Drugs for Pulmonary Hypertension and DVT/PE (Wolff) Flashcards Preview

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Flashcards in Drugs for Pulmonary Hypertension and DVT/PE (Wolff) Deck (35)
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1
Q

What are the 5 drug classes used to treat Pulmonary Hypertension? (P/EA/PI/GCS/C)

A

prostanoids, endothelin antagonists, PDE 5 inhibitors, Guanylate cyclase sensitizers, CCBs

2
Q

What are the 4 Prostanoids used for Pulmonary Hypertension? (E/T/I/S)

A

epoprostenol
treprostinil
iloprost
selexipag

3
Q

What are the 3 Endothelin antagonists used for Pulmonary Hypertension? (B/A/M)

A

bosentan
ambrisentan
macicentan

4
Q

What are the 2 PDE 5 inhibitors (S/T) and what is the 1 guanylate cyclase sensitizer (R) used for Pulmonary Hypertension?

A

PDE 5 –> sildenafil and tadalafil

GCS –> riociguat

5
Q

What is a known genetic mutation that is linked to PAH and what are two drugs that can cause PAH? (Fen/Phen)

A

Genetics: BMPR2 (bone morphogenic protein receptor 2)
- seen in < 25% of idiopathic PAH

Drugs: fenfluramine/phentermine
- weight loss pills

6
Q

What is the difference between these WHO FC for PAH:

Class 1
Class 2
Class 3
Class 4

A
  1. pulmonary HTN without resulting limitation of physical activity
  2. pulmonary HTN with SLIGHT limitation of physical activity; ordinary activity causes symptoms
  3. pulmonary HTN with MARKED limitation of physical activity; less than ordinary activity causes symptoms; still comfortable at rest
  4. pulmonary HTN with INABILITY to carry out physical activity without symptoms; manifest signs of RIGHT HEART FAILURE
7
Q

What is the Vasopressor Test and what are positive findings?

A
  • recommended that Group 1 PAH undergo vasopressor testing; administration of short-acting vasodilators

(+) = PAP dec. > 10 mmHg, MPAP < 40 mmHg, or CO is unchanged or increased

  • see more response from idiopathic, familial, or anorexigen-induced PAH

50% of these patients benefit from treatment with CALCIUM CHANNEL BLOCKERS - nifedipine, diltiazem, amlodipine

8
Q

Epoprostenol

What is its MOA, what is it used for, how is it administered, and what is its major serious adverse effect?

A

MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH

  • administered as continuous IV due to 6 minute half-life; used with pump that can keep the drug COLD

AE: sepsis due to chronic catheter

9
Q

Treprostinil

What is its MOA, what is it used for, how is it administered, and what is its major adverse effect?

A

MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH

  • administered with pump IV in dilution 1:2 and DOESN’T require refrigeration; has 4 hour half-life
    • used to be SubQ but was too painful

AE: sepsis due to chronic catheter

10
Q

Iloprost

What is its MOA, what is it used for, how is it administered, and what is its major adverse effect?

A

MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH

  • administered by INHALATION 6-9x day

AE: fainting due to hypotension (especially if SBP < 85 mmHg)

11
Q

Selexipag

What is its MOA, what is it used for, and how is it administered?

Who benefits from this medication?

A

MOA: mimics endogenous prostacyclin –> vascular relaxation/inhib. platelet agg. and exerts effects by binding to G-protein on cell membrane to generate cAMP; used for PAH

  • administered ORALLY twice daily, but is EXPENSIVE

kids with PAH and/or their caregivers often refuse central line for IV, so this is a good alternative

12
Q

Bosentan

What is its MOA, what is it used for, how is it administered, and what are its two serious adverse effects?

What are two drug interactions this drug has?

A

MOA: nonspecific ETa and ETb endothelin receptor blocker used for PAH

  • administered ORALLY

AE: hepatotoxicity and teratogenesis

DI: accelerates metabolism of WARFARIN and ORAL CONTRACEPTIVES
- all patients MUST use 2 forms of birth control

13
Q

Ambrisentan

What is its MOA, what is it used for, how is it administered, what is its serious adverse effect?

