Composition, structure and packing
Gel for external use only 1% of transparent or slightly opalescent, colorless, with the smell of alcohol.
1 g of a pack. Testosterone 10 mg / 25 mg.
Excipients: isopropyl myristate, ethanol 96%, Carbopol 980, sodium hydroxide, purified water. Gel for external use only 1% of transparent or slightly opalescent, colorless, with the smell of alcohol.
1 g of a pack. Testosterone 10 mg / 50 mg.
Excipients: isopropyl myristate, ethanol 96%, Carbopol 980, sodium hydroxide, purified water.
Clinico-pharmacological group: androgenic drug.
Pharmacological action
Androgenic drug. Endogenous androgens (mainly testosterone) secreted by the testes, and their major metabolite dihydrotestosterone are responsible for the development of external and internal genital organs and secondary sexual characteristics (stimulating hair growth, deepening of the voice, the development of libido).
Has a general effect on protein anabolism, the development of skeletal muscle and distribution of subcutaneous fat, reducing the urinary excretion of nitrogen, sodium, potassium, chloride, phosphate and water. Testosterone does not cause the development of testicles: it reduces the secretion of pituitary gonadotropins. Effects of testosterone on some target organs are shown after peripheral conversion of testosterone to estradiol, which then binds to the estrogen receptor in the nuclei of target-organs (such as the pituitary, adipose tissue, brain, bone and testicular Leydig cells).
Pharmacokinetics
Absorption
The degree of absorption of testosterone through the skin varies from approximately 9% to 14% of the deposited dose.
Distribution
After absorption of testosterone enters the systemic circulation in relatively constant concentrations over a 24-hour cycle. Concentrations of serum testosterone increased from the first hour after application of the drug, reaching a constant value from the second day of treatment.
Daily fluctuations in concentrations of testosterone have the same amplitude as observed in the circadian rhythms of change in the content of endogenous testosterone. For exterior routes of administration of the drug, thus, can avoid the peaks of distribution in the blood, resulting in injecting use. In contrast to oral therapy with androgens, external application of the drug did not cause the increase of concentrations of steroids in the liver above the physiological norms.
Application of 5 g Androgelya causes an average increase in the concentration of testosterone in plasma of approximately 2.5 ng / ml (8.7 nmol / L).
Metabolism
The major active metabolites of testosterone are dihydrotestosterone and estradiol.
Withdrawal
After the cessation of treatment the concentration of testosterone begins to decline after about 24 hours after the last application. Concentration returns to its original level after about 72-96 hours after receiving the last dose. The drug is substantially excreted with urine and feces in the form of conjugated metabolites of testosterone.
Statement
replacement therapy with testosterone deficiency.
Dosage regimen
The recommended daily dose is 5 g of gel (ie, 50 mg testosterone).
The drug is used 1 times / day at approximately the same time of day, preferably in the morning. The daily dose may be adjusted depending on the clinical and laboratory parameters, but should not exceed 10 g of gel. Correction of dosage regimen should be conducted in steps of 2.5 g gel / day. To correct dose is necessary to determine the concentration of serum testosterone in the morning, before the application of the drug, the third day after the start of treatment (one week). The dose can be reduced if the content of testosterone in plasma increased or conversely to increase if the concentration of testosterone is low.
Rules of the drug
The gel is applied to a clean, dry, intact skin of shoulders, forearms and / or abdomen. You may not apply the gel on the genital area, because high content of ethanol in the product may cause local irritation. After opening the bag must be immediately put on the skin of all its contents and distribute a thin layer. You do not have to rub it into the skin. You can allow it to dry for at least 3-5 minutes before dressing. After the application should wash your hands with soap and water.
Side effect
Local reactions: common - irritation and dryness of the skin at the site of application of the drug, especially when it is often the application.
On the part of the endocrine and reproductive systems: in isolated cases - the changes of the prostate, gynecomastia (mainly in patients receiving treatment for hypogonadism), mammalgia.
From the central nervous system and peripheral nervous system: in isolated cases - dizziness, headache, amnesia, mood changes, paresthesia, hyperesthesia.
