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Drug Interactions between eplerenone and riociguat

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

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Interactions between your drugs

Moderate

eplerenone riociguat

Applies to: eplerenone and riociguat

MONITOR: Riociguat may potentiate the action of antihypertensive agents and other vasodilators. 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.

References

  1. (2013) "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc

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Drug and food interactions

Major

eplerenone food

Applies to: eplerenone

GENERALLY AVOID: Coadministration with grapefruit juice may increase the plasma concentrations of eplerenone. The primary mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. Inhibition of hepatic CYP450 3A4 may also contribute. In drug interaction studies, administration of a single 100 mg dose of eplerenone in combination with grapefruit juice resulted in a 25% increase in eplerenone systemic exposure (AUC). High blood levels of eplerenone can increase the risk of side effects including hyperkalemia. 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.

MANAGEMENT: It may be advisable for patients to avoid the consumption of grapefruit, grapefruit juice, or supplements that contain grapefruit during treatment with eplerenone.

References

  1. (2002) "Product Information. Inspra (eplerenone)." Searle
  2. (2021) "Product Information. Eplerenone (eplerenone)." MSN Laboratories Europe Ltd
  3. (2023) "Product Information. Eplerenone (Apotex) (eplerenone)." Apotex Pty Ltd

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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: Riociguat dosages higher than 2.5 mg three times a day may be considered in cigarette smokers, if tolerated, so as 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.

References

  1. (2013) "Product Information. Adempas (riociguat)." Bayer Pharmaceutical Inc

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Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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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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