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Pharmacology > Pharm of vasoactive peptides > Flashcards

Pharm of vasoactive peptides Flashcards

1
Q

What are the 5 vasoactive peptides?

A

1) angiotensin (I, II, III)
2) kinins (bradykinin)
3) endothelins
4) vasopressin
5) ANP

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2
Q

True or false: all vasoactive peptides act on cell surface receptors

A

TRUE (mostly via GPCRs)

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3
Q

True or false: angiotensin II is the only active form of AT that produces profound vasoconstriction

A

true

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4
Q

What enzyme converts angtiotensinogen to angtiotensin I

A

renin

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5
Q

What enzyme converts angiotensin I to angiotensin II?

A

ACE

angiotensin converting enzyme

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6
Q

Which drugs are known to produce an increase in angiotensin?

A

corticosteroids
estrogens
thyroid hormones
angiotensin II

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7
Q

AT I is a decapeptide while ATII is a ____________

A

octapeptide

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8
Q

What are 2 other names for ACE?

A

peptidyl dipeptidase

kininase II

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9
Q

Where is ACE found?

A

widely distributed in the vasculature on the luminal structure of the endothelial cells

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10
Q

What enzyme hydrolyzes ATII to ATIII?

A

angiotensinase

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11
Q

What is the danger of too much ATII production?

A

hypertension

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12
Q

True or false: ATII promotes the release of epi and nor epi from adrenal medulla

A

true

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13
Q

What 3 parts of angiotensin pathway are targeted by drugs?

A

1) renin secretion
2) converstion of ATI to ATII
3) block AT receptors

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14
Q

In addition of blocking the conversion of ATI to ATII, what else do ACE inhibitors do?

A

inhibit degradation of bradykinins (as well as substance P and enkephalin)

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15
Q

Why do you see hypotensive effects after treatment with ACE inhibitors/

A

because ACE inhibitors inhibit the degradation of bradykinins

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16
Q

What are the orally active ACE inhibitors?

A

captopril

enalapril

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17
Q

What is the chemistry behind angiotensin receptor blockers?

A

substitution of sarcosine for phenylalanine in position 8 of ATII

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18
Q

What class does saralasin belong to?

A

peptide ARBs

angiotensin receptor blockers

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19
Q

What are the nonapeptide ARBs?

A

losartan

valsartan

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20
Q

What enzymes produce kinins?

A

kallikreins (kininogenases)

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21
Q

True or false: kinins can be generated by insect bites

A

true

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22
Q

What enzyme converts plasma prekallikrein to plasma kallikrein?

A 
trypsin
kallikrein
hageman factor (factor XIIa)
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23
Q

kallikrein converts __________ to __________

A

kininogen to bradykinin

24
Q

Where are kallikreins made?

A

liver

25
Q

Where are kallikreins present?

A 
plasma
kideny
pancreas
GI tract
sweat glands
salivary glands
26
Q

What is Fletcher factor?

A

plasmatic prekallikrein

promotes coag process via intrinsic system

27
Q

Why do DIC patients develop hypotension?

A

increased kallikrein production

28
Q

What are kininogens?

A

substrates for kallikreins

29
Q

What 2 varieties of kininogens are there?

A

low molecular weight

high molecular weight

30
Q

plasma kallilkrein cleaves ________ to generate bradykinin

A

HMW kininogen (high molec weight)

31
Q

What are the 3 kinds of kinins?

A

1) bradykinin
2) lysyl bradykinin
3) meth-lysylbradykinin

32
Q

Bradykinin is released by ________ __________

A

plasma kallikrein

33
Q

lysyl bradykinin is released by __________ ________

A

glandular kallikrein

34
Q

meth-lysylbradykinin is released by _______

A

pepsin

35
Q

Where in the body are the 3 kinins found

A

plasma

urine

36
Q

True or false: kinins stimulate the release of NO

A

true

37
Q

What are the 2 types of kinin receptors?

A 
B1 = predominant receptors
B2 = targeted by drugs
38
Q

What is another name for kininase II?

A

ACE (can also inactivate bradykinin)

39
Q

What does icatibant target?

A

second generation B2 receptor inhibitor (treat hypotension)

40
Q

How do ACE inhibitors affect bradykinin?

A

augment its effects by blocking the degradation of it

41
Q

How does aspirin affect the kallikrein kinin system?

A

blocks the algesic effects of prostaglandins

42
Q

What are the effects of vasopressin

A

increased blood pressure (short term vasoconstrictor actions)

43
Q

What is the clinically used analogue of vasopressin?

A

desmopressin

44
Q

What is the effect of desmopressin?

A

increases factor 8 activity and von willebrand factor

45
Q

What do the drugs omapatrilat, sampartilat, and fasidotrilat do?

A

enhance vasodilation, reduce vasoconstriction, and increase sodium excretion (via increasing levels of natriuretic peptides)

46
Q

What do the endothelins do?

A

vasoCONSTRICT

47
Q

What are the 2 receptors for endothelin actions?

A

ETa and ETb

48
Q

What is Bosentan?

A

a non selective antagonist of endothelin (treats pulm hypertension)

49
Q

What is VIP?

A

vasodilator made in nervous system

50
Q

What is substance P?

A

vasodilator (releases NO by upregulating iNOS)

51
Q

What is neurotensin

A

vasodilator

52
Q

Where is calcitonin gene related peptide found?

A

thyroid gland, CNS, GI

53
Q

What is adrenomodulin?

A

increases in exercise, hypertension, renal failure, septic shock

vasodilator

54
Q

What is neuropeptide Y?

A

vasoconstrictor

55
Q

What is urotensin?

A

vasoconstrictor (increases with end stage heart failure)

56
Q

When patients are treated with ACE inhibitors for hypertension, why might they go into shock?

A

excessive generation of bradykinin

Pharmacology (21 decks)

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