Drospirenone interactions

Food & lifestyle

• grapefruit juice

  Moderate

  Metabolism

  Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. 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.

  What to do: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4. Grapefruit and grapefruit juice should be avoided if an interaction is suspected. Orange juice is not expected to interact with these drugs.

  32 sources

  1. Edgar B, Bailey D, Bergstrand R, et al. "Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics on felodipine and its potential clinical relevance." Eur J Clin Pharmacol 42 (1992): 313-7
  2. Jonkman JH, Sollie FA, Sauter R, Steinijans VW "The influence of caffeine on the steady-state pharmacokinetics of theophylline." Clin Pharmacol Ther 49 (1991): 248-55
  3. Bailey DG, Arnold JM, Munoz C, Spence JD "Grapefruit juice--felodipine interaction: mechanism, predictability, and effect of naringin." Clin Pharmacol Ther 53 (1993): 637-42
  4. Bailey DG, Arnold JMO, Spence JD "Grapefruit juice and drugs - how significant is the interaction." Clin Pharmacokinet 26 (1994): 91-8
  5. Sigusch H, Hippius M, Henschel L, Kaufmann K, Hoffmann A "Influence of grapefruit juice on the pharmacokinetics of a slow release nifedipine formulation." Pharmazie 49 (1994): 522-4
  6. Bailey DG, Arnold JM, Strong HA, Munoz C, Spence JD "Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics." Clin Pharmacol Ther 54 (1993): 589-94
  7. Yamreudeewong W, Henann NE, Fazio A, Lower DL, Cassidy TG "Drug-food interactions in clinical practice." J Fam Pract 40 (1995): 376-84
  8. "Grapefruit juice interactions with drugs." Med Lett Drugs Ther 37 (1995): 73-4

  Show all 32 sourcesShow fewer sources

  9. Hukkinen SK, Varhe A, Olkkola KT, Neuvonen PJ "Plasma concentrations of triazolam are increased by concomitant ingestion of grapefruit juice." Clin Pharmacol Ther 58 (1995): 127-31
  10. Min DI, Ku YM, Geraets DR, Lee HC "Effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of quinidine in healthy volunteers." J Clin Pharmacol 36 (1996): 469-76
  11. Majeed A, Kareem A "Effect of grapefruit juice on cyclosporine pharmacokinetics." Pediatr Nephrol 10 (1996): 395
  12. Clifford CP, Adams DA, Murray S, Taylor GW, Wilkins MR, Boobis AR, Davies DS "Pharmacokinetic and cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice." Br J Clin Pharmacol 42 (1996): p662
  13. Josefsson M, Zackrisson AL, Ahlner J "Effect of grapefruit juice on the pharmacokinetics of amlodipine in healthy volunteers." Eur J Clin Pharmacol 51 (1996): 189-93
  14. Kantola T, Kivisto KT, Neuvonen PJ "Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid." Clin Pharmacol Ther 63 (1998): 397-402
  15. Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A "Interaction between grapefruit juice and diazepam in humans." Eur J Drug Metab Pharmacokinet 23 (1998): 55-9
  16. Bailey DG, Malcolm J, Arnold O, Spence JD "Grapefruit juice-drug interactions." Br J Clin Pharmacol 46 (1998): 101-10
  17. Bailey DG, Kreeft JH, Munoz C, Freeman DJ, Bend JR "Grapefruit juice felodipine interaction: Effect of naringin and 6',7'-dihydroxybergamottin in humans." Clin Pharmacol Ther 64 (1998): 248-56
  18. Garg SK, Kumar N, Bhargava VK, Prabhakar SK "Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy." Clin Pharmacol Ther 64 (1998): 286-8
  19. Lilja JJ, Kivisto KT, Neuvonen PJ "Grapefruit juice-simvastatin interaction: Effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors." Clin Pharmacol Ther 64 (1998): 477-83
  20. Fuhr U, Maier-Bruggemann A, Blume H, et al. "Grapefruit juice increases oral nimodipine bioavailability." Int J Clin Pharmacol Ther 36 (1998): 126-32
  21. Lilja JJ, Kivisto KT, Neuvonen PJ "Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin." Clin Pharmacol Ther 66 (1999): 118-27
  22. Eagling VA, Profit L, Back DJ "Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-I protease inhibitor saquinavir by grapefruit juice components." Br J Clin Pharmacol 48 (1999): 543-52
  23. Damkier P, Hansen LL, Brosen K "Effect of diclofenac, disulfiram, itraconazole, grapefruit juice and erythromycin on the pharmacokinetics of quinidine." Br J Clin Pharmacol 48 (1999): 829-38
  24. Lee AJ, Chan WK, Harralson AF, Buffum J, Bui BCC "The effects of grapefruit juice on sertraline metabolism: An in vitro and in vivo study." Clin Ther 21 (1999): 1890-9
  25. Dresser GK, Spence JD, Bailey DG "Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition." Clin Pharmacokinet 38 (2000): 41-57
  26. Gunston GD, Mehta U "Potentially serious drug interactions with grapefruit juice." S Afr Med J 90 (2000): 41
  27. Takanaga H, Ohnishi A, Maatsuo H, et al. "Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model." Br J Clin Pharmacol 49 (2000): 49-58
  28. Libersa CC, Brique SA, Motte KB, et al. "Dramatic inhibition of amiodarone metabolism induced by grapefruit juice." Br J Clin Pharmacol 49 (2000): 373-8
  29. Bailey DG, Dresser GR, Kreeft JH, Munoz C, Freeman DJ, Bend JR "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients." Clin Pharmacol Ther 68 (2000): 468-77
  30. Zaidenstein R, Soback S, Gips M, Avni B, Dishi V, Weissgarten Y, Golik A, Scapa E "Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers." Ther Drug Monit 23 (2001): 369-73
  31. Sato J, Nakata H, Owada E, Kikuta T, Umetsu M, Ito K "Influence of usual intake of dietary caffeine on single-dose kinetics of theophylline in healthy human subjects." Eur J Clin Pharmacol 44 (1993): 295-8
  32. Flanagan D "Understanding the grapefruit-drug interaction." Gen Dent 53 (2005): 282-5; quiz 286

