TESTOSTERONE ENANTHATE 1 ml / 250 mg
Testoterone Enanthate USP29, Ph.Eur.5.5 Micronized grade
Formula: C26H40O3(CAS-315-37-7, ATC-G03BA03)
Active life: 8 days
Detection time: 3 months
Anabolic/Androgenic ratio: 100:100
TESTO 250® is a steroid compound that is described chemically as 17(3- Hydroxyandrost-4- en-3-one heptanoate. It is the principal hormone of the testis. The ester, Enanthate, is a stable, white or yellowish-white crystalline powder that is insoluble in water but very soluble in dehydrated alcohol, freely soluble in fatty oil and dichloromethane. Esterification of the 17 beta-hydroxy group produces compounds which havea longerduration of action.
TESTO 250® is a sterile solution of Testosterone Enanthate USP29, Ph.Eur.5.5 Micronized grade in Miglyol 840, Ethyl oleate. Benzyl benzoate. Benzyl alcohol.
Endogenous androgens are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics.These effects include the growth and maturation of the prostate, seminal vesicles, penis, and scrotum; the development of male hair distribution, such as the beard, and pubic, chest, and axillary hair, laryngeal enlargement, vocal-cord thickening; alterations in body musculature; and fat distribution. Drugs in this class also cause retention of nitrogen, sodium, potassium, and phosphorus and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein.
Androgens are responsible for the growth spurt of adolescence and for the eventual termination of linear growth which is brought about by fusion of the epiphyseal growth centers. In children, exogenous androgens accelerate linear growth rates but may cause a disproportionate advancement in bone maturation. Use over long periods may result in fusion of the epiphyseal growth centers and termination of the growth process. Androgens have been reported to stimulate the production of red blood cells by enhancing the production of erythropoietic stimulating factor.
During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). At large doses of exogenous androgens, spermatogenesis may also be suppressed through feedback inhibition of pituitary follicle stimulating hormone (FSH).
There is lack of substantial evidence that androgens are effective in fractures, surgery, convalescence, and functional uterine bleeding.
TESTO 250® is less polar than free testosterone. TESTO 250® in oil injected intramuscularly is absorbed slowly from the lipid phase; thus, it can be given at intervals of 2 to 3 times perweek.
Testosterone in plasma is 98% bound to a specific testosterone estradiol binding globulin, and about 2% is free. Generally, the amount of this sex-hormone binding globulin in the plasma will determine the distribution of testosterone between free and bound forms, and the free testosterone concentration will determine halflife.
About 90% of a dose of testosterone is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver. Testosterone is metabolized to various 17-ketosteroids through two different pathways. The half-life of testosterone as reported in the literature varies considerably; it ranges from 10 to 100 minutes.
In many tissues the activity of testosterone appears to depend on reduction to dihydrotestosterone, which binds to cytosol receptor proteins. The steroid- receptor complex is transported to the nucleus where is initiates transcription eventsand cellular changes related to androgen action.
INDICATIONS AND USAGE:
Males: TESTO 250® is indicated for replacement therapy in conditions associated with a deficiency or absence of endogenous testosterone:
A. Primary hypogonadism (congenital or acquired) -testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, or orchidectomy.
B. Hypogonadotropic hypogonadism (congenital or acquired) - idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.
If the above conditions occur prior to puberty, androgen replacement therapy will be needed during the adolescent years for development of secondary sexual characteristics. Prolonged androgen treatment will require to maintain sexual characteristics in these and other males who develop testosterone deficiency after puberty.
C. TESTO 250® may be used to stimulate puberty in carefully selected males with clearly delayed puberty that is not secondary to a pathologic disorder; puberty is expected to occur spontaneously at a relatively late date. Brief treatment with conservative doses may occasionally be justified in these patients if they do not respond to psychologic support.The potential adverse effect on bone maturation should be discussed with the patient and parents prior to androgen administration. An x-ray of the hand and wrist to determine bone age should be obtained every 6 months to assess the effect of treatment on the epiphyseal centers (See WARNINGS).
Females: TESTO 250® may be used secondarily in women with advancing in operable metastatic (skeletal) mammary cancer who are 1 to 5 years postmenopausal. Primary goals of therapy in these women include ablation of the ovaries. Other methods of counteracting estrogen activity are adrenalectomy, hypophysectomy,and/orantiestrogen therapy.
This treatment has also been used in premenopausal women with breast cancer who have benefited from oophorectomy and are considered to have a hormone- responsive tumor. Judgement concerning androgen therapy should be made by an oncologist with expertise in this field.
TESTO 250® has been used for the management of postpartum breast pain and engorgement. (There is no satisfactory evidence that this drug prevents or suppresses lactation.)
TESTO 250® is contraindicated in men with carcinomas of the breast or with known or suspected carcinomas of the prostate and in women who are or may become pregnant. When administered to pregnant women, androgens cause virilization of the external genitalia of the female fetus. This virilization includes clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is related to the amount of drug given and the age of the fetus and is most likely to occur in the female fetus when the drugs are given in the first trimester. If the patient becomes pregnant while taking these drugs, she should be apprised of the potential hazard of thefetus.