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648900290[A03101661]
[º¸ÇèÄڵ忡 µû¸¥ ¾àǰ±âº»Á¤º¸ Á÷Á¢Á¶È¸]
\0 ¿ø/1Á¤(2007.11.15)(ÇöÀç¾à°¡)
\59 ¿ø/1Á¤(2006.03.01)(º¯°æÀü¾à°¡)
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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Prazosin]
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| Related FDA Approved Drug |
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µå·°ÀÎÆ÷ ÀǾàǰ ¿ä¾à/»ó¼¼Á¤º¸
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ÀüüÀӽŠ±â°£º°·Î ¿©·¯µî±ÞÀÌ Á¸ÀçÇÒ ¼ö ÀÖÀ¸¸ç °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ º¸¿©Áý´Ï´Ù. ´Ü, º¹ÇÕÁ¦ÀÇ °æ¿ì ¸ðµç º¹ÇÕÁ¦¼ººÐ¿¡ ´ëÇÑ ÀÓºÎÅõ¿©µî±ÞÀÌ Ç¥½ÃµÈ°ÍÀº Àý´ë ¾Æ´Ï¸ç Ç¥½ÃµÈ°ÍÁß¿¡ °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ ³ªÅ¸³³´Ï´Ù.
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 FDA : Dµî±Þ
(polythiazide; )
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| * |
»ó±â ÀÓºÎÅõ¿©¿¡ ´ëÇÑ Á¤º¸´Â Àü»êó¸® µÇ¸é¼ ÀÔ·Â ¿À·ù °¡´É¼ºÀÌ Á¸ÀçÇÕ´Ï´Ù. ¿À·ù °¡´É¼ºÀ» ÃÖ¼ÒÈÇϱâ À§ÇÏ¿© ¸¹Àº ³ë·ÂÀ» ±â¿ïÀ̰í ÀÖÀ¸³ª, ±× Á¤È®¼º¿¡ ´ëÇÏ¿© È®½ÅÀ» µå¸± ¼ö ¾ø½À´Ï´Ù. ÀÌ¿¡ ´ëÇØ ȸ»ç´Â Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù.
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¹Ýµå½Ã °ø½Å·Â ÀÖ´Â ¹®ÇåÀ» ´Ù½Ã Çѹø Âü°í ÇϽñ⠹ٶó¸ç ÀÇ»ç ¶Ç´Â ¾à»çÀÇ ÆÇ´Ü¿¡ µû¶ó Åõ¿©¿©ºÎ°¡ °áÁ¤µÇ¾î¾ß ÇÕ´Ï´Ù.
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| Pharmacokinetics |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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| Mechanism of Action |
Polythiazide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ As a diuretic, polythiazide inhibits active chloride reabsorption at the early distal tubule via the thiazide-sensitive Na-Cl cotransporter (TSC), resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like polythiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of polythiazide may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Prazosin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Prazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.
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| Pharmacology |
Prazosin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Prazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Prazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Prazosin results from a decrease in systemic vascular resistance and the parent compound Prazosin is primarily responsible for the antihypertensive activity.
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| Protein Binding |
Prazosin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 97%
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| Half-life |
Prazosin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-3 hours
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| Absorption |
Prazosin¿¡ ´ëÇÑ Absorption Á¤º¸ Well-absorbed from gastrointestinal tract; bioavailability is variable (50 to 85%).
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| Pharmacokinetics |
PolythiazideÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÌ´¢È¿°ú ¹ßÇö½Ã°£ : 2½Ã°£ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 24-48½Ã°£
Prazosin HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Ç÷¾Ð°ÇÏÈ¿°ú ¹ßÇö½Ã°£ : 2½Ã°£ À̳»
- ÃÖ´ëÈ¿°ú ¹ßÇö½Ã°£ : 2-4½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 10-24½Ã°£
- ºÐÆ÷¿ëÀû : Vd : 0.5L/kg (¼ºÀÎ °íÇ÷¾Ð ȯÀÚ)
- ´Ü¹é°áÇÕ : 92-97%
- ´ë»ç : ÁÖ·Î °£¿¡¼ ´ë»çµÈ´Ù.
