Estosterone Cypionate - clinical Pharmacology
Endogenous androgens are responsible for the normal growth and development of the male genitalia and for maintaining secondary sexual characteristics. These effects include the growth and maturation of the prostate, seminal vesicles, penis, and scrotum; the development of the distribution of male hair, such as beard, pubis, breast, and axillary hair; laryngeal enlargement, thickening of the vocal cord, and changes in the distribution of musculature and body fat. Drugs in this class also cause retention of nitrogen, sodium, potassium, and nitrogen, phosphorus, and decreased urinary calcium excretion. Androgens have been reported to increase protein anabolism and reduce protein catabolism. The nitrogen balance increases only if there is a sufficient intake of calories and proteins.
Androgens are responsible for the growth spurt of adolescence and for the eventual cessation of linear growth caused by thermonuclear centers of epiphyseal growth. In children, exogenous androgens accelerate the rate of linear growth, but may lead to a disproportionate improvement in bone maturation. Use for a long time can lead to thermonuclear centers of epiphyseal growth and termination of the growth process. Androgens have been reported to stimulate the production of red blood cells by increasing the production of erythropoietic stimulation factor.
In exogenous androgen administration, the release of endogenous testosterone is hindered by feedback inhibition of pituitary luteinizing hormone (LH). In high doses of exogenous androgens, through feedback inhibition of pituitary follicle stimulating hormone (FSH) can also be suppressed by spermatogenesis.
There is a lack of sufficient evidence that androgens are effective in fractures, surgery, recovery, and functional uterine bleeding.
Testosterone esters are less polar than free testosterone. The testosterone esters in the oil, administered intramuscularly, are slowly absorbed from the lipids stage; thus, Testosterone Cypionate can be given every two to four weeks.
The testosterone in the plasma is 98 percent bound to the globulin binding specific testosterone estradiol, and about 2 percent is free. Typically, the amount of globulin required by this sex hormone in the plasma will determine the distribution of testosterone between free and bound forms, and free testosterone will determine its half-life.
About 90 percent of the dose of testosterone from the body is in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of the dose from the body is in the feces, mainly in conjugated form. Testosterone inactivation occurs mainly in the liver. Testosterone is metabolized by different 17-Keto steroids through two different pathways.
The half-life of Testosterone Cypionate when administered intramuscularly is approximately eight days.
In many tissues, testosterone activity appears to be affected by the reduction of dihydrotestosterone, which binds to cytosol receptor proteins. The steroid receptor complex is transported to the nucleus, where it initiates transcription events and cellular changes associated with androgen action.
Indications and use for Testosterone Cypionate
Injection of Testosterone Cypionate, USP is indicated for replacement therapy in Male in conditions associated with the symptoms or absence of endogenous testosterone.
Major hypogonadism (congenital or acquired) testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome; or orchidectomy.
Hypogonadotropic hypogonadism (congenital or acquired) Idiopathic gonadotropin or LHRH deficiency or pituitary hypothalamic injury from tumors, trauma, or radiation.
- Known hypersensitivity to the drug
- Men with breast carcinoma
- Men with known or suspected prostate carcinoma
- Women who are or who may become pregnant
- Patients with serious heart, liver, and kidney diseases
Hypercalcemia may occur in immobilized patients. In this case, the drug should be discontinued.
Long-term use of high-dose androgens (mainly 17-? alkyl androgens) has been associated with the development of liver tumors, hepatocellular carcinoma, and peliosis hepatis ? all potentially life-threatening complications.
Geriatric patients with androgens may be at increased risk of developing prostatic hypertrophy adenoma and prostate carcinoma, despite the lack of compelling evidence to support this concept.
Edema, with or without heart failure, can be a serious complication in patients with pre-existing heart, kidney, or liver diseases.
Gynecomastia can develop and sometimes persists in patients due to hypogonadism.
This product contains benzyl alcohol. Benzyl alcohol is reported to be associated with fatal ?shortness of breath syndrome? in premature newborns.
Androgen therapy should be used cautiously in healthy men with delayed puberty. The effects on bone maturation should be monitored by assessing the age of the wrist and arm bones every 6 months. In children, androgen treatment can accelerate bone maturation without giving compensatory benefits in linear growth. This negative impact can lead to compromised adult authority. The younger the child, the greater the risk of damage to the final mature height.
This drug has not been shown to be safe or effective for improving athletic performance. Due to the potential risk of serious adverse health effects, this drug should not be used for such a purpose.
|Active substance||Testosterone, Testosterone Cipionato|
|Active ingredient, mg||200|
|1 bottle, ml||10|
|Bottles in the package, pcs||1|
|Manufacturer||Zhengzhou Pharmaceutical Co. Ltd|