Pulmonary HTN Flashcards
(20 cards)
Epoprostenol (vasoreactivity test)
Route, Dose, SE, Half-Life
Route: IV
Dose: 2-10 mcg/kg/min
SE: HA, nausea, light-headedness
Half-life: 3-6 min
Nitric Oxide (Vasoreactivity Test) Route, Dose, SE, Half-Life
Route: Inhaled
Dose: 10-80 ppm
SE: increased left ventricle filling pressure in susceptible patients
Half life: 15-30 seconds
Adenosine (Vasoreactivity Test)
Route, Dose, SE, Half-Life
*Not used very often* Route: IV Dose: 50-250 mcg/kg/min SE: AV block, dyspnea, chest pain Half life: 5-10 sec
Amlodipine
PK, ADE, DDI
Used if intolerant to Diltiazem or Nifedipine LA
PK: Half life=30-50 hrs
ADE: Peripheral edema, dizziness, constipation
DDI: 3A4 substrate
Nifedipine LA
Dose, PK, ADE, DDI
Dose: 120-240 mg/day
PK: Extensive 1st pass, Half life=2-5 hrs
ADE: Peripheral edema, dizziness, constipation
DDI: 3A4 substrate
Diltiazem
Dose, PK, ADE, DDI
Dose: 240-720 mg/day
PK: Extensive 1st pass, Half life=4-6 hrs
ADE: Peripheral edema, dizziness, constipation, negative inotropic effect
DDI: 3A4 substrate, P-GP inhibitor
Sildenafil
Dose, PK, DDI
Dose: Initial 20 mg TID (titrate to 100 mg TID)
PK: Half life=4 hrs, hepatic metabolism
DDI: Sub/Inhib of 3A4, 2C9; Intx with vasodilators (nitrates)
Tadalafil
Dose, PK, DDI
Dose: 40 mg daily; if CrCl <80 mg/mL then 20 mg daily
PK: Half life=35 hrs, hepatic metabolism
DDI: 3A4, Intx with vasodilators
Bosentan (Tracleer)
MOA, Dose, PK, Preg Risk, ADE, DDI
MOA: non-specific ETa/b receptor antagonist
Dose: Initial 62.5 mg PO BID x 4wks; Increase to 125 mg PO BID
PK: Protein bound, hepatic metabolism
Pregnancy Category X (REMS program)
ADE: Hepatotoxicity, anemia, peripheral edema, flushing
DDI: Sub/Inducer of 3A4, 2C9, Inducer 2C19
Ambrisentan (Letairis)
MOA, Dose, PK, Preg Risk, ADE, DDI
MOA: Specific ETa receptor antagonist
Dose: Initial 5 mg PO QD; increase to 10 mg PO QD
PK: Protein bound, hepatic metabolism
Pregnancy Category X (REMS program)
ADE: Hepatotoxicity, anemia, peripheral edema, flushing
DDI: Sub 3A4, 2C9, PGP, UGT
Macitentan (Opsumit)
MOA, Dose, PK, Preg Risk, ADE, DDI
Not in treatment algorithm
MOA: non-specific ETa/b receptor antagonist
Dose: 10 mg PO QD
PK: Protein bound, hepatic metabolism
Pregnancy Category X (REMS program)
ADE: anemia, nasal congestion, influenza, UTI, HA
DDI: Substrate 3A4 (minor 2C19)
Bosentan Drug Intx
CI with glyburide and cyclosporine
Increases LFT more and decrease glyburide levels
Macitentan Drug Intx
Cyclosporine: increases M; no dose change
Ketoconazole: increase M; do not administer
Rifampin: decrease M; do not administer
Sildenafil: increase sildenafil; no dose change
warfarin; no worries
Epoprostenol (Flolan)
Dose, PK, Preg, ADE, Intx
Dose: Initially 2-4 ng/kg/min IV; titrate to 20-40 ng/kg/min
PK: Half-life=3-6 min; very unstable drug
Preg: B
ADE: rebound HTN, hypotension, flushing, jaw pain, HA
Intx: PD with anti-HTN and anti-platelet
Treprostinil (Remodulin)-IV and SubQ
Dose, PK, Preg, ADE, Intx
Dose: Initially 1.25 ng/kg/min continuous subQ or IV; Decrease to 0.625 ng/kg/min if not tolerate; Increase by no more than 1.25 ng/kg/min weekly for first 4 weeks and no more than 2.5 ng/kg/min weekly for duration
Preg: B
ADE: SubQ site, hypotension, flushing, jaw pain, HA
Intx: PD with anti-HTN and anti-platelet
Treprostinil (Tyvaso) Inhaled
Dose
ADE
Initially; 3 breaths (18 mpg) QID during waking hours
Reduce to 1-2 breaths if not tolerated
Increase to 3 breaths when tolerance improves
Titrate by increasing 3 breaths at 1 to 2 week intervals if tolerated
GOAL: 9 breaths QID
Higher dose is QTc prolonging
Only studied as adjunct to ETRA or sildenafil
Treprostinil (Orenitram) Oral
Dose
Warning/Precautions
DDI
0.25 mg PO BID
Titrate by 0.25-0.5 mg BID or 0.125 mg TID every 3-4 days
Max dose=tolerability
Careful in hepatic impairment
If miss 2 doses, must restart at lower dose
Can be lodged in diverticulum
No Alcohol
Increased absorption with high fat meal
Reduce starting dose to 0.125 mcg BID with 0.125 mcg dose increments with 2C8 inhibitors gemfibrozil
Iloprost (Ventavis)
Dose
Initially: 2.5 mcg inhaled 6-9x per day
Titrate to 5 mcg per dose with max daily of 45 mcg
Caution in hepatic impairment
Riociguat (Adempas)
MOA, Dose, Warnings, CI/DDI, ADE
- MOA: Stabilizes NO-cGMP complex, binds to cGMP -
- Dose: Initially; 1 mg PO TID, start with 0.5 mg PO TID if hypotension is concern; Increase dose at least 2 wks apart by 0.5 mg TID; Max=2.5 mg TID; Restart if miss 3 days or more
- Preg Category X
- CI: nitrates, PDE5
- DDI: Consider starting at 0.5 mg PO TID if on strong inhibitors, space antacids by 1 hour
- ADE: hypotension, bleeding, vena-occlusive, HA, dyspepsia, nasal congestion
Selexipag (Uptravi)
MOA, Dose, Warnings, CI/DDI, ADE
-MOA: prostaglandin receptor agonist
-Dose; 200 mcg PO BID, titrate weekly, max=1600 mcg BID
-Moderate hepatic impairment: initial 200 mcg PO QD
If miss 3 days or more, retitrate
-Potent active metabolite
-Avoid with strong 2C8 inhibitors
-ADE: hypotension, jaw pain, diarrhea
