Usage
- Dienogest + Ethinyl Estradiol is primarily prescribed for contraception (preventing pregnancy). It is also used to treat heavy menstrual bleeding (menorrhagia) and moderate acne in women who desire oral contraception.
- Pharmacological Classification: Combined oral contraceptive (COC), hormonal contraceptive.
- Mechanism of Action: This combination primarily works by suppressing ovulation (release of eggs from the ovaries). The progestin component (dienogest) thickens cervical mucus, hindering sperm penetration, and alters the uterine lining, making implantation less likely. Ethinyl estradiol, a synthetic estrogen, stabilizes the uterine lining and contributes to cycle control.
Alternate Names
- Various generic names exist depending on the specific formulation and manufacturer.
- Brand Names: Natazia, Valette, and others depending on the region and formulation.
How It Works
- Pharmacodynamics: Dienogest, a progestin, exhibits antiandrogenic activity (blocks the effects of androgens) which contributes to its efficacy in treating acne. Ethinyl estradiol stabilizes the endometrium and helps regulate the menstrual cycle. The combined effect suppresses the hypothalamic-pituitary-ovarian axis, inhibiting ovulation.
- Pharmacokinetics: Both components are absorbed orally. Ethinyl estradiol undergoes hepatic metabolism (primarily by CYP3A4), while dienogest is metabolized by various pathways. Both are primarily eliminated via hepatic and renal routes. The quadriphasic formulation of estradiol valerate and dienogest (Natazia) has varying estrogen doses throughout the cycle. Dienogest has no glucocorticoid, anti-mineralocorticoid, or anti-estrogenic activity.
- Mode of Action: Dienogest binds to progesterone receptors, inhibiting ovulation and thickening cervical mucus. Ethinyl estradiol binds to estrogen receptors, influencing endometrial development and cycle regulation.
- Elimination Pathways: Primarily hepatic and renal excretion for both components. CYP3A4 plays a significant role in ethinyl estradiol metabolism.
Dosage
Standard Dosage
Adults:
- One tablet daily, taken orally at the same time each day, following the order on the blister pack (especially important for quadriphasic formulations like Natazia).
- Use backup contraception for the first 9 days.
- Do not skip or delay tablets by more than 12 hours.
Children:
- Not recommended for use before menarche (onset of menstruation). Use in adolescents should follow adult dosing guidelines but requires careful consideration of individual development and potential risks.
Special Cases:
- Elderly Patients: Not typically prescribed for post-menopausal women.
- Patients with Renal Impairment: Limited studies available; use with caution.
- Patients with Hepatic Dysfunction: Contraindicated in severe hepatic impairment. Use with caution in mild to moderate dysfunction.
- Patients with Comorbid Conditions: Use with caution in patients with controlled hypertension, diabetes, dyslipidemia, or history of gallbladder disease. Contraindicated in patients with uncontrolled hypertension, history of thromboembolic events, or hormone-sensitive cancers.
Clinical Use Cases
- The provided sources do not list dosages related to Intubation, Surgical Procedures, Mechanical Ventilation, Intensive Care Unit (ICU) Use, or Emergency Situations. Dienogest + Ethinyl Estradiol is a contraceptive and not indicated for these purposes.
Dosage Adjustments
- Dose adjustments are not typically made based on specific factors other than those listed in the Special Cases section. For interactions with certain medications, adjustments of the other medication might be needed.
Side Effects
Common Side Effects:
- Nausea, breast tenderness, headache, weight changes, mood changes, acne, irregular bleeding, vaginal discharge, changes in appetite, fatigue.
Rare but Serious Side Effects:
- Blood clots (deep vein thrombosis, pulmonary embolism, stroke), heart attack, liver problems (jaundice), high blood pressure, angioedema.
Long-Term Effects:
- Increased risk of certain cancers (breast, cervical) with long-term use has been associated with combined hormonal contraceptives in some studies, but the current evidence is not conclusive for this specific combination.
Adverse Drug Reactions (ADR):
- Thromboembolic events, hypersensitivity reactions (angioedema), significant changes in liver function tests, uncontrolled hypertension.
