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PHRM 844 > Vasodilators/Vasoconstricters > Flashcards

Vasodilators/Vasoconstricters Flashcards

1
Q

why does increasing K+ channel opening relax vascular smooth muscle?

A

the harder it is to depolarize the membrane enough to open Ca2+ gated channels

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2
Q

name the 3 K+ channel openers

A

minoxidil, diazoxide, adenosine

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3
Q

side effect of minoxidil

A

hypertrichosis (excess hair)

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4
Q

diazoxide administration and uses

A

IV for drug-resistant HTN
inhibits release of insulin
used for hypoglycemia secondary to hyperinsulinemia

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5
Q

what does adenosine do to the membrane?

A

hyperpolarization and relaxation

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6
Q

what does adenosine bind

A

A1 a GPCR

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7
Q

what is adenosine used for

A

coronary stress test
supraventricular arrhythmias

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8
Q

what does adenosine activate that kicks K+ out of the cell?

A

GIRK

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9
Q

what happens in vascular endothelium

A

calcium-calmodulin activates eNOS which helps convert arginine to NO

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10
Q

where is eNOS found

A

endothelium

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11
Q

where is guanylate cyclase found

A

vascular smooth muscle

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12
Q

what does NO do in smooth muscle

A

binds heme group on guanylate cyclase and stimulates cGMP and activation of protein kinase g

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13
Q

how does protein kinase G relax smooth muscle? (4 ways)

A

inhibits Cav 1.2
stimulation of Ca/K channels (BKca)
decreased MLC phosphorylation
enhanced Ca uptake in ER (phospholambam)

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14
Q

organic nitrates MOA

A

non selective vasodilators
breakdown to NO (bioactivation)

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15
Q

do organic nitrates require functional endothelium

A

no

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16
Q

what are nitrates used for?

A

sublingually for angina
oral for prolonged prophylaxis

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17
Q

what happens with continuous admin of nitrates”?

A

tolerance

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18
Q

asian population has an allele that decreases efficacy of what?

A

glycerol trinitrate
lys 504 allele

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19
Q

sodium nitroprusside dilates what

A

veins and arterioles

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20
Q

what is sodium nitroprusside metabolized to and where?

A

in erythrocytes to NO and CN which limits duration of treatment (toxic)

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21
Q

what does hydralazine dilate?

A

arterioles

22
Q

what does hydralazine interfere with

A

release of Ca from ER

23
Q

what can hydralazine be combined with?

A

isobride dinitrate in BiDil which is useful for African Americans with CHF

24
Q

what does human type B natriuretic peptide do?

A

activates guanyl cyclase domain
increases cGMP

25
Q

B type peptide drugs

A

nesiritide and sacubitril

26
Q

what is nesiritide used for?

A

acutely decompensated HF

27
Q

how does nesiritide work?

A

binds and activates membrane bound guanyl cyclase

28
Q

how does sacubitril work?

A

inhibits neprilysin which breaks down BNP
so we have increased BNP and enhanced action
increased bradykinin so don’t use with ACE inhib

29
Q

PDE3 inhibitors

A

amrinone and milrinone

30
Q

PDE5 inhibitors

A

dipyridamole, sildenafil, tadalafil, vardenafil

31
Q

what does PDE3 prefer

A

cAMP

32
Q

what does PDE5 prefer

A

cGMP

33
Q

what are PDE3 inhibitors used for?

A

IV for CHF

34
Q

what has 10 fold selectivity over inhibiton of PDE6?

A

sildenfail (blue vision)

35
Q

what pde is predominant in the corpus cavernosum?

A

PDE5

36
Q

where is PDE6 located?

A

retina

37
Q

PDE5 with longest duration of action?

A

tadalafil

38
Q

PDE5 with shortest time to onset

A

vardenafil

39
Q

PDE5 contraindicated with what?

A

nitrates

40
Q

endothelium receptor antagonists

A

-entans
bosentan, macitentan

41
Q

what do bosentan and macitentan do

A

blcok ETa and ETb

42
Q

what does ambrisentatn do

A

block ETa

43
Q

what are the -entan endothelien antagonists used for

A

pulmonary arterial hypertension

44
Q

what are the -entans contraindicated in and why

A

pregnancy, hepatotoxicity

45
Q

what do prostacyclin analogs do

A

relax pulmonary vascular smooth muscle

46
Q

where is prostacyclin produced?

A

endothelium

47
Q

what are the prostacyclin analogs?

A

PGI2, treprostinil, Iloprost, selexipag

48
Q

activator of sGC drug

A

riociguat

49
Q

what does riociguat do?

A

increases cGMP concentration in vascualr smooth muscle

50
Q

what is riociguat a substrate for?

A

pgp, CYP 1A1, 3A

51
Q

alpha 1 agonist drugs

A

epinephrine, phenylephrine, midodrine, droxidopa

52
Q
A

PHRM 844 (16 decks)

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