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Glyceryl trinitrate

Indications
Administration/Absorption
  • The effectiveness of glyceryl trinitrate is limited by development of tolerance/tachyphylaxis within 2-3 weeks of sustained use
  • Continuous administration and absorption accelerate onset of tolerance and limit the usefulness of the agent
  • Thus glyceryl trinitrate works best when used only short term, pulse dosing
    • tablet placed under the tongue or a spray into the mouth
Dosage

Distribution

Mechanism
  • Vasodilator
  • prodrug which must first be denitrated to produce the active metabolite NO
  • NO is a potent activator of guanylyl cyclase (GC) by heme-dependent mechanisms
    • results in cGMP formation from guanosine triphosphate (GTP)
    • cGMP then activates myosin light chain phosphatase via a cGMP-dependent protein kinase.
Excretion

Side effects
Interactions
Contraindications
  • Anaemia
  • Cerebrovascular disease
  • Toxic pulmonary oedema
Comments