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16) ½ÉÇ÷°ü°è : ÈäÅë, ºó¸Æ, ¼¸Æ, ½É°èÇ×Áø
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19) ´ÙÀ½Àº ÇÁ·ÎÅæÆßÇÁ¾ïÁ¦Á¦ÀÇ ½ÃÆÇ ÈÄ Á¶»ç¸¦ ÅëÇØ º¸°íµÈ ÀÌ»ó¹ÝÀÀÀÌ´Ù. ÀÌ ÀÌ»ó¹ÝÀÀÀº ºÒƯÁ¤ ´Ù¼öÀÇ Àα¸Áý´Ü¿¡¼ ÀÚ¹ßÀûÀ¸·Î º¸°íµÈ °ÍÀ̱⠶§¹®¿¡, Ç×»ó ¹ß»ý·üÀ» ½Å·Ú¼º ÀÖ°Ô ¿¹ÃøÇϰųª ¾à¹° Åõ¿©¿ÍÀÇ Àΰú°ü°è¸¦ È®¸³ÇÒ ¼ö ÀÖÁö´Â ¾Ê´Ù.
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2) CYP450È¿¼Ò°è¸¦ ÅëÇØ ´ë»çµÇ´Â ¾à¹°°ú »óÈ£ÀÛ¿ëÀÌ ÀÖÀ» ¼ö ÀÖ´Ù. ¿À¸ÞÇÁ¶óÁ¹Àº ºÎºÐÀûÀ¸·Î CYP3A4¿¡ ÀÇÇÏ¿© ´ë»çµÇÁö¸¸ ÀÌ È¿¼Ò¸¦ ¾ïÁ¦ÇÏÁö´Â ¾Ê´Â´Ù. µû¶ó¼ ¿À¸ÞÇÁ¶óÁ¹Àº CYP3A4¿¡ ÀÇÇÏ¿© ´ë»çµÇ´Â ¾à¹°ÀÎ ½ÃŬ·Î½ºÆ÷¸°, ¸®µµÄ«ÀÎ, Äû´Ïµò, ¿¡½ºÆ®¶óµð¿Ã, ¿¡¸®Æ®·Î¸¶À̽Š¹× ºÎµ¥¼Ò´Ïµå¿Í °°Àº ¾à¹°ÀÇ ´ë»ç¿¡ ¿µÇâÀ» ¹ÌÄ¡Áö ¾Ê´Â´Ù.
ÀÌ ¾à°ú ´Ù¸¥ ¾à¹°µéÀÇ »óÈ£ÀÛ¿ë ¿¬±¸¿¡¼ ÀÌ ¾à 1ÀÏ 20 ¡ 40 mg Åõ¿©½Ã ¾à¹°´ë»ç¿¡ ´ëÇÑ CYPÈ¿¼Ò°è¿¡ ´ëÇÑ ¿µÇâÀº À¯ÀÇÇÏ°Ô ³ªÅ¸³ªÁö ¾Ê¾Ò´Ù. ´ÙÀ½ ¿¹¿¡¼ °¢°¢ÀÇ CYP°è È¿¼Ò ±âÁú°úÀÇ ´ë»ç »óÈ£ÀÛ¿ëÀÌ °ÅÀÇ ³ªÅ¸³ªÁö ¾ÊÀ½À» º¸¿©ÁØ´Ù. : CYP1A2 (¿¹, Ä«ÆäÀÎ, Å׿ÀÇʸ°), CYP2C9(¿¹, ¿Í¸£ÆÄ¸°, ÇǷϽÃį,µðŬ·ÎÆä³«, ³ªÇÁ·Ï¼¾), CYP2D6(¿¹, ¸ÞÅäÇÁ·Ñ·Ñ, ÇÁ·ÎÇÁ¶ó³î·Ñ), CYP2E1(¿¹, ¿¡Åº¿Ã)
3) ÀÌ ¾àÀº CYP2C19°ú CYP3A4¿¡ ÀÇÇØ ´ë»çµÇ¹Ç·Î CYP2C19 ÀúÇØÁ¦, CYP3A4 ÀúÇØÁ¦ ¶Ç´Â ±× ¸ðµÎ¸¦ ÀúÇØÇÑ´Ù°í ¾Ë·ÁÁø ¾à¹°(Ŭ·¡¸®Æ®·Î¸¶À̽Å, º¸¸®ÄÚ³ªÁ¹)Àº ¿À¸ÞÇÁ¶óÁ¹ÀÇ ´ë»çÀ²À» °¨¼Ò½ÃÅ´À¸·Î¼ ¿À¸ÞÇÁ¶óÁ¹ÀÇ Ç÷û¼öÄ¡¸¦ Áõ°¡½ÃŲ´Ù. º¸¸®ÄÚ³ªÁ¹°úÀÇ º´¿ë Åõ¿©´Â ÀÌ ¾àÀÇ ³ëÃâÀ» µÎ ¹è ÀÌ»ó Áõ°¡½Ãų ¼ö ÀÖ´Ù. °í¿ë·®ÀÇ ¿À¸ÞÇÁ¶óÁ¹Àº Àß ³»¾àµÇ±â ¶§¹®¿¡ ÀϽÃÀûÀÎ º´¿ëÅõ¿©±â°£ µ¿¾È ¿ë·® Á¶ÀýÀº ÇÊ¿ä¾ø´Ù. CYP2C19 ȤÀº CYP3A4 ȤÀº ±× µÑÀº À¯µµÇÑ´Ù°í ¾Ë·ÁÁø ¾à¹°(¸®ÆÊÇǽŰú ¼¼ÀÎÆ®Á¸½º¿öÆ®)Àº ¿À¸ÞÇÁ¶óÁ¹ÀÇ ´ë»çÀ²À» Áõ°¡½ÃÅ´À¸·Î¼ ¿À¸ÞÇÁ¶óÁ¹ÀÇ Ç÷û¼öÄ¡¸¦ °¨¼Ò½Ãų ¼ö ÀÖ´Ù.
