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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
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°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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Alprazolam¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Alprazolam¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects 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 the inhibitory neurotransmitter 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 |
Alprazolam¿¡ ´ëÇÑ Pharmacology Á¤º¸ Alprazolam, a benzodiazepine, is used to treat panic disorder and anxiety disorder. Unlike chlordiazepoxide, clorazepate, and prazepam, alprazolam has a shorter half-life and metabolites with minimal activity. Like other triazolo benzodiazepines such as triazolam, alprazolam may have significant drug interactions involving the hepatic cytochrome P-450 3A4 isoenzyme. Clinically, all benzodiazepines cause a dose-related central nervous system depressant activity varying from mild impairment of task performance to hypnosis. Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking.
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| Metabolism |
Alprazolam¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Alprazolam¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 80% (mainly to albumin)
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| Half-life |
Alprazolam¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 6.3-26.9 hours
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| Absorption |
Alprazolam¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%.
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| Pharmacokinetics |
AlprazolamÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ºÐÆ÷¿ëÀû(Vd) : 0.9-1.2 L/kg, À¯Áó¿¡ ºÐÆ÷µÈ´Ù.
- ´Ü¹é°áÇÕ : 80%
- ´ë»ç : ÁÖ·Î °£´ë»çµÇ¸ç ÁÖ´ë»çü´Â ºñȰ¼ºÇüÀÌ´Ù.
- ¹Ý°¨±â : 12-15 ½Ã°£
- ¼Ò½Ç : ´ë»çü¿Í ¿ø¾à¹°ÀÌ ½Å¹è¼³µÈ´Ù.
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| Biotransformation |
Alprazolam¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Hydroxylated in the liver to ¥á-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides.
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| Toxicity |
Alprazolam¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral, mouse: LD50=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
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| Drug Interactions |
Alprazolam¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amprenavir Increases the effect and toxicity of benzodiazepineAprepitant Increases the effect and toxicity of benzodiazepineCarbamazepine Reduces the effect of the benzodiazepineCimetidine Increases the effect of the benzodiazepineClarithromycin The macrolide increases the effect of the benzodiazepineClozapine Increased risk of toxicityDelavirdine The antiviral agent increases the effect and toxicity of benzodiazepineDigoxin The benzodiazepine increases the effectEfavirenz The antiviral agent increases the effect and toxicity of benzodiazepineErythromycin The macrolide increases the effect of the benzodiazepineEthotoin Possible increased levels of the hydantoin, decrease of benzodiazepineFluconazole Increases the effect of the benzodiazepineIndinavir The protease inhibitor increases the effect of the benzodiazepineItraconazole The imidazole increase 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 Increases the effect of the benzodiazepinePhenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineRitonavir The protease inhibitor increases the effect of the benzodiazepineSaquinavir The protease inhibitor increases the effect of the benzodiazepineTelithromycin Increases the effect/toxicity of the benzodiazepineVoriconazole The imidazole increases the effect of the benzodiazepineErythromycin The macrolide increases the effect of the benzodiazepineFosamprenavir Amprenavir increases the effect and toxicity of benzodiazepineFosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineJosamycin The macrolide increases the effect of the benzodiazepineKava Kava increases the effect of the benzodiazepineSt. John's Wort St. John's Wort could reduce the benzodiazepine effect
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Alprazolam¿¡ ´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 |
Alprazolam¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food.Avoid excessive quantities of coffee or tea (Caffeine).Avoid taking with grapefruit juice.
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| Drug Target |
[Drug Target]
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| Description |
Alprazolam¿¡ ´ëÇÑ Description Á¤º¸ A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238)
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| Dosage Form |
Alprazolam¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Alprazolam¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-anxiety AgentsBenzodiazepinesGABA ModulatorsHypnotics and Sedatives
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| Smiles String Canonical |
Alprazolam¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12
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| Smiles String Isomeric |
Alprazolam¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12
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| InChI Identifier |
Alprazolam¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C17H13ClN4/c1-11-20-21-16-10-19-17(12-5-3-2-4-6-12)14-9-13(18)7-8-15(14)22(11)16/h2-9H,10H2,1H3
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| Chemical IUPAC Name |
Alprazolam¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
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| Drug-Induced Toxicity Related Proteins |
ALPRAZOLAM ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Platelet-activating factor receptor Drug:Alprazolam Toxicity:anterograde amnesia. [¹Ù·Î°¡±â] Replated Protein:Benzodiazepine receptor Drug:Alprazolam Toxicity:anterograde amnesia. [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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