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Drug Interactions between Elestrin and Serzone

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

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Interactions between your drugs

Moderate

estradiol nefazodone

Applies to: Elestrin (estradiol) and Serzone (nefazodone)

MONITOR: The coadministration with nefazodone may increase the plasma concentrations and pharmacologic effects of ethinyl estradiol and other estrogens. The mechanism is nefazodone inhibition of CYP450 3A4, the isoenzyme responsible for the metabolism of estrogens. In one case report, a woman taking a low-dose oral contraceptive (ethinyl estradiol-desogestrel, 20 mcg-150 mcg) developed breast tenderness, bloating, weight gain, and increased premenstrual irritability within a week following the initiation of nefazodone therapy. These symptoms were not present prior to initiating nefazodone and were described as identical to those previously experienced with oral contraceptives containing higher dosages of estrogen that she did not tolerate. In addition, her menstrual period, which had been regular for the past 18 months, was delayed by 5 days. The problems resolved after nefazodone was discontinued.

MANAGEMENT: Clinicians and patients should be aware of the potential for increased pharmacologic effects of estrogens during concomitant administration with nefazodone. Adjustments in the estrogen dosage may be required if an interaction is suspected. Alternatively, antidepressants that do not significantly interfere with CYP450 3A4 metabolism may be considered, including the SSRIs (except fluvoxamine) and venlafaxine.

References

  1. Adson DE, Kotlyar M "A probable interaction between a very low-dose oral contraceptive and the antidepressant nefazodone: a case report." J Clin Psychopharmacol 21 (2001): 618-9

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Drug and food interactions

Moderate

nefazodone food

Applies to: Serzone (nefazodone)

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol. Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

References

  1. Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7
  2. Gilman AG, eds., Nies AS, Rall TW, Taylor P "Goodman and Gilman's the Pharmacological Basis of Therapeutics." New York, NY: Pergamon Press Inc. (1990):
  3. "Product Information. Fycompa (perampanel)." Eisai Inc (2012):
  4. "Product Information. Rexulti (brexpiprazole)." Otsuka American Pharmaceuticals Inc (2015):
View all 4 references

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Minor

estradiol food

Applies to: Elestrin (estradiol)

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. "Can grapefruit juice influence ethinyl estradiol bioavailability?" Contraception 53 (1996): 41-7
  2. Schubert W, Eriksson U, Edgar B, Cullberg G, Hedner T "Flavonoids in grapefruit juice inhibit the in vitro hepatic metabolism of 17B-estradiol." Eur J Drug Metab Pharmacokinet 20 (1995): 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

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