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What is mesterolone?

Mesterolone is a drug indicated for the treatment of hypogonadism. It is indicated for patients with androgen deficiency as mesterolone replaces androgen for male with hypogonadism. Patients are recommended to make all biochemical and clinical laboratory tests in order to depict the deficiency of androgen. Mesterolone is rapidly absorbed after oral administration and is rapidly metabolized. Generally, mesterolone does not suppress gonadotrophins or endogenous testosterone production.


·Avoid mesterolone if you have a known hypersensitivity to the drug or to any of its ingredients. If the allergic reaction to the product develops during therapy with it, report about it immediately and get prompt treatment.

·It is contraindicated the use of mesterolone in patients with carcinoma of the prostate;

·Patients with previous or existing liver tumours or breast cancer are contraindicated this product;

·Avoid the use of mesterolone if you have hypercalcemia;

Precautions with mesterolone

Prior to the initiation of therapy with the drug, consult a doctor and establish the diagnosis of hypogonadism due to the fact that androgens are not suitable for enhancing muscular development in healthy individuals. Therefore, patients require a full endocrinological assessment in order to evaluate the general health condition of the patient. The full examination means evaluation of history of the patient, expert interpretation of serial measurements of serum testosterone and other additional tests in order to identify the underlying disorders.

·Patients with prostate disease are not recommended the use of mesterolone. Exclude the therapy with mesterolone if you have prostate disease. Make the necessary examinations and discuss with a doctor all possible side effects from therapy with this drug.

·Patients with hepatic impairment should exercise caution to the use of mesterolone. It is recommended the monitoring of hepatic function on a regular basis. Exercise caution to the administered doses of mesterolone.

·Patients with cardiovascular disorders or renal impairment, epilepsy, migraine or hypertension are susceptible to aggravated conditions while on therapy with mesterolone.

·It is not recommended to receive higher doses of mesterolone than prescribed over a prolonged period of time. The side effect patients may occur if prolonging the therapy and taking higher doses of mesterolone is peliosis hepatis. If the patients experience upper abdominal pain, it is necessary to report about it immediately and get the respective treatment.

·Patients may experience increased libido. For any symptoms, consult a doctor.

·Therapy with mesterolone may precipitate the urinary obstruction.

·It is not recommended the use of mesterolone by patients under 18 years of age due to premature closure of the epiphyses and stop of linear growth.

·While on therapy with mesterolone, diabetes mellitus, sleep apnoea or androgen-sensitive polycythaemia may be exacerbated. Make regular checks at a physician and take all protective measures in order to avoid such adverse events.

·Patients with a history of porphyria are not recommended to use mesterolone due to safety issues.

·There is no clinical evidence of the use of mesterolone in pregnant women. It is not recommended for use in pregnant women due to the fact that it is a drug indicated for male patients only.

·There has also not been investigated the genotoxic potential of mesterolone.


Dosage and administration

Mesterolone is a drug available for oral administration and comes in form of tablets. As already mentioned, patients need to get the diagnosis of hypogonadism prior to commencement of therapy with mesterolone. It is recommended to take the tablets exactly as prescribed. It is indicated to swallow the tablets whole with plenty of water or other liquid. For the treatment of hypogonadism it is indicated an initial dose of 1-2 tablets three times a day. In order to completely treat the symptoms, the therapy with mesterolone may take several months. Patients with hepatic impairment are recommended a dose of 1 tablet twice a day in order to not precipitate the existing symptoms. For other information related to the administration of mesterolone, consult a doctor and read carefully the package insert.

Potential interactions with other drugs

Prior to commencement of therapy with mesterolone, prevent your doctor about all medicines you are currently taking, including prescription, non-prescription ones, herbal products, vitamins, minerals and natural supplements. Generally, medicines with increased clearance of sex hormones in interaction with mesterolone may decrease its therapeutic efficacy. Therefore, it is not indicated the concomitant administration of mesterolone with phenytoin and phenobarbital.

Also, it is not recommended the concurrent administration of mesterolone with medicines that may be affected by the activity of androgens and their concomitant administration may lead to increased toxicity. Through these medicines, are the following:




·Anticoagulants such as warfarin.


Possible adverse effects with mesterolone

Like most of the medicines, mesterolone may cause side effects when used in prescribed doses. Generally, the side effects with mesterolone are more rare and mild to moderate in severity. The following adverse reactions with mesterolone have been reported while on therapy with it:

·Frequent or persistent erections. If such adverse event is reported, there is need of dose reduction or discontinuation of therapy with this drug.


·Fluid retention;

·Altered lipids and hematological parameters;

·Abnormal liver function tests;

·Impaired glucose tolerance;

·Prostate hyperplasia;



·Increased libido;


·Precocious sexual development;



·Premature epiphyseal closure;

·Psychiatric disturbances including mania, depression, emotional lability, aggression, hypomania;

·Neoplasms including liver and prostate.


Do not get alarmed by the long list of possible adverse events with mesterolone. Some patients may not experience any side effects. However, if any symptoms and adverse reactions occur while on therapy with this drug, report about it immediately and get prompt treatment. If the side effects are persistent and bothersome, decrease the doses or discontinue completely with the drug.


Overdosage with mesterolone

There have not been reported cases of acute overdosage with mesterolone. After overdosage with mesterolone, patients may experience the following adverse events: neoplasms, liver abnormalities, atherogenic blood lipid profile, reduced glucose tolerance, increased risk of cardiovascular disease, hypogonadal states, virilization, psychiatric disturbances, gastrointestinal bleeding and tendon damage. If any of the enumerated symptoms occur after accidental ingestion of great quantities of mesterolone, go to the nearest hospital and seek immediate medical care and assistance. Discontinue with the drug and take all appropriate measures in order to eliminate the drug from the body.


If you miss a dose of mesterolone

If you forgot to take a dose of mesterolone, do not worry; take it as soon as you remember. If it is already too late to take the missed dose, leave it and continue your usual schedule. Remember; do not take greater doses of mesterolone to make up for the skipped ones. However, try to not miss more than two doses in a row. If you have any questions related to the missed dose of mesterolone, ask a pharmacist or contact your physician.



It is recommended to store mesterolone in a clean and dry place at the room temperature below 30 degrees C. Keep the medicine in its original packaging out of the reach and sight of children. Do not leave the medicines in the bathroom or near sink in order to avoid moisture. Also, try to keep mesterolone away from direct sunlight and heat. If you have any questions related to the disposal ways of mesterolone, ask a pharmacist or a physician. Do not flush expired medicines down the toilet.

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