- 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
Drug Actions
Drug Actions
- Drugs may act in a number of different ways to exert their effect
- Drug actions can be classified as being due to:
- Physicochemical properties of the drug
- Interaction with enzymes
- Interaction with voltage-gated ion channels
- Interaction with receptors
- 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
- See the next page on receptors