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Drug Interactions between Aralen Phosphate and gepirone

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

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Interactions between your drugs

Major

chloroquine gepirone

Applies to: Aralen Phosphate (chloroquine) and gepirone

Consumer information for this interaction is not currently available.

GENERALLY AVOID: Chloroquine and hydroxychloroquine can cause dose-related prolongation of the QT interval. Theoretically, coadministration with other agents that can prolong the QT interval may result in additive effects and increased risk of ventricular arrhythmias including torsade de pointes and sudden death. In general, the risk of an individual agent or a combination of agents causing ventricular arrhythmia in association with QT prolongation is largely unpredictable but may be increased by certain underlying risk factors such advanced age, congenital long QT syndrome, cardiac disease, and electrolyte disturbances (e.g., hypokalemia, hypomagnesemia). In addition, the extent of drug-induced QT prolongation is dependent on the particular drug(s) involved and dosage(s) of the drug(s). Currently available data seem to suggest a significantly higher risk of QTc prolongation (>= 60 msec increase from baseline or absolute QTc >=500 msec ) in COVID-19 patients treated with hydroxychloroquine or chloroquine, with or without azithromycin, than has been previously reported in other settings. Because COVID-19 may disproportionately affect the elderly and individuals with preexisting heart disease, and cardiac complications such as myocarditis and cardiomyopathy as well as organ failure may occur in patients with severe COVID-19, it appears likely that hospitalized patients with COVID-19 may represent a particularly susceptible and high-risk population, and other, less critically ill patients may not have the same arrhythmic risk.

MANAGEMENT: Coadministration of chloroquine or hydroxychloroquine with other drugs that can prolong the QT interval should generally be avoided, particularly in patients with baseline QT prolongation (e.g., QTc >=500 msec) or congenital long QT syndrome. Close monitoring of QTc interval, electrolyte levels, and renal and hepatic function is recommended if concomitant use is required and benefits are anticipated to outweigh the risks. Electrolyte abnormalities should be corrected prior to initiating treatment with chloroquine or hydroxychloroquine. Patients should be advised to seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitation, irregular heart rhythm, shortness of breath, or syncope. Because chloroquine and hydroxychloroquine are eliminated slowly from the body, the potential for drug interactions should be observed for a prolonged period following their discontinuation.

References

  1. "Product Information. Plaquenil (hydroxychloroquine)." Apothecon Inc (2022):
  2. "Product Information. Chloroquine Phosphate (chloroquine)." West Ward Pharmaceutical Corporation (2005):
  3. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  4. "Product Information. Hydroxychloroquine Sulfate (hydroxychloroquine)." Prasco Laboratories (2017):
  5. US Food and Drug Administration "Hydroxychloroquine or Chloroquine for COVID-19: Drug Safety Communication - FDA Cautions Against Use Outside of the Hospital Setting or a Clinical Trial Due to Risk of Heart Rhythm Problems. https://www.fda.gov/safety/medical-product-safety-information/h" (2020):
  6. US Food and Drug Administration "FACT SHEET FOR HEALTH CARE PROVIDERS EMERGENCY USE AUTHORIZATION (EUA) OF HYDROXYCHLOROQUINE SULFATE SUPPLIED FROM THE STRATEGIC NATIONAL STOCKPILE FOR TREATMENT OF COVID-19 IN CERTAIN HOSPITALIZED PATIENTS. https://www.fda.gov/media/136537/download" (2020):
  7. US Food and Drug Administration "FACT SHEET FOR HEALTH CARE PROVIDERS EMERGENCY USE AUTHORIZATION (EUA) OF CHLOROQUINE PHOSPHATE SUPPLIED FROM THE STRATEGIC NATIONAL STOCKPILE FOR TREATMENT OF COVID-19 IN CERTAIN HOSPITALIZED PATIENTS. https://www.fda.gov/media/136535/download" (2020):
  8. National Institutes of Health (NIH) "Coronavirus Disease 2019 (COVID-19) Treatment Guidelines. https://covid19treatmentguidelines.nih.gov/" (2020):
  9. Mercuro NJ, Yen CF, Shim DJ, et al. "Risk of QT interval prolongation associated with the use of hydroxychloroquine with or without concomitant azithromycin among hospitalized patients testing positive for coronavirus disease 2019 (COVID-19)" JAMA Cardiol May 1:e201834 (2020): epub ahead of print
  10. Bonow RO, Hernandez AF, Turakhia M "Hydroxychloroquine, coronavirus disease 2019, and QT prolongation." JAMA Cardiol May 1 (2020): epub ahead of print
  11. Bessiere F, Roccia H, Deliniere A, et al. "Assessment of QT intervals in a case series of patients with coronavirus disease 2019 (COVID-19) infection treated with hydroxychloroquine alone or in combination with azithromycin in an intensive care unit." JAMA Cardiol May 1 (2020): epub ahead of print
  12. Saleh M, Gabriels J, ChangD, et al. "The effect of chloroquine, hydroxychloroquine and azithromycin on the corrected QT interval in patients with SARS-CoV-2 infection." Circ Arrhythm Electrophysiol Apr 29 (2020): epub ahead of print
  13. Javelot H, El-Hage W, Meyer G, Becker G, Michel B, Hingray C "COVID-19 and (hydroxy)chloroquine-azithromycin combination: should we take the risk for our patients?" Br J Clin Pharmacol Apr 29 (2020): epub ahead of print
  14. Sacher F, Fauchier L, Boveda S, et al. "Use of drugs with potential cardiac effect in the setting of SARS-CoV-2 infection." Arch Cardiovasc Dis Apr 24 (2020): epub ahead of print
  15. Smit C, Peeters MYM, van den Anker JN, Knibbe CAJ "Chloroquine for SARS-CoV-2: Implications of its unique pharmacokinetic and safety properties." Clin Pharmacokinet Ar 18 (2020): epub ahead of print
  16. Roden DM, Harrington RA, Poppas A, Russo AM "Considerations for drug interactions on QTc in exploratory COVID-19 (Coroanvirus disease 2019) treatment." Heart Rhythm Apr 14 (2020): epub ahead of print
  17. Sapp JL, Alqarawi W, MacIntyre CJ, et al. "Guidance on minimizing risk of drug-induced ventricular arrhythmia during treatment of COVID-19: A statement from the Canadian Heart Rhythm Society." Can J Cardiol Apr 8 (2020): epub ahead of print
  18. Kapoor A, Pandurangi U, Arora V, et al. "Cardiovascular risks of hydroxychloroquine in treatment and prophylaxis of COVID-19 patients: A scientific statement from the Indian Heart Rhythm Society." Indian Pacing Electorphysiol J Apr 8 (2020): epub ahead of print
  19. Giudicessi JR, Noseworthy PA, Friedman PA, Ackerman MJ "Urgent guidance for navigating and circumventing the QTc-prolonging and torsadogenic potential of possible pharmacotherapies for coronavirus disease 19 (COVID-19)" Mayo Clin Proc Apr 7 (2020): epub ahead of print
  20. Borba MGS, Val FFA, Sampaio VS, et al. "Effect of high vs low doses of chloroquine diphosphate as adjunctive therapy for patients hospitalized with severe acute respiratory syndrome coronavirus 1 (SARS-CoV-2) infection: A randomized clinical trial." JAMA Netw Open Apr 1 (2020): epub ahead of print
  21. mitra RL, Greenstein SA, Epstein lm "An algorithm for managing QT prolongation in coronavirus disease 2019 (COVID-19) patients treated with either chloroquine or hydroxychloroquine in conjunction with azithromycin; Possible benefits of intravenous lidocaine." HeartRythm Case Rep Apr 1 (2020): epub ahead of print
View all 21 references

