Prostaglandins - Synthesis and Drug Profile

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Chapter: Medicinal Chemistry : Prostaglandins

i. Prostaglandin E1 (PGE1) ii. Prostaglandin D2 [PGD2] - Synthesis and Drug Profile, Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose


SYNTHESIS AND DRUG PROFILE

 

i. Prostaglandin E1 (PGE1)


Synthesis


Dose: A dose of misoprostol, 2oo μg three times a day for acute duodenal ulcer and comparable with cimetidine.

 

ii. Prostaglandin D2 [PGD2]


Synthesis


PGF2α


Synthesis


Metabolism: PGs are rapidly metabolized and inactivated by various oxidative and reductive pathways. The initial step involves rapid oxidation of the 15 α-OH group to the corresponding ketone by the PG-specific enzyme called PG 15 α-OH dehydrogenase. This is followed by a reduction of the C-13 and C-14 double bond by PG Δ13-reductase to the corresponding dihydroketone, which represent the major metabolite in plasma. Subsequently, enzymes normally involved in 13 and ω oxidation of fatty acids more slowly cleave the α-chain and oxidize the C-20 terminal methyl group to the carboxylic acid derivative, respectively.

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