What are its drug interactions?

A

MOA: selective ETa receptor blocker used for PAH

  • administered ORALLY

AE: teratogenesis (does NOT DAMAGE LIVER)

DI: does NOT accelerate Warfarin or oral contraceptive metabolism, but pts should STILL USE 2 forms of contraception

14
Q

Macicentan

What is it and what is its half-life?

A
  • non-selective Endothelin Antagonist

- half-life of 18 hrs allows for one/day dosing

15
Q

Sildenafil

What is its MOA, what is it used for, how is it administered, and what are its 3 most common complications (H/F/D)?

What is Tadalafil?

A

MOA: selectively blocks phosphodiesterase Type 5, an enzyme that breaks down cGMP, and is used to treat PAH

  • administered ORALLY with a 4 hr half-life

AE: headache, flushing, dyspepsia

  • mild hypotension when used alone
  • inc. hypotension with alpha-blockers/nitrates

Tadalafil = LONGER half-life than Sildenafil

16
Q

Riociguat

What is its MOA, what is it used for, how is it administered, and what are its two major adverse effects?

A

MOA: sensitizes soluble guanylate cyclase to NO by stabilizing NO-sGC binding AND directly stimulates sGC independent of NO; used to treat PAH and type 4 PH

  • administered ORALLY with half-life of 12 hours

AE: may cause fetal harm and should NOT be administered with NO donors or Type 5 PDE inhibitors

17
Q

What is a very common PAH drug combination used to PAH patients?

A

tadalafil + ambrisentan

18
Q

What are 3 Tissue-type Plasminogen Activator Drugs that can be used for thrombus busting? (A/R/T)

How do these drugs work?

A

TpD = Alteplase, Reteplase, Tenecteplase
- all end in suffix “-teplase”

  • activate plasminogen in thrombus ONLY
19
Q

What are the 5 Parenteral indirect thrombin/Xa inhibitors that can be used for DVT and PE? (H/E/D/T/F)

A

heparin

enoxaparin, dalteparin, tinzaparin

fondaparinux

20
Q

What are the 2 Parenteral direct thrombin inhibitors that can be used for DVT and PE? (B/A)

A

bivalirudin, argatroban

21
Q

DVT and PE Drug Treatment

What is the Oral coumarin derivative?

What are the 3 Oral direct Factor Xa inhibitors? (R/A/E)

What is the Oral direct thrombin inhibitor?

A

CD: warfarin

XaI: ribaroxaban, apixaban, endoxaban

TI: dabigatran

22
Q

Heparin

What is its MOA, what does it block, and what is its antidote?

How does it affect pregnancy?

A

MOA: binds to/activates antithrombin III to inhibit Factor Xa and thrombin (blocks generation and inactivates thrombin)

  • large negative charge, cannot cross membranes

Antidote: Protamine
Pregnancy: doesn’t cross placenta, so CAN use in pregnancy

23
Q

Heparin

What are 3 major contraindications to use? (T/B/S)

What is Heparin-induced Thrombocytopenia?

A
  1. thrombocytopenia
  2. uncontrollable bleeding
  3. surgery involving brain, eye, spinal cord

Heparin-induced Thrombocytopenia

  • reduced platelet counts w/paradoxical inc. in thrombotic events
  • Abs to heparin-platelet complexes

LMW heparins can also cause thrombocytopenia and severe bleeding

24
Q

Enoxaparin, Dalteparin, Tinzaparin

What is their MOA, what are they used for, and what is their antidote?

How do they affect pregnancy?

A

MOA: shorter length heparin molecules that selectively block Factor Xa but NOT thrombin; used for DVT and red thrombus prevention

  • FIRST CHOICE TREATMENTS FOR DVT
  • easier to use (can be used at home; long 1/2 lives)

Antidote: protamine
Pregnancy: SAFE

25
Q

Fondaparinux

What is its MOA, what is it used for, and what is its antidote?

