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¿¡ÄûÅæÁ¡¾È¾× EQUITON EYE.[Aminoquine carbamide HCl , Pilocarpine HCl , Timolol maleate]
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| Related FDA Approved Drug |
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(pilocarpine;timolol; )
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»ó±â ÀÓºÎÅõ¿©¿¡ ´ëÇÑ Á¤º¸´Â Àü»êó¸® µÇ¸é¼ ÀÔ·Â ¿À·ù °¡´É¼ºÀÌ Á¸ÀçÇÕ´Ï´Ù. ¿À·ù °¡´É¼ºÀ» ÃÖ¼ÒÈÇϱâ À§ÇÏ¿© ¸¹Àº ³ë·ÂÀ» ±â¿ïÀ̰í ÀÖÀ¸³ª, ±× Á¤È®¼º¿¡ ´ëÇÏ¿© È®½ÅÀ» µå¸± ¼ö ¾ø½À´Ï´Ù. ÀÌ¿¡ ´ëÇØ ȸ»ç´Â Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù.
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| Mechanism of Action |
Pilocarpine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
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.
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| Pharmacology |
Pilocarpine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.
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.
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| Metabolism |
Pilocarpine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2A6 (CYP2A6)
Timolol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Timolol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ ~10%
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| Half-life |
Pilocarpine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 0.76 hours
Timolol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.5-5 hours
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| Absorption |
Pilocarpine¿¡ ´ëÇÑ Absorption Á¤º¸ There was a decrease in the rate of absorption of pilocarpine from SALAGEN Tablets when taken with a high fat meal by 12 healthy male volunteers
Timolol¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is about 60%
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| 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%
- ´ë»ç : ÃÊȸÅë°úÈ¿°ú Å. °£¿¡¼ ¸¹Àº ¾çÀÌ ´ë»çµÊ.
- ¹Ý°¨±â : 2-2.7 ½Ã°£. ½Å±â´ÉºÎÀü½Ã Áõ°¡
- ¼Ò½Ç : ½Å ¹è¼³ (¹Ìº¯Èü·Î¼ 15-20%)
Pilocarpine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Á¡¾È :
- Ãൿ :
- ÀÛ¿ë¹ßÇö½Ã°£ : 10-30ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-8 ½Ã°£
- ¾È¾Ð °¨¼Ò :
- ÀÛ¿ë¹ßÇö½Ã°£ : 1½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-12 ½Ã°£
- OcusertR Pilo »ðÀÔ :
- Ãൿ ¹ßÇö½Ã°£ : 1.5-2 ½Ã°£
- ¾È¾Ð °¨¼Ò :
- ÀÛ¿ë¹ßÇö½Ã°£ : 1.5-2 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 1ÁÖÀÏ
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| Biotransformation |
Pilocarpine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Possibly occurs at the neuronal synapses and in the plasma
Timolol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.
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| Toxicity |
Pilocarpine¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
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.
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| Drug Interactions |
Pilocarpine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Timolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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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
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| Drug Target |
[Drug Target]
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| Description |
Pilocarpine¿¡ ´ëÇÑ Description Á¤º¸ A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem]
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 |
Pilocarpine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Gel OphthalmicLiquid OphthalmicLiquid OralSolution OphthalmicSolution / drops OralTablet Oral
Timolol¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid OphthalmicSolution OphthalmicSolution / drops OphthalmicTablet Oral
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| Drug Category |
Pilocarpine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Cholinergic AgentsMioticsMuscarinic Agonists
Timolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AntagonistsAnti-Arrhythmia AgentsAntihypertensive Agents
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| Smiles String Canonical |
Pilocarpine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCC1C(COC1=O)CC1=CN=CN1C
Timolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)(C)NCC(O)COC1=NSN=C1N1CCOCC1
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| Smiles String Isomeric |
Pilocarpine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC[C@H]1[C@H](COC1=O)CC1=CN=CN1C
Timolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1
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| InChI Identifier |
Pilocarpine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1
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 |
Pilocarpine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one
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] PILOCARPINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Mu-type opioid receptor Drug:pilocarpine Toxicity:pilocarpine-induced seizures. [¹Ù·Î°¡±â] Replated Protein:Delta-type opioid receptor Drug:pilocarpine Toxicity:pilocarpine-induced seizures. [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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ÃÖ±ÙÁ¤º¸¼öÁ¤ÀÏ 2021-12-09
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
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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. PILOCARPINE[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) 4.6[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 4.6[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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