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1. °üµ¿¸Æ½ÉÁúȯ(¸¸¼º¾ÈÁ¤ÇüÇù½ÉÁõ, ÀÌÇüÇù½ÉÁõ)
2. °íÇ÷¾Ð(°íÇ÷¾Ð¼º¹ßÁõ Æ÷ÇÔ)
3. ·¹À̳뺴 ¹× ·¹À̳ëÁõÈıº
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6) ¼Òȱâ°è : µå¹°°Ô »óº¹ºÎÅëÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ÀÌ·¯ÇÑ °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÏ´Â °ÍÀÌ ¹Ù¶÷Á÷ÇÏ´Ù. ¶§¶§·Î ±¸¿ª, ±¸Åä, º¯ºñ, µå¹°°Ô ¼³»ç, º¹ºÎºÒÄè°¨, ±¸°¥, °¡½¿¾²¸², ½Ä¿åºÎÁø, ¼ÒȺҷ®, °íâ ¸Å¿ì µå¹°°Ô ¾Ë·¹¸£±â¼º °£¿°, À§½Äµµ°ý¾à±Ù ±â´ÉºÎÀü µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
7) °ú¹ÎÁõ : ¶§¶§·Î ¹ßÁø, °¡·Á¿ò, µå¹°°Ô ±¤°ú¹ÎÁõ, ÀÚ¹Ý, ¾Ë·¯Áö ¹ÝÀÀ, ¾Ë·¯Áö¼º ºÎÁ¾/Ç÷°ü ºÎÁ¾(ÈĵΠºÎÁ¾ Æ÷ÇÔ), ¾Æ³ªÇʶô½Ã½º ¹ÝÀÀ µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î ÀÌ·¯ÇÑ °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÑ´Ù.
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9) °ñ°Ý±Ù : µå¹°°Ô ¿°Áõ, °üÀý°æÁ÷, ±ÙÀ°Åë, ±Ù°æ·Ã, »çÁö¸¶ºñ°¨, °üÀý ºÎÁ¾ µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
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2) ÀÌ ¾àÀ» ´ÙÀ½°ú °°Àº Ç×°íÇ÷¾Ð Á¦Á¦¿Í º´¿ëÇÒ °æ¿ì Ç÷¾Ð°ÇÏ ÀÛ¿ëÀÌ Áõ°µÉ ¼ö ÀÖ´Ù : ÀÌ´¢Á¦, ¥â-Â÷´ÜÁ¦, ACE-ÀúÇØÁ¦, ¾ÈÁö¿ÀÅÙ½Å1(ATI)¼ö¿ëü-±æÇ×Á¦(¿¹, ¿°»êÇÁ¶óÁ¶½Å), ´Ù¸¥ Ä®½·±æÇ×Á¦, ¥á-¾Æµå·¹³¯¸° Â÷´ÜÁ¦(¿¹, ·¹¼¼¸£ÇÉ), PDE 5 ¾ïÁ¦Á¦, ¾ËÆÄ-¸ÞÄ¥µµÆÄ
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3) µð°î½Å, Å׿ÀÇʸ°, Æä´ÏÅäÀÎÀÇ Ç÷Á߳󵵸¦ »ó½Â½Ãų ¼ö ÀÖ´Ù.
ÀÌ ¾à°ú µð°î½ÅÀ» º´¿ëÅõ¿©ÇÒ °æ¿ì µð°î½ÅÀÇ Á¦°ÅÀ²ÀÌ °¨¼ÒµÉ ¼ö Àֱ⿡ µð°î½ÅÀÇ Ç÷Áß ³óµµ°¡ »ó½ÂµÉ ¼ö ÀÖ´Ù. µû¶ó¼ µÎ ¾à¹°À» º´¿ëÅõ¿©Çϴ ȯÀÚµéÀº µð°î½Å °ú·®Åõ¿© Áõ»óÀ» ÁÖÀÇÇÏ¿© °üÂûÇØ¾ß Çϸç ÇÊ¿äÇÒ °æ¿ì µð°î½ÅÀÇ Ç÷Áß ³óµµ¸¦ °í·ÁÇÏ¿© µð°î½Å(±Û·çÄڽõå) ¿ë·®À» °¨¼Ò½ÃÄÑ¾ß ÇÑ´Ù.
