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Neuroscience 2 > Kruse Cholinergic Agonists and Antagonists > Flashcards

Kruse Cholinergic Agonists and Antagonists Flashcards

1
Q

muscarinic receptors activation of what kind of receptor?

A

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

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2
Q

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

A

M3, contraction of smooth m.

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3
Q

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

A

also m. contraction; heart

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4
Q

how are cholinergic agonists classified? how do they work?

A

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

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5
Q

MOA of direct-acting?

A

agonists at cholinergic receptors

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6
Q

choline esters have what kind of charge? consequence

A

permanently charged!, poor absorption

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7
Q

choinergic esters are broken down by what enzyme?

A

acetylcholinesterase

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8
Q

most choline esters have a greater activity on which AchR?

A

muscarinic

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9
Q

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

A

alkaloids, uncharged tertiary amines, well absorbed

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10
Q

what are the 3 groups of AchE inhibitors?

A

alcohols, carbamic acid esters, organophosphates

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11
Q

which AchE inhibitor is irreversible?

A

organophosphate

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12
Q

what dictates the PK of an AchE inhibitor?

A

chemistry

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

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13
Q

cholinergic agonists have what kind of effect on the body?

A

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

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14
Q

what is acetylcholine approved for?

A

intraocular surgery and causes misosis (reduces pupil size)

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15
Q

bethanechol is selective for what receptor? primarily effective where?

A

mAchR; urinary and GI tracts

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16
Q

what is varenicline (chantix)? MOA?

A

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

17
Q

what are the adverse effects of varenicline?

A

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

18
Q

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

A

diseases of the eye

GI/GU disorders

19
Q

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

A

glaucoma

accomodative estropia: misalignment of eyes caused by hypermetropic accomodative error

20
Q

What toxicities do muscarinic stimulation have?

A

N/V

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

21
Q

which pt populations have contraindication for muscarinic stimulants?

A

asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease

22
Q

what are the nicotinic agonists toxicities?

A

effects on NMJ

23
Q

Cholinergic antagonists have what kind of effect on the body?

A

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

24
Q

antinicotinic drugs work where?

A

NMJ: skeletal m. relaxants
ganglia: RARELY USED

25
Q

what is the prototype antimuscarinic agent?

A

atropine

26
Q

what do antimuscarinic agents do?

A

block effects of parasympathetic autonomic discharge

27
Q

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

A

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

28
Q

what respiratory disorders can be treated with anticholinergics? drugs?

A

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

29
Q

What GI disorders can be treated with anticholinergics?

A

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

30
Q

lomotil is a combo of what drugs and why?

A

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

31
Q

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

A

M3- present in bladder wall and sphincter smooth m.

32
Q

what is the prototype for GU disorders?

A

oxybutynin, effects not long enough though

33
Q

what can cause cholinergic poisoning?

A

cholinesterase inhibitor insecticides, wild mushrooms, chemical warfare nerve gasses

34
Q

what is the treatment for cholinergic poisoning?

A

atropine (antimuscarinic agents)- reduce mAchR stimulation

35
Q

when is atropine useless?

A

mushroom posioning

36
Q

what conditions are contraindicated for anticholinergics?

A

glaucoma, prostatic hyperplasia, acid-peptic disease

37
Q

What flows thru an activating Nn receptor?

A

Na, K

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