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DOSING AND ADMINISTRATION

OPSYNVI® Contains 2 Proven Therapies in 1 Tablet1-3

Titrating OPSYNVI® (macitentan/tadalafil)1

For patients who are treatment naïve to any PAH therapy or transitioning from ERA monotherapy1

Starting dose:

1 OPSYNVI® 10 mg/20 mg tablet

once daily for 1 week

If tolerated, up-titrate to

1 OPSYNVI® 10 mg/40 mg tablet

once daily

For patients who are transitioning from a stable-dose PDE5i monotherapy or ERA + PDE5i loose-dose combinations1

No titration needed. Start with

1 OPSYNVI® 10 mg/
40 mg tablet

once daily

OPSYNVI® dosing differs from other combination therapy treatments. Explore the differences

  • For females of reproductive potential, exclude pregnancy prior to initiation of therapy and ensure use of effective contraceptive methods prior to the initiation of treatment, during treatment and for one month after discontinuation.

1 once-daily tablet

  • OPSYNVI® can be administered with or without food
  • Tablets should not be cut, crushed, or chewed
  • If the patient misses a dose of OPSYNVI®, tell the patient to take it as soon as possible and then take the next dose at the regularly scheduled time. Tell the patient not to take 2 doses at the same time if a dose has been missed
  • The use of OPSYNVI® is not recommended in patients undergoing dialysis. Avoid use of OPSYNVI® in patients with severe renal impairment
  • OPSYNVI® was not studied in patients with severe hepatic impairment. OPSYNVI® must not be initiated in patients with severe hepatic cirrhosis (Child-Pugh class C), or clinically significant elevated hepatic aminotransferases (>3 x ULN)

Drug Interactions1

MedicationEffect
Nitrates
  • Administration of nitrates within 48 hours after the last dose of OPSYNVI® is contraindicated
Strong inducers of CYP3A4 (eg, rifampin)
  • Significantly reduce macitentan exposure
  • Use of OPSYNVI® with strong CYP3A4 inducers should be avoided
Strong CYP3A4 inhibitors (eg, ketoconazole)
  • Increase macitentan and tadalafil exposure
  • Avoid concomitant use of OPSYNVI® with strong CYP3A4 inhibitors such as ritonavir, ketoconazole and itraconazole
  • Use other PAH treatment options when strong CYP3A4 inhibitors are needed
Moderate dual or combined inhibitors of CYP3A4 and CYP2C9 (eg, fluconazole)
  • Predicted to increase macitentan exposure 4-fold
  • Concomitant use of OPSYNVI® with moderate dual inhibitors of CYP3A4 and CYP2C9 should be avoided
  • Concomitant use of OPSYNVI® with both a moderate CYP3A4 inhibitor and moderate CYP2C9 inhibitor should also be avoided
Alpha-blockers
  • PDE5 inhibitors, including tadalafil, and alpha-blockers are both vasodilators with blood pressure-lowering effects
  • Concomitant administration of alpha-blockers and tadalafil may lead to symptomatic hypotension
  • Combination of OPSYNVI® with doxazosin is not recommended
Antihypertensives
  • PDE5i, including tadalafil, are mild systemic vasodilators
  • In pharmacology studies, small reductions in blood pressure occurred following coadministration of tadalafil with selected antihypertensive medications* vs placebo
Alcohol
  • Both alcohol and tadalafil are mild vasodilators
  • When taken in combination, blood pressure-lowering effects of each individual compound may increase
  • Substantial consumption of alcohol (ie, ≥5 units) in combination with OPSYNVI® can increase the potential for orthostatic signs and symptoms, including increase in heart rate, decrease in standing blood pressure, dizziness, and headache
  • Tadalafil (10 mg or 20 mg) did not affect alcohol plasma concentrations and alcohol did not affect tadalafil plasma concentrations

Once-daily OPSYNVI® (macitentan/tadalafil) ERA + PDE5i combination therapy with the fewest pills1,3-5

PER DAY

PER WEEK

OPSYNVI® maintenance dose
1 once-daily macitentan 10 mg/tadalafil 40 mg tablet1

pill

1

pill

7

pills

ERA + tadalafil 20 mg
3 tablets, once daily3,4

tad tablets

3

pills

21

pills

ERA + sildenafil 20 mg
4 to 13 tablets daily,
in 3 divided doses3,5

tablets

up to

13

pills

up to

91

pills

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*

Selected antihypertensive medications include amlodipine, angiotensin II receptor blockers, bendroflumethiazide, enalapril, and metoprolol.

CYP=cytochrome P450; ERA=endothelin receptor antagonist; PAH=pulmonary arterial hypertension; PDE5i=phosphodiesterase type 5 inhibitor; ULN=upper limit of normal.

References: 1. OPSYNVI® (macitentan/tadalafil) full Prescribing Information. Actelion Pharmaceuticals US, Inc. 2. Galie N, Brundage BH, Ghofrani HA, et al; Pulmonary Arterial Hypertension and Response to Tadalafil (PHIRST) Study Group. Tadalafil therapy for pulmonary arterial hypertension. Circulation. 2009;119(22):2894-2903. doi:10.1161/CIRCULATIONAHA.108.839274 3. Pulido T, Adzerikho I, Channick RN, et al; SERAPHIN Investigators. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med. 2013;369(9):809-818 and suppl 1-21. doi:10.1056/NEJMoa1213917 4. ADCIRCA® Prescribing Information. Eli Lilly & Co. 5.  REVATIO® Prescribing Information. Pfizer.