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[Drugbank ÀÇ ¼ººÐÁ¤º¸¿¶÷] [Clonidine]
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°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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Clonidine¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Clonidine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Clonidine acts as an agonist at presynaptic alpha(2)-receptors in the nucleus tractus solitarius of the medulla oblongata. Stimulation of these receptors results in the supression of efferent sympathetic pathways and the subsequent decrease in blood pressure and vascular tone in the heart, kidneys, and peripheral vasculature. Clonidine is also a partial agonist at presynaptic alpha(2)-adrenergic receptors of peripheral nerves in vascular smooth muscle.
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| Pharmacology |
Clonidine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Clonidine is an antihypertensive agent and an epidural agent for refractory cancer pain. Similar to guanabenz in mechanism of action, clonidine is used in the treatment of hypertension, opiate and nicotine withdrawal, vascular headaches, diabetic diarrhea, glaucoma, ulcerative colitis, Gilles de la Tourette's syndrome, menopause symptoms, severe pain in cancer patients refractory to opiate agonists, and neuropathic pain and in the diagnosis of pheochromocytoma.
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| Protein Binding |
Clonidine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 20-40%
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| Half-life |
Clonidine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 12-16 hours
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| Absorption |
Clonidine¿¡ ´ëÇÑ Absorption Á¤º¸ Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.
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| Pharmacokinetics |
Clonidine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ÃÖ´ëÈ¿°ú¹ßÇö½Ã°£ : 2-4½Ã°£
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- »ýü³»ÀÌ¿ë·ü : 75-95%
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- ¼Ò½Ç : ¼Òº¯À¸·Î 65%(32% ¹Ìº¯Èü), 22%´Â ´ëº¯À¸·Î ¹è¼³
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| Biotransformation |
Clonidine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Metabolized through minor pathways. The major metabolite, p-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine.
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| Toxicity |
Clonidine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 is 150 mg/kg in rat and 30 mg/kg in dog. Symptoms of overdose include constriction of pupils of the eye, drowsiness, high blood pressure followed by a drop in pressure, irritability, low body temperature, slowed breathing, slowed heartbeat, slowed reflexes, and weakness.
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| Drug Interactions |
Clonidine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol Increased hypertension when clonidine stoppedAmitriptyline The tricyclic decreases the effect of clonidineAmoxapine The tricyclic decreases the effect of clonidineAtenolol Increased hypertension when clonidine stoppedBetaxolol Increased hypertension when clonidine stoppedBevantolol Increased hypertension when clonidine stoppedBisoprolol Increased hypertension when clonidine stoppedCarteolol Increased hypertension when clonidine stoppedCarvedilol Increased hypertension when clonidine stoppedClomipramine The tricyclic decreases the effect of clonidineDesipramine The tricyclic decreases the effect of clonidineDoxepin The tricyclic decreases the effect of clonidineImipramine The tricyclic decreases the effect of clonidineNortriptyline The tricyclic decreases the effect of clonidineEsmolol Increased hypertension when clonidine stoppedLabetalol Increased hypertension when clonidine stoppedMetoprolol Increased hypertension when clonidine stoppedMirtazapine Possible hypertensive crisisNadolol Increased hypertension when clonidine stoppedPenbutolol Increased hypertension when clonidine stoppedPindolol Increased hypertension when clonidine stoppedPractolol Increased hypertension when clonidine stoppedPropranolol Increased hypertension when clonidine stoppedSotalol Increased hypertension when clonidine stoppedTimolol Increased hypertension when clonidine stoppedProtriptyline The tricyclic decreases the effect of clonidineTrimipramine The tricyclic decreases the effect of clonidineOxprenolol Increased hypertension when clonidine stopped
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Clonidine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol.
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| Drug Target |
[Drug Target]
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| Description |
Clonidine¿¡ ´ëÇÑ Description Á¤º¸ An alpha-2 adrenergic agonist that crosses the blood-brain barrier. Clonidine acts centrally by reducing sympathetic tone, resulting in a fall in diastolic and systolic blood pressure and a reduction in heart rate. It also acts peripherally, and this peripheral activity may be responsible for the transient increase in blood pressure seen during rapid intravenous administration. (From Martindale, the Extra Pharmacopoeia, 30th ed, p350)
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| Drug Category |
Clonidine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic alpha-AgonistsAnalgesicsAntihypertensive AgentsCentral Alpha-AgonistsSympatholytics
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| Smiles String Canonical |
Clonidine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ ClC1=CC=CC(Cl)=C1NC1=NCCN1
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| Smiles String Isomeric |
Clonidine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ ClC1=CC=CC(Cl)=C1NC1=NCCN1
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| InChI Identifier |
Clonidine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)/f/h12,14H
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| Chemical IUPAC Name |
Clonidine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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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. CLONIDINE[GGT Increase][Composite Activity](Score) A(Marginal) 0(Active) 2[Alkaline Phosphatase Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 11.5[SGOT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[SGPT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 7.6[LDH Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[GGT Increase](Activity Score) A(Number of Rpts) ¡Ã4(Index value) 9.5
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