Pulmonary Hypertension Drugs

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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:
- Nifedipine
- Amlodipine
- Diltiazem
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?

Oral
What are adverse effects for CCB
- Hypotension
- Peripheral edema
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
- Prostacyclin analog
What is ET-1 recetpr?

A potent vasoconstrictor
Is bosentan a selecteive blocker of ET-1 receptors?

No, nonselevtive
Which receptor is Ambrisentan selective for?

ETa
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

True
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?

Macitentan
What is the therapeutic use for ET-1 receptor antagonist?

Pulmonary hypertension
What is the route of administration for ET-1 receptor antagonist?

Oral
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
- Peripheral edema
- Hepatotoxicity
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?

Pregnancy
What are 2 agents of PDE5 inhibitor?
- Sildenafil
- Tadalafil
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
- Oral
- Iv
What are adverse effects for Sildenafil?
- Flushing
- Headache
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?

Oral
What are adverse effects of riociguat?
- Embryo-fetal toxicity
- Hypotension
- Bleeding
What are contraindications for riociguat?
- Pregnancy
- Nitrates
- PDE inhibitors
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?
- Epoprostenol
- Iloprost
- Treprostinil
What is the route of administration for epoproostenol?

IV
What is the route of administration for trepostinil?

IV, SQ, inhalation, oral
What is the route of administration for iloprost?

Inhalation
What are adverse effects for IV prostacyclin analogs?
- Flushing
- Headache
- Diarrhea
- Infusion site pain (esp trepostinil)
What are adverse effects for inhaled prostacyclin analogs?
- Flushing
- Jaw pain
What are some IV prostacyclin analogs?
- Epoprostenol
- Trepostinil
What are inhaled prostacyclin analog?
- Iloprost
- trepostinil
What is an oral prostacyclin analog?

Trepostinil
What is a SQ prostacyclin analog?

Trepostinil

Author

lykthrnn

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Card Set

Pulmonary Hypertension Drugs

Description

Pulmonary Midterm

Updated

2019-02-15T05:05:35Z

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