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Drug Interactions between Adempas and macitentan

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

macitentan riociguat

Applies to: macitentan and Adempas (riociguat)

Consumer information for this interaction is not currently available.

MONITOR: Riociguat may potentiate the action of antihypertensive agents and other vasodilators including systemic phosphodiesterase (PDE) type 3 and 4 inhibitors. Symptomatic hypotension may occur. Riociguat stimulates soluble guanylate cyclase (sGC), an enzyme in the cardiopulmonary system that binds with nitric oxide (NO) to catalyze the synthesis of cyclic guanosine monophosphate (cGMP). The resultant accumulation of cGMP in vascular smooth muscle cells leads to peripheral vasodilation and blood pressure decreases.

MANAGEMENT: Caution is advised if riociguat is prescribed in combination with antihypertensive agents or other vasodilators. A reduction in the starting dosage of riociguat to 0.5 mg three times a day should be considered for patients who may not tolerate the hypotensive effect of riociguat. Periodic systemic blood pressure monitoring is recommended. If systolic blood pressure remains greater than 95 mmHg and the patient has no signs or symptoms of hypotension, the dosage may be increased by 0.5 mg three times a day every 2 weeks as tolerated, up to a maximum of 2.5 mg three times a day. If hypotension develops at any time during treatment, the dosage should be reduced by 0.5 mg three times a day.

Drug and food/lifestyle interactions

Moderate

macitentan food/lifestyle

Applies to: macitentan

Consumer information for this interaction is not currently available.

GENERALLY AVOID: Coadministration with grapefruit juice may increase the plasma concentrations of macitentan, which is primarily metabolized by CYP450 3A4. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. The interaction has not been studied with grapefruit juice but has been reported for ketoconazole, a potent CYP450 3A4 inhibitor. In ten healthy subjects, coadministration of a single 10 mg oral dose of macitentan on day 5 of treatment with ketoconazole (400 mg daily for 24 days) resulted in an approximately 2-fold increase in macitentan systemic exposure compared to administration alone. However, the clinical significance of the interaction is unclear. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: Until further information is available, patients receiving macitentan therapy should avoid the consumption of grapefruit or grapefruit juice.

Moderate

riociguat food/lifestyle

Applies to: Adempas (riociguat)

Chemical substances present in cigarette smoke may reduce the blood levels of riociguat. This means that the medication may be less effective if you smoke during treatment. Let your doctor know if you are a smoker, or if you start smoking or stop smoking during treatment with riociguat, because the dosage may need to be adjusted. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Food may affect the absorption and blood levels of riociguat. To avoid significant fluctuations in blood levels of the medication, riociguat should be taken about the same time each day consistently either with or without food.

Therapeutic duplication warnings

Therapeutic duplication is the use of more than one medicine from the same drug category or therapeutic class to treat the same condition. This can be intentional in cases where drugs with similar actions are used together for demonstrated therapeutic benefit. It can also be unintentional in cases where a patient has been treated by more than one doctor, or had prescriptions filled at more than one pharmacy, and can have potentially adverse consequences.

Duplication

Agents for pulmonary hypertension

Therapeutic duplication

The recommended maximum number of medicines in the 'agents for pulmonary hypertension' category to be taken concurrently is usually one. Your list includes two medicines belonging to the 'agents for pulmonary hypertension' category:

  • Adempas (riociguat)
  • macitentan

Note: In certain circumstances, the benefits of taking this combination of drugs may outweigh any risks. Always consult your healthcare provider before making changes to your medications or dosage.

See also

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer