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¿¡Ä¡¿ÃÁÖ»ç500mg ETHYOL INF.VIAL.[Amifostine]
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| Brandname Á¤º¸ |
Amifostine
Brand Names/Synonyms
- Amifostine Ethiofos
- Aminopropylaminoethyl Thiophosphate
- Apaetp
- Ethiofos
- Ethyol
- Gammaphos
- SAPEP
Brand Name MixturesNot Available
Chemical IUPAC Name2-(3-aminopropylamino)ethylsulfanylphosphonic acid
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(amifostine; )
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| Mechanism of Action |
Amifostine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ The thiol metabolite is responsible for most of the cytoprotective and radioprotective properties of amifostine. It is readily taken up by cells where it binds to and detoxifies reactive metabolites of platinum and alkylating agents as well as scavenges free radicals. Other possible effects include inhibition of apoptosis, alteration of gene expression and modification of enzyme activity.
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| Pharmacology |
Amifostine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Amifostine is an organic thiophosphate cytoprotective agent indicated to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer or non-small cell lung cancer and also to reduce the incidence of moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer. Amifostine is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite, believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues. Healthy cells are preferentially protected because amifostine and metabolites are present in healthy cells at 100-fold greater concentrations than in tumour cells.
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| Metabolism |
Amifostine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Alkaline phosphatase
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| Protein Binding |
Amifostine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Amifostine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8 minutes
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| Absorption |
Amifostine¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Pharmacokinetics |
AmifostineÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Èí¼ö : °æ±¸·Î´Â ºÒ¿ÏÀüÇÔ
- ºÐÆ÷ : Vd : 3.5L
- ´ë»ç : µÎ°¡Áö ´ë»çü·Î °£¿¡¼ dephosphorylationµÊ
- ¹è¼³ : ½ÅÀå Ç÷Àå Ŭ¸®¾î·±½º : 2.17 L/min
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| Biotransformation |
Amifostine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Amifostine is rapidly dephosphorylated by alkaline phosphatase in tissues primarily to the active free thiol metabolite and, subsequently, to a less active disulfide metabolite.
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| Toxicity |
Amifostine¿¡ ´ëÇÑ Toxicity Á¤º¸ Rat LD50: 826 mg/kg
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| Drug Interactions |
Amifostine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Amifostine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Amifostine¿¡ ´ëÇÑ Description Á¤º¸ A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia. [PubChem]
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| Dosage Form |
Amifostine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Powder, for solution Intravenous
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| Drug Category |
Amifostine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Radiation-Protective Agents
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| Smiles String Canonical |
Amifostine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ NCCCNCCSP(O)(O)=O
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| Smiles String Isomeric |
Amifostine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ NCCCNCCSP(O)(O)=O
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| InChI Identifier |
Amifostine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C5H15N2O3PS/c6-2-1-3-7-4-5-12-11(8,9)10/h7H,1-6H2,(H2,8,9,10)/f/h8-9H
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| Chemical IUPAC Name |
Amifostine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-(3-aminopropylamino)ethylsulfanylphosphonic acid
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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. AMIFOSTINE[GGT Increase][Composite Activity](Score) I(Marginal) 0(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGOT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[SGPT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0[LDH Increase](Activity Score) I(Number of Rpts) <4(Index value) 41.5[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0
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