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Pharm Practice 4 > Pulmonary Arterial Hypertension > Flashcards

Pulmonary Arterial Hypertension Flashcards

1
Q

Guidelines and endorsing organization for the guidelines

A

Journal of the American College of Cardiology (JACC)

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2
Q

Pharmacotherapy classes used to treat PAH

A 
CCBs
Soluble guanylate cyclase (sGC) stimulators
Phosphodiesterase (PDE5) inhibitors
Endothelin receptor antagonists (ERAs)
Prostacyclin analogs
Prostacyclin IP-receptor agonists
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3
Q

Goals of therapy

A 
improve NYHA functional class
Improve exercise tolerance
Improve hemodynamic profile and symptoms
Slow time to clinical worsening
Slow disease progression
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4
Q

Pharmacotherapy for PAH restricted through REMs

A

sCG stimulator: Riociguat (Adempas)- birth defects
ERAs: Ambrisentan (Letairis)- birth defects, Bosentan (Tracleer)- hepatotoxicity, birth defects, Macitentan (Opsumit)- birth defects

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5
Q

Drugs/toxins that cause PAH

A

cocaine, phenylpropanolamine, St. John’s Wort, SSRIs in newborns, amphetamine-like drugs, interferon alpha and beta

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6
Q

Soluble guanylate cyclase (sGC) inhibitors

A

MOA: sensitize sGC to endogenous NO => vasodilation. Also directly stimulates sGC, increasing cGMP w/ subsequent vasodilation

Riociguat (Adempas)

Must give med guide w/ prescription

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7
Q

Riociguat

A

Adempas - sGC inhibitor
Dose: 1mg PO TID; 0.5mg PO TID w/ intolerable hypotension
Pearls: SBP >95mmHg w/ no s/s of hypotension increase dose by 0.5mg TID every 2wks to 2.5mg TID or highest tolerated dose
metabolized via BCRP, CYP2C8/3A4 and eliminated by p-gp
adjust dose in smokers and pts w/ multi-pathway CYP and P-gp/BCRP inhibitors
CI: pregnancy, co-administration of nitrates, PDE5 inhibitors
No dose adjustment for CrCl >15ml/min or mild/mod hepatic impairment

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8
Q

Riociguat AEs

A

fetal harm, hypotension, HA, dizziness, dyspepsia, bleeding

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9
Q

PDE5 Inhibitors

A

MOA: prevent the breakdown of cGMP
(NO –> guanylate cyclase –> increase cGMP => vasodilation)

FDA approved: sildenafil (Revatio), tadalafil (Adcirca)
Non-FDA approved: vardenafil (Levitra)

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10
Q

Sildenafil citrate

A

Revatio - PDE5 inhibitor
Dose: 5-40mg po TID (max: 240mg/day)
Pearls: metabolized by CYP3A4, avoid grapefruit juice
CI: nitrates, riociguat, protease inhibitors
Counsel on priapism

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11
Q

Sildenafil citrate AEs

A

flushing, HA, hypotension (associated w/ alcohol use and antihypertensives), diarrhea, visual disturbances, reports of hearing loss

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12
Q

Tadalafil

A

Adcirca - PDE5 inhibitor
Dose: 40mg QD (max: 40mg/day)
Pearls: metabolized by CYP3A4, avoid grapefruit juice,
CI: nitrates, riociguat, protease inhibitors –> dose adjust w/ ritonavir
Dose adjust CrCl 31-80 ml/min and mild-mod hepatic impairment: 20mg QD (renally active metabolite)

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13
Q

Tadalafil AEs

A

flushing, HA, hypotension (associated w/ alcohol use and antihypertensives), nausea, myalgia, visual disturbances

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14
Q

Endothelin Receptor Antagonists

A

Competitively inhibits endothelin-1 receptors
ETa receptor: pulmonary vascular smooth muscle, stimulation –> vasoconstriction and cellular proliferation
ETb receptor: pulmonary vascular endothelial cells and smooth muscle cells, stimulation –> vasodilation, anti-proliferative effects and endothelin clearance

CI: pregnancy

Ambrisentan (Letairis)
Bosentan (Tracleer)
Macitentan (Opsumit)

Must give med guide w/ prescription

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15
Q

Ambrisentan

A

Letairis - Endothelin Receptor Antagonists
» affinity for ETa receptor
Dose: 5mg QD (max: 10mg/day)
Pearls: minor metabolism by CYP 2C19/3A4, eliminated by P-gp, don’t exceed 5mg/day w/ cyclosporine (decreases metabolism)
Adjust dose in hepatic impairment that develops (LFTs 5x ULN - decrease dose)
Don’t crush/split/chew

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16
Q

Bosentan

A

Tracleer - Endothelin Receptor Antagonists
ETa and ETb receptor affinity (A»B)
Dose: <40kg: 62.5mg BID, >40kg: 62.5mg BID x4 wks, increase to 125mg BID
Pearls: Minor metabolism by CYP2C9/3A4, induces CYP2C9 (weak/mod)/3A4 (mod), avoid grapefruit juice, dose adjust w/ ritonavir
Adjust dose in hepatic impairment that develops
CI: concurrent cyclosporine or glyburide (increases LFTs)

17
Q

Macitentan

A

Opsumit - Endothelin Receptor Antagonists
Tissue selective ET receptor antagonist, ETa and ETb receptor affinity (A»B)
Dose: 10mg QD (max: 10mg/day)
Pearls: metabolized by CYP3A4, Don’t crush/split/chew
Fewer drug-drug interactions than ambrisentan and bosentan

