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Flashcards in Cholinergic Agonists- T1 Deck (23):
1

The three classes of muscarinic agonists and examples

1. Ach derivatives: Ach, carbachol, bethanachol, methacholine
2. alkaloids: pilocarpine
3. synthetic- cevimeline

2

example of nicotinic agonist drug

chantix

3

cholinergic agonists have predominant actions on:

1. autonomic effector organs innervated by postganglionic parasympathetic nerves
2. cells containing cholinergic receptors.

4

cholinergic agonists primarily divided into:

1. Ach and synthetic choline esters
2. cholinomimetic natural alkaloids and analogs.

5

cholinergic agonists also activate__ found in

nicotinic receptors found in the ganglia, neuromuscular junction and CNS

6

Describe Ach

-endogenous NT; no selectivity for muscarinic vs. nicotinic receptors
-rapid metabolism by Achesterase
-Ach is a (+) polar molecule, ester, that undergoes hydrolysis--> carboxylic acid and an alcohol.

7

derivatives of choline esters are generally

generally more resistant to AChE metabolism and have altered cholinergic receptor selectivity.

8

give the susceptibility to cholinesterase metabolism

Ach>methacholine> carbachol> bethanechol

9

activation of specific muscarinic receptors in various organs. (10)

decreases heart rate, vasodilation, increase intestinal smooth muscle contraction, motility, urinary( increased detrusor muscle contraction), increase bronchial constriction, increased salivation, increased salivation, increased mitosis, increased accommodation for near vision

10

What determines Gs/GI, GQ for signal transaction of muscarinic receptors

alpha subunit

11

all receptors coupled to phosphoionsitide are

GQ

12

coupling of muscarinic receptors to effectors via GO/I

-M2 receptor activation results in decreased heart rate and decreased neurotransmitter release from cholinergic nerves.
-M2 receptors regulate cAMP by decreasing adenylyl cyclase activity. cAMP regulates heart rate and contractility.

13

beta receptor-->

Q activity of cardiac myocytes, also activate potassium channels, stimulating the depolarization of cardiac cells.

14

what drug(s) can produce mitosis during eye surgery and decrease intraocular pressure

Ach and carbachol. pupil constriction via M3 receptors.

15

what drug for airway hyperactivity test

methacholine--> causes constriction and increased resistance to airflow.

16

what drug for urinary urgency and increase GI motility

bethanechol. bethanechol increases tension on the bladder.

17

cholinergic agonist natural alkaloids are

more selective for muscarinic vs nicotinic receptors, pilocarpine is the only one of therapeutic value, and tend to give long duration of action.

18

pilocarpine cardiovascular effects

decreases heart rate and blood pressure

19

alkaloids smooth muscle effects

pupillary constriction, initial increase followed by a decreased intraocular pressure, decreased far vision, increase bronchial and GI muscle contraction, promote urination.

20

alkaloids exocrine gland effects

sweating, N/V, salivation, lacrimation.

21

therapeutic use of pilocarpine

glaucoma

22

describe chant and what type of drug it is

nicotinic agonist.
-partial agonist of the alpha2beta4 neuronal nicotinic receptor.
-activates the receptor at sub-threshold levels but prevents binding of nicotine.

23

why does chant work for stopping smoking?

it you give an antagonist, you would get full blown nicotine withdrawal. but since chantix is a partial agonist it has a dual effect: antagonistic and partial agonist.