Usage
Dienogest is primarily prescribed for the treatment of endometriosis, a condition characterized by the presence of endometrial-like tissue outside the uterus. It’s classified as a progestin, a synthetic form of progesterone. Dienogest works by suppressing estrogen production, inhibiting endometrial tissue growth and reducing inflammation, thus alleviating endometriosis-associated pain and other symptoms. It is also prescribed for heavy menstrual bleeding in women without any diagnosed uterine conditions.
Alternate Names
Dienogest is also known as Visanne (a popular brand name), Dinogest, or DIENOGEST 2 mg DYNA.
How It Works
Pharmacodynamics: Dienogest exerts its therapeutic effects primarily through progestogenic actions. By binding to progesterone receptors, it counteracts estrogen’s effects on endometrial tissue, reducing its growth and minimizing inflammation. This leads to a reduction in endometriosis-related pain and symptoms. While Dienogest primarily inhibits ovulation, it’s not classified as a contraceptive.
Pharmacokinetics:
- Absorption: Orally administered Dienogest is rapidly and almost completely absorbed, reaching peak serum concentration (around 47 ng/mL) approximately 1.5 hours post-ingestion. Bioavailability is around 91%.
- Distribution: Dienogest binds to serum albumin but doesn’t interact with sex hormone-binding globulin (SHBG) or corticoid-binding globulin (CBG). About 10% exists as free steroid, while 90% is non-specifically bound to albumin. The apparent volume of distribution is 40 L.
- Metabolism: Dienogest is completely metabolized, predominantly by the cytochrome P450 (CYP) 3A4 enzyme system, through various metabolic pathways including hydroxylation, glucuronidation and sulfation.
- Elimination: Dienogest and its metabolites are primarily excreted via urine and feces.
Dosage
Standard Dosage
Adults:
The recommended dosage is 2 mg orally once daily, taken continuously without interruption, irrespective of menstrual bleeding. Ideally, the tablet should be taken at the same time each day, with some liquid if needed. Continue taking the tablets even during menstruation. Upon finishing a pack, start the next one immediately without any break.
Children (Post-Menarche):
For adolescents (12-18 years) with endometriosis-associated pelvic pain, the dosage is the same as for adults: 2 mg orally once daily, taken continuously. However, Dienogest has not been tested for periods exceeding 12 months in adolescents. BMD monitoring is recommended. The drug is not indicated for children prior to menarche.
Special Cases:
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Elderly Patients: There’s no specific indication for Dienogest use in the elderly population.
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Patients with Renal Impairment: No dosage adjustment is required for patients with renal impairment.
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Patients with Hepatic Dysfunction: Dienogest is contraindicated in patients with current or past severe liver disease.
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Patients with Comorbid Conditions: Use with caution in patients with diabetes, cardiovascular disease, history of thromboembolism, migraine with aura, and other conditions mentioned in the contraindications section.
Clinical Use Cases
Dienogest is not indicated for use in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary indication is the management of endometriosis.
Dosage Adjustments
No specific dosage adjustments are routinely recommended beyond those outlined for hepatic/renal impairment, elderly, and pediatric patients.
Side Effects
Common Side Effects:
- Headache
- Menstrual irregularities (changes in bleeding pattern, amenorrhea, intermenstrual bleeding/spotting)
- Breast tenderness/pain
- Acne
- Mood changes (depression, anxiety)
- Weight changes
- Nausea, vomiting, abdominal pain
- Hot flushes
Rare but Serious Side Effects:
- Venous thromboembolism (VTE), including deep vein thrombosis and pulmonary embolism
- Arterial thromboembolic events (e.g., stroke, myocardial infarction)
- Liver dysfunction (jaundice, elevated liver enzymes)
- Allergic reactions
- Hypertension
- Hypertriglyceridemia
- Decreased bone mineral density (BMD), especially in adolescents
Long-Term Effects:
- Potential for decreased bone mineral density with prolonged use, particularly in adolescents
- Unknown long-term effects on bone health and osteoporosis risk
Adverse Drug Reactions (ADR):
Any signs of thromboembolic events, liver dysfunction, allergic reactions, or significant changes in mood require prompt medical attention.
