Megestrol에 대한 Mechanism_Of_Action 정보 Several investigators have reported on the appetite enhancing property of megestrol acetate and its possible use in cachexia. The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time. The biochemical mechanism of progestin antitumour activity is not well but may involve interaction with progesterone and glucocorticoid receptors, androgenic properties. Megestrol also has direct cytotoxic effects on breast cancer cells in tissue culture and suppresses luteinising hormone release from the pituitary.
Pharmacology
Megestrol에 대한 Pharmacology 정보 Megestrol is a synthetic progestin and has the same physiologic effects as natural progesterone. The precise mechanism of megestrol’s antianorexic and anticachetic effects is unknown. Initially developed as a contraceptive, it was first evaluated in breast cancer treatment in 1967.
Protein Binding
Megestrol에 대한 단백결합 정보 Not Available
Half-life
Megestrol에 대한 반감기 정보 34 hours
Absorption
Megestrol에 대한 Absorption 정보 Variable, but well absorbed orally.
Pharmacokinetics
Megestrol Acetate의 약물동력학자료
작용발현시간 :
적어도 2 개월이상의 지속적 치료 필요
흡수 : 경구 : 잘 흡수
대사 : 간에서 free steroids 및 glucuronide conjugates로 대사
작용지속시간 :
난소암 : 경구 : 5-6 개월
혈중최고농도 도달시간 : 1-3 시간
소실 : 신소실 : 10 일이내 57-78 % 소실
변으로의 소실 : 10일이내 8-30 %소실
Biotransformation
Megestrol에 대한 Biotransformation 정보 Primarily hepatic. Megestrol metabolites which were identified in urine constituted 5% to 8% of the dose administered. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces. No active metabolites have been identified.
Toxicity
Megestrol에 대한 Toxicity 정보 No serious unexpected side effects have resulted from studies involving megestrol acetate oral suspension administered in dosages as high as 1200 mg/day.
Drug Interactions
Megestrol에 대한 Drug_Interactions 정보 Amobarbital The enzyme inducer decreases the effect of hormonesAprobarbital The enzyme inducer decreases the effect of hormonesButabarbital The enzyme inducer decreases the effect of hormonesButalbital The enzyme inducer decreases the effect of hormonesButethal The enzyme inducer decreases the effect of hormonesHeptabarbital The enzyme inducer decreases the effect of hormonesHexobarbital The enzyme inducer decreases the effect of hormonesGriseofulvin The enzyme inducer decreases the effect of hormonesEthotoin The enzyme inducer decreases the effect of hormonesFosphenytoin The enzyme inducer decreases the effect of hormonesPhenytoin The enzyme inducer decreases the effect of hormonesMephenytoin The enzyme inducer decreases the effect of hormonesTalbutal The enzyme inducer decreases the effect of hormonesSecobarbital The enzyme inducer decreases the effect of hormonesPrimidone The enzyme inducer decreases the effect of hormonesPentobarbital The enzyme inducer decreases the effect of hormonesPhenobarbital The enzyme inducer decreases the effect of hormonesMethohexital The enzyme inducer decreases the effect of hormonesMethylphenobarbital The enzyme inducer decreases the effect of hormones
Megestrol에 대한 Description 정보 17-Hydroxy-6-methylpregna-3,6-diene-3,20-dione. A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer. [PubChem]
Drug Category
Megestrol에 대한 Drug_Category 정보 Antineoplastic Agents, HormonalContraceptives, Oral, Synthetic
Smiles String Canonical
Megestrol에 대한 Smiles_String_canonical 정보 CC(=O)C1(O)CCC2C3C=C(C)C4=CC(=O)CCC4(C)C3CCC12C
Smiles String Isomeric
Megestrol에 대한 Smiles_String_isomeric 정보 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C
InChI Identifier
Megestrol에 대한 InChI_Identifier 정보 InChI=1/C22H30O3/c1-13-11-16-17(20(3)8-5-15(24)12-19(13)20)6-9-21(4)18(16)7-10-22(21,25)14(2)23/h11-12,16-18,25H,5-10H2,1-4H3/t16-,17+,18+,20-,21+,22+/m1/s1
Chemical IUPAC Name
Megestrol에 대한 Chemical_IUPAC_Name 정보 (8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one
사용자컨텐츠
항목
내용
최근정보수정일 2022-12-19
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