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5.4 VASOACTIVE PEPTIDES
Terms in this set (31)
- block renin release
- inhibit the conversion of ANG I to ANG II
- block angiotensin AT 1 receptors
- inhibit the enzymatic action of renin
MOA of Agents/drugs that block the formation or action of Angiotensin II (4)
Clonidine and Beta-blockers
What are the agents/drugs that block renins release? (2)
Inhibits renin release by causing a centrally mediated reduction in renal sympathetic nerve activity, and it may also exert a direct intrarenal action.
Given in ER, sublingually for HTN urgency. Fast acting.
Blocks the intrarenal and extrarenal β receptors involved in the neural control of renin release
- decrease systemic vascular resistance without increasing heart rate
- they promote natriuresis
- treatment of hypertension
- decrease morbidity and mortality in heart failure and left ventricular dysfunction after myocardial infarction
- delay the progression of diabetic nephropathy
What are the effects of ACE inhibitors?
Bradykinin, Substance P, Enkephalins
ACE inhibitors inhibit the degradation of (3)
Cough and Angioedema
AEs of ACE inhibitors (2)
Fetal kidney damage
Teratogenic effect of ACE inhibitors
Peptide and Non-pepdtide
2 Classes of Angiotendin II antagonists
Peptide Angiotensin II antagonist (Partial antagonist only)
Saralasin is a
Non-peptide Angiotensin II blockers
alternative when ACE inhibitors not well tolerated
Valsartan, Losartan, Candesartan, Olmesartan, Telmisartan, Irbesratan, Eprosartan
Examples of non-peptide angiotensin II blockers
Cleavage of angiotensinogen by renin
rate-limiting step in formation of ANG II
Aliskiren is a...
system that has several features in common with the renin-angiotensin system
potent vasodilator peptide
Kinin is a...
precursors of kinins and substrates of kallikreins
Tisse and Plasma kallikreins
2 types of kallikreins
1. low molecular-weight form (LMW kininogen) - crosses capillary walls
2. high-molecularweight form (HMW kininogen) - confined to bloodstream
Kininogens (2 types)
1. substrate for tissue kallikreins
2. substrate for plasma kallikrein
s predominant kinin in plasma
1. Produce marked arteriolar dilation
2. Effects on veins - contraction (via PGF2-alpha)
3. Contraction of most visceral smooth muscle - modulate tone of salivary and pancreatic ducts; help regulate gastrointestinal motility ; local modulators of blood flow
4. development and maintenance of inflammatory processes
5. protective role in cardiovascular diseases and ischemic stroke-induced brain injury
PHYSIOLOGIC AND PATHOLOGIC EFFECTS OF KININS
second-generation kinin B2 receptor antagonist - blocks effects of kinins on pain, hyperalgesia, and inflammation
used in Hereditary angioedema
Icabitant is a...
TRIGLYCYL LYSINE VASOPRESSIN - synthetic vasopressin analog converted to lysine vasopressin in body.
- Has more selectivity for V1 receptors.
- Used in treatment for Vasodilatory shock.
TERLIPRESSIN is also known as...
Tolvaptan - currently approved only for use in hyponatremia; Selective antagonist at V2 ADH receptors
Conivaptan - both V 1a and V 2 antagonist activity; treatment of hyponatremia and congestive heart failure.
Tolvaptan and Conivaptan are drugs that acts as...
atrial stretch via mechanosensitive ion channels
most important stimulus for release of ANP
sodium excretion and urine flow
It also inhibits the release of renin, aldosterone and AVP
ATRIAL NATRIURETIC PEPTIDE (ANP) increases...
agonist of natriuretic peptide receptors
NESIRITIDE is an...
VASOPEPTIDASE INHIBITORS - drugs that combine neprilysin inhibition with ACE inhibition; simultaneously increase the levels of natriuretic peptides and decrease the formation of ANG II.
OMAPATRILAT, SAMPATRILAT , FASIDOTRILAT
DRUG THAT BLOCK ENDOTHELIN-CONVERTING ENZYME
Substance P antagonist - USE: prevention of chemotherapy-induced and postoperative nausea and vomiting
Aprepitant is a...
Prodrug that is converted to aprepitant
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