2023-10-21T22:30:59+03:00[Europe/Moscow] en true <p>sustained vasoconstriction, vascular remodeling, in situ thrombosis </p>, <p>prostacyclin, NO</p>, <p>cGMP; cAMP</p>, <p>ET-1 </p>, <p>sildenafil, tadalafil </p>, <p>-Prost suffix</p>, <p>selexipag </p>, <p>entan- suffix</p>, <p>activates sGC---activating cGMP pathway, causing vasodilation and inhibition of proliferation</p>, <p>neonates, PAH diagnosis </p>, <p>CYP3A4/2C9</p>, <p>f; selective for PDE5</p>, <p>b</p>, <p>a</p>, <p>c</p>, <p>c</p>, <p>localized actions; short half-lives</p>, <p>relax smooth muscle, inhibit platelet aggregation, increase BF &amp; GFR in kidney</p>, <p>decrease CA influx-prevent contraction; inhibit myosin light chain-relaxation; inhibit signaling cascades-antiproliferation </p>, <p>b</p>, <p>a</p>, <p>a</p>, <p>c</p>, <p>mitogen </p>, <p>a</p>, <p>b</p>, <p>a</p>, <p>a</p>, <p>b,c</p>, <p>b</p>, <p>pregnancy; teratogenic </p>, <p>c</p>, <p>activin signaling inhibitor; reverses vascular remodeling </p>, <p>TGF-B induces fibroblast/myofibroblast proliferation; causes ECM deposition that leads to scarred lung tissue </p>, <p>inhibits TGF-B, TNF-a, &amp; IL-1B</p>, <p>inhibits receptor Tyr-K by binding to ATP pocket; inhibits VEGFR and FGFR</p> flashcards
Pharmacology of PAH & Fibrosis

Pharmacology of PAH & Fibrosis

  • sustained vasoconstriction, vascular remodeling, in situ thrombosis

    What are the mechanisms of PAH? (3)

  • prostacyclin, NO

    Which mediators induce vasodilation? (2)

  • cGMP; cAMP

    NO produces ________ & PGI2 produces ________; both of which result in vasodilation.

  • ET-1

    What is the most potent vasoconstrictor?

  • sildenafil, tadalafil

    What are the PDE5 inhibitors? (2)

  • -Prost suffix

    What are the prostacyclin analogs?

  • selexipag

    What is the prostacyclin agonist?

  • entan- suffix

    What are the Endothelin receptor antagonists?

  • activates sGC---activating cGMP pathway, causing vasodilation and inhibition of proliferation

    Inhaled NO MOA?

  • neonates, PAH diagnosis

    Who is Inhaled NO indicated for? (2)

  • CYP3A4/2C9

    Which enzymes metabolize PDE5 inhibitors? (2)

  • f; selective for PDE5

    Sildenafil is a nonselective inhibitor of PDE5. T/F?

  • b

    Which can cause blue-green tinting of vision?

    a) tadalafil

    b) sildenafil

    c) riociguat

    d) inhaled NO

  • a

    Which has a longer half-life?

    a) tadalafil

    b) sildenafil

  • c

    Which stimulates sGC independently of NO?

    a) tadalafil

    b) sildenafil

    c) riociguat

    d) inhaled NO

  • c

    Which has a BBW for embryo-fetal toxicity?

    a) tadalafil

    b) sildenafil

    c) riociguat

    d) inhaled NO

  • localized actions; short half-lives

    Prostacyclins have ________ & _________.

  • relax smooth muscle, inhibit platelet aggregation, increase BF & GFR in kidney

    What are the physiological effects of Prostacyclin (PGI2)? (3)

  • decrease CA influx-prevent contraction; inhibit myosin light chain-relaxation; inhibit signaling cascades-antiproliferation

    Prostacyclin agonists MOA? (3)

  • b

    Which is inhaled?

    a) selexipag

    b) Illoprost

    c) Epoprostenol

    d) Treprostinil

  • a

    Which is a prodrug?

    a) selexipag

    b) Illoprost

    c) Epoprostenol

    d) Treprostinil

  • a

    Which has the longest half-life?

    a) selexipag

    b) Illoprost

    c) Epoprostenol

    d) Treprostinil

  • c

    Which is a synthetic PGI2?

    a) selexipag

    b) Illoprost

    c) Epoprostenol

    d) Treprostinil

  • mitogen

    -a small bioactive protein or peptide that induces a cell to begin cell division,

    or enhances the rate of division (mitosis)

  • a

    Primarily located on Vascular smooth muscle.

    a) ET-A

    b) ET-B

  • b

    Primarily located on endothelial cells.

    a) ET-A

    b) ET-B

  • a

    Which is most dominant?

    a) ET-A

    b) ET-B

  • a

    Which is more selective for ET-A?

    a) Ambrisentan

    b) Macitentan

    c) Bosentan

  • b,c

    Which are equally selective for ET-A & ET-B?

    a) Ambrisentan

    b) Macitentan

    c) Bosentan

  • b

    Which has increased lipophilicity & receptor affinity?

    a) Ambrisentan

    b) Macitentan

    c) Bosentan

  • pregnancy; teratogenic

    The Endothelin Receptor Antagonists are contraindicated in ________

    because of their _______ effects.

  • c

    Which has the worst hepatotoxicity?

    a) Ambrisentan

    b) Macitentan

    c) Bosentan

  • activin signaling inhibitor; reverses vascular remodeling

    Sotatercept MOA?

  • TGF-B induces fibroblast/myofibroblast proliferation; causes ECM deposition that leads to scarred lung tissue

    How does Pulmonary Fibrosis occur? (2)

  • inhibits TGF-B, TNF-a, & IL-1B

    Pirfenidone MOA?

  • inhibits receptor Tyr-K by binding to ATP pocket; inhibits VEGFR and FGFR

    Nintedenaib MOA?