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Drug Interactions between nisoldipine and rifabutin

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

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Interactions between your drugs

Major

rifabutin nisoldipine

Applies to: rifabutin and nisoldipine

GENERALLY AVOID: Potent inducers of CYP450 3A4 may significantly decrease the plasma concentrations of most calcium channel blockers (CCBs), as CYP450 3A4 is the primary isoenzyme responsible for their metabolism. Some drug interaction studies have reported a significant reduction in plasma levels for certain CCBs. For example, when a single dose of nimodipine (60 mg) was administered to patients with epilepsy (n=8) who were also receiving chronic treatment with a potent CYP450 3A4-inducing antiepileptic agent (phenytoin, phenobarbital and/or carbamazepine), the mean areas under the plasma nimodipine concentration curve (AUC) were lowered by about 7-fold compared to the control group. In another drug interaction study comparing nisoldipine pharmacokinetics in epileptic patients on concurrent phenytoin therapy (n=12) to healthy controls (n=12), the AUC of nisoldipine was approximately 90% lower (1.6 vs 15.2 mcg/L/h) in patients on concomitant phenytoin therapy. Clinical data for all calcium channel blockers with potent CYP450 3A4 inducers are not available.

MANAGEMENT: Concomitant use of calcium channel blockers (CCBs) primarily metabolized by CYP450 3A4 with potent CYP450 3A4 inducers should generally be avoided. Additional monitoring and dose adjustments may be required if coadministration is necessary, particularly during initiation, titration, or discontinuation of the CYP450 3A4 inducer. Individual product labeling for the CCB should be consulted for further guidance.

References (5)
  1. Tada Y, Tsuda Y, Otsuka T, et al. (1992) "Case report: nifedipine-rifampicin interaction attenuates the effect on blood pressure in a patient with essential hypertension." Am J Med Sci, 303, p. 25-7
  2. (2001) "Product Information. Mycobutin (rifabutin)." Pharmacia and Upjohn
  3. (2001) "Product Information. Rifadin (rifampin)." Hoechst Marion Roussel
  4. Michelucci R, Cipolla G, Passarelli D, Gatti G, et al. (2024) Reduced plasma nisoldipine concentrations in phenytoin-treated patients with epilepsy https://pubmed.ncbi.nlm.nih.gov/8917062/
  5. Tartara A, Galimberti CA, Manni R, zucca c, et al. (2024) Differential effects of valproic acid and enzyme-inducing anticonvulsants on nimodipine pharmacokinetics in epileptic patients https://pubmed.ncbi.nlm.nih.gov/1777370/

Drug and food interactions

Moderate

nisoldipine food

Applies to: nisoldipine

GENERALLY AVOID: The consumption of grapefruit juice may be associated with significantly increased plasma concentrations of some calcium channel blockers (CCBs) when they are administered orally. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. The interaction has been reported with the dihydropyridine CCBs (in roughly decreasing order of magnitude) felodipine, nisoldipine, nifedipine, and nimodipine, often with a high degree of interindividual variability. Grapefruit juice caused more than twofold increases in felodipine, nifedipine, and nisoldipine AUCs.

MANAGEMENT: The manufacturers of nifedipine and nisoldipine recommend avoiding grapefruit juice. Patients treated orally with other calcium channel blockers should be advised to avoid consumption of large amounts of grapefruits and grapefruit juice to prevent any undue fluctuations in serum drug levels. Increased effects on blood pressure may persist for up to 4 days after the consumption of grapefruit juice. Monitoring for calcium channel blocker adverse effects (e.g., headache, hypotension, syncope, tachycardia, edema) is recommended.

References (19)
  1. Edgar B, Bailey D, Bergstrand R, Johnsson G, Regardh CG (1992) "Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics of felodipine--and its potential clinical relevance." Eur J Clin Pharmacol, 42, p. 313-7
  2. (2002) "Product Information. Plendil (felodipine)." Merck & Co., Inc
  3. (2002) "Product Information. Procardia (nifedipine)." Pfizer U.S. Pharmaceuticals
  4. Bailey DG, Arnold JM, Munoz C, Spence JD (1993) "Grapefruit juice--felodipine interaction: mechanism, predictability, and effect of naringin." Clin Pharmacol Ther, 53, p. 637-42
  5. Bailey DG, Arnold JMO, Spence JD (1994) "Grapefruit juice and drugs - how significant is the interaction." Clin Pharmacokinet, 26, p. 91-8
  6. Bailey DG, Arnold JM, Strong HA, Munoz C, Spence JD (1993) "Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics." Clin Pharmacol Ther, 54, p. 589-94
  7. Yamreudeewong W, Henann NE, Fazio A, Lower DL, Cassidy TG (1995) "Drug-food interactions in clinical practice." J Fam Pract, 40, p. 376-84
  8. (1995) "Grapefruit juice interactions with drugs." Med Lett Drugs Ther, 37, p. 73-4
  9. (2001) "Product Information. Sular (nisoldipine)." Astra-Zeneca Pharmaceuticals
  10. Josefsson M, Zackrisson AL, Ahlner J (1996) "Effect of grapefruit juice on the pharmacokinetics of amlodipine in healthy volunteers." Eur J Clin Pharmacol, 51, p. 189-93
  11. Bailey DG, Malcolm J, Arnold O, Spence JD (1998) "Grapefruit juice-drug interactions." Br J Clin Pharmacol, 46, p. 101-10
  12. Bailey DG, Kreeft JH, Munoz C, Freeman DJ, Bend JR (1998) "Grapefruit juice felodipine interaction: Effect of naringin and 6',7'-dihydroxybergamottin in humans." Clin Pharmacol Ther, 64, p. 248-56
  13. Fuhr U, Maier-Bruggemann A, Blume H, et al. (1998) "Grapefruit juice increases oral nimodipine bioavailability." Int J Clin Pharmacol Ther, 36, p. 126-32
  14. Gunston GD, Mehta U (2000) "Potentially serious drug interactions with grapefruit juice." S Afr Med J, 90, p. 41
  15. Takanaga H, Ohnishi A, Maatsuo H, et al. (2000) "Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model." Br J Clin Pharmacol, 49, p. 49-58
  16. Bailey DG, Dresser GR, Kreeft JH, Munoz C, Freeman DJ, Bend JR (2000) "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients." Clin Pharmacol Ther, 68, p. 468-77
  17. Ho PC, Ghose K, Saville D, Wanwimolruk S (2000) "Effect of grapefruit juice on pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers." Eur J Clin Pharmacol, 56, p. 693-8
  18. Fuhr U, Muller-Peltzer H, Kern R, et al. (2002) "Effects of grapefruit juice and smoking on verapamil concentrations in steady state." Eur J Clin Pharmacol, 58, p. 45-53
  19. Cerner Multum, Inc. "UK Summary of Product Characteristics."

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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