Mesterolone

Package leaflet (information for patients)

Tradename
Mesterolone

Dosage form
Tablets 50 mg.

Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.

Composition
Active ingredient: Mesterolone 50 mg.
Auxiliary components: microcrystalline cellulose 102, aerosil ® 200 (a hydrophilic fumed silica), calcium stearate, colorant.

Pharmacotherapeutic group
Androgen

Pharmacological properties
Pharmacokinetics :
After oral administration, mesterolone is rapidly and almost completely absorbed in a wide range of doses from 25 to 100 mg. Maximum serum drug levels are 3.1 + 1.1 ng / ml after 1.6 + 0.6 hours. Then the serum level of the drug decreases with a terminal half-life of 12-13 hours. 98% of meesterolone binds to serum proteins. Binding to albumin is 40%, while binding to SHBG (sex steroid binding globulin) is 58%.
Mesterolone is rapidly metabolized... The rate of metabolic clearance in serum is 4.4 + 1.6 ml min-1 kg-1. The drug is not excreted by the kidneys in an unchanged state. The main metabolite is 1-methyl-androsterone, the conjugated form of which is 55-70% of the metabolites excreted by the kidneys. The ratio of the main metabolite of glucuronide to its sulfate is about 12: 1. Another metabolite, accounting for about 3% of metabolites excreted by the kidneys, is 1-methyl-5-androstane-3, 17-diol. There is no metabolic conversion to estrogens or corticosteroids.
About 77% of the meterolone dose is excreted as metabolites in the urine and about 13% of the dose in the faeces.
Within 7 days, 90% of the dose is excreted, 50% of which is excreted by the kidneys within 24 hours.
The absolute bioavailability of mesterolone when taken orally is about 3%. Pharmacodynamics : The drug is an androgenic drug for oral administration. The presence of the C-1 methyl group in the structure of the drug determines the special properties of this steroid: unlike testosterone and its derivatives used for androgenic therapy, it is not metabolized into estrogen. This difference fully explains the observational data according to which, in the standard therapeutic dose used in healthy men, mesterolone does not cause significant suppression of the release of gonadotropins from the pituitary gland. In this regard, mesterolone does not affect spermatogenesis and does not affect the body's own testosterone production, which distinguishes it from other androgens that replace testosterone levels with suppression of endogenous androgen production. Unlike other oral androgens, meterolone is well tolerated by the liver, which may be due to the absence of alkyl substitution at the C-17 position of the steroid nucleus.

Indications for use
Mesterolone is prescribed for men with:
• psychovegetative disorders and decreased performance in middle-aged and elderly patients;
• violations of potency;
• reduced function of the sex glands - hypogonadism;
• infertility caused by oligospermia and lack of Leydig cells;
• aplastic anemia and so on.

Method of administration and dosage
Adults:
Initial dose:
3 or 4 tablets daily for several months, followed by maintenance therapy: 2-3 tablets (50-75mg) daily.
Children:
not recommended for children.

Side effects
It is not toxic to the liver in moderate dosages, which makes it safe to take during the course for several weeks. Does not suppress the hypothalamus-pituitary-testes axis. Given its chemical nature and similarities to DHT, side effects such as prostate hypertrophy and male-pattern baldness are possible.
In some cases
- frequent or very prolonged erections

Contraindication
- prostate cancer (because androgens can stimulate the growth of an existing tumor)
- current or history of liver tumors
- hypersensitivity to mesterolone or any other component of the drug

Overdose
Symptoms: No adverse effects due to overdose have been reported, so treatment is usually not required.
Treatment: if no more than two to three hours have passed since the overdose, and the overdose was so significant that the appointment of therapy seems to be justified, in such cases, gastric lavage may be a safe method.

Precautions
- Pregnancy: May cause virilization in female fetuses.
- Breastfeeding: It is not known how Mesterolone is excreted in breast milk. In accordance with the adverse reactions that may occur in infants, it is necessary to decide whether to stop breastfeeding or stop taking the drug.
- Pediatrics: the use of the drug can have serious consequences, the benefits of them should be assessed before starting therapy.

Interaction with other medicinal products
Not known

Special instructions
During treatment, regular examinations of the prostate gland are recommended in order to exclude prostate cancer.
If in some cases there are frequent or very prolonged erections, then you should reduce the dose or stop treatment in order to avoid complications as a result of prolonged erection.
In rare cases, against the background of the use of substances with hormonal activity, including those included in the drug meterolone, benign, and even less often - malignant tumors in the liver were observed, which in some cases can lead to life - threatening intra - abdominal bleeding. In case of severe pain in the abdomen, enlarged liver or signs of intra-abdominal bleeding, the possibility of a liver tumor should be considered in differential diagnosis. Patients with hereditary disorders such as fructose intolerance, Lapp-lactase deficiency or glucose-galactose malabsorption should take into account the amount of lactose contained in mesterolone.

Pregnancy and elbowing
This drug should not be used during pregnancy and lactation.
During pregnancy, the drug can cause virilization in female fetuses.
During breastfeeding, it is not known how Mesterolone is excreted in breast milk. In accordance with the adverse reactions that may occur in infants, it is necessary to decide whether to stop breastfeeding or stop taking the drug.

Influence on the ability to drive vehicles and work with mechanisms
Does not affect

Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 °C, out of the reach of children.

Shelf life
3 years. Do not use after the expiration date printed on the package.

Vacation conditions
On prescription.

Packaging
Mesterolone 50 mg Tablets. There are 25 tablets in a blister. 2 blisters are packed in a cardboard box together with an enclosed leaflet.