4) À§»êÀÇ pH¿¡ ÀÇÁ¸ÀûÀ¸·Î Èí¼öµÇ´Â ¾à¹°ÀÎ °æ¿ì¿¡ ÀÌ ¾à(¿À¸ÞÇÁ¶óÁ¹)À¸·Î Ä¡·áÇÏ´Â Áß¿¡ À§³» »êµµÀÇ °¨¼Ò·Î ÀÎÇØ ¾à¹° Èí¼ö°¡ Áõ°¡ÇÒ ¼öµµ ÀÖ°í °¨¼ÒÇÒ ¼öµµ ÀÖ´Ù.
5) ¿À¸ÞÇÁ¶óÁ¹°ú ÄÉÅäÄÚ³ªÁ¹, ÀÌÆ®¶óÄÚ³ªÁ¹ ¹× ¿¤·ÎƼ´ÕÀº º´¿ëÇÏÁö ¾Ê´Â´Ù. ¾à¹°(Á¦»êÁ¦, À§»êºÐºñ ¾ïÁ¦Á¦, ¼öÅ©¶öÆäÀÌÆ®) Åõ¿©·Î ÀÎÇØ À§»êÀÇ pH°¡ Áõ°¡Çϸé À§¿¡¼ÀÇ ÄÉÅäÄÚ³ªÁ¹ Á¤Á¦ÀÇ ¿ëÃâÀÌ °¨¼ÒµÇ¾î ÄÉÅäÄÚ³ªÁ¹ÀÇ À¯È¿ Ç÷Á߳󵵿¡ À̸£Áö ¸øÇÑ´Ù. ¿À¸ÞÇÁ¶óÁ¹°ú ÀÌÆ®¶óÄÚ³ªÁ¹ÀÇ º´¿ë½Ã ÀÌÆ®¶óÄÚ³ªÁ¹ÀÇ Ç÷Áß³óµµ¿Í AUC´Â ¾à 65 %±îÁö °¨¼ÒµÇ¾ú´Âµ¥ ÀÌ´Â pH¿¡ ÀÇÁ¸ÀûÀÎ Èí¼ö°¡ ³·Àº °á°ú¿¡ ÀÇÇÑ °ÍÀÌ´Ù.
6) °Ç°ÇÑ ÇÇÇèÀڵ鿡°Ô ¿À¸ÞÇÁ¶óÁ¹(1ÀÏ 20 mg)°ú µð°î½ÅÀ» ÇÔ²² º´¿ëÅõ¿©ÇÏ¸é µð°î½ÅÀÇ »ýüÀÌ¿ë·üÀÌ 10 % Áõ°¡Çß´Ù. µð°î½ÅÀÇ µ¶¼ºÀÌ µå¹°°Ô º¸°íµÇ¾ú´Ù. ±×·¯³ª ¿À¸ÞÇÁ¶óÁ¹ÀÌ °í·ÉÀÚ¿¡°Ô °í¿ë·®À¸·Î Åõ¿©µÉ ¶§ ÁÖÀÇÇØ¾ß ÇÑ´Ù. Ä¡·áÀûÀÎ ¾à¹°¸ð´ÏÅ͸µÀº °ÈµÇ¾î¾ß ÇÑ´Ù.
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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: OMEPRAZOLE SODIUMNEXIUM IV (ESOMEPRAZOLE SODIUM)
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| Mechanism of Action |
Omeprazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Omeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, omeprazole blocks the final step in acid production, thus reducing gastric acidity.
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| Pharmacology |
Omeprazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ Omeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Omeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, omeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
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| Metabolism |
Omeprazole¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C19 (CYP2C19)
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| Protein Binding |
Omeprazole¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95%
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| Half-life |
Omeprazole¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 0.5-1 hour
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| Absorption |
Omeprazole¿¡ ´ëÇÑ Absorption Á¤º¸ Absorption is rapid, absolute bioavailability (compared to intravenous administration) is about 30-40% at doses of 20-40 mg.
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| Biotransformation |
Omeprazole¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Omeprazole¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, and dry mouth.
