Generic Cyproterone Acetate And Ethinylestradiol (Cyproterone acetate and ethinylestradiol)

Introduction

Cyproterone acetate and ethinylestradiol is a combined oral contraceptive pill that contains the anti-androgen cyproterone acetate (2 mg) and the estrogen ethinylestradiol (.035 mg). The medication belongs to the class of combined hormonal contraceptives and is also indicated for androgen-dependent dermatologic conditions in women. It is manufactured by several licensed pharmaceutical companies and is available in a single-strength tablet (2/.035 mg). In addition to its contraceptive role, the combination is prescribed for severe acne, hirsutism, and, in some clinical settings, gender-affirming hormone therapy (off-label).

What is Cyproterone acetate and ethinylestradiol?

Cyproterone acetate and ethinylestradiol is the generic version of well-known medications, containing the active compound Cyproterone acetate and ethinylestradiol. Our online pharmacy provides this generic alternative as a cost-effective treatment option.

• Classification: Combined hormonal contraceptive (anti-androgen + synthetic estrogen).
• Development history: Cyproterone acetate was first synthesized in the s as a potent progesterone receptor agonist with anti-androgenic activity. Ethinylestradiol, a synthetic estradiol derivative, has been used in oral contraceptives since the early s. The two agents were combined to create a pill that suppresses ovulation while counteracting androgen excess.
• Manufacturers: Multiple European and Asian manufacturers produce the generic tablet; brand-name equivalents include Diane-35, Yasmin-C, and Dianette.

How Cyproterone acetate and ethinylestradiol Works

Cyproterone acetate binds to androgen receptors, blocking the action of endogenous testosterone and dihydrotestosterone (anti-androgen effect). It also exerts progestogenic activity, contributing to suppression of the hypothalamic-pituitary-gonadal axis. Ethinylestradiol activates estrogen receptors and provides negative feedback on luteinizing hormone (LH) and follicle-stimulating hormone (FSH), preventing follicular development and ovulation. The combined actions result in:

• Reliable inhibition of ovulation (contraceptive effect).
• Reduction of circulating free androgens, improving skin and hair outcomes in androgen-dependent conditions.

Pharmacokinetically, both compounds are absorbed rapidly after oral ingestion. Cyproterone acetate reaches peak plasma concentrations within 4 hours and has a half-life of approximately 30 hours, allowing once-daily dosing. Ethinylestradiol peaks in 1-2 hours and has a half-life of ~24 hours. Both are metabolised by hepatic CYP3A4 enzymes and excreted in urine and feces.

Conditions Treated with Cyproterone acetate and ethinylestradiol

• Contraception (primary indication). The combination reliably prevents pregnancy when taken correctly for every menstrual cycle.
• Severe acne vulgaris in women. By blocking androgen receptors, cyproterone acetate reduces sebum production and inflammatory lesions.
• Hirsutism (excessive facial/ body hair). Anti-androgenic activity diminishes hair growth in androgen-sensitive areas.

These indications are approved by the European Medicines Agency (EMA) and many national health agencies. The therapeutic benefit arises from simultaneous estrogen-mediated suppression of ovulation and androgen antagonism.

Off-Label and Investigational Uses of Cyproterone acetate and ethinylestradiol

• Gender-affirming hormone therapy for transgender women. Clinical series have reported that the combination reduces masculine secondary sexual characteristics and provides estrogenic support, although it is not approved for this purpose in most jurisdictions.
• Polycystic ovary syndrome (PCOS)-related hyperandrogenism. Some endocrinology guidelines cite combined anti-androgen-estrogen pills as an option when first-line agents (e.g., oral contraceptives without cyproterone) are insufficient.
• Premenstrual dysphoric disorder (PMDD). Small trials suggest improvement in mood symptoms, likely related to hormonal stabilization, but the indication remains investigational.

These applications have not received formal regulatory approval. Patients should discuss any off-label use with a qualified healthcare professional, and treatment must be monitored for safety.

Is Cyproterone acetate and ethinylestradiol the Right Medication for You?

• Suitable patients include:

  • Women of reproductive age seeking reliable oral contraception.
  • Individuals with clinically diagnosed severe acne or hirsutism unresponsive to topical therapies.
  • Patients without a history of estrogen-sensitive malignancy, thromboembolic disease, or uncontrolled hypertension.

• Clinical scenarios where it is particularly recommended:

  • Women requiring both contraception and anti-androgen therapy (e.g., acne-dominant patients).
  • Patients preferring a single-pill regimen that addresses multiple symptoms.

• Contraindications (examples):

  • Known or suspected pregnancy.
  • Active liver disease or cholestasis.
  • History of venous thromboembolism, stroke, or myocardial infarction.
  • Hormone-dependent neoplasms (e.g., breast cancer).
  • Smoking ≥15 cigarettes per day in women over 35 years of age.

Risks, Side Effects, and Interactions

Common

• Nausea or abdominal discomfort.
• Breast tenderness or enlargement.
• Headache, especially in the first few cycles.
• Weight fluctuation or mild fluid retention.
• Mood changes or mild depression.

Rare

• Elevated liver enzymes or cholestatic hepatitis.
• Decreased libido or sexual dysfunction.
• Dysmenorrhea or breakthrough bleeding.

