Generic Cyproterone Acetate And Ethinylestradiol ( Cyproterone acetate and ethinylestradiol )

Buy Generic Cyproterone Acetate And Ethinylestradiol (Cyproterone acetate and ethinylestradiol) without prescription in Canada

In our Canadian pharmacy, you can buy Cyproterone Acetate / Ethinylestradiol without a prescription, with delivery across Canada within 5‑14 days. Discreet and anonymous packaging.

This combination product contains cyproterone acetate, a potent anti‑androgen progestin, and ethinylestradiol, an estrogen. It is primarily used for the treatment of severe, treatment‑resistant acne and hirsutism (excessive hair growth) in women of childbearing age, and it simultaneously provides effective contraception. Cyproterone acetate works by blocking androgen receptors in the skin and reducing the production of androgens by the ovaries, while ethinylestradiol increases sex‑hormone‑binding globulin (SHBG), which lowers free testosterone levels. Together they address the hormonal imbalance that drives androgen‑dependent skin conditions.

Usual adult dose: One tablet is taken orally once daily, at approximately the same time each day, for 21 consecutive days, followed by a 7‑day tablet‑free interval during which withdrawal bleeding usually occurs. Each active tablet contains 2 mg of cyproterone acetate and 0.035 mg of ethinylestradiol. The next pack is started on the day after the tablet‑free interval, regardless of whether bleeding has stopped. Contraceptive protection is maintained throughout the cycle provided tablets are taken correctly. For acne and hirsutism, treatment is usually continued for several months, and should be stopped 3 to 4 cycles after the condition has resolved. If used for contraception alone, this product is not first‑line because of its higher thromboembolic risk; its use is restricted to women with proven androgen‑dependent conditions.

Dosage form: Oral tablets, each containing cyproterone acetate 2 mg and ethinylestradiol 0.035 mg, supplied in 21‑day blister packs.

Onset of action: Contraceptive protection begins immediately if the first tablet is taken on the first day of menstrual bleeding (Day 1 start). For acne, improvement is typically seen after 3 to 6 cycles of regular use, with maximum benefit often achieved after 6 to 12 months. Hirsutism may take 9 to 12 months to respond noticeably.

Duration of action: Contraceptive protection is maintained throughout the 28‑day cycle. The anti‑androgenic effects persist with continued use and gradually diminish after discontinuation, with acne and hirsutism often returning over subsequent months.

Alcohol recommendation: Moderate alcohol consumption does not directly interfere with the contraceptive action, but excessive drinking may increase the risk of vomiting or severe diarrhoea, which can impair tablet absorption. Alcohol should be limited, and a backup contraceptive method should be considered if vomiting occurs within 3‑4 hours of taking an active tablet.

Most common side effects: Nausea, breast tenderness, headache, mood changes, weight changes, and irregular uterine bleeding (especially in the first few months). Cyproterone acetate can cause fatigue, reduced libido, and, rarely, liver dysfunction. The most serious risk is venous thromboembolism (VTE), which is higher than with levonorgestrel‑containing pills and is the reason this product is not first‑line for contraception alone. Rare but serious side effects include hepatotoxicity and benign liver tumours, which have been associated with the cyproterone component at higher doses. This product is no longer approved in Canada due to its VTE risk but may be imported for personal use under a physician’s supervision.

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General Information about Cyproterone Acetate / Ethinylestradiol

• INN (International Nonproprietary Name): Cyproterone Acetate and Ethinylestradiol
• Brand names available in Canada: This combination is not marketed in Canada. The original brand name Diane‑35® (Bayer Inc.) was withdrawn from the Canadian market in 2003 due to concerns about an increased risk of venous thromboembolism. The product is, however, widely available internationally under brand names such as Diane‑35®, Dianette®, and others. Our pharmacy supplies internationally sourced tablets through the international supply chain for personal importation.
• ATC code: G03HB01 (antiandrogens and estrogens; cyproterone and estrogen).
• Dosage forms and strengths: Oral tablets: 2 mg cyproterone acetate / 0.035 mg ethinylestradiol. Supplied in 21‑day blister packs.
• Manufacturers in Canada: None. The product is not manufactured in Canada. It is manufactured internationally by Bayer AG and various generic pharmaceutical companies. Our pharmacy obtains it through the international supply chain for personal use.
• Registration status in Canada: Not marketed. Diane‑35 was previously approved by Health Canada but was withdrawn from the market in 2003. No subsequent re‑approval has been granted. The active combination is available internationally and may be imported under a valid prescription through the Health Canada Special Access Programme or for personal use.
• OTC / Rx classification: Prescription only (Rx). A valid prescription from a licensed Canadian healthcare professional is required for personal importation.

