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CPR II > Cholinergic Agonists and Antagonists- Kruse > Flashcards

Cholinergic Agonists and Antagonists- Kruse Flashcards

1
Q

what is the parasympathetic neurotransmitter

A

Ach

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2
Q

what are the parasympathetic receptors

A

nAchR, mAChR

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3
Q

what are the sympathetic neurotransmitters

A

NE>Epi (DA) and Ach

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4
Q

what are the sympathetic receptors

A

alpha, beta, (D), nAchR, and mAChR

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5
Q

what are the 4 steps that occur at the cholinergic nerve terminal

A

1) ACh synthesis
2) ACh storage
3) ACh release
4) ACh destruction

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6
Q

what are the 4 steps that occur at the adrenergic nerve terminal

A

1) Synthesis
2) Storage
3) Release
4) Reuptake

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7
Q

two molecules that come together to synthesize Ach

A

AcCoA and Choline

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8
Q

Enzyme that synthesizes Ach

A

ChAT

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9
Q

Ach is stored in…

A

a vesicle

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10
Q

what stimulates the Ach vesicle to fuse and release the Ach

A

Ca2+

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11
Q

Ach is destroyed by

A

Acetylcholinesterase

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12
Q

enzyme that synthesizes dopa from tyrosine

is this outside/inside the vesicle

A

tyrosine hydroxylase

outside the vesicle

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13
Q

enzyme that synthesizes dopamine from dopa

is this outside/inside the vesicle

A

aromatic amino acid decarboxylase

outside the vesicle

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14
Q

dopamine is then stored in…

A

a vesicle

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15
Q

dopamine is converted to NE by…

A

dopamine Beta hydroxylase

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16
Q

what stimulates fusion of dopamine/NE vesicle

A

Ca2+

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17
Q

Once the catecholamines bind to receptor they are..

A

taken up again into the pre-synaptic cleft

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18
Q

M1, M3, and M5 are what type of GPCRs

A

Gq/11 that use the IP3, DAG cascade

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19
Q

M2 and M4 are what type of GPCRs

A

Gi/o that inhibit cAMP production

M2 also activates K+ channels

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20
Q

M1 main location?

A

nerves

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21
Q

M2 main locations?

A

heart, nerves, smooth muscle

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22
Q

M3 main locations?

A

glands, smooth muscle, endothelium

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23
Q

M4 and M5 main locations?

A

CNS

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24
Q

In most organs, except heart, which Muscarinic receptor is predominant

A

M3

25
Q

which M receptor is dominant in the heart

A

M2

26
Q

two types of cholinergic agonists are?

A

direct-acting drugs
and
indirect-acting drugs (by inhibiting the action of acetylcholinesterase)

27
Q

what are the 4 direct-acting cholinergic agonists that are uncharged and highly absorbed

A

Muscarine and Pilocarpine (action mainly at muscarinic)

AND

Nicotine and Lobeline (action mainly nicotinic)

28
Q

what are the 4 direct-acting cholinergic agonists that are charged and poorly absorbed

A

Acetylcholine, Methacholine, Carbachol, and Bethanechol

29
Q

What are the 3 groups of AChE inhibitors

A

Alcohols (reversible)

Carbamic acid esters (reversible, but longer lasting than alcohols)

Organophosphates (irreversible)

30
Q

what are the 4 charged and poorly absorbed AChE inhibitors

A

Neostigmine, Carbaryl, Physostigmine, Edrophonium

31
Q

what are the 6 uncharged and highly absorbed AChE inhibitors

A

Echothiophate, Soman, Parathion, Paraoxon, Malathion, Malaoxon

32
Q

what is the treatment if there is toxicity due to the action of direct-acting cholinergic agonists

A

atropine and parenteral anticonvulsants

33
Q

Use of Acetylcholine as a direct-acting agent

A

approved for intraocular use during surgery and causes miosis (reduction in pupil size)

