Skip to main content

Advertisement

SpringerLink
Log in

Telmisartan

A Review of its Use in Hypertension

  • Adis Drug Evaluation
  • Published:
Drugs Aims and scope Submit manuscript

Summary

Abstract

Telmisartan is an angiotensin II receptor antagonist that is highly selective for type 1 angiotensin II receptors. It was significantly more effective than placebo in large (n >100), double-blind, randomised, multicentre clinical trials in patients with mild to moderate hypertension. Telmisartan 20 to 160mg once daily produced mean reductions in supine trough systolic blood pressure and diastolic blood pressure of up to 15.5 and 10.5mm Hg, respectively. Maximum blood pressure reduction occurred with a dosage of 40 to 80 mg/day.

Telmisartan 40 to 120 mg/day was as effective as amlodipine 5 to 10 mg/day or atenolol 50 to 100 mg/day in dose-titration studies. Telmisartan 20 to 160 mg/day was generally similar in efficacy to enalapril 5 to 20 mg/day or lisinopril 10 to 40 mg/day in both titration-to-response and other studies. Hydrochlorothiazide was coadministered in most of the titration-to-response studies if patients remained hypertensive.

Telmisartan 80 mg/day was more effective than submaximal dosages of losartan (50 mg/day) or valsartan (80 mg/day) and was as effective as a fixed-dose combination of losartan 50mg plus hydrochlorothiazide 12.5mg over the last 6 hours of the dosage interval and the whole 24-hour postdose interval. In patients with severe hypertension, telmisartan 80 to 160 mg/day was as effective as enalapril 20 to 40 mg/day (both agents could be titrated and combined sequentially with hydrochlorothiazide 25mg and amlodipine 5mg).

The addition of hydrochlorothiazide to telmisartan was more effective than each agent alone at lowering blood pressure in patients with hypertension.

Telmisartan was well tolerated in patients with mild to moderate hypertension and was significantly less likely to cause persistent, dry cough than lisinopril.

Conclusion: Telmisartan is an effective antihypertensive agent with a tolerability profile similar to that of placebo. Comparative data have shown telmisartan to be as effective as other major classes of antihypertensive agents at lowering blood pressure. Compared with lisinopril, telmisartan is associated with a significantly lower incidence of dry, persistent cough. Therefore, telmisartan is a useful therapeutic option in the management of patients with hypertension.

Pharmacodynamic Properties

Telmisartan is an angiotensin II (AII) receptor antagonist that is highly selective for type 1 AII (AT1) receptors.

In normotensive male volunteers enrolled in a randomised, double-blind, placebo-controlled study, telmisartan 20 to 80mg dose-dependently attenuated AII-induced increases in diastolic blood pressure (DBP), systolic blood pressure (SBP) and heart rate (HR). Single doses of telmisartan 20 to 80mg inhibited AII-induced increase in DBP by >25% within 0.3 to 1.1 hours when administered 30 minutes after intravenous administration of AII (the dose of AII was that which produced maximal increases in SBP). During repeated challenges, AII-induced increases in blood pressure were inhibited by >25% for 26.9, 35.4 and 40.5 hours among those randomised to telmisartan 20, 40 and 80mg, respectively. Plasma levels of AII and active renin increased to maxima within 4 hours of treatment. In concert with these neurohormonal changes, urinary flow and sodium and potassium excretion were significantly and dose-dependently increased in the first 3 hours after administration of telmisartan 20 to 80mg.

In untreated patients with hypertension telmisartan had a significant natriuretic effect during the first 3 days of treatment. Urinary sodium excretion was significantly greater in recipients of telmisartan 80 mg/day than in those randomised to telmisartan 40 mg/day or placebo. The differences between groups were no longer significant after 15 days of treatment, although a trend toward greater total daily sodium excretion was apparent in recipients of the higher telmisartan dosage.

Significant increases in plasma renin activity and AII levels occurred in patients treated with telmisartan 40 to 120 mg/day in a randomised, placebo-controlled 4-week study.

Telmisartan has a potassium-sparing effect in patients with hypertension that attenuated the kaliuretic effect of hydrochlorothiazide when the 2 drugs were coadministered.

Systemic vascular resistance was reduced and systemic vascular and brachial artery compliance increased in patients with hypertension during treatment with telmisartan 40 mg/day. Telmisartan 40 mg/day reduced arterial stiffness in patients with type 2 diabetes mellitus and hypertension in a randomised, double-blind, placebo-controlled, 3-week, crossover study.

During 9 months of treatment with telmisartan 40 or 80 mg/day, blood pressure and left ventricular (LV) mass index were significantly reduced compared with baseline in patients with hypertension and mild to moderate LV hypertrophy. When introduced 7 days after the withdrawal of ACE inhibitors, single doses of telmisartan 10 to 80mg improved haemodynamic variables in patients with stable mild to moderate congestive heart failure enrolled in a multicentre, randomised, double-blind, placebo-controlled study.

