Understanding a Key Progestin: What Does Dienogest Do to the Body?

October 10, 2025 •

4 min read

Endometriosis affects up to 10% of women of reproductive age, often causing debilitating pain [1.3.3]. One primary medical treatment is a synthetic progestin, but what does dienogest do to the body to alleviate these symptoms and what are its other uses?

Quick Summary

Dienogest is a synthetic progestin that primarily treats endometriosis by creating a hypoestrogenic environment that shrinks lesions and reduces pain. It also functions as a contraceptive when combined with estrogen.

Key Points

Primary Function: Dienogest is a synthetic progestin that primarily treats endometriosis and, when combined with estrogen, acts as an oral contraceptive [1.2.1].
Endometriosis Treatment: It reduces endometriosis-associated pain and lesions by suppressing estrogen, inhibiting cell proliferation, and reducing inflammation and blood vessel growth (angiogenesis) [1.3.2, 1.3.1].
Mechanism of Action: Dienogest selectively binds to progesterone receptors, creating a hypoestrogenic state that causes the atrophy (shrinking) of ectopic endometrial tissue [1.2.4, 1.3.2].
Contraception: In birth control pills, dienogest's main function is to inhibit ovulation, preventing pregnancy [1.3.2, 1.5.1].
Side Effects: The most common side effects include menstrual changes (spotting, bleeding), headache, breast discomfort, and mood changes. These are often mild and decrease over time [1.4.4, 1.4.5].
Unique Properties: Unlike some other progestins, dienogest has antiandrogenic properties, which can help with symptoms like acne, and it has negligible androgenic side effects [1.3.2, 1.6.3].
Bone Density: Long-term use can be associated with a small, and often partially reversible, decrease in bone mineral density [1.2.5].

Introduction to Dienogest

Dienogest is an oral, fourth-generation synthetic progestin, a type of hormone medication [1.2.1, 1.3.3]. It is a derivative of 19-nortestosterone and is unique because it combines the properties of both progesterone and 19-norprogestin derivatives [1.2.1, 1.2.3]. This unique pharmacological profile allows it to be highly selective for the progesterone receptor, exerting strong progestational effects while also having beneficial antiandrogenic properties [1.3.2, 1.6.4]. It is primarily prescribed as a monotherapy for the treatment of endometriosis and is also used in combination with an estrogen (like ethinylestradiol or estradiol valerate) as an oral contraceptive [1.2.1, 1.5.7].

How Dienogest Works in the Body

The primary way dienogest works is by binding with high selectivity to progesterone receptors in various tissues, most notably the uterus [1.2.4, 1.2.8]. This action leads to several key effects on the body, depending on its use.

For Endometriosis

Endometriosis is an estrogen-dependent condition where tissue similar to the lining of the uterus grows outside the uterus, causing inflammation, pain, and endometriotic lesions [1.3.1]. Dienogest treats this condition through multiple mechanisms:

Hormone Suppression: Dienogest moderately inhibits the secretion of gonadotropins from the pituitary gland. This leads to a modest reduction in the body's own production of estradiol (a type of estrogen) [1.3.2].
Creating a Hypoestrogenic Environment: By reducing estrogen levels and exerting strong progestogenic effects, dienogest creates a local hypoestrogenic (low estrogen) and hypergestagenic (high progestogen) environment [1.3.2]. This state is unfavorable for the growth of estrogen-dependent endometriotic tissue.
Decidualization and Atrophy: The hormonal environment created by dienogest causes the ectopic endometrial tissue to undergo a process called decidualization, which is then followed by the atrophy (shrinking) of the lesions [1.3.2].
Antiproliferative and Anti-inflammatory Effects: Dienogest directly inhibits the proliferation of endometrial cells and modulates the production of prostaglandins and inflammatory cytokines, thereby reducing the inflammation associated with endometriosis [1.2.3, 1.2.5].
Antiangiogenic Properties: It also inhibits angiogenesis, which is the formation of new blood vessels that are essential for the growth and survival of endometriotic implants [1.3.2, 1.3.1].

Studies have shown that a 2 mg daily dose of dienogest is effective at reducing endometriosis-associated pelvic pain and the size of lesions, with an efficacy comparable to that of GnRH agonists but with fewer hypoestrogenic side effects like severe bone density loss [1.3.2, 1.3.6].

For Contraception

Dienogest is also a component of several combined oral contraceptive pills [1.5.4]. Its contraceptive effect stems from several actions:

Inhibition of Ovulation: At a daily dose of 2 mg, dienogest effectively suppresses ovulation, preventing the release of an egg from the ovary [1.3.2]. This is its main contraceptive mechanism.
Changes to Cervical Mucus and Uterine Lining: Like other progestins used for birth control, it also causes changes in the cervical mucus and the uterine lining, making it more difficult for sperm to reach the uterus and for a fertilized egg to implant [1.5.6].

It's important to note that when dienogest is prescribed as a monotherapy (e.g., brand name Visanne) for endometriosis, it is not officially classified as a contraceptive, and the use of non-hormonal barrier methods like condoms is recommended [1.3.2, 1.5.5].

