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Cholinergic Agonists - Coggle Diagram

- - - - which include ACh (natural) and synthetic esters of choline
      - such as bethanechol, carbachol and methacholine.
      - Acetylcholine
        
        in general
        
        Cannot penetrate membranes (poor lipid solubility)
        
        Activates both muscarinic and nicotinic receptors
        
        Rapidly inactivated by the AChE
        
        Therefore, it is injected (mostly intraocular or IV injections).
        
        its effect
        
        Primary effect of Ach is on ocular system
        
        …used during ophthalmic surgery.
        
        Produce miosis
        
        Cardiac effects
        
        Decrease in heart rate and cardiac output
        
        GI and GU effects
        
        not so much
        
        Vascular effects and blood pressure
        
        Decreases blood pressure by producing vasodilation.
      - Bethanechol
        
        its effect
        
        Primary effect is on the GI and GU systems
        
        GI System: Enhances GI Motility
        
        GU System: Stimulates the detrusor muscle of the bladder, promoting urination.
        
        Side effects
        
        in
        
        Cardiovascular: Hypotension and bradycardia
        
        Respiratory: Bronchoconstriction .. So, contraindicated for asthma & COPD patients.
        
        GI: Diarrhea due to increased GI secretions and increased GI motility.
        
        Glands: Increased sweating yielding diaphoresis.
        
        Toxicology
        
        give atropine
      - Carbachol
        
        Primarily used topically in the eye to induce miosis of the pupil
        
        lowers pressure in the eye by increasing the amount of fluid that drains
        
        used prior to certain ophthalmological surgeries
        
        treatment of open-angle or narrow-angle glaucoma.
    - - such as nicotine and pilocarpine.
      - Pilocarpine
        
        Primarily used topically in the eye and mouth
        
        As Carbachol, it induces pupillary miosis and is used in the treatment of open-angle
        or narrow-angle glaucoma.
        
        promotes salivation
        
        treatment of
        xerostomia (dry mouth)
        
        Toxicity
        
        characterized by exaggeration of sweating (diaphoresis) and salivation
        
        use atropine
- - - - non-specific and acts on
        both nicotinic and muscarinic receptors
  - - - Physostigmine
      - Neostigmine
      - Edrophonium
      - Pyridostigmine
      - اقري الجدول بسيييط
    - - have very long duration of action and are extremely toxic
      - are used as insecticides.
      - Echothiophate
        
        Once bound to AChE, these compounds phosphorylate the esteratic site on AChE,
        which permanently inactivates the enzyme
        
        restoration of enzymatic activity requires the synthesis of new enzyme molecules
        
        Its actions include
        
        cholinergic stimulation
        
        paralysis of motor
        function
        
        (causing breathing difficulties - most important cause of acute deaths in
        cholinesterase inhibitor toxicity) and convulsions
        
        Used in the treatment of open-angle glaucoma
        
        also used to treat certain eye-focusing disorders
        
        should not be used in the treatment of narrow-angle glaucoma
        
        Toxicology
        
        (mostly organophosphate) are used as agricultural
        insecticides
        
        (cholinergic crisis)
        
        Many deaths occur within hours
        
        respiratory failure due to central respiratory depression, respiratory muscle
        weakness, and/or direct pulmonary effects
        
        Management
        
        Atropine
        
        to prevent muscarinic side effects of these agents
        
        Diazepam
        
        to reduce the persistent
        convulsion caused by these agents.
        
        Pralidoxime (2-PAM)
        
        can reactivate inhibited AChE.
        
        it is unable to penetrate into the CNS