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PHRM 825 Therapeutics > Exam 1 Random Info > Flashcards

Exam 1 Random Info Flashcards

1
Q

True or false: Postganglionic neurons for sweat glands release ACh in stress-related excretion

A

False (ACh is for thermoregulation, NE is released in response to stress)

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2
Q

sympathomimetics mimic _____ and are considered adrenergic __________

a. ACh, antagonists
b. NE, antagonists
c. ACh, agonists
d. NE, agonists

A

d. NE, agonists

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3
Q

Activated alpha 1 receptors lead to which of the following: (there are 2 answers)

a. vasoconstriction
b. increased concentration of cAMP
c. increased conversion of GDP to GTP
d. opening of potassium channels

A

a. vasoconstriction
c. increased conversion of GDP to GTP

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4
Q

beta ___ receptors are located in the heart

A

1

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5
Q

beta 2 receptors are found in __________ muscle cells

A

smooth (vasodilation)

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6
Q

What happens as a result of activated nicotinic receptors? (2 of them)

a. the adrenal gland releases epinephrine into systemic circulation
b. adenylyl cyclase is stimulated to produce more cAMP
c. activates phospholipase C
d. sodium ions pass through into the cell membrane

A

a. the adrenal gland releases epinephrine into systemic circulation
d. sodium ions pass through into the cell membrane

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7
Q

what is the mechanism of action of vesamicol?

a. inhibit choline uptake
b. inhibit ACh release
c. inhibits vesicular storage
d. muscarinic antagonist

A

c. inhibits vesicular storage

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8
Q

True or false: an increased size of the trimethylammonium head of cholinergic agonists leads to decreased activity

A

true

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9
Q

an alpha substitution on the choline chain leads to: (2 answers)

a. decreased muscarinic activity
b. decreased nicotinic activity
c. increased nicotinic selectivity
d. increased muscarinic selectivity

A

a. decreased muscarinic activity
c. increased nicotinic selectivity

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10
Q

What structural modification makes a cholinergic agonist resistant to cholinesterases?

a. amide
b. alcohol
c. benzene
d. carbamyl

A

d. carbamyl

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11
Q

what is SLUD?

A

salivation, lacrimation, urination, defecation

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12
Q

M2 receptors signal via __________ and are located in the __________

a. intracellular Ca2+ release, heart
b. cAMP decrease, smooth muscle cells
c. cAMP decrease, heart
d. cAMP increase, sympathetic postganglionic cells

A

c. cAMP decrease, heart

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13
Q

importance of tertiary amine vs quaternary amine?

A

tertiary amines are more lipophilic due to non-charged amine and can cross BBB

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14
Q

tertiary amines are useful in ___ and ___ applications

A

CNS and ocular

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15
Q

describe the difference between depolarizing and nondepolarizing nicotinic receptor antagonists

A

depolarizing: keeps nicotinic receptor in open state leading to persistent membrane depolarization, which is unresponsive to new impulses

nondepolarizing: competitive inhibitors of ACh

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16
Q

describe the effect of norepinephrine on blood pressure and heart rate

A

increase bp, decrease heart rate

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17
Q

describe the effect of epinephrine on blood pressure and heart rate

A

no change in bp, increase heart rate

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18
Q

describe the effect of isoproterenol on blood pressure and heart rate

A

decrease bp, increase heart rate

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19
Q

MOA of albuterol?

a. nonselective beta agonist
b. selective beta 2 agonist
c. selective beta 1 agonist
d. selective alpha agonist

A

b. selective beta 2 agonist

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20
Q

True or false: Increase in the amount of alkyl substituents on the amine of an adrenergic receptor agonist leads to more alpha selectivity

A

false

(leads to more beta selectivity)

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21
Q

how does an alpha substitution on the alkyl chain of adrenergic receptor agonists affect MAO oxidation?

