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Drug Interactions between rilpivirine and Zagam Respipac

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

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Interactions between your drugs

Major

sparfloxacin rilpivirine

Applies to: Zagam Respipac (sparfloxacin) and rilpivirine

CONTRAINDICATED: Sparfloxacin may cause dose-related prolongation of the QT interval in some patients. 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. Torsade de pointes has been reported in a few patients receiving sparfloxacin alone and with antiarrhythmic agents like amiodarone and disopyramide.

MANAGEMENT: Coadministration of sparfloxacin with other drugs that can prolong the QT interval is considered contraindicated.

References

  1. Thomas M, Maconochie JG, Fletcher E "The dilemma of the prolonged QT interval in early drug studies." Br J Clin Pharmacol 41 (1996): 77-81
  2. Jaillon P, Morganroth J, Brumpt I, Talbot G "Overview of electrocardiographic and cardiovascular safety data for sparfloxacin. Sparfloxacin Safety Group." J Antimicrob Chemother 37(suppl a) (1996): 161-7
  3. Zix JA, GeerdesFenge HF, Rau M, Vockler J, Borner K, Koeppe P, Lode H "Pharmacokinetics of sparfloxacin and interaction with cisapride and sucralfate." Antimicrob Agents Chemother 41 (1997): 1668-72
  4. "Product Information. Zagam (sparfloxacin)." Rhone Poulenc Rorer PROD (2001):
  5. Demolis JL, Charransol A, Funck-Brentano C, Jaillon P "Effects of a single oral dose of sparfloxacin on ventricular repolarization in healthy volunteers." Br J Clin Pharmacol 41 (1996): 499-503
  6. Dupont H, Timsit JF, Souweine B, Gachot B, Wolff M, Regnier B "Torsades de pointe probably related to sparfloxacin." Eur J Clin Microbiol Infect Dis 15 (1996): 350-1
  7. Lipsky BA, Dorr MB, Magner DJ, Talbot GH "Safety profile of sparfloxacin, a new fluoroquinolone antibiotic." Clin Ther 21 (1999): 148-59
  8. Owens RC "Risk assessment for antimicrobial agent-induced QTc interval prolongation and torsades de pointes." Pharmacotherapy 21 (2001): 301-19
  9. Iannini PB, Doddamani S, Byazrova E, Curciumaru I, Kramer H "Risk of torsades de pointes with non-cardiac drugs." BMJ 322 (2001): 46-7
  10. Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9
  11. Kang J, Wang L, Chen XL, Triggle DJ, Rampe D "Interactions of a series of fluoroquinolone antibacterial drugs with the human cardiac K+ channel HERG." Mol Pharmacol 59 (2001): 122-6
  12. Oliphant CM, Green GM "Quinolones: a comprehensive review." Am Fam Physician 65 (2002): 455-64
  13. Owens RC Jr, Ambrose PG "Torsades de pointes associated with fluoroquinolones." Pharmacotherapy 22 (2002): 663-8; discussion 668-72
  14. Iannini PB "Cardiotoxicity of macrolides, ketolides and fluoroquinolones that prolong the QTc interval." Expert Opin Drug Saf 1 (2002): 121-8
  15. Owens RC "QT Prolongation with Antimicrobial Agents : Understanding the Significance." Drugs 64 (2004): 1091-124
  16. Katritsis D, Camm AJ "Quinolones: cardioprotective or cardiotoxic." Pacing Clin Electrophysiol 26 (2003): 2317-20
  17. Stahlmann R "Clinical toxicological aspects of fluoroquinolones." Toxicol Lett 127 (2002): 269-77
  18. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  19. Canadian Pharmacists Association "e-CPS. http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink" (2006):
  20. Falagas ME, Rafailidis PI, Rosmarakis ES "Arrhythmias associated with fluoroquinolone therapy." Int J Antimicrob Agents 29 (2007): 374-9
  21. Cerner Multum, Inc. "Australian Product Information." O 0
View all 21 references

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Drug and food interactions

Moderate

rilpivirine food

Applies to: rilpivirine

GENERALLY AVOID: Coadministration with grapefruit or grapefruit juice may increase the plasma concentrations of rilpivirine. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruit. In 15 study subjects given rilpivirine (150 mg once daily) with the potent CYP450 3A4 inhibitor ketoconazole (400 mg once daily), mean rilpivirine peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Cmin) were increased by 30%, 49% and 76%, respectively. In 16 study subjects given a single 500 mg dose of a less potent CYP450 3A4 inhibitor chlorzoxazone two hours after rilpivirine (150 mg once daily), mean rilpivirine Cmax, AUC, and Cmin were increased by 17%, 25%, and 18%, respectively. Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability). 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. Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

ADJUST DOSING INTERVAL: The administration of rilpivirine in a fasting state may decrease its oral absorption. Under fasted conditions, the systemic exposure to rilpivirine was 40% lower compared to normal or high-fat caloric meals (533 to 928 Kcal). The systemic exposure was 50% lower when rilpivirine was taken with a protein-rich nutritional beverage.

MANAGEMENT: Coadministration of grapefruit or grapefruit juice with rilpivirine should preferably be avoided. For optimal absorption, it is recommended to take rilpivirine on a regular schedule with a meal.

References

  1. "Product Information. Edurant (rilpivirine)." Tibotec Pharmaceuticals (2011):
  2. Cerner Multum, Inc. "Canadian Product Information." O 0 (2015):

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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

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