Cyproterone Acetate Ethinylestradiol:Mechanism,Uses,Information

Cyproterone Acetate Ethinylestradiol:Mechanism,Uses,Information Part 1

 

1. What is Cyproterone Acetate Ethinylestradiol?    
2. Cyproterone Acetate Mechanism of Action    
3. Cyproterone Acetate half life    
4. What is the use of Cyproterone Acetate Enthinylestradiol?    
Cyproterone acetate uses- prevent these actions of the androgens:    
Cyproterone Acetate uses-Cyproterone Acetate birth control:    
Cyproterone Acetate uses-Treatment in Women with Acne    
5. Is cyproterone acetate a progesterone?    
6. What forms does Cyproterone Acetate come in?    
7. How should I take Cyproterone Acetate?    
8. What other information should I know before taking Cyproterone
Acetate?    
Other medicines, foods and drink    
Alcohol    
Treatment for other conditions    
If you have diabetes    
Contraception    
Fertility    
9. What are Cyproterone Acetate possible side effects?    
10. Cyproterone Acetate drug interaction    
 

 

1. What is Cyproterone Acetate Ethinylestradiol?

Cyproterone Acetate Ethinylestradiol, CAS No.427-51-0, belongs to a group of medications known as steroidal antiandrogens. It is used to treat advanced prostate cancer.Antiandrogens such as cyproterone block the effect of the hormone called testosterone. This causes a reduction in the production of testosterone in the testicles, which prostate cancer cells require for growth.

Cyproterone acetate may be available under multiple brand names and/or in several different forms. it is sold alone under the brand name Androcur or with ethinylestradiol (EE) under the brand names Diane or Diane-35 among others. 

Cyproterone is an antiandrogen. It suppresses the actions of testosterone (and its metabolite dihydrotestosterone) on tissues. It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels).

Cyproterone Acetate Chemical Information

Name	Cyproterone Acetate,Ethinylestradiol
CAS	427-51-0
Molecular Formula	C24H29ClO4
Structure
Molecular Weight	416.94
Melt Point	200-201°C
Storage Temp	2-8°C
Appearance	white powder
Factory	www.aasraw.com
Package	foil bag or customization

 

 

 

 

 

 

 

 

 

 

 

 

 

 

2. Cyproterone Acetate Mechanism of Action

Cyproterone acetate is a hormonal therapy drug used to treat prostate cancer,hormonal therapies affect different people in different ways.What is Cyproterone Acetate mechanism of action? How does Cyproterone Acetate work?

The direct antiandrogenic effect of cyproterone actate is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.

Cyproterone acetate is metabolized by the CYP3A4 enzyme, forming the active metabolite 15beta-hydroxycyproterone acetate, which retains its antiandrogen activity, but has reduced progestational activity.

3. Cyproterone Acetate half life 

Cypropterone Acetate half life is not long. 

Elimination:

Following oral or intramuscular administration, the plasma half-life is 38 and 96 hours, respectively.

Time to peak concentration:

Peak plasma concentrations are reached three to four hours after oral administration. Following intramuscular administration, mean peak blood concentrations are attained 3.4 days after injection.

Elimination:

Biliary—
        60% in the form of glucuronidized metabolites within 72 hours.

Renal—
        33% mainly in the form of unconjugated metabolites within 72 hours.

4. What is the use of Cyproterone Acetate Enthinylestradiol?

Cyproterone acetate uses is a type of medicine called an anti-androgen. Androgens are male hormones and are produced by women as well as men. They are responsible for stimulating the growth of the skin, including the sebaceous glands that produce oil (sebum), and the hair that grows from the skin. However, if your body produces too much androgen, or if your skin is particularly sensitive to the effects of androgens, the sebaceous glands may produce too much sebum. This can cause the sebaceous glands to become blocked, resulting in infection, inflammation and acne spots. The androgens may also cause excessive growth of the hair on the face and body - a condition known as hirsutism. Both these problems are common in women with polycystic ovary syndrome (PCOS).

Cyproterone acetate uses- prevent these actions of the androgens: 

It works by blocking the receptors in the body that the androgens normally work on. This means that the androgens can no longer affect the skin or the hair and acne and hirsutism can improve. Cyproterone acetate also decreases the production of androgens by the ovaries, so that there are less of these male hormones circulating.

You should notice that your skin becomes less greasy within a few weeks of treatment with this medicine, but it may take a few months of treatment before you see a definite improvement in your acne or excessive hair growth.

Cyproterone Acetate uses-Cyproterone Acetate birth control: 

This medicine is also an effective combined oral contraceptive pill. Cyproterone acetate is a progestogen derivative, and the other ingredient, ethinylestradiol, is a synthetic version of the naturally-occurring female hormone, oestrogen. The medicine works as a contraceptive by preventing the ripening and release of eggs from the ovaries, as well as increasing the thickness of the cervical mucus, which makes it more difficult for sperm to cross from the vagina into the womb. It also changes the lining of the womb so that it is less suitable for any fertilised eggs to successfully implant in.

Cyproterone Acetate is as effective a contraceptive as any other combined pill, but it should not be used solely for this purpose. It is used to treat severe acne and hirsutism in women and has the advantage of also providing contraception(cyproterone acetate birth control). This means you do not need to use any other method of contraception while you are using this medicine(cyproterone acetate birth control), unless you miss a pill, have a stomach upset, or are prescribed certain other medicines as well. See below for more information about all of these scenarios.

Cyproterone Acetate uses-Treatment in Women with Acne

The therapeutic effect of topically applied cyproterone acetate for acne treatment was clearly demonstrated. Topically applied sexual steroids in combination with liposomes are as effective as oral antiandrogen medication in acne treatment, while reducing the risk of adverse effects and avoiding high serum cyproterone acetate concentrations.

HORMONAL approaches to the treatment of acne have been the subject of much interest ever since the sebaceous gland was demonstrated to be sensitive to androgens. The use of topical antiandrogens has had theoretical appeal since the pilosebaceous unit was found to be an androgen-dependent structure. 

5. Is cyproterone acetate a progesterone?

Cyproterone acetate is a 17-hydroxyprogesterone acetate derivative with strong progestagenic properties. Cyproterone acetate acts as an antiandrogen by competing with DHT and testosterone for binding to the androgen receptor. There is also some evidence that cyproterone acetate and ethinyl estradiol in combination can inhibit 5α-reductase activity in skin.Cyproterone acetate is not available in the United States but has been used in other countries. The drug usually is administered daily in cyproterone acetate doses of 50 to 100 mg on days 5 through 15 of the treatment cycle. Because of its slow metabolism, it is administered early in the treatment cycle; when ethinyl estradiol is added, it is usually administered in 50-µg doses on days 5 through 26. This regimen is needed for menstrual control and is usually referred to as the reverse sequential regimen. Cyproterone acetate doses of 50 to 100 mg/day, combined with ethinyl estradiol at 30 to 35 µg/day, is as effective as the combination of spironolactone (100 mg/day) and an oral contraceptive in the treatment of hirsutism. In smaller doses (2 mg), cyproterone acetate has been administered as an oral contraceptive in daily combination with 50 or 35 µg of ethinyl estradiol. This regimen is primarily suited for individuals with a milder form of hyperandrogenism.