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Autonomics > Dr. Proteau's Musc Ag/Antag Notes > Flashcards

Dr. Proteau's Musc Ag/Antag Notes Flashcards

1
Q

which stereochemical formation of ACh has the lowest energy in solution?

A

Synclinal

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2
Q

which stereochemical formation of ACh is most favored with nicotinic receptors?

A

Antiplanar

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3
Q

which stereochemical formation of ACh is most favored with muscarinic receptors?

A

Anticlinal

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4
Q

which stereochemical formation of ACh has the highest energy?

A

Synplanar

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5
Q

The use of Ach is limited to being directly injected into the eye to cause?

A

myosis in surgery (constriction)

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6
Q

what does the addition of the cyclopropyl ring do to ACh?

A

locks the conformation of the backbone preventing rotation

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7
Q

which isomer of ACTM is the active conformation of ACh at muscarinic receptors?
what is the name for the conformation it is locked into?

A

trans isomer

anticlinal conformation

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8
Q

which isomer is more potent at muscarinic receptors, (+) trans or (-) trans

A

(+) trans

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9
Q

Carbachol: drug class

A

non-select. muscarinic and nicotinic agonist used as a musc. agonist

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10
Q

why does Carbachol have a longer duration of effect?

A

Carbamate in place of ester

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11
Q

how do quaternary ammoniums effect oral bioavailability?

A

decrease oral bioavailability

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12
Q

T/F acetyl B-methylcholine chloride is used as a racemate

A

True

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13
Q

T/F acetyl B-methylcholine chloride is selective for musc Rs as an agonist

A

True

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14
Q

Bethanechol chloride is what drug class?

A

musc agonist

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15
Q

T/F Bethanechol chloride is likely susceptible to hydrolysis

A

false, fairly resistant to hydrolysis

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16
Q

why is Bethanechol chloride poorly oral bioavailable?

A

due to its carbamate structure

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17
Q

T/F Bethanechol chloride is used as a racemate

A

True

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18
Q

which enantiomer of Bethanechol chloride is more active?

A

S enantiomer

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19
Q

2S,3R,5S-muscarine chloride has how many isomers?
drug class?
SEs?

A

8
musc. agonist
hypersalivation, miosis, sweating

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20
Q

muscarinic agonists must have a _ atom capable of bearing positive charge

A

Nitrogen

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21
Q

muscarinic agonists must have a _ atom capable of participating in a hydrogen bond

A

Oxygen

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22
Q

there must be a _______ between the oxygen and nitrogen

A

2-carbon unit

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23
Q

pilocarpine:

drug class?

A

musc. agonist

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24
Q

T/F pilocarpine is a synthetically made product

A

False, plant natural product

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25
Q

what is a side effect of Sjogren’s syndrome?

A

dry mouth

26
Q

Cevimeline:
drug class?
what does it treat?

A

musc. agonist

dry mouth due to sjogren’s syndrome

27
Q

T/F Cevimeline is used as a racemate

A

True

28
Q

what route of metabolism does Cevimeline undergo?
what is formed?
is the formation active or inactive?

A

Cyp3A4 or 2D6
sulfoxide formation
inactive

29
Q

for muscarinic antagonists, what bulky group is important for antagonist action?

A

bulky ester group

30
Q

T/F atropine is given as a racemic mixture

A

True

31
Q

what primary effect does atropine have?

A

pupil dilation

32
Q

if an agonist has an ester group, _ carbons will be between the ester group and the nitrogen
if an antagonist has an ester group, _ carbons will be between the ester group and the nitrogen

A

2

3

33
Q

what process inactivates atropine?

A

hydrolysis

34
Q

which enantiomer of Atropine is active?

A

S enantiomer

35
Q

what drug is the isolate of Atropine that is only the (-)-S-isomer

A

hyoscyamine

36
Q

T/F scopolamine is given as a racemic mixture

A

True

37
Q

which enantiomer of scopolamine is active?

A

S enantiomer

38
Q

what feature of scopolamine differentiates it from atropine that makes it more chemically reactive?

A

an epoxide group

39
Q

what side effect does scopolamine have (CNS effect)

A

CNS depression

40
Q

the expected effective duration of tiotropium bromide would be?

A

long duration due to a very bulky ester

41
Q

tiotropium bromide is metabolized by?

A

hydrolysis, P450, and glutathione conjugation at epoxide

42
Q

what metabolism would you expect from aclidinium bromide?

A

fast metabolism by hydrolysis

43
Q

aclidinium bromide is considered long-acting or short-acting?

A

long acting

44
Q

what metabolism would you expect from umeclidinium bromide?

A

no ester hydrolysis, Cyp2D6-O-Dealkjylation, and hydroxylation

45
Q

what unique structural feature does oxybutynin have?

A

a butyne bridge

46
Q

what metabolism would you expect from oxybutynin?

A

CYP3A4

47
Q

what are the two metabolites of oxybutynin?

A

N-desethyl metabolite or secondary amine metabolite

48
Q

which metabolite of oxybutynin is active?

A

secondary amine metabolite

49
Q

solifenacin succinate is used as what enantiomer?

A

1S,3R enantiomer

50
Q

what metabolism would you expect from solifenacin succinate?

A

CYP3A4

51
Q

what are the two metabolites of solifenacin succinate?

which is active? inactive?

A

4R-hydroxy metabolite or N-oxide metabolite

both inactive

52
Q

what’s unique about Fesoterodine?

A

its a prodrug

53
Q

Tolterodine is used a single _-enantiomer

A

R

54
Q

what metabolism would you expect from Darifenacin?

are metabolites active? inactive?

A

3A4 or 2D6

inactive

55
Q

trospium chloride has no major ___ metabolism

A

P450

56
Q

trospium chloride is likely metabolized by?

A

ester hydrolysis

57
Q

glycopyrrolate bromide is currently approved to be used as?

A

a combo drug for COPD

58
Q

tropicamide is used for?

A

eye exams

59
Q

Benztropine mesylate is considered what drug class?

A

antiparkinsonian musc. antag.

60
Q

what unique feature of Benztropine mesylate contributes to its use?

A

it is lipophilic

61
Q

Biperidon hydrochloride is considered what drug class?

A

antiparkinsonian musc. antag.

62
Q

what shared feature of Benztropine mesylate and Biperidon hydrochloride contribute to their indication?

A

non-polar

Autonomics (14 decks)

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