Common and Serious Side Effects

While generally well-tolerated, dienogest can cause side effects [1.4.4]. Many are typical for progestogens.

Most Common Side Effects:

Menstrual Irregularities: This is the most frequent side effect, especially in the first few months of treatment. It can include spotting, breakthrough bleeding, or amenorrhea (absence of a period) [1.3.3, 1.4.5]. These changes usually decrease with continued use [1.2.5].
Headache: Reported in up to 9% of users in some studies [1.4.4].
Breast Discomfort: Includes tenderness, pain, or swelling [1.4.4].
Mood Changes: Depressed mood and irritability have been reported [1.4.2, 1.4.4].
Acne: Can occur in some individuals [1.4.4].
Weight Gain: This is another commonly reported side effect [1.4.2].

Less Common but Serious Side Effects:

Blood Clots: Like other hormonal medications, there is a risk of venous thromboembolism, stroke, or heart attack, especially in women with other risk factors [1.4.1, 1.5.6].
Bone Mineral Density (BMD) Loss: Long-term use can be associated with a small decrease in BMD, particularly in adolescents [1.4.2, 1.2.5]. The clinical significance of this decrease is still under investigation, and some recovery of BMD is seen after stopping treatment [1.2.5].
Liver Problems: Though rare, signs like yellowing skin or eyes or severe abdominal pain require immediate medical attention [1.4.6].

Comparison with Other Progestins

Dienogest has a distinct profile compared to other progestins used in gynecology.


Feature	Dienogest	Norethisterone Acetate (NETA)	Medroxyprogesterone Acetate (MPA)
Generation	Fourth-generation [1.3.3]	First-generation	First-generation
Antiandrogenic Effect	Yes, beneficial for symptoms like acne [1.3.2]	No, has some androgenic activity [1.6.5]	Yes, has androgenic activity [1.6.5]
Receptor Specificity	Highly selective for progesterone receptor [1.2.4, 1.6.5]	Also binds to androgen and estrogen receptors [1.6.5]	Also binds to androgen and glucocorticoid receptors [1.6.5]
Endometriosis Efficacy	Equivalent to GnRH agonists for pain relief [1.3.2]	Used for endometriosis, but may require higher doses	Used for endometriosis pain
Endometrial Thinning	Produces a better rate of regression than NETA in some studies [1.6.6]	Effective, but may have more persistence in some cases [1.6.6]	Effective endometrial thinning agent

Conclusion

Dienogest works in the body primarily by acting on progesterone receptors to create a low-estrogen, high-progestin state. This makes it a highly effective treatment for endometriosis by causing the atrophy of painful lesions and reducing inflammation [1.3.2]. When combined with estrogen, it acts as a reliable contraceptive by inhibiting ovulation [1.5.1]. Its unique profile, including its antiandrogenic properties and high receptor selectivity, distinguishes it from other progestins [1.6.5]. While it is associated with side effects like irregular bleeding and headaches, it is generally considered a well-tolerated and effective long-term treatment option for managing chronic conditions like endometriosis [1.4.4, 1.2.5].

For more information on the efficacy and safety of dienogest, you can refer to the National Institutes of Health (NIH) literature, such as this review on its long-term use: https://pmc.ncbi.nlm.nih.gov/articles/PMC3140813/

Frequently Asked Questions

Dienogest is a synthetic hormone (progestin) that primarily acts on progesterone receptors. This helps treat endometriosis by reducing estrogen levels and shrinking uterine-like tissue that has grown outside the uterus. It also stops ovulation, which is how it works as a contraceptive [1.3.2, 1.5.1].

Dienogest often causes changes in menstrual bleeding patterns. Many users experience irregular bleeding or spotting, especially initially, while some may experience amenorrhea (the absence of a period) over time. These changes are expected and tend to decrease with continued use [1.2.5, 1.3.3].

Although a 2 mg daily dose of dienogest inhibits ovulation in most women, when prescribed alone for endometriosis (e.g., Visanne), it is not officially approved as a contraceptive. Therefore, it is recommended to use a non-hormonal barrier method of birth control (like condoms) to prevent pregnancy [1.3.2, 1.5.5].

Dienogest reduces pain by creating a low-estrogen environment, which causes endometriotic lesions to shrink (atrophy). It also has anti-inflammatory and anti-angiogenic (inhibits new blood vessel growth) effects, which further helps to alleviate pain [1.3.1, 1.3.2].

The most frequently reported side effects are changes in bleeding patterns (spotting, irregular bleeding), headaches, breast discomfort, depressed mood, and acne. These are generally mild to moderate and often lessen over time [1.4.4].

Not exactly. Dienogest is the progestin component in some combined oral contraceptives (like Natazia or Qlaira), where it's paired with an estrogen [1.5.4]. When used alone in a 2mg dose (Visanne), its primary indication is the treatment of endometriosis, not contraception [1.5.7].

Dienogest has a relatively short elimination half-life of about 9-10 hours, meaning it is cleared from the body fairly quickly. Ovarian activity typically resumes rapidly after treatment is stopped [1.2.1, 1.3.2].