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Cholenergic drugs

Kaplan

QuestionAnswer
What are the subtypes of Nicotinic receptors and where they are found? Nn and Nm Nn: located in cell bodies in ganglia of both PANS and SANS Nm: located on the skeletal muscle motor end plate (innervated by somatic motor nerves)
Where are Muscarinic (M1-3) receptors found? M1 in brain M2 in heart (inhibitory effect) M3 everywhere else
Which organ is part of the sympathetic nervous system but still has muscarinic receptors? SWEAT GLANDS and Pilorectal muscles (small sm in hair follicle responsible for goosebumps)
What is the rate limiting step in Ach synthesis? the UPTAKE of CHOLINE (choline + acetyl-CoA = Ach)
Ach gets broken down by which enzyme in the presynaptic cleft and into what metabolism? by Acetylcholine Esterase (reason ach has short half life) metabolism: Choline + Acetate
Which receptor on the presynaptic neuron causes negative feedback? Alpha2 autoreceptor is a Gi coupled receptor
MOA of Botulinum toxin CLEAVES SNARES --> no release of Ach Botulinum toxin enters the presynaptic neuron
Nicotinic receptors are what type of receptors? ION CHANNELS (Na/K channels)
What are the Muscarinic agonists? (4) 1. Bethanechol (bowels and bladder) 2. Metacholine (to diagnose bronchial hypersensitivity) 3. Pilocarpine 4. Cevimeline
What are the Acetylcholinesterase Inhibitors? (7) 1. Edrophonium (diagnose myasthenia gravis) 2. Physostigmine 3. Neostigmine + 4. Pyridostigmine 5.Donepezil 6. Rivastigmine 7. Organophosphates (irreversible inhibitors)
Which Acetylcholinesterase inhibitors used to treat Alzheimer disease? (2) 1. Rivastigmine 2. Donepezil
What are the irreversible Acetylcholinesterase inhibitors? Malathion, Parathion (insecticides Sarin (nerve gas)
What are the effects of excessive muscarinic and nicotinic stimulations? DUMBBEELSS Diarrhea, Urination, Miosis, Bradycardia, Bronchoconstriction, Emesis, Excitation, Lacrimation, Salivation and Sweating
Which drug is used to REGENERATE Acetylcholinesterase and it binds what? PRALIDOXIME (2-PAM) binds to alkyl group of organophosphate (irreversibe AchE inhibitors) within 4 hours, before aging/hydrolysis occurs.
Which AchE inhibtor is used to treat Myasthenia gravis? 1. Neostigmine 2. Pyridostigmine they used for reversal of nondepolarizing Nm blockers
Which AchE inhibitor is an antidote in atropine overdose? Physostigmine (also used for glaucoma)
What is a prototypic muscarinic receptoe antagonist? ATROPINE
What other classes of drugs has antimuscarinic effects? (6) 1. Antihistamines (1st gen) 2. TCAs (antidepressants) 3. Antipsychotics 4. Quinidine 5. Amantadine 6. Meperidine
Antidote for Muscarinic blockers? PHYSOSTIGMINE
What are the other Muscarinic receptor blockers? 1. Tropicamide (used for eye exams) 2. Oxybutynin (overactive bladder) 3. Ipratropium, Tiotropium (asthma + COPD) 4. Scopalamine (motion sickness- cause sedation + temp memory block) 5. Benztropine, Trihexyphenidyl (parkinsonism)
Where are Muscarinic receptors found? Eyes Heart Lungs GIT Bladder Glands Sphincters
What happens when a ganglion blocking drug is administered? prevent reflex changes in heart rate eliceted by vasoconstriction and vasodilation (B2)
What are the Nicotinic receptor antagonists/ blockers? (2) 1. Hexamethonium 2. Mecamylamine (not used anymore dt many side effects)
Created by: DVD27
 

 



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