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Pharmacology- Katzung (Spring 2019) > Vasoactive peptides (Katzung) > Flashcards

Vasoactive peptides (Katzung) Flashcards

1
Q

Renin Release Blockers

A

Clonidine

Propranolol

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2
Q

Renin Release Blockers - Effects

A

Arteriolar dilation
Decreased aldosterone secretion
Increased sodium and water excretion

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3
Q

Renin Release Blockers - Clinical use

A

Hypertension

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4
Q

Clonidine - MoA

A

Causing a centrally mediated reduction in renal sympathetic nerve activity, and it may also exert a direct intrarenal action.

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5
Q

Propranolol - MoA

A

Blocking the intrarenal and extrarenal β receptors involved in the neural control of renin release.

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6
Q

Angiotensin Receptor Antagonists

A 
Losartan
Valsartan
Eprosartan
Irbesartan
Candasartan
Olmesatran
Telmisartan
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7
Q

Angiotensin Receptor Antagonists - MoA

A

Selective competitive antagonist of angiotensin AT1 receptors

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8
Q

Angiotensin Receptor Antagonists - Effects

A

Arteriolar dilation
Decreased aldosterone secretion
Increased sodium and water excretion

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9
Q

Angiotensin Receptor Antagonists - Clinical use

A

Hypertension
Diabetic nephropathy
Heart failure (Alternative when ACE inhibitors are not tolerated)
Combination therapy with an ACE inhibitor

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10
Q

Angiotensin Receptor Antagonists - Adverse effects and Contraindication

A

Cough (low incidence)
Sprue-like enteropathy

Contraindication: Nondiabetic renal disease and pregnancy

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11
Q

Losartan - Clinical use

A

Marfan syndrome (By blocking ANG II, which decrease TGF-β, which is usually increased in Marfan syndrome)

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12
Q

Valsartan - Clinical use

A

Decrease the incidence of diabetes in patients with impaired glucose tolerance.

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13
Q

Angiotensin-Converting Enzyme Inhibitors

A

Enalapril

Captopril

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14
Q

Angiotensin-Converting Enzyme Inhibitors - MoA

A

Inhibits conversion of angiotensin I to angiotensin II

They also inhibit the degradation of other substances, including bradykinin, substance P, and enkephalins.

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15
Q

Angiotensin-Converting Enzyme Inhibitors - Effects

A

Arteriolar dilation
Decreased aldosterone secretion
Increased sodium and water excretion

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16
Q

Angiotensin-Converting Enzyme Inhibitors - Clinical use

A

Hypertension
Heart failure
Left Ventricular dysfunction
Diabetic nephropathy

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17
Q

Angiotensin-Converting Enzyme Inhibitors - Adverse effects and Contraindications

A

Cough
Angioedema

Contraindications: Pregnancy because they cause fetal kidney damage.

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18
Q

Renin Inhibitors

A

Aliskiren

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19
Q

Renin Inhibitors - MoA

A

Inhibits plasma renin activity

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20
Q

Renin Inhibitors - Effects

A

Arteriolar dilation
Decreased aldosterone secretion
Increased sodium and water excretion

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21
Q

Renin Inhibitors - Clinical use

A

Hypertension

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22
Q

Aliskiren - Contraindication

A

Pregnancy

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23
Q

Kinin Inhibitors

A

Icatibant
Ecallantide
Cinryze, Berinert
Aprotinin

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24
Q

Kinin Inhibitors - MoA

A

Selective antagonist of kinin B2 receptors

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25
Q

Kinin Inhibitors - Effects

A

Blocks effects of kinins on pain, hyperalgesia, and inflammation

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26
Q

Kinin Inhibitors - Clinical use

A

Hereditary angioedema

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27
Q

Icatibant - Clinical use

A 
Drug-induced angioedema
Airway disease
Thermal injury
Ascites
Pancreatitis
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28
Q

Which kinin inhibitor is a plasma kallikrein inhibitor

A

Ecallantide

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29
Q

Which kinin inhibitor is a kinin synthesis inhibitor

A

Aprotinin

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30
Q

Vasopressin Agonists

A

Arginine vasopressin
Terlipressin
Selepressin

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31
Q

Vasopressin Agonists - MoA

A

Agonist of vasopressin V1 (and V2) receptors

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32
Q

Vasopressin Agonists - Effects

A

Vasoconstriction

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33
Q

Vasopressin Agonists - Clinical use

A

Vasodilatory shock

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34
Q

Arginine vasopressin - MoA

A

Selective V2 antidiuretic analog

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35
Q

Terlipressin - MoA

A

More selective for V1 receptor but also stimulate V2 receptors

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36
Q

Selepressin - MoA

A

Selective V1a receptor agonist

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37
Q

Selepressin - Clinical use

A

Septic shock

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38
Q

Vasopressin Antagonists

A

Conivaptan
Relcovaptan
Tolvaptan

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39
Q

Vasopressin Antagonists - MoA

A

Antagonist of vasopressin V1 (and V2) receptors

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40
Q

Vasopressin Antagonists - Effects

A

Vasodilation

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41
Q

Vasopressin Antagonists - Clinical use

A

Potential use in Raynaud`s disease, hypertension, heart failure, brain edema and hyponatremia

