What is Dienogest (progestin) Oral Tablet 2 mg?

What is Dienogest Oral Tablet 2 mg?

Dienogest 2 mg is a selective oral progestin medication primarily indicated for the treatment of endometriosis, with additional applications in hormone replacement therapy for premature ovarian insufficiency and as a progestin component in combined oral contraceptives. 1

Primary Indication: Endometriosis Treatment

Dienogest functions as a highly selective progesterone receptor agonist with unique pharmacological properties that make it particularly effective for endometriosis management 1:

• Mechanism of action: Exhibits strong progestational effects with moderate antigonadotrophic activity, antiproliferative effects on endometrial tissue, and anti-inflammatory properties in endometriotic lesions 1, 2
• Receptor selectivity: Has 10% the affinity of progesterone for progesterone receptors but lacks androgenic, glucocorticoid, or mineralocorticoid activity 1, 2
• Hormonal effects: Moderately suppresses estradiol levels (does not reduce to zero like GnRH agonists), maintaining some beneficial estrogen effects while treating endometriosis 1, 2

Clinical Efficacy Evidence

Pain reduction: In randomized trials, dienogest 2 mg daily significantly reduced pelvic pain compared to placebo in patients with confirmed endometriosis 1:

• A large Korean cohort study (3,356 patients) demonstrated mean visual analogue scale (VAS) pain reduction of -28.19 ± 28.39 mm from baseline (P < 0.0001) 3
• Non-inferior to depot leuprorelin for pelvic pain reduction over 16-24 weeks 1
• Sustained efficacy demonstrated during long-term treatment exceeding 1 year 1

Pharmacokinetic Properties

Dienogest has favorable pharmacokinetics for once-daily dosing 1, 2:

• Oral bioavailability: Greater than 90% 2
• Half-life: Approximately 10 hours, preventing drug accumulation 2
• Protein binding: Lacks affinity for sex hormone-binding globulin (SHBG), which enhances its antiandrogenic activity compared to other 19-nortestosterone derivatives 2

Safety and Tolerability Profile

Bleeding patterns: The most common adverse effect is abnormal uterine bleeding, reported in 4.14% of patients as an adverse drug reaction 3:

• Most bleeding events are spotting or breakthrough bleeding that decrease with continued treatment 1, 4
• Amenorrhea rates increase with treatment duration: 29.63% at 3 months, 41.25% at 6 months, 46.26% at 12 months, and 53.20% beyond 12 months 3
• Bleeding irregularities are generally well-tolerated with few discontinuations 1

Other adverse effects reported in the large Korean cohort study 3:

• Weight gain: 2.57% of patients
• Headache: 1.22% of patients
• Overall adverse drug reaction incidence: 13.27%

Metabolic and cardiovascular safety: Dienogest demonstrates no significant effects on metabolic or cardiovascular systems, distinguishing it from other 19-nortestosterone derivatives 2

Hypoestrogenic effects: Fewer hypoestrogenic side effects compared to GnRH agonists, as dienogest maintains some circulating estradiol levels 1, 2

Use in Hormone Replacement Therapy

Dienogest serves as a progestin option in hormone replacement regimens for premature ovarian insufficiency 5:

• Continuous combined regimen: Tablets containing 1-2 mg of 17β-estradiol and 2 mg of dienogest administered continuously without interruptions when avoiding withdrawal bleeding is required 5
• Alternative to dydrogesterone: Can be used as a 5 mg dydrogesterone alternative in continuous hormone replacement protocols 5

Use in Combined Oral Contraceptives

Dienogest represents a fourth-generation progestin designed with anti-androgenic properties 5:

• Combined with ethinyl estradiol or estradiol valerate in various contraceptive formulations 2
• Provides high endometrial stability, resulting in stable menstrual cycles 2
• The American Academy of Dermatology notes dienogest-containing contraceptives as options for women requiring hormonal contraception 6

Important Clinical Considerations

Contraceptive effect uncertainty: No studies have definitively established dienogest 2 mg monotherapy as providing reliable contraception, so barrier methods should be recommended concurrently when used for endometriosis treatment 7

Cost considerations: Dienogest therapy costs more than other available progestins and combined oral contraceptives, which may limit accessibility for long-term daily use 7

Dosing: The standard therapeutic dose for endometriosis is 2 mg once daily, taken continuously 1, 3