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Cardiopulm/Renal Exam 2 > Pulmonary Hypertension Drugs > Flashcards

Pulmonary Hypertension Drugs Flashcards

1
Q

Prostanoids

Epoprostenol: MOA

A

• Mimics the actions of endogenous prostacyclin, compound that

  • promotes vascular relaxation
  • suppresses growth of vascular smooth muscle cells
  • inhibits platelet aggregation

• Exerts these effects by binding to G-protein coupled receptor on cell membrane to generate cAMP

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2
Q

Prostanoids

Epoprostenol: Effects

A
  • lowers pulmonary arterial resistance
  • decreases pulmonary arterial pressure

• increases exercise
tolerance

• improves short- term survival

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3
Q

Prostanoids

Epoprostenol: Clinical Applications

A

PAH

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4
Q

Prostanoids

Epoprostenol: Pharmacokinetics

A

has very short half-life (~ 6 min) and must be given by continuous IV infusion with a pump that can keep the drug cold

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5
Q

Prostanoids

Epoprostenol: Toxicities

A

• Serious adverse effects:

  • sepsis due to chronic catheter
  • life-threatening problems if pump lines become clogged

• common side effects:

  • nausea and vomiting (32%)
  • headache (49%)
  • flushing (58%)
  • jaw pain
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6
Q

Prostanoids

Treprostinil: MOA

A

• Mimics the actions of endogenous prostacyclin, compound that

  • promotes vascular relaxation
  • suppresses growth of vascular smooth muscle cells
  • inhibits platelet aggregation

• Exerts these effects by binding to G-protein coupled receptor on cell membrane to generate cAMP

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7
Q

Prostanoids

Treprostinil: Effects

A
  • lowers pulmonary arterial resistance
  • decreases pulmonary arterial pressure

• increases exercise
tolerance

• improves short-term survival

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8
Q

Prostanoids

Treprostinil: Clinical Applications

A

PAH

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9
Q

Prostanoids

Treprostinil: Pharmacokinetics

A

• Initially approved for continuous SUBCUTANEOUS INFUSION, BUT –> PAIN
- now, often diluted 1:2 and administered with pump IV similar to epoprostenol

  • Has LONGER HALF- LIFE (~4 hrs) vs 6 min of epoprostenol, and DOESN’T REQUIRE REFRIGERATION
  • qid inhalation form is now also available
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10
Q

Prostanoids

Treprostinil: Toxicities

A

• Serious adverse effects:
- sepsis due to chronic catheter

• Common side effects: 
- site pain with subcutaneous
infusion (~85%)
- jaw pain
- diarrhea
- edema
- nausea

• if inhaled: cough (54%), headache (41%), throat irritation (25%), plus lower incidences of nausea, flushing and dizziness

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11
Q

Prostanoids

Iloprost: MOA

A

• Mimics the actions of endogenous prostacyclin, compound that

  • promotes vascular relaxation
  • suppresses growth of vascular smooth muscle cells
  • inhibits platelet aggregation

• Exerts these effects by binding to G-protein coupled receptor on cell membrane to generate cAMP

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12
Q

Prostanoids

Iloprost: Effects

A
  • lowers pulmonary arterial resistance
  • decreases pulmonary arterial pressure

• increases exercise
tolerance

• improves short- term survival

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13
Q

Prostanoids

Iloprost: Clinical Applications

A

PAH

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14
Q

Prostanoids

Iloprost: Pharmacokinetics

A

Administered by INHALATION 6-9 times per

day

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15
Q

Prostanoids

Iloprost: Toxicities

A

• Serious adverse effects:
- fainting due to hypotension (especially if SBP < 85 mm Hg)

• Common side effects:

  • cough (39%)
  • headache (30%)
  • flushing (27%)
  • jaw pain (12%)
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16
Q

Prostanoids

Selexipag: MOA

A

• Mimics the actions of endogenous prostacyclin, compound that

  • promotes vascular relaxation
  • suppresses growth of vascular smooth muscle cells
  • inhibits platelet aggregation

• Exerts these effects by binding to G-protein coupled receptor on cell membrane to generate cAMP

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17
Q

Prostanoids

Selexipag: Effects

A
  • lowers pulmonary arterial resistance
  • decreases pulmonary arterial pressure

• increases exercise
tolerance

• improves short- term survival

18
Q

Prostanoids

Selexipag: Clinical Applications

19
Q

Prostanoids

Selexipag: Pharmacokinetics **

A
  • ADMINISTERED ORALLY, BID. **

* tablets are $225 ea, $350 ea for higher doses **

20
Q

Prostanoids

Selexipag: Toxicities

A

• Common side effects:

