FRCA Notes


Drug Actions


  • Drugs may act in a number of different ways to exert their effect
  • Drug actions can be classified as being due to:
    1. Physicochemical properties of the drug
    2. Interaction with enzymes
    3. Interaction with voltage-gated ion channels
    4. Interaction with receptors
  • There are a number of drugs which demonstrate this property:
    • Sugammadex, which selectively chelates rocuronium and other aminosteroid NMBA
    • Mannitol, which exerts an osmotic effect that induces diuresis and draws fluid from the interstitium
    • Activated charcoal, which has a high surface area to mass ratio and binds ingested poisons
    • Antacids, which neutralise gastric acid
    • Chelating agents such as penicillamine (copper) and dicobalt edetate (cyanide, sodium nitroprusside), which remove toxic chemicals from the body

  • Enzymes are biological catalysts - they speed up a reaction without themselves being used up
  • They are often highly specific to a given substrate, and their function is dependent to an extent on local pH and temperature

  • Most drugs that interact with enzymes are inhibitors
  • Enzyme inhibition can increase the concentration of a substrate normally metabolised by the enzyme e.g. anticholinesterases increasing acetylcholine concentration at the NMJ
  • Or conversely inhibition can reduce the concentration of the product of the enzymatic reaction e.g. ACE-inhibitors inhibit the catalysis of angiotensin I to angiotensin II conversion

  • Enzyme inhibition may be competitive, non-competitive or irreversible

  • Voltage-gated ion channels are involved in the conduction of action potentials/impulses in excitable tissue such as muscle and nerves
  • Examples of drugs that bind voltage-gate ion channels to produce a therapeutic effect include:
    • Local anaesthetics, which bind the intracellular portion of Na+ channels in nerve membranes
    • Anticonvulsants, which bind Na+ channels in the brain
    • Calcium channel blockers, which bind ion channels in vascular smooth muscle
    • Anti-arrhythmic agents, which block a variety of myocardial ion channels