42
Q

Conivaptan - MoA

A

Selective V1 receptor antagonist

43
Q

Relcovaptan - MoA

A

V1 and V2 receptor antagonist

44
Q

Tolvaptan - MoA

A

V2 receptor antagonist

45
Q

Natriuretic Peptides

A

Carperitide
Nesiritide
Uraritide

46
Q

Natriuretic Peptides - MoA

A

Agonist of natriuretic peptide receptors

47
Q

Natriuretic Peptides - Effects

A

Increased sodium and water excretion

Vasodilation

48
Q

Natriuretic Peptides - Clinical use

A

Heart failure

49
Q

Carperitide - MoA

A

Recombinant ANP

50
Q

Nesiritide - MoA

A

Recombinant BNP

51
Q

Vasopeptidase Inhibitors

A

Omapatrilat
Sampatrilat
Fasidotrilat

52
Q

Vasopeptidase Inhibitors - MoA

A

Inhibit Neprilysin and ACE

53
Q

Vasopeptidase Inhibitors - Effects

A

Vasodilation

Increased sodium and water excretion

54
Q

Vasopeptidase Inhibitors - Clinical use

A

Hypertension

Heart failure

55
Q

Endothelin Antagonists

A

Bosentan
Sitaxsentan
Ambrisentan
Phosphoramidon

56
Q

Endothelin Antagonists - MoA

A

Nonselective antagonist of endothelin ETA and ETB receptors

57
Q

Endothelin Antagonists - Effects

A

Vasodilation and decreased arterial pressure

58
Q

Endothelin Antagonists - Clinical use

A

Pulmonary arterial hypertension

Other conditions (Although not very effective):
Resistant hypertension
Chronic renal disease
Connective tissue disease
Subarachnoid hemorrhage
59
Q

Endothelin Antagonists - Adverse effects

A 
Dose-dependent hepatotoxicity
Systemic hypotension
Increased heart rate
Facial flushing or edema
Headaches
GI effects
60
Q

Endothelin Antagonists - Contraindications

A

Pregnancy because of teratogenic effects

61
Q

Bosentan - MoA

A

Nonselective antagonist of endothelin ETA and ETB receptors

62
Q

Bosentan - Adverse effects

A

Fatal hepatotoxicity (Patients should have monthly liver functions test)

63
Q

Sitaxsentan, Ambrisentan - MoA

A

Selective for ETA receptors

64
Q

Phosphoramidon - MoA

A

Block formation of endothelins by inhibiting endothelin-converting enzyme

65
Q

Vasoactive Intestinal Peptide Agonists

A

PB1046 (Vasomera)

66
Q

Vasoactive Intestinal Peptide Agonists - MoA

A

Agonist of VPAC1 and VPAC2 receptors

67
Q

Vasoactive Intestinal Peptide Agonists - Effects

A

Smooth muscle relaxation and vasodilation

Multiple metabolic, endocrine, and other effects

68
Q

Vasoactive Intestinal Peptide Agonists - Clinical use

A

Systemic and pulmonary hypertension and Heart failure

69
Q

Vasoactive Intestinal Peptide Agonists - Adverse effects

A

Hypotension

70
Q

PB1046 (Vasomera) - MoA

A

Long-acting selective VPAC2 receptor agonist

71
Q

PB1046 (Vasomera) - Effects

A

Reduces blood pressure

72
Q

Substance P Antagonists

A

Aprepitant

Fosaprepitant

73
Q

Substance P Antagonists - MoA

A

Selective antagonist of tachykinin NK1 receptors

74
Q

Substance P Antagonists - Effects

A

Blocks several central nervous system effects of substance P

75
Q

Substance P Antagonists - Clinical use

A

Prevention of chemotherapy- induced and postoperative nausea and vomiting, as well as Depression and Cancer

76
Q

Neurotensin Agonists

77
Q

Neurotensin Agonists - MoA

A

Agonist of central neurotensin receptors

78
Q

Neurotensin Agonists - Effects

A

Interacts with central dopamine systems

79
Q

Neurotensin Agonists - Clinical use

A

Potential for treatment of schizophrenia and Parkinson’s disease

80
Q

Neurotensin Agonists - Adverse effects

A

Hypothermia and Hypotension

81
Q

Neurotensin Antagonists

A

Meclinertant

82
Q

Neurotensin Antagonists - MoA

A

Antagonist of central and peripheral neurotensin receptors

83
Q

Neurotensin Antagonists - Effects

A

Blocks some central and peripheral (vasodilator) actions of neurotensin

84
Q

Neurotensin Antagonists - Clinical use

A

None identified

85
Q

Calcitonin Gene-Related Peptide Antagonists

A

Telcagepant

Olcegepant

86
Q

Calcitonin Gene-Related Peptide Antagonists - MoA

A

Antagonists of the calcitonin gene-related peptide (CGRP) receptor

87
Q

Calcitonin Gene-Related Peptide Antagonists - Effects

A

Blocks some central and peripheral (vasodilator) actions of CGRP

88
Q

Calcitonin Gene-Related Peptide Antagonists - Clinical use

89
Q

Telcagepant - Adverse effects

A

Liver toxicity

90
Q

Neuropeptide Y Antagonists

A

BIBP3226
BIIE0246
MK-0557

91
Q

Neuropeptide Y Antagonists - MoA

A

Selective antagonist of neuropeptide Y1 receptors

92
Q

Neuropeptide Y Antagonists - Effects

A

Blocks vasoconstrictor response to NPY

93
Q

Neuropeptide Y Antagonists - Clinical use

A

Potential Antiobesity agent

94
Q

BIIE0246 - MoA

A

Selective for Y2 receptor

95
Q

MK-0557 - MoA

A

Selective for Y5 receptor

96
Q

Urotensin Antagonist

A

Urantide

Palosuran

97
Q

Urotensin Antagonist - MoA

A

Antagonist of urotensin receptors

98
Q

Urotensin Antagonist - Effects

A

Blocks vasoconstrictor action of urotensin

99
Q

Urotensin Antagonist - Clinical use

A

Beneficial in renal failure

-Not in hypertensive patients with type 2 diabetic nephropathy

100
Q

Palosuran - Clinical use

A

Diabetic renal failure

Pharmacology- Katzung (Spring 2019) (52 decks)

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