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| Drug Interactions |
Omeprazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alprazolam Omeprazole increases the effect of benzodiazepineDiazepam Omeprazole increases the effect of benzodiazepineClonazepam Omeprazole increases the effect of benzodiazepineClorazepate Omeprazole increases the effect of benzodiazepineChlordiazepoxide Omeprazole increases the effect of benzodiazepineEstazolam Omeprazole increases the effect of benzodiazepineFlurazepam Omeprazole increases the effect of benzodiazepineHalazepam Omeprazole increases the effect of benzodiazepineKetazolam Omeprazole increases the effect of benzodiazepineMidazolam Omeprazole increases the effect of benzodiazepinePrazepam Omeprazole increases the effect of benzodiazepineQuazepam Omeprazole increases the effect of benzodiazepineTriazolam Omeprazole increases the effect of benzodiazepineMephenytoin Omeprazole increases the effect of hydantoinPhenytoin Omeprazole increases the effect of hydantoinFosphenytoin Omeprazole increases the effect of hydantoinEthotoin Omeprazole increases the effect of hydantoinVoriconazole Voriconazole increases the effect and toxicity of omeprazoleSt. John's Wort St. John's Wort decreases the levels/effects of omeprazole Methotrexate Omeprazole increases the levels of methotrexateCilostazol Omeprazole increases the effect of cilostazolAtazanavir This gastric pH modifier decreases the levels/effects of atazanavirCyclosporine Omeprazole increases the effect and toxicity of cyclosporineDasatinib Possible decreased levels of dasatinibEnoxacin The agent decreases the absorption of enoxacinIndinavir Omeprazole decreases the absorption of indinavirItraconazole The proton pump inhibitor decreases the absorption of the imidazoleKetoconazole The proton pump inhibitor decreases the absorption of the imidazoleDisopyramide The beta-blocker increases toxicity of disopyramide
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Omeprazole¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2C19
Proton Pump Inhibitors:
**omeprazole**
lansoprazole
pantoprazole
rabeprazole
Anti-epileptics:
diazepam
phenytoin
phenobarbitone
amitriptyline
clomipramine
clopidogrel
cyclophosphamide
progesterone
INHIBITORS
CYP 2C19
fluoxetine
fluvoxamine
ketoconazole
lansoprazole
**omeprazole**
ticlopidine
INDUCERS
CYP 2C19
N/A
SUBSTRATES
CYP 2C19
Proton Pump Inhibitors:
**omeprazole**
lansoprazole
pantoprazole
rabeprazole
Anti-epileptics:
diazepam
phenytoin
phenobarbitone
amitriptyline
clomipramine
clopidogrel
cyclophosphamide
progesterone
INHIBITORS
CYP 2C19
fluoxetine
fluvoxamine
ketoconazole
lansoprazole
**omeprazole**
ticlopidine
INDUCERS
CYP 2C19
N/A
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| Food Interaction |
Omeprazole¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take 30-60 minutes before meals.
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| Drug Target |
[Drug Target]
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| SNP Á¤º¸ |
Name:Omeprazole (DB00338)
Interacting Gene/Enzyme:Cytochrome P450 2C19 (Gene symbol = CYP2C19) Swissprot P33261
SNP(s):CYP2C19*3 rs4986893 (A Allele, homozygote)
Effect:Poor metabolizer, lower dose requirement, improved drug efficacy
Reference(s):Furuta T, Ohashi K, Kamata T, Takashima M, Kosuge K, Kawasaki T, Hanai H, Kubota T, Ishizaki T, Kaneko E: Effect of genetic differences in omeprazole metabolism on cure rates for Helicobacter pylori infection and peptic ulcer. Ann Intern Med. 1998 Dec 15;129(12):1027-30. [PubMed]
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| Description |
Omeprazole¿¡ ´ëÇÑ Description Á¤º¸ A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H(+)-K(+)-ATPase (H(+)-K(+)-exchanging ATPase) in the proton pump of gastric parietal cells. [PubChem]
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| Dosage Form |
Omeprazole¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralCapsule, delayed release OralTablet, delayed release Oral
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| Drug Category |
Omeprazole¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Ulcer AgentsEnzyme InhibitorsProton-pump Inhibitors
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| Smiles String Canonical |
Omeprazole¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(C=C1)N=C(N2)S(=O)CC1=NC=C(C)C(OC)=C1C
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| Smiles String Isomeric |
Omeprazole¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C=C1)N=C(N2)[S@@](=O)CC1=NC=C(C)C(OC)=C1C
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| InChI Identifier |
Omeprazole¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H19N3O3S/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17/h5-8H,9H2,1-4H3,(H,19,20)/f/h20H
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| Chemical IUPAC Name |
Omeprazole¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 6-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole
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| Drug-Induced Toxicity Related Proteins |
OMEPRAZOLE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Potassium-transporting ATPase Drug:omeprazole Toxicity:block gastric acid secretion. [¹Ù·Î°¡±â]
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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.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
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. OMEPRAZOLE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.8[SGOT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 1.2[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.9[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.5[GGT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.8
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