Pharmacology - Prostaglandins
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PROSTAGLANDINS
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First isolated from semen and thought to be produced by the prostate gland
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Synthesized from fatty acid arachidonic acid in a wide range of tissues
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Conversion of arachidonic acid to prostaglandin endoperoxide by the enzyme cyclo-oxygenase is inhibited by aspirin and NSAIDs
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Specific cyclo-oxygenase 2 (COX-2) inhibitors are less likely to cause GI side-effects (meloxicam, sulindac)
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Metabolised by the liver and tissues and excreted by the kidney
Clinical use
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Dinoprostone (PGE2) is used for induction of labour (Prostin®, Propess®). It is active orally (less active than following vaginal administration) but side-effects are more frequent
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Dinoprost (PGF2-alpha) - used for pregnancy termination. Similar side-effects to dinoprostone but may be more severe
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Gemeprost (PGE1) - used for cervical preparation prior to surgical evacuation of the uterus and for medical termination of pregnancy. Side-effects similar to PGE2
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Carboprost - administered by deep intramuscular or intra-myometrial injection to treat severe post-partum haemorrhage
Side –effects
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Nausea & vomiting
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Diarrhoea (increased peristalsis)
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Fever
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Hypertension
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Bronchospasm
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Uterine hypertonus or hyperstimulation
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Fetal distress
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Placental abruption
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Amniotic fluid embolism.
Misoprostol
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Synthetic analogue of PGE1 - inhibits gastric acid secretion and is used in the treatment of gastric ulcers.
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Unlicensed use for cervical preparation prior to surgical evacuation of the uterus, medical termination of pregnancy and induction of labour.
Side-effects
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Diarrhoea
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Nausea, vomiting & abdominal pain
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Vaginal bleeding including menorrhagia, inter-menstrual and post-menopausal bleeding
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