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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C33H30N4O2
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RX_link
http://www.rxlist.com/cgi/generic2/telmisartan.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
514.617 g/mol
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Melting Point
261-263oC
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H2O Solubility
Practically insoluble
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State
Solid
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LogP
7.245
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Dosage Forms
Tablets
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Indication
For the treatment of hypertension.
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Pharmacology
Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects. This observation is currently being explored in clinical trials. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmisartan works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.
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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).
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side effects and 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.
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Patient Information
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Organisms Affected
Humans and other mammals