Instruction for use: Androgel

Active substance:

Testosterone [mixture of esters]

ATX code

G03BA03 Testosterone

Pharmacological group

Androgens, antiandrogens

Nosological classification (ICD-10)

E29 Testicular dysfunction

Hypofunction of gonads in men, Androgenic dysfunction, Dysfunction of the sex glands, Dysfunction of gonads in men, Underdevelopment of the genitals in men, Primary hypogonadism in men

Composition

Gel for external use 1 pack.

Testosterone 25 mg\50 mg

Auxiliary substances: isopropyl myristate; Ethanol 96%; Carbopol 980; Sodium hydroxide; purified water

Description of dosage form

Transparent or slightly opalescent colorless gel with the smell of alcohol.

pharmachologic effect

The pharmacological action is androgenic.

To the beginning ^

Pharmacodynamics

Endogenous androgens, mainly testosterone, secreted by the testicles, and their main metabolite, dihydrotestosterone, are responsible for the development of external and internal genital organs and the preservation of secondary sexual characteristics (stimulation of hair growth, coarsening of the voice, development of the libido). They affect the anabolism of proteins; Development of skeletal muscles and distribution of subcutaneous fat; Reduce urinary excretion of nitrogen, sodium, potassium, chlorides, phosphates and water. Testosterone does not cause development of testicles: it reduces the pituitary secretion of gonadotropins.

The effects of testosterone on certain target organs are manifested after the peripheral conversion of testosterone to estradiol, which then binds to estrogen receptors in the target cell nuclei (such as the pituitary gland, adipose tissue, brain, bones, etc.).

Pharmacokinetics

The degree of absorption of testosterone through the skin varies between 9-14% of the applied dose.

After absorption through the skin, testosterone enters the systemic circulation at relatively constant concentrations for 24 hours.

Concentrations of testosterone in the serum increase from the 1 st h after application of the drug, reaching a constant value from the 2nd day of treatment. Daily fluctuations in testosterone concentrations have the same amplitude as the changes in endogenous testosterone content observed in circadian rhythms. With the external route of administration of the preparation, there are no supraphysiological peaks of testosterone concentration in the blood arising from the injection method of application (Figure 1).

In contrast to oral androgen therapy, external use of the drug does not cause an increase in the concentrations of steroids in the liver above physiological norms. The use of Androgel® in a dose of 5 g causes an average increase in plasma testosterone concentration of approximately 2.5 ng / ml (8.7 nmol / L).

After discontinuation of treatment, testosterone concentration begins to decrease approximately 24 hours after the last dose. Concentration returns to the baseline level approximately 72-96 hours after the last dose.

The main active metabolites of testosterone are dihydrotestosterone and estradiol.

Androgel® is excreted mainly with urine and feces in the form of conjugated testosterone metabolites.

Indication

Replacement therapy with testosterone deficiency.

Contraindications

Hypersensitivity to testosterone or other components of the drug;

Carcinoma of the breast or prostate cancer or suspected of their presence.

The experience of using Androgel® in women and children is absent.

With caution: malignant neoplasms (due to the danger of hypercalcemia and hypercalciuria); Severe cardiac, hepatic or renal insufficiency; Ischemic heart disease, hypertension; Epilepsy, migraine.

pregnancy and lactation

Pregnant women should avoid any contact with the drug because of its possible virilizing effect on the fetus. In case of contact with the preparation, it is necessary to wash the place of contact with soap as soon as possible.

Side effects

The most frequent undesirable effects when applied at the recommended dose (5 grams of gel per day) were skin reactions: reaction at the site of application, erythema, acne, dry skin.

During the clinical trials of Androgel®, the following undesirable effects were noted (> 1/100, <1/10).

From the blood and lymphatic system: changes in the results of laboratory tests (polycythemia, changes in lipid levels).

From the genitourinary system: changes in the prostate gland, gynecomastia, mastodynia.

From the nervous system: dizziness, paresthesia, amnesia, hyperesthesia, mood changes.

From the CCC: an increase in blood pressure.

From the digestive tract: diarrhea.

From the skin and its appendages: alopecia, hives.

General disorders: headache.

The drug contains alcohol, so when it is often applied to the skin may appear irritation and dryness.

Interaction

Androgel® should be administered with caution to oral anticoagulants; It is possible to enhance the effect of oral anticoagulants by modifying the synthesis of the hepatic coagulation factor and competitive inhibition of binding to plasma proteins. It is recommended to monitor the PV. Patients receiving oral anticoagulants require frequent monitoring, especially at the beginning and / or end of the course of treatment with androgens.

Co-administration of testosterone and ACTH or corticosteroids may increase the risk of edema. These medications should be administered together cautiously, especially to patients suffering from heart, kidney or liver disease.

Impact on laboratory tests: androgens may reduce levels of thyroxine-binding globulin, leading to a decrease in serum T4 concentrations and an increase in sensitivity to T3 and T4. Levels of free thyroid hormones, however, remain unchanged, and there are no clinical manifestations of hypothyroidism.

Dosing and Administration

Outer, at the same time, preferably in the morning. The gel is applied to clean, dry, undamaged skin of the shoulders, shoulder and / or abdomen. After opening the sachet, it is necessary to immediately apply all of its contents to the skin and distribute it in a thin layer. It is not necessary to rub it into the skin. Allow the gel to dry for at least 3-5 minutes before dressing. Wash hands with soap after application.

The recommended dose is 5 g of gel (i.e., 50 mg of testosterone), applied once a day at about the same time, preferably in the morning. The individual daily dose can be adjusted by the doctor depending on the clinical and laboratory parameters in patients, but should not exceed 10 g of gel per day. Correction of the dosing regimen should be carried out stepwise, 2.5 g of gel per day.

