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PHRM 825 > ANS-3 > Flashcards

ANS-3 Flashcards

Cholinergic Agents 1/12/23

1
Q

parasympathomimetic (agonist) actions: Direct agonist

A

activates cholinoceptors by binding directly to them

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2
Q

parasympathomimetic (agonist) actions: Indirect agonist

A

binds to and inhibits acetylcholinesterase (AChE), Stimulates ACh release

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3
Q

ACh has a higher affinity for which receptor (M or N)

A

muscarinic receptors

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4
Q

Mnemonic to remember M1, M2, M3 GPCR action

A

qiq, M1 = Gq, M2 = Gi, M3 = Gq

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5
Q

M1 tissue and response

A

postganglionic, depolarization

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6
Q

M2 tissue and response

A

Heart, inhibition

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7
Q

M3 tissue and response

A

smooth muscles, exocrine glands, endothelium,

contraction, secretion, relaxation

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8
Q

M4 tissue and response

A

CNS, hyperpolarization (Gi)

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9
Q

M5 tissue and response

A

CNS, depolarization (Gq)

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10
Q

Nm tissue and response

A

skeletal muscle, motor end plate depolarization/contraction

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11
Q

Nn tissue and response

A

postganglionic, depolarization

adrenal medulla, catecholamine secretion

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12
Q

ACh Biosynthesis: Step 1 - ______ is transported into the presynaptic nerve terminal by a ___________

A

Choline, Sodium-dependent choline transporter (CHT)

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13
Q

The sodium-dependent choline transporter (CHT) can be inhibited by _________, which has no current clinical use

A

hemicholinium

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14
Q

ACh Biosynthesis: Step 2 - ACh is synthesized from ______ and ______ by the enzyme _________

A

choline, acetyl-CoA, choline acetyltransferase (ChAT)

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15
Q

ACh Biosynthesis: Step 3 - ACh is then transported into the _______ by a second carrier, the ________

A

storage vesicle, vesicle-associated transporter (VAT)

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16
Q

The vesicle-associated transporter (VAT) is inhibited by ______, which has no current clinical use

A

vesamicol

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17
Q

ACh Biosynthesis: Step 4 - Release of transmitter occurs when an ___1____ opens ____2____ and increases the intracellular ____3____. Fusion of vesicles with the ___4____ results in release of ___5___.

A

1 - action potential
2 - voltage sensitive calcium channels
3 - calcium
4 - surface membrane
5 - ACh

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18
Q

The release of ACh caused by and influx of Ca2+ and the vesicle merging with the surface membrane (Step 4) can be blocked by ________

A

botulinum toxin (botox)

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19
Q

ACh Biosynthesis: Step 5 - after release, ACh binds to ______ receptors on the ______ cell

A

cholinoceptors, postsynaptic

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20
Q

ACh Biosynthesis: Step 6 - The action of ACh is terminated through its metabolism by the enzyme ______

A

acetylcholinesterase (AChE)

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21
Q

ACh Biosynthesis: Step 7 - _____ and receptors on the presynaptic nerve ending modulate _______

A

autoreceptors, transmitter release

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22
Q

What are muscarinic receptors named after?

A

mushroom: Amanita Muscaria

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23
Q

Muscarinic Agonists: PSNS Symptoms of “Fast” Mushroom Poisoning

A

Bradycardia (M2)
nausea, cramps, vomiting, diarrhea (M3)
Bronchoconstriction (M3)
Salivation (M3)
Visual disturbances (M1)

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24
Q

Muscarinic Agonists: SNS Symptoms of “Fast” Mushroom Poisoning

A

Sweating (M3)

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25
Q

Muscarinic Agonists: Uninnervated Symptoms of “Fast” Mushroom Poisoning

A

Hypotension (caused by uninnervated muscarinic receptors in the blood vessel endothelium cells mediating vasodilation via NO)

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26
Q

Cholinergic Agonists Classification: Direct Acting - Choline Esters

A

ACh, Methacholine, Carbachol, Bethanechol

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27
Q

Cholinergic Agonists Classification: Direct Acting - Alkaloids

A

Muscarine and Pilocarpine

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28
Q

Cholinergic Agonists Classification: Indirect Acting - Reversible

A

Edrophonium, Physostigmine, Neostigmine

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29
Q

Cholinergic Agonists Classification: Indirect Acting - Irreversible

A

Organophosphates

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30
Q

Muscarinic Agonist Effects: Heart

A

Bradycardia - M2 activation leads to decrease in HR, conduction, and force

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31
Q

Muscarinic Agonist Effects: Exocrine Glands

A

M3 activation increases secretion in:
Lachrymal, Tracheobronchial, Salivary, Digestive, Sweat glands

32
Q

Muscarinic Agonist Effects: Smooth Muscles

A

M3 activation increases contraction (M2 inhibits relaxation)

33
Q

Muscarinic Agonist Effects: Sphincters

A

M3 activation causes relaxation

34
Q

Muscarinic Agonists Effects: CNS

A

Mediated by M1:
tremor, hypothermia, increased locomotor activity, improved cognition

*not all muscarinic agonists are able to access CNS (charged)

35
Q

What is this?