In patients with mild to moderate congestive heart failure, no significant change in exercise capacity, ejection fraction, New York Heart Association class or health-related quality of life score occurred when enalapril 10mg twice daily as replaced with telmisartan 10 to 40 mg/day in a 12 week, randomised, double-blind, multicentre trial.

Pharmacokinetic Properties

There is a high degree of interindividual variability in the plasma concentration profile of telmisartan. As a result of saturable first-pass metabolism, the oral bioavailability of telmisartan is dose dependent (42.4% after a single 40mg oral dose) and maximum plasma concentrations (Cmax) increase disproportionately after oral administration. Administration with food reduced the bioavailability of a 40mg dose by 6%, thus telmisartan may be taken with or without food. Steady-state plasma concentrations were achieved after approximately 5 to 7 days. The area under the plasma concentration-time curve (AUC) of telmisartan was 1.2-fold greater in elderly females than males after administration of 120 mg/day for 7 days.

Telmisartan is extensively distributed to tissues (mean apparent volume of distribution at steady state was 460 to 510L in healthy male volunteers) and is highly bound (99.5%) to plasma proteins, including albumin, α-1-acid glycoprotein, γ-globulin and lipoproteins.

A pharmacologically inactive acylglucuronide conjugate, which comprised 16% of the drug in circulation after a single 40mg dose, is the only metabolite of telmisartan. Biliary-faecal excretion is the primary route of elimination of telmisartan and its metabolite. The mean terminal elimination half-life of the drug was ≈24 hours in healthy volunteers and patients with hypertension.

Cmax, AUC0–24 and AUC0–∞ of telmisartan were markedly reduced and the mean free fraction of the drug in plasma was approximately doubled in patients undergoing dialysis compared with healthy volunteers.

The absolute bioavailability of telmisartan was increased in patients with hepatic impairment (to 97.2%) and the Cmax and AUC0–∞ of telmisartan were approximately 3-fold greater in hepatically-impaired patients compared with healthy controls.

In healthy male volunteers, telmisartan had a small effect on plasma warfarin concentrations, but there was no change in the international normalised ratio.

AUC, Cmax and minimum plasma concentrations of digoxin increased during coadministration with telmisartan in healthy male volunteers. The increase in Cmin did not exceed the predefined range for a lack of interaction, but serum digoxin concentrations should be monitored during concomitant therapy with telmisartan.

Telmisartan had no effect on the pharmacokinetics of amlodipine, glibenclamide (glyburide), hydrochlorothiazide, ibuprofen, paracetamol (acetaminophen) or simvastatin.

Therapeutic Efficacy

Placebo-Controlled and Dose-Finding Studies

Oral telmisartan 20 to 160mg once daily consistently reduced supine SBP and DBP (primary end-point) to a significantly (p ≤ 0.05) greater extent than placebo at trough or throughout the 24-hour dosage interval in randomised, double-blind, multicentre studies in patients with mild to moderate hypertension or isolated systolic hypertension.

Generally, telmisartan 20 to 160 mg/day did not show a significant dose-response relationship with the exception of 1 study, where a statistically significant linear dose-response relationship for SBP was observed. Dosages above 80mg once daily did not result in further blood pressure reduction in patients with mild to moderate hypertension. The drug was generally more effective in White than in Black patients, although Black patients still experienced clinically meaningful reductions in blood pressure with telmisartan.

Comparisons with Other Antihypertensive Agents

Telmisartan 40mg titrated to 80 or 120mg once daily produced similar anti-hypertensive effects, as assessed by primary end-points, to amlodipine 5mg titrated to 10mg once daily or atenolol 50mg titrated to 100mg once daily (with or without the addition of hydrochlorothiazide if patients remained hypertensive) in 232 to 533 patients with mild to moderate hypertension in randomised, double-blind, multicentre, titration-to-response trials. Ambulatory blood pressure monitoring (ABPM) has shown that telmisartan 40mg titrated to 120mg provides better blood pressure control during night-time and in the last 4 hours of the dosage interval than amlodipine 5mg titrated to 10mg.

In randomised, double-blind studies of 4 to 52 weeks’ duration in patients with mild to moderate hypertension, telmisartan 20mg once daily titrated to 80 or 160mg (when patients remained hypertensive) was similar in efficacy to enalapril 5mg once daily titrated to 20mg or lisinopril 10mg once daily titrated to 40mg (hydrochlorothiazide was also added when patients remained hypertensive in these studies) and telmisartan 40 to 160mg once daily was at least as effective at reducing blood pressure as enalapril 20mg once daily and similar in efficacy to lisinopril 20mg once daily. Telmisartan 40 mg/day titrated to 80mg and enalapril 10 mg/day titrated to 20mg [with furosemide (frusemide) if patients remained hypertensive] appeared to reduce blood pressure to a similar extent in patients with mild to moderate hypertension and moderate renal failure.

