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| Related FDA Approved Drug |
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| Mechanism of Action |
Timolol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle and beta(2)-receptors in the bronchial and vascular smooth muscle. Beta(1)-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta(2)-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor.
|
| Pharmacology |
Timolol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage.
|
| Metabolism |
Timolol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
|
| Protein Binding |
Timolol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ ~10%
|
| Half-life |
Timolol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.5-5 hours
|
| Absorption |
Timolol¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is about 60%
|
| Pharmacokinetics |
Timolol maleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Ç÷¾Ð°ÇÏÈ¿°ú ¹ßÇö½Ã°£ : °æ±¸ : 15-45ºÐ À̳»
- ÃÖ°íÈ¿°ú ¹ßÇö½Ã°£ : 0.5-2.5 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4½Ã°£±îÁö. Á¡¾È ÈÄ ¾È¾Ð Çϰȿ°ú´Â 24½Ã°£±îÁö Áö¼Ó
- ´Ü¹é°áÇÕ : 60%
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|
| Biotransformation |
Timolol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.
|
| Toxicity |
Timolol¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.
|
| Drug Interactions |
Timolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
|
CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Timolol¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2D6
Beta Blockers:
S-metoprolol
propafenone
**timolol**
Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
aripiprazole
codeine
dextromethorphan
duloxetine
flecainide
mexiletine
ondansetron
tamoxifen
tramadol
venlafaxine
INHIBITORS
CYP 2D6
amiodarone
buproprion
chlorpheniramine
cimetidine
clomipramine
duloxetine
fluoxetine
haloperidol
methadone
mibefradil
paroxetine
quinidine
ritonavir
INDUCERS
CYP 2D6
N/A
|
| Drug Target |
[Drug Target]
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| Description |
Timolol¿¡ ´ëÇÑ Description Á¤º¸ A beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorders and tremor. [PubChem]
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| Dosage Form |
Timolol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OphthalmicSolution OphthalmicSolution / drops OphthalmicTablet Oral
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| Drug Category |
Timolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AntagonistsAnti-Arrhythmia AgentsAntihypertensive Agents
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| Smiles String Canonical |
Timolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)(C)NCC(O)COC1=NSN=C1N1CCOCC1
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| Smiles String Isomeric |
Timolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1
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| InChI Identifier |
Timolol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1
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| Chemical IUPAC Name |
Timolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
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| Drug-Induced Toxicity Related Proteins |
MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [¹Ù·Î°¡±â] TIMOLOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Timolol Toxicity:Increased beta-blockade. [¹Ù·Î°¡±â]
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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