Mechanism of Action and Pharmacokinetics Trembolone

TREMBOLONE is a strong androgen that lacks estrogenic activity. Structurally, TREMBOLONE is a 19-steroid nor, derived from nandrolone. The double bonds in C9 and C11 make TREMBOLONA very different in appearance than its relative nandrolone Its estrogenic activity has been eliminated. This is the result of the double C9-10 link. This link does not appear to be metabolically removed, which is the only possible way for this compound to convert into estrogen. Although nandrolone is rarely conceived as an estrogenic steroid, conversion to estradiol is still possible to some extent. Therefore, the fact that TREMBOLONE does not convert to estradiol remains a significant difference between the two steroids. The androgenic activity of TREMBOLONA is also much stronger than that of its relative, nandrolone. This is due to two interesting features: first, TREMBOLONE does not appear to favor the reduction of 5-alpha in humans. As such, it does not show a strong anabolic-androgenic dissociation like nandrolone, which makes it much more androgenic. In addition, the induction of the double bond in C9 and C11 seems to increase the linkage with androgenic receptors. This represents a second way in which the power of the TREMBOLONE is increased. TREMBOLONE also suppresses the natural production of testosterone rapidly, this may require the use of a testosterone stimulating drug in order to avoid a sharp fall at the time when its use is discontinued. Although listed as a “non-progestational” steroid in the literature, several studies clearly demonstrate that TREMBOLONE is linked to these receptors. As we know that all sex steroids promote the inhibition of negative feedback from testosterone production.

Mechanism of Action and Pharmacokinetics Testosterone

Testosterone is absorbed in the digestive tract, through the skin and oral mucosa. However, it undergoes extensive hepatic first-pass metabolism when administered orally and, therefore, is usually administered intramuscularly, subcutaneously or transdermally. In addition, the basic testosterone molecule has been modified to obtain active derivatives orally and prolong the duration of the effect. The alkylation of position 17 a produces derivatives that are metabolized more slowly in the liver and, for this reason, can be administered orally. Esterification of group 17 to hydroxyl increases liposolubility and leads to a slower systemic absorption if administered by intramuscular injection. The absorption rate of the esters is related to the size of the ester group. Testosterone esters are hydrolyzed to testosterone after absorption. Testosterone binds approximately 80% to the sex hormone binding globulin. The 19-nostestosterone derivatives and the 17-methylated derivatives are characterized by reduced binding to this globulin. The plasma elimination half-life of testosterone ranges from 10 to 100 min. It is mainly metabolized in the liver through an oxidation in the 17-OH group with the formation of androstenedione, which is further metabolized to androstenolone, weakly androgenic, and ethiocolanolone, inactive, which are excreted in the urine mainly as glucuronoconjugates and sulfates. Approximately 6% is excreted unmodified by feces after undergoing enterohepatic recirculation. Testosterone is transformed into the most active dihydrotestosterone derivative in some target organs by the effect of 5 a-reductase. 19-nortestosterone derivatives are less sensitive to this enzyme. Small amounts of testosterone are aromatized in the body, leading to the formation of estrogenic derivatives in the body. Derivatives with a saturated A ring, such as mesterolone, aromatize less estrogen.

Mechanism of Action and Pharmacokinetics Methenolone

Anabolic androgens are steroids derived from testosterone in which it tries to chemically decrease androgenic and virilizing effects and increase anabolic actions. According to their chemical structure and function they are divided into three groups. The second group is that of dihydrotestosterone (DHT) and derivatives, methenolone. Testosterone and androgens easily cross the cell membrane and bind to specific intracellular receptors, these receptors that have been purified are proteins with a molecular weight of approximately 120 kilodaltons. Its synthesis is genetically determined on the X chromosome. DHT binds at a receptor site near a carboxyl terminal group. The steroid receptor complex is activated and transported to the cell nucleus and binds to a DNA receptor site, increasing the activity of RNA polymerase and the formation of messenger RNAs stimulating the synthesis of cellular proteins responsible for the physiopharmacological actions. By intramuscular vis they are pharmacologically active, testosterone is introduced by simple diffusion into daily cells given its liposolubility, in many target tissues it is enzymatically converted to DHT by the action of an enzyme called t5-alpha-reductase, it is more active than testosterone . Biotransformation occurs in the liver, the main metabolites are eliminated in the urine. Maximum concentrations are reached 6-11- days after the injection given. The absolute bioavailability of methenolone enanthate is 100%.