Since the cardiovascular system: in isolated cases - increase blood pressure.
On the part of the digestive system: in isolated cases - diarrhea.
Dermatological reactions: erythema, acne, and in rare cases - alopecia.
Other: changes in the results of laboratory tests (polycythemia, reduction of lipid). In the appointment of the drug in high doses may develop the following clinical signs: irritability, nervousness, increased body weight, prolonged or frequent erections.
These states require dose adjustment.
Contraindications
carcinoma of the breast or a suspicion of its existence;
prostate cancer or suspicion of its existence;
Hypersensitivity to testosterone or other components of the drug.
Experience with Androgelya women and children missing.
Precautions should be prescribed the drug for malignant tumors (because of the risk of hypercalcaemia and hypercalciuria), with a heavy heart, liver or kidney disease, with coronary heart disease, hypertension, epilepsy, migraine.
Pregnancy and lactation
The drug does not apply to women. In the case of pregnancy, sexual partners of patients should be more attentive to comply with precautionary measures. Pregnant women should avoid any skin contact.
In case of contact with the drug a woman, you must immediately wash exposed with soap and water.
Application for violations of liver function
Patients with severe hepatic insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately.
Application for violations of renal function
Patients with severe renal insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately.
Cautions
Androgel should be used only when testosterone deficiency accompanied by clinical manifestations such as regression of secondary sex characteristics, changes in body composition, asthenia, decreased libido, erectile dysfunction. Before treatment is necessary to exclude other possible causes that underlie these symptoms. Currently there are no clear rules on the age-dependent values of testosterone. However, one should take into account the fact that physiological levels of serum testosterone levels decline with advancing age.
Because of variability in laboratory values, determination of the concentration of testosterone should be in the same laboratory. Androgel is not applied for the treatment of male infertility or erectile dysfunction, the cause of which is not associated with testosterone deficiency.
Prior to the appointment of testosterone, all patients should be screened to exclude the presence of prostate cancer because androgens may accelerate the progression of subclinical prostate cancer and benign prostatic hyperplasia. It should conduct a careful and regular monitoring of prostate cancer (digital rectal study, the definition of prostate specific antigen (PSA) in serum) and mammary glands, at least once a year every year, and in elderly patients and patients at risk (with clinical or familial factors) - twice a year. Androgel should be used with caution in patients with malignant neoplasms because of the risk of hypercalcemia (and associated hypercalciuria), due to bone metastases.
In these patients it is recommended to control the concentration of calcium in serum.
Patients with severe heart, hepatic or renal insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately. In addition, you may need treatment with diuretics. Androgel should carefully assign patients with CHD. Testosterone may increase blood pressure, and therefore Androgel should carefully assign patients with arterial hypertension.
In patients receiving androgens over a long period, in addition to laboratory measurements of the concentration of testosterone necessary to periodically check the following laboratory parameters: hemoglobin, hematocrit (to detect polycythemia), and liver function tests. Androgel should be used with caution in patients with epilepsy and migraine, as these conditions may worsen. Data were published to increase the risk of sleep apnea in patients with hypogonadism, treatment esters of testosterone, especially those who had risk factors such as obesity and chronic respiratory diseases.
Patients receiving androgens, upon reaching normal concentrations of testosterone in the blood plasma can be observed an increase in sensitivity to insulin. Some clinical symptoms: irritability, nervousness, weight gain, prolonged or frequent erections may indicate excessive androgen exposure requiring dose adjustment. If the patient has severe local reaction, treatment should be reviewed and, if necessary, terminated.
Using Androgelya the athletes need to take into account the fact that the drug contains testosterone, which can give a positive reaction in doping tests.
The potential transfer of testosterone
In appointing Androgelya must inform the patient about safety measures. To ensure the safety of sexual partner, the patient should be advised to observe the interval between the application and Androgelya intercourse or wear a shirt that covers the place of application of the gel, during the period of contact, or take a shower before intercourse. It is preferable to observe an interval of at least 6 hours between applying the gel and taking a bath or shower. However, the random douche in the period from 1 to 6 h after application of 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 area causing the gel clothing after the gel has dried;
take a shower before any situation in which contact with another person is inevitable.