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4) ½Ã¸ÞƼµòÀº ½ÃÅäÅ©·Ò P450 3A4¸¦ ¾ïÁ¦½Ã۱⠶§¹®¿¡ ÀÌ ¾àÀÇ Ç÷Áß ³óµµ¸¦ Áõ°¡½Ã۸ç Ç×°íÇ÷¾Ð È¿°ú¸¦ Áõ°½Ãų ¼ö ÀÖ´Ù.
5) ¸®ÆÊÇǽŰúÀÇ º´¿ë¿¡ ÀÇÇØ ÀÌ ¾àÀÇ ÀÛ¿ëÀÌ °¨¾àµÉ ¼ö ÀÖÀ¸¹Ç·Î º´¿ëÅõ¿©ÇÏÁö´Â ¾Ê´Â´Ù(¸®ÆÊÇǽÅÀº ½ÃÅäÅ©·Ò P450 3A4°èÀÇ È¿¼ÒÀÛ¿ëÀ» °ÇÏ°Ô À¯µµÇÑ´Ù. µû¶ó¼ ¸®ÆÊÇǽÅÀ» ÀÌ ¾à°ú º´¿ëÇÒ °æ¿ì ÀÌ ¾àÀÇ »ý¹°ÇÐÀûÀÌ¿ë·üÀÌ ¶Ñ·ÇÇÏ°Ô °¨¼ÒÇÏ¿© ÀÌ ¾àÀÇ À¯È¿¼ºÀÌ °¨¼ÒµÈ´Ù.)
6) ÀÌ ¾àÀº Áú»ê¿°Á¦Á¦¿Í º´¿ëÅõ¿©ÇÒ ¼ö ÀÖÀ¸³ª ÀÌ·¯ÇÑ º´¿ë¿¡ ´ëÇÑ Çù½ÉÁõ¿¡¼ÀÇ À¯È¿¼ºÀº È®¸³µÇ¾î ÀÖÁö ¾Ê´Ù.
7) Äí¸¶¸°°è Ç×ÀÀ°íÁ¦¿Í º´¿ëÅõ¿©½Ã µå¹°°Ô ÇÁ·ÎÆ®·Òºó½Ã°£À» ¿¬Àå½ÃÄ×´Ù´Â º¸°í°¡ ÀÖÀ¸³ª ÀÌ·¯ÇÑ °ü·Ã¼ºÀº ºÒÈ®½ÇÇÏ´Ù.
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9) Åõº¸Äí¶ó¸°°ú °°Àº ±ÙÀ°ÀÌ¿ÏÁ¦¿Í º´¿ëÅõ¿©½Ã Åõº¸Äí¶ó¸°ÀÇ È¿°ú¸¦ Áõ°½ÃŲ´Ù´Â º¸°í°¡ ÀÖ´Ù
10) ½Ã»çÇÁ¸®µå¿ÍÀÇ º´¿ë¿¡ ÀÇÇØ ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ »ó½ÂÇß´Ù´Â º¸°í°¡ ÀÖ´Ù.
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[Nifedipine]
 [Nifedipine] CAS number/21829-25-4 ATC code/C08CA05 PubChem/4485 DrugBank/APRD00590 Formula/C17H18N2O6 Mol. mass/346.335 g/mol Bioavailability/45-56% Metabolism/Gastrointestinal, Hepatic Excretion/Renal: >50%, Biliary: 5-15% Pregnancy cat./
C: (USA) Legal status/ Routes/Oral Protein binding/92-98%
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| Mechanism of Action |
Nifedipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Nifedipine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
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| Pharmacology |
Nifedipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Nifedipine, the prototype of the dihydropyridine class of calcium-channel antagonists, is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. Nifedipine is used to treat Prinzmetal's angina, hypertension, and other vascular disorders such as Raynaud's phenomenon. By blocking the calcium channels, Nifedipine inhibits the spasm of the coronary artery and dilates the systemic arteries, results in a increase of myocardial oxygen supply and a decrease in systemic blood pressure.
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| Metabolism |
Nifedipine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2E1 (CYP2E1)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Nifedipine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 92-98%
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| Half-life |
Nifedipine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 hours
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| Absorption |
Nifedipine¿¡ ´ëÇÑ Absorption Á¤º¸ Rapidly and fully absorbed following oral administration.