Telmisartan 80mg once daily was more effective at reducing blood pressure measured by ABPM over the 18- to 24-hour postdose interval or the whole 24-hour postdose interval than submaximal dosages of losartan (50mg once daily) or valsartan (80mg once daily) and was as effective as the fixed-dose combination of losartan 50mg plus hydrochlorothiazide 12.5mg once daily. These randomised trials were conducted in patients with mild to moderate hypertension; 2 trials were nonblind, 1 was double-blind.

In patients with severe hypertension, telmisartan 80 mg/day titrated to 160 mg/day reduced blood pressure as effectively as enalapril 20 mg/day titrated to 40 mg/day (in patients who remained hypertensive on monotherapy, hydrochlorothiazide 25 mg/day and amlodipine 5 mg/day were added sequentially) in a randomised, nonblind, multicentre study.

In Combination and in Comparison with Hydrochlorothiazide

In randomised, double-blind trials, the combination of telmisartan 40 or 80 mg/day and hydrochlorothiazide 12.5 mg/day (as a fixed-dose combination in some trials) was more effective than each agent alone in patients with mild to moderate hypertension. Telmisartan monotherapy was generally more effective than hydrochlorothiazide monotherapy at lowering blood pressure in a similar patient group, but these agents were similar in efficacy in patients with isolated systolic hypertension. Telmisartan 40 or 80mg once daily administered alone or in combination with other antihypertensive agents produced a sustained antihypertensive effect for up to 1 (≈64% of patients) or >3 years (≈84% of patients) in 2 noncomparative extension studies.

Tolerability

According to pooled tolerability data, adverse events reported by >5300 patients who received telmisartan (including 1758 patients in placebo-controlled studies) were generally mild and transient and occurred at a similar incidence as those reported by placebo recipients. The only adverse events occurring at a markedly higher incidence with telmisartan than placebo were back pain (2.6 vs 0.9%), diarrhoea (2.8 vs 1.1%) and upper respiratory tract infection (6.7 vs 5.1%), although headache was much more common with placebo than telmisartan (7.1 vs 15.1%) [statistical analysis not reported]. 2.8% of patients who received telmisartan and 6.1% of placebo recipients discontinued treatment because of adverse events.

In randomised, double-blind or nonblind, comparative trials, telmisartan had a similar tolerability profile to amlodipine or atenolol (with or without hydrochlorothiazide), other AII receptor antagonists (valsartan and losartan) and hydrochlorothiazide alone or telmisartan in combination with hydrochlorothiazide (including telmisartan 40 or 80mg with hydrochlorothiazide as a fixed-dose combination), although oedema was more common with amlodipine than telmisartan.

Telmisartan was also at least as well tolerated as the ACE inhibitors lisinopril and enalapril. Furthermore, telmisartan produced a significantly lower incidence of dry cough than lisinopril in patients with a history of ACE inhibitor-related cough in a study for which this parameter was the primary end-point (15.6 vs 60%; p = 0.001). Telmisartan and enalapril, both in combination with hydrochlorothiazide and amlodipine, were similarly tolerated in patients with severe hypertension.

Dosage and Administration

Telmisartan, alone and in combination with other antihypertensive agents, is indicated for the treatment of hypertension. The usual recommended dosage is 40mg once daily. Some patients may experience benefit at a dosage of 20 mg/day. In patients in whom a satisfactory blood pressure response is not achieved, the dosage may be increased to a maximum of 80mg once daily. The maximum antihypertensive effect is generally attained 4 to 8 weeks after the start of treatment. As hydrochlorothiazide complements the blood pressure-lowering effect of telmisartan, the combination of telmisartan and a thiazide diuretic may be appropriate in some patients. Telmisartan may be given with or without food.

Dosage adjustments are not required on the basis of age, gender or renal dysfunction. The manufacturer recommends that telmisartan be used with caution in patients with hepatic impairment, in whom the dosage should not exceed 40 mg/day, and those with depleted intravascular volume.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Subscribe and save

Springer+ Basic
$34.99 /Month
  • Get 10 units per month
  • Download Article/Chapter or eBook
  • 1 Unit = 1 Article or 1 Chapter
  • Cancel anytime
Subscribe now

Buy Now

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Table I
Fig. 1
Table II
Table III
Table IV
Table V
Table VI
Table VII
Fig. 2
Fig. 3

Similar content being viewed by others

Notes

  1. The dose of AII that produced the maximal increase in SBP (≈30mm Hg) was determined the day prior to the study for each individual and ranged from 2 to 5μg. AII challenges were repeated for 48 hours after administration of telmisartan or placebo.

