartan on the steady-state pharmacokinetics of digoxin in healthy male volunteers. J Qin Pharmacol 2000 40(12 Pt l) 1373-9. 

Stangier J, Su CA, Fraunhofer A, Tetzloff W. Pharmacokinetics of acetaminophen and ibuprofen when coadministered with telmisartan in healthy volunteers. J Clin Pharmacol 2000 40(12 Pt 1) 1338 6. 

Indometacin may attenuate the antihypertensive effect of losar-tan, valsartan, or other angiotensin II receptor antagonists. However, low-dose aspirin does not appear to alter the antihypertensive effect of losartan. No clinically relevant pharmacokinetic interactions occur between telmisartan and ibuprofen or paracetamol (acetaminophen), or between valsartan and indometacin. The combination of an NSAID and angiotensin II receptor antagonist can increase the risk of renal impairment and hyperkalaemia. 

In a crossover study in 12 healthy subjects, telmisartan 120 mg daily had no effect on the pharmacokinetics of ibuprofen 400 mg three times a day for 7 days. Similarly, the pharmacokinetics of telmisartan were unaffeet-ed by the concurrent use of ibuprofen, when compared with previous studies of telmisartan alone. ... 

No significant pharmacokinetic interactions occur between nifedipine and candesartan or irbesartan, or between amlodipine and telmisartan or valsartan. Calcium-channel blockers have been given safely with eprosartan or irbesartan. 

Slangier J, Su C-APF. Pharmacokinetics of repeated oral doses of amlodipine and amlodipine plus telmisartan in healthy volunteers. J Clin Pharmacol (2000) 40,1347-54. 

Symptomatic hypotension may occur when an angiotensin II receptor antagonist is started in patients taking high-dose diuretics. Potassium levels may be either increased, decreased or not affected. No clinically relevant pharmacokinetic interactions appear to occur between candesartan, eprosartan, irbesartan, losartan, telmisartan or valsartan and hydrochlorothiazide, although the bioavailability of hydrochlorothiazide may be modestly reduced. Similarly, there is no clinically significant pharmacokinetic interaction between valsartan and furosemide. 

In a randomised, crossover study in 13 healthy subjects, telmisartan 160 mg daily was given with hydrochlorothiazide 25 mg daily for 7 days. There was no difference in AUC and maximum plasma concentrations of either drug compared with when they were given alone. Similarly, no pharmacokinetic interactions were found between irbesartan and hydrochlorothiazide. ... 

Yoi C-L, Dias VC, Stai ier J. Multiple-dose pharmacokinetics of telmisartan and of hydrochlorothiazide foUowii concurrent administration in healthy subjects. J Clin Pharmacol (2000) 40,1323-30. 

The available pharmacokinetic and pharmacodynamic studies showing that the angiotensin II receptor antagonists (candesartan, eprosartan, irbe-sartan, losartan, telmisartan, valsartan) do not interact with warfarin, and the lack of any published evidence to the contrary, suggest that no warfarin dose adjustments should be needed if these drugs are used. 

Irbesartan and telmisartan appear not to alter the pharmacokinetics of simvastatin, fluvastatin does not alter the pharmacokinetics of losartan or its active metabolite, and ohnesartan appears not to interact with pravastatin. 

A study in 12 healthy subjects found that irbesartan 300 mg had no significant effect on the pharmacokinetics of a single 50-mg dose of simvastatin, or its metabolite simvastatin acid, and the combination was well-tolerated. No clinically relevant interaction was noted when telmisartan was given with simvastatin. ... 

Drug-drug interactions Mycophenolate mofetil In a pharmacokinetic study of telmisartan, valsartan, and candesartan in combination with mycophenolate mofetil in renal transplant patients, telmisartan increased the elimination of mycophenolic acid there was no interaction with valsartan or candesartan [57 ]. It was suggested that this was due to activation by... 

Miura M, Satoh S, Kagaya H, Saito M, Inoue T, Ohkubo T, Habuchi T, Suzuki T. Effect of telmisartan, valsartan and candesartan on mycophenolate mofe-til pharmacokinetics in Japanese renal transplant recipients. J Clin Pharm Ther 2009 34 683-92. 

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