What Is the History of Sickle Cell Anemia?

Cyproterone is a white crystalline powder chemical, alias: cycloprogesterone acetate, chemical formula is C ₂₄ H ₂₉ ClO ₄ , molecular weight is 416.93800, melting point is 237.5 ~ 240ºC, almost insoluble in water, slightly Soluble in absolute ethanol; easily soluble in acetone, soluble in methanol, very soluble in dichloromethane, protected from light. Cyproterone is mainly used clinically to treat male libido, hirsutism in women, acne, precocity, hypersexuality, and prostate cancer.

Chinese name: Cyproterone
Foreign name: cyproterone
CAS NO.: 2098-66-0

Molecular formula: C24H29ClO4
Molecular weight: 416.94
Melting point: 237.5-240ºC

Cyproterone Basic Information

Chinese name: Cycloprogesterone

Chinese alias: Ciprodil Progesterone Impurity F

English name: cyproterone

English alias: Cyproterone

CAS number: 2098-66-0 ^[1]

Molecular formula: C ₂₄ H ₂₉ ClO ₄

Molecular weight: 416.93800

Chemical structure:

Exact mass: 416.17500

PSA: 60.44000

LogP: 4.60760

Physicochemical Properties of Cyproterone

Density: 1.29 g / cm ³

Melting point: 237.5-240ºC

Boiling point: 521ºC at 760 mmHg

Flash point: 268.9ºC

Refractive index: 1.604

Vapor pressure: 4.92E-13mmHg at 25 ° C ^[1]

Summary of basic information about cyproterone

Cyproterone Drug Name

Chinese name: Cycloprogesterone

English name: Cyproterone

Alias: Cyproterone acetate; Seprone; Cyclo medroxyprogesterone; Anjunco; Meclodigestrel ^[2-3]

Classification of cyproterone

Drugs of endocrine system> Drugs for gonadal diseases ^[2]

Cyproterone dosage form

1. Tablets: 50mg each;

2. Cream: 1%;

3. Diane-35 tablets: Each tablet contains 2mg of CPA and 35g of ethinyl estradiol ^[2] .

Cyproterone pharmacological action

Cyproterone pharmacokinetics

Cyproterone can be absorbed after oral administration, and the blood peak can be reached in 3 to 4 hours. In the first 24 hours, due to systemic distribution and excretion, the blood drug concentration decreased rapidly. The terminal elimination t1 / 2 is about 38h. The main metabolite is 15-hydroxycycloprogesterone, which has an anti-androgenic effect. About 35% of the dosage is excreted in urine with the original drug and conjugate, and the rest is found in feces ^[2] .

Cyproterone indication

It is clinically used to treat abnormal libido in men, hirsutism in women, acne, precocious puberty, hypersexuality, and prostate cancer ^[2] .

Cyproterone contraindications

1. Liver disease, cachexia or weight loss are forbidden ^[3] .

2. Severe chronic depression, undeveloped adults, those with a history of thrombosis and pregnant women are contraindicated ^[2] .

Cyproterone precautions

1. Sickle cell anemia, depression and those with a history of thromboembolism should be used with caution.

2. Do not drive or operate machinery during medication ^[3] .

3. During the medication, liver function should be checked frequently.

4. Because ethanol can reduce the effect of cyproterone, chronic alcoholism is not effective ^[2] .

Cyproterone adverse reactions

1. The use of cycloprogesterone in men can inhibit spermatogenesis, reduce sperm flow, cause infertility, and can be reversed after stopping the drug.

2. May produce abnormal sperm, male breast development, galactorrhea and benign nodules ^[3] .

3. Can cause sedation, emotional changes, changes in hair distribution, skin reactions and anemia.

4. Occasionally osteoporosis ^[3] .

5. Large doses can cause liver damage and asthma.

6. May have headache, anemia, gastrointestinal reactions, etc.

7. Oral Diane-35 may have nausea, headache, hyposexuality, depression, irregular uterine bleeding, breast pain, facial pigmentation, etc. ^[2-3] .

Cyproterone dosage

1. Take 50mg orally 2 times a day.

2. Advanced prostate cancer: Start to take 300mg orally every day, taking 2 to 3 times a day, maintaining the amount of 200 to 300mg a day, taking in divided doses.

3. Female severe acne: oral cycloprogesterone 2mg and ethinylestradiol 35g, taking medication from the first day of menstruation, and even taking 21 days as the first course of treatment; the second course of treatment starts from the seventh day of menstrual cramps, Take it 14 days in a row; in addition, apply 1% cream twice a day for 12 weeks. Oral Diane-35 (each tablet contains 2 mg of cycloprogesterone and 35 g of ethinyl estradiol), one tablet per day starting from the first day of the menstrual cycle for 21 consecutive days, stopping for 7 days is a course of treatment, and 6 courses can be repeated. This method is particularly suitable for women with acne who need contraception ^[3] .

4. Female hirsutism: 50 to 100 mg orally daily.

5. Androgen-induced hair loss in women: oral CPA 50mg, ethinylestradiol 50g, or oral Diane-35 ^[2]

Cyproterone drug interactions

1. Ethanol can reduce the effect of cyproterone, and you should not drink alcohol during the medication ^[3] .

2. When women take cyproterone and ethinyl estradiol, similar interactions with oral contraceptives can occur, making oral contraceptives ineffective ^[2] .

Cyproterone Expert Review

Cyproterone is a 17-hydroxyprogesterone derivative, which has a strong anti-androgenic effect and also has progestin activity. Can inhibit the secretion of pituitary gonadotropins, and reduce testosterone levels in the body. For men, it can still inhibit spermatogenesis, significantly reduce the number of sperm and its mobility, reduce the biochemical composition of sperm and the ability of sperm to penetrate cervical mucus, and they are all reversible. It is clinically used for abnormal libido in men, hirsutism in women, acne, precocious puberty, and prostate cancer. It has inhibitory effect on male hypersexuality, but it has the effect of inhibiting spermatogenesis. The dosage and time of use should be mastered when using it. Cyproterone acetate is a potent anti-androgenic drug. It has an effective rate of 100% in treating acne and can significantly reduce sebum spillage. It is reported that the sebum spillage rate is reduced by 85.5 in the third month of treatment %, A 96.2% decrease in the 6th month. For women with acne who have contraceptive requirements can be used as first-line drugs. For refractory acne in patients with ovarian cysts, satisfactory results can also be obtained. It is also effective for female hirsutism and female androgen-induced hair loss. Not generally used by men. Also be alert for its liver toxicity and potential carcinogenicity. ^[2]