Anti/Cholinergic drugs

Question 1

Choline ester drugs and indications.

Answer 1

Metacholine- test for asthma
Carbachol- post-ocular surgery
Bethanechol- urinary retention

Question 2

Choline esters MOA and SEs

Answer 2

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

Question 3

Quaternary ammonium MOA

Answer 3

QA is responsible for reversibly binding for inhibiting AChE from hydrolyzing ACh.

Question 4

Other AChEi drugs and indications

Answer 4

Reversible AChEis:
Donepezil and Tacrine for Dementia, Alzheimers
Edrophonium for myasthenia gravis

Question 5

MOA as a SUICIDE inhibitor (gets destroyed in process) which binds AChE then hydrolyzed SLOWLY (REVERSIBLE effect)

Answer 5

Carbamate Esters:
Neostigmine, Physostigmine, Pyridostigmine
*BEST TAKEN ON EMPTY STOMACH

Question 6

Echothiophate, Malathion, Parathion (insecticides) and Soman (nerve gas) are what kind of indirect AChi? MOA? Indication?

Answer 6

Organophosphates. SUICIDE inh. binds AChE, converted to a phosphorylated form, hydrolyzed extremely slowly (IRREVERSIBLE effect) -insecticides
Indicated for Chronic Open Angle Glaucoma

Question 7

Anticholinergic drugs examples that are muscarinic antagonists for PD, anesthesia, motion sickness , asthma

Answer 7

Tertiary amines (lipophilic): Atropine, Scopolamine, Benztropine, Trihexyphenydyl
Quaternary amines (less lipo): Ipratropium, Tiotropium and Glycopyrrolate

Question 8

MOA and SAR that is responsible for its muscarinic antagonists.

Answer 8

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

Question 9

Blocks nicotinic receptors in neuromuscular junction and drug examples.

Answer 9

Nicotinic muscular (Nm) antagonists.
Depolarizing: Succinylcholine
Non: Atracurium, Vecu, Tubo, Pancuronium (lethal inj)
Indication gen. anes.

Question 10

MOA for Nm antagonists and SEs

Answer 10

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

Question 11

Anticholinergic with both depo. and non depo. blockade of nicotinic ion channel and provide SAR.

Answer 11

Nicotinic ganglionic (Ng) antagonists: Mecamylamine (smoking cess) Trimetaphan (HTN emerg)
4* amine necessary for function 
2* to improve absorption in GI tract

Question 12

About PSNS (differentiating from SNS)

Answer 12

originates from sacral and cranial
short postganglionic, long pre nerve fibers
ganglia near innervated organs
NT: ACh

Question 13

Cholinergic receptor Nicotinic1 main location?

Answer 13

Adrenal medulla and autonomic ganglia

Question 14

Cholinergic receptor Nicotinic2 main location?

Answer 14

Skeletal muscles

Question 15

Cholinergic receptor Muscular1 main location?

Answer 15

ANS, striatum, cortex and hippocampus

Question 16

Cholinergic receptor Muscarinic2 main location?

Answer 16

ANS, heart, intestinal smooth muscle, hindbrain and cerebellum

Question 17

Adrenergic drugs that releases Catecholamines from vesicles into nerve terminals and indications.
*drug abuse

Answer 17

Indirect acting symp.c amines: Amphetamine (amp), Hydroxyamp, Methyl amp, Ephedrine, Pseudoeph, tyramine
For indicated for Narcolepsy, ADD, ADD

Question 18

Amphetamine-like drugs SEs

Answer 18

stomach upset, adverse ♥️ events, restlessness, events of adrenoceptors, Tyramine-induced HTN-sive crisis with MAOi interactions

Question 19

Cathecolamine reuptake inhibitors from synaptic terminals drugs and indications.

Answer 19

SSRI: Cita, Escita, Parox, Sert
5HT/NE: Ven, Desven, Dulox
DOPA: Cocaine
For depression, ADD, local anes (cocaine)
SE: adverse ♥️ events