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| Pharmacokinetics |
NifedipineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£
- °æ±¸ 20ºÐ À̳»
- ¼³ÇÏÁ¤ 1-5ºÐ À̳»
- ´Ü¹é°áÇÕ : 92-98% (³óµµÀÇÁ¸Àû)
- ´ë»ç : °£¿¡¼ ºñȰ¼º´ë»çü·Î ´ë»çµÊ
- »ýü³»ÀÌ¿ëÀ²
- ݼ¿Á¦ 45-75%
- ¼¹æÇüÁ¦Á¦ 65-86%
- ¹Ý°¨±â
- Á¤»ó ¼ºÀÎÀº 2-5½Ã°£
- °£°æÈ°¡ ÀÖ´Â ¼ºÀÎÀº 7½Ã°£
- ¼Ò½Ç : ´¢¸¦ ÅëÇØ ¹è¼³
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| Biotransformation |
Nifedipine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Nifedipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include dizziness, drowsiness, nausea, severe drop in blood pressure, slurred speech, and weakness. LD50=494 mg/kg (orally in mice); LD50=1022 mg/kg (orally in rats)
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| Drug Interactions |
Nifedipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The barbiturate decreases the effect of the calcium channel blockerAprobarbital The barbiturate decreases the effect of the calcium channel blockerButabarbital The barbiturate decreases the effect of the calcium channel blockerButalbital The barbiturate decreases the effect of the calcium channel blockerButethal The barbiturate decreases the effect of the calcium channel blockerCimetidine Cimetidine increases the effect of the calcium channel blockerCisapride Cisapride increases the effect and toxicity of nifedipineCyclosporine Increased risk of gingivitisGinseng Ginseng increases the effect and toxicity of nifedipineHeptabarbital The barbiturate decreases the effect of the calcium channel blockerHexobarbital The barbiturate decreases the effect of the calcium channel blockerImatinib Imatinib increases the effect and toxicity of nifedipineMelatonin Melatonin can possibly decrease the effect of nifedipineMethohexital The barbiturate decreases the effect of the calcium channel blockerMethylphenobarbital The barbiturate decreases the effect of the calcium channel blockerPentobarbital The barbiturate decreases the effect of the calcium channel blockerPhenobarbital The barbiturate decreases the effect of the calcium channel blockerPrimidone The barbiturate decreases the effect of the calcium channel blockerSecobarbital The barbiturate decreases the effect of the calcium channel blockerTalbutal The barbiturate decreases the effect of the calcium channel blockerRifampin Rifampin decreases the effect of the calcium channel blockerQuinidine Decreased quinidine effect, increased nifedipine effectQuinidine barbiturate Decreased quinidine effect, increased nifedipine effectDihydroquinidine barbiturate Decreased quinidine effect, increased nifedipine effectQuinupristin Synercid increases the effect of ziprasidoneTacrolimus Nifedipine increases serum levels of tacrolimusSt. John's Wort St. John's Wort decreases the effect of nifedipine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Nifedipine¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
erythromycin
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
**nifedipine**
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
cerivastatin
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
erythromycin
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Food Interaction |
Nifedipine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Avoid taking with grapefruit juice.Avoid natural licorice.Take with low fat meal.
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| Drug Target |
[Drug Target]
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| Description |
Nifedipine¿¡ ´ëÇÑ Description Á¤º¸ A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. [PubChem]
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| Drug Category |
Nifedipine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Calcium Channel BlockersDihydropyridinesTocolytic AgentsVasodilator Agents
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| Smiles String Canonical |
Nifedipine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC
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| Smiles String Isomeric |
Nifedipine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OC
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| InChI Identifier |
Nifedipine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H18N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8,15,18H,1-4H3
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| Chemical IUPAC Name |
Nifedipine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Drug-Induced Toxicity Related Proteins |
NIFEDIPINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Adenosylhomocysteinase Drug:nifedipine Toxicity:side effects. [¹Ù·Î°¡±â]
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| ÃֽŹ®Çå°ËÅä |
Sex Differences in Blood Pressure Response toAntihypertensive Therapy in Chinese Patients with Hypertension
BACKGROUND: Ç×°íÇ÷¾ÐÁ¦¿¡ ´ëÇÑ ¼ºº°°£ ¹ÝÀÀ¼ºÀÇ Â÷ÀÌ¿¡ ´ëÇØ¼´ÂÀß ¾Ë·ÁÁ® ÀÖÁö ¾Ê´Ù.
