Cyproterone Acetate Ethinylestradiol:Mechanism,Uses,Information Part2
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).
| 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.
6. What forms does Cyproterone Acetate come in?
Each cyproterone acetate tablets off-white, round, flat-faced, bevelled-edged tablet, embossed "CYP" over "50" and scored on one side, contains cyproterone acetate 50 mg. Nonmedicinal ingredients: colloidal silicon dioxide, croscaramellose sodium, and magnesium stearate.
7. How should I take Cyproterone Acetate?
Cyproterone Acetate(Ethinylestradiol)is available as an oral (by mouth) tablet and as a long-acting injectable. The recommended dose for cyproterone acetate tablets is 200 mg to 300 mg (4 to 6 tablets) daily, divided into 2 to 3 doses and taken after meals.
For men who have had an orchiectomy (removal of testicles), a lower dose of 100 mg to 200 mg daily in divided doses is recommended. The recommended dose for the long-acting form of cyproterone (Androcur® Depot) is 300 mg in injected into a muscle once a week.
Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way you are using the medication without consulting your doctor.
Cyproterone Acetate(Ethinylestradiol)can cause weakness and tiredness when you first start to take it. After about the third month, your body will become accustomed to the medication and this effect should be lessened.
It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.
Alcohol intake should be limited while taking cyproterone because it may reduce the effectiveness of the medication.
Store the medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.
Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.
8. What other information should I know before taking Cyproterone Acetate?
Other medicines, foods and drink
Cancer drugs can interact with some other medicines and herbal products. Tell your doctor or pharmacist about any medicines you are taking. This includes vitamins, herbal supplements and over the counter remedies.
Alcohol
Avoid drinking alcohol while having this treatment because alcohol reduces the effect of the drug.
Treatment for other conditions
Always tell other doctors, nurses, pharmacists or dentists that you’re having this treatment if you need treatment for anything else, including teeth problems.
If you have diabetes
This drug may affect your blood sugar levels if you have diabetes. You need to check your blood sugar more often when you are having this treatment.
Contraception
It is important not to father a child while you are having treatment with this drug and for a few months afterwards. This drug may harm a baby developing in the womb. Talk to your doctor or nurse about effective contraception before starting treatment.
Fertility
This drug can cause infertility in some men, but it is usually temporary. Fertility can return some months after treatment ends but the time it takes can vary. The effects of long term treatment on fertility is not known.
Talk to your doctor before starting treatment if you think you may want to have a baby in the future.
9. What are Cyproterone Acetate possible side effects?
Tell your doctor as soon as possible if you do not feel well while you are taking cyproterone acetate or if you have any questions or concerns.
Do not be alarmed by the following lists of cyproterone acetate side effects. You may not experience any of them. All medicines can have side effects. Sometimes they are serious but most of the time they are not.
Infertility and impotence are expected effects of cyproterone acetate and cannot generally be avoided.
Tell your doctor if you notice any of the following.
This list includes the more common side effects. Mostly, these are mild:
-tiredness
-weight changes
-headache
-changes in sex drive
-nausea and gut upset
-unusual secretion of breast milk
-sleep disturbances
-hot flushes
-restlessness
10. Cyproterone Acetate drug interaction
There may be an interaction between cyproterone and any of the following:
ethinyl estradiol
testosterone and androgens
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:
stop taking one of the medications,
change one of the medications to another,
change how you are taking one or both of the medications, or
leave everything as is.
An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, decongestants, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.
