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PHRM 844 Therapeutics > Exam 5 - Vasodilators Hockerman > Flashcards

Exam 5 - Vasodilators Hockerman Flashcards

1
Q

3 K+ channel agonists/opener drugs

A

minoxidil
diazoxide
adenosine

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2
Q

minoxidil can lead to what rare condition?

A

hypertrichosis

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3
Q

minoxidil is activated in vivo by what enzyme?

A

sulfotransferase 1A1

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4
Q

minoxidil is given _____ for HTN

A

orally (topically for hair growth)

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5
Q

diazoxide is given _____ to treat acute HTN

a. orally
b. topically
c. IV
d. subQ

A

c. IV

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6
Q

diazoxide is given _____ for hypoglycemia secondary to hyperinsulinemia

a. orally
b. topically
c. IV
d. subQ

A

a. orally

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7
Q

what drug inhibits release of insulin from pancreatic beta cells?

a. minoxidil
b. diazoxide
c. adenosine

A

b. diazoxide

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8
Q

what kind of receptor is the A1 receptor that adenosine binds to?

A

GPCR

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9
Q

which is given IV during a coronary stress test?

a. minoxidil
b. diazoxide
c. adenosine

A

c. adenosine

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10
Q

what does GIRK channel stand for?

A

G-protein activated inwardly rectifying K+ channel

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11
Q

which G protein subunit(s) binds and activates GIRK, leading to K+ efflux and membrane hyperpolarization?

A

beta, gamma subunits

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12
Q

which nitric oxide synthase (NOS) isoform is important for this lecture?

a. nNOS
b. iNOS
c. eNOS

A

c. eNOS

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13
Q

where is nitric oxide produced and what is it activated by?

A

vascular endothelium; Ca2+-CAM

(idk what that stands for)

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14
Q

NOS is in the vascular endothelium, and NO diffuses to the vascular _____ _____

A

smooth muscle

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15
Q

eNOS is found in which cells of the vasculature?

A

endothelial

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16
Q

NO is a key activator of _____ _____ found in vasc sm muscle

A

guanylate cyclase

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17
Q

__________ relaxes smooth muscle via NO

a. phenylephrine
b. acetylcholine
c. hemoglobin
d. L-NMMA

A

b. acetylcholine

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18
Q

where does NO bind in guanylate cyclase to stim production of cGMP and activating protein kinase G?

A

heme iron prosthetic group

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19
Q

what AA is a precursor to NO?

A

arginine

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20
Q

4 ways protein kinase G relaxes smooth muscle

A

-inhib of L-type Ca2+ channels
-stim of Ca2+-activated K+ channels
-dec MLC phosphorylation
-enhanced Ca2+ uptake into ER

(all of these add up to vasodilatory effect of PKG)

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21
Q

protein kinase G relaxes smooth muscle via inhib of which Ca2+ channels?

a. CaV1.2
b. BKca
c. myosin phosphatase 1
d. phospholamban

A

a. CaV1.2

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22
Q

protein kinase G relaxes smooth muscle via stimulation of which channel?

a. CaV1.2
b. BKca
c. myosin phosphatase 1
d. phospholamban

A

b. BKca

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23
Q

protein kinase G decreases MLC phosphorylation via which enzyme?

a. myosin phosphatase 1
b. myosin phosphatase 2
c. myosin phosphatase 3
d. myosin phosphatase 4

A

a. myosin phosphatase 1

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24
Q

protein kinase G phosphorylates _____ to enhance Ca2+ uptake into the ER

a. CaV1.2
b. BKca
c. myosin phosphatase 1
d. phospholamban

A

d. phospholamban

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25
Q

true or false: organic nitrates require functional endothelium

A

false

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26
Q

organic nitrates are __________ vasodilators

a. selective
b. non-selective

A

b. non-selective

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27
Q

which has the highest oral bioavailability and half-life?

a. GTN (glyceryl trinitrate)
b. ISDN (isosorbide dinitrate)
c. 5-ISMN (isosorbide mononitrate)

A

c. isosorbide mononitrate

(bioavailability: GTN < 1%, ISDN 20%, 5-ISMN 100%

half life: GTN 3 min, ISDN 10 min, 5-ISMN 280 min)

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28
Q

organic nitrates are given __________ in tx of acute attacks of angina, and __________ or __________ for prolonged prophylaxis

A

sublingually; orally; transdermally

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29
Q

what was the importance of the munitions workers from lecture?

