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내용 |
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| Mechanism of Action |
Ribavirin에 대한 Mechanism_Of_Action 정보
Ribavirin is readily phosphorylated intracellularly by adenosine kinase to ribavirin mono-, di-, and triphosphate metabolites. Ribavirin triphosphate (RTP) is a potent competitive inhibitor of inosine monophosphate (IMP) dehydrogenase, viral RNA polymerase and messenger RNA (mRNA) guanylyltransferase (viral). Guanylyltranserase inhibition stops the capping of mRNA. These diverse effects result in a marked reduction of intracellular guanosine triphosphate (GTP) pools and inhibition of viral RNA and protein synthesis. Ribavirin is also incorporated into the viral genome causing lethal mutagenesis and a subsequent decrease in specific viral infectivity.
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| Pharmacology |
Ribavirin에 대한 Pharmacology 정보
Ribavirin is an anti-viral drug active against a number of DNA and RNA viruses. It is a member of the nucleoside antimetabolite drugs that interfere with duplication of the viral genetic material. The drug inhibits the activity of the enzyme RNA dependent RNA polymerase, due to it's resemblence to building blocks of the RNA molecules. The oral form is used in the treatment of hepatitis C, in combination with interferon drugs. The aerosol form is used to treat respiratory syncytial virus-related diseases in children. The primary serious adverse effect of ribavirin is hemolytic anemia, which may worsen preexisting cardiac disease.
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| Protein Binding |
Ribavirin에 대한 단백결합 정보
Not Available
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| Half-life |
Ribavirin에 대한 반감기 정보
9.5 hours
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| Absorption |
Ribavirin에 대한 Absorption 정보
Rapidly and extensively absorbed following oral administration. However, due to first-pass metabolism, the absolute bioavailability averages 64%.
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| Pharmacokinetics |
Ribavirin의 약물동력학자료
- 흡수 : 비강 또는 경구 흡입시 호흡기를 통해 전신으로 흡수된다.
- 흡수되는 양은 호흡인자 (respiratory factors)와 약물수송 방법에 따라 다르다.
- 기관지 삽관 후 에어로졸 제제를 사용할 때 최대로 흡수된다.
- 분포 : 기관지, 적혈구에 가장 높은 농도로 분포한다.
- 대사 : 세포내에서 대사되어 활성화된다.
- 반감기 : 혈중 :
- 최고혈중농도 도달시간 : 흡입 : 60-90 분
- 소실 : 주 소실 경로는 간대사이며, 40% 정도가 미변화체 및 대사체로 신배설된다.
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| Biotransformation |
Ribavirin에 대한 Biotransformation 정보
Hepatic. Results of in vitro studies using both human and rat liver microsome preparations indicated little or no cytochrome P450 enzyme-mediated metabolism of ribavirin, with minimal potential for P450 enzyme-based drug interactions. Ribavirin has two pathways of metabolism: (1) a reversible phosphorylation pathway in nucleated cells; and (2) a degradative pathway involving deribosylation and amide hydrolysis to yield a triazole carboxylic acid metabolite.
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| Toxicity |
Ribavirin에 대한 Toxicity 정보
Side effects include "flu-like" symptoms, such as headache, fatigue, myalgia, and fever. The LD50 in mice is 2 g/kg orally and is associated with hypoactivity and gastrointestinal symptoms (estimated human equivalent dose of 0.17 g/kg, based on body surface area conversion).
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| Drug Interactions |
Ribavirin에 대한 Drug_Interactions 정보
Not Available
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CYP450
Drug Interaction |
[CYP450 Table직접조회]
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| Drug Target |
[Drug Target]
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| Description |
Ribavirin에 대한 Description 정보
A nucleoside antimetabolite antiviral agent that blocks nucleic acid synthesis and is used against both RNA and DNA viruses. [PubChem]
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| Dosage Form |
Ribavirin에 대한 Dosage_Form 정보
Aerosol Respiratory (inhalation)
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| Drug Category |
Ribavirin에 대한 Drug_Category 정보
AntimetabolitesAntiviral Agents
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| Smiles String Canonical |
Ribavirin에 대한 Smiles_String_canonical 정보
NC(=O)C1=NN(C=N1)C1OC(CO)C(O)C1O
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| Smiles String Isomeric |
Ribavirin에 대한 Smiles_String_isomeric 정보
NC(=O)C1=NN(C=N1)[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
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| InChI Identifier |
Ribavirin에 대한 InChI_Identifier 정보
InChI=1/C8H12N4O5/c9-6(16)7-10-2-12(11-7)8-5(15)4(14)3(1-13)17-8/h2-5,8,13-15H,1H2,(H2,9,16)/t3-,4-,5-,8-/m1/s1/f/h9H2
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| Chemical IUPAC Name |
Ribavirin에 대한 Chemical_IUPAC_Name 정보
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,4-triazole-3-carboxamide
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| Drug-Induced Toxicity Related Proteins |
RIBAVIRIN 의 Drug-Induced Toxicity Related Protein정보
Replated Protein:Haptoglobin
Drug:ribavirin
Toxicity:affect hepatic functions.
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Replated Protein:Epidermal growth factor receptor
Drug:ribavirin
Toxicity:affect hepatic functions.
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Replated Protein:Hepatocyte growth factor
Drug:ribavirin
Toxicity:affect hepatic functions.
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