Drugs for Pulmonary HTN Flashcards

1
Q

Drugs in prostanoid class

A
  • epoprostenol
  • treprostinil
  • iloprost
  • selexipag
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2
Q

MOA prostanoids

A

mimics endogenous prostacyclin to cause vascular relaxation, decrease growth of vascular smooth muscle, and inhibit platelet aggregation

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3
Q

describe epoprostenol

A
  • prostanoid
  • short 1/2 life (6 min)
  • need to give in continuous IV that keeps the bag cold
  • risk of sepsis due to indwelling catheter
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4
Q

describe treprostinil

A
  • prostanoid
  • given subcutaneously
  • longer 1/2 life and no need for refrigeration (like epoprostenol)
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5
Q

describe iloprost

A
  • prostanoid

- given by inhalation 6-9x per day

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6
Q

describe selexipag

A
  • prostanoid
  • given orally; BID
  • EXPENSIVE $225- $350 each dose
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7
Q

What are the endothelin antagonists?

A
  • Bosentan
  • Ambrisentan
  • Macitentan
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8
Q

describe Bosetan

A
  • endothelin antagonist
  • blocks ETa/ETb receptor
  • improves exercise tolerance
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9
Q

side effects Bosetan

A
  • hepatotoxicity
  • teratogenesis
  • BAD w/ oral contraceptive
  • accelerates warfarin metabolism
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10
Q

describe Ambrisentan

A
  • endothelin antagonist
  • blocks ETa receptor
  • teratogen
  • no change in warfarin metabolism
  • still need to use 2 forms of contraceptives
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11
Q

describe Macitentan

A
  • endothelin antagonist
  • non selective agent
  • take 1x per day (long 1/2 life)
  • teratogen
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12
Q

What is a concern for all endothelin receptor blockers

A

teratogenesis

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13
Q

MOA PDE 5 inhibitors

A

block conversion cGMP –> 5’ GMP to promote vascular relaxation

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14
Q

PDE5 inhibitors used for pulmonary HTN

A
  • Sildenafil (viagra)

- Tadalafil (cialis)

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15
Q

benefits of using PDE5 inhibitors in pulmonary HTN

A

improve exercise tolerance and slow Sx progression

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16
Q

MOA guanylate cyclase sensitizer

A

sensitizes soluble guanylate cyclase (sGC) to endogenous nitric oxide by stabilizing NO-sGC binging
(increased cGMP means increased vasodilation)

17
Q

describe Riociguat

A
  • guanylate cyclase sensitizer
  • may cause fetal harm
  • may interact with drugs at CYP450
18
Q

definition pulmonary HTN

A

MAP >25 mmHg at rest

19
Q

Who is pulmonary HTN common in?

A

young mothers, but more common in females of any age

20
Q

Pulmonary artery changes in PAH

A

1) vasoconstriction
2) inflammation
3) localized thrombus formation
4) obstructive remodeling of vessel wall

21
Q

When are CCBs used

A

if vasopressor test is positive

22
Q

what CCBs are used with positive vasopressor test

A
  • nifedipine
  • diltiazem
  • amlodipine
23
Q

describe vaspressor test

A
  • short acting vasodilator administered
  • test is positive if PAP falls more than 10 mmHg/MAP is less than 40 mmHG
  • give CCBs in addition if positive
24
Q

Symptoms pulmonary HTN

A
  • dyspnea on exertion
  • syncope
  • swelling in legs/ankles
  • cyanotic lips/skin
25
Q

Risk factors pulmonary HTN

A
  • family history
  • BMPR2 gene
  • HIV infection
  • portal HTN
  • fen/phen use
26
Q

Symptomatic profile of WHO functional class I of pulmonary HTN

A

patients with pulmonary HTN but without resulting limitation of physical activity

27
Q

Symptomatic profile of WHO functional class II of pulmonary HTN

A

patients with pulmonary HTN resulting in slight limitation of physical activity. Comfortable at rest. Ordinary physical activity causes dyspnea/fatigue

28
Q

Symptomatic profile of WHO functional class III of pulmonary HTN

A

patients with pulmonary HTN resulting in marked limitation of physical activity. Comfortable at rest. Less than ordinary physical activity causes dyspnea/fatigue

29
Q

Symptomatic profile of WHO functional class IV of pulmonary HTN

A

Patients with pulmonary HTN with inability to carry out any physical activity without symptoms. Manifest signs of right heart failure

30
Q

Which class of drugs has caused sudden hearing loss and/or visual disturbances (e.g., lack of color discrimination) when used by some patients?

A

PDE 5 inhibitors

31
Q

What drug combo is typically used for patients with WHO FC II pulmonary HTN?

A

ambrisentan and tadalafil

32
Q

At what point are prostanoids indicated for treatment-naive patients requiring therapy for pulmonary hypertension?

A

WHO FC III, evidence of rapid disease progression