Mechanism of Action and Pharmacology

Cyproterone acetate is a steroidal anti‑androgen that competes with dihydrotestosterone (DHT) and testosterone for binding to androgen receptors in target tissues, including the sebaceous glands and hair follicles. By blocking these receptors, it reduces sebum production and inhibits the androgen‑dependent growth of hair. It also has a progestational action that suppresses ovarian androgen synthesis, and it inhibits the secretion of gonadotropins (LH and FSH) from the pituitary, which reduces ovarian production of testosterone and androstenedione. Ethinylestradiol is a synthetic estrogen that stimulates hepatic production of sex‑hormone‑binding globulin (SHBG). Elevated SHBG binds free testosterone, reducing the biologically active fraction and further diminishing androgenic stimulation. Ethinylestradiol also stabilises the endometrium, provides cycle control, and contributes to the contraceptive effect by inhibiting ovulation. The combination therefore acts synergistically: the cyproterone acetate blocks the androgen receptor and suppresses androgen production, while the ethinylestradiol increases androgen binding to SHBG and ensures reliable ovulation inhibition. The contraceptive efficacy of this formulation is high, comparable to other combined oral contraceptives. After oral administration, both components are rapidly absorbed, with peak plasma levels reached within 1–2 hours. Cyproterone acetate has a long terminal half‑life of approximately 1.6–4.3 days due to accumulation in adipose tissue, which is why it can have therapeutic effects for weeks after discontinuation. Ethinylestradiol has a half‑life of approximately 10–20 hours. Both are metabolised in the liver and excreted in the urine and faeces.

Indications

• Treatment of androgen‑dependent conditions in women of reproductive age, specifically severe acne vulgaris that has not responded to topical therapies and oral antibiotics, and moderate to severe hirsutism. The contraceptive effect provides an additional benefit, but this product should not be used solely for contraception because of its elevated thromboembolic risk compared with other combined oral contraceptives.
• May also be used for androgenetic alopecia (female pattern hair loss) in selected patients, though this is an off‑label use.
• Not indicated for use in men, children before menarche, or postmenopausal women.

Important Warnings and Precautions

At‑risk groups

• Pregnancy: This product is absolutely contraindicated during pregnancy. Cyproterone acetate can cause feminisation of male fetuses if exposure occurs during the critical period of sexual differentiation (first trimester). If pregnancy occurs, the medication must be discontinued immediately. Women of childbearing potential should have a negative pregnancy test before starting therapy and use effective contraception (which is provided by the product itself).
• Breastfeeding: Cyproterone acetate and ethinylestradiol are excreted in breast milk in small amounts. Combined hormonal contraceptives may reduce milk production and alter milk composition. Use during breastfeeding is not recommended; a progestin‑only contraceptive is preferred.
• Paediatrics (< menarche): Safety and efficacy have not been established in children or adolescents before menarche. The product is indicated only for women of reproductive age.
• Elderly: Not indicated for use in postmenopausal women.
• Venous thromboembolism (VTE): This combination is associated with a higher risk of VTE than levonorgestrel‑containing pills. The risk is highest during the first year of use and in women with a personal or family history of VTE, thrombophilia, obesity, or prolonged immobilisation. The estimated incidence of VTE in users of cyproterone acetate/ethinylestradiol is approximately 9–12 per 10,000 woman‑years, compared with 5–7 per 10,000 for levonorgestrel‑containing pills and 2 per 10,000 for non‑users. This product should be discontinued at least 4 weeks before major elective surgery and during prolonged immobilisation. It is contraindicated in women with a history of VTE or known thrombophilia.
• Arterial thromboembolism: The risk of myocardial infarction and stroke is increased, particularly in women who smoke, are over 35 years of age, have hypertension, or have migraine with aura.
• Hypertension: Contraindicated in women with uncontrolled hypertension. Blood pressure should be measured before starting therapy and periodically thereafter.
• Liver disease: Cyproterone acetate has been associated with hepatotoxicity, including benign and malignant liver tumours, cholestatic jaundice, and acute liver failure, particularly at higher doses (e.g., 50–100 mg used for prostate cancer). Liver function tests must be performed before starting treatment, and the drug is contraindicated in patients with active liver disease or a history of liver tumours. If abnormal liver function develops, the product must be stopped immediately.
• Migraine: Contraindicated in women with migraine with aura (focal neurological symptoms). In women who develop new‑onset migraine or worsening of migraines, the medication should be discontinued.
• Diabetes mellitus: Low‑dose combined oral contraceptives have a small effect on glucose and lipid metabolism. Women with diabetes should be monitored, and their insulin or oral hypoglycaemic requirements may need adjustment.
• Breast and reproductive cancers: Long‑term use of combined oral contraceptives is associated with a slight increase in the risk of breast and cervical cancer. The product is contraindicated in women with known or suspected breast carcinoma or other estrogen‑ or progestin‑dependent neoplasia.
• Depression: Cyproterone acetate can cause depressed mood and fatigue. Women with a history of depression should be monitored, and the drug should be discontinued if severe depression recurs.
• Allergy: Do not take this product if you have a known hypersensitivity to cyproterone acetate, ethinylestradiol, or any excipient in the tablet.

