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Drug Interactions between cariprazine and Xermelo

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

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Interactions between your drugs

Moderate

cariprazine telotristat ethyl

Applies to: cariprazine and Xermelo (telotristat)

GENERALLY AVOID: Coadministration with inducers of CYP450 3A4 is expected to alter the pharmacokinetics of cariprazine and its major active metabolites. However, the interaction has not been studied; therefore, the net effect on active drug and metabolites is unclear. Cariprazine is primarily metabolized by CYP450 3A4 and, to a lesser extent, by CYP450 2D6 to desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR). DCAR is further metabolized to DDCAR by CYP450 3A4 and 2D6, and DDCAR is then metabolized by CYP450 3A4 to a hydroxylated metabolite. Both DCAR and DDCAR have in vitro receptor binding profiles similar to the parent drug and are considered pharmacologically equipotent to cariprazine.

MANAGEMENT: Concomitant use of cariprazine with CYP450 3A4 inducers has not been evaluated and is not recommended.

References

  1. "Product Information. Vraylar (cariprazine)." Allergan Inc (2022):
  2. "Product Information. Reagila (cariprazine)." Recordati Pharmaceuticals Ltd (2022):
  3. "Product Information. Reagila (cariprazine)." Gedeon Richter Australia Pty Ltd (2022):
  4. "Product Information. Vraylar (cariprazine)." AbbVie Corporation (2022):
View all 4 references

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Drug and food interactions

Moderate

cariprazine food

Applies to: cariprazine

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of cariprazine. The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism of cariprazine by certain compounds present in grapefruit. When cariprazine (0.5 mg/day) was coadministered with the potent CYP450 3A4 inhibitor, ketoconazole (400 mg/day), cariprazine peak plasma concentration (Cmax) and systemic exposure (AUC) increased by approximately 3.5- and 4-fold, respectively, while Cmax and AUC of DDCAR increased by approximately 1.5-fold each. The Cmax and AUC of another active metabolite, desmethyl cariprazine (DCAR), decreased by approximately one-third. 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 cariprazine may increase the risk of adverse effects such as extrapyramidal symptoms, cognitive and motor impairment, hyperglycemia, dyslipidemia, weight gain, orthostatic hypotension, leucopenia, neutropenia, seizures, and dysphagia.

MANAGEMENT: Patients should avoid the consumption of grapefruit and grapefruit juice during treatment with cariprazine.

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  2. "Product Information. Vraylar (cariprazine)." Actavis Pharma, Inc. (2015):

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Moderate

telotristat ethyl food

Applies to: Xermelo (telotristat)

ADJUST DOSING INTERVAL: Food increases the systemic exposure to both telotristat ethyl and its active metabolite, telotristat. Following administration of a single 500 mg dose of telotristat ethyl (twice the recommended dose) with a high-fat meal, telotristat ethyl peak plasma concentration (Cmax) and systemic exposure (AUC) were 112% and 264% higher, respectively, compared to administration under fasted conditions. The Cmax and AUC values for telotristat were also increased by 47% and 33%, respectively. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase has been shown to be approximately 29 times higher than that of the parent drug.

MANAGEMENT: Telotristat ethyl should be administered with food.

References

  1. "Product Information. Xermelo (telotristat ethyl)." Lexicon Pharmaceuticals, Inc. (2017):

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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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