  2. In Canada the recommended dosage is 80 mg/day.[79]

References

  1. Nicholls MG, Charles CJ, Crozier IG, et al. Blockade of the renin-angiotensin system. J Hypertens 1994; 12 Suppl. 10: S95-103

    Google Scholar 

  2. Dzau VJ. Molecular biology of angiotensin II biosynthesis and receptors. Can J Cardiol 1995 Aug; 11 Suppl. F: 21F–6F

    PubMed  CAS  Google Scholar 

  3. Siegl PKS, Kivlighn SD, Broten TP, et al. Pharmacology of angiotensin II receptor antagonists: comparison with renin inhibitors and angiotensin-converting enzyme inhibitors. Expert Opin Invest Drug 1994; 3(9): 925–44

    Article  CAS  Google Scholar 

  4. Burnier M, Brunner HR. Angiotensin II receptor antagonists. Lancet 2000; 355(9204): 637–45

    Article  PubMed  CAS  Google Scholar 

  5. Rodgers JE, Patterson JH. Angiotensin II-receptor blockers: clinical relevance and therapeutic role. Am J Health Sys Pharm 2001; 58(8): 671–83

    CAS  Google Scholar 

  6. McClellan KJ, Markham A. Telmisartan. Drugs 1998 Dec; 56(6): 1039–44

    Article  PubMed  CAS  Google Scholar 

  7. Wienen W, Entzeroth M, van Meel JCA, et al. A review on telmisartan: A novel, long-acting angiotensin II-receptor antagonist. Cardiovasc Drug Rev 2000; 18(2): 127–56

    Article  CAS  Google Scholar 

  8. Wienen W, Hauel N, Busch U, et al. Characterization of the pharmacodynamic/PK profile of BIBR 277-1-O-acylglucuronide, the metabolite of telmisartan [abstract no. P.42 and poster]. J Hum Hypertens 1999 May; 13 Suppl. 3: S11

    Article  Google Scholar 

  9. Wienen W, Hauel N, van Meel JCA, et al. Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br J Pharmacol 1993 Sep; 110: 245–52

    Article  PubMed  CAS  Google Scholar 

  10. Wienen W, Entzeroth M. Effects on binding characteristics and renal function of the novel, non-peptide angiotensin II antagonist BIBR 277 in the rat. Hypertension 1994; 12: 119–28

    Article  CAS  Google Scholar 

  11. Entzeroth M, Hadamovsky S. Angiotensin II receptors in the rat lung are of the A11-1 subtype. Eur J Pharmacol — Molec Pharmacol 1991; 206: 237–41

    Article  CAS  Google Scholar 

  12. Wienen W, Entzeroth M, Diederen W, et al. Pharmacology and antihypertensive effects of telmisartan, an AT1-selective angiotensin II receptor antagonist [poster]. 1st International Symposium on Angiotensin II Antagonism; 1997 Sep 28–Oct 1; London

  13. Wagner J, Drab M, Bohlender J, et al. Effects of AT1 receptor blockade on blood pressure and the renin-angiotensin system in spontaneously hypertensive rats of the stroke prone strain. Clin Exp Hypertens 1998; 20(2): 205–21

    Article  PubMed  CAS  Google Scholar 

  14. van Meel JCA, Redemann N, Haigh RM. Hypotensive effects of the angiotensin II antagonist telmisartan in conscious chronically-instrumented transgenic rats. Arzneimittel Forschung 1996 Aug; 46(II) (8): 755–9

    PubMed  Google Scholar 

  15. Wienen W, Richard S, Champeroux P, et al. Comparative antihypertensive and renoprotective effects of telmisartan and lisinopril after long-term treatment in hypertensive diabetic rats. J RAAS 2001; 2(1): 31–6

    CAS  Google Scholar 

  16. Winquist R, Panzenbeck M, Madwed J, et al. The effects of BIBR277, an angiotensin II type I (AT1) receptor antagonist in conscious monkeys [abstract no. 5113]. FASEB J 1994 Mar 18; 8 (5 Pt II): A882

    Google Scholar 

  17. Böhm M, Lee MA, Kreutz R, et al. Angiotensin II receptor blockade in TGR(mREN2)27: effects of renin-angiotensin-system gene expression and cardiovascular functions. J Hypertens 1995 Aug; 13: 891–9

    Article  PubMed  Google Scholar 

  18. Böhm M, Lippoldt A, Wienen W, et al. Reduction of cardiac hypertrophy in TGR(mREN2)27 by angiotensin II receptor blockade. Mol Cell Biochem 1996 Oct–Nov; 163–164: 217–21

    Article  Google Scholar 

  19. Schierok H, Pairet M, Hauel N, et al. Effects of telmisartan on renal excretory function in conscious dogs. J Int Med Res 1997; 29: 131–9

    Google Scholar 

  20. Nakai T, Satoh K, Kosugi T, et al. Participation of angiotensin II and bradykinin in contractile function in dog stunned myocardium. Eur J Pharmacol 1999; 382(3): 187–96