Contraindications
- History of or current thromboembolic disorders, stroke, heart disease, uncontrolled hypertension, hormone-sensitive cancers (breast, endometrial, cervical), liver tumors or disease, undiagnosed abnormal uterine bleeding, pregnancy, breastfeeding (generally not recommended), smokers over 35 years old.
Drug Interactions
- Several drug interactions can affect the efficacy of Dienogest + Ethinyl Estradiol or increase the risk of side effects.
- CYP450 Interactions: Ethinyl estradiol is metabolized by CYP3A4. Enzyme inducers (e.g., rifampicin, St. John’s wort) can decrease its effectiveness, while inhibitors (e.g., ketoconazole) can increase the risk of side effects.
- Interactions with:
- Certain antiepileptics (carbamazepine, phenytoin)
- Some antibiotics (rifampicin, rifabutin)
- Antifungals (griseofulvin)
- Anti-HIV drugs (nelfinavir, ritonavir)
- Lamotrigine (reduced seizure control).
- Other: Alcohol, grapefruit juice, potassium-sparing diuretics.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not assigned under the new FDA labeling system. Contraindicated in pregnancy. Discontinue if pregnancy occurs.
- Breastfeeding: Not recommended during breastfeeding. Ethinyl estradiol can be excreted in breast milk and may affect milk production. Alternative contraception is advised.
Drug Profile Summary
- Mechanism of Action: Suppresses ovulation, thickens cervical mucus, alters uterine lining.
- Side Effects: Nausea, breast tenderness, headache, irregular bleeding, serious thromboembolic events.
- Contraindications: Thromboembolic disorders, uncontrolled hypertension, hormone-sensitive cancers, liver disease, pregnancy.
- Drug Interactions: CYP3A4 inducers/inhibitors, certain antibiotics, antifungals, anti-HIV drugs.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy, not recommended during breastfeeding.
- Dosage: One tablet daily, at the same time, following blister pack order (for quadriphasic formulations).
- Monitoring Parameters: Blood pressure, liver function tests, signs of thromboembolic events.
Popular Combinations
- Dienogest + Ethinyl Estradiol is itself a combination product. There are no commonly recommended combinations with other drugs beyond what is necessary to manage side effects or co-existing conditions.
Precautions
- General Precautions: Assess medical history, including risk factors for thromboembolic events, liver disease, and hormone-sensitive cancers. Monitor blood pressure and liver function.
- Specific Populations: See Dosage - Special Cases and Pregnancy and Breastfeeding sections.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Dienogest + Ethinyl Estradiol?
A: One tablet daily, at the same time, following the order on the blister pack. Specific formulations may vary (e.g., quadriphasic formulations like Natazia).
Q2: How effective is Dienogest + Ethinyl Estradiol as contraception?
A: Highly effective when taken correctly. However, no contraceptive is 100% effective.
Q3: What are the most common side effects?
A: Nausea, breast tenderness, headache, breakthrough bleeding, mood changes.
Q4: Can this medication be used to treat acne in all women?
A: No. It should only be used to treat moderate acne in women who also choose oral contraception, and only after topical treatments or oral antibiotics have not worked.
Q5: What are the serious risks associated with Dienogest + Ethinyl Estradiol?
A: Blood clots (DVT, PE, stroke), heart attack, liver problems, high blood pressure.
Q6: What should a patient do if they miss a dose?
A: Take the missed dose as soon as remembered. If it is close to the time for the next dose, skip the missed dose and continue the regular schedule. Use backup contraception if more than 12 hours late.
Q7: Can Dienogest + Ethinyl Estradiol be used while breastfeeding?
A: Not generally recommended. Other forms of contraception are preferable during breastfeeding. Discuss with your doctor.
Q8: Does this pill protect against sexually transmitted infections (STIs)?
A: No. Dienogest + Ethinyl Estradiol does not protect against STIs. Consistent condom use is recommended for STI prevention.
Q9: Are there any drug interactions I should be aware of?
A: Yes. Certain medications, such as some antiepileptics and antibiotics, can interfere with the effectiveness. Consult your doctor regarding all concomitant medications, including over-the-counter drugs and herbal supplements.
Q10: What should I do if I experience any side effects?
A: Contact your doctor to discuss management strategies or if the side effects are severe or persistent.
