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Grapefruit-drug interactions and Estrogen Pills

Posted in Q & A Health | Wednesday, March 26th, 2008 | Trackback

Q & A HEALTH

Grapefruit-drug interactions and Estrogen Pills

By Richard Harkness, Pharm, CDM, Natural Medicines Specialist

March 2008

QUESTION: I read your column on grapefruit-drug interactions and this was the first time I’ve heard about an interaction with estrogen. I take Activella. What are the effects on this drug?

ANSWER: Activella is an estradiol-norethindrone combination prescribed for menopausal symptoms. Estradiol is the estrogen component. Natural compounds in grapefruit block enzymes that normally break down estrogen and certain other drugs for removal from the body.

Most clinical sources rate the grapefruit-estrogen interaction as relatively minor. However, I’d still be wary of this combination.

That’s because orally taken estrogen has high first-past metabolism. This means that most of the drug is broken down in the gut and liver before it reaches the general blood circulation. The recommended dose of estrogen takes this into account.

Grapefruit inhibits drug breakdown in the gut and liver, so it tends to have a more pronounced effect on such drugs. The result is that higher-than-expected amounts of drug make it into the bloodstream. It’s similar to taking an excessive dose.

Increased blood levels of estrogen could boost the risk of harmful blood clots and other adverse effects.

That’s why it’s best to use the lowest effective dose of estrogen.

Grapefruit lovers might consider asking their doctor to prescribe estrogen in the form of a skin patch. In this case, estrogen passes through the skin directly into the bloodstream, bypassing the gut and liver, thus minimizing the grapefruit effect.

__________________

Richard Harkness is a consultant pharmacist, natural medicines specialist, and author of eight published books. Write him at 1224 King Henry Drive, Ocean Springs, MS 39564.

Richard Harkness, Pharm, CDM, Natural Medicines Specialist

Email Richard Harkness at: rharkn@aol.com

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