How is it administered and what does it NOT potentially cause in patients?

A

MOA: synthetic pentasaccharide that selectively inhibits Factor Xa and prevents DVT

  • more effective than Enoxaparin, but inc. bleeding risk
  • can be used in conjunction with Warfarin
  • administered SubQ with 17-21 hr 1/2 life

Antidote: NONE (not affected by protamine)
- does NOT cause Heparin-induced Thrombocytopenia

26
Q

Bivalirudin (Hirudin-analog)

What is its MOA, what drug is it commonly used with, and how is it administered?

What is its antidote?

A

MOA: synthetic peptide that directly (reversibly) inhibits thrombin; given w/GP IIb/IIIa antagonists in pts. undergoing coronary angioplasty

  • must be given IV like heparin (expensive though!!)
    Antidote: NONE
27
Q

Argatroban

What is its MOA, what is it used for, and how is it administered?

What patient population is it used in?

A

MOA: directly binds to catalytic site of thrombin and reduced new thrombus development, specifically pts. with Heparin-induced thrombocytopenia
- treatment monitored with aPTT

  • given IV (short half-life)
28
Q

Warfarin

What is its MOA, what is it used for, and what is it NOT useful for?

What is a consideration when using this drug?

A

MOA: vitamin K antagonist that dec. production of active forms of calcium-dependent clotting factors (2, 7, 9, 10) and protein C/S (anti-clotting factors)

  • for long-term thrombosis prophylaxis
  • for mechanical heart valves and atrial fibrillation
  • NOT useful for emergencies (delayed effects)

remember: slow onset and slow offset, monitor frequently when other drugs are added/subtracted

29
Q

Warfarin

What is a major complication of use and how can it be corrected?

What is its effect in pregnancy?

A

MC: BLEEDING; if occurs, discontinue immediately

  • effects can be reversed with Vitamin K (12-24 hrs)
  • give fresh blood for quick change
  • can cause cutaneous necrosis (loss of Protein C causes procoagulant state)

Pregnancy: DO NOT USE ON PREGNANT PTS
- crosses the placenta

has greatest affects on Factor VII and Protein C

30
Q

Rivaroxaban (Apixaban, Endoxaban)

What is its MOA, what are its 2 uses, and what is its antidote?

How does it affect pregnancy?

A

MOA: direct inhibitor of Factor X (binds in active center); used for DVT prevention and stroke prevention in pts with nonvalvular A Fib (not as good w/mechanical valve)

Antidote: andexanet alfa
Pregnancy: appears UNSAFE
- do NOT use with other anticoagulants
- avoid in pts. with renal/hepatic involvement

31
Q

Dabigatran

What is its MOA, what is it used for, and what is it contraindicated in?

What is its antidote?

A

MOA: reversible direct thrombin inhibitor that has advantages over Warfarin (no monitor, lower bleeding risk, same dosing)

  • used for stroke and systemic embolism prevention
  • in pts. with nonvalvular Atrial Fibrillation

CI: pts. with MECHANICAL HEART VALVES
- also pills are unstable (bleeding major concern)

Antidote: idarucizumab

32
Q

What is definitive imaging used to diagnose PE?

A

CT Pulmonary Angiography

33
Q

What are two surgical preventative measures for DVT and PE?

A
  1. IVC filter used to break apart thrombi

2. stent placement in common iliac veins to help keep them open

34
Q

What is the treatment for PE due to air?

A
  • position patient in left lateral decubitus position with head down OR use Trendelenburg machine to avoid further venous embolization
  • immediately administer high flow oxygen/mechanical ventilation –> inc. rate with which the embolized air is resorbed
  • secure access for administration of IV fluids and/or vasopressors to restore adequate tissue perfusion
35
Q

What is the treatment for PE due to fat?

A
  • no definitive treatments available; treatment is largely supportive while fat emboli resolve spontaneously
  • can give fluid resuscitation, oxygenation, rare use of vasopressors +/- noninvasive/invasive mechanical support
  • corticosteroids and heparin are NOT commonly used