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Sold under the brand names Cerazette and Mircette among many others, it is a progestin medication used in women’s birth control pills.
It is also used to treat menopausal symptoms in women. The drug is available and is used alone or in combination with an estrogen. It is taken orally.
Desogestrel side effects include menstrual irregularities, headaches, nausea, breast tenderness, mood swings, acne , increased hair growth, and others.
Desogestrel is a progestin, or a synthetic progestin, and therefore is a progesterone receptor agonist, the biological target of progestogens like progesterone.
The drug is a prodrug of etonogestrel (3-ketodesogestrel) in the body.
Desogestrel was discovered in 1972 and introduced for medical use in Europe in 1981.
It became available in the United States in 1992. Desogestrel is sometimes referred to as a “third generation” progestin.
Along with norethisterone, it is one of the only progestins that is widely available as a progestin-only “mini pill” for birth control.
Desogestrel is widely marketed throughout the world. It is available as a generic drug.
Medical uses
Desogestrel is used in hormonal contraception in women, specifically in birth control pills.
It is used only in progestin pills (“mini pills”) and in combination with the estrogen ethinyl estradiol in combined oral contraceptive pills.
Along with norethisterone, it is one of the only progestins that is widely used as a progestin-only “mini pill.”
It is also the only new generation progestin with reduced androgenic activity used in such formulations.
In addition to hormonal contraception, desogestrel has been used in combination with estrogens such as estradiol as a component of menopausal hormone therapy.
The drug has also been used in the treatment of endometriosis.
Available shapes
Desogestrel is available only as 75 μg oral tablets and a 150 μg dose in combination with 20 or 30 μg ethinyl estradiol oral tablets. These formulations are all specifically indicated for contraceptive purposes.
Contraindications
Desogestrel contraindications include:
- Allergy to desogestrel or any other ingredient.
- Active thrombosis (deep vein thrombosis or pulmonary embolism).
- Jaundice or severe liver disease.
- Hormone-sensitive cancers (eg, breast cancer).
- Unexplained vaginal bleeding
- Desogestrel is not indicated for use in pregnancy.
It is not contraindicated during lactation.
Side effects
Common side effects of desogestrel can include menstrual irregularities, amenorrhea, headaches, nausea, breast tenderness, and mood swings (eg, depression), as well as weight gain, acne, and hirsutism .
However, it has also been reported that it does not adversely affect weight. Also, acne and hirsutism are negligible when combined with ethinyl estradiol, and this combination can actually be used to treat such symptoms.
Desogestrel can also cause changes in total, LDL, and HDL cholesterol.
Uncommon side effects of desogestrel can include vaginal infection, contact lens intolerance, vomiting, hair loss, dysmenorrhea, ovarian cysts, and fatigue, while rare side effects include rash, hives, and erythema nodosum.
Breast discharge, ectopic pregnancy, and worsening angioedema can also occur with desogestrel.
Serious side effects of desogestrel-containing combined oral contraceptives can include venous thromboembolism, arterial thromboembolism, hormone-dependent tumors (eg, liver tumors, breast cancer), and melasma.
Overdose
No serious harmful effects have been reported with desogestrel overdose.
Symptoms can include nausea, vomiting, and, in young girls, light vaginal bleeding. In safety studies, doses up to 750 μg / day of desogestrel in women showed no adverse effects in the laboratory or other parameters and had no reported subjective side effects.
There is no antidote to desogestrel overdose and treatment should be based on symptoms.
Interactions
Inducers of liver enzymes can increase the metabolism of desogestrel and etonogestrel and reduce their circulating levels.
This can lead to contraceptive failure.
Examples of liver enzyme inducers include barbiturates (eg, phenobarbital), bosentan, carbamazepine, efavirenz, phenytoin, primidone, rifampin, and possibly also felbamate, griseofulvin, oxcarbazepine, rifabutin, St. John’s wort, and topiramate.
Many HIV / AIDS and HCV antivirals, such as boceprevir, nelfinavir, nevirapine, ritonavir, and telaprevir, can increase or decrease desogestrel and etonogestrel levels.
CYP3A4 inhibitors including strong inhibitors such as clarithromycin, itraconazole, and ketoconazole and moderate inhibitors such as diltiazem, erythromycin, and fluconazole can increase desogestrel and etonogestrel levels.
Hormonal contraceptives can interfere with the metabolism of other drugs, resulting in increased levels (eg Cyclosporine) or decreased levels (eg Lamotrigine).