A

Tells us about tolerance to glyceryl trinitrate. Workers would mix it by hand, get headaches, but became more tolerant through the week, then after being away for the weekend they would come back and get headaches again

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30
Q

what enzyme is important in GTN tolerance?

A

ALDH2 (aldehyde dehydrogenase 2)

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31
Q

why is GTN not as efficacious for Asian pts?

A

30-50% of Asians have at least one Lys 504 allele, which is less efficient in metabolizing GTN

(this allele also accounts for alcohol intolerance)

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32
Q

what polymorphism is common in ALDH2 in regards to GTN?

A

Glu 504 Lys polymorphism (Glu 504 is 10X more efficient in metabolizing GTN)

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33
Q

bioactivation of ISMN and ISDN are ALDH2-__________

a. dependent
b. independent

A

b. independent

34
Q

methylglyoxal _____ vasorelaxation stimulated by ACh/NO

A

inhibits (higher conc of methylglyoxal leads to dec ACh relaxation)

35
Q

sodium nitroprusside (SNP) is given IV for ?

A

acute management of hypertensive crisis and severe decompensated HF

36
Q

what element is in the center of nitroprusside structure?

A

iron

37
Q

true or false: SNP constricts veins and arterioles

A

false (dilates)

38
Q

SNP is metabolized in erythrocytes to what 3 things?

A

NO radical
4 CN-
cyanmethemoglobin

(limits treatment duration)

39
Q

why can sodium nitroprusside lead to lactic acidosis?

A

cyanide (CN-) is a product of metabolism and inhibits oxidative metabolism, so lactic acid accumulates

40
Q

for sodium nitroprusside, CN- is converted to less toxic SCN- by __________, excreted via kidney

(blank is a mitochondrial enzyme)

A

rhodanase

41
Q

what 2 agents can be used for SNP detoxification?

A

sodium thiosulfate
hydroxycobalamin (injectable B12)

(for hydroxocobalamin, CN will bind to cobalt in middle of complex)

42
Q

what drug can induce a Lupus-like syndrome?

A

hydralazine

43
Q

what is the combo product of hydralazine + ISDN?

A

BiDil

44
Q

true or false: BiDil (hydralazine + ISDN) increases mortality in African Americans with CHF

A

false (decreases)

45
Q

which enzymes play key roles in the vasodilation mediated by glyceryl trinitrate?

A. eNOS and soluble guanylyl cyclase
B. ALDH2 and soluble guanylyl cyclase
C. ALDH2 and membrane-bound guanylyl cyclase
D. eNOS and membrane-bound guanylyl cyclase

A

b. ALDH2 and soluble guanylyl cyclase

46
Q

where is human B type natriuretic peptide made?

A

in the ventricles

47
Q

which drug is related to BNP and is given IV in acutely decompensated HF?

a. nesiritide
b. sacubitril
c. GTN
d. amrinone

A

a. nesiritide (brand name = Natrecor)

48
Q

Natrecor (nesiritide) activates __________ guanylate cyclase

a. soluble
b. membrane-bound

A

b. membrane-bound

49
Q

sacubitril drug class

A

neprilysin inhibitor

50
Q

how does sacubitril work?

A

inhibits neprilysin to prevent breakdwon of BNP (enhances BNP action, as well as Ang II and bradykinin)

51
Q

entresto is a combo of what two drugs?

A

sacubitril and valsartan

52
Q

why is entresto given as a combo drug?

