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Updated: Dec 16 2018

Cholinomimetic Agents

  • Direct agonists
    • Most direct agonists are resistant to acetylcholinesterase (AChE)
      • thereby prevents breakdown of agonist
      • increases cholinergic effect
    • Direct AgonistsUsesMechanism of Action
      Methacholine• Challenge test for bronchial airway hyperactivity/asthma
        • Rapid onset of contraction of smooth muscles in the airways and increases tracheobronchial secretions
        • Slightly resistant to acetylcholine-esterase (AChE)
          Pilocarpine• Management of glaucoma
            • Contracts the pupillary sphincter (miosis) and ciliary muscle (improved accommodation)
            • Lowers intraocular pressure by reducing resistance to aqueous humor outflow
            • Resistant to AChE
              Bethanechol• Acute postoperative and postpartum urinary retention
              • Neurogenic ileus
                • Causes bladder contractions which initiates urination
                • stimulates gastric motility and tone restoring peristalsis
                • Resistant to AChE
                  Carbachol• Lowers intraocular pressure treating glaucoma
                  • Pupillary contraction
                    • Stimulates muscarinic receptors causing miosis
                    • Resistant to AChE
                  • Indirect Agonists (Cholinesterase Inhibitors)
                    • Mechanism of action
                      • all work by inhibiting ACHE
                      • thereby preventing the degradation of ACH prolonging its effects
                    • Indirect Agonist


                      • Glaucoma
                      • Atropine overdose orAtropa belladonna (deadly nightshade) ingestion
                        • CNS penetration
                        • Absorbs well on all bodily surfaces
                          Neostigmine• Postoperative and neurogenic ileus and urinary retention
                          • Myasthenia gravis
                          • Reversal of neuromuscular junction blockade (postoperative)

                            • No CNS penetration
                              Pyridostigmine• Myasthenia gravis
                                • No CNS penetration
                                  Edrophonium• Diagnosis of myasthenia gravis
                                  • Ileus
                                  • Arrhythmias
                                    • Extremely short lived (5 - 15 min)
                                      Echothiophate• Glaucoma
                                        • Long-lasting (100 hours)
                                        • No CNS penetration
                                        • Insecticides: malathion is safe in humans but parathion is harmful and both can penetrate the CNS
                                      • Cholinesterase Inhibitor Poisoning
                                        • Cholinesterase poisoning symptoms
                                          • due to ingestion of parathion or cholinesterase inhibitors
                                          • symptoms result from the overstimulation of systemic cholinergic receptors
                                            • Glands: sweating, salivation, and lacrimation
                                            • GI and GU: diarrhea, abdominal cramping, urination
                                            • Heart: bradycardia
                                            • Respiratory: bronchospasm
                                            • Musculoskeletal: skeletal muscle overexcitation
                                            • Eye: miosis
                                          • Mnemonic: Diarrhea, Urination, Miosis, Bradycardia, Emesis, Lacrimation, Lethargy, and Salivation
                                        • Treatment
                                          • atropine: blocks muscarinic receptors
                                          • pralidoxime: regenerated AChE
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