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Therapeutics
Pulmonary
23
Pharmacology
Professional
04/12/2017

Additional Pharmacology Flashcards

 


 

Cards

Term
Prostacyclin (PGI-2) on smooth muscle cells
Definition
causes muscle relaxation, vasodilation, inhibits muscle proliferation
Term
PGI-2 on platelets
Definition
inhibits platelet aggregation
Term
Thromboxane A2
Definition
produced by activated platelets as well as endothelial cells
Term
Thromboxane A2 on smooth muscle cells
Definition
results in contraction
Term
Thromboxane A2 on platelets
Definition
causes aggregation
Term
Prostacyclin drugs
Definition
Epoprostenol, Treprostinil, Iloprost
Term
Epoprostenol
Definition
only drug shown to improve mortality
short t1/2, lack of stability, given as continuous infusion, expensive
SE: HA, Flushing, jaw pain, diarrhea
Term
Treprostinil
Definition
longer t1/2, stable at rt, given IV or subQ,
4x/day, indicated for less severe PAH
Term
Oral Treprostinil
Definition
Only approved as monotherapy in treatment-naive patients with PAH
Term
Iloprost
Definition
synthetic analog, inhalation, short t1/2
6-9x/day, causes CG & bronchoconstriction becuase it sensitizes airway sensory nerves
Term
Non-Prostanoid
Definition
Selexipag
Term
Selexipag
Definition
longer t1/2 7.9 hrs
SE: HA,Diarrhea, Nausea
Term
Endothelin receptor A
(ET-A)
Definition
mainly expressed in Pulmonary vascular smooth muscles, contribute to ET-1 induced contraction and proleferation
Term
Endothelin receptor B
(ET-B)
Definition
expressed in endothelial cells
lead to ET-1 clearance and vasodilation
Term
ET-A AND ET-B
Definition
both expressed on smooth muscle cells but ET-A dominates
Term
ET-1 Antagonist
Definition
Bosentan, Ambrisentan, Macitentan
Term
Bosentan
Definition
Non selective antagonist, improves mortality, abnormal liver function test, potential teratogenic,
improve 6 min walk test
Term
Ambrisentan
Definition
selective for ET-A, low risk for liver toxicity and drug-drug interaction, peripheral edema. teratogenic
Term
Macitentan
Definition
non selective antagonist, anemia, low liver toxicity, teratogenic and contraindicated in pregnancy
Term
Nitric oxide Agents
PDE5-I
Definition
Sildenafil, Tadalafil
Term
Sildenafil
Definition
elevate cGAMP, vasodilatory, antiproliferative effects
IV injection and oral (20mg 3x/day lower than erectile dysfunction dose)
Term
Tadalafil
Definition
t1/2-17.5 hrs, 1x/day,elevate cGAMP, vasodilatory, antiproliferative effects
improve 6min walk test
Term
Riociguat
Definition
stimulates soluble Guanylate cyclase
oral 3x/day, combining with PDE5-I is potentially harmful
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