A

neprilysin isn’t specific for breakdown of NP, also Ang II and bradykinin

53
Q

entresto indication

A

HF (both HFrEF and HFpEF)

54
Q

two PDE3 inhibitor drugs to know

A

amrinone
milrinone

55
Q

PDE3 is selective for _____ while PDE5 is selective for _____

a. cAMP; cGMP
b. cGMP; cAMP

A

a. cAMP; cGMP

56
Q

are amrinone/milrinone mainly used in acute or chronic CHF treatment?

A

acute

57
Q

amrinone/milrinone route of administration

a. oral
b. IV
c. subQ
d. topical

A

b. IV

58
Q

which is incorrect about amrinone/milrinone?

a. has direct positive inotropic effect on myocardium
b. given IV
c. large chronotropic effect
d. direct vasodilatory effect on vasc sm muscle

A

c. large chronotropic effect

(minimal chronotropic effect)

59
Q

why can sildenafil cause bluish vision?

A

it has 10 fold selectivity of PDE6, which is present in photoreceptors in the retina

60
Q

3 selective PDE5 inhibitor drugs

A

sildenafil (Viagra)
tadalafil (Cialis)
vardenafil (Levitra)

61
Q

true or false: tadalafil and vardenafil are more selective for PDE5 than viagra

A

true

62
Q

vardenafil (Levitra) has a _____ time to onset than Viagra

a. shorter
b. longer

A

a. shorter

63
Q

which has the longest duration of action?

a. sildenafil
b. tadalafil
c. vardenafil

A

b. tadalafil

64
Q

entresto should not be used with what drug class?

A

ACE inhibitors

65
Q

what is the contraindication for PDE5 inhibitors and why?

A

CI: any PDE5 inhibitor with organic nitrates
Reason: huge drop in BP, both inc accum of cGMP. cGMP also inhibits PDE3, increasing cAMP levels in vasc sm muscle. cGMP and cAMP both stimulate vasodilation

66
Q

__________ signaling is increased in pulmonary arterial hypertension (PAH)

A

endothelin

67
Q

3 vasoconstrictor/endothelin antagonist drugs

A

bosentan (Tracleer)
macitentan (Opsumit)
ambrisentan (Letairis)

68
Q

endothelin antagonists indication

A

pulmonary arterial hypertension (PAH)

69
Q

which has a contraindication of hepatoxicity?

a. bosentan
b. macitentan
c. ambrisentan

A

a. bosentan

70
Q

true or false: endothelin antagonists can be used in pregnancy

A

false

71
Q

main difference between ambrisentan compared to bosentan and macitentan

A

ambrisentan blocks only ETa receptors while the other two block both ETa and ETb receptors

72
Q

the endothelin ETa receptor is found in

a. vasc sm muscle
b. endothelium
c. both

A

a. vasc sm muscle

73
Q

the endothelin ETb receptor is found in

a. vasc sm muscle
b. endothelium
c. both

A

c. both

74
Q

how do prostacyclin analogs work for vasodilation?

A

they relax pulmonary vasc sm muscle (used for PAH)

75
Q

what are the route of adminstration and half-lives of each prostacyclin analog drug?

PGI2 (epoprostenol)
treprostinil (Remodulin)
iloprost (Ventavis)
selexipag (Uptravi)

A

PGI2 -> IV; 3-5 min
treprostinil -> oral, IV; ~4 hours
iloprost -> inhalation; ~30 min
selexipag -> oral; 6-13 hours

76
Q

drug for pulmonary hypertension that is an allosteric activator of sGC (soluble guanylate cylclase) and can inc cGMP conc in vasc sm muscle

A

Riociguat (Adempas)

77
Q

Riociguat should not be combined with nitrates or PDE5 inhibitors and is contraindicated in __________

A

pregnancy

78
Q

Riociguat has a risk of __________

A

hemorrhage

79
Q

Riociguat (allosteric sGC activator), is a substrate for what 3 things? (2 of them are cyps)

A

P-gp
CYP1A1
CYP3A

80
Q

sildenafil and tadalafil are both indicated for treatment of _____ due to enhanced vasodilatory effect of NO

A

PAH

PHRM 844 Therapeutics (28 decks)

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