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1. ½Å°æÁõ¿¡¼ÀÇ ºÒ¾È¡¤±äÀå
2. ¸¶ÃëÀü Åõ¾à
3. ¾ËÄÚ¿Ã ±Ý´ÜÁõ»ó
4. °æ·Ã¹ßÀÛ ¶Ç´Â °£Áú Áßø»óÅÂ
5. °Ë»çÀü Åõ¾à(ºÒ¾È¡¤±äÀå °æ°¨) : ³»½Ã°æ°Ë»ç, ½ÉÀ²µ¿Àüȯ
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4. ¸¶ÃëÀüÅõ¾à : ÀÌ ¾àÀ¸·Î¼ ¼ö¼úÀü 10§·À» ±ÙÀ°ÁÖ»çÇÑ´Ù.
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6) ¾ËÄÚ¿Ã ¶Ç´Â ¾à¹°ÀÇÁ¸¼º ȯÀÚ
7) ÁßÁõÀÇ °£ºÎÀü ȯÀÚ
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1) ÀÇÁ¸¼º : º¥Á¶µð¾ÆÁ¦ÇÉ°è ¾à¹°Ä¡·á¿¡ ÀÇÇØ ÀÇÁ¸¼ºÀÌ ÀϾ ¼ö ÀÖÀ¸¸ç Àå±â°£ Åõ¿© ȯÀÚ, °í¿ë·® Åõ¿© ȯÀÚ, ƯÈ÷ ¾ËÄÚ¿Ã Áßµ¶·Â ȯÀÚ, ¾à¹° ³²¿ë·Â ȯÀÚ, ÀΰÝÀå¾Ö ȯÀÚ, Á¤½Åº´ ¼ÒÀÎÀÌ Àִ ȯÀÚ¿¡¼ ÀÇÁ¸¼º ¹ß»ý À§Ç輺ÀÌ Áõ°¡µÇ¹Ç·Î ´ë»ó ÁúȯÀ» ÃæºÐÈ÷ °í·ÁÇÑ ÈÄ Åõ¿©ÇÏ°í °¡´ÉÇÑ ÇÑ ´Ü±â°£ µ¿¾È¸¸ Åõ¿©ÇÑ´Ù. Åõ¿©¿ë·®ÀÌ Å©°í, Ä¡·á±â°£ÀÌ ±æ¼ö·Ï ÀÇÁ¸¼º À§ÇèÀÌ Áõ°¡ÇÑ´Ù. Àå±â°£ Åõ¿©½Ã¿¡´Â Åõ¿©¿¡ µû¸¥ À¯Àͼº°ú À§Ç輺À» ¸é¹ÐÈ÷ °ËÅäÇÑ ÈÄ °áÁ¤ÇÑ´Ù.
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5) ´« : ¾È±¸ÁøÅÁ, ½Ã·ÂºÒ¼±¸í µî ½Ã·ÂÀå¾Ö°¡ ³ªÅ¸³¯ ¼ö ÀÖ´Ù.
6) Ç÷¾× : ¶§¶§·Î ¹éÇ÷±¸°¨¼Ò, °ú¸³±¸°¨¼Ò, Ç÷¾×ÀÌÈ¥ÈÁõ µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÏ´Â µî ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
7) °£Àå : ¶§¶§·Î Ȳ´Þ, µå¹°°Ô ALT, AST, ALPÀÇ »ó½Â µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÏ´Â µî ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
8) ¼øÈ¯±â°è : ¶§¶§·Î ºó¸Æ, ¼¸Æ, Ç÷¾ÐÀúÇÏ, ¼øÈ¯¼º ¼ï µîÀÌ ³ªÅ¸³¯ ¼ö ÀÖÀ¸¹Ç·Î °üÂûÀ» ÃæºÐÈ÷ Çϰí ÀÌ»óÀÌ ÀÎÁ¤µÇ´Â °æ¿ì¿¡´Â Åõ¿©¸¦ ÁßÁöÇÏ´Â µî ÀûÀýÇÑ Ã³Ä¡¸¦ ÇÑ´Ù.
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| Related FDA Approved Drug |
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Diazepam / N05BA01
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(ÀÓ»ó ½ÃÇè¿¡¼ ÀӽŠ1±â¿Í 3±â¿¡ À§Ç輺 º¸°íµÊ. -Briggs G, et al. Drugs in Pregnancy and Lactation 7th edit. )
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| Mechanism of Action |
Diazepam¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
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| Pharmacology |
Diazepam¿¡ ´ëÇÑ Pharmacology Á¤º¸ Diazepam, a benzodiazepine, generates the same active metabolite as chlordiazepoxide and clorazepate. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.
