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3) ÁßÁõÀÇ ÀÌÇü Çù½ÉÁõ ȯÀÚ
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6) µ¿±â´ÉºÎÀüÁõÈıº ȯÀÚ
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10) ÇÁ·ÎŸÆä´Ñ(floctafenine) º´¿ëȯÀÚ
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| Related FDA Approved Drug |
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µå·°ÀÎÆ÷ ÀǾàǰ ¿ä¾à/»ó¼¼Á¤º¸
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[A03950451]
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| Brandname Á¤º¸ |
Betaxolol
Brand Names/Synonyms
- Betaxolol HCL
- Betaxololum [INN-Latin]
- Betaxon
- Betoptic
- Betoptic S
- Kerlone
Brand Name MixturesNot Available
Chemical IUPAC Name1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(1-methylethylamino)propan-2-ol
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Taxol¿¡ ´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 |
Betaxolol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Betaxolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Betaxolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.
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| Pharmacology |
Betaxolol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Betaxolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Betaxolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as betaxolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Betaxolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.
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| Metabolism |
Betaxolol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
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| Protein Binding |
Betaxolol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 50%
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| Half-life |
Betaxolol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 14-22 hours
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| Absorption |
Betaxolol¿¡ ´ëÇÑ Absorption Á¤º¸ Absorption of an oral dose is complete. There is a small and consistent first-pass effect resulting in an absolute bioavailability of 89% ¡¾ 5% that is unaffected by the concomitant ingestion of food or alcohol.
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| Pharmacokinetics |
Betaxolol HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : 1-1.5 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 12½Ã°£ ÀÌ»ó
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- ´ë»ç : °£´ë»ç (¿©·¯°¡Áö ´ë»çü Á¸Àç)
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- ÃÖ°íÇ÷Áß³óµµ µµ´Þ½Ã°£ : 2½Ã°£ À̳»
- ¼Ò½Ç : ½Å¹è¼³
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| Biotransformation |
Betaxolol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. Approximately 15% of the dose administered is excreted as unchanged drug, the remainder being metabolites whose contribution to the clinical effect is negligible.
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| Toxicity |
Betaxolol¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. Predicted symptoms of overdose include bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia.
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| Drug Interactions |
Betaxolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Drug Target |
[Drug Target]
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| Description |
Betaxolol¿¡ ´ëÇÑ Description Á¤º¸ A cardioselective beta-1-adrenergic antagonist with no partial agonist activity. [PubChem]
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| Drug Category |
Betaxolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AntagonistsAntihypertensive AgentsEENT DrugsSympatholytics
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| Smiles String Canonical |
Betaxolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)NCC(O)COC1=CC=C(CCOCC2CC2)C=C1
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| Smiles String Isomeric |
Betaxolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)NC[C@@H](O)COC1=CC=C(CCOCC2CC2)C=C1
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| InChI Identifier |
Betaxolol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3
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| Chemical IUPAC Name |
Betaxolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
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| Drug-Induced Toxicity Related Proteins |
BETAXOLOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Betaxolol Toxicity:Increased beta-blockade. [¹Ù·Î°¡±â]
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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. BETAXOLOL[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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