    Article  PubMed  CAS  Google Scholar 

  21. Strohmenger H-U, Lindner KH, Wienen W, et al. Effects of the AT1-selective angiotensin II antagonist, telmisartan, on hemodynamics and ventricular function after cardiopulmonary resuscitation in pigs. Resuscitation 1997; 35: 61–8

    Article  PubMed  CAS  Google Scholar 

  22. Stangier J, Su CAPF, van Heiningen PNM, et al. The inhibitory effect of telmisartan on the blood pressure response to angiotensin II challenge [abstract no. PN.23 and poster]. J RAAS 2001 Mar; 2(1): 83

    Google Scholar 

  23. Neutel JM, Smith DHG. Dose response and antihypertensive efficacy of the AT1 receptor antagonist telmisartan in patients with mild to moderate hypertension. Adv Ther 1998 Jul/Aug; 15: 206–17

    CAS  Google Scholar 

  24. Karlberg BE, Lins L-E, Hermansson K. Efficacy and safety of telmisartan, a selective AT1 receptor antagonist, compared with enalapril in elderly patients with primary hypertension. TEES Study Group. J Hypertens 1999 Feb; 17: 293–302

    Article  PubMed  CAS  Google Scholar 

  25. Lacourcière Y, Lenis J, Orchard R, et al. A comparison of the efficacies and duration of action of the angiotensin II receptor blockers telmisartan and amlodipine. Blood Pres Monit 1998; 3(5): 295–302

    Google Scholar 

  26. Mallion JM, Siche JP, Lacourcière Y, et al. ABPM comparison of the antihypertensive profiles of the selective angiotensin II receptor antagonists telmisartan and losartan in patients with mild-to-moderate hypertension. J Hum Hypertens 1999; 13(10): 657–64

    Article  PubMed  CAS  Google Scholar 

  27. Littlejohn T, Mroczek W, Marbury T, et al. A prospective, randomized, open-label trial comparing telmisartan 80 mg with valsartan 80 mg in patients with mild to moderate hypertension using ambulatory blood pressure monitoring. Can J Cardiol 2000 Sep; 16(9): 1123–32

    PubMed  CAS  Google Scholar 

  28. McGill JB, Reilly PA. Combination treatment with telmisartan and hydrochlorothiazide in black patients with mild to moderate hypertension. Clin Cardiol 2001 Jan; 24: 66–72

    Article  PubMed  CAS  Google Scholar 

  29. Delgado AJ, Delgado-Almeida AR, Celis SI, et al. Improved LV function, systemic vascular and brachial artery parameters in hypertension: the Venezuelan telmisartan study [abstract no. P-294]. Am J Hypertens 2001 Apr; 14 (4 Pt 2): 127A

    Article  Google Scholar 

  30. Smith DHG, Matzek KM, Kempthorne-Rawson J. Dose response and safety of telmisartan in patients with mild to moderate hypertension. J Clin Pharmacol 2000; 40: 1380–90

    PubMed  CAS  Google Scholar 

  31. Burgess ED, Buckley S. Acute natriuretic effect of telmisartan in hypertensive patients [abstract]. Can J Cardiol 2000 Sep; 16 Suppl. F: 106F

    Google Scholar 

  32. Burgess ED, Buckley S. Long-term effect of telmisartan on sodium excretion in hypertensive patients [abstract]. Can J Cardiol 2000 Sep; 16 Suppl. F: 106F

    Google Scholar 

  33. McGill JB, Reilly PA. Telmisartan reverses the potassium loss associated with high doses of hydrochlorothiazide [abstract no. PC.22 and poster]. J RAAS 2001 Mar; 2(1): 63

    Google Scholar 

  34. Asmar R, Gosse P, Topouchian J, et al. Effects of telmisartan on arterial compliance and endothelial function in type 2 diabetes patients with essential hypertension [abstract no. P-254]. Am J Hypertens 2001 Apr; 14 (4 Pt 2): 114A

    Article  Google Scholar 

  35. Mattioli AV, Fortanesi L, Vandelli R, et al. Regression of left ventricular hypertrophy on serial echocardiography in patients treated with telmisartan [abstract no. P-261]. Am J Hypertens 2001 Apr; 14 (4 Pt 2): 116A

    Article  Google Scholar 

  36. Parker AB, Azevedo ER, Baird MG, et al. ARCTIC: assessment of haemodynamic response in patients with congestive heart failure to telmisartan: A multicentre dose-ranging study in Canada. Am Heart J 1999; 138 (5 Pt 1): 843–8

    Article  PubMed  CAS  Google Scholar 

  37. Dunselman PHJM. Effects of the replacement of the angiotensin converting enzyme inhibitor enalapril by the angiotensin II receptor blocker telmisartan in patients with congestive heart failure. Int J Cardiol 2001 Feb; 77: 131–8

