Anti/Cholinergic drugs Flashcards
Choline ester drugs and indications.
Metacholine- test for asthma
Carbachol- post-ocular surgery
Bethanechol- urinary retention
Choline esters MOA and SEs
ACh mimetics- bind muscarinic and nicotinic receptors to activate corres. signalling pathways
SE: blurred vision, eye pain dizziness headache nausea cramps urinary urgency -SEs due to non selective agonists
Quaternary ammonium MOA
QA is responsible for reversibly binding for inhibiting AChE from hydrolyzing ACh.
Other AChEi drugs and indications
Reversible AChEis:
Donepezil and Tacrine for Dementia, Alzheimers
Edrophonium for myasthenia gravis
MOA as a SUICIDE inhibitor (gets destroyed in process) which binds AChE then hydrolyzed SLOWLY (REVERSIBLE effect)
Carbamate Esters:
Neostigmine, Physostigmine, Pyridostigmine
*BEST TAKEN ON EMPTY STOMACH
Echothiophate, Malathion, Parathion (insecticides) and Soman (nerve gas) are what kind of indirect AChi? MOA? Indication?
Organophosphates. SUICIDE inh. binds AChE, converted to a phosphorylated form, hydrolyzed extremely slowly (IRREVERSIBLE effect) -insecticides
Indicated for Chronic Open Angle Glaucoma
Anticholinergic drugs examples that are muscarinic antagonists for PD, anesthesia, motion sickness , asthma
Tertiary amines (lipophilic): Atropine, Scopolamine, Benztropine, Trihexyphenydyl Quaternary amines (less lipo): Ipratropium, Tiotropium and Glycopyrrolate
MOA and SAR that is responsible for its muscarinic antagonists.
Competitive m antagonists
Piperidine and pyrrolidine (quasi ring) essential for selective m inhibitors.
The longer the HC chain on N, the weaker the anti muscarinic
Blocks nicotinic receptors in neuromuscular junction and drug examples.
Nicotinic muscular (Nm) antagonists.
Depolarizing: Succinylcholine
Non: Atracurium, Vecu, Tubo, Pancuronium (lethal inj)
Indication gen. anes.
MOA for Nm antagonists and SEs
Quaternary amine group is essential for activity. Cyclic HC chains account for lipophicity and rapid diffusion.
SE: elevated ♥️ rate, excessive salivation, sweating, muscle weakness, resp impairment, hypotension
Anticholinergic with both depo. and non depo. blockade of nicotinic ion channel and provide SAR.
Nicotinic ganglionic (Ng) antagonists: Mecamylamine (smoking cess) Trimetaphan (HTN emerg) 4* amine necessary for function 2* to improve absorption in GI tract
About PSNS (differentiating from SNS)
originates from sacral and cranial
short postganglionic, long pre nerve fibers
ganglia near innervated organs
NT: ACh
Cholinergic receptor Nicotinic1 main location?
Adrenal medulla and autonomic ganglia
Cholinergic receptor Nicotinic2 main location?
Skeletal muscles
Cholinergic receptor Muscular1 main location?
ANS, striatum, cortex and hippocampus
Cholinergic receptor Muscarinic2 main location?
ANS, heart, intestinal smooth muscle, hindbrain and cerebellum
Adrenergic drugs that releases Catecholamines from vesicles into nerve terminals and indications.
*drug abuse
Indirect acting symp.c amines: Amphetamine (amp), Hydroxyamp, Methyl amp, Ephedrine, Pseudoeph, tyramine
For indicated for Narcolepsy, ADD, ADD
Amphetamine-like drugs SEs
stomach upset, adverse ♥️ events, restlessness, events of adrenoceptors, Tyramine-induced HTN-sive crisis with MAOi interactions
Cathecolamine reuptake inhibitors from synaptic terminals drugs and indications.
SSRI: Cita, Escita, Parox, Sert 5HT/NE: Ven, Desven, Dulox DOPA: Cocaine For depression, ADD, local anes (cocaine) SE: adverse ♥️ events
