Expiration date: 06/2026
Release form and composition:
Gel for external use 1% is a transparent or slightly opalescent, colourless, with a smell of alcohol.
1 gram contains: testosterone 10 mg
1 pack contains: testosterone 50 mg
Excipients: methyl ethyl ketone, ethanol 96%, carbopol 980, sodium hydroxide, purified water.
5 g - bags, disposable (30) - packs of cardboard.
Pharmacological action:
Androgenic drug. Endogenous androgens (mainly testosterone) secreted by the testicles, and their main metabolite dihydrotestosterone responsible for the development of external and internal genital organs and secondary sexual characteristics (stimulating hair growth, deepening of the voice, development of libido). Have a General effect on protein anabolism, development of skeletal muscles and the distribution of subcutaneous fat, reduction of excretion of nitrogen, sodium, potassium, chlorides, phosphates and water. Testosterone doesn't cause testicular development: it reduces the pituitary secretion of gonadotropins.
Effects of testosterone on some target organs develop after peripheral conversion of testosterone to estradiol, which then binds to estrogen receptors in cell nuclei of target organs (such as pituitary, adipose tissue, brain, bone and testicular Leydig cells).
Pharmacokinetics:
Suction
The degree of absorption of testosterone through the skin varies from about 9% to 14% of the applied dose.
Distribution
After the intake of testosterone enters the systemic circulation at relatively constant concentrations during the 24-hour cycle. Testosterone concentrations in serum increased from the first hour after treatment, reaching a constant value from the second day of treatment. Daily fluctuations in concentrations of testosterone have the same amplitude, as observed in circadian rhythms changes in the content of endogenous testosterone.
For external routes of administration of the drug, thus, it is possible to avoid peaks in the distribution in the blood, occurs when the injection method of application. In contrast to oral androgen therapy, external application of the drug does not cause high concentrations of steroids in the liver is higher than the physiological norms. The use of 5 g of Androgel causes a secondary increase in the concentration of testosterone in plasma is approximately 2.5 ng/ml (8.7 nmol/l).
Metabolism
The major active metabolites of testosterone are dihydrotestosterone and estradiol.
Excretion
After cessation of treatment the concentration of testosterone begins to decline after about 24 h after the last application. The concentration returns to the original level after approximately 72-96 h after last dose. The drug is excreted mainly in the urine and faeces in form of conjugated metabolites of testosterone.
Indications:
— replacement therapy in deficiency of testosterone.
Dosing regimen:
The recommended daily dose is 5 g gel (i.e. 50 mg of testosterone). The drug is used 1 times/day around the same time of day, preferably in the morning. The daily dose may be adjusted depending on clinical and laboratory parameters, but should not exceed 10 g of gel. The correction mode should be carried out stepwise by 2.5 g of gel/day.
For the correction dose you need to determine the concentration of testosterone in the serum in the morning, to the drug, with the third day after the start of treatment (within one week). The dose can be reduced if the testosterone in plasma is increased, or Vice versa increase if the concentration of a low testosterone.
Rules for the use of the drug
The gel is applied to clean, dry, intact skin of the shoulders, arms and/or abdomen. It is impossible to apply the gel to the genital area, because the high content of ethyl alcohol in the drug can cause local irritation.
After opening the bag should be immediately applied to the skin all its contents, and spread a thin layer. Do not have to RUB it into the skin. You can give it dry for at least 3-5 minutes before dressing. After applying should wash their hands with soap and water.
Side effects:
Local reactions: the most frequently - irritation and dryness of the skin at the site of application of the drug, especially in its frequent application.
From the endocrine and reproductive system: in rare cases - changes of the prostate gland, gynecomastia (mostly in patients receiving treatment for hypogonadism), mastodinia.
CNS and peripheral nervous system: in rare cases - dizziness, headache, amnesia, mood changes, paresthesia, hyperesthesia.
From cardiovascular system: in isolated cases - increase in blood pressure.
From the digestive system: in rare cases - diarrhea.
Dermatological reactions: erythema, acne in rare cases - alopecia.
Other: changes in results of laboratory tests (polycythaemia, reducing the level of lipids).
In appointing the drug in high doses may develop the following clinical signs: irritability, nervousness, increased body weight, prolonged or frequent erections. State data require dose adjustment.
Contraindications:
— carcinoma of the breast or suspected of being present
— prostate cancer or a suspicion of its presence
— hypersensitivity to testosterone or other components of the drug.
Experience with the use of Androgel in women and children.
With caution should designate product in malignant tumors (due to risk of hypercalciuria and hypercalcemia), and severe cardiac, hepatic or renal failure, with ischemic heart disease, arterial hypertension, epilepsy, migraine.
Pregnancy and lactation:
The drug is not used in women.
In case of pregnancy, a sexual partner of the patient must be attentive to safety precautions. Pregnant women should avoid any contact with skin. In case of contact with the drug, the woman must quickly wash exposed place with soap and water.