Persons who are not applying Androgel, in the case of contact with the area of application of the gel, not pre-washed with water, as soon as possible with soap and water area of the skin, which could get testosterone. Tell the doctor about the appearance and development of such symptoms giperandrogenizatsii as acne or modified conventional hair growth. Patients applying Androgel, in contact with children are recommended to wear a T-shirt that covers the place causing the gel to avoid the risk of contact with the skin of children with the drug. Androgel should not be considered in patients who are unable to comply with safety instructions (eg, severe chronic 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 that requires increased attention and quickness of psychomotor reactions.
Overdose
No cases of overdose when using Androgelya not fixed. Described only one case of overdose after application of testosterone, introduced by injection. It was a stroke patient with a high concentration of testosterone in plasma of 114 ng / ml (395 nmol / L). However, it is unlikely that such concentrations of testosterone in the plasma can be achieved when applying the product to the skin.
Drug Interactions
With simultaneous application Androgelya and indirect anticoagulants may be increased by the latter by modifying the synthesis of hepatic coagulation factors and competitive inhibition of binding to plasma proteins. Patients receiving oral anticoagulants during treatment with Androgelya, it is recommended to monitor the prothrombin time, especially frequent in the beginning and / or at the end of treatment with androgens.
Combined use Androgelya with ACTH or corticosteroids may increase the risk of swelling. Care should be taken under the joint use of these drugs, especially in patients with heart disease, kidney or liver disease. Androgens may decrease levels of thyroxine binding globulin, leading to a decrease in serum concentrations of T4 and increase sensitivity to T3 and T4. The levels of free thyroid hormones, however, remain unchanged, and thus no clinical manifestations of hypothyroidism.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children at or above 25 ° C.
Shelf life - 3 years.
Gel for external use only 1% of transparent or slightly opalescent, colorless, with the smell of alcohol.
1 g of a pack. Testosterone 10 mg / 25 mg.
Excipients: isopropyl myristate, ethanol 96%, Carbopol 980, sodium hydroxide, purified water. Gel for external use only 1% of transparent or slightly opalescent, colorless, with the smell of alcohol.
1 g of a pack. Testosterone 10 mg / 50 mg.
Excipients: isopropyl myristate, ethanol 96%, Carbopol 980, sodium hydroxide, purified water.
Clinico-pharmacological group: androgenic drug.
Pharmacological action
Androgenic drug. Endogenous androgens (mainly testosterone) secreted by the testes, and their major metabolite dihydrotestosterone are responsible for the development of external and internal genital organs and secondary sexual characteristics (stimulating hair growth, deepening of the voice, the development of libido).
Has a general effect on protein anabolism, the development of skeletal muscle and distribution of subcutaneous fat, reducing the urinary excretion of nitrogen, sodium, potassium, chloride, phosphate and water. Testosterone does not cause the development of testicles: it reduces the secretion of pituitary gonadotropins. Effects of testosterone on some target organs are shown after peripheral conversion of testosterone to estradiol, which then binds to the estrogen receptor in the nuclei of target-organs (such as the pituitary, adipose tissue, brain, bone and testicular Leydig cells).
Pharmacokinetics
Absorption
The degree of absorption of testosterone through the skin varies from approximately 9% to 14% of the deposited dose.
Distribution
After absorption of testosterone enters the systemic circulation in relatively constant concentrations over a 24-hour cycle. Concentrations of serum testosterone increased from the first hour after application of the drug, reaching a constant value from the second day of treatment.
Daily fluctuations in concentrations of testosterone have the same amplitude as observed in the circadian rhythms of change in the content of endogenous testosterone. For exterior routes of administration of the drug, thus, can avoid the peaks of distribution in the blood, resulting in injecting use. In contrast to oral therapy with androgens, external application of the drug did not cause the increase of concentrations of steroids in the liver above the physiological norms.
