pulm HTN Flashcards
What are the Prostanoid drungs?
epoprostenol
treprostinil
iloprost
selexipag
what are the the PDE 5 inhibitors
sildenafil
tadalafil
what are the endothelin antagonists
bosentan
ambrisentan
macicentan
what are the Guanylate cyclase sensitizer
riociguat
If the patient has a positive vasopressor test what drugs to use
CCB
nifedipine
diltiazem
amlodipine
epoprostenol MOA and effects and Clinical applications
MOA: mimics endogenous prostacyclin
- promotes vascular relaxation
- suppresses growth of vascular smooth muscle
- inhibits platelet aggregation
via binding to G protein to generate cAMP
effects: lowers pulmonary arterial resistance
- decreases PHTN
- increases exercise intolerance
- improves short term survival
epoprostenol pk and toxicities
Short half life so given IV
Toxicities: sepsis due to chronic catheter
- nasuea + vomiting
- headache
- flushing
- jawpain
Treprostinil MOA, and Effects
MOA: mimics endogenous prostacyclin
- promotes vascular relaxation
- suppresses growth of vascular smooth muscle
- inhibits platelet aggregation
via binding to G protein to generate cAMP
effects: lowers pulmonary arterial resistance
- decreases PHTN
- increases exercise intolerance
- improves short term survival
Treprostinil pk and toxicities
pk: subcutaneous infusion but painful
longer half life
can be inhaled and has extended release oral
Toxicities: sepsis due to chronic catheter
- pain in injection
- nausea + vomiting
- diarrhea
- edema
-if inhaled cough, HA, throat irritation lower incidiences of nausea and dizziness and flushing
iloprost MOA and effects
MOA: mimics endogenous prostacyclin
- promotes vascular relaxation
- suppresses growth of vascular smooth muscle
- inhibits platelet aggregation
via binding to G protein to generate cAMP
effects: lowers pulmonary arterial resistance
- decreases PHTN
- increases exercise intolerance
- improves short term survival
iloprost pk and toxicities
Pk: administered by inhalation
Toxicities: Fainting due to hypotension
- cough
- headache
- flushing
- jaw pain
Selexipag MOA and Effects
MOA: mimics endogenous prostacyclin
- promotes vascular relaxation
- suppresses growth of vascular smooth muscle
- inhibits platelet aggregation
via binding to G protein to generate cAMP
effects: lowers pulmonary arterial resistance
- decreases PHTN
- increases exercise intolerance
- improves short term survival
Selexipag pk and toxicities
PK: administered orally BID
-expensive
Toxicities:
- HA
- flushing
- diarrhea, nausea, vomiting
- jaw and limb muscle pain
- skin rash
Bosentan MOA and effects
MOA: nonspecifically blocks ETa and ETb endothelin receptors
Effects: improves excercise tolerance and slows symptoms progression
Bosentan PK and toxicities
PK: oral drug and metabolized by liver
Toxicities:
- Hepatotoxicity
- teratogenesis
-headache, flushing, peripheral edema, nasal congestion, anemia and reduced sperm production
Drug interactions:
- warfarin
- oral contraceptives
Ambrisentan MOA and effects
MOA: selectively blocks ETa receptors that causes vasoconstriction and promote cell proliferation
effects: improves exercise tolerance and slows symptom progression
Ambrisentan pk and toxicities
Pk; oral drug
toxicities:
- teratogenesis
- others include peripheral edema, nasal congestion, anemia and reduced sperm production
Drug interactions:
-oral contraceptives
Macitentan
Non selective ETa and ETb agent that has a long half life but inhibits cP450
Sildenafil MOA and effects
Viagra, Revatio
MOA: Selectively blocks phosphodiesterase type V enzyme that breaks down cGMP an important intracellular mediator smooth muscle relaxation
effects: improves exercise tolerance and slows symptom progression
Slidenafil PK and toxicities:
PK: oral drug
Toxicites:
- priapism
- HA, flushing, and dyspepsia
- visual disturbances, + hearing losses
- milde hypotension
what is tadalafil
cialis, adcirca
selectively blocks phosphodiesterase type V with longer half lifw
Riociguat MOA and effects
MOA: Dual mode of action
-sensitizes soluble guanylate cyclase to endogenous NO by stabilizing NO-sGC binding
-directly stimulates sGC independant of NO and promotes vasodilation
effects:
- Improves excercise tolerance and slows symptom progression
Riociguat PK and Toxicites
PK: oral drug with long half life
Toxicities:
- hypotension, headache, dizziness and dyspepsia are among the more common significant adverse effects; rarely see severe bleeding
- Tertagonesis
- no administered wit NO or type V phosphodiesterase inhibitors
- interacts with both pg transporters and cP450
4 classes of PHTN
1 = PHTN no limitation
2= PHTN some limitation
3= PHTN marked limitation
4 =PHTN and cant carry out Physical activity
what is a common PHTN drug combination
Tadalafil and ambrisentan
