(THER) Vasoactive Peptides Flashcards

1
Q

Captopril MOA and Route

A

MOA: Ace Inhibitor

Route: Oral

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2
Q

Captopril Indications and Side Effects

A

Ind: Hypertension

SE: severe stomach pain; chest pain; allergic reaction

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3
Q

Enalapril MOA and Route

A

MOA: ACE inhibitor

Route: Oral

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4
Q

Enalapril Indications and Side Effects

A

Ind: Hypertension

SE: Hypotension; severe stomach pain

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5
Q

Losartan MOA and Route

A

MOA: Angiotensin receptor inhibitor

Route: Oral

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6
Q

Losartan Indications and Side Effects

A

Ind: Hypertension

SE: Diarrhea; insomnia; nasal congestion

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7
Q

Valsartan MOA and Route

A

MOA: Angiotensin receptor inhibitor

Route: Oral

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8
Q

Valsartan Indications and Side Effects

A

Ind: Hypertension

SE: Stomach pain; nausea

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9
Q

Icatibant MOA and Route

A

MOA: Bradykinin receptor inhibitor

Route: Oral

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10
Q

Icatibant Indications and Side Effects

A

Ind: Inflammation

SE: stomach pain; nausea

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11
Q

Desmopressin (DDAVP) MOA and Route

A

MOA: Vasopressin analogue; Increases the factor VIII activity of patients with mild hemophilia and VWD.

Route: IV

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12
Q

Desmopressin Indications and Side Effects

A

Ind: Bleeding (Initially developed for Pt. w/ diabetes insipidus)

SE: Headache; stomach pain; nausea

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13
Q

Bosentan MOA and Route

A

MOA: Endothelin receptor inhibitor

Route: Oral/ IV

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14
Q

Bosentan Indications and Side Effects

A

Ind: Pulmonary arterial hypertension

SE: Liver problems; stomach pain; nausea

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15
Q

Name the (3) most important vasoactive peptides

A
  1. Angiotensins (I, II and III)
  2. Bradykinin/related kinins
  3. Endothelins
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16
Q

Which of the angiotensins is the active form ( I, II, or III?)

A

Angiotensin II is the only active form and produces profound vasoconstriction and other pharmacologic responses

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17
Q

Angiotensinogen

A

A circulating protein from which renin cleaves to form angiotensin I

18
Q

What is the purpose of ACE and what are the other names associated with it?

A

It catalyzes the conversion of angiotensin I into angiotensin II

aka Peptidyl dipeptidase or Kininase II

19
Q

Pharmacologic actions of Angiotensin II

What can happen if there is excessive production?

A

Exerts profound effects in the regulation (constriction) of vascular tone, fluid and electrolyte balance.

Excessive production results in hypertension and disorders of hemodynamics.

20
Q

What are the 3 types of drugs which block the formation/action of angiotensin II?

A
  1. Drugs blocking renin secretion/action
  2. ACE inhibitors
  3. Angiotensin receptor blockers
21
Q

In addition to blocking the formation of angiotensin II, ACE inhibitors also function to block…

What can this lead to?

A

Bradykinin metabolism

This can lead to a signficant hypotensive effect, which has been reported as a severe side effect.

22
Q

Name the 2 ACE inhibitors used clinically

A
  1. Captopril
  2. Enalapril
23
Q

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

A

No

24
Q

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

A

No. Increases in bradykinin levels would lead to increased hypotension.

25
Q

Describe the steps which lead to Bradykinin formation

A

HMW kininogen is converted to Bradykinin via Plasma kallikrein.

26
Q

What is responsible for the degradation of Bradykinin to inactive fragments

A

Kininases I and II

27
Q

Activated kallikrein can generate ________ and cause profound _______________

A

Kinins; hypotension

28
Q

Why do many patients with consumption coagulapathy (DIC) develop hypotension?

A

Due to increased kallikrein production

29
Q

HMWK

A

High Molecular Weight Kininogen

It is cleaved by plasma kallikrein to generate bradykinin

30
Q

What is the role of Kinins in inflammation and pain

A

Kinins promote rubor, calor, dolar, and tumor.

31
Q

Aspirin and bradykinin

A

Aspirin is known to block the algesic effects of prostaglandins generated by bradykinin

32
Q

General effects of naturiuretic peptides

A

Diuretic and vasorelaxant

33
Q

What are Kallikreins?

A

Kallikreins are glycoprotein enzymes produced in the liver as prekallikreins and are present throughout the body.

34
Q

Fletcher factor? What factor can activate it?

A

Plasmatic prekallikrein. Promotes Coagulation process via intrinsic system. Can be activated by factor XIIa (Hageman factor).

35
Q

Name the two different types of kininogens present in the plasma?

A

Low molecular weight kininogen and HMWK

36
Q

Compare the potency of Kinins to the potency of histamine

A

Kinins are 10 times more potent than histamine

37
Q

What do kinins stimulate the release of?

A

NO and prostaglandins

38
Q

How can kinins lead to edema?

A

Kinins promote water and solution passage from the blood to extracellular fluid

39
Q

What are the 2 types of receptors which mediate the biologic actions of kinins? What is the function of each?

A

Two receptor types:

B1: predominant receptor for biologic responses of kinins

B2: drugs that block the actions of bradykinin target these receptors

40
Q

Main function of Trilats (omapatrilat, sampartilat and fasidotrilat) (3)

A
  1. Enhance vasodilation
  2. Reduce Vasoconstriction
  3. Increase Sodium excretion

Enhance levels of natriuretic peptides