Driving and alcohol

This product has no known influence on the ability to drive or operate machinery. However, some women may experience fatigue or dizziness, particularly during the first cycles. Moderate alcohol consumption does not directly interfere with the contraceptive effect; however, excessive drinking can lead to vomiting or severe diarrhoea, which may reduce the absorption of the active tablets. Women who vomit within 3‑4 hours of taking an active tablet should use a backup contraceptive method. Alcohol intake should be limited, particularly in view of the potential for additive liver effects with cyproterone acetate.

Dosage Instructions

• Standard regimen: One tablet daily for 21 days, followed by a 7‑day tablet‑free interval. Withdrawal bleeding usually occurs 2‑3 days after the last active tablet. The next pack is started on the day after the tablet‑free interval, even if bleeding continues.
• Starting therapy:
  • Day 1 start: Take the first tablet on the first day of menstrual bleeding. Contraceptive protection begins immediately.
  • Switching from another combined hormonal contraceptive: Start the next day after the last active tablet of the previous product.
  • After childbirth or second‑trimester abortion: Start no earlier than 4 weeks postpartum (6 weeks if breastfeeding). If intercourse has occurred, pregnancy must be excluded.
  • After first‑trimester abortion: Start immediately.
• Missed tablet(s): Follow standard missed‑pill guidelines. If one tablet is missed by less than 24 hours, take it immediately and continue as normal. If two or more tablets are missed, a backup barrier method should be used for 7 days, and the instructions for missed pills should be consulted based on the week of the cycle.
• Duration of treatment for acne/hirsutism: Improvement is gradual. Treatment is usually continued for at least 6 to 12 months. Once the condition has resolved, an additional 3–4 cycles should be completed before stopping to reduce the risk of recurrence. If the condition returns after discontinuation, treatment may be restarted. Long‑term use requires periodic re‑evaluation of risks and benefits, especially given the VTE risk.

Side Effects and Contraindications

• Very common (≥ 10%): Nausea, breast tenderness, headache, and breakthrough bleeding or spotting (especially in early cycles).
• Common (1‑10%): Weight gain, fluid retention, decreased libido, depressed mood, fatigue, and chloasma (melasma). The anti‑androgenic effects may lead to a reduction in acne and sebum production, which is a desired outcome.
• Serious but rare: Venous thromboembolism (deep vein thrombosis, pulmonary embolism) — the most important safety concern and the reason for market withdrawal in Canada. Hepatotoxicity, including hepatitis, jaundice, and benign or malignant liver tumours (cyproterone acetate has a black box warning for hepatotoxicity at higher doses, and although the 2 mg dose is much lower, rare cases have been reported). Arterial thromboembolism (myocardial infarction, stroke). Gallbladder disease. Pancreatitis if severe hypertriglyceridemia is present. Retinal thrombosis.
• Contraindications: History of or current venous or arterial thromboembolic disease (deep vein thrombosis, pulmonary embolism, stroke, myocardial infarction), thrombophilia, migraine with aura, uncontrolled hypertension, active liver disease or liver tumours, known or suspected breast cancer or other estrogen‑dependent neoplasia, undiagnosed genital bleeding, pregnancy, breastfeeding, and hypersensitivity to any ingredient.

Drug Interactions

• Enzyme‑inducing drugs (reduce contraceptive efficacy): Rifampicin, rifabutin, carbamazepine, phenobarbital, phenytoin, primidone, oxcarbazepine, topiramate, griseofulvin, and St. John’s wort. A barrier method should be used during and for 28 days after stopping the inducer.
• Antibiotics (controversial): With the exception of rifampicin‑like drugs, most antibiotics do not consistently reduce contraceptive efficacy. Women who experience breakthrough bleeding during antibiotic therapy may choose to use additional protection.
• Lamotrigine: Ethinylestradiol can reduce lamotrigine levels, potentially increasing seizure risk.
• Cyclosporine: Ethinylestradiol may increase cyclosporine levels, increasing nephrotoxicity risk.
• Hepatotoxic drugs: Concomitant use with other drugs known to cause liver injury (e.g., methotrexate, isoniazid, ketoconazole) should be undertaken with caution due to the additive hepatotoxic potential of cyproterone acetate.
• Alcohol: Chronic heavy alcohol use may increase the risk of liver injury when combined with cyproterone acetate. Alcohol should be limited.

