Skip to main content

Drug Interactions between methylnaltrexone and naldemedine

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

Edit list (add/remove drugs)

Interactions between your drugs

Moderate

methylnaltrexone naldemedine

Applies to: methylnaltrexone and naldemedine

GENERALLY AVOID: Concomitant use of peripherally-acting mu-opioid receptor antagonists, such as methylnaltrexone, naldemedine and naloxegol, with other opioid antagonists may result in additive pharmacologic effects and increased risk of opioid withdrawal. Symptoms consistent with opioid withdrawal including hyperhidrosis, chills, diarrhea, abdominal pain, nausea, vomiting, anxiety, irritability, increased lacrimation, rhinorrhea, and yawning have occurred in patients treated with peripherally-acting mu-opioid receptor antagonists. Patients with disruptions to the blood-brain barrier may be at increased risk.

MANAGEMENT: Concomitant use of peripherally-acting mu-opioid receptor antagonists with other opioid antagonists should generally be avoided.

References

  1. (2008) "Product Information. Relistor (methylnaltrexone)." Wyeth Laboratories
  2. (2014) "Product Information. Movantik (naloxegol)." Astra-Zeneca Pharmaceuticals
  3. (2017) "Product Information. Symproic (naldemedine)." Shionogi USA Inc

Switch to consumer interaction data

Drug and food interactions

Moderate

methylnaltrexone food

Applies to: methylnaltrexone

ADJUST DOSING INTERVAL: Food may reduce the rate and extent of absorption of methylnaltrexone following oral administration. When a single 450 mg oral dose of methylnaltrexone was administered with a high-fat breakfast (approximately 800 to 1000 calories; 60% from fat, 25% from carbohydrate, and 15% from protein) in healthy study subjects, methylnaltrexone peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 60% and 43%, respectively, while time to reach Cmax delayed by 2 hours.

MANAGEMENT: Oral methylnaltrexone should be taken with water on an empty stomach at least 30 minutes before the first meal of the day.

References

  1. (2008) "Product Information. Relistor (methylnaltrexone)." Wyeth Laboratories

Switch to consumer interaction data

Moderate

naldemedine food

Applies to: naldemedine

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of naldemedine. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. In pharmacokinetic studies, naldemedine systemic exposure (AUC) was increased approximately 90% by the moderate CYP450 3A4 inhibitor fluconazole and nearly 200% by the potent inhibitor itraconazole. The interaction has not been studied with grapefruit juice. 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. Increased exposure to naldemedine may precipitate opioid withdrawal symptoms such as hyperhidrosis, lacrimation, rhinorrhea, chills, diarrhea, abdominal pain, anxiety, insomnia, irritability, restlessness, and yawning.

Food does not significantly affect the overall bioavailability of naldemedine. When administered with a high-fat meal, the rate of naldemedine absorption was decreased, but not the extent. Specifically, naldemedine peak plasma concentration (Cmax) was decreased by approximately 35% and time to achieve Cmax was delayed from 0.75 hours in the fasted state to 2.5 hours in the fed state, while naldemedine AUC was not significantly changed.

MANAGEMENT: Naldemedine may be taken with or without food. Patients should avoid consumption of grapefruit and grapefruit juice during treatment with naldemedine.

References

  1. (2017) "Product Information. Symproic (naldemedine)." Shionogi USA Inc

Switch to consumer interaction data

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

Peripheral opioid receptor antagonists

Therapeutic duplication

The recommended maximum number of medicines in the 'peripheral opioid receptor antagonists' category to be taken concurrently is usually one. Your list includes two medicines belonging to the 'peripheral opioid receptor antagonists' category:

  • methylnaltrexone
  • naldemedine

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

Report options

Loading...
QR code containing a link to this page

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