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Torasemide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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 the distal sites of hydrogen and potassium ion secretion, while plasma volume contraction increases aldosterone production. The increased delivery and high aldosterone levels promote sodium reabsorption at the distal tubules, and By increasing the delivery of sodium to the distal renal tubule, torasemide indirectly increases potassium excretion via the sodium-potassium exchange mechanism. Torasemide's effects in other segments of the nephron have not been demonstrated. Thus torasemide increases the urinary excretion of sodium, chloride, and water, but it does not significantly alter glomerular filtration rate, renal plasma flow, or acid-base balance. Torasemide's effects as a antihypertensive are due to its diuretic actions. By reducing extracellular and plasma fluid volume, blood pressure is reduced temporarily, and cardiac output also decreases.
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| Pharmacology |
Torasemide¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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- reabsorption is accomplished by a Na+/K+/2Cl- symporter. The thick ascending limb has a high reabsorptive capacity and is responsible for reabsorbing 25% of the filtered load of Na+. The loop diuretics act by blocking this symporter. Because of the large absorptive capacity and the amount of Na+ delivered to the ascending limb, loop diuretics have a profound diuretic action. In addition, more distal nephron segments do not have the reabsorptive capacity to compensate for this increased load. The osmotic gradient for water reabsorption is also reduced resulting in an increase in the amount of water excreted.
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Torasemide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C8 (CYP2C8)Cytochrome P450 2C9 (CYP2C9)
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| Protein Binding |
Torasemide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ > 99%
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| Half-life |
Torasemide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 3.5 hours
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| Absorption |
Torasemide¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed following oral administration. Absolute bioavailability is 80%. Food has no effect on absorption.
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| Pharmacokinetics |
TorasemideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÌ´¢È¿°ú ¹ßÇö½Ã°£ : 30-60ºÐ
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 1-4½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 6½Ã°£±îÁö
- Èí¼ö : °æ±¸ : ºü¸£°Ô Èí¼öµÈ´Ù.
- ´Ü¹é°áÇÕ : 97-99% (Ç÷Àå)
- ´ë»ç : °£¿¡¼ cytochrome P-450¿¡ ÀÇÇØ ´ë»ç (80%)
- »ýü³»ÀÌ¿ë·ü : 80-90%
- ¹Ý°¨±â
- Á¤»ó : 2-4½Ã°£
- °æÈ(cirrhosis) : 7-8½Ã°£ (¿ë·® Á¶ÀýÀÌ ÇÊ¿äÇÏÁö´Â ¾Ê´Ù)
- ¼Ò½Ç : 20%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³µÈ´Ù. Åõ¼®À¸·Î ¼Ò½ÇÀÌ Áõ°¡µÇÁö ¾Ê´Â´Ù.
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| Biotransformation |
Torasemide¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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.
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| Toxicity |
Torasemide¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
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| Drug Interactions |
Torasemide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Torasemide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Torasemide¿¡ ´ëÇÑ Description Á¤º¸ Torasemide (rINN) or torsemide (USAN) is a pyridine-sulfonylurea type loop diuretic mainly used in the management of edema associated with congestive heart failure. It is also used at low doses for the management of hypertension. It is marketed under the brand name Demadex. [Wikipedia]
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| Dosage Form |
Torasemide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Injection, solution IntravenousTablet Oral
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| Drug Category |
Torasemide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsDiuretics
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| Smiles String Canonical |
Torasemide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)NC(=O)NS(=O)(=O)C1=C(NC2=CC=CC(C)=C2)C=CN=C1
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| Smiles String Isomeric |
Torasemide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)NC(=O)NS(=O)(=O)C1=C(NC2=CC=CC(C)=C2)C=CN=C1
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| InChI Identifier |
Torasemide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H20N4O3S/c1-11(2)18-16(21)20-24(22,23)15-10-17-8-7-14(15)19-13-6-4-5-12(3)9-13/h4-11H,1-3H3,(H,17,19)(H2,18,20,21)/f/h18-20H
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| Chemical IUPAC Name |
Torasemide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 3-[4-[(3-methylphenyl)amino]pyridin-3-yl]sulfonyl-1-propan-2-ylurea
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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