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Cardioquin and Loperamide and Simethicone

Determining the interaction of Cardioquin and Loperamide and Simethicone and the possibility of their joint administration.

Check result:
Cardioquin <> Loperamide and Simethicone
Relevance: 21.01.2023 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

QuiNIDine may significantly increase the blood levels of loperamide. This can lead to serious and potentially fatal complications such as irregular heart rhythm and cardiac arrest, especially if you use more than the recommended doses of loperamide. You may also be more susceptible if you have a heart condition called congenital long QT syndrome, other cardiac diseases, conduction abnormalities, or electrolyte disturbances (for example, magnesium or potassium loss due to severe or prolonged diarrhea or vomiting). Do not exceed the dose and frequency or duration of use of loperamide recommended on the product label or prescribed by your doctor. Talk to your doctor if you have any questions or concerns. Your doctor may be able to prescribe alternatives that do not interact, or you may need a dose adjustment or more frequent monitoring to safely use both medications. You should seek immediate medical attention if you develop sudden dizziness, lightheadedness, fainting, shortness of breath, or heart palpitations during treatment with these medications. 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.

Professional:

MONITOR CLOSELY: Coadministration with quinidine may increase the concentrations of loperamide in plasma and central nervous system (CNS). Opioid and other adverse effects may be enhanced. The proposed mechanism is inhibition of P-glycoprotein (P-gp) efflux transporter by quinidine, resulting in increased gastrointestinal absorption as well as increased penetration of loperamide across the blood brain barrier. Following administration of loperamide 16 mg and quinidine 600 mg to healthy subjects (n=8), mean loperamide systemic exposure (AUC) increased by 2.5 fold and respiratory response to carbon dioxide decreased. The interaction may also occur with quinine, the isomer of quinidine and also a potent P-gp inhibitor.

MONITOR CLOSELY: The use of higher than recommended dosages of loperamide (e.g., through abuse or misuse) has been associated with serious and potentially fatal cardiac adverse events, including syncope, cardiac arrest, and arrhythmia related to prolongation of the QT interval. Under such circumstances, coadministration with other agents that can prolong the QT interval such as quinidine or quinine may result in additive effects and increased risk of ventricular arrhythmias such as torsade de pointes and sudden death. According to the FDA, the agency received reports of 48 cases of serious heart problems associated with use of loperamide from when it was first approved in 1976 through 2015. Thirty-one of these cases resulted in hospitalizations, and 10 patients died. The serious heart problems occurred mostly in patients who were using loperamide dosages that were much higher than recommended in an attempt to achieve euphoria, prevent opioid withdrawal, or treat diarrhea. In the most severe cases, individuals self-treated with dosages ranging from 70 to 1600 mg/day, or 4 to 100 times the recommended dosage. In other cases, patients were taking the recommended dosage, but with concomitant interacting drugs such as quinidine or quinine that caused an increase in loperamide levels. There have been additional cases of serious heart problems associated with loperamide use reported in the medical literature. 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 as 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).

MANAGEMENT: Caution is recommended if loperamide is used with quinidine, a drug that can prolong the QT interval as well as increase the plasma and CNS concentrations of loperamide. Patients should be counseled to not exceed the recommended dosage and frequency or duration of use of loperamide, and 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. If loperamide-induced cardiotoxicity is suspected, promptly discontinue loperamide and initiate therapy to manage and prevent cardiac arrhythmias and adverse outcomes. Electrical pacing or cardioversion may be necessary if torsade de pointes persists despite pharmacotherapy. In many of the reported cases of loperamide-induced cardiotoxicity, standard antiarrhythmic drugs were ineffective, and electrical pacing or cardioversion was necessary.

References
  • US Food and Drug Administration "FDA warns about serious heart problems with high doses of the antidiarrheal medicine loperamide (Imodium), including from abuse and misuse. Available from: URL: http://www.fda.gov/downloads/Drugs/DrugSafety/UCM505108.pdf." ([2016, Jun 7]):
  • Sadeque AJ, Wandel C, He H, Shah S, Wood AJ "Increased drug delivery to the brain by P-glycoprotein inhibition." Clin Pharmacol Ther 68 (2000): 231-7
  • Adachi Y, Suzuki H, Sugiyama Y "Quantitative evaluation of the function of small intestinal P-glycoprotein: comparative studies between in Situ and in Vivo." Pharm Res 20 (2003): 1163-9
  • Crowe A, Wong P "Potential roles of P-gp and calcium channels in loperamide and diphenoxylate transport." Toxicol Appl Pharmacol 193 (2003): 127-37
Cardioquin

Generic Name: quinidine

Brand name: Quin-G, Cardioquin, Quinora, Quinidex Extentabs, Quinaglute Dura-Tabs, Quin-Release

Synonyms: n.a.

Loperamide and Simethicone

Generic Name: loperamide / simethicone

Brand name: Imodium Multi-Symptom Relief

Synonyms: n.a.

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

Interaction with food and lifestyle