Application of 5 g Androgelya causes an average increase in the concentration of testosterone in plasma of approximately 2.5 ng / ml (8.7 nmol / L).
Metabolism
The major active metabolites of testosterone are dihydrotestosterone and estradiol.
Withdrawal
After the cessation of treatment the concentration of testosterone begins to decline after about 24 hours after the last application. Concentration returns to its original level after about 72-96 hours after receiving the last dose. The drug is substantially excreted with urine and feces in the form of conjugated metabolites of testosterone.
Statement
replacement therapy with testosterone deficiency.
Dosage regimen
The recommended daily dose is 5 g of gel (ie, 50 mg testosterone).
The drug is used 1 times / day at approximately the same time of day, preferably in the morning. The daily dose may be adjusted depending on the clinical and laboratory parameters, but should not exceed 10 g of gel. Correction of dosage regimen should be conducted in steps of 2.5 g gel / day. To correct dose is necessary to determine the concentration of serum testosterone in the morning, before the application of the drug, the third day after the start of treatment (one week). The dose can be reduced if the content of testosterone in plasma increased or conversely to increase if the concentration of testosterone is low.
Rules of the drug
The gel is applied to a clean, dry, intact skin of shoulders, forearms and / or abdomen. You may not apply the gel on the genital area, because high content of ethanol in the product may cause local irritation. After opening the bag must be immediately put on the skin of all its contents and distribute a thin layer. You do not have to rub it into the skin. You can allow it to dry for at least 3-5 minutes before dressing. After the application should wash your hands with soap and water.
Side effect
Local reactions: common - irritation and dryness of the skin at the site of application of the drug, especially when it is often the application.
On the part of the endocrine and reproductive systems: in isolated cases - the changes of the prostate, gynecomastia (mainly in patients receiving treatment for hypogonadism), mammalgia.
From the central nervous system and peripheral nervous system: in isolated cases - dizziness, headache, amnesia, mood changes, paresthesia, hyperesthesia.
Since the cardiovascular system: in isolated cases - increase blood pressure.
On the part of the digestive system: in isolated cases - diarrhea.
Dermatological reactions: erythema, acne, and in rare cases - alopecia.
Other: changes in the results of laboratory tests (polycythemia, reduction of lipid). In the appointment of the drug in high doses may develop the following clinical signs: irritability, nervousness, increased body weight, prolonged or frequent erections.
These states require dose adjustment.
Contraindications
carcinoma of the breast or a suspicion of its existence;
prostate cancer or suspicion of its existence;
Hypersensitivity to testosterone or other components of the drug.
Experience with Androgelya women and children missing.
Precautions should be prescribed the drug for malignant tumors (because of the risk of hypercalcaemia and hypercalciuria), with a heavy heart, liver or kidney disease, with coronary heart disease, hypertension, epilepsy, migraine.
Pregnancy and lactation
The drug does not apply to women. In the case of pregnancy, sexual partners of patients should be more attentive to comply with precautionary measures. Pregnant women should avoid any skin contact.
In case of contact with the drug a woman, you must immediately wash exposed with soap and water.
Application for violations of liver function
Patients with severe hepatic insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately.
Application for violations of renal function
Patients with severe renal insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately.
Cautions
Androgel should be used only when testosterone deficiency accompanied by clinical manifestations such as regression of secondary sex characteristics, changes in body composition, asthenia, decreased libido, erectile dysfunction. Before treatment is necessary to exclude other possible causes that underlie these symptoms. Currently there are no clear rules on the age-dependent values of testosterone. However, one should take into account the fact that physiological levels of serum testosterone levels decline with advancing age.
Because of variability in laboratory values, determination of the concentration of testosterone should be in the same laboratory. Androgel is not applied for the treatment of male infertility or erectile dysfunction, the cause of which is not associated with testosterone deficiency.
