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QuickView for Telmisartan (compound)


PubChem
Name: telmisartan
PubChem Compound ID: 65999
Molecular formula: C33H30N4O2
Molecular weight: 514.617 g/mol
Synonyms:
(1,1'-Biphenyl)-2-carboxylic acid, 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-; Kinzalmono; 144701-48-4; 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid; YM-086; KBio3_001958; Spectrum4_001261; Micardis (TN); Pritor; Spectrum2_001976.
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DrugBank
Identification
Name: telmisartan
Name (isomeric): DB00966
Drug Type: small molecule
Synonyms:
BIBR 277; BIBR 277SE
Brand: Pritor, Micardis, Micardis HCT
Brand name mixture: Micardis Plus(Hydrochlorothiazide + Telmisartan)
Category: Angiotensin II Type 1 Receptor Blockers, Angiotensin-converting Enzyme Inhibitors
CAS number: 144701-48-4
Pharmacology
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).
Pharmacology:
Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPARγ agonistic proper...
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Mechanism of Action:
Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT1-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 dec...
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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).
Protein binding: Highly bound to plasma proteins (>99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent.
Biotransformation: Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.
Route of elimination: 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).
Half Life: Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.
Clearance: >800 mL/min
Toxicity: Intravenous LD50 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.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
PotassiumPotassium may increase the hyperkalemic effect of Telmisartan. Monitor serum potassium levels during concomitant use.
TrandolaprilThe angiotensin II receptor blocker, Telmisartan, may increase the adverse effects of Trandolapril.
PiroxicamConcomitant use of Telmisartan and Piroxicam may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
Potassium ChloridePotassium Chloride may increase the hyperkalemic effect of Telmisartan. Monitor serum potassium levels during concomitant use.
NabumetoneConcomitant use of Telmisartan and Nabumetone may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
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