Serious

• Venous thromboembolism (deep-vein thrombosis, pulmonary embolism).
• Arterial thrombosis (stroke, myocardial infarction).
• Severe hepatic impairment or liver failure.
• Meningioma (rare tumor linked to long-term high-dose cyproterone).
• Severe allergic reactions (anaphylaxis).

Drug-Drug Interactions

• Enzyme inducers (e.g., rifampicin, carbamazepine, St. John’s wort) can lower plasma concentrations, reducing efficacy.
• CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase drug levels, raising the risk of side effects.
• Anticoagulants (warfarin) - estrogen component can enhance anticoagulant effect, requiring closer INR monitoring.
• Photosensitising agents (tetracyclines) - may increase risk of photosensitivity reactions.

Drug-Food Interactions

• Grapefruit juice can inhibit CYP3A4 and modestly increase drug exposure; occasional consumption is unlikely to be clinically significant but should be discussed with a provider.

Use: Dosing, Missed Dose, Overdose

• Standard dosing: One tablet (2 mg/.035 mg) taken daily at the same time, preferably with food to minimise gastrointestinal upset. A 21-day active regimen followed by a 7-day hormone-free interval is typical for contraception.
• Missed dose: If a tablet is missed by less than 12 hours, take it as soon as remembered and continue with the next scheduled dose. If more than 12 hours have passed, take the missed tablet immediately, discard any subsequent tablets for that day, and use a backup non-hormonal contraceptive (e.g., condoms) for the next 7 days.
• Overdose: Acute overdose is unlikely to be life- threatening. Patients should seek immediate medical attention, monitoring for nausea, vomiting, and signs of estrogen toxicity (e.g., hypertension). Supportive care is the mainstay of management.
• Precautions: Avoid alcohol excess, as it may increase liver strain. Do not operate heavy machinery if dizziness or severe headache occurs.

FAQ

• **Can I travel internationally with this medication? Yes. Keep the tablets in their original packaging, carry a copy of the prescription (if required by local law), and store them at room temperature away from direct sunlight.

• **Does the pill affect hormonal birth-control testing for sports? Yes. The synthetic estrogen can be detected in anti-doping urine screens; athletes should disclose use to the relevant governing body.

• **What does the tablet look like? Generic 2/.035 mg tablets are usually round, white or off-white, and may be scored for ease of splitting; the exact imprint varies by manufacturer.

• **Are there any inactive ingredients I should be aware of? Common excipients include lactose, magnesium stearate, and microcrystalline cellulose. Patients with lactose intolerance should verify the specific formulation.

• **Is the medication safe for smokers? Smoking ≥15 cigarettes per day in women over 35 substantially increases the risk of thromboembolic events; such patients should consider non-estrogenic contraceptive methods.

• **How does storage in hot climates affect the pill? High temperatures may degrade the active ingredients. Store the medication below 30 °C (86 °F) and avoid exposure to direct sunlight, especially in tropical regions.

• **Can the pill be taken with grapefruit juice? Grapefruit can modestly increase ethinylestradiol levels. Occasional consumption is unlikely to cause problems, but regular large amounts should be discussed with a clinician.

• **What monitoring is required for long-term use? Baseline blood pressure, liver function tests, and lipid profile are recommended annually, with more frequent checks if risk factors are present.

• **Is there a difference between the generic and brand-name products? Both contain the same active ingredients and are bioequivalent; differences may lie in inactive fillers, tablet appearance, or cost.

• **Can the pill be used while breastfeeding? It is contraindicated during breastfeeding because ethinylestradiol can reduce milk production and cyproterone acetate may enter breast milk. Alternative contraceptives are advised.

Glossary

Anti-androgen

A substance that blocks the effects of male hormones (androgens) at their receptor sites, reducing symptoms such as excess hair growth or acne.

Contraceptive failure rate

The percentage of women who become pregnant while using a particular birth-control method correctly for one year; combined pills have a typical-use failure rate of about 7 %.

Venous thromboembolism (VTE)

A condition in which a blood clot forms in a vein (deep-vein thrombosis) and may travel to the lungs (pulmonary embolism), a serious complication associated with estrogen-containing contraceptives.

Buying Cyproterone acetate and ethinylestradiol from Our Online pharmacy

Cyproterone acetate and ethinylestradiol can be purchased from our online pharmacy. We source the generic tablet from licensed, internationally accredited manufacturers, ensuring that each batch meets stringent quality standards. Our pricing is close to the manufacturer’s cost, providing a more affordable alternative to brand-name products.

Patients who encounter limited access through local pharmacies or whose insurance does not cover this medication find a reliable solution with us. Orders are processed discreetly, packaged in unmarked envelopes, and shipped with tracking-typically within 7 days for express service or around 3 weeks for standard airmail. As a pharmacy broker service, we collaborate with overseas licensed pharmacies, allowing us to offer a broader selection of medicines while maintaining strict verification and privacy safeguards.

Disclaimer

The information presented about Cyproterone acetate and ethinylestradiol is intended for general education only and does not substitute professional medical advice. All therapeutic decisions, including those involving off-label applications, should be made under the guidance of a qualified healthcare provider. Readers are presumed to be competent adults capable of evaluating health-related information responsibly. Our online pharmacy makes this medication available for individuals who may have restricted access through conventional pharmacies or insurance plans and who are seeking cost-effective generic alternatives. Before initiating, altering, or stopping any medication, please consult a qualified medical professional.