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Drug Interactions between colestipol and Estratest

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

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Interactions between your drugs

Moderate

esterified estrogens colestipol

Applies to: Estratest (esterified estrogens / methyltestosterone) and colestipol

ADJUST DOSING INTERVAL: Coadministration with bile-acid binding resins such as cholestyramine may decrease the plasma concentrations and therapeutic effects of estrogens and progestins. The proposed mechanism involves delaying or reducing the absorption of concomitant orally administered drugs by cholestyramine. In addition, it has also been suggested that bile-acid binding resins may interfere with the enterohepatic recycling of estrogens and therefore increase their elimination.

MANAGEMENT: Estrogens and/or progestin-containing oral medications should be administered at least one hour before or four to six hours after bile-acid binding resins such as cholestyramine, colestipol, and colesevelam. Patients receiving this combination should be advised to closely follow dosing schedules to prevent loss of therapeutic effects.

References

  1. (2002) "Product Information. Questran (cholestyramine)." Par Pharmaceutical Inc
  2. Cerner Multum, Inc. "Australian Product Information."
  3. Agencia Española de Medicamentos y Productos Sanitarios Healthcare (2008) Centro de información online de medicamentos de la AEMPS - CIMA. https://cima.aemps.es/cima/publico/home.html
  4. Cerner Multum, Inc. (2015) "Canadian Product Information."
  5. Underhill KL, Rotter BA, Thompson BK, Prelusky DB, Trenholm HL (1995) "Effectiveness of cholestyramine in the detoxification of zearalenone as determined in mice." Bull Environ Contam Toxicol, 54, p. 128-34
  6. Arts CJM, Govers CARL, van den Berg H, Wolters MGE, van Leeuwen P, Thijssen JHH (1991) "In vitro binding of estrogens by dietary fiber and the in vivo apparent digestibility tested in pigs." J Steroid Biochem Mol Biol, 38, p. 621-8
  7. (2021) "Product Information. Nextstellis (drospirenone-estetrol)." Mayne Pharma
View all 7 references

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Drug and food interactions

Moderate

colestipol food

Applies to: colestipol

ADJUST DOSING INTERVAL: Bile acid sequestrants and the phosphate binder, sevelamer, can decrease the absorption of fat-soluble vitamins A, D, E, and K. In non-clinical safety studies, rats administered colesevelam at doses greater than 30-fold the projected human clinical dose developed hemorrhage in association with vitamin K deficiency. In a crossover study involving healthy subjects, coadministration of sevelamer with calcitriol resulted in a significant reduction in bioavailability for calcitriol (calcitriol with sevelamer vs calcitriol alone: AUC 137 pg*h/mL vs 318 pg*h/mL and Cmax 40.1 pg/mL vs 49.7 pg/mL, respectively).

MANAGEMENT: Oral vitamin supplements should be administered at least 4 hours before colesevelam and either 1 hour before or 4 to 6 hours after other bile acid sequestrants and sevelamer.

References

  1. (2001) "Product Information. Rocaltrol (calcitriol)." Roche Laboratories
  2. (2001) "Product Information. Welchol (colesevelam)." Daiichi Sankyo, Inc.
  3. (2005) "Product Information. Fosamax Plus D (alendronate-cholecalciferol)." Merck & Co., Inc
  4. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  5. Cerner Multum, Inc. "Australian Product Information."
  6. Peirce D, Hossack S, Poole L, et al. (2011) "The effect of sevelamer carbonate and lanthanum carbonate on the pharmacokinetics of oral calcitriol." Nephrol Dial Transplant, 26, p. 1615-21
View all 6 references

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Minor

esterified estrogens food

Applies to: Estratest (esterified estrogens / methyltestosterone)

Coadministration with grapefruit juice may increase the bioavailability of oral estrogens. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall induced by certain compounds present in grapefruits. In a small, randomized, crossover study, the administration of ethinyl estradiol with grapefruit juice (compared to herbal tea) increased peak plasma drug concentration (Cmax) by 37% and area under the concentration-time curve (AUC) by 28%. Based on these findings, grapefruit juice is unlikely to affect the overall safety profile of ethinyl estradiol. However, as with other drug interactions involving grapefruit juice, the pharmacokinetic alterations are subject to a high degree of interpatient variability. Also, the effect on other estrogens has not been studied.

References

  1. Weber A, Jager R, Borner A, et al. (1996) "Can grapefruit juice influence ethinyl estradiol bioavailability?" Contraception, 53, p. 41-7
  2. Schubert W, Eriksson U, Edgar B, Cullberg G, Hedner T (1995) "Flavonoids in grapefruit juice inhibit the in vitro hepatic metabolism of 17B-estradiol." Eur J Drug Metab Pharmacokinet, 20, p. 219-24

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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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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