Cholinomimetics (Direct & InDirect) -...

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Page 1 CHOLINOMIMETICS (DIRECT AND INDIRECT) DIRECT-ACTING CHOLINOMIMETICS INDIRECT-ACTING CHOLINOMIMETICS (AchEIs) GENERAL MECH. OF ACTION GENERAL MECH OF ACTION 1. Muscarinic receptor (M-receptor) stimulation 2. Nicotinic (N-) receptor stimulation, OR 3. Stimulation of both N- & M- receptors - Acetylcholinesterase (AchE) inhibition prolonged action of Ach (on both M- and N- receptors). The Irreversible inhibition caused by organophosphate is called Organonphosphate Poisoning ORGAN EFFECTS, CLINICAL USE & TOXICITY CNS CNS Effects: 1. Muscarinic stimulation causes a. seizures M1 Toxicity b. Tremor and Hyopthermia in RATs (M2) c. appetite + body fat 2. Nicotinic stimulation a. Mild Alertness - @ low conc b. Addiction to nicotine a low or high conc. - Chronic Toxicity c. Tremor, Emesis & resp. centre stimulation ( resp arrest ), Convulsion that leads to Coma & resp arrest at High conc - Acute Toxicity Clinical use: 1. Smoking cessation - Nicotine (gum, patches, nasal sprays or inhalers.) is usu. combined with Varenicline for tx of Nicotine addiction . a. Nicotine within the gums, patches, etc are slowly absorbed less binding to N- receptors less desire for nicotine b. Varenicline is a partial agonist of CNS N- receptors, which, in the presence of Nicotine (an agonist), becomes an antagonist, making it useful in smoking cessation. Nausea and vomiting, & ed psychosis, limits the use of varenicline Effects: is the net effect of nicotinic stimulation 1. Alertness -- at Low conc. 2. Convulsion Coma and Resp arrest --- at high conc - Acute Toxicity Clinical use: 1. To treat Alzheimer’s dx a neurodegenerative dxo that produces memory loss and cognition loss; mainly due to loss of cholinergic stimulations in the neocortex a. Drugs used include: Tacrine (less usage becos of hepatotoxicity); Donepezil (less hepatotoxic); Rivastigmine and Galatamine Toxicity: a. Tacrine Hepatotoxic b. Organonphophates cause Neuropathy (delayed) associated with demyelination of Neurons due to inhibition of Neuropathy Target esterases (that resembles AchE) EYE EYE Effects:
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  • Spring '17
  • Acute toxicity, nicotinic stimulation

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