Kruse Cholinergic Agonists and Antagonists

Question 1

muscarinic receptors activation of what kind of receptor?

Answer 1

G proteins, Gs and Gi,
M2 and M4= Gi
M1, 3, 5= Gs

Question 2

in most end organs what is the muscarinic receptor? what do we normally see when activated

Answer 2

M3, contraction of smooth m.

Question 3

what does M2 cause throughout body? specific found in high concentration in what organ?

Answer 3

also m. contraction; heart

Question 4

how are cholinergic agonists classified? how do they work?

Answer 4

direct-acting (bind to receptors) or indirecting (increase Ach concentration)

Question 5

MOA of direct-acting?

Answer 5

agonists at cholinergic receptors

Question 6

choline esters have what kind of charge? consequence

Answer 6

permanently charged!, poor absorption

Question 7

choinergic esters are broken down by what enzyme?

Answer 7

acetylcholinesterase

Question 8

most choline esters have a greater activity on which AchR?

Answer 8

muscarinic

Question 9

what are the other kinds of cholinergic agonists? charge? consequence?

Answer 9

alkaloids, uncharged tertiary amines, well absorbed

Question 10

what are the 3 groups of AchE inhibitors?

Answer 10

alcohols, carbamic acid esters, organophosphates

Question 11

which AchE inhibitor is irreversible?

Answer 11

organophosphate

Question 12

what dictates the PK of an AchE inhibitor?

Answer 12

chemistry

charged: not lipid soluble, poorly absorbed
neutral: lipid soluble, well absorbed

Question 13

cholinergic agonists have what kind of effect on the body?

Answer 13

parasympathetic effects (even slowing of the heart is not clinically useful from cholinergic agonist= beta blocker instead)

Question 14

what is acetylcholine approved for?

Answer 14

intraocular surgery and causes misosis (reduces pupil size)

Question 15

bethanechol is selective for what receptor? primarily effective where?

Answer 15

mAchR; urinary and GI tracts

Question 16

what is varenicline (chantix)? MOA?

Answer 16

partial agonist for nAchRs, stimulation of moderate, sustained release of mesolimbic dopamine to reduce craving and withdrawal

Question 17

what are the adverse effects of varenicline?

Answer 17

behavior, mood changes, agitation, suicidal ideation, etc.

Question 18

what are the 2 major uses of direct-acting cholinergic agonists?

Answer 18

diseases of the eye

GI/GU disorders

Question 19

what are some of the diseases of the eye direct-acting cholinergic agonists can be used for?

Answer 19

glaucoma

accomodative estropia: misalignment of eyes caused by hypermetropic accomodative error

Question 20

What toxicities do muscarinic stimulation have?

Answer 20

N/V

SLUDGE= salivation, lacrimation, urinary urgency, vasoDilation, GI effects

Question 21

which pt populations have contraindication for muscarinic stimulants?

Answer 21

asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease

Question 22

what are the nicotinic agonists toxicities?

Answer 22

effects on NMJ

Question 23

Cholinergic antagonists have what kind of effect on the body?

Answer 23

sympathetic
pupil dilation, dry mouth, relaxation of bronchi, accelerate heart, GI secretion reduced, constipation, retention of urine

Question 24

antinicotinic drugs work where?

Answer 24

NMJ: skeletal m. relaxants
ganglia: RARELY USED

Question 25

what is the prototype antimuscarinic agent?

Answer 25

atropine

Question 26

what do antimuscarinic agents do?

Answer 26

block effects of parasympathetic autonomic discharge

Question 27

how are antagonists used to help with parkinson dz? drugs?

Answer 27

mAchR antagonists can reduce tremors, not as effective as dopaminergic therapy; tertiary amines benztropine, trihexyphenidol, and one more than i missed, he's going too fast

Question 28

what respiratory disorders can be treated with anticholinergics? drugs?

Answer 28

asthma and COPD; ipratropium and tiotropium (longer dilation effect, once daily)

Question 29

What GI disorders can be treated with anticholinergics?

Answer 29

common traveler's diarrhea and other mild or self-limited conditions of hypermotility

Question 30

lomotil is a combo of what drugs and why?

Answer 30

atropine and diphenoxylate; opoid and anticholinergics- to discourage abuse of drug

Question 31

GU disorders can be treated with drugs selective to what subtype?

Answer 31

M3- present in bladder wall and sphincter smooth m.

Question 32

what is the prototype for GU disorders?

Answer 32

oxybutynin, effects not long enough though

Question 33

what can cause cholinergic poisoning?

Answer 33

cholinesterase inhibitor insecticides, wild mushrooms, chemical warfare nerve gasses

Question 34

what is the treatment for cholinergic poisoning?

Answer 34

atropine (antimuscarinic agents)- reduce mAchR stimulation

Question 35

when is atropine useless?

Answer 35

mushroom posioning

Question 36

what conditions are contraindicated for anticholinergics?

Answer 36

glaucoma, prostatic hyperplasia, acid-peptic disease

Question 37

What flows thru an activating Nn receptor?

Answer 37

Na, K