A

blocks MAO oxidation

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22
Q

Altering the catechol ring of an adrenergic receptor agonist leads to

a. increased metabolism via esterases
b. decreased metabolism via COMT
c. decreased metabolism via MAO
d. decreased metabolism by preventing reuptake

A

b. decreased metabolism via COMT

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23
Q

quinazolines or “-zosin” drugs are

a. beta blockers
b. alpha 1 antagonists
c. alpha 2 antagonists
d. nonselective alpha antagonists

A

b. alpha 1 antagonists

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24
Q

beta 1 antagonists are considered __________-selective

A

cardio

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25
Q

MOA of reserpine?

A

VMAT inhibitor, prevents packaging of norepinephrine into vesicles

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26
Q

describe the effect of chronic beta receptor blockade

A

upregulation of beta receptors post synapse (so must taper dose)

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27
Q

sweat glands stress response, what NT is released?

A

norepinephrine

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28
Q

sweat glands thermoregulation response, what NT is released?

A

acetylcholine

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29
Q

kidneys postganglionic exception

A

postganglionic neurons release dopamine

30
Q

adrenal gland exception

A

adrenal gland releases epinephrine

31
Q

drug used adjunctively in Parkinsons patients to minimize effects of L-DOPA

A

benztropine (Congentin)

32
Q

drug used in combination with beta agonists in COPD

A

ipratropium (quaternary amine)

33
Q

this drug binds to nicotinic receptors and keeps the ion channel open, which allows for a continuous influx of sodium and prevents the neuron from repolarizing and creating a new action potential

A

succinylcholine

34
Q

common side effects of anticholinergic drugs, what is the saying to remember them?

A

can’t see, can’t pee, can’t spit, can’t shit (red as a beet, dry as a bone, blind as a bat, mad as a hatter) -> blurry vision, incontinence, dry mouth, constipation, delirium

35
Q

which of the following is not a clinical use of neostigmine?

a. myasthenia gravis
b. bladder distension
c. Alzheimer’s disease
d. postoperative ileus

A

c. Alzheimer’s

(neostigmine is quaternary amine so can’t cross BBB, something like physostigmine would be better for Alzheimer’s since it is tertiary)

36
Q

is pyridostigmine a tertiary or quaternary amine?

A

quaternary amine

37
Q

what complication of a cholinergic crisis cannot be reverse with atropine? why?

A

excitation of skeletal muscles and CNS. This is mediated via nicotinic receptors, but atropine only binds muscarinic. This causes permanent depolarization of diaphragm

38
Q

nicotine is classified as a parasympathomimetic, yet it is know to raise bp and heart rate? Why is this?

A

nicotine stimulates the release of catecholamines by stimulating nicotinic receptors in the adrenal glands. Remember the adrenal glands are one of the sympathetic pathway exceptions

39
Q

catecholamines are all synthesized from the same building block __________

A

tyrosine

40
Q

the antihypertensive effects of clonidine can be attributed to its ability to:

a. block activity of the Gi coupled alpha 2 receptor, thus stimulating the cardiovascular control center in the brain
b. selectively bind beta 2 receptors in the vascular smooth muscle to cause vasodilation
c. block alpha 1 receptors in the vascular smooth muscle to inhibit vasoconstriction
d. activate Gi coupled GPCR on alpha 2 receptor which inhibits adenyl cyclase and turns off the cardiovascular control center in the brain

A

d. activate Gi coupled GPCR on alpha 2 receptor which inhibits adenyl cyclase and turns off the cardiovascular control center in the brain

41
Q

if you wanted to raise the bp of a patient who is hypotensive, which drug would you use?

a. epinephrine
b. norepinephrine
c. dobutamine
d. isoproterenol

A

b. norepinephrine

42
Q

which of the following is a physiologic effect of clonidine?

a. dec heart rate
b. dec renin release
c. inc heart contractility
d. vasodilation
e. A, B, and D

A

e. A, B, and D

(clonidine is an alpha 2 agonist, turns off cardiovascular control center in brain, which reduces sympathethic signaling

43
Q

salmeterol and fomoterol are beta 2 selective agonists that are used in long term treatment of asthma. Their long half life can be attributed to:

a. avoiding renal clearance
b. block the activity of COMT
c. avoid metabolism by MAO
d. have higher receptor affinity

