Lecture 9: Anticholinergic Agents

Question 1

what is the primary NT of the parasympathetic nervous system?

Answer 1

Ach

Question 2

what are the target tissue receptors of the parasympathetic nervous system?

Answer 2

muscarinic receptors

Question 3

which muscarinic receptors are most often modified pharmacologically

Answer 3

M2 and M3

Question 4

muscarinic antagonists cause the opposite of ____

Answer 4

SLUDGE

Question 5

muscarionc antagonists cause what 2 changes in the eye?

Answer 5

pupil dilation; transient increase in IOP

Question 6

heart rate can be decreased slightly during parasympathetic activation, but returns to normal quite quickly due to other ____ of the cardiovascular system

Answer 6

other compensatory mechanisms

Question 7

in the lungs, blocking the actions of Ach promotes ____ which is a beneficial effect in asthma and COPD

Answer 7

bronchodilation

Question 8

muscarinic receptor antagonists are typically called ____ agents

Answer 8

anticholinergic

Question 9

what is the prototypic example of anticholinergic agent?

Answer 9

atropine

Question 10

what are 3 beneficial applications of anticholinergic agents?

Answer 10

asthma, COPD, motion sickness

Question 11

atropine can still be used today to treat____

Answer 11

cholinergic poisoning by pesticides and nerve gases

Question 12

inverse agonists stabilize the ___ form of a receptor

Answer 12

inactive

Question 13

neutral antagonists show no ___ and cause no change in ____

Answer 13

binding preference; basal activity

Question 14

some anticholinergic agents, such as ___ have been determined to be inverse agonists of muscarinic receptors

Answer 14

atropine

Question 15

we may expect that the effects of an inverse agonist of muscarinic receptors to be ____ than those of another anticholinergic antagonists

Answer 15

greater

Question 16

what properties may cause the effects of inverse agonist to NOT be greater than those of anticholinergic antagonists?

Answer 16

level of constitutive receptor activity, the drug’s receptor affinity and concentrations reaching the target

Question 17

is it clear whether inverse agonists have a clinical advantage over neutral antagonists?

Answer 17

no

Question 18

for most therapeutic considerations, we can generalize that anticholinergic agents are ____ competitive muscarinic antagonists

Answer 18

non-selective

Question 19

should anticholinergic agents be used locally or systemically?

Answer 19

locally

Question 20

the use of anticholinergic agents in the treatment of asthma is achieved by delivering them in what manner?

Answer 20

inhaled

Question 21

____ is an example of inhaled muscarinic antagonists

Answer 21

tiotropium

Question 22

the quaternary amine of tiotropium causes the drug to be ___

Answer 22

charged

Question 23

charged molecules do not cross the membrane easily, so when tiotropium is inhaled, it remains in the ___ where it acts without having too many adverse systemic effects

Answer 23

lungs

Question 24

if large quantities of tiotropium are swallowed instead of inhaled we might expect to see anticholinergic effects in the ____ as we’ll

Answer 24

GI system

Question 25

along with bronchodilation, anticholinergics also do what to contribute to clearing airways?

Answer 25

decreased mucus secretions

Question 26

the use of anticholinergic agents in the treatment of asthma is achieved by delivering them in what manner?

Answer 26

inhaled

Question 27

tropic amide eyedrops have a ____ duration and are often used for what procedure?

Answer 27

short; eye examinations

Question 28

the quaternary amine of tiotropium causes the drug to be ___

Answer 28

charged

Question 29

charged molecules do not cross the membrane easily, so when tiotropium is inhaled, it remains in the ___ where it acts without having too many adverse systemic effects

Answer 29

lungs

Question 30

if large quantities of tiotropium are swallowed instead of inhaled we might expect to see anticholinergic effects in the ____ as we’ll

Answer 30

GI system

Question 31

along with bronchodilation, anticholinergics also do what to contribute to clearing airways?

Answer 31

decreased mucus secretions

Question 32

tropic amid eyedrops are an example of a ___ drug

Answer 32

anticholinergic

Question 33

why re tropic amide eyedrops used in eye exams?

Answer 33

they dilate pupil, allowing more light to enter for improved examination of the retina and its vasculature

Question 34

t/f because scopolamine is used systemically, it can have unintended effects, but when used for short durations, these effects can be tolerable

Answer 34

true

Question 35

what is scopolamine?

Answer 35

tertiary amine muscarinic receptor antagonist

Question 36

what form is scopolamine available as?

Answer 36

transdermal patch

Question 37

scopolamine is absorbed ____ (locally or systemically)

Answer 37

systemically

Question 38

the anticholinergic activity of diphenhydramine and dimenhydramine can effectively reduce ___ but also causes anticholinergic and antihistamine effects in other systems: ___, ____, ___ and ___ may occur in some patients

Answer 38

nausea; sedation, dry mouth, ataxia and confusion

Question 39

t/f because scopolamine is used systemically, it can have unintended effects, but when used for short durations, these effects can be tolerable

Answer 39

true

Question 40

one example of a commonly used drug having off-target anticholinergic effects are the first generation antihistamines such as ___

Answer 40

diphenhydramine

Question 41

gravol; or the generic name dimenhydrinate is a combination of ____ and ___

Answer 41

diphenhydramine and a stimulant – chlorotheophylline

Question 42

first generation antihistamines are notorious for having ___ effects, thus the addition of stimulant makes it less sedative than diphenhydramine itself

Answer 42

sedative

Question 43

the anticholinergic activity of diphenhydramine and dimenhydramine can effectively reduce ___ but also causes anticholinergic and antihistamine effects in other systems: ___, ____, ___ and ___ may occur in some patients

Answer 43

nausea; sedation, dry mouth, ataxia and confusion

Question 44

drugs that act on multiple receptors are often called ___- drugs

Answer 44

dirty