Ch.11: Anticholinesterase Drugs Flashcards Preview

Pharmacology > Ch.11: Anticholinesterase Drugs > Flashcards

Flashcards in Ch.11: Anticholinesterase Drugs Deck (31):
1

anti-cholinesterase agent

drugs that inhibit the enzyme AChE, which degrades Ach. Result is to intensify Ach actions via INDIRECT activation of cholinergic receptors

2

are anti-cholinesterase agents agonists or antagonists?

NEITHER. They indirectly activate cholinergic receptors

3

Butyrlcholinesterase (BuChe) fx

(not on list)
hydrolyzes Ach and other esters
unknown physiological role
inhibited by most AChE inhibitors

4

What happens to BP after administration of AChE inhibitor?

drops

5

classification of Anti-cholinesterase agents is based on:*

the duration of enzyme inhibitioin by the inhibitor, which is related to the speed with which inhibitor dissociates from the esteratic site of AChE. Chemical structure determines all of this.

6

rank 3 types of anti-cholinesterase agents in order of shortest to longest acting

quaternary < carbamates < organophosphates

7

therapeutic uses of reversible anti-AChE agents

-ophthalmic
-GI stimulant
-Diagnostic for myasthenia Gravis
-Anti-parasitic action

8

How does edrophonium work?

blocks Ach breakdown at neuromuscular jx and promotes Ach stimulation of nicotiic receptors on skeletal muscle. Is a short acting agent

9

contraindications for use of Anti-AChe agents

-ill or debilitated
-hepatic dz
-resp. dz
-pregnancy
-GI/urinary tract obstruction
-recent exp. to anti-AChE agents
-food or dairy animals
-very young or old

10

Is edrophonium hydrolyzed by AChE?

NO

11

How is edrophonium eliminated?

renal excretion (rapid)

12

therapeutic uses of edrophonium

-temporary reversal of competitive muscle relaxants
-differential diagnosis of myasthenia gravis

13

Therapeutic uses of neostigmine

-glaucoma
-treat myasthenia gravis
-ruminal or GI stimulant
-reversal agent for muscle relaxants
(anti-parasitic, pupillary constriction)

14

duration of action of neostigmine

intermediate (1-3 hrs)

15

does neostigmine cross BBB?

NO

16

class of neostigmine

reversible anticholinesterase

17

How is neostigmine eliminated?

hydrolyzed by AChE and pseudo-ChE

18

class of physostigmine

reversible anticholinesterase

19

therapeutic uses of physostigmine

similar to neostigmine, but exhibits greater CNS activity

20

Drugs potentiated by anti-AChE agents**

-succinylcholine
-cocaine
-cholinomimetics
-morphine**
-acepromazine**
-adrenolytic agents

21

Drugs antagonized by anti-AChE agents**

-atropine
-pancuronium
-glycopyrrolate
-N-butylscopolammonium

22

drug that antagonizes Anti-AChE agent

quinine

23

OP-Type acetylcholinesterase inhibitors are used in what setting?

agriculture for pest/rodent control, as nerve gas. Not used clinically

24

parathion metabolism

metabolized in liver to active form (paraxon)

25

How do OP agents work?

form covalent bond with AChE to inhibit it. Becomes irreversible

26

What class is parathion?

irreversible anticholinesterase (OP-type inhibitor)

27

most common uses of parathion***

agricultural insecticide, urban mosquito control, cattle dip or spray

28

How can you recover from OP-type AChE inhibitors?

only way to recover is to make new enzyme (takes a long time!)

29

Signs of acute OP poisoning

inhaled: ocular, respiratory
oral: GI, systemic, SLUD*
cutaneous: sweating, muscle fasciculations, systemic signs

30

SLUD is assoc. with overstimulation of:

parasympathetic transmission in the body

31

tx for OP poisoning***

tx SLUD symptoms with atropine. Treat with praladoxime or 2-PAM ONLY IF YOU ARE CERTAIN IT IS OP POISONING AND IT IS WITHIN THE FIRST 24 HOURS (acts as a cholinesterase inhibitor)