34
Q

Use of Bethanechol as a direct-acting agent

A

primarily affects urinary and GU tracts

35
Q

Use of Carbachol as a direct-acting agent

A

treatment for glaucoma or produce miosis during surgery

36
Q

Use of Cevimeline as a direct-acting agent

A

treats dry mouth (xerostomia) in patients with Sjogren

37
Q

Use of Pilocarpine as a direct-acting agent

A

approved for xerostomia in pts with Sjogren, miosis during surgery, and glaucoma

38
Q

What is the FDA approved drug for smoking cessation

A

Varenicline (Chantix)

39
Q

Varenicline (Chantix) is…

A

a partial agonist that binds with high affinity and selectivity to nAChRs

40
Q

MOA of Varenicline

A

sustained release of dopamine to help with withdrawl symptoms of smoking cessation

41
Q

Adverse effects of Varenicline

A

nausea, neuropsychiatric symptoms

42
Q

clinical uses of indirect-acting cholinergic agonists

A

Glaucoma, Dementia, Antidote to anticholinergic poisoning, Reversal of neuromuscular paralysis, Myasthenia gravis, AChE inhibitor toxicity(SLUDGE symptoms, effects on NMJ)

43
Q

prototype antimuscarinic agent is…

A

atropine

44
Q

drug used for motion sickness

A

scopolamine

45
Q

drugs used for GI disorders

A

atropine, dicyclomine, glycopyrrolate, hyoscyamine

46
Q

drugs used in opthalmology

A

atropine, cyclopentolate, homatropine, scopolamine, tropicamide

47
Q

drugs for respiratory disorders

A

ipratropium, tiotropium

48
Q

drugs for urinary disorders

A

Darifenacin, Oxybutynin, Solifenacin, Toterodine, Trspium

49
Q

Drugs used for cholinergic poisoning

A

atropine and pralidoxime

50
Q

drugs for movement disorders

A

benztropine, biperiden, orphenadrine, procyclidine, trihexyphenidyl

51
Q

Anticholinergics for Parkinson

A

mAChR antagonists can reduce tremors
not as effective as standard dopaminergic therapy

tertiary amines benztropine, trihexyphenidyl, and procyclidine

52
Q

Anticholinergics for motion sickness

A

Scopolamine

53
Q

Anticholinergics for Anesthesia

A

Atropine given to block vagal reflexes induced by manipulation of visceral organs

Atropine or glycopyrrolate paired with cholinesterase inhibitor to block parasympatheitc effects

54
Q

anticholinergics for opthalmologic disorders

A

mAChR used for cycloplegia or prolonged mydriasis is required

alpha adrenergic receptor agonists are shorter acting and have less adverse effects

Homatropine and atropine used to prevent synechia formation in uveitis and iritis (long-acting agents)

55
Q

Anticholinergics for respiratory disorders

A

asthma and COPD will use Ipratrpium and tiotropium; these are inhalation mAChR antagonists

56
Q

Anticholinergics for GI disorders

A

mAChR antagonists treats Traveler’s diarrhea

often combined with opioid antidiarrheal drug to discourage abuse of opioid agent (ex. Lomotil - combo of atropine and diphenoxylate)

57
Q

Anticholinergics for GU disorders

A

mAChR antagonists provide relief in urinary urgency

agents are usually selective of the M3 subtype

Oxybutynin is prototype selective M3 antagonist- has side effects of dry mouth, dizziness, constipation

Darifenacin, Solifenacin, and Tolterodine are also selective for M3- have longer half-lives and reduced incidence of xerostomia and onstipation

58
Q

anticholinergics for cholinergic poisoning

A

atropine given, no effective treatment at nAChR (pralidoxime)

atropine useless in delayed onset mushroom poisoning

59
Q

anticholinergics adverse effects and contraindications

A

glaucoma
prostatic hyperplasia
acid-peptic disease

CPR II (3 decks)

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