Conditions

Conditions in which Drospirenone needs care, as documented in this source.

• Hyperkalemia

  Major

  The progestin drospirenone (DRSP) has antialdosterone activity, including the potential for hyperkalemia in high-risk patients. The use of DRSP-containing combination hormone is contraindicated in patients with conditions that predispose to hyperkalemia (renal impairment, hepatic impairment, and adrenal insufficiency). Use caution when prescribing these agents to women who regularly take other medications that can increase potassium, such as nonsteroidal anti-inflammatory drugs (NSAIDs), potassium-sparing diuretics, potassium supplements, angiotensin converting enzyme (ACE) inhibitors, angiotensin-II receptor antagonists, heparin and aldosterone antagonists. It is recommended to monitor serum potassium concentrations during the first month of dosing in high-risk patients who take strong CYP3A4 inhibitors long-term and concomitantly.

  3 sources

  1. "Product Information. Yasmin (drospirenone-ethinyl estradiol)." Berlex Laboratories (2001):
  2. "Product Information. Angeliq (drospirenone-estradiol)." Berlex Laboratories (2005):
  3. "Product Information. Beyaz (drospirenone/ethinyl estradiol/levomefolate)." Bayer Pharmaceutical Inc (2010):

• Eye Diseases

  Moderate

  Estrogens and progestogens may cause retinal thrombosis. Oral contraceptives should be discontinued if there is unexplained partial or complete loss of vision; onset of proptosis or diplopia; papilledema; or retinal vascular lesions. Therapy with these agents should be administered cautiously in patients who have preexisting ocular problems and appropriate diagnostic and therapeutic measures should be instituted. Contact lens wearers who develop visual changes or changes in lens tolerance should be assessed by an ophthalmologist.

  13 sources

  1. "Product Information. Ortho-Novum 1/35 (ethinyl estradiol-norethindrone)." Ortho McNeil Pharmaceutical
  2. "Product Information. Ortho-Novum 10/11 (ethinyl estradiol-norethindrone)." Ortho McNeil Pharmaceutical
  3. "Product Information. Ortho-Cept (desogestrel-ethinyl estradiol)." Ortho McNeil Pharmaceutical (2001):
  4. "Product Information. Demulen 1/50 (ethinyl estradiol-ethynodiol)." Searle
  5. "Product Information. Triphasil (ethinyl estradiol-levonorgestrel)." Wyeth-Ayerst Laboratories (2001):
  6. "Product Information. Ortho-Cyclen (ethinyl estradiol-norgestimate)." Ortho McNeil Pharmaceutical (2001):
  7. "Product Information. Lo/Ovral (ethinyl estradiol-norgestrel)." Wyeth-Ayerst Laboratories (2001):
  8. "Product Information. Ortho-Novum 1/50 (mestranol-norethindrone)." Ortho McNeil Pharmaceutical

  Show all 13 sourcesShow fewer sources

  9. "Product Information. Norplant System (levonorgestrel)." Wyeth-Ayerst Laboratories (2001):
  10. "Product Information. Micronor (norethindrone)." Ortho McNeil Pharmaceutical (2001):
  11. "Product Information. Ovrette (norgestrel)." Wyeth-Ayerst Laboratories (2001):
  12. "Product Information. Prometrium (progesterone)." Virtus Pharmaceuticals LLC (2001):
  13. "Product Information. Nextstellis (drospirenone-estetrol)." Mayne Pharma (2021):

Therapeutic duplication

Drug classes that overlap with Drospirenone, so taking both doubles up the same effect. This source publishes no per-row citations for duplication.

• potassium sparing diuretics

  The recommended maximum number of medicines in the 'potassium sparing diuretics' category to be taken concurrently is usually one.Your list includes two medicines belonging to the 'potassium sparing diuretics' category.

  Example product in the source data (US market): Hydrochlorothiazide/triamterene

• potassium sparing diuretics

  The recommended maximum number of medicines in the 'potassium sparing diuretics' category to be taken concurrently is usually one.Your list includes two medicines belonging to the 'potassium sparing diuretics' category.

  Example product in the source data (US market): Moduretic 5-50

• potassium sparing diuretics

  The recommended maximum number of medicines in the 'potassium sparing diuretics' category to be taken concurrently is usually one.Your list includes two medicines belonging to the 'potassium sparing diuretics' category.

  Example product in the source data (US market): Hydrochlorothiazide/spironolactone

• progestins

  The recommended maximum number of medicines in the 'progestins' category to be taken concurrently is usually one.Your list includes two medicines belonging to the 'progestins' category.

  Example product in the source data (US market): Oriahnn