  • headache
  • flushing
  • diarrhea, nausea, vomiting
  • jaw, limb, muscle pain
  • skin rash
21
Q

Endothelin Antagonist

Bosentan: MOA

A

NONSPECIFICALLY blocks ET(A) and ET(B) endothelin

receptors

22
Q

Endothelin Antagonist

Bosentan: Effects

A

improves exercise

tolerance and slows symptom progression

23
Q

Endothelin Antagonist

Bosentan: Clinical Application

24
Q

Endothelin Antagonist

Bosentan: Pharmacokinetics

A

• oral drug

•~50% bioavailability in
presence or absence of food

• metabolized by liver, highly
protein-bound

25
Endothelin Antagonist Bosentan: Toxicities
• Serious Adverse Effects: - hepatotoxicity (11%, potentially fatal) - teratogenesis (FDA category X) • Other Adverse Effects: - headache, flushing, peripheral edema, nasal congestion, anemia and reduced sperm production • Drug Interactions: - Accelerates metabolism - warfarin - ORAL CONTRACEPTIVES... must use 2 forms of birth control - Increases levels of many other drugs including cyclosporine or glyburide
26
Endothelin Antagonist Ambrisentan: MOA
SELECTIVELY blocks ET(A) receptors, the | receptors that cause vasoconstriction and promote cell proliferation
27
Endothelin Antagonist Ambrisentan: Effects
improves exercise | tolerance and slows symptom progression
28
Endothelin Antagonist Ambrisentan: Clinical Applications
PAH
29
Endothelin Antagonist Ambrisentan: Pharmacokinetics
Oral drug
30
Endothelin Antagonist Ambrisentan: Toxicities
• Serious adverse effects: - teratogenesis (FDA category X) - (does not damage liver) • Others include peripheral edema, nasal congestion, anemia and reduced sperm production • Drug Interactions: - Does NOT accelerate metabolism of warfarin and oral contraceptives, but still must use 2 forms of birth control
31
non-selective agent distinguished by ~18 hr half life that permits once/day dosing; cytochrome P450 effects similar to bosentan
macitentan
32
Phosphodiesterase Type V Inhibitors: Sildenafil (Viagra): MOA
SELECTIVELY BLOCKS PHOSPHODIESTERASE TYPE V, enzyme that breaks down cGMP, an important intracellular mediator of smooth muscle relaxation
33
Phosphodiesterase Type V Inhibitors: Sildenafil (Viagra): Effects
improves exercise | tolerance and slows symptom progression
34
Phosphodiesterase Type V Inhibitors: Sildenafil (Viagra): Clinical Applications
PAH
35
Phosphodiesterase Type V Inhibitors: Sildenafil (Viagra): Pharmacokinetics
oral drug, half-life ~ 4 hrs
36
Phosphodiesterase Type V Inhibitors: Sildenafil (Viagra for ED and Revatio for PAH): Toxicities
* well tolerated, with headache, flushing and dyspepsia being most common * rarely see priapism * can also rarely cause visual disturbances (e.g., lack of color discrimination) and sudden hearing loss * causes mild hypotension when used alone, but much greater drops are seen if used along with α-blockers for hypertension or nitrates for anginal pain
37
longer t1/2 than Sildenafil
Tadalafil
38
Phosphodiesterase Type V Inhibitors: Riociguat: MOA
• Dual mode of action - sensitizes soluble guanylate cyclase (sGC) to endogenous nitric oxide (NO) by stabilizing the NO-sGC binding - directly stimulates sGC independent of NO - increased generation of cGMP --> increased vasodilation
39
Phosphodiesterase Type V Inhibitors: Riociguat: Effects
improves exercise | tolerance and slows symptom progression
40
Phosphodiesterase Type V Inhibitors: Riociguat: Clinical Applications
PAH, also type 4 PH
41
Phosphodiesterase Type V Inhibitors: Riociguat: Pharmacokinetics
oral drug, half-life in | patients of ~ 12 hrs
42
Phosphodiesterase Type V Inhibitors: Riociguat: Toxicities
* hypotension, headache, dizziness and dyspepsia are among the more common significant adverse effects; rarely see severe bleeding * may cause fetal harm, so only available to women with negative pregnancy test and should avoid pregnancy for 1 month after stopping * should not be administered with nitric oxide donors or type V phosphodiesterase inhibitors * multiple potential drug interactions at both transporters and cytochrome P450

Cardiopulm/Renal Exam 2 (3 decks)

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