100 g of gel contains:
- Active ingredient – Testosterone – 1.62 g
- Excipients: isopropyl myristate, ethanol 96%, carbomer 980, 0.1 M sodium hydroxide solution, purified water.
The degree of absorption of testosterone when Androgel 16.2 mg is applied to the skin varies from 1% to 8.5%.
After absorption through the skin, testosterone enters the systemic circulation at relatively constant concentrations over a 24-hour cycle.
Serum testosterone concentrations increase from the first hour after the use of the drug, reaching a constant value from the second day of treatment. Daily fluctuations in the concentration of testosterone have the same amplitude as the changes in the level of endogenous testosterone observed in circadian rhythms. Thus, transdermal administration helps to avoid the peaks in blood testosterone concentrations that occur after injections. Unlike oral androgens, this method of administration does not cause an increase in the concentration of steroids in the liver above physiological values.
The use of the drug Androgel 16, 2 mg / g at a dose of 5 g, causes an average
an increase in plasma testosterone levels of approximately 2.3 ng / ml (8.0 nmol / l).
After stopping treatment, testosterone levels begin to decline.
approximately 2 hours after the last application. The concentration returns to baseline approximately 72-96 hours after the last dose.
The main active metabolites of testosterone are
dihydrotestosterone and estradiol.
Testosterone is primarily excreted in the urine as conjugated
metabolites, a small amount is excreted unchanged in the feces.
Endogenous androgens, mainly testosterone, secreted by the testicles and their main metabolite, dihydrotestosterone (DHT), are responsible for:
– for the development of external and internal genital organs
– preservation of secondary sexual characteristics (growth of hair on the body, libido development)
– androgens also affect protein anabolism, development skeletal muscle and the distribution of fat in the body, reducing urinary excretion of nitrogen, sodium, potassium, chlorides, phosphorus and water.
Testosterone reduces the secretion of gonadotropins by the pituitary gland. The effects of testosterone on several target organs appear after the peripheral conversion of testosterone to estradiol, which then binds to nuclear estrogen receptors in target organ cells (eg, pituitary gland, adipose tissue, brain, bone, and Leydig cells in the testes).
Indications for use
Testosterone replacement therapy for male hypogonadism when testosterone deficiency is confirmed by clinical symptoms and biochemical tests.
Dosage and administration
Adults and older men
The recommended dose is 2.5g, which corresponds to two pumps (or 40.5mg of testosterone) once a day, at about the same time, preferably in the morning. The daily dose is adjusted by the physician depending on the clinical or biological response of the individual patient, but should not exceed 5 g of gel (81 mg of testosterone) per day. Dose adjustment is carried out by successive clicks on the dispenser.
The dose is determined based on the measurement of testosterone levels in the blood, which should be carried out in the morning before using the drug. Steady-state plasma testosterone concentration is reached from about the 2nd day of treatment with Androgel. Dose adjustments are made based on testosterone levels measured after steady state, in the morning before application. The level of testosterone in the blood must be periodically assessed. The dosage may be reduced if the testosterone level exceeds the required level. If the concentration of testosterone in the blood plasma is low, the dose can be gradually increased, but should not exceed 81 mg of testosterone (four clicks on the dispenser).
|Number of clicks||Gel Amount (g)||Amount of testosterone
applied to the skin (mg)
Treatment should be discontinued if, at a daily dose of 20.25 mg testosterone (1.25 g of gel or 1 pump of the dispenser), the testosterone level in the blood is constantly above the normal range, and also if the normal testosterone level is not achieved at the highest possible level. a dose of 81 mg (5 g of gel, or 4 clicks on the dispenser).
The gel is applied by the patient to clean, dry, intact skin of the shoulders and upper arms.
The gel is applied in a thin layer on the surface of the skin and does not require rubbing.
Let the gel dry for 3-5 minutes before dressing. Wash your hands with soap and water after applying the gel.
In situations where, after applying the drug, contact with the skin of another person is expected, it is necessary to wash the places where the gel was applied in advance with soap and water.
Do not apply the gel to the genital area, as the high content of ethyl alcohol in the preparation may cause local irritation.
Before you receive the first full dose, you must pump the dispenser. Holding the vial vertically, slowly and completely press the dispenser 3 times, then remove the gel that has come out of the dispenser. Pumping the dispenser is required only before the first use.
After pumping, press the dispenser to ensure that 1.25 g of gel enters the palm of your hand; apply it on the skin of the shoulders and shoulder girdle and dress after the gel dries.
Androgel is not used in children and adolescents under 18 years of age. The safety and efficacy of the drug have not been established. No data available.