A

ACh (also called Miochol)

36
Q

What is this?

A

Methacholine (Provocholine)

37
Q

What is this?

A

Carbachol (Isoptocarbachol)

38
Q

What is this?

A

Bethanechol (Urecholine)

39
Q

What is this?

A

Muscarine

40
Q

Why are cholinergic agonists that have carbamate longer lasting?

A

AChE breaks down ACh fast, so if we replace it CH3 with NH2, the esterase won’t recognizes/break it down as fast.

41
Q

What is this?

A

Pilocarpine (Isoptocarpine)

42
Q

What is this?

A

(+)-Muscarine

43
Q

What is this?

A

(+)-Methacholine

44
Q

What is this?

A

(-)-Methacholine

45
Q

What is this?

A

Pilocarpine

46
Q

Why are antimuscarinic drugs contraindicated in glaucoma?

A

M3 receptor on ciliary muscle opens drainage. If we block this, pressure will build up making glaucoma worse

47
Q

Stereochemistry of cholinergic drugs need to have _____ orientation in able to function

A

positive (+)

48
Q

Jaborandi meaning

A

“what causes slobbering”

49
Q

Pilocarpus jaborandi was used by Brazilian tribes as an antidote to various toxins because of its availability to promote _______, _______, and _______

A

sweating, urination, salivation

50
Q

T or F: Pilocarpine can cross the BBB

A

True, no positive charge

51
Q

rank transmitters most to least susceptible to AChE

A

ACh, Methacholine, Carbachol, Bethanechol = Pilocarpine

52
Q

Clinical use of Pilocaprine

A

open-angle glaucoma, dry mouth (Sjogren’s or cancer radiotherapy)

53
Q

Clinical use of Bethanechol

A

GI stimulation or treatment of urinary retention

54
Q

Clinical use of Methacholine

A

Provocative test for hyperactive airways

55
Q

Clinical use of Carbachol

A

ocular (surgery, glaucoma)

56
Q

Muscarinic Receptor Agonists PSNS Side Effects: DUMBBELS(S)

A

Diarrhea, Urination, Miosis, Bradycardia, Bronchoconstriction, Emesis, Lacrimation, Salivation, Sweating (SNS effect)

57
Q

Muscarinic Receptor Agonists should be used with caution in patients with what?

A

asthma, coronary insufficiency, or peptic ulcers

58
Q

Nicotinic Agonist Response

A

Opening ligand gated Na+ channels = depolarization

Leads to opening of voltage gated Na+ channels to produce action potential

59
Q

Where are nicotinic receptors located?

A

Nm - skeletal muscle endplate (somatic)

Nn/g (ANS)- autonomic ganglia (both SNS and PSNS ganglia)

Nn (CNS) - brain

60
Q

T or F: Nicotinic receptors are less stereoselective

A

True

61
Q

T or F: Nicotine is dibasic

A

True; pka = 6.16 and 10.96

62
Q

Effects of low dose nicotine

A

stimulates alertness and dopamine release (addictive)

63
Q

Effects of high dose nicotine

A

CV effects (hypertension, tachycardia)

64
Q

Toxic effects of nicotine

A

seizures, neuromuscular blockade, and loss of receptor selectivity which causes: brochorrhea, excessive secretions, GI disturbance (nausea and vomiting)

65
Q

Acute nicotine toxicity effects

A

convulsion, coma, hypertension, arrhythmias, neuromuscular failure

66
Q

Nicotine withdrawal symptoms

A

irritability, anxiety, dysphoria, difficulty concentrating, restlessness, decreased HR, increased appetite

67
Q

Varenicline (Chantix) is a _____ neuronal nicotinic receptor ______ that binds in the _____.

A

a4B2, partial agonist, CNS

68
Q

Varenicline (Chantix) produces low to moderate release of ________ at reward centers in brain,
mimicking nicotine’s effect and reducing ______ symptoms

A

Dopamine, withdrawal

69
Q

Varenicline (Chantix) blocks the binding of _____ and therefore the _________ obtained through smoking

A

nicotine, positive reinforcement

70
Q

Half-life of Varenicline (Chantix)

A

24 hr

71
Q

Adverse effects of Varenicline (Chantix)

A

Nausea, headache, abnormal dreams, constipation, vomiting

72
Q

Varenicline (Chantix) is more effective than ______ and ____, may be more effective than _______

A

nicotine patch, gum, bupropion

73
Q

What is this?

A

Varenicline (Chantix)

74
Q

Bupropion (Wellbutrin) weakly inhibits ____ and ____ resulting in increased levels of ____ and ____ in the synaptic cleft

A

NET, DAT, NE, DA

75
Q

What is this?

A

Bupropion (Wellbutrin)

76
Q

Clinical use of Bupropion (Wellbutrin)

A

depression, smoking cessation

77
Q

Problems with Bupropion (Wellbutrin)

A

effect delayed by a few weeks, lowers seizure threshold (high doses), and potential for hypertensive crisis with MAOIs

PHRM 825 (49 decks)

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