Testosterone Propionate is a synthetic androgen that acts like testosterone and testosterone and inhibits the secretion of adrenocortical gonadotropins and promotes protein synthesis. Testosterone propionate is a propionate derivative of testosterone, and the ratio of testosterone propionate and protein assimilation is 1:1. Androgen activity is stronger. Oral ineffective, intramuscular injection can last 2 to 3 days. Hepatotoxicity is small. At present, it is considered that topical rubbing with ointment containing testosterone propionate is the standard method for the treatment of sclerosing moss, but its efficacy varies from person to person, and some lesions are improved, but there are also no significant effect. Can improve the serum testosterone concentration, enhance sexual function, and the role of a longer duration, easy to use. Testosterone propionate has a strong and long-lasting effect, and it has a strong anti-inflammatory and inflammatory-absorbing effect. Women’s general disease dosage does not exceed 300 mg per month, and caution is required in patients with hypertension and heart failure. Clinically applicable to the testicular deficiency (no testis and cryptorchidism) supplementary treatment, gynecological diseases such as menorrhagia, functional uterine bleeding. Mainly used for advanced breast cancer, is now less used. Also used for multiple myeloma and kidney cancer. The drug is used for advanced breast cancer and is effective in patients with menopause and menopause less than 5 years. The effective rate is 20% to 30%, lower than the use of estrogen. The hormone receptor positive rate was 46%, and the negative rate was only 8%. The effective survival was 18 to 20 months, and the ineffective rate was 7 to 10 months. The effect on bone metastases was better, and 80% of the patients could relieve symptoms. The effective rate of soft tissue and lymph node metastasis is 20%, and visceral metastasis is rarely effective.
The pharmacological effects of testosterone propionate
The ratio of testosterone propionate androgens and protein assimilation is 1:1. After entering the body, it is first converted to Dihydrodroitone (Dihy-drotestosterone by 5α reductase, and then it binds to cellular receptors, enters the nucleus, and interacts with chromatin, activates RNA polymerase, promotes protein synthesis and cell metabolism, and reduces protein Decomposition, muscle growth, weight gain, reduce azotemia; promote calcium and phosphorus reabsorption, increase bone calcium and phosphorus deposition and bone formation. In adolescence, it can promote the development of male secondary sexual characteristics. In addition to maintaining secondary sexual characteristics and sexual function, adults can also suppress the secretion of endogenous gonadotropin, atrophy the testis, and inhibit endometrial hyperplasia. In addition, testosterone propionate stimulates the production and differentiation of red blood cells by erythropoietin, improves blood circulation, and improves the general condition of advanced cancer patients. Prolonged administration may have effects on the granulocyte system and the megakaryocyte system. The role of bone marrow hematopoietic function is indirectly through stimulating the kidney to secrete erythropoietin. It may also directly stimulate bone marrow and promote hemoglobin synthesis. Promote the secretion of sebaceous glands. Testosterone propionate is a rapid and potent person with androgenic activity. Can promote the development and maturation of male organs and parasexual sex, and maintain its mature state. Small doses can promote the secretion of gonadotropins by the pituitary gland, thus exerting positive feedback; high doses are the opposite. It acts against estrogen and inhibits endometrial growth and ovarian and pituitary function. Assimilation is obvious.
Pharmacokinetics of testosterone propionate
Easy to absorb orally, but some drugs are rapidly destroyed in the liver. After intramuscular injection of testosterone propionate, the absorption was slower and its onset time was 2 to 4 days. In blood, 98% bind to plasma proteins and only 2% are free. The half-life is 10-20 min. Most of the testosterone propionate is metabolized in the liver into less active androsterone and inactive 5β-androsterone, of which 90% is associated with uronic acid and sulfuric acid and is excreted with urine. About 6% of unbound metabolites are Bile is excreted, and a small part is excreted by the feces, and a small part of them can still be reabsorbed to form the enterohepatic circulation
Dosage of testosterone propionate
1. Adult: (1) male sex gland functional low hormone replacement therapy: 25-50mg every time, 2-3 times per week. (2) postmenopausal women with advanced breast cancer: 50 to 100mg per session, 3 times a week. (3) functional uterine bleeding: between 25 and 50mg, 1 time per day, 3 to 4 times. (4) aplastic anemia: once every 100mg, daily or alternate days, the course should be over 3-6 months. (5) menorrhagia and uterine fibroids: sanhe hormone (injection, each containing 25 mg testosterone propionate, benzoic acid, two female two female 1.25 mg 1.25 mg estradiol and progesterone) 1 intramuscular injection, bleeding time, repeated after 6-8 h when necessary. The blood stops after the estrogen and progesterone maintenance (see diethylstilbestrol). (6) senile osteoporosis: 25mg per time, 2-3 times per week, 3-6 months. (7) androgen deficiency: between 10 and 50mg every time, 2-3 times per week. Children: male youth development delay: between 12.5 and 25mg, 2-3 times per week, no more than 4-6 months.
2. Vulva sclerosing moss: clinical general with 200 mg of testosterone propionate add 10 g 2% vaseline ointment or cream mixture preparation inunction affected part, wipe slightly to massage, after the initial one month three times a day, use drug 1 months or so can appear curative effect, and 1 times a day, a total of 2 months, the last 2 times per week to share 3 months to half a year, itching disappeared after 1-2 years, drug use frequency can reduce gradually, until the amount of 1-2 times per week to maintain. If there is a local masculine adverse reaction after testosterone propionate, it can be observed that the symptoms are still more obvious with the use of progesterone 100mg to be added to the 30g vaseline ointment.
3. Androgen deficiency: intramuscular injection: 10-50mg, 2-3 times per week.
4. Nearly menopausal dysfunctional uterine bleeding: testosterone propionate 25 mg compatibility progesterone 10 mg, intramuscular injection, 5-7 days, 20 days or so every time the menstrual cycle began, can apply 3-4 weeks continuously.
5. Female breast cancer and bone metastasis: intramuscular injection: 50-100mg, 1 time on the next day, 2-3 months.
6. Uterine fibroids, renal carcinoma, ovarian cancer and multiple myeloma: 25-50mg per time, 2 times per week, intramuscular injection.