Prior to the appointment of testosterone, all patients should be screened to exclude the presence of prostate cancer because androgens may accelerate the progression of subclinical prostate cancer and benign prostatic hyperplasia. It should conduct a careful and regular monitoring of prostate cancer (digital rectal study, the definition of prostate specific antigen (PSA) in serum) and mammary glands, at least once a year every year, and in elderly patients and patients at risk (with clinical or familial factors) - twice a year. Androgel should be used with caution in patients with malignant neoplasms because of the risk of hypercalcemia (and associated hypercalciuria), due to bone metastases.
In these patients it is recommended to control the concentration of calcium in serum.
Patients with severe heart, hepatic or renal insufficiency, treatment Androgelem can cause complications, characterized by edema with congestive heart failure or without her. In this case, treatment should be stopped immediately. In addition, you may need treatment with diuretics. Androgel should carefully assign patients with CHD. Testosterone may increase blood pressure, and therefore Androgel should carefully assign patients with arterial hypertension.
In patients receiving androgens over a long period, in addition to laboratory measurements of the concentration of testosterone necessary to periodically check the following laboratory parameters: hemoglobin, hematocrit (to detect polycythemia), and liver function tests. Androgel should be used with caution in patients with epilepsy and migraine, as these conditions may worsen. Data were published to increase the risk of sleep apnea in patients with hypogonadism, treatment esters of testosterone, especially those who had risk factors such as obesity and chronic respiratory diseases.
Patients receiving androgens, upon reaching normal concentrations of testosterone in the blood plasma can be observed an increase in sensitivity to insulin. Some clinical symptoms: irritability, nervousness, weight gain, prolonged or frequent erections may indicate excessive androgen exposure requiring dose adjustment. If the patient has severe local reaction, treatment should be reviewed and, if necessary, terminated.
Using Androgelya the athletes need to take into account the fact that the drug contains testosterone, which can give a positive reaction in doping tests.
The potential transfer of testosterone
In appointing Androgelya must inform the patient about safety measures. To ensure the safety of sexual partner, the patient should be advised to observe the interval between the application and Androgelya intercourse or wear a shirt that covers the place of application of the gel, during the period of contact, or take a shower before intercourse. It is preferable to observe an interval of at least 6 hours between applying the gel and taking a bath or shower. However, the random douche in the period from 1 to 6 h after application of 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 area causing the gel clothing after the gel has dried;
take a shower before any situation in which contact with another person is inevitable.
Persons who are not applying Androgel, in the case of contact with the area of application of the gel, not pre-washed with water, as soon as possible with soap and water area of the skin, which could get testosterone. Tell the doctor about the appearance and development of such symptoms giperandrogenizatsii as acne or modified conventional hair growth. Patients applying Androgel, in contact with children are recommended to wear a T-shirt that covers the place causing the gel to avoid the risk of contact with the skin of children with the drug. Androgel should not be considered in patients who are unable to comply with safety instructions (eg, severe chronic 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 that requires increased attention and quickness of psychomotor reactions.
Overdose
No cases of overdose when using Androgelya not fixed. Described only one case of overdose after application of testosterone, introduced by injection. It was a stroke patient with a high concentration of testosterone in plasma of 114 ng / ml (395 nmol / L). However, it is unlikely that such concentrations of testosterone in the plasma can be achieved when applying the product to the skin.
Drug Interactions
With simultaneous application Androgelya and indirect anticoagulants may be increased by the latter by modifying the synthesis of hepatic coagulation factors and competitive inhibition of binding to plasma proteins. Patients receiving oral anticoagulants during treatment with Androgelya, it is recommended to monitor the prothrombin time, especially frequent in the beginning and / or at the end of treatment with androgens.
Combined use Androgelya with ACTH or corticosteroids may increase the risk of swelling. Care should be taken under the joint use of these drugs, especially in patients with heart disease, kidney or liver disease. Androgens may decrease levels of thyroxine binding globulin, leading to a decrease in serum concentrations of T4 and increase sensitivity to T3 and T4. The levels of free thyroid hormones, however, remain unchanged, and thus no clinical manifestations of hypothyroidism.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children at or above 25 ° C.
Shelf life - 3 years.
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