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Pharmacology > Drugs Affecting Cholinergic Neurotransmission > Flashcards

Drugs Affecting Cholinergic Neurotransmission Flashcards

1
Q

Which amino acid can be converted to make ACh?

A

serine

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2
Q

Which 3 amino acids are involved in ACh metabolism?

A

Glu, His, Ser

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3
Q

Muscarinic receptor

A

identified by the ability of the natural product muscadine to bind to the receptor
7 transmembrane domains, 5 subtypes
all are GPCR
important in drug therapy

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4
Q

Nicotinic Receptor

A

identified by the ability of the natural product nicotine to bind to the receptor

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5
Q

Which 3 amino acids are involved in muscarinic receptor domains?

A

Asp, Thr, Tyr

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6
Q

General effects of muscarinic receptor activation

A

Diarrhea/Defecation
Urination
Miosis/ Constriction of pupil
Bradycardia (slow heart rate)
Bronchonconstriction
Excitation of CNS
Lacrimation
Salivation
Sweating
Abdominal Cramps/GI contraction

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7
Q

M1

A

PLC activation (increased IP3, DAG, Calcium, and PKC)
increase congnitive function and secretions
decrease dopamine release and locomotion

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8
Q

M3

A

PLC activation (increased IP3, DAG, Calcium, and PKC)
increased smooth muscle contraction and salivary gland secretion

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9
Q

M5

A

PLC activation (increased IP3, DAG, Calcium, and PKC)
facilitates dopamine release; augments drug seeking behavior and reward

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10
Q

M2

A

Inhibition of adenylyl cyclades and voltage gated calcium channels
decreased heart rate
increased smooth muscle contraction

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11
Q

M4

A

Inhibition of adenylyl cyclades and voltage gated calcium channels
facilitates dopamine release, inhibits transmitter release in the CNS

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12
Q

Which receptors activate phospholipase C

A

odd numbered/ G alpha Q

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13
Q

Which receptors are inhibitory and decrease cAMP

A

Gi/even numbered receptors

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14
Q

Which receptors decrease voltage gated calcium channels?

A

Go / even numbered receptors

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15
Q

What are the issues with using ACh as a drug?

A

non-selective
minimal bioavailability

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16
Q

The positive nitrogen on ACh and muscarine is good for forming ionic bonds with receptors but poor for ?

A

absorption

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17
Q

Methacholine

A

used for diagnostic tests
selective for muscarinic vs nicotinic receptors
equipotent with ACh but decreased rate of hydrolysis

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18
Q

Carbachol

A

isosteric change to ACH
carbamate is not as easily hydrolyzed as an ester
used in ophthalmics

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19
Q

Bethanechol

A

has carbamate and methyl group added on to ACh
used orally for urinary retention

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20
Q

Pilocarpine

A

act as muscarinic agonist
natural alkaloid
used opthalmically and orally for dry mouth

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21
Q

Cevimeline

A

synthetic muscarinic agonist
used orally for dry mouth

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22
Q

Alzheimer’s disease

A

ACh deficiency; progressive degeneration of cholinergic neurons

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23
Q

AChE inhibitors

A

indirect ACh agonists
will produce a non specific response
useful for glaucoma treatment- miosis, myasthenia gravis- incr ACh duration of action, Alzheimer’s- slow decline of memory, and to reverse mydriasis or effects of nondepolarizing neuromuscular blocking agents

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24
Q

Myasthenia gravis

A

chronic autoimmune neuromuscular disorder
fluctuation weakness of voluntary muscle groups

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25
Q

In pseudoirreversible inhibitors a carbamate is left on a Ser, what is the speed of hydrolysis ?

A

slow

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26
Q

Aryl Carbamates

A

have increased affinity for AChE, making them better inhibitors
includes physostigmine, neostigmine, pyridostigmine, and rivastigmine

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27
Q

Order of rate of carbamylation of AChE

A

carbamic acid esters>methylcarbamic acid esters>dimethylcarbamic acid esters> methyl, ethyl

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28
Q

Neostigmine and pyridostigmine treat

A

myasthenia gravis

29
Q

physostigmine treats

A

open-angle glaucoma

30
Q

rivastigmine treats

A

alzheimer’s

31
Q

Donepezil, Galantamine, and Ambenonium Chloride are?

A

Non-carbamoylating AChE inhibitors

32
Q

Can quarternary salts cross the blood brain barrier?

A

no

33
Q

A slower carbamylation leads to slower?

