Lecture 3 Muscarinic Agonists

Question 1

Diabetic neuropathy mechanisms:

1. ____ insult to nerve fibers
2. _____ insufficiency
3. _____ damage
4. _____ ____ factor defeciency

Answer 1

metabolic
neurovascular
auto-immune
neurohumoral growth

Question 2

Most important form of autonomic neuropathy? Increased risk of what?

Answer 2

cardiovascular;

“silent” ischemia aka painless ischemia

Question 3

_____ from excess alcohol is toxic to nerves. Chronic alcohol use can also cause _____, which further preciptates autonomic dysfunction

Answer 3

acetaldehyde;

chronic liver disease

Question 4

Advanced chronic liver disease patients will suffer from peripheral _____ ____ and increased plasma levels of ____. Patients often present with _____ ____

Answer 4

arterial vasodilation;
catecholamines;

orthostatic hypotension

Question 5

botulinim toxin interacts with ____ proteins, preventing vesicle ____ release

Answer 5

SNARE; ACh

Question 6

Graves disease: increased secretion of T3 and T4 causes an increase in ______ _____ expression. This can cause ______ heartbeat and _____cardia. Treatment should be _____, which prevents conversion of T4–>T3. Muscarinic agonists are contra-indicated due to increased risk of _____

Answer 6

beta adrenergic;
irregular, tachy;
beta blockers;
Atrial fib

Question 7

Reduced body weight/stress causes ______ to be released by the adrenal gland. This inhibits formation of ___. This causes a ____ of Sympathetic activation and a _____ of parasympathetic activation

Answer 7

glucocorticoids; T3

decrease; increase

Question 8

Elevated body weight causes an ____ in T3 and a ____ in sympathetic nervous system activation

Answer 8

increase; increase

Question 9

desensitization of the adrenergic system can exacerbate ______thyroidism. Sensitization of the adrenergic system can exacerbate _____thyroidism

Answer 9

hypo, hyper

Question 10

treatment of hypothyroidism is typically with ____, rather than symptomatic treatment with ____ agonists.

Answer 10

hormones;

muscarinic

Question 11

why isn’t clinical use of muscarine recommended?

Answer 11

can cross the BBB and cause convulsions

Question 12

ACh, carbachol, methacholine, and bethanechol have a _____ ammonium and thus have limited ____ distribution and ___ absorption

Answer 12

quarternary;
CNS, GI

typically given GI or IM

Question 13

What 2 muscarinic agonists are hydrolyzed quickly by AchE? Which three can bind to nicotinic receptors as well?

Answer 13

Ach, methacholine;

Ach, carbachol, methacholine

Question 14

Hydrolysis by AchE means the drug is ___ acting. nAchR activity increases the risk of fatal _____ weakness

Answer 14

short;

muscle

Question 15

____ is used to diagnose bronchial hyperactivity and COPD due to its short action. Patients with COPD will show signs of respiaratory insufficiency at a ____ dose than healthy individuals

Answer 15

methacholine;

lower

Question 16

____ angle glaucoma is due a clogged or obstructed canal of schlemm. This is a ____ progressing disease

Answer 16

open; slowly

Question 17

___ angle glaucoma is due to drainage blocked by the iris muscles or lens, blocking the trabecular meshwork This is a ____ progressing disease

Answer 17

closed/narrow; rapidly

MEDICAL EMERGENCY

Question 18

Open angle treatment: M3 muscarinic agonist mechanism of action:

Narrow angle treatment: M3 muscarinic agonist mechanism of action:
(what is the normal treatment?)

Answer 18

Open: stretch trabecular meshwork by contracting ciliary body–>reduce clogging

Closed: contracts sphincter muscles->
usually laser iridotomy

Question 19

muscarinic agonists used for treatment of glaucoma:
____ is shorter acting, is a partial agonist, = ____ side effects

_____ has a longer duration

which can cross the BBB?

Answer 19

pilocarpine; less

carbachol

pilocarpine can cross BBB (seizure risk)

Question 20

Uses of bethanechol: 2

It is ____ selective

Answer 20

urinary retention, post-operative illeus

muscarinic

Question 21

2 drugs used for xerostomia (ie Sjogren’s or head/neck irradiation)

Answer 21

cevimeline, pilocarpine

Question 22

2 NAChR agonists used for smoking cessation:

which is a full and which is a partial agonist?

Answer 22

nicotine (full), varenicline (partial–>blocks nicotine from binding)

Question 23

contraindication of nicotine? due to increased ____ and ____

Answer 23

cardiovascular disease;

blood pressure, heart rate