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Basic Sciences & Clinical Skills (NUCOG 1) » Notes
Pharmacology - Prostaglandins
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PROSTAGLANDINS

  • First isolated from semen and thought to be produced by the prostate gland
  • Synthesized from fatty acid arachidonic acid in a wide range of tissues
  • Conversion of arachidonic acid to prostaglandin endoperoxide by the enzyme cyclo-oxygenase is inhibited by aspirin and NSAIDs
  • Specific cyclo-oxygenase 2 (COX-2) inhibitors are less likely to cause GI side-effects (meloxicam, sulindac)
  • Metabolised by the liver and tissues and excreted by the kidney


Clinical use

  • 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
  • Dinoprost (PGF2-alpha) - used for pregnancy termination. Similar side-effects to dinoprostone but may be more severe
  • Gemeprost (PGE1) - used for cervical preparation prior to surgical evacuation of the uterus and for medical termination of pregnancy. Side-effects similar to PGE2
  • Carboprost - administered by deep intramuscular or intra-myometrial injection to treat severe post-partum haemorrhage


Side –effects

  • Nausea & vomiting
  • Diarrhoea (increased peristalsis)
  • Fever
  • Hypertension
  • Bronchospasm
  • Uterine hypertonus or hyperstimulation
  • Fetal distress
  • Placental abruption
  • Amniotic fluid embolism.


Misoprostol

  • Synthetic analogue of PGE1 - inhibits gastric acid secretion and is used in the treatment of gastric ulcers.
  • Unlicensed use for cervical preparation prior to surgical evacuation of the uterus, medical termination of pregnancy and induction of labour.


Side-effects

  • Diarrhoea
  • Nausea, vomiting & abdominal pain
  • Vaginal bleeding including menorrhagia, inter-menstrual and post-menopausal bleeding
     
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