A

regeneration of AChE

34
Q

Carbamylating agents may lead to ?

A

increased cholinergic effects

35
Q

Irreversible AChE inhibitors

A

used in as low of a dose as possible
used in a lot of insecticides

36
Q

Symptoms of Organophosphate toxicity

A

increased GI peristalsis
miosis, loss of ocular accomodation, ocular pain
rhinorrhea
chest tightness and wheezing
increased lacrimation, salivation, and sweating
bradycardia and hypotension
confusion
convulsions
weakness, muscle paralysis, respiratory paralysis

37
Q

What combination can reverse anti-AChE toxicities ?

A

atropine and pralidoxime

38
Q

Pralidoxime Chloride

A

antidote to reverse muscle paralysis resulting from organophosphate AChE peticide poisoning

it’s oxime has a higher affinity for phosphate as opposed to a hydroxyl group

39
Q

Muscarinic receptor antagonists block?

A

muscarinic actions of ACh
DUMBELLS

40
Q

What are the 3 main stimulators of gastric acid release?

A

ACh, histamine, and gastrin

41
Q

What are the first line drugs for treatment of COPD?

A

ipratropium and tiotropium

42
Q

Alkaloid

A

nitrogen containing compound that is isolated from natural sources and possesses a pharmacological action

43
Q

Ing’s Rule of 5

A

5-6: Agonist
7-8: Partial Agonist
>9: Antagonist

44
Q

When an active site is occupied and the auxiliary site is not used, then the receptor exists in a conformation that produces an?

A

agonist effect

45
Q

When both active and auxiliary sets are occupied what kind of effect is produced?

A

Antagonist effect

46
Q

Ipratropium, Tiotropium, and Aclidinium Bromide are all?

A

Bronchodilators
quaternary ammonium anticholinergic agents

47
Q

ACh action at M1 and M3 receptors causes bronchoxxx?

A

bronchoconstriction

48
Q

Amino Alcohol Esters (Synthetic Antimuscarinic Drugs)

A

glyopyrroolate, propantheline, flavoxate, dicyclomine, cyclopentolate, and mepenzolate bromide

49
Q

Amino Ethers (Synthetic Antimuscarinic Drugs)

A

diphenhydramine, bentropine, and orphenadrine

50
Q

Amino Alcohols (Synthetic Antimuscarinic Drugs)

A

procyclidine, trihexyphenidyl, biperiden

51
Q

Tropicamide and Tolterodine are ?

A

Synthetic Antimuscarinic Drugs

52
Q

All synthetic anti muscarinic drugs are selective for?

A

the muscarine receptor

53
Q

Where are nicotinic receptors located?

A

sympathetic and parasympathetic ganglia

54
Q

How many ACh binding site are on the extracellular domain of each receptor molecule?

A

2

55
Q

What kind of antagonists are nicotinic antagonists?

A

competitive

56
Q

How can you reverse nicotinic antagonists ?

A

by administering an AChE inhibitor

57
Q

Skeletal Neuromuscular Blocking Agent

A

used in anesthesia
nicotinic antagonist

58
Q

Ganglion is blocking agents

A

orphan drug for treatment of nicotine- responsive psychiatric disorders and nicotine and codein addiction

nicotinic antagonist

59
Q

What structural features do synthetic neuromuscular blocking drugs need

A

2 quaternary ammonium groups/ tertiary amines spread 10-12 atoms apart

60
Q

Succinylcholine Chloride

A

ultrashort duration; depolarizing
cannot be reversed by neostigmine
used for rapid induction of muscle relaxation
administered IV

61
Q

Pancuronium Bromide

A

Long duration; competitive
don’t use in patients with CAD

62
Q

Vecuronium Bromide

A

intermediate duration; competitive

63
Q

Rocuronium Bromide

A

intermediate duration; competitive

64
Q

Atacurium Besylate

A

intermediate duration; competitive
depends on renal elimination

65
Q

Mivacurium Chloride

A

Short duration; competitive

66
Q

Pancuronium Bromide, Vecuronium Bromide, and Rocuronium Bromide are all?

A

steroid based blocking drugs

67
Q

Atacurium Beslyate and Mivacurium Chloride are ?

A

tetrahydroisoquinoline based blocking drugs

68
Q

Adverse effects of neuromuscular blockers

A

hypotension, bronchospasm, cardiac disturbances, twitching before relaxation, histamine release

Pharmacology (16 decks)

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