Usage
Cyproterone + Ethinyl Estradiol + Folic Acid is a hormonal medication primarily prescribed for the treatment of Polycystic Ovary Syndrome (PCOS) in women. It addresses symptoms such as acne, hirsutism (excessive hair growth), and irregular menstrual cycles. This combination is also effective in treating severe acne and hirsutism unrelated to PCOS. It acts as an oral contraceptive but should not be prescribed for contraception alone.
Pharmacological Classification: Hormonal contraceptive, anti-androgen.
Mechanism of Action: Cyproterone acetate is an anti-androgen that blocks the effects of male hormones (androgens). Ethinyl estradiol is a synthetic estrogen that regulates the menstrual cycle and enhances the effect of cyproterone. Folic acid is included to address potential folate deficiency induced by the hormonal components.
Alternate Names
No commonly used alternate names for this specific combination exist. Brand names may vary regionally.
Brand Names: Examples of Brand Names: Diane-35, Estelle-35, Harmoni-F (Brand names vary depending on the region, please consult local pharmaceutical resources for details).
How It Works
Pharmacodynamics: Cyproterone acetate competes with androgens for receptor binding, reducing androgenic effects like sebum production and hair growth. Ethinyl estradiol suppresses the release of gonadotropin-releasing hormone (GnRH), leading to decreased luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. This, in turn, suppresses ovulation. Ethinyl estradiol also potentiates cyproterone’s anti-androgenic action. Folic acid is essential for cell growth and division.
Pharmacokinetics:
- Absorption: Ethinyl estradiol and cyproterone acetate are readily absorbed after oral administration. Food may slightly delay absorption.
- Metabolism: Both ethinyl estradiol and cyproterone acetate are extensively metabolized in the liver, primarily by CYP enzymes, including CYP3A4.
- Elimination: Metabolites are excreted in urine and feces.
Receptor Binding: Cyproterone acetate binds to androgen receptors.
Enzyme Inhibition: Ethinyl estradiol can inhibit certain CYP enzymes involved in drug metabolism.
Elimination Pathways: Primarily hepatic metabolism followed by renal and biliary excretion of metabolites.
Dosage
Standard Dosage
Adults: One tablet daily for 21 consecutive days, starting on the first day of the menstrual cycle. This is followed by a 7-day pill-free interval, during which withdrawal bleeding occurs.
Children: This medication is not recommended for use in children.
Special Cases: Dosage adjustments are generally not recommended in special populations. Individualized assessment is crucial, and the drug should be used with caution in patients with:
- Elderly patients
- Renal impairment
- Hepatic dysfunction
- Comorbid conditions
Clinical Use Cases
This medication is not indicated for use in these specific clinical settings:
- Intubation
- Surgical procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) use
- Emergency Situations
Dosage Adjustments
Dose adjustments are generally not recommended, and this combined therapy is typically avoided in the presence of severe hepatic or renal impairment. Close monitoring is advised in such cases.
Side Effects
Common Side Effects:
Nausea, breast tenderness, headache, weight changes, mood swings, breakthrough bleeding, changes in libido, stomach pain.
Rare but Serious Side Effects:
Blood clots (deep vein thrombosis, pulmonary embolism, stroke), liver problems (jaundice, hepatitis), high blood pressure, heart attack, migraine with aura, gallbladder disease, allergic reactions.
Long-Term Effects:
Increased risk of certain cancers (breast, cervical) with long-term use.
Adverse Drug Reactions (ADR):
Any signs of blood clots or thromboembolic events, severe allergic reactions, jaundice, unexplained vaginal bleeding require immediate medical attention.
Contraindications
Current or past history of blood clots, breast or estrogen-dependent cancers, liver disease or tumors, unexplained vaginal bleeding, migraine with aura, pregnancy, hypersensitivity to any of the components.
Drug Interactions
Several drug interactions can occur, notably with:
- CYP inducers/inhibitors: Rifampicin, antiepileptic drugs (e.g. carbamazepine, phenytoin), HIV medications (e.g. ritonavir) may alter efficacy.
- Other medications: Certain antibiotics, St. John’s wort may reduce effectiveness; anticoagulants may be affected.
Pregnancy and Breastfeeding
Contraindicated in pregnancy. This medication can be excreted in breast milk and may have adverse effects on the nursing infant. Not recommended during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Anti-androgen, estrogenic, and folate supplementation.
- Side Effects: Nausea, breast tenderness, headache, weight gain, mood changes, rare but serious thromboembolic events.
- Contraindications: History of blood clots, breast/estrogen-dependent cancers, liver disease, pregnancy.
- Drug Interactions: CYP inducers/inhibitors, certain antibiotics, St. John’s wort.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: One tablet daily for 21 days followed by a 7-day break.
- Monitoring Parameters: Blood pressure, liver function tests, signs of thromboembolic events.
Popular Combinations
Not applicable. Avoid co-administration with other hormonal contraceptives.
Precautions
Detailed medical history including risk factors for blood clots, liver disease, and cancers is essential. Regular breast exams and monitoring for adverse effects are recommended. Lifestyle factors like smoking and alcohol consumption should be considered.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Cyproterone + Ethinyl Estradiol + Folic Acid?
A: One tablet daily for 21 consecutive days followed by a 7-day pill-free interval.
Q2: Can this combination be used solely for contraception?
A: While it provides contraceptive effects, it is primarily indicated for managing PCOS symptoms and shouldn’t be prescribed solely for birth control.
Q3: What are the major contraindications for this medication?
A: History of blood clots, breast/estrogen-dependent cancers, liver diseases, and pregnancy.
Q4: Are there any specific drug interactions to be aware of?
A: Yes, interactions exist with CYP450 inducers/inhibitors, certain antibiotics, and St. John’s Wort. It’s vital to review concomitant medications with patients.
Q5: Can this medicine be used during pregnancy or while breastfeeding?
A: No, it’s contraindicated in both pregnancy and breastfeeding.
Q6: What are the common side effects patients might experience?
A: Nausea, breast tenderness, headache, weight changes, mood fluctuations, and breakthrough bleeding are common side effects.
A: Signs of blood clots (leg pain, swelling, shortness of breath, chest pain), jaundice, severe allergic reactions, and unexplained vaginal bleeding should prompt immediate medical evaluation.
Q8: How should patients be monitored while on this medication?
A: Monitor blood pressure, liver function (with liver function tests as needed), and be vigilant for signs of thromboembolic events. Regular breast self-exams are also recommended.
Q9: How does folic acid interact with the other components of this medication?
A: Folic acid is included to supplement potential folate deficiency that can be induced by ethinyl estradiol and cyproterone acetate. Ethinyl estradiol in particular can interfere with folate metabolism.