- »ýüÀÌ¿ë·ü : °æ±¸ : 43-82%
- ¹Ý°¨±â : 2-4½Ã°£(¿ïÇ÷¼º ½ÉºÎÀü ȯÀÚ¿¡¼´Â ´õ ±æ¾îÁø´Ù.)
- ¼Ò½Ç : 6-10%°¡ ¹Ìº¯Èü·Î ½Å¹è¼³ µÈ´Ù.
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| Biotransformation |
Prazosin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. Several metabolites have been identified in humans and animals (6- O -demethyl, 7- O -demethyl, 2-[1-piperazinyl]-4-amino-6, 7-dimethoxyquinazoline, 2,4-diamino-6,7-dimethoxyquinazoline).
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| Toxicity |
Prazosin¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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| Drug Interactions |
Prazosin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol Risk of hypotension at the beginning of therapyAtenolol Risk of hypotension at the beginning of therapyBetaxolol Risk of hypotension at the beginning of therapyBevantolol Risk of hypotension at the beginning of therapyBisoprolol Risk of hypotension at the beginning of therapyCarteolol Risk of hypotension at the beginning of therapyCarvedilol Risk of hypotension at the beginning of therapyEsmolol Risk of hypotension at the beginning of therapyLabetalol Risk of hypotension at the beginning of therapyMetoprolol Risk of hypotension at the beginning of therapyNadolol Risk of hypotension at the beginning of therapyOxprenolol Risk of hypotension at the beginning of therapyDigoxin Prazosin increases the effect of digoxinPenbutolol Risk of hypotension at the beginning of therapyPindolol Risk of hypotension at the beginning of therapyPractolol Risk of hypotension at the beginning of therapyPropranolol Risk of hypotension at the beginning of therapySotalol Risk of hypotension at the beginning of therapyTimolol Risk of hypotension at the beginning of therapyVerapamil Risk of hypotension at the beginning of therapyTadalafil Risk of significant hypotension with this association
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Prazosin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid natural licorice.Take without regard to meals.
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| Drug Target |
[Drug Target]
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| Description |
Polythiazide¿¡ ´ëÇÑ Description Á¤º¸ A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p826)
Prazosin¿¡ ´ëÇÑ Description Á¤º¸ A selective adrenergic alpha-1 antagonist used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud&
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| Dosage Form |
Polythiazide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
Prazosin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Polythiazide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsDiureticsSodium Chloride Symporter Inhibitors
Prazosin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AntagonistsAlpha-adrenergic Blocking AgentsAntihypertensive Agents
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| Smiles String Canonical |
Polythiazide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C(CSCC(F)(F)F)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
Prazosin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1
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| Smiles String Isomeric |
Polythiazide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1[C@@H](CSCC(F)(F)F)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
Prazosin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1=CC=CO1
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| InChI Identifier |
Polythiazide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C11H13ClF3N3O4S3/c1-18-10(4-23-5-11(13,14)15)17-7-2-6(12)8(24(16,19)20)3-9(7)25(18,21)22/h2-3,10,17H,4-5H2,1H3,(H2,16,19,20)/f/h16H2
Prazosin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H21N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22)/f/h20H2
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| Chemical IUPAC Name |
Polythiazide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 6-chloro-2-methyl-1,1-dioxo-3-(2,2,2-trifluoroethylsulfanylmethyl)-3,4-dihydrobenzo[e][1,2,4]thiadiazine-7-sulfonamide
Prazosin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-furan-2-ylmethanone
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. PRAZOSIN[GGT Increase][Composite Activity](Score) NA(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[SGOT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[SGPT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[LDH Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[GGT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA
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