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QuickView for Torasemide (compound)


PubChem
Name: torsemide
PubChem Compound ID: 41781
Molecular formula: C16H20N4O3S
Molecular weight: 348.421 g/mol
Synonyms:
KBio2_007392; Unat; CAS-56211-40-6; CCRIS 6736; GJ-1090; Luprac (TN); Torasemidum [INN-Latin]; KBio2_002256; Luprac; Torasemida [INN-Spanish].
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DrugBank
Identification
Name: torsemide
Name (isomeric): DB00214
Drug Type: small molecule
Synonyms:
Torasemidum [INN-Latin]; Torasemida [INN-Spanish]; Torsemide
Brand: Demadex, Luprac
Category: Diuretics, Antihypertensive Agents
CAS number: 56211-40-6
Pharmacology
Indication: For the treatment of edema associated with congestive heart failure, renal disease, or hepatic disease. Also for the treatment of hypertension alone or in combination with other antihypertensive agents.
Pharmacology:
Torasemide (INN) or torsemide (USAN) is a novel loop diuretic belonging to pridine sulphonyl urea. It differs form other thiazide diuretics in that a double ring system is incorporated into its structure. Like thiazides, loop diuretics must be secreted into the tubular fluid by proximal tubule cells. In the thick ascending loop Na+ and Cl- reabsorp...
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Mechanism of Action:
Torasemide inhibits the Na+/K+/2Cl--carrier system (via interference of the chloride binding site) in the lumen of the thick ascending portion of the loop of Henle, resulting in a decrease in reabsorption of sodium and chloride. This results in an increase in the rate of delivery of tubular fluid and electrolytes to...
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Absorption: Rapidly absorbed following oral administration. Absolute bioavailability is 80%. Food has no effect on absorption.
Protein binding: > 99%
Biotransformation: Metabolized via the hepatic CYP2C8 to 5 metabolites. The major metabolite, M5, is pharmacologically inactive. There are 2 minor metabolites, M1, possessing one-tenth the activity of torasemide, and M3, equal in activity to torasemide. Overall, torasemide appears to account for 80% of the total diuretic activity, while metabolites M1 and M3 account for 9% and 11%, respectively.
Route of elimination: Torsemide is cleared from the circulation by both hepatic metabolism (approximately 80% of total clearance) and excretion into the urine (approximately 20% of total clearance in patients with normal renal function).
Half Life: 3.5 hours
Toxicity: Symptoms of overdose include dehydration, hypovolemia, hypotension, hyponatremia, hypokalemia, hypochloremic alkalosis, and hemoconcentration. Oral LD50 in rat is 5 g/kg, and intravenous LD50 in rat is 500 mg/kg.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
NicardipineNicardipine, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Nicardipine is initiated, discontinued or dose changed.
MiconazoleMiconazole, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Miconazole is initiated, discontinued or dose changed.
SitaxentanSitaxsentan, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Sitaxsentan is initiated, discontinued or dose changed.
GentamicinIncreased ototoxicity
CapecitabineCapecitabine, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Capecitabine is initiated, discontinued or dose changed.
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