    Article  PubMed  CAS  Google Scholar 

  38. Stangier J, Su CAPF, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. J Int Med Res 2000; 28(4): 149–67

    PubMed  CAS  Google Scholar 

  39. Stangier J, Su C-APF, Bickl R, et al. Pharmacokinetics of single-dose telmisartan 120 mg given during and between hemodialysis in subjects with severe renal insufficiency: comparison with healthy volunteers. J Clin Pharmacol 2000; 40: 1365–72

    PubMed  CAS  Google Scholar 

  40. Stangier J, Su C-APF, Schöndorfer G, et al. Pharmacokinetics and safety of intravenous and oral telmisartan 20 mg and 120 mg in subjects with hepatic impairment compared with healthy volunteers. J Clin Pharmacol 2000; 40: 1355–64

    PubMed  CAS  Google Scholar 

  41. Boehringer Ingelheim Pharmaceuticals Inc. Micardis (telmisartan) tablets 40mg and 80mg prescribing information. Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT, USA: Jun 1999

  42. Stangier J, Schmid J, Türck D, et al. Absorption, metabolism, and excretion of intravenously and orally administered [14C]telmisartan in healthy volunteers. J Clin Pharmacol 2000; 40: 1312–22

    PubMed  CAS  Google Scholar 

  43. Ebner T, Heinzel G, Prox A, et al. Disposition and chemical stability of telmisartan 1-O-acylglucuronide. Drug Metab Dispos 1999; 27(10): 1143–9

    PubMed  CAS  Google Scholar 

  44. Schmid J, Beschke K, Busch U, et al. Structure elucidation of the main metabolite of telmisartan [abstract no. P.47 and poster]. J Hum Hypertens 1999 May; 13 Suppl. 3: S13

    Google Scholar 

  45. Ebner T, Roth W. In vitro glucuronidation of telmisartan, a novel angiotensin II receptor antagonist [abstract no. P.44 and poster]. J Hum Hypertens 1999 May; 13 Suppl. 3: S12

    Google Scholar 

  46. Stangier J, Su C-APF, Hendriks MGC, et al. Steady-state pharmacodynamics and pharmacokinetics of warfarin in the presence and absence of telmisartan in healthy male volunteers. J Clin Pharmacol 2000; 40: 1331–7

    PubMed  CAS  Google Scholar 

  47. Stangier J, Su C-APF, Hendriks MGC, et al. The effect of telmisartan on the steady-state pharmacokinetics of digoxin in healthy male volunteers. J Clin Pharmacol 2000; 40: 1373–9

    PubMed  CAS  Google Scholar 

  48. Schaefer A, Lücker PW, Birkel M, et al. Pharmacokinetic evidence of a lack of interaction between telmisartan and simvastatin. Poster presented at the 4th International Symposium on Angiotensin II Antagonism; 2001 Apr 3–5; London

  49. Stangier 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

    PubMed  CAS  Google Scholar 

  50. Heuer HJ, Dilger C, Michael-Hepp J, et al. Influence of repeated oral doses of telmisartan on the clinical pharmacology of glibenclamide in healthy subjects [abstract no. 38]. Eur J Clin Pharmacol 1998 Aug; 54(6): A12

    Google Scholar 

  51. Stangier J, Su C-APF, Fraunhofer A, et al.Pharmacokinetics of acetaminophen and ibuprofen when coadministered with telmisartan in healthy volunteers. J Clin Pharmacol 2000; 40: 1338–46

    PubMed  CAS  Google Scholar 

  52. Yong C-L, Dias VC, Stangier J. Multiple-dose pharmacokinetics of telmisartan and of hydrochlorothiazide following concurrent administration in healthy subjects. J Clin Pharmacol 2000; 40: 1323–30

    Google Scholar 

  53. Guidelines Subcommittee of the World Health Organization — International Society of Hypertension. 1999 World Health Organization — International Society of Hypertension Guidelines for the Management of Hypertension. J Hypertens 1999 Feb; 17: 151–83

    Google Scholar 

  54. Joint National Committee on Prevention Detection Evaluation and Treatment of High Blood Pressure, National High Blood Pressure Education Program Coordinating Committee. The Sixth Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. Arch Intern Med 1997 Nov 24; 157: 2413–46

    Article  Google Scholar 

  55. Ramsay LE, Williams B, Johnston GD, et al. Guidelines for management of hypertension: report of the third working party of the British Hypertension Society. J Hum Hypertens 1999 Sep; 13: 569–92

    Article  PubMed  CAS  Google Scholar 

  56. Ramsay LE, Williams B, Johnston GD, et al. British Hypertension Society guidelines for hypertension management 1999: summary. BMJ 1999 Sep 4; 319: 630–5

    Article  PubMed  CAS  Google Scholar 

  57. Kolloch RE, Neutel JM, Plouin PF. Comparison of telmisartan monotheraphy with losartan + hydrochlorothiazide in mild-to-moderate hypertension [abstract no. P2.33 and poster]. J Hypertens 2000 Jun; 18 Suppl. 2: S97