Indications

TREMBOLONE is a steroid used to increase appetite.
Its strong androgenic and non-estrogenic properties made it ideal for increasing muscle hardness, definition and strength without fluid retention. Increase in erythropoiesis (increase in blood count).

• It is used in the treatment of male hypogonadism. It is usually active in combination with testosterone enanthate.
• It is used in acute renal failure in the form of oily solutions for intramuscular route, topical route is used
• It is used as an adjunct in postmenopausal breast carcinoma, some postmenopausal disorders and late puberty in children.

It is indicated in states that increase protein synthesis is required to improve the general condition of the patient or prevent damage from catabolic processes such as consumptive diseases, cachexia, advanced breast carcinoma or postmenopausal osteoporosis.

Contraindications

TREMBOLONE may affect cardiovascular function to some extent, which means that it is not suitable for those patients who suffer from any deficiency at this level or in those who regularly participate in sports or activity in which they require a decent level of effort cardiovascular.

TESTOSTERONES should be avoided in the following cases:

• Pregnancy: There are reports of virilization of the female fetus after maternal treatment with testosterone or methyl testosterone during pregnancy.
• Breastfeeding: the use of testosterones in nursing mothers should be avoided, due to the potential androgenic effect on the infant.
• Porphyria: Androgens are not considered safe in patients with porphyria, although contradictory experimental evidence of porphyrinogenesis is available.

Adverse reactions

• It is highly toxic to both the liver and the kidneys.
• Its prolonged use can cause prostatic hyperplasia.
• It is reported in the forums that talk about the subject, without scientific basis, that at any dose it produces a significant increase in aggressiveness.
• Another very common symptom reported by consumers of TREMBOLONA consists of a sensation of suffocation and cough for a few seconds immediately after the administration of the product, especially those produced by handicraft or high in benzyl alcohol.
• In the English forums they call him “Train cough”.
• Hyperprolactinemia or increase in normal prolactin values ​​with their associated consequences, in which gynecomastia stands out.
• High blood pressure that is perceived as severe headaches.
• Other androgens own side effects: acne, sexual dysfunction, insomnia, alopecia, sweating before performing normal activities etc.

Testosterone and other androgens can cause side effects related to its androgenic and anabolic activities: increased retention of nitrogen, water and sodium, edema, increased vascularity of the skin, hypercalcemia, impaired glucose tolerance and increased growth Bone and skeletal weight. Other effects consist of an increase in cholesterol values ​​linked to low density lipoproteins, decrease in cholesterol values ​​linked to high density lipoproteins, increased hematocrit and increased fibrinolytic activity. Androgens can cause headache, depression and gastrointestinal bleeding. It has been indicated that androgens can induce sleep apnea in predisposed patients.

Abnormal results of liver function tests have been described and case reports on hepatotoxicity, such as jaundice and cholestatic hepatitis, have been published. These adverse liver effects have been predominantly identified with 17-alkylated derivatives.

In men, high doses suppress spermatogenesis and cause degenerative changes in the seminiferous ducts. Priapism is a sign of excessive doses that is observed especially in elderly men. Gynecomastia has been described. Androgens can cause prostatic hyperplasia and would accelerate the growth of malignant prostate neoplasms.

In women, the androgen inhibitory action on ovarian activity and menstruation. Its continuous use produces symptoms of virilization, it is not reversible in all cases, even after the interruption of treatment.

Boys experience signs of virilization: boys have early sexual development with phallic hypertrophy and more frequent erections, and girls, clitoral hypertrophy. Some boys may have gynecomastia.

Restrictions of Use

Do not use in case of hypersensitivity to some of its components; during pregnancy and breastfeeding period. Also, do not use in patients with hypertension, or in patients with cardiovascular problems without thorough medical control.

Overdose

Treatment in case of overdose: There have been no reports of overdose with the product.