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| Metabolism |
Diazepam¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 1A2 (CYP1A2)
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| Protein Binding |
Diazepam¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 98.5%
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| Half-life |
Diazepam¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Biphasic 1-2 days and 2-5 days, active metabolites with long half lives.
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| Absorption |
Diazepam¿¡ ´ëÇÑ Absorption Á¤º¸ Essentially complete, with a bioavailability of 93%.
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| Biotransformation |
Diazepam¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam.
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| Toxicity |
Diazepam¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
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| Drug Interactions |
Diazepam¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amprenavir Amprenavir increases the effect and toxicity of benzodiazepineCimetidine Cimetidine increases the effect of the benzodiazepineClarithromycin The macrolide increases the effect of the benzodiazepineClozapine Increased risk of toxicityDigoxin The benzodiazepine increases the effect of digoxinErythromycin The macrolide increases the effect of the benzodiazepineEthotoin Possible increased levels of the hydantoin, decrease of benzodiazepineFluconazole Fluconazole increases the effect of the benzodiazepineFosamprenavir Amprenavir increases the effect and toxicity of benzodiazepineFosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineIndinavir The protease inhibitor increases the effect of the benzodiazepineItraconazole The imidazole increases the effect of the benzodiazepineJosamycin The macrolide increases the effect of the benzodiazepineKava Kava increases the effect of the benzodiazepineKetoconazole The imidazole increases the effect of the benzodiazepineMephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineNelfinavir The protease inhibitor increases the effect of the benzodiazepineOmeprazole Omeprazole increases the effect of benzodiazepinePhenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineQuinupristin This combination presents an increased risk of toxicityRifampin Rifampin decreases the effect of benzodiazepineRitonavir The protease inhibitor increases the effect of the benzodiazepineSaquinavir The protease inhibitor increases the effect of the benzodiazepineSt. John's Wort St. John's Wort could reduce the benzodiazepine effectVoriconazole The imidazole increases the effect of the benzodiazepine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Diazepam¿¡ ´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 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 |
Diazepam¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food.Avoid excessive quantities of coffee or tea (caffeine).Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Diazepam¿¡ ´ëÇÑ Description Á¤º¸ A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589)
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| Dosage Form |
÷°¡Á¦1 º¥Áú¾ËÄÚ¿Ã (ÁÖ»çÁ¦¿¡ ÇÑÇÔ.) ¡Û °æ°í
º¥Áú¾ËÄÚ¿ÃÀº ¹Ì¼÷¾Æ¿¡¼ Ä¡¸íÀûÀÎ °¡»Û È£ÈíÁõ»ó°ú ¿¬°üÀÌ ÀÖ´Â °ÍÀ¸·Î º¸°íµÇ¾ú´Ù.
¡Û ´ÙÀ½ ȯÀÚ¿¡´Â Åõ¿©ÇÏÁö ¸» °Í.
½Å»ý¾Æ, ¹Ì¼÷¾Æ(º¥Áú¾ËÄÚ¿ÃÀ» ÇÔÀ¯Çϰí ÀÖ´Ù.)
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| Drug Category |
Diazepam¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adjuvants, AnesthesiaAnesthetics, IntravenousAnti-anxiety AgentsAnticonvulsantsAntiemeticsGABA ModulatorsHypnotics and SedativesMuscle Relaxants, Central
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| Smiles String Canonical |
Diazepam¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN1C(=O)CN=C(C2=CC=CC=C2)C2=C1C=CC(Cl)=C2
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| Smiles String Isomeric |
Diazepam¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CN1C(=O)CN=C(C2=CC=CC=C2)C2=C1C=CC(Cl)=C2
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| InChI Identifier |
Diazepam¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
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| Chemical IUPAC Name |
Diazepam¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
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| Drug-Induced Toxicity Related Proteins |
DIAZEPAM ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:benzodiazepine omega 2 receptor subtype Drug:diazepam Toxicity:sedation. [¹Ù·Î°¡±â] Replated Protein:benzodiazepine omega 2 receptor subtype Drug:diazepam Toxicity:amnesia. [¹Ù·Î°¡±â] Replated Protein:benzodiazepine omega 1 receptor subtype Drug:diazepam Toxicity:anxiolysis. [¹Ù·Î°¡±â] Replated Protein:benzodiazepine omega 1 receptor subtype Drug:diazepam Toxicity:amnesia. [¹Ù·Î°¡±â] Replated Protein:benzodiazepine omega 2 receptor subtype Drug:diazepam Toxicity:anxiolysis. [¹Ù·Î°¡±â] Replated Protein:CYP2C19 Drug:Diazepam Toxicity:Prolonged sedation. [¹Ù·Î°¡±â] Replated Protein:benzodiazepine omega 1 receptor subtype Drug:diazepam Toxicity:sedation. [¹Ù·Î°¡±â]
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