Vasodilators II

Question 1

Organic Nitrates - Hydralazine

dilates arterioles ___ Mechanism not clear
- interferes with release of ___ from ER
- may also prevent ___ of NO

given PO or IV
- can induce a ___ -like syndrome

Combined with ___ in BiDil
- ___ activity potentiates vasodilatory activity of ___. BiDil decreases mortality in ___with CHF

Answer 1

• preferentially
• Ca2+
• oxidation
• lupus
• ISDN
• antioxidant, ISDN, african americans

Question 2

Natrecor (nesiritide)
- given ___
- in acutely decompensated HF
- binds to and activates ___ bound ___ cyclase in vascular smooth muscle and endothelial cells
- synthesized and secreted from ___ muscle in response to increased blood ___

Answer 2

• IV
• HF
• membrane, guanylate volume
• heart

Question 3

Sacubitril
combined with ARB, ___ , (Entresto) ARNI
- PO ___ daily
- ___ activated by esterases
- prevents breakdown of ___, enhancing its action (and angiotensin II and bradykinin)
- not used with ___ inhbitors
- use to treat ___ both (HFrEF and HFpEF)

Answer 3

• valsartan
• twice
• prodrug
• BNP
• ACE
• HF

Question 4

cAMP Phosphodiesterase Inhbitors

Amrinone/Milrinone

Question 5

cGMP Phosphodiesterase Inhibitors

sildenafil is a potent and specific inhibitor of CGMP PDE5
10 fold selectivity over PDE 6 (retina)
bluish vsion
4000 fold selectivity over inhibition of PDE (CV)
lack of systemic vasodilation

Question 6

Selective PDE 5 inhibitors

contraindicated: any PDE5 inhibitor with organic nitrates

Question 7

Endothelin signaling - increased in PAH

Question 8

Vasoconstrictor antagonists

bosentan (Tracleer) and macitentan (Opsumit)

ambrisentan (Letaris)

Question 9

Vasodilators - Prostacyclin analogs

Relax pulmonary vascular SM

Question 10

Allosteric Activator of sGC

riociguant (Adempas)
for pulmonsry hypertension
-potentiaites the efect of NO
stimulated sGC activity allosterically
increases cGMP concentrationin vascular smooth muscle

Question 11

Selective PDE 5 inhibitors