The frequency of side effects is determined according to the following criteria: very often (≥ 1/10), often (≥ 1/100 to < 1/10), infrequently (≥ 1/1000 to < 1/100), rarely ( ≥ 1/10000 to < 1/1000), very rare (< 1/10000)
Adverse reactions in clinical studies
MedRA organ system class
> 1/100 to <1/10
1/1000 to <1/100
Mood swings, emotional disturbances, anger, aggression, irritability, insomnia, unusual dreams, increased libido
Arterial hypertension, hot flashes, phlebitis
Diarrhea, bloating, mouth pain
Skin and subcutaneous tissue disorders
Acne, alopecia, dry skin, skin lesions, contact dermatitis, discoloration of the hair, rash, hypersensitivity, itching at the site of application
Genital and breast disorders
Gynecomastia, nipple pain, testicular pain, increased erection
General disorders and disorders at the injection site
Edema with the formation of yellowish crusts at the site of application
Impact on laboratory results
Elevated prostate specific antigen, increased hematocrit and hemoglobin
Post-marketing adverse reactions
MedRA organ system class
Blood and lymphatic system disorders
Insomnia, depression, anxiety, aggression
Nervous System Disorders
Headache, dizziness, paresthesia
Vasodilation (flushing), deep vein thrombosis
Skin and subcutaneous tissue disorders
Application site reactions, acne, alopecia, sweating, hypertrichosis, weight gain
Musculoskeletal and connective tissue disorders
Renal and urinary tract disorders
Difficulties with urination
Violations of the genital organs of the breast
Gynecomastia, testicular disorders, prostate enlargement, oligospermia, benign prostatic hyperplasia
General disorders and disorders at the injection site
Asthenia, edema, malaise
Impact on laboratory results
Increased levels of prostate-specific antigen, hematocrit and hemoglobin
- Breast cancer or suspected of having it
- Prostate cancer or suspicion of its presence
- Hypersensitivity to testosterone or other components of the drug
- Does not apply to females
With the simultaneous use of Androgel and indirect anticoagulants, it is possible to enhance the effect of the latter by modifying the synthesis of the hepatic coagulation factor and competitive inhibition of plasma protein binding. Patients receiving oral anticoagulants while using Androgel are advised to control prothrombin time, especially often at the beginning and / or at the end of androgen treatment.
The combined use of Androgel with ACTH or corticosteroids may increase the risk of edema. Caution should be exercised when these drugs are used together, especially in patients with heart, kidney or liver disease.
Androgens can decrease thyroxine-binding globulin levels, leading to a decrease in serum T4 concentrations and an increase in sensitivity to T3 and T4. The levels of free thyroid hormones, however, remain unchanged, and clinical manifestations of hypothyroidism are absent.
Changes have been reported with androgens
insulin sensitivity, glucose tolerance, glucose levels, blood sugar and hemoglobin levels. Patients with diabetes may need to reduce the dose of antidiabetic drugs.
The use of sunscreen or lotion does not reduce
the effectiveness of the drug.
Washing off the gel from the skin surface 2 hours after application is not
has a significant effect on the level of testosterone in the blood.
Androgel should only be used in cases of confirmed hypogonadism (hypo- and hypergonadotropic). Any other underlying causes of clinical symptoms should be excluded prior to treatment. Testosterone deficiency should clearly correlate with clinical manifestations, such as underdevelopment or regression of secondary sexual characteristics, changes in body structure, asthenia, decreased libido, erectile dysfunction, etc. and confirmed by 2 independent measurements of plasma testosterone levels.
Currently, there is no consensus regarding clear age norms for testosterone levels. However, it should be taken into account that physiological levels of serum testosterone decrease in men with age.
Due to the variability in laboratory values, the determination of testosterone concentration should be carried out in the same laboratory.
Androgel is not indicated for the treatment of male infertility or erectile dysfunction, the cause of which is not related to testosterone deficiency.
Before starting treatment, all patients should undergo a thorough examination to exclude the presence of prostate cancer. Careful and regular monitoring of the condition of the prostate gland (digital rectal examination, determination of prostate-specific antigen (PSA) in serum) and mammary glands should be carried out at least once a year in all patients taking testosterone, and in elderly patients and patients at risk ( with clinical or family factors) – 2 times a year.
Androgens may accelerate the progression of subclinical prostate cancer or benign prostatic hyperplasia.
Androgel should be used with caution in patients with malignant neoplasms due to the risk of hypercalcemia (and concomitant hypercalciuria) due to bone metastases. In these patients, it is recommended to monitor the concentration of calcium in the serum.
In patients suffering from severe cardiac, hepatic or renal insufficiency, coronary heart disease, testosterone treatment can cause severe 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 with ischemic heart disease, Androgel should be used with caution.
Testosterone can cause an increase in blood pressure, so Androgel should be used with caution in men with hypertension.
Measurement of testosterone levels in the blood should be carried out before starting treatment and at regular intervals during treatment. The doctor must control the dose of the drug in each individual patient to ensure that testosterone levels are maintained within normal limits.
