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Drug Interactions between riociguat and Tracleer

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

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Interactions between your drugs

Moderate

bosentan riociguat

Applies to: Tracleer (bosentan) and riociguat

MONITOR: Coadministration with inducers of CYP450 3A4 may decrease the plasma concentrations of riociguat, which is partially metabolized by the isoenzyme. According to the product labeling, administration of riociguat with the moderate CYP450 3A4 inducer bosentan resulted in an approximately 30% decrease in riociguat systemic exposure (AUC). The magnitude of interaction is expected to be greater with more potent inducers.

MANAGEMENT: The potential for diminished therapeutic effects of riociguat should be considered when prescribed in combination with CYP450 3A4 inducers. No dose adjustment is necessary for concomitant use with moderate CYP450 3A4 inducers. Data are not available to guide dosing of riociguat when coadministered with potent CYP450 3A4 inducers such as carbamazepine, enzalutamide, phenobarbital, phenytoin, rifamycins, and St. John's wort. Patients should be closely monitored and alternative agents with no or minimal CYP450 3A4-inducing activity should be considered whenever possible.

References (3)
  1. (2013) "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc
  2. (2023) "Product Information. Adempas (riociguat)." Merck Sharp & Dohme (UK) Ltd
  3. (2014) "Product Information. Adempas (riociguat)." Bayer Australia Limited

Drug and food interactions

Moderate

riociguat food

Applies to: riociguat

ADJUST DOSE: Smoking may decrease the plasma concentrations of riociguat. The proposed mechanism is induction of the CYP450 1A1-mediated metabolism of riociguat by polycyclic aromatic hydrocarbons present in cigarette smoke. CYP450 1A1 is responsible for the formation of the major active metabolite, M1, which has just 1/3 to 1/10 the pharmacologic activity of riociguat. According to the product labeling, plasma concentrations of riociguat are reduced by 50% to 60% in smokers compared to nonsmokers.

MANAGEMENT: Patients should be advised to stop smoking. Riociguat dosages higher than 2.5 mg three times a day may be considered in cigarette smokers, if tolerated, to match the exposure seen in nonsmoking patients. However, safety and effectiveness of higher dosages have not been established. A dosage reduction should be considered in patients who stop smoking during treatment with riociguat. The tablet form of riociguat can generally be taken with or without food. Some authorities recommend not to switch between fed and fasted riociguat intake because of increased peak plasma levels of riociguat in the fasting compared to the fed state.

References (3)
  1. (2013) "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc
  2. (2023) "Product Information. Adempas (riociguat)." Merck Sharp & Dohme (UK) Ltd
  3. (2014) "Product Information. Adempas (riociguat)." Bayer Australia Limited

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:

  • riociguat
  • Tracleer (bosentan)

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.

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