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

Vasoactive peptides (Katzung) COPY 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
Kinin Inhibitors - Effects
Blocks effects of kinins on pain, hyperalgesia, and inflammation
26
Kinin Inhibitors - Clinical use
Hereditary angioedema
27
Icatibant - Clinical use
``` Drug-induced angioedema Airway disease Thermal injury Ascites Pancreatitis ```
28
Which kinin inhibitor is a plasma kallikrein inhibitor
Ecallantide
29
Which kinin inhibitor is a kinin synthesis inhibitor
Aprotinin
30
Vasopressin Agonists
Arginine vasopressin Terlipressin Selepressin
31
Vasopressin Agonists - MoA
Agonist of vasopressin V1 (and V2) receptors
32
Vasopressin Agonists - Effects
Vasoconstriction
33
Vasopressin Agonists - Clinical use
Vasodilatory shock
34
Arginine vasopressin - MoA
Selective V2 antidiuretic analog
35
Terlipressin - MoA
More selective for V1 receptor but also stimulate V2 receptors
36
Selepressin - MoA
Selective V1a receptor agonist
37
Selepressin - Clinical use
Septic shock
38
Vasopressin Antagonists
Conivaptan Relcovaptan Tolvaptan
39
Vasopressin Antagonists - MoA
Antagonist of vasopressin V1 (and V2) receptors
40
Vasopressin Antagonists - Effects
Vasodilation
41
Vasopressin Antagonists - Clinical use
Potential use in Raynaud`s disease, hypertension, heart failure, brain edema and hyponatremia
42
Conivaptan - MoA
Selective V1 receptor antagonist
43
Relcovaptan - MoA
V1 and V2 receptor antagonist
44
Tolvaptan - MoA
V2 receptor antagonist
45
Natriuretic Peptides
Carperitide Nesiritide Uraritide
46
Natriuretic Peptides - MoA
Agonist of natriuretic peptide receptors
47
Natriuretic Peptides - Effects
Increased sodium and water excretion | Vasodilation
48
Natriuretic Peptides - Clinical use
Heart failure
49
Carperitide - MoA
Recombinant ANP
50
Nesiritide - MoA
Recombinant BNP
51
Vasopeptidase Inhibitors
Omapatrilat Sampatrilat Fasidotrilat
52
Vasopeptidase Inhibitors - MoA
Inhibit Neprilysin and ACE
53
Vasopeptidase Inhibitors - Effects
Vasodilation | Increased sodium and water excretion
54
Vasopeptidase Inhibitors - Clinical use
Hypertension | Heart failure
55
Endothelin Antagonists
Bosentan Sitaxsentan Ambrisentan Phosphoramidon
56
Endothelin Antagonists - MoA
Nonselective antagonist of endothelin ETA and ETB receptors
57
Endothelin Antagonists - Effects
Vasodilation and decreased arterial pressure
58
Endothelin Antagonists - Clinical use
Pulmonary arterial hypertension ``` Other conditions (Although not very effective): Resistant hypertension Chronic renal disease Connective tissue disease Subarachnoid hemorrhage ```
59
Endothelin Antagonists - Adverse effects
``` Dose-dependent hepatotoxicity Systemic hypotension Increased heart rate Facial flushing or edema Headaches GI effects ```
60
Endothelin Antagonists - Contraindications
Pregnancy because of teratogenic effects
61
Bosentan - MoA
Nonselective antagonist of endothelin ETA and ETB receptors
62
Bosentan - Adverse effects
Fatal hepatotoxicity (Patients should have monthly liver functions test)
63
Sitaxsentan, Ambrisentan - MoA
Selective for ETA receptors
64
Phosphoramidon - MoA
Block formation of endothelins by inhibiting endothelin-converting enzyme
65
Vasoactive Intestinal Peptide Agonists
PB1046 (Vasomera)
66
Vasoactive Intestinal Peptide Agonists - MoA
Agonist of VPAC1 and VPAC2 receptors
67
Vasoactive Intestinal Peptide Agonists - Effects
Smooth muscle relaxation and vasodilation | Multiple metabolic, endocrine, and other effects
68
Vasoactive Intestinal Peptide Agonists - Clinical use
Systemic and pulmonary hypertension and Heart failure
69
Vasoactive Intestinal Peptide Agonists - Adverse effects
Hypotension
70
PB1046 (Vasomera) - MoA
Long-acting selective VPAC2 receptor agonist
71
PB1046 (Vasomera) - Effects
Reduces blood pressure
72
Substance P Antagonists
Aprepitant | Fosaprepitant
73
Substance P Antagonists - MoA
Selective antagonist of tachykinin NK1 receptors
74
Substance P Antagonists - Effects
Blocks several central nervous system effects of substance P
75
Substance P Antagonists - Clinical use
Prevention of chemotherapy- induced and postoperative nausea and vomiting, as well as Depression and Cancer
76
Neurotensin Agonists
PD149163
77
Neurotensin Agonists - MoA
Agonist of central neurotensin receptors
78
Neurotensin Agonists - Effects
Interacts with central dopamine systems
79
Neurotensin Agonists - Clinical use
Potential for treatment of schizophrenia and Parkinson’s disease
80
Neurotensin Agonists - Adverse effects
Hypothermia and Hypotension
81
Neurotensin Antagonists
Meclinertant
82
Neurotensin Antagonists - MoA
Antagonist of central and peripheral neurotensin receptors
83
Neurotensin Antagonists - Effects
Blocks some central and peripheral (vasodilator) actions of neurotensin
84
Neurotensin Antagonists - Clinical use
None identified
85
Calcitonin Gene-Related Peptide Antagonists
Telcagepant | Olcegepant
86
Calcitonin Gene-Related Peptide Antagonists - MoA
Antagonists of the calcitonin gene-related peptide (CGRP) receptor
87
Calcitonin Gene-Related Peptide Antagonists - Effects
Blocks some central and peripheral (vasodilator) actions of CGRP
88
Calcitonin Gene-Related Peptide Antagonists - Clinical use
Migraine
89
Telcagepant - Adverse effects
Liver toxicity
90
Neuropeptide Y Antagonists
BIBP3226 BIIE0246 MK-0557
91
Neuropeptide Y Antagonists - MoA
Selective antagonist of neuropeptide Y1 receptors
92
Neuropeptide Y Antagonists - Effects
Blocks vasoconstrictor response to NPY
93
Neuropeptide Y Antagonists - Clinical use
Potential Antiobesity agent
94
BIIE0246 - MoA
Selective for Y2 receptor
95
MK-0557 - MoA
Selective for Y5 receptor
96
Urotensin Antagonist
Urantide | Palosuran
97
Urotensin Antagonist - MoA
Antagonist of urotensin receptors
98
Urotensin Antagonist - Effects
Blocks vasoconstrictor action of urotensin
99
Urotensin Antagonist - Clinical use
Beneficial in renal failure | -Not in hypertensive patients with type 2 diabetic nephropathy
100
Palosuran - Clinical use
Diabetic renal failure

Pharmacology- Katzung (Spring 2019) (52 decks)

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