OBJECTIVE: Community-basedprospective clinical trial·Î Ç×°íÇ÷¾ÐÁ¦¿¡ ´ëÇÑ ¼ºº°°£ ¹ÝÀÀ¼º Â÷À̰¡ ÀÖ´ÂÁö¸¦ È®ÀÎÇϱâ À§ÇÏ¿© ÀÌ ¿¬±¸¸¦ ½ÃÇàÇÏ¿´´Ù.
METHODS: Áß±¹³»ÀÇ 7°³ÀÇ Áö¿ª¿¡¼ ÀÌÀü¿¡ °íÇ÷¾Ð Ä¡·á¸¦ ¹ÞÁö ¾Ê¾Ò´ø 4075¼¼ ȯÀÚ 3535¸í(¿©¼º:2326¸í)À» ¸ðÁýÇÏ¿´´Ù. ȯÀڵ鿡°Ô atenolol, hydrochlorothiazide (HCTZ), captopril, sustained-releasednifedipine Áß¿¡ 1°³ÀÇ ¾à¹°À» ¹«ÀÛÀ§ ¹èÁ¤ÇÏ¿©8ÁÖµ¿¾È ½ÃÇèÀ» ÁøÇàÇÏ¿´´Ù. ÀÌÈÄ ³²¼º°ú ¿©¼º »çÀÌÀÇ Æò±Õ Ç÷¾Ð °¨¼ÒÁ¤µµ, Ç÷¾ÐÀÌ Á¶ÀýµÇ´Â ºñÀ², ÀÌ»ó¹ÝÀÀÀÇ ¹ß»ý·üÀ» ºñ±³ÇÏ¿´´Ù.
RESULTS: ¿©¼ºÀÇ HCTZ¿¡ ´ëÇÑ ¹ÝÀÀ¼ºÀº À̿ϱâÇ÷¾Ð¿¡À־²¼ºº¸´Ù´õÁÁ¾Ò°í(1.8mmHg ´õ°¨¼Ò, p < 0.05) ³²¼ºº¸´Ù 57%ÀÌ»ó ´õ ¸ñÇ¥ÇÑÀ̿ϱâÇ÷¾Ð¿¡µµ´ÞÇÏ¿´´Ù(p < 0.05). Atenolol group¿¡¼´Â ¿©¼ºÀÌ ³²¼ºº¸´Ù Æò±Õ¼öÃà±â Ç÷¾ÐÀÌ 3.9 mmHgÀÌ»ó ´õ °¨¼ÒÇÏ¿´°í(p <0.05), ¿©¼ºÀÌ ³²¼ºº¸´Ù 65%ÀÌ»ó ´õ ¸ñÇ¥ÇÑ ¼öÃà±â Ç÷¾Ð¿¡ µµ´ÞÇÏ¿´À¸¸ç 57% ÀÌ»ó ´õ ¸ñÇ¥ÇÑ À̿ϱâÇ÷¾Ð¿¡µµ´ÞÇϱ⽬¿ü´Ù(p < 0.05).Nifedipine°ú captopril group¿¡¼ ¾à¹°°ú °ü·ÃµÈ ÀÌ»ó¹ÝÀÀÀÌ ¼ºº°°ú °ü·ÃÇÏ¿©À¯ÀǼº ÀÖ´Â Â÷À̸¦ º¸¿´Áö¸¸ (Nifedipine-15.8% in women vs 9.8% in men; p =0.017, captopril- 14.3% in women vs 8.4% in men; p = 0.005) HCTZ°ú atenolol group¿¡¼´Â À¯ÀǼº ÀÖ´Â Â÷À̸¦ º¸ÀÌÁö ¾Ê¾Ò´Ù.
CONCLUSIONS: ¿©¼ºÀÌ HCTZ¿Í atenolol¿¡ ´ëÇØ ´õ ÁÁÀº Ç÷¾Ð ¹ÝÀÀ¼ºÀ» ³ªÅ¸³»°í sustained-release nifedipine°ú captopril¿¡´ëÇØ ³²¼ºº¸´Ù ´õ ¸¹Àº ÀÌ»ó¹ÝÀÀÀ» ³ªÅ¸³»¾ú´Ù. À̰ÍÀº Ç×°íÇ÷¾ÐÁ¦¸¦ ¼±ÅÃÇϴµ¥ ÀÖ¾î¼ ¼ºº°À» °í·ÁÇÒ ¼öÀÖ´Ù´Â °ÍÀ» ÀǹÌÇÑ´Ù.
Ann Pharmacother2008;42:1772-81
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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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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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