    Google Scholar 

  58. Alcocer L, Fernandez-Bonetti P, Olvera-Ruiz R, et al. Superior antihypertensive efficacy of telmisartan, a new AT1 antagonist compared to atenolol at relative low fixed doses [abstract no. P3.34]. J Hypertens 2000 Jun; 18 Suppl. 2: S160

    Google Scholar 

  59. Lacourciere Y. The incidence of cough: a comparison of lisinopril, placebo and telmisartan, a novel angiotensin II antagonist. Telmisartan Cough Study Group. Int J Clin Pract 1999; 53: 99–103

    CAS  Google Scholar 

  60. Elliot HL. The efficacy and safety of telmisartan compared to atenolol and placebo in patients with hypertension [abstract no. E116 and poster]. Am J Hypertens l998 Apr; 11(4): 124A

    Article  Google Scholar 

  61. Hannedouche T, Chanard J, Baumelou B. Safety and efficacy of telmisartan versus enalapril in moderate renal failure patients with mild-to-moderate hypertension [abstract no. PF10 and poster]. J RAAS 2000 Mar; 1: 96

    Google Scholar 

  62. Smith DHG, Neutel JM, Morgenstern P. Once-daily telmisartan compared with enalapril in the treatment of hypertension. Adv Ther 1998 Jul/Aug; 15(4): 229–40

    CAS  Google Scholar 

  63. Manolis AJ, Reid JL, de Zeeuw D, et al. Angiotensin II receptor antagonist micardis in isolated systolic hypertension (ARAMIS) study: efficacy and safety of telmisartan 20, 40 or 80 mg versus hydrochlorothiazide or placebo [abstract no. P2.154]. J Hypertens 2001 Jun; 19 Suppl. 2: S147

    Google Scholar 

  64. Freytag F, Schelling A, Meinicke T, et al. Comparison of 26-week efficacy and tolerability of telmisartan and atenolol, in combination with hydrochlorothiazide as required, in the treatment of mild to moderate hypertension: a randomized, multicenter study. Clin Ther 2001 Jan; 23: 108–23

    Article  PubMed  CAS  Google Scholar 

  65. Neutel JM, Frishman WH, Oparil S, et al. Comparison of telmisartan with lisinopril in patients with mild-to-moderate hypertension. Am J Ther 1999; 6(3): 161–6

    Article  PubMed  CAS  Google Scholar 

  66. Neutel JM, Smith DHG, Reilly PA. The efficacy and safety of telmisartan compared to enalapril in patients with severe hypertension. Int J Clin Pract 1999; 53: 175–8

    PubMed  CAS  Google Scholar 

  67. Hansson L, Hedner T, Dahlöf B. Prospective randomized open blinded end-point (PROBE) study. A novel design for intervention trials. Blood Press 1992; 1: 113–9

    CAS  Google Scholar 

  68. Laws D. Safety and efficacy of long-term exposure to monotherapy or combination therapy with telmisartan [abstract no. PC.35 and poster]. J RAAS 2001 Mar; 2: 66

    Google Scholar 

  69. Lacourcière Y, Tytus R, O’Keefe D, et al. Efficacy and tolerability of a fixed-dose combination of telmisartan plus hydrochlorothiazide in patients uncontrolled with telmisartan monotherapy. J Hum Hypertens. In press

  70. Lacourcière Y, Martin K. Comparison of a fixed-dose combination of telmisartan 40 mg plus hydrochlorothiazide 12.5 mg with telmisartan 40 mg in the control of mild-to-moderate hypertension. Am J Ther. In press

  71. McGill JB, Reilly PA. Telmisartan plus hydrochlorothiazide versus telmisartan or hydrochlorothiazide monotherapy in patients with mild to moderate hypertension: a multicenter, randomized, double-blind, placebo-controlled, parallel-group trial. Clin Ther 2001 June; 23(6): 833–50

    Article  PubMed  CAS  Google Scholar 

  72. Neutel JM. Ambulatory blood pressure monitoring to assess the comparative efficacy and duration of action of a novel new angiotensin II receptor blocker — telmisartan. Blood Press 2001; 10 Suppl. 1: 27–32

    Article  Google Scholar 

  73. Holwerda NJ, Freytag F, Meinicke T, et al. Long-term, open-label follow-up study of telmisartan monotherapy and combination therapy [abstract no. 72]. J Hypertens 2001 Jun; 19 Suppl. 2: S268

    Google Scholar 

  74. Neutel JM, Klein C, Meinick TW, et al. Long-term efficacy and tolerability of telmisartan as monotherapy and in combination with other antihypertensive medications [abstract no. P-232 and poster]. Am J Hypertens 2001 Apr; 14 (4 Pt 2): 106A

