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News About Telmisartan

14-September-2008 18:02:41 - Telmisartan Telmisartan Systematic IUPAC name 2-4-4-methyl-6-1-methylbenzoimidazol-2-yl- 2-propyl-benzoimidazol-1-ylmethylphenyl benzoic acid Identifiers CAS number 144701-48-4 ATC code C09CA07 PubChem 65999 DrugBank APRD01247 Chemical data Formula C33H30N4O2 Mol. mass 514.617 g/mol Pharmacokinetic data Bioavailability 42-100% Protein binding ≥99.5% Metabolism Minimal hepatic Half life 24 hours Excretion Faecal 97% Therapeutic considerations Pregnancy cat. D Au, D U.S. Legal status S4 Au, POM UK, ℞-only U.S. Routes Oral Telmisartan INN pronounced /tɛlmɪˈsɑrtən/ is an angiotensin II receptor antagonist ARB used in the management of hypertension. It is marketed under the trade names Pritor or Kinzal Bayer Schering Pharma, Micardis Boehringer Ingelheim, Telma Glenmark Pharma, Telday Torrent Pharmaceuticals and Teleact D by Ranbaxy. Contents 1 Administration 2 Mode of action 3 Indication 4 Key Recent Clinical Trials 5 External links 6 References Administration The usually effective dose is 40mg once daily. Some patients may already benefit at a daily dose of 20mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum of 80mg once daily. 1 Mode of action Telmisartan is an Angiotensin Receptor Blocker ARB that shows high affinity for the angiotensin II type 1 AT1 receptors, has a long duration of action, and has the longest half-life of any ARB. 1,2 In addition to blocking the Renin-Angiotensin System RAS, telmisartan acts as a selective modulator of Peroxisome Proliferator-Activated Receptor-gamma PPAR-γ, a central regulator of insulin and glucose metabolism. It is believed that telmisartan's dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease CVD. 1,2 Indication Telmisartan is indicated in the treatment of essential hypertension. 1 Main article: Angiotensin II receptor antagonist Key Recent Clinical Trials ONTARGET The ONTARGET Trial Programme The Ongoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial was one of the largest ARB clinical study programmes ever undertaken. 3 Professor Salim Yusuf, Lead Investigator and Director of the Population Health Research Institute at McMaster University, Hamilton, Canada, presented the results of the landmark ONTARGET trial at the hotline session of the 57th Annual Scientific Session of the American College of Cardiology ACC in Chicago, USA. 4 The results were then published in The New England Journal of Medicine in April 2008. 3 25,620 patients from 733 centres in 41 countries were randomised for 5.5 years of treatment of either telmisartan, the ACE inhibitor ramipril or a combination of the two. The study aimed to investigate the role of telmisartan in Cardiovascular CV protection through the primary composite outcome of death from CV causes, myocardial infarction, stroke or hospilization for heart failure, in high CV risk patients. The results revealed that telmisartan was as effective as ramipril but with lower rates or cough and angioedema which led to fewer discontinuations. The combination group experienced similar efficacy but with increased risk of hypotensive symptoms. The results showed that telmisartan is as effective as ramipril, better tolerated and associated with higher treatment compliance. Moreover, even in a patient population selected to tolerate ACE inhibitors, telmisartan was shown to be better tolerated and associated with higher treatment compliance than ramipril. 4 TRANSCEND As part of the ONTARGET study, patients who could not tolerate ACE inhibitors were randomly assigned to receive either telmisartan or placebo as part of the TRANSCEND Telmisartan Randomized Assessment Study in ACE Intolerant Subjects with Cardiovascular Disease CVD study. Results from the TRANSCEND study are to be released in late 2008. 3 PROTECTION The PROTECTION programme Programme of Research tO show Telmisartan End-organ proteCTION consisted of ten trials with 6,875 patients from 32 countries. 5 The programme examined the efficacy of telmisartan or telmisartan/ hydrochlorothiazide at different stages of the cardiovascular and renal continuum. The trials were conducted in patients with varying degrees of cardiovascular risk from around the world. The 10 studies in the PROTECTION programme evaluated the effect of telmisartan on blood pressure control in two general patient populations: patients at high risk for cardiovascular disease and patients with various renal pathologies. In all the studies, telmisartan was compared either to placebo or to a gold standard medication such as the ACE inhibitors ramipril and enalapril or the ARBs losartan and valsartan. Telmisartan met and sometimes exceeded the gold standards ACEIs and other ARBs during the PROTECTION programme. In at-risk patient populations, telmisartan induced strong and sustained blood pressure lowering throughout the critical morning period where CV risk is highest and renoprotective effects at every stage of the renal continuum. 5,6 External links http://www.pritor.com http://www.micardis.com/com/index.jsp http://www.pslgroup.com/dg/e6dce.htm http://www.ICMAedu.com http://www.emea.europa.eu References 1 Pritor prescribing information 2 Benson SC et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension 2004 May; 435: 993-1002. 3 The ONTARGET Investigators. Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events N Engl J Med 2008;358:1547-59. 4 http://www.ICMAedu.com 5 Weber M. The telmisartan Programme of Research tO show Telmisartan End-organ proteCTION PROTECTION® programme. J Hypertens 2003;21 Suppl 6:S37-S46. 6 http://www.pritor.com v d e Agents acting on the renin-angiotensin system C09 ACE inhibitors Alacepril Benazepril Captopril Cilazapril Delapril Enalapril Fosinopril Imidapril Lisinopril Moexipril Perindopril Quinapril Ramipril Rentiapril Spirapril Temocapril Trandolapril Zofenopril Angiotensin II receptor antagonists AIIRA Azilsartan Candesartan Eprosartan Irbesartan Losartan Olmesartan Tasosartan Telmisartan Valsartan Renin inhibitors Aliskiren Remikiren Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Telmisartan Categories: Angiotensin II receptor antagonists | Pharmacology stubs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Español Italiano Magyar Nederlands Polski Português This page was last modified on 9 September 2008, at 11:56

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