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Pharmacology > Vasoactive Peptide Pharmacology > Flashcards

Vasoactive Peptide Pharmacology Flashcards

1
Q

Where in the cell do vasoactive peptides typically act?

A

Cell surface receptors (largely GPCRs to affect production of second messengers or open ion channels)

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2
Q

Angiotensin

What enzyme catalyzes its creation from angiotensinogen?

A

Renin

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3
Q

How many AAs in angiotensin I?

A

10

Decapeptide

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4
Q

Which angiotensin is most active?

A

Angiotensin II

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5
Q

What enzyme catalyzes conversion of angiotensin I to angiotensin II?

A

ACE

Angiotensin Converting Enzyme

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6
Q

What enzyme converts angiotensin II to angiotensin III?

A

Aminopeptidase

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7
Q

What enzymes degrades angiotensin?

A

Angiotensinases

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8
Q

How many AAs in angiotensin II?

A

8

Octapeptide

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9
Q

ACE is also known as…?

A

Kininase II

Peptidyl dipeptidase

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10
Q

List the pharmacologic actions of angiotensin II

A
  • Vasoconstriction
  • Aldosterone production from adrenal cortex
  • lucocorticoid biosynthesis
  • Mitogenic agent for vascular and cardiovascular muscle cells
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11
Q

What are the two general mechanisms by which we inhibit angiotensin?

A
  • ACE inhibitors

- Angiotensin receptor blockers

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12
Q

ACE inhibitors inhibit the conversion of…?

A

Angiotensin I to Angiotensin II

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13
Q

ACE inhibitors inhibit the degradation of…?

A

Bradykinin

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14
Q

List two ACE Inhibitors

A

Captopril

Enalapril

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15
Q

List the Angiotensin Receptor Antagonists

A

Losartan

Valsartan

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16
Q

Plasma prekallikrein is activated by what to become plasma kallikrein?

A

Factor 12a (Hageman Factor)
Trypsin
Kallikrein

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17
Q

What does plasma kallikrein catalyze?

A

Conversion of HMW kininogen to bradykinin

18
Q

What does tissue kallikrein catalyze?

A

Conversion of LMW kininogen to Kallidin (Lysylbradykinin)

19
Q

What is the function of kininases I and II?

A

Degrade bradykinin and kallidin into inactive fragments

20
Q

An excess of kallikrein will lead to….

A

Excess bradykinin production, leading to hypotension

21
Q

What is the predominant peptide in hypotensive shock?

A

Bradykinin

22
Q

What drug would you never give to a septic patient? Why?

A

ACE Inhibitor
They would inhibit kininase II (ACE), preventing the degradation of bradykinin and exacerbating the problem of hypotension in septic shock

23
Q

What are the various physiological actions of kinins?

A
  • Vasodilation
  • Stimulate NO release (active NOS2)
  • Prostaglandin release
  • Potent algesics (cause pain)
  • Promote water and solutions’ movement into the EC space, causing edema
24
Q

How are kinins involved in pain?

A

They are algesics (they cause pain).

They promote redness, local heat, swelling, and pain

25
Q

What are the two bradykinin receptors and their primary functions?

A

B1 - mediating biological actions of bradykinin

B2 - drugs that block the action of bradykinin target B2 receptor

26
Q

Why is kininase II important in bradykinin regulation?

A

Kininase II (ACE) degrades bradykinin into inactive products.

27
Q

Icatibant

MOA

A

B2 receptor inhibitor

28
Q

Icatibant

Indications

A

Angio-neurotic edema (edema of an unknown immunologic nature)

29
Q

What drug can be used to block the algesic effects of kinins?

A

Aspirin

30
Q

Vasopressin (ADH)

General role in hemostasis

A

Long term control of blood pressure through kidney and increased H2O reabsorption

31
Q

Desmopressin

Indications

A
  • Used in pediatrics.
  • Analog of ADH that is used in blood banking, mild hemophilia, and vWF deficiency.
  • Mild surgical/dental procedures
32
Q

Desmopressin

MOA

A

Increases Factor 8 activity

33
Q

Vasopeptide Inhibitor Drugs

Physiological effects

A

Increase natriuretic peptide levels and decrease formation of angiotensin II.
Vasodilation
Increased sodium excretion

34
Q

Vasopeptide Inhibitors

List 3

A

Omapatrilat
Sampartilat
Fasidotrilat

35
Q

Endothelins

What effect do they have on vascular tone?

A

Vasoconstrictors

36
Q

What drug is a non-selective antagonist of endothelins?

A

Bosentan

37
Q

Bosentan

MOA

A

Antagonist of Endothelin

38
Q

Bosentan

Indication

A

Pulmonary artery hypertension

39
Q

VIP causes vaso…..?

A

Vasodilation

40
Q

Substance P causes vaso….? How?

A

Vasodilation by stimulating the release of NO

41
Q

Neurotensin

A

Causes vasodilation, hyperglycemia

42
Q

Adrenomodulin levels are increased during…

A

Exercise
Hypertension
Renal failure
Septic shock

Pharmacology (67 decks)

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