Do not apply gel to the genital area, because A high content of ethyl alcohol in the preparation can cause local irritation.

The constant concentration of testosterone in the plasma is reached approximately on the 2nd day of treatment with Androgel®. To adjust the dose of testosterone, it is necessary to determine the concentration of testosterone in the serum in the morning, before the drug, from the 3rd day after the start of treatment (within 1 week). Dosage can be reduced if the testosterone content in the plasma is increased. If the concentrations are low, the dose can be increased, but not more than 10 g of gel per day.

Overdose

Cases of overdose with the use of the drug Androgel ® is not fixed.

Only one case of an overdose after the injection of testosterone injected: a stroke in a patient with a high plasma testosterone concentration of 114 ng / ml (395 nmol / L) was described.

However, it is unlikely that such concentrations of testosterone in the plasma can be achieved by applying the drug to the skin.

special instructions

Androgel® should be used only when testosterone deficiency is accompanied by such clinical manifestations as underdevelopment or regression of secondary sexual characteristics, changes in body structure, violation of carbohydrate and lipid metabolism, obesity, asthenia, sexual dysfunction (decreased libido, erectile dysfunction, etc.) , Decreased bone mineral density, mood swings, depression, hot flashes, etc.

Before starting treatment, other possible causes underlying the above symptoms should be excluded. At present, there are no clear age standards for testosterone values. However, it should be taken into account that the physiological levels of serum testosterone begin to decline from 30-40 years, and the level of globulin binding sex steroids increases. Accordingly, this leads to a decrease in the level of biologically active testosterone.

Due to the variability of laboratory values, the determination of testosterone concentration should be carried out in the same laboratory.

Androgel® is not used to treat male infertility or erectile dysfunction, the cause of which is not related to testosterone deficiency.

Before the appointment of testosterone, all patients must undergo a checkup to rule out the risk of prostate cancer, Androgens can accelerate the progression of subclinical prostate cancer and BPH. Careful and regular monitoring of the prostate gland (digital rectal examination, determination of serum PSA) and mammary glands should be carried out at least once a year, and in elderly patients and at-risk patients (with clinical or family factors) 2 times per year.

Testosterone preparations should be used with caution in patients with malignant neoplasms because of the risk of hypercalcemia (and concomitant hypercalciuria) due to bone metastases. In these patients, it is recommended that the concentration of calcium in the serum be monitored.

In patients with severe cardiac, hepatic or renal insufficiency, treatment with testosterone preparations can cause complications characterized by edema with or without congestive heart failure. In this case, treatment should be stopped immediately. In addition, diuretic therapy may be required.

In patients taking androgens for a long period, in addition to laboratory measurements of testosterone concentrations, it is periodically necessary to check the following laboratory parameters: hemoglobin, hematocrit (for polycythemia detection), functional liver samples and lipid profile.

Data have been published on the increased risk of sleep apnea in patients with hypogonadism receiving treatment with esters of testosterone, especially in those who have risk factors such as obesity and chronic respiratory diseases.

In patients with diabetes, receiving androgens, when the normal concentration of testosterone in the blood plasma can be increased sensitivity to insulin.

Some clinical symptoms - irritability, nervousness, weight gain, prolonged or frequent erections - may indicate excessive androgen exposure, requiring dosage adjustment.

If a patient develops a severe local reaction, treatment should be reviewed and, if necessary, discontinued.

When using Androgel® in athletes, it is necessary to take into account the fact that this drug contains an active substance (testosterone), which can give a positive reaction in the anti-doping tests.

Potential transfer of testosterone

When prescribing Androgel®, the patient should be informed of the safety measures. To ensure the safety of the partner, the patient needs, for example, to advise to have sex before using the drug or to keep the interval between using Androgel® and sexual intercourse. If the sexual intercourse is performed within 6 hours after applying Androgel®, it is recommended to wear a T-shirt covering the place of application of the gel during the contact period or take a shower before the sexual intercourse.

It is preferable to observe an interval of not less than 6 hours between applying the gel and taking a bath or shower. However, occasional showering from 1 to 6 hours after the application of the gel does not have a significant effect on the treatment. The following precautions are recommended.

For the patient:

- Wash hands with soap after applying the gel;

- Close the area of application of the gel with clothing after the gel has dried;

- Take a shower before before contacting a partner.

For persons not using Androgel®:

- in case of contact with the area of application of the gel (previously not washed with water), it is necessary to rinse as soon as possible with water and soap the skin area on which testosterone could be ingested;

- It is necessary to inform the doctor about the appearance and development of such signs of hyperandrogenization, as acne or a change in normal hair growth.

In the case of a partner's pregnancy, the patient needs to be more careful about the observance of precautions. Pregnant women should avoid any contact of the drug with the skin. In case of contact with the drug, a woman should wash the contact area with soap and water as soon as possible.

When contacting children, it is recommended to wear a T-shirt covering the place of application of the gel in order to avoid the risk of skin contact of children with the drug.

Androgel® should not be given to patients who can not follow safety instructions (for example, patients with severe chronic alcoholism, substance abuse, severe mental disorders).

Impact on the ability to drive and other mechanisms. At present, there is no evidence of the effect of Androgel® on the ability to drive and control cars and mechanisms.

Form of issue

Gel for external use, 1%. For 2.5 or 5 grams of gel in single-use bags of PE and laminated aluminum foil. For 10 or 30 bags are placed in a cardboard box.

Terms of leave from pharmacies

On prescription.

storage Conditions

At a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiry date printed on the package.