A.9

Question 1

Cholinomimetics

Answer 1

1. Direct cholinomimetics: Pilocarpine, Carbachol.
2. Indirect cholinomimetics:
   -Tertiary amines: Rivastigmin, Physostigmin.
   -Quaternary amines: Edrophonium, Neostigmin, Pyridostigmin

Question 2

Pilocarpine

Answer 2

MOA: directly bind ACh-R (either M or N) and activates it;
Kinetics: Alkaloid!! tertiary amine (can cross BBB), administered p.o;
IND: Glaucoma, xerostomia caused by radiotherapy, Sjorgen’s syndrome;
SEs: DUMBBLES (diarrhea, urination, miosis, bronchospasm, bradycardia, lacrimation, excitation of muscles, sweat&salivation)

Question 3

Carbachol

Answer 3

MOA: directly bind ACh-R (either M or N) and activates it;
Kinetics: Cholinester!! quaternary amine, poor GI absorption&CNS penetration, excreted by the kidney, NO sensitivity to Cholinesterase;
IND: glaucoma, eye surgery;

Question 4

Rivastigmin

Answer 4

MOA: AChE-inhibitor;
DOA: long T1/2;
IND: Alzheimer’s disease (→ ↑ACh);
ROA: p.o or transdermal patch;
SEs: nausea, vomiting, diarrhea, bradycardia;
Extra: can cross BBB

Question 5

Physostigmin

Answer 5

IND: antidote for anticholinergic (antimuscarinic, e.g. Atropine) intoxication

Question 6

Irreversible AChE inhibitors

Answer 6

Organophosphates (e.g. Parathion);
SE: DUMBBLES;
Th: Atropine (to prevent overactivation of PSY, then pralidoxime to regenerate AChE):

Question 7

Edrophonium

Answer 7

MOA: competititve reversible AChE inhibitor;
DOA: short, 5-15min;
IND: tensilon test to digagnose MG, overcome the effect of muscle relaxants;
ROA: i.v

Question 8

Edrophonium

Answer 8

MOA: competititve reversible AChE inhibitor;
DOA: short, 5-15min;
IND: tensilon test to digagnose MG, overcome the effect of muscle relaxants;
ROA: i.v

Question 9

Neostigmin

Answer 9

MOA: AChE-inhibitor;
ROA: parentral;
IND: Reverse non-depol. neuromuscular block (→e.g. after anesthesia), Non-obstructive ileus, urinary retention;
DOA: 0.5-2h

Question 10

Pyridostigmin

Answer 10

MOA: AChE-inhibitor;
IND: MG;
DOA: 3-6h;
Extra: quaternary amine- cannot cross BBB

Question 11

Reversible AChE inhibitors

Answer 11

-tertiary amines: (e.g. Rivastigmin, physostigmin) can penetrate biol. membranes::examples of them, permeability feature.
-Quaternary amines: e.g. Neostigmin, Pyridostigmin, Edrophonium. cannot cross the BBB