Micardis


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Micardis

TelmisartanSystematic (IUPAC) name2-(4-{methyl}phenyl)benzoic acidIdentifiersCAS number144701-48-4ATC codeC09CA07PubChem65999DrugBankAPRD01247Chemical dataFormulaC33H30N4O2 Mol. mass514.617 g/molPharmacokinetic dataBioavailability42–100%Protein binding≥99.5%MetabolismMinimal hepaticHalf life24 hoursExcretionFaecal 97%Therapeutic considerationsPregnancy cat.D (Au), D (U.S.)Legal statusS4 (Au), POM (UK), ℞-only (U.S.)RoutesOralTelmisartan (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).// AdministrationThe usually effective dose Telmisartan ( Teli marketed by Cadila) is 40 mg once daily. Some patients may already benefit at a daily dose of 20 mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum of 80 mg once daily. Mode of actionTelmisartan ( Teli marketed by cadila pharma) 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. 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). Telmisartan has binding affinity 3000 times with AT-2 receptor then AT-1 receptor.Telmisartan is also having maximum half life in sartans - 24 Hrs. IndicationTelmisartan is indicated in the treatment of essential hypertension. Key Recent Clinical Trials ONTARGETThe 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.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. The results were then published in The New England Journal of Medicine in April 2008.25,620 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 of 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. TRANSCENDAs 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 were published in the Lancet, September 2008. In an accompanying editorial, the following is stated: "Overall, data supporting use of angiotensin-receptor blockers to prevent vascular events in various cardiovascular groups, other than heart failure, are incomplete. TRANSCEND's results challenge the non-inferiority shown in ONTARGET and suggest no more than a modest effect, if any at all." PROTECTIONThe PROTECTION programme (Programme of Research tO show Telmisartan End-organ proteCTION) consisted of ten trials with 6,875 patients from 32 countries.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. See alsoAngiotensin Receptor Blockers: Drug discovery and development
.Results of a randomized trial show no evidence that extended-release dipyridamole (Aggrenox, Boehringer Ingelheim), aspirin, or telmisartan (Micardis, Boehringer Ingelheim) have neuroprotective effects on either disability due to a recurrent stroke or cognitive decline


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Micardis

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About MICARDIS | Micardis

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