cholinergic

Question 1

cholinergic

Answer 1

any system affected by/involving ACh

Question 2

M3

Answer 2

secretory
any muscle contraction
circulatory muscles in eye

Question 3

M2

Answer 3

cardiac
decrease heart rate
slows SA node and slows down AV node

Question 4

M1

Answer 4

cholinergic pathways
affected in Alheimerz
circuits involved in memory and cognition

Question 5

Muscarinic agonist

Answer 5

activate all
increase SLUD
decrease HR
bronchoconstriction

Question 6

what would a muscarinic agonist be useful in treating

Answer 6

tachycardia
dry mouth
constipation
glaucoma

Question 7

muscarinic antagonist

Answer 7

decrease SLUD

increase HR

Question 8

muscarinic antagonist would be effective in treating

Answer 8

urinary urgency
eye surgery
IBS-D type

Question 9

nicotinic receptors

Answer 9

Na+ gated ion channels

Question 10

Nicotinic receptor types

Answer 10

Ng = autonomic ganglia = para or symp
Nm = neuromuscular = some selective nicotinic

Question 11

AChE

Answer 11

acetylcholinesterase
wherever ACh is released this enzyme is present
highest turnover rate of all enzymes

Question 12

lack of AChE =

Answer 12

slower metabolism of ACh
increase SLUD
decrease HR
increase in cholinergic activity of the brain

Question 13

ACh

Answer 13

made from ACh and choline
choline on its own would be broken down by cholinesterases => ACh is less resistant and will not be broken down as quickly

Question 14

muscarinic receptors are _____ and nicotinic receptors are ____

Answer 14

gpcr

Na+ gated ion channels

Question 15

hemicholiniums

Answer 15

block the transporter bring choline into the cell = result would be less formation of ACh

Question 16

Vesamicol

Answer 16

inhibits VAT that puts ACh into the vesicle to prepare for its release

Question 17

Botulinum toxin

Answer 17

prevents the release of the ACh vesicles

Question 18

two mechanisms that block the release of ACh on the presynaptic ganglia

Answer 18

heteroreceptor = alpha 2
ACh autoreceptor = N2
when both are activated = decrease in ACh release

Question 19

AChE is found on the post synaptic neuron awaiting binding for rapid hydrolysis, but ACh can also be broken down by

Answer 19

plasma esterases such as butyrylcholinesterase (BuChE)

Question 20

Muscarinic receptors:
odd numbers =
even numbers =

Answer 20

Gq / excitatory

Gi / inhibitory

Question 21

M1 function

Answer 21

increase cognitive function
seizure activity
increase secretions
increase autonomic ganglia depolarization
decrease DA release and locomotion

Question 22

M2 function

Answer 22

autonomic nerve terminals / heart
decrease heart rate
increase smooth muscle contractions
decrease ganglionic transmission
neural inhibition in CNS
increase tremors, hypothermia, analgesia

Question 23

M3 function

Answer 23

CNS, smooth muscle
smooth muscle contraction
increase salivary glands
increase food intae
body fat deposits
inhibition of DA release
synthesis of NO

Question 24

treat parkinsons using

Answer 24

an M1 antagonist

Question 25

treat Alzheimers using

Answer 25

an M1 agonists

Question 26

structure requirements for an muscarinic agonist

Answer 26

1) ammonium group - want N to be capable of bearing a positive charge 2) Ethylene bridge - 2 C atoms between N and O; Ings Rule of 5 - start at nitrogen to terminal H; no more than 5 atoms 3) acyloxy group - ester, ether, ketone; must be O atom

Question 27

The B carbon works on agonist by

Answer 27

increasing affinity for Muscarinic over nicotinic

Question 28

carbamate

Answer 28

slows hydrolysis by ACh

Question 29

if your patient had an obstruction (bladder or GI)

Answer 29

do not use an agonist

Question 30

functions of muscarinic agonists

Answer 30

non - obstructive urinary retention disabling anticholinergic side effect from medications like tricyclic antidepressants bronchial airway hyper-reactivity in subjects who do not have asthma lowering of intraoccular pressure in glaucoma miosis induction after ophthalmoscopic exmination xerostomia caused by radiation therapy for cancer of the head and neck

Question 31

when would you not give a muscarinic agonist

Answer 31

IBS-d asthma - airways would close severe bradycardia - slow down HR

Question 32

SAR requirments for muscarinic antagonists

Answer 32

1) N is tertiary or quaternary ammonium 2) R1 and R2 are carbocyclic or heterocyclic rings 3) R3 is generally a H, OH, or part of the ring systems 4) X is usually an ester or even a C atom 5) length is usually 2 to 4 atoms

Question 33

Muscarinic antagonists (antimuscarinics)

Answer 33

``` COPD Parkinsons Overactive bladder Mydriatics/Cycloplegics IBS-D ```

Question 34

antimuscarinics ADR?

Answer 34

``` dry mouth dry eyes blurred vision dry skin increase HR hallucinations delirium limit CNS effects = if ionized ```

Question 35

ophthalmic

Answer 35

used to dilate pupils paralyze the lens for procedures loss of accommodation

Question 36

relaxation of sphincter of the iris =

Answer 36

midrasis = dialation

Question 37

relaxation of ciliary muscle of the iris

Answer 37

change lens thickness unable to accommodate blurred vision

Question 38

COPD drugs

Answer 38

ipratropium umeclidium glycopyrrolate aclidium

Question 39

parkinsons drugs

Answer 39

benztropine | trihexyphenydil

Question 40

IBS drugs

Answer 40

dicyclomine

Question 41

Nausea due to motion sickness drugs

Answer 41

scopolamine