Practical Advice

• Administration: Take one tablet at the same time each day for 21 days, then a 7‑day break. Tablets may be taken with or without food. If you miss a dose, follow the missed‑pill instructions.
• Monitoring: Liver function tests (ALT, AST) should be performed before starting treatment and periodically during therapy. Blood pressure should be checked at baseline and every 6‑12 months. Women should be counselled on the signs and symptoms of VTE and instructed to report leg swelling, chest pain, or shortness of breath immediately. Any new or worsening migraines, vision changes, or abdominal pain should be reported.
• Storage: Store at room temperature (15‑30 °C), protected from moisture and light. Keep out of the reach of children.
• Lifestyle: This product does not protect against HIV or other sexually transmitted infections. A condom should be used for STI protection. Avoid smoking, particularly if over 35, as it greatly increases cardiovascular risk. Limit alcohol. If you plan to become pregnant, discontinue the product and allow at least one spontaneous menstrual cycle before trying to conceive. If surgery is planned, the product should be stopped 4 weeks in advance.
• When to seek medical review: Stop the medication and contact your doctor immediately if you experience: signs of a blood clot (leg pain/swelling, sudden chest pain, difficulty breathing, coughing up blood), signs of liver problems (jaundice, dark urine, right upper abdominal pain, severe fatigue), sudden severe headache or migraine with aura, significant rise in blood pressure, or a new breast lump.
• Disposal: Return unused or expired tablets to a pharmacy for safe disposal. Do not flush down the toilet.

Alternative Medications

• Other combined oral contraceptives with anti‑androgenic progestins: Yaz® and Yasmin® contain drospirenone, a progestin with anti‑mineralocorticoid and anti‑androgenic properties, approved in Canada for acne. They have a lower risk of VTE than cyproterone acetate‑containing pills, but are still associated with an elevated risk compared with levonorgestrel pills. Alesse®, Marvelon®, and other COCs are primarily contraceptive but may improve mild acne.
• Spironolactone: An anti‑androgen used off‑label for acne and hirsutism, often at doses of 50–200 mg/day. It does not provide contraception and must be combined with a reliable contraceptive method because of its teratogenic potential (feminisation of male fetus).
• Topical acne therapies: Retinoids (tretinoin, adapalene), benzoyl peroxide, and topical antibiotics are first‑line for mild‑to‑moderate acne, and can be used in combination with oral therapy.
• Oral isotretinoin (Accutane®): For severe nodulocystic acne, isotretinoin is highly effective but requires a mandatory pregnancy prevention program due to its potent teratogenicity. It does not contain estrogen or progestin.
• Non‑pharmacological: Laser hair removal and electrolysis are effective long‑term treatments for hirsutism, and can be used alongside medical therapy.

Clinical Efficacy

The combination of cyproterone acetate 2 mg and ethinylestradiol 0.035 mg has been shown in numerous clinical trials to be highly effective for the treatment of moderate to severe acne and hirsutism. In placebo‑controlled studies, it reduces inflammatory and non‑inflammatory acne lesion counts by 50–80% over 6–12 cycles. The anti‑androgenic effect results in a gradual reduction in sebum production and improvement in hirsutism scores. Contraceptive efficacy is comparable to other combined oral contraceptives, with a Pearl Index of approximately 0.1–0.2 per 100 woman‑years when used perfectly. However, the elevated risk of venous thromboembolism led to its withdrawal from the Canadian market in 2003. Internationally, it remains available and is considered a second‑line therapy for acne and hirsutism when other treatments have failed, with the understanding that it should not be used solely for contraception. The prescribing physician must carefully weigh the risk of VTE against the benefit of anti‑androgenic therapy, and limit use to women who require anti‑androgen treatment and have no risk factors for thromboembolism.

Important:

This combination product (cyproterone acetate/ethinylestradiol) is a prescription medication that has not been approved for marketing in Canada due to a higher risk of life‑threatening blood clots (venous thromboembolism). It should only be used under the supervision of a qualified healthcare professional, and only for the treatment of severe acne or hirsutism when other therapies have failed—never for contraception alone. You must not use this product if you have a history of blood clots, liver disease, migraine with aura, uncontrolled high blood pressure, or if you are pregnant or may become pregnant. Seek immediate medical attention if you develop symptoms of a blood clot (leg pain or swelling, sudden chest pain, difficulty breathing), signs of liver injury (jaundice, dark urine, severe fatigue), or a new severe headache with visual changes. This information is not a substitute for professional medical advice, diagnosis, or treatment.

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