About: Telmisartan     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/description
  • Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11558835 # Smith DH: Treatment of hypertension with an angiotensin II-receptor antagonist compared with an angiotensin-converting enzyme inhibitor: a review of clinical studies of telmisartan and enalapril. Clin Ther. 2002 Oct;24(10):1484-501. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12462282 # Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20502601 # Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20448797 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours. (en)
http://linked.open...ugbank/indication
  • Used alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors). (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Telmisartan (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT<sub>1</sub>-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPAR&gamma;, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPAR&gamma; activators. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively). (en)
http://linked.open.../drugbank/synonym
  • Telmisartan (en)
  • Micardis (en)
  • BIBR 277 (en)
  • 4'-[(1,7'-Dimethyl-2'-propyl-1H,3'h-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid (en)
  • 4'-((1,4'-Dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid (en)
  • 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid (en)
  • 4'-[(1,4'-Dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid (en)
http://linked.open...drugbank/toxicity
  • Intravenous LD<sub>50</sub> in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. (en)
http://linked.open...umeOfDistribution
  • * 500 L (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • Highly bound to plasma proteins (&gt;99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent. (en)
http://linked.open...ynthesisReference
  • # Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20502601 (en)
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foaf:page
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http://linked.open...ugbank/absorption
  • Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food). (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...aco2-Permeability
http://linked.open...casRegistryNumber
  • 144701-48-4 (en)
http://linked.open...rugbank/clearance
  • * >800 mL/min (en)
http://linked.open...gbank/containedIn
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