Drospirenone And Ethinyl Estradiol

 
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What is/are Drospirenone And Ethinyl Estradiol?

Drospirenone (INN, USAN), also known as 1,2-dihydrospirorenone, is a synthetic hormone used in birth control pills.

It is sold under the brand names Yasmin, Yasminelle, Yaz, Beyaz, Ocella, Zarah, and Angeliq, all of which are combination products of drospirenone with an estrogen such as ethinylestradiol.

Medical uses

Drospirenone is an ingredient in some birth control pills and hormone replacement therapy. In combination with ethinyl estradiol it is used as contraception, and for women who want contraception it is also approved by the U.S. Food and Drug Administration (FDA) to treat moderate acne and premenstrual dysphoric disorder.

Adverse effects

Women who take contraceptive pills containing drospirenone have a six- to sevenfold risk of developing thromboembolism (dangerous blood clots) compared to women who do not take any contraceptive pill, and have twice the risk compared to women who take a contraceptive pill containing levonorgestrel.

Drospirenone can increase potassium to dangerous levels (hyperkalemia). It is likely to be especially dangerous or fatal for patients taking other drugs that also may increase potassium levels, such as ACE inhibitors, angiotensin-II receptor agonists, potassium-sparing diuretics, potassium supplementation, heparin, aldosterone antagonists, and NSAIDs.

Yasmin was the first oral contraceptive that used drospirenone, and Yaz, the best-selling oral contraceptive in the US, also contains drospirenone. The labels for all contraceptives containing drospirenone warn that the drugs should not be used by women with hepatic dysfunction, renal insufficiency, or adrenal insufficiency. Like all oral contraceptives, these birth control pills should also not be used by women who smoke or have a history of DVT, stroke, or other blood clots.

While all oral contraceptives can increase the risk for venous thrombembolic events, including fatal blood clots, several studies have reported a greater risk for women taking contraceptives containing drospirenone. One study showed more than a 600 percent increased risk of these blood clots compared to non-users, compared to 360 percent higher for women taking birth control pills containing levonorgestrel, a different type of progesterone found in many generic birth control pills.

When the U.S. Food and Drug Administration (FDA) became concerned about the risks of drospirenone, they funded studies based on the medical records of more than 800,000 women taking oral contraceptives. They found that the risk of VTE, which includes dangerous and potentially fatal blood clots, was 93% higher for women who had been taking oral contraceptives made with drospirenone for only 3 months or less and 290% higher for women taking drospirenone oral contraceptives for 7–12 months, compared to women taking other types of oral contraceptives. To determine the exact risk for women of different ages and different circumstances, further study is warranted.

The FDA recently updated the label for contraceptives containing drospirenone to include warnings for stopping use prior to and after surgery, and to warn that contraceptives with drospirenone may have a higher risk of dangerous blood clots.

Pharmacology

Pharmacodynamics

Drospirenone differs from other synthetic progestins in that its pharmacological profile in preclinical studies shows it to be closer to the natural progesterone. As such it has potent antimineralocorticoid properties, counteracts the estrogen-stimulated activity of the renin-angiotensin-aldosterone system, and has also been shown to possess mild antiandrogen activity.

The antimineralocorticoid properties exhibited by drospirenone promote sodium excretion and prevent water retention.

Pharmacokinetics

Drospirenone is taken orally with about 76% bioavailability. It is bound not by sex hormone-binding globulin or corticosteroid binding globulin, but by other serum proteins. Metabolites have not been shown to be biologically active, show up in urine and feces, and are essentially completely excreted within 10 days.

This article uses material from the Wikipedia article Drospirenone And Ethinyl Estradiol, which is released under the Creative Commons Attribution-Share-Alike License 3.0.

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