L 16-17 Flashcards Preview

Pharmacology Fall 2015 > L 16-17 > Flashcards

Flashcards in L 16-17 Deck (28):
1

Non-selective, direct acting cholinergic agonists

Acetylcholine
Methacholine, Carbachol

2

Selective, direct acting cholinergic agonists

Bethanechol, Pilocarpine
selective for Muscarinic

3

Effect of Ach IV infusion

Acts on M3 receptors to cause inc NO–> inc cGMP –> vasodilation

4

Choline Esters

Resist AchE better than Ach
Methacholine, Carbachol, Bethanechol

5

Alkaloids

Like Muscarine
Pilocarpine, Nicotine

6

Drug to increase GI activity

Bethanechol

7

Drug to increase salivation

Pilocarpine

8

Drug to help increase bladder function

Bethanechol

9

Drug to increase lacrimation, salivation, sweat etc.

Pilocarpine

10

Best drug for dry mouth

Pilocarpine can be used, but has side effects from stimulating all M receptors
Cevimeline: better because M3 specific

11

Nicotine overdose

Nicotine goes to the brain quickly and causes CNS problems
Cardiac will first beat faster causing hypertension and arrhythmias before causing hypotension
Nicotinic receptors desensitize quickly and lead to paralysis
Treat with Atropine to block M receptors and decrease PS response

12

Varenicline

Partial N agonist
Used to decrease cravings from nicotine withdrawal
Side effects: flatulence, psychosis. vomiting

13

What are drugs that end in -stigmine or -onium?

Cholinesterase inhibitors

14

Acetylcholine

Non-selective cholinergic agonist

15

Bethanechol

M-selective cholinergic agonist
In choline ester group
Used for GI and Bladder problems

16

Carbachol

Non-selective cholinergic agonist
Choline ester group

17

Pilocarpine

M-selective cholinergic agonist
used in eye, and for glands
Alkaloid

18

Methacholine

Non-selective cholinergic agonist
Choline ester

19

Neostigmine

Cholinesterase inhibitor
Cleaved by AchE, then occupies site
Duration 2-4hr
No CNS
Poor oral absorption
Use: inc bladder function, Myasthenia Gravis, reverse N.M. blockade in surgery

20

Physostigmine

Cholinesterase inhibitor
Crosses CNS–>side effects
Only good for Atropine overdose

21

Pyridostigmine

Cholinesterase inhibitor
Longer duration 4-6hr

22

Edrophonium

Cholinesterase inhibitor
Short duration 5-20 min
Injection only, no CNS
Use: diagnose Myasthenia Gravis

23

Organophosphates

Cholinesterase inhibitor
Lipid soluble–>storage and slow release
Becomes irreversible with aging

24

Pralidoxime (2-PAM)

Prevents aging of organophosphates
Doesn't work with carbamates
No CNS
Can itself bind AchE so must only be used in correct amount

25

General Effects of AchE Inhibitors

In general, Parasympathetic effects dominate

26

Donepezil

Cholinesterase inhibitor
Used for Alzheimers because some inc in PS activity causes inc alertness and better memory
Has long duration and low peripheral effects

27

Echothiophate

Organophosphate but not lipid soluble
Used in eye, effects last for days because not well absorbed

28

Symptoms of AchE Toxicity

High Ach=> high Parasymp. effects including SLUDGE
Neuromuscular effects => desensitization and paralysis
Muscarinic agonist has no muscle effect
Treatment: Atropine, 2-PAM
If carbamate: atropine only, no 2-PAM