Pulmonary Hypertension Drugs
What determines whether a patient can be on calcium channel blockers to treat pulmonary hypertension?
If he/she responds to acute vasoreactive test
What is vasoreactive testing?
Helps identify patients that may benefit from CCB
Name 3 CCB agents:
What is the mechanism of action for calcium channel blocker?
decrease influx of Ca2+ L type
What is the therapeutic indication for CCB?
Pulmonary hypertension in vasoreactive patients
What is the route of administration for CCB?
What are adverse effects for CCB
What is a contraindication for CCB?
Significant right heart failure
What are treatment options when patient does not respond to vasoreactive test?
Endothelin receptor antagonist
PDE 5 inhibitor
What is ET-1 recetpr?
A potent vasoconstrictor
Is bosentan a selecteive blocker of ET-1 receptors?
Which receptor is Ambrisentan selective for?
True/False: Endothelin-1 can bind onto ETb on endothelial cell and would lead to release of NO and resulting in vascular smooth muscle cell relaxation
What is the effect of Endothelin-1 binding to ETa and ETb receptors on smooth muscle cell?
Smooth muscle cell contraction
What is the effect of endothelin-1 binding to ETb receptor on endothelial cell?
Ultimately lead to smooth muscle cell relaxation
Which ET-1 receptor antagonist is most efficacious and safe?
What is the therapeutic use for ET-1 receptor antagonist?
What is the route of administration for ET-1 receptor antagonist?
What other cellular component might ET-1 receptor antagonist have an effect on?
Induce CYP3A4 and CYP2CP- could metabolize other drugs sooner
What are adverse effects of ET-1 receptor antagonist
What is a required test that patients on ET-1 receptor antagonists must do on a monthly basis?
Liver function test
What is a contraindication for ET-1 receptor antagonist?
What are 2 agents of PDE5 inhibitor?
What is the biochemical effect of PDE5 inhibitor use?
Would degrade PDE 5 (PDE 5 degrades cGMP; cGMP allows for smooth muscle relaxation), which would ultimately lead to smooth muscle cell relaxation
What is the route of administration for Sildenafil?
Powder for suspension
What are adverse effects for Sildenafil?
What is a contraindication for Sildenafil?
Nitrate use – otherwise could lead to hypotension
What is the mechanism of action for riociguat?
Stimulate soluble guanylate cyclase
What is the route of administration of riociguat?
What are adverse effects of riociguat?
What are contraindications for riociguat?
What is the mechanism of action for prostacyclin analogs?
Bind prostacyclin receptor enhance adenyl cyclase decrease intracellular Ca2+ -> vascular relaxation
What are 3 agents of prostacyclin analogs?
What is the route of administration for epoproostenol?
What is the route of administration for trepostinil?
IV, SQ, inhalation, oral
What is the route of administration for iloprost?
What are adverse effects for IV prostacyclin analogs?
Infusion site pain (esp trepostinil)
What are adverse effects for inhaled prostacyclin analogs?
What are some IV prostacyclin analogs?
What are inhaled prostacyclin analog?
What is an oral prostacyclin analog?
What is a SQ prostacyclin analog?
Pulmonary Hypertension Drugs