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Mechanism of Action
Levobunolol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Levobunolol's mechanism of action in reducing IOP is believed to be due to a reduction of the production of aqueous humor via inhibition of adrenergically driven processes within the ciliary processes.
Pharmacology
Levobunolol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Levobunolol is an ophthalmic beta-blocker, equally effective at ¥â(1)- and ¥â(2)-receptor sites. The levorotatory isomer of bunolol, levobunolol is used for the treatment of IOP due to open-angle glaucoma or ocular hypertension.
Metabolism
Levobunolol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
Half-life
Levobunolol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 20 hours
Absorption
Levobunolol¿¡ ´ëÇÑ Absorption Á¤º¸ 80%
Pharmacokinetics
Levobunolol HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
È¿°ú¹ßÇö ½Ã°£ : ¾È¾ÐÇϰ È¿°ú : 2½Ã°£ À̳»
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ÃÖ°í Ç÷Áß³óµµ µµ´Þ ½Ã°£ : °æ±¸ : 3½Ã°£
ÃÖ°í ¾È¹æ¼ö ³óµµ µµ´Þ ½Ã°£ : Á¡¾ÈÁ¦ : 30ºÐ
ÀÛ¿ë Áö¼Ó ½Ã°£ : 1-7 ÀÏ
Èí¼ö : °æ±¸ : °ÅÀÇ ¿ÏÀüÈ÷ Èí¼ö
»ýü³» ÀÌ¿ë·ü : 60% (30-100 %)
À½½Ä¹° ¿µÇâ : Èí¼ö ¹× ÃÖ°í Ç÷Áß³óµµ : 20-45 % °¨¼Ò
ºÐÆ÷¿ëÀû : Vd : 5.5 L/kg
´ë»ç : °£´ë»ç : Ȱ¼ºÇü ´ë»çü dihydrolevobunolol
¼Ò½Ç : ´¢¹è¼³ (78 %), ´ëº¯¹è¼³ (3%)
¹Ý°¨±â : 6.1½Ã°£
Biotransformation
Levobunolol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic
Toxicity
Levobunolol¿¡ ´ëÇÑ Toxicity Á¤º¸ Bradycardia, hypotension, bronchospasm, and acute cardiac failure, LD50 =700 mg/kg (orally in rat).
Drug Interactions
Levobunolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Drug Target
[Drug Target]
Description
Levobunolol¿¡ ´ëÇÑ Description Á¤º¸ A nonselective beta-adrenoceptor antagonist used in the treatment of glaucoma. [PubChem]
Dosage Form
Levobunolol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OphthalmicSolution Ophthalmic
Drug Category
Levobunolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AntagonistsEENT DrugsSympatholytics
Smiles String Canonical
Levobunolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)(C)NCC(O)COC1=CC=CC2=C1CCCC2=O
Smiles String Isomeric
Levobunolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)(C)NC[C@H](O)COC1=CC=CC2=C1CCCC2=O
InChI Identifier
Levobunolol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H25NO3/c1-17(2,3)18-10-12(19)11-21-16-9-5-6-13-14(16)7-4-8-15(13)20/h5-6,9,12,18-19H,4,7-8,10-11H2,1-3H3/t12-/m0/s1
Chemical IUPAC Name
Levobunolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 5-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-2H-naphthalen-1-one
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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.
LEVOBUNOLOL [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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