PROPIOLAB 100

Testosterone is an androgen, derived from the steroid cyclopentaneperhydrophenanthrene, that has 19 carbon atoms, a double bond between C4 and Cs, an oxygen atom at C3, and a hydroxyl radical (OH) at C17. This structure is necessary to maintain androgenic activity. At various sites of action, testosterone is not the active form of the hormone, in target organs it is converted through the steroid 5-reductase to dihydrotestosterone, which is more active. Most of the steroid 5-reductase 1 is found in the non-genital region and the liver and the steroid 5-reductase 2 is found primarily in the male urogenital tract and genital skin of both sexes. Testosterone itself is also believed to be the main mediator of luteinizing hormone regulation by the hypothalamic-pituitary system and spermatogenesis. Testosterone or dihydrotestosterone binds to an intracellular protein receptor and the hormone-receptor complex binds in the nucleus to specific regulatory elements on the chromosome, and acts to increase the synthesis of specific RNA and proteins. The human androgen receptor is a typical member of the thyroid hormone and steroid superfamily. It is encoded by a gene on the X chromosome and contains androgen-binding, DNA-binding, and functional domains; testosterone and dihydrotestosterone are believed to act to promote male virilization. Esterification of testosterone in OH and C17 increases the lipid solubility of testosterone and prolongs its action. Testosterone propionate is particularly active parenterally.

Esterification of the 17-hydroxyl group increases lipid solubility and leads to slower systemic absorption if administered via intramuscular injection. Esters absorption rate is related to the size of the ester group. Testosterone esters are hydrolyzed to testosterone after absorption.

Testosterone is about 80% bound to sex hormone binding globulin. Derivatives of 19-nostestosterone and derivatives of 17-methylated are characterized by a reduced binding to this globulin. Plasma elimination half-life of testosterone is between 10 and 100 min. It is metabolized mainly in the liver through an oxidation in the 17-OH group with the formation of androstenedione that is meabolized in addition to androstenolone, weakly androgenic, and ethiocholanolone, inactive, which are excreted mainly in the urine as glucuronide and sulfates . Approximately 6% is excreted unchanged in the faeces after undergoing enterohepatic recirculation. Testosterone is transformed into the more active derivative dihydrotestosterone in some target organs by the effect of 5-reductase. The 19-nortestosterone derivatives are less sensitive to this enzyme. Small amounts of testosterone aromatize in the body as a result of the formation of estrogen derivatives in the body. In derivatives with a saturated one ring such as mesterolone, fewer estrogens are aromatized.

It is used to treat male hypogonadism. It is commonly used in combination with Testosterone Enanthate.

It is used in renal failure as acute oily solutions for intramuscular administration.

It is used as an adjunct in the treatment of postmenopausal breast carcinoma, some postmenopausal disorders, and delayed puberty in boys.

In male hypogonadism: In adults, as oily solutions for intramuscular administration, doses of 10 to 50 mg, two or three times a week.

In acute renal failure: dose 25 mg / day, for a maximum of 10 days.

Contraindications

Testosterones should be avoided in the following cases:

Pregnancy: There are no reports of virilization of the female fetus after treatment of the mother with testosterone or methyl testosterone during pregnancy.

Breastfeeding: the use of testosterone in breastfeeding women should be avoided, due to the potential androgenic effect on the baby.

Porphyria: Androgens are not considered safe for patients with porphyria, although there is experimental evidence of porphyrinogen contraction.

Testosterone and other androgens can produce side effects related to androgenic and anabolic activities: increased nitrogen, water and sodium retention, edema, increased vascularity of the skin, hypercalcemia, impaired glucose tolerance and increased of bone growth and skeletal weight. Other effects include increased low-density lipoprotein cholesterol values, decreased high-density lipoprotein cholesterol values, increased hematocrit and fibrinolytic activity. Androgens can cause headaches, depression, and gastrointestinal bleeding. Androgens have been reported to induce sleep apnea in patients prone to this disturbance.

Abnormal liver test results have been described and case reports of hepatotoxicity, such as jaundice, and cholestatic hepatitis have been published. These adverse liver effects have been identified predominantly with 17-alkylated derivatives. In men, high doses suppress spermatogenesis and produce degenerative changes in the seminiferous tubules. Priapism is a sign of overdose seen especially in older men. Gynecomastia has been described. Androgens can cause prostatic hyperplasia and can accelerate the growth of malignant prostate tumors.

In women, an inhibitory action of androgens was observed on the activity of the ovaries and menstruation. Continued use causes virilization symptoms, not reversible in all cases, even after discontinuation treatment. Boys experience signs of virilization: boys show early sexual development with phallic hypertrophy and increased frequency of erections and girls, hypertrophy of the clitoris. Some children may experience gynecomastia.

Use with caution in patients with cardiovascular diseases, kidney or liver failure, epilepsy, migraine, diabetes and other conditions that may be aggravated by the potential for water retention or induced edema. It should not be administered to patients with hypercalcemia and hypercalciuria, and so it should be used with caution if there are conditions that pose a risk that these appear, such as bone metastases. Patients with liver failure should not take 17-alkylated derivatives, since these drugs increase the risk of hepatotoxicity; In addition, they are totally contraindicated if the failure is serious. Androgens and anabolic steroids should be used with caution in pediatric patients due to the masculinizing effects and premature closure of the epiphyses, which can lead to linear growth inhibition and short stature. During treatment, bone maturation should be monitored.

It should not be administered during pregnancy due to the risk of virilization of the female fetus. Androgens and anabolic steroids interfere with various laboratory tests, such as glucose tolerance and thyroid function.

Interactions:

Testosterone and other androgens and anabolic steroids have been reported to enhance the activity of a number of drugs, with consequent increased toxicity. Among the drugs affected are cyclosporine, antidiabetics, levothyroxine, and anticoagulants such as warfarin. A resistance to the effects of neuromuscular blockers has also been described.

Usage restrictions:

Do not use in cases of hypersensitivity to some components, during pregnancy and lactation. It should not be used in patients with hypertension, or in patients with cardiovascular, liver and kidney dysfunction.

Adverse events have been reported with the use of doses higher than those recommended therapeutically. These are a consequence of the illegal use of androgens and anabolic steroids by athletes. These effects are abnormal results of liver function tests and liver neoplasia, increased risk of cardiovascular disease, and decreased glucose tolerance. They often induce states of zoospermia or oligospermia and testicular atrophy in men and amenorrhea or oligomenorrhea in women. Gynecomastia is relatively common in men, as is virilization in women. Psychiatric disorders have been described, such as states of mania, hypomania, depression, aggressiveness, and emotional lability.

In case of accidental overdose contact the Emergency Medical Center.

VIAL with a 10 ml x 100 mg solution.

Keep at room temperature, in a dry place and out of the reach of children.