Drug and food interactions

Moderate

chloroquine food

Applies to: Aralen Phosphate (chloroquine)

You may want to limit your consumption of grapefruit or grapefruit juice during treatment with chloroquine. Grapefruit juice can significantly increase the blood levels and effects of chloroquine, which may result in an irregular heart rate or other conduction disturbances. Talk to your doctor if you have any questions or concerns. You should seek immediate medical attention if you develop sudden dizziness, lightheadedness, fainting, shortness of breath, or heart palpitations during treatment with chloroquine. 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.

Switch to professional interaction data

Moderate

gepirone food

Applies to: gepirone

Consumer information for this interaction is not currently available.

GENERALLY AVOID: Grapefruit and/or grapefruit juice may increase the plasma concentrations and effects of gepirone. The proposed mechanism is inhibition of CYP450 3A4 mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with grapefruit juice, but has been reported for other CYP450 3A4 inhibitors. For example, when subjects who were at steady state on the strong CYP450 3A4 inhibitor ketoconazole (200 mg twice daily) received a single dose of gepirone (36.3 mg), the maximum plasma concentration (Cmax) and systemic exposure (AUC) of gepirone increased by approximately 5-fold. Similarly, when subjects who were at steady state on the moderate CYP450 3A4 inhibitor verapamil (80 mg three times daily) received a single dose of gepirone (18.2 mg), the maximum plasma concentration (Cmax) and systemic exposure (AUC) of gepirone increased by approximately 2.6-fold. In general, the effects of grapefruit products are concentration-, dose-, and preparation-dependent and can vary widely among both brands and individual patients. Some preparations have demonstrated strong CYP450 3A4 inhibition, while others have demonstrated moderate inhibition.

ADJUST DOSING INTERVAL: Food enhances the bioavailability of gepirone and its major active metabolites (3'-OH-gepirone and 1-PP). The magnitude of the effect is dependent on the fat content of the meal, but the systemic exposure of gepirone and its major metabolites was consistently higher under fed conditions as compared to the fasted state. The peak plasma concentration (Cmax) of gepirone after intake of a low-fat (about 200 calorie) breakfast was 27% higher, after a medium-fat (about 500 calorie) breakfast was 55% higher, and after a high-fat (about 850 calorie) breakfast was 62% higher than the Cmax achieved in the fasted state. Likewise, the systemic exposure (AUC) of gepirone was about 14% higher after a low-fat breakfast, 22% higher after a medium-fat breakfast, and 32% to 37% higher after a high-fat breakfast when compared to the AUC achieved in the fasted state. The effect of varying amounts of fat on the AUC and Cmax of 3'-OH-gepirone and 1-PP were similar to that of gepirone.

MANAGEMENT: Coadministration of gepirone with grapefruit products should be avoided. If grapefruit juice is consumed, monitoring for adverse effects (e.g., QT prolongation, serotonin syndrome, dizziness, nausea, insomnia, abdominal pain, and/or dyspepsia) should be considered. Gepirone should be taken orally with food at the approximately the same time each day. Tablets should be swallowed whole.

References

  1. "Product Information. Exxua (gepirone)." Mission Pharmacal Company 1 (2023):
  2. FDA. U.S. Food and Drug Administration "Grapefruit juice and some drugs don't mix. https://www.fda.gov/consumers/consumer-updates/grapefruit-juice-and-some-drugs-dont-mix" (2024):
  3. Chen M, Zhou S, Fabriaga E, Zhang P, Zhou Q "Food-drug interactions precipitated by fruit juices other than grapefruit juice: an update review. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9326888/" (2024):
  4. Kiani J, Imam SZ "Medicinal importance of grapefruit juice and its interaction with various drugs. https://nutritionj.biomedcentral.com/articles/10.1186/1475-2891-6-33" (2024):
View all 4 references

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

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