Antiandrogenic And Antiestrogenic Steroids Powder Megestrol Acetate
CAS : 595-33-5
Molecular Weight : 384.51
Melting point :214 degree centigrade
Boiling Point :507.1 degree centigrade at 760 mmHg
Flash Point :218.5 degree centigrade
Function: Provera (a progestin) intermediate.
Packing:According to Your Requirements
Appearance: White or light yellow crystalline powder (methanol), odorless and tasteless. Melt point 214-216. Soluble in acetone, slightly soluble in ethanol, ethyl ether, insoluble in water
Megestrol acetate though sometimes referred to simply as megestrol, it is important to clarify that megestrol acetate is not the same as megestrol, which is a closely related but different compound.
Megestrol acetate has powerful antiandrogenic and antiestrogenic effects in humans at sufficient doses, capable of decreasing circulating androgen and estrogen concentrations to castrate levels in both sexes and significantly lowering the expression of the androgen receptor (AR) and the estrogen receptor (ER) in the body; as an example, one study in men with benign prostatic hyperplasia who were treated with 120-160 mg of megestrol acetate per day for 3 to 11 days found average decreases in AR quantity of 73% and 86% in the cytoplasm and nucleus of prostatic cells, respectively. These actions are likely the result of a strong activation of the PR, which suppresses the secretion of the gonadotropins-peptide hormones responsible for signaling the body to produce not only progesterone but also the androgens and the estrogens-from the pituitary gland as a form of negative feedback inhibition, and hence downregulates the hypothalamic-pituitary-gonadal (HPG) axis, resulting in decreased levels of the sex hormones and their associated enzymes, carriers (e.g., sex hormone-binding globulin), and receptors.It is the antiandrogenic and antiestrogenic effects of megestrol acetate mediated by suppression of the HPG axis that are believed to be largely responsible for its beneficial effects against androgen and estrogen-sensitive cancers, respectively.
1. Mainly used for short-acting oral contraceptives, also can be used for intramuscular injection of long-acting contraceptives.
2. For the treatment of dysmenorrhea, amenorrhea, dysfunctional uterine bleeding, endometriosis and endometrial adenocarcinoma.
3. Megestrol acetate is used mainly as an appetite stimulant in a variety of conditions and as an antineoplastic agent in the treatment of breast, endometrial, and prostate cancers.
4. When given in relatively high doses, it can substantially increase appetite in most individuals, even those with advanced cancer, and is often used to boost appetite and induce weight gain i n patients with cancer or HIV/AIDS-associated cachexia. It is also used as a contraceptive in combination with an estrogen at relatively low doses.
5. In addition to its use in humans, megestrol acetate has been used extensively in veterinary medicine in the treatment of medical conditions in cats and dogs.
1. Treatment of amenorrhea, 1 time, 2 ~ 3 times a day, take 2 ~ 3, the withdrawal of 2 ~ 7, which have a withdrawal bleeding.
2. Treatment of functional bleeding, 1 4 mg, 1 every 8 hours, every 3, reduction, reduction of no more than the original dose of 1/2, and maintain volume 4 mg daily, a total of 20.
3. Treatment of endometriosis, 4 mg 1 time, 2 times a day, even served 7 to 3 times a day in the future, every 4 mg, 7 later changed to 2 times a day.1 8 mg, take 7 again, and then rose to 20 mg daily, 6 weeks as a course of treatment.
4. Breast cancer, one 40 mg, 4 times a day, 160 mg daily amount, for two consecutive months.
5. Endometrial carcinoma, 1 times 10 ~ 80 mg, 4 times a day, 40 ~ 320 mg daily, 1 or 160 mg, 1 times a day.