Contraindications
- Pregnancy and lactation
- Active venous thromboembolic disorder
- History of arterial or cardiovascular disease (e.g., myocardial infarction, stroke)
- Diabetes mellitus with vascular involvement
- Severe hepatic disease or liver tumors
- Known or suspected sex hormone-dependent malignancies
- Undiagnosed vaginal bleeding
- Ocular lesions related to ophthalmic vascular disease (e.g., vision loss)
- Migraine with aura
Drug Interactions
- Hormonal contraceptives: Dienogest can reduce the efficacy of hormonal birth control. Non-hormonal contraception is recommended.
- CYP3A4 inducers (e.g., rifampicin, carbamazepine, phenytoin, St. John’s Wort): Can decrease Dienogest levels, reducing its effectiveness.
- CYP3A4 inhibitors (e.g., azole antifungals, some macrolides, grapefruit juice): Can increase Dienogest levels, potentially increasing the risk of side effects.
- Some medications like bosentan, dexamethasone, nafcillin and tranexamic acid may have serious interactions with dienogest.
Pregnancy and Breastfeeding
Dienogest is contraindicated during pregnancy and breastfeeding. It’s crucial to rule out pregnancy before starting treatment. If pregnancy occurs during treatment, discontinue immediately. Dienogest is excreted in breast milk and could have adverse effects on the nursing infant.
Drug Profile Summary
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Mechanism of Action: Progestogenic; suppresses estrogen, inhibits endometrial growth, and reduces inflammation.
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Side Effects: Headache, menstrual changes, breast tenderness, acne, mood changes, weight changes, nausea, VTE risk.
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Contraindications: Pregnancy, lactation, VTE, cardiovascular disease, liver disease, hormone-dependent cancers, undiagnosed vaginal bleeding.
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Drug Interactions: Hormonal contraceptives, CYP3A4 inducers/inhibitors.
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Pregnancy & Breastfeeding: Contraindicated.
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Dosage: 2 mg orally once daily continuously.
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Monitoring Parameters: Menstrual bleeding patterns, mood changes, signs of VTE, liver function tests (especially in high-risk patients), BMD in adolescents.
Popular Combinations
Dienogest is typically used as monotherapy and not in combination with other medications for endometriosis treatment. Using non-hormonal contraceptive methods concomitantly is common when contraception is needed.
Precautions
- Rule out pregnancy before starting treatment.
- Evaluate for pre-existing medical conditions (VTE risk factors, cardiovascular disease, liver disease, etc.).
- Monitor for changes in menstrual bleeding, mood, signs of VTE.
- Monitor BMD in adolescents.
- Patients with risk factors for osteoporosis should be carefully evaluated before considering long-term treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Dienogest?
A: 2 mg orally once daily, taken continuously regardless of menstrual bleeding.
Q2: How does Dienogest work in endometriosis?
A: By suppressing estrogen, inhibiting endometrial tissue growth outside the uterus, and reducing inflammation.
Q3: Can Dienogest be used as a contraceptive?
A: No, while it inhibits ovulation in most patients, it’s not a reliable contraceptive. Non-hormonal methods are recommended if contraception is desired.
Q4: What are the common side effects of Dienogest?
A: Headache, menstrual irregularities, breast tenderness, acne, mood changes, and weight changes.
Q5: Is Dienogest safe during pregnancy?
A: No, Dienogest is contraindicated in pregnancy and should be discontinued if pregnancy occurs.
Q6: What should be done if a dose of Dienogest is missed?
A: Take the missed dose as soon as remembered, unless it is close to the next scheduled dose. Do not double the dose.
Q7: Are there any drug interactions with Dienogest?
A: Yes, Dienogest interacts with CYP3A4 inducers and inhibitors, and hormonal contraceptives.
Q8: Can Dienogest be used in adolescents?
A: Yes, in adolescents (12-18 years post-menarche) for endometriosis-associated pain, the dosage is the same as for adults (2 mg once daily). BMD monitoring is recommended.
Q9: What are the long-term effects of Dienogest use?
A: One potential long-term effect is decreased bone mineral density, especially in adolescents. Long-term effects on bone health are unknown.
Q10: Can Dienogest be used in patients with liver problems?
A: No, Dienogest is contraindicated in patients with severe liver disease. Caution is advised in patients with any history of liver problems.
