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► Med - Pharmacology > Pharmacology of Vasoactive Peptides > Flashcards

Pharmacology of Vasoactive Peptides Flashcards

1
Q

What are the 2 functions of angiotensin converting enzyme (ACE)?

A
  1. Converts ATI to ATII

2. Kininase II activity to metabolize bradykinin

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2
Q

What is ACE also known as?

A

Kininase II

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3
Q

What are 2 drugs that are known as ACE Inhibitors?

A

Captopril

Enalapril

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4
Q

What is that action of bradykinin?

A

Vasodilation

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5
Q

What is the action of atrial natriuretic peptide?

A

Lowers blood pressure by stimulating Na excretion, antagonized the effects of aldosterone

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6
Q

What is the action of kallikreins?

A

They promote coagulation process via intrinsic system AND exert control to lower blood pressure via generation of kinins (like bradykinin)

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7
Q

What is the action of endothelins?

A

Potent vasoconstrictors

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8
Q

What is the function of vasoactive intestinal peptide (VIP)?

A

VIP is present in the central and peripheral nerves where it functions as a neuromodulator. VIP produces marked vasodilation.

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9
Q

What is the function of substance P?

A

Substance P induces vasodilation by stimulating the release of nitric oxide.

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10
Q

What is the function of calcitonin gene-related peptide (CGRP)?

A

CGRP is present in large amounts in the thyroid gland. CGRP is also found in the CNS and GI tract with substance P. Intravenous administration of CGRP can cause hypotension and tachycardia.

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11
Q

What is the effect of desmopressin on endothelial cells?

A

Desmopressin increase the factor VIII and vWF activity of patients with mild hemophilia and von Willebrand disease. It is effective in the control of bleeding in mild surgical process.

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12
Q

What is the effect of aprotonin on the actions of kallikrein?

A

Kallkrein inhibitor that leads to the blockage of bradykinin generation

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13
Q 
Which of the following enzymes is responsible for the generation of Angiotensin II?
A. Renin
B. Kininase-I 
C. Kininase-II 
D. Plasmin
E. Kallikrein
A

C. Kininase-II

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14
Q 
An elderly diabetic patient was treated with an ACE inhibitor for hypertension. During hospitalization he developed sepsis and sustained a severe drop in blood pressure. What is the likely cause for this condition?
A. Inhibition of renin
B. Excessive generation of angiotensin
C. Excessive generation of bradykinin
D. Inhibition of plasmin
E. Inhibition of kallikrein
A

C. Excessive generation of bradykinin

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15
Q

What is the general MOA of vasoactive peptides?

A

These peptides all act on cell surface receptors. Most act via G protein-coupled receptors and cause the production of second messengers, some may open ion channels.

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16
Q

What converts ATII to ATIII?

A

Aminopeptidase

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17
Q

What converts angiotensinogen to ATI?

A

Renin

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18
Q

What converts ATI to ATII?

A

ACE

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19
Q

What is the only active AT?

A

ATII

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20
Q

What is the action of ATII?

A

Produces profound vasoconstriction

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21
Q

Angiotensinase

A

A group of peptidases which hydrolyze angiotensin II and angiotensin III into smaller fragments.

22
Q

What is the function of ACE inhibitors?

A

Controls hypertension.

ACE inhibitors not only block the conversion of angiotensin I to angiotensin II but also inhibits the degradation of other vasopeptides such as bradykinin

23
Q

What are angiotensin receptor antagonists?

A

Antagonize the action of angiotensin II

24
Q

What are some angiotensin receptor antagonists?

A

Losartan

Valsartan

25
Q

What is the action of plasma kallikrein?

A

Conversion of HMW kininogen to bradykinin

26
Q

What is plasma kallikrein also known as?

A

Fletcher Factor

27
Q

What is plasma prekallikrein activated by?

A

XIIa (Hageman factor)

28
Q

What is a cause of hypotension in DIC patients?

A

Many of the patients with consumption coagulapathy (DIC) develop hypotension due to increased kallikrein production.

29
Q

Do the angiotensin antagonists have any effect on the actions on ACE?

A

No

30
Q

Can these angiotensin antagonists be given to a hypertensive patient with sepsis?

A

Yes

31
Q

What is the role of kinins in inflammation and pain?

A

Kinins promote redness, local heat, swelling and pain. Kinins are potent algesic agents.

32
Q

How can hypotension occur as a result of ACE inhibitors?

A

Angiotensin converting enzyme inhibitors such as captopril therefore can inhibit the generation of angiotensin II simultaneously bradykinin levels may increase resulting in hypotension.

33
Q

Are there specific kinin antagonist drugs?

A

No

34
Q

What is ictibant?

A

Ictibant is a second generation B2 kinin receptor inhibitor which has undergone limited clinical trials in pain and inflammation.

35
Q

What is the action of vasopressin?

A

It plays an important role in the long term control of blood pressure through its action on the kidney to increase water resorption. It has short term vasoconstrictor actions.

36
Q

What is the action of these drugs: omapatrilat, sampartilat and fasidotrilat?

A

These drugs enhance vasodilation, reduce vasoconstriction and increase sodium excretion via inhibition of metaloproteases

37
Q

What is a non-selective antagonist of endothelin receptors?

A

Bosentan

38
Q

What is the action of neurotensin?

A

In peripheral circulation it causes vasodilation, hypotension, vascular permeability, hyperglycemia and inhibition of gastric motility.

39
Q

What is the action of adrenomodulin?

A

It is widely distributed and circulates in blood and mediates hypothyroid responses. Circulating adrenomodulin levels are increased during intensive exercise, patients with hypertension, renal failure and septic shock.

40
Q

What is the action of neuropeptide Y?

A

Besides a CNS effect it produces vasoconstriction and mediates hypertensive responses.

41
Q

What is the action of urotensin?

A

It is a potent vasoconstrictor primarily acting on arterial beds. It is one of the most potent vasoconstrictors.

42
Q

Captopril and Enalapril MOA and Indication

A

ACE Inhibitors

Hypertension

43
Q

Losartan and Valsartan MOA and Indication

A

Angiotensin receptor inhibitor

Hypertension

44
Q

What is ROA of Captopril and Enalapril and Losartan and Valsartan?

A

Oral

45
Q

Icatibant MOA and ROA

A

Bradykinin receptor inhibitor

Oral

46
Q

Icatibant Indication

A

Inflammatory responses

47
Q

Aprotonin MOA and ROA

A

Kallikrein inhibitor

IV

48
Q

Aprotonin Indication

A

Inflammation

49
Q

Desmopressin (DDAVP) MOA and ROA

A

Vasopressin analogue

IV

50
Q

Desmopressin Indication

A

Bleeding

51
Q

Bosentan MOA and ROA

A

Endothelin receptor inhibitor

Oral

52
Q

Bosentan Indication

A

Pulmonary hypertension

► Med - Pharmacology (74 decks)

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