    Article  Google Scholar 

  75. Boehringer Ingelheim. Micardis: product monograph. Second ed., 2000

  76. Overlack A. ACE inhibitor-induced cough and bronchospasm: incidence, mechanisms and management. Drug Saf 1996 Jul; 15(1): 72–8

    Article  PubMed  CAS  Google Scholar 

  77. Morice AH, Brown MJ, Higenbottam T. Cough associated with angiotensin converting enzyme inhibition. J Cardiovasc Pharmacol 1989; 13 Suppl. 3: S59-62

    Google Scholar 

  78. Boehringer Ingelheim. Micardis summary of product characteristics. European Agency for the Evaluation of Medicinal Products. European public assessment report [on line]. Available from: URL: http://www.eudra.org/humandocs/humans/EPAR/Micardis/Micardis.htm [Accessed 2001 Jul 24]

  79. Boehringer Ingelheim. Micardis (telmisartan) tablets 40 mg and 80 mg. Boehringer Ingelheim (Canada) Ltd, Burlington, (ON)

  80. Telmisartan. British National Formulary 41. London British Medical Association, Royal Pharmaceutical Society of Great Britain, 2001 Mar: 96

  81. Blackwell B. Drug therapy: patient compliance. N Engl J Med 1973 Aug 2; 289(5): 249–52

    Article  PubMed  CAS  Google Scholar 

  82. Meredith PA. Intrinsically long-acting agents compared with long-acting chronoformulations. Blood Press Monit 2000; 5 Suppl. 1: S25–30

    Article  PubMed  Google Scholar 

  83. Kaplan NM. Should new drugs be used without outcome data? Implications of ALLHAT and ELITE II. Arch Intern Med 2001 Feb 26; 161: 511–2

    Article  PubMed  CAS  Google Scholar 

  84. Lasagna L. Diuretics vs alpha-blockers for treatment of hypertension: lessons from ALLHAT. JAMA 2000 Apr 19; 283(15): 2013–4

    Article  PubMed  CAS  Google Scholar 

  85. The ALLHAT Officers and Coordinators for the ALLHAT Collaboration Research Group. Major cardiovascular events in hypertensive patients randomized to doxazosin vs chlorthalidone: the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). JAMA 2000 Apr 19; 283(15): 1967–75

    Article  Google Scholar 

  86. Boehringer Ingelheim. ONTARGET fact sheet: ongoing telmisartan alone and in combination with ramipril global end-point trial. Boehringer Ingelheim 2001. (Data on file)

  87. Boehringer Ingelheim. TRANSCEND fact sheet: The ACE-I intolerant study telmisartan randomized assessment study in ACE-I intolerant subjects with cardiovascular disease. Boehringer Ingelheim 2001. (Data on file)

  88. Song JC, White CM. Pharmacologic, pharmacokinetic, and therapeutic differences among angiotensin II receptor antagonists. Pharmacotherapy 2000; 20(2): 130–9

    Article  PubMed  CAS  Google Scholar 

  89. Oparil S. Newly emerging pharmacologic differences in angiotensin II receptor blockers. Am J Hypertens 2000; 13 (1 Pt 2): 18S–24S

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Miriam Sharpe, Blair Jarvis & Karen L. Goa

Authors
  1. Miriam Sharpe
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Blair Jarvis
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Karen L. Goa
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Miriam Sharpe.

Additional information

Various sections of the manuscript reviewed by: R.W. Bilous, James Cook University Hospital, Middlesbrough, England; L. Brown, Department of Physiology and Pharmacology, University of Queensland, Brisbane, Queensland, Australia; R.R. Castillo, Manila Doctors Hospital, Manila, The Philippines; L. de Angelis, Dipartimento di Scienze Biomediche, Università degli Studi di Trieste, Trieste, Italy; P.A. Meredith, Department of Medicine and Therapeutics, Gardiner Institute, Western Infirmary, Glasgow, Scotland; M. Tan, Mount Elizabeth Medical Centre, Singapore; M.H. Weinberger, Hypertension Research Center, Indiana University School of Medicine, Indianapolis, Indiana, USA.

Data Selection

Sources: Medical literature published in any language since 1966 on telmisartan, identified using Medline and EMBASE, supplemented by AdisBase (a proprietary database of Adis International). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.

Search strategy: Medline search terms were ‘telmisartan’ or ‘BIBR 277’. EMBASE search terms were ‘telmisartan’ or ‘BIBR 0277’ or ‘BIBR 277’. AdisBase search terms were ‘telmisartan’ or ‘BIBR 277’. Searches were last updated 23 July, 2001.

Selection: Studies in patients with hypertension who received telmisartan. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.

Index terms: Hypertension, telmisartan, pharmacodynamics, pharmacokinetics, therapeutic use.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Sharpe, M., Jarvis, B. & Goa, K.L. Telmisartan. Drugs 61, 1501–1529 (2001). https://doi.org/10.2165/00003495-200161100-00009

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-200161100-00009

Keywords

Search

Navigation