Special instructions:
The androgel should be applied only in case of insufficiency of testosterone accompanied by clinical symptoms such as regression of secondary sexual characteristics, change in body composition, asthenia, reduced libido, erectile dysfunction. Before treatment to rule out other possible causes underlying the above symptoms.
Currently, there are no clear rules about age dependent quantities of testosterone. However, you should take into account the fact that physiological serum levels of testosterone decrease with increasing age.
Due to variability in laboratory values, to determine the concentration of testosterone should be carried out in the same laboratory.
The androgel is used to treat male infertility, or erectile dysfunction, the cause of which is not connected with the deficiency of testosterone.
Before prescribing testosterone, all patients should undergo a medical examination to exclude the presence of prostate cancer because androgens may accelerate the progression of subclinical prostatic cancer and benign prostatic hyperplasia. Should be careful and regular monitoring of the prostate gland (digital rectal examination, determination of prostate specific antigen (PSA) in serum), and breast, at least once a year every year, and older patients and patients from the risk group (with clinical or familial factors) twice a year.
The androgel should be used with caution in patients with malignancies because of the risk of hypercalcemia (and associated hypercalciuria) due to bone metastases. In these patients it is recommended to monitor the concentration of calcium in serum.
In patients suffering from severe cardiac, hepatic or renal insufficiency, treatment with Androgel may cause complications characterized by edema with congestive heart failure or without. In this case, the treatment should be terminated immediately. In addition, you may need diuretic therapy.
The androgel should be used with caution in patients with coronary artery disease.
Testosterone can cause increased blood pressure, and so the Androgel should be used with caution in patients with hypertension.
In patients receiving 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 (to detect polycythemia) and liver function tests.
The androgel caution should be used in patients with epilepsy and migraine as these conditions may be exacerbated.
Published data on the increased risk of developing sleep apnea in patients with hypogonadism treated esters of testosterone, especially those who had risk factors such as obesity and chronic respiratory diseases.
In patients receiving androgens, upon reaching normal concentrations of testosterone in plasma can be observed an increase in insulin sensitivity.
Certain clinical signs: irritability, nervousness, weight gain, prolonged or frequent erections may indicate excessive androgen exposure requiring dosage adjustment.
If the patient develops severe local reaction, the treatment should be reviewed and, if necessary, terminated.
If you are using Androgel athletes must take into account the fact that the drug contains testosterone, which can give a positive reaction in antidoping tests.
The potential transfer of testosterone
In the appointment of Androgel you need to inform the patient about the security measures. To guarantee the safety of the sexual partner, the patient should be advised to observe the interval between application of Androgel intercourse, or wear a t-shirt covering the application of the gel, during the period of contact, or to shower before sexual intercourse.
Preferably to observe an interval of at least 6 hours between gel application and bathing or showering. However, a random shower in the period from 1 to 6 hours after applying the gel has no significant effect on treatment.
Patients are advised to observe the following precautions:
— wash hands with soap and water after applying the gel
— close the area of application of the gel with clothing after the gel dries
— shower before any situation in which contact with another person is inevitable.
Persons who do not use Androgel in case of contact with the area of application of the gel, not pre-washed with water, must be washed with soap and water the skin area, which may be testosterone. You must inform your doctor about the appearance and development of such signs of hyperandrogenism like acne or a change in the normal hair growth.
Patients applying Androgel, in contact with children are recommended to wear a t-shirt covering the application of the gel to avoid the risk of skin contact of children with the drug.
The androgel should not be prescribed to patients who are not able to comply with safety instructions (e.g. severe alcoholism, substance abuse, severe mental disorders).
Effects on ability to drive vehicles and management mechanisms
The drug has no effect on the ability to perform work requiring increased attention and psychomotor speed reactions.
Overdose:
No cases of overdose with the use of Androgel is not fixed. Described only one case of an overdose after application of the administered testosterone injection. It was a stroke in a patient with a high concentration of testosterone in the plasma of 114 ng/ml (395 nmol/l). However, it is unlikely that such concentrations of testosterone in plasma can be achieved when applying the drug to the skin.
Drug interactions:
While the use of Androgel and anticoagulants may increase the action of the latter by modification of the synthesis of hepatic coagulation factors and competitive inhibition of binding to plasma proteins. Patients receiving oral anticoagulants application of Androgel, it is recommended to monitor the prothrombin time, most often at the beginning and/or end of course of treatment with androgens.
The combined use of Androgel with ACTH or corticosteroids may increase the risk of swelling. Caution should be exercised when coadministration of these drugs, especially in patients with heart disease, kidney or liver.
Androgens may decrease levels of thyroxine binding globulin, leading to lower serum concentrations of T4 and increased sensitivity to T3 and T4. Free levels of thyroid hormones, however, remain unchanged, and no clinical manifestations of hypothyroidism.
Terms and conditions of storage:
List B. the Drug should be stored out of reach of children at temperature not above 25°C . Shelf life - 3 years.