A

c. avoid metabolism by MAO

44
Q

phenoxybenzamine is a(n) __________ alpha blocker whereas phentolamine is a(n) alpha blocker

a. reversible, irreversible
b. irreversible, reversible
c. covalent, ionic
d. ionic, covalent

A

b. irreversible, reversible

45
Q

which of the following is not a physiologic effect of propranolol?

a. dec cardiac output
b. inhibition of renin release
c. decreased HDL
d. promotes lipolysis

A

d. promotes lipolysis

46
Q

which beta blockers possess intrinsic sympathomimetic activity? (3 of them)

A

pindolol, carteolol, acebutolol

47
Q

is metoprolol cardioselective, non-selective, or mixed?

A

cardioselective (one aromatic ring)

48
Q

is propranolol cardioselective, non-selective, or mixed?

A

non-selective (two aromatic rings fused together)

49
Q

is carvedilol cardioselective, non-selective, or mixed?

A

mixed (1 aromatic ring, not connected)

50
Q

True or false: premature labor contractions can be halted by administration of a beta 2 receptor antagonist

A

false

(Beta-adrenergic receptor activation will cause relaxation of uterine smooth muscle which will prevent premature labor contractions. A beta-adrenergic receptor antagonist will have the opposite effect)

51
Q

true or false: norepinephrine would be considered a sympathomimetic

A

true

52
Q

true or false: Pre-ganglionic neurons in the sympathetic system are short and form ganglia at the paravertebral sympathetic
ganglia near the spinal cord

A

true

(In the sympathethic nervous system, pre-ganglionic neurons do form their ganglia at the paravertebral sympathetic ganglia near the spinal cord. This is in contrast to the parasympathetic nervous system where the ganglia form near the target
organs)

53
Q

true or false: A parasympathomimetic acting on it’s receptor in the ciliary muscle will cause an elevation in cAMP levels in that
tissue

A

false

(ciliary muscle -> M3 -> Gq not Gs)

54
Q

true or false: When acetylcholine activates nicotinic receptors, sodium is the primary ion that flows through the channel.

A

true

55
Q

true or false: when an M2 receptor antagonist acts in the heart, heart rate increases

A

true

(M2 activation slows heart rate, so an antagonist acting on M2 increases heart rate)

56
Q

true or false: alpha 1 adrenergic receptors and M3 muscarinic receptors both couple to the Gi/o protein to reduce intracellular cAMP

A

false

(Gq)

57
Q

glaucoma slide: 3 main parts and the medications

A

ciliary muscle -> M3 agonist -> pilocarpine
ciliary body -> alpha 2 agonist -> brimonidine
-ciliary epithelium -> NE-beta -> timolol (beta antagonist)

58
Q

how does scopolamine work?

A

it is an antimuscarinic

59
Q

are alpha 2 receptors pre or post synaptic? what does it inhibit?

A

pre, it inhibits adenylyl cyclase

60
Q

vasodilation of skeletal muscle, what receptor? (1)

A

beta 2

61
Q

vasoconstriction what receptors? (2)

A

alpha 1, alpha 2

62
Q

endothelium cholinergic response, what receptor?

A

M3

63
Q

bronchodilation, what receptor?

A

beta 2

64
Q

bronchoconstriction, what receptor?

A

M2, M3

65
Q

pupillary constriction: what is it called, what muscle, what receptor?

A

miosis, circular muscle, M3 (parasymp)

66
Q

pupillary dilation: what is it called, what muscle, what receptor?

A

mydriasis, radial muscle, alpha 1

67
Q

contraction of radial muscle leads to __________

A

mydriasis

68
Q

contraction of circular muscle leads to __________

A

miosis

69
Q

what receptor slows heart rate?

A

M2

70
Q

what receptor acts on smooth muscle, exocrine glands/GI tract, and endothelium?

A

M3

71
Q

what drug inhibits the catalysis of L-DOPA to dopamine and is used in Parkinson’s disease?

A

carbidopa

PHRM 825 Therapeutics (25 decks)

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