18
Q

Endothelin Receptor Antagonists AEs

A

HA, anemia, fluid retention/peripheral edema, respiratory complications, decrease spermatogenesis, hepatic impairment, flushing and dyspepsia w/ Ambrisentan

19
Q

Prostacyclin Analogs

A

MOA: vasodilate pulmonary arteries, impair platelet aggregation, anti-proliferative effects on pulmonary endothelial cells
IV and SQ forms (high potential for calculation-related med errors)

IV: epoprostenol (Flolan, Veletri), trepostonil (Remodulin)
SQ: trepostonil (Remodulin)
Inhaled: trepostonil (Tyvaso), Iloprost (Ventavis)
Oral: trepostonil (Orenitram)

20
Q

Epoprostenol

A

Flolan, Veletri - Prostacyclin Analogs
Continuous Infusion: 2ng/kg/min via central venous catheter
MD: 25-40 ng/kg/min
Dose adjust based on PAH symptoms and tolerability to side effects
ISMP list b/c of heighened risk of significant pt harm if used in error
Pearls: special ambulatory infusion pumps: Veletri: stable at room temp, Flolan: must be kept on ice, use caution in pts w/ risks for bleeding, chronic CI associated w/ local infections and serious blood stream infections of indwelling central venous catheter, DC if pt develops pulmonary edema
CI: HF (w/ low EF) due to severe left ventricular dysfunction
Only available from CVS Caremark or Accredo Health Inc

21
Q

Epoprostenol AEs

A

AEs are used as a guide for dose-titration for pt tolerance

flushing, HA, n/v, hypotension, anxiety/agitation, chest pain, jaw pain

22
Q

Treprostonil (SQ and IV)

A

Remodulin - Prostacyclin Analogs
SQ: administer via ambulatory pump 1.25 ng/kg/min, can administer up to 72hrs at >98F
IV: infused via central venous catheter infusion pump 1.25 ng/kg/min, can administer up to 48hrs >98F
SQ and IV: can decrease to 0.625 ng/kg/min due to AEs (site reaction won’t get better)

23
Q

Treprostonil (Remodulin) AEs

A

Infusion site pain/reaction (~85% of pts), rash, dose related: HA, n/v, jaw pain
hypotension

24
Q

Treprostonil inhaled

A

Tyvaso - Prostacyclin Analogs
Dose: 18mcg (or 3 inhalations) QID
If tolerated increase by additional 3 inhalations at 1-2 wk intervals, target/max dose: 54mcg (9 puffs) QID

Safety/efficacy hasn’t been established in underlying pulmonary disease (asthma, COPD)

25
Q

Treprostonil (Tyvaso) AEs

A

cough/throat irritation, dose related: HA, dizziness, nausea, diarrhea, flushing

26
Q

Treprostonil (Tyvaso, Remodulin) clinical pearls

A

avoid abrupt DC, metabolized through CYP2C8, concomittant diuretics, antihypertensives, vasodilators may increase risk of hypotension, may inhibit platelet aggregation –> increased risk of bleeding
IV/SQ: prescribing/access restriction - only available from CVS Caremark or Accredo Health Inc., mild-mod hepatic impairment adjust dose: 0.625ng/kg/min using IBW –> use w/ caution and titrate slowly

27
Q

Iloprost

A

Ventavis - Prostacyclin Analogs
Dose: Inhaled: 2.5mcg w/ specific inhalation system, if tolerated increase to 5mcg inhaled 6-9x/day, no more than q2h (45mcg) during waking hrs
Max dose: 45mcg/day (5mcg/dose 9 times per day)
Pearls: Don’t start is SBP <85mmHg (b/c of hypotension), safety and efficacy haven’t been established in concurrent pulmonary diseases (COPD, severe asthma, acute pulmonary infection), may induce bronchospasm in hyper-reactive airways, may inhibit platelet aggregation –> increase bleeding risk, hepatic impairment- consider increasing dosing interval (q3-4h)

28
Q

Iloprost AEs

A

cough, flu-like symptoms, dose related: nausea, HA, hypotension/syncope, flushing, jaw pain

29
Q

Prostacyclin IP-receptor agonists

A

IP receptor: 1 of 4 prostanoid receptors, regulates vascular tone, platelet activation, immunologic cell responses, expressed in vascular smooth muscle cells (SMC) and platelets, activation of IP receptor triggers SMC vasodilation and inhibition of SMC proliferation and platelet aggregation

Selexipag (Uptravi) - agonist of the prostacyclin IP receptor

30
Q

Selexipag

A

Uptravi - Prostacyclin IP-receptor agonists
Dose: 200mcg PO BID, increase by 200mcg BID weekly to highest tolerated dose (max: 1600mcg BID)
Pearls: major substrate of BCRP, CYP2C8, take w/ food, avoid use in severe hepatic impairment, DC if pt develops pulmonary edema

31
Q

Selexipag AEs

A

flushing, HA, GI (n/v/d), myalgia, jaw pain, pulmonary edema

32
Q

General Considerations w/ PAH

A

avoid heavy lifting (syncope), participate in low level graded aerobic activity (improves peak oxygen consumption), avoid high altitudes (may need supplemental oxygen on planes), salt restriction to <2400mg/day, avoid in pregenancy, get immunizations (flu, pneumoccal)

Pharm Practice 4 (8 decks)

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