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Cholinergic Agonist

  • Cholinergic Agonists are drugs that lead to stimulation of cholinergic receptors which include nicotinic and muscarinic receptors. Given the broad function of cholinergic receptors in the CNS, autonomic nervous system, and neuromuscular junction, cholinergic agonists have broad pharmacological effects which limit their therapeutic usefulness. These drugs can be divided into direct-acting agonists that directly bind cholinergic receptors or indirect-acting agonists that inhibit destruction of acetylcholine at cholinergic synapses (i.e. anticholinesterases).
Mechanisms of Actions
  • Direct Cholinergic Agonists
    • These drugs directly bind and activate nicotinic and muscarinic receptors with variable amounts of selectivity.
  • Indirect Cholinergic Agonists: The Anticholinesterases
    • These drugs inhibit anticholinesterase the enzyme which destroys acetylcholine secreted into the synapse by the cholinergic neuron. By inhibiting destruction these drugs extend the the half-life of synaptic acetylcholine and thus boost systemic cholinergic activity.
Drug Classes