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Enflurane¿¡ ´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 |
Enflurane¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Enflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Enflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Enflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.
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| Pharmacology |
Enflurane¿¡ ´ëÇÑ Pharmacology Á¤º¸ Enflurane is an extremely stable halogenated ether inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. Enflurane induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. Induction of and recovery from anesthesia with enflurane are rapid. Enflurane may provide a mild stimulus to salivation or tracheobronchial secretions. Pharyngeal and laryngeal reflexes are readily obtunded. In the cardiovascular system, enflurane is a mild negative inotrope, causing a marked decrease in systemic vascular resistance, thus leading to a decrease in mean arterial pressure. This results in a reflex tachycardia. Enflurane also decreases coronary vascular resistance and sensitizes the myocardium to circulating catecholamines. Enflurane is a strong respiratory depressant. It decreases tidal volume but may increase respiratory rate. It also causes bronchodilatationa and inhibits pulmonary macrophage activity and mucociliary activity. Enflurane principle action in the CNS is general anaesthesia with little analgesic effect. It causes increased cerebral blood flow in concentrations and may induce tonic/clonic muscle activity and epileptiform EEG traces. It also causes a marked decrease in skeletal muscle tone. Actions in the genitourinary system include a decreased renal blood flow and glomerular filtration rate and the tone of pregnant uterus is decreased.
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| Metabolism |
Enflurane¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2E1 (CYP2E1)
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| Protein Binding |
Enflurane¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 97%
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| Half-life |
Enflurane¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available
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| Absorption |
Enflurane¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly absorbed into the circulation via the lungs.
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| Pharmacokinetics |
EnfluraneÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ºÐÆ÷ :
- Ç÷¾×/±âü ºÐ¹è°è¼ö : 2.1
- ºÐÆ÷¿ëÀû : 8.6 L/kg
- ´ë»ç : Fluoride ion, difluoromethoxydifluoroacetic acid ¹× ±âŸ »ê ´ë»çü·Î ´ë»çµÊ
- ¹Ý°¨±â : ¸»±â»ó : 106ºÐ
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| Biotransformation |
Enflurane¿¡ ´ëÇÑ Biotransformation Á¤º¸ 2.4% of the dose is slowly metabolized hepatically via oxidation and dehalogenation (primarily through the actions of cytochrome P450 2E1). Leads to low levels of serum fluoride (15 µmol/L).
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| Toxicity |
Enflurane¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=5.4 ml/kg (oral, rat). Symptoms of acute overdose include nausea, vomiting, irritation to the eyes, skin and nose/throat, headache, dizziness, and drowsiness. Symptoms of chronic overdose include hypotension, cardiac arrhythmias, respiratory depression, and liver/kidney dysfunction.
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| Drug Interactions |
Enflurane¿¡ ´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 |
Enflurane¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Enflurane¿¡ ´ëÇÑ Description Á¤º¸ An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. [PubChem]
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| Drug Category |
Enflurane¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anesthetics, InhalationGeneral Anesthetics
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| Smiles String Canonical |
Enflurane¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ FC(F)OC(F)(F)C(F)Cl
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| Smiles String Isomeric |
Enflurane¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ FC(F)OC(F)(F)[C@@H](F)Cl
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| InChI Identifier |
Enflurane¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C3H2ClF5O/c4-1(5)3(8,9)10-2(6)7/h1-2H
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| Chemical IUPAC Name |
Enflurane¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-chloro-1-(difluoromethoxy)-1,1,2-trifluoroethane
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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. ENFLURANE[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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