In patients taking androgens for a long period,
in addition to laboratory measurements of testosterone concentration, the following laboratory parameters should be checked periodically: hemoglobin, hematocrit (to detect polycythemia) and liver function tests and lipid profile.
Available Efficacy and Safety Data
Androgel in patients over 65 years of age are limited. There is currently no consensus regarding clear age norms for testosterone levels. However, it should be taken into account that physiological levels of serum testosterone decrease in men with age.
Androgel should be taken with caution in patients with epilepsy
and migraine, as their condition may worsen during testosterone treatment.
There is evidence in the scientific literature of an increased risk of developing
sleep apnea in hypogonadal patients treated with testosterone esters; patients with obesity and chronic respiratory diseases are particularly at risk.
In patients with diabetes mellitus receiving androgens, when normal plasma testosterone concentrations are reached, an increase in insulin sensitivity may be observed.
Some clinical symptoms: irritability, nervousness, weight gain, prolonged or frequent erections may indicate excessive androgen exposure requiring dose adjustment. Some clinical symptoms: irritability, nervousness, weight gain, prolonged or frequent erections may indicate excessive androgen exposure requiring dose adjustment.
If a patient develops a severe
local reaction, treatment should be reviewed and, if necessary, discontinued.
High doses of androgens may cause suppression of spermatogenesis
through negative feedback through pituitary follicle-stimulating hormone (FSH), which could potentially lead to adverse effects on sperm parameters such as sperm count.
Hypogonadal patients treated with androgens may occasionally develop gynecomastia.
Androgel should not be used in women due to possible masculinization.
Athletes should be informed that the drug contains testosterone as an active substance, which can give a positive result in doping control.
Risk of accidental testosterone transfer
In the absence of precautions, the transfer of testosterone to another person after the use of the drug can occur at the time of close contact of the skin with the area of application of the gel, which leads to an increase in testosterone levels, and, in case of repeated contact (accidental androgenization), to the possible occurrence of side effects (increase in height facial and/or body hair, deepening of the voice, menstrual irregularities in women, precocious puberty and genital development in children). If virilization occurs, testosterone treatment should be discontinued immediately until the cause is identified.
The physician should inform the patient of the risk of transmission
testosterone and precautions (see below). ANDROGEL 16.2 mg/g gel should not be administered to patients at risk of non-compliance with safety instructions (eg, in cases of severe alcoholism, drug addiction, severe mental disorders).
The potential risk of transmission is greatly reduced (but not eliminated) by wearing clothing (such as a long-sleeved shirt) that covers the area where the gel is to be applied. Most residual testosterone is removed from the skin surface by washing with soap and water just prior to contact.
The following precautions are recommended:
For the patient:
– wash hands with soap after applying the gel;
– cover the application area with clothing (for example, a shirt with
sleeves) after the gel dries;
– take a shower and thoroughly rinse the places where the gel was applied with water
soap before any contact with the risk of testosterone transfer.
Persons not using Androgel 16.2 mg / g:
in case of contact with the skin of the patient in the area of application of the gel, wash the surface of the skin on which the transfer could occur as soon as possible with soap and water;
– report the appearance and development of signs of androgenization, such as acne or changes in normal hair growth.
According to the results of an in vivo testosterone absorption study using Androgel gel, it is preferable that patients take a bath or shower at least 2 hours after applying the gel. However, a bath or shower accidentally taken between 2 and 6 hours after applying the gel does not significantly affect the effectiveness of the treatment.
To ensure the safety of the partner, the patient should be instructed to wash the gel application area with soap and water before intercourse or, if this is not possible, to wear clothing covering the application site.
Patients taking Androgel in contact with children
It is recommended to wear a T-shirt covering the site of application of the gel to avoid the risk of children’s skin contact with the drug.
Pregnancy and lactation
The drug is not used in pregnant and lactating mothers. Pregnant women should avoid any contact with the gel application area. In case of contact with the skin, wash the area with soap and water as soon as possible.
In case of pregnancy, the patient is obliged to strengthen the precautionary measures described above. This drug may have an undesirable virilizing effect on the fetus.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
Studies on the effect of Androgel on the ability to drive a car and equipment have not been conducted. Androgel has no or little effect on the ability to drive vehicles and mechanisms.
Cases of overdose with the use of Androgel were not noted.
Only one case of overdose after the use of injectable testosterone has been described: a stroke in a patient with a high plasma testosterone concentration of 114 ng / ml (395 nmol / l). However, it is unlikely that similar plasma testosterone concentrations can be achieved when the drug is applied to the skin.
Treatment in case of overdose is carried out by discontinuation of the drug in combination with appropriate supportive therapy.
At a temperature not higher than 25°С
Keep out of the reach of children!
Shelf life – 3 years
Do not use after the expiration date!