Androgel

General characteristics. Structure:

Active ingredient: testosterone of 25 mg and 50 mg;
excipients: isopropyl myristate; ethanol of 96%; карбопол 980; sodium hydroxide; the water purified;

Pharmacological properties:

Pharmacodynamics. The endogenous androgens, generally testosterone cosecreted by testicles and their main metabolite — dihydrotestosterone — are responsible for development of outside and internal generative organs and for preservation of secondary sexual characteristics (stimulation of growth of hair, a voice posterization, development of a libido). They influence anabolism of proteins; development of skeletal muscles and distribution of a hypodermic fatty tissue; reduction of excretion is promoted with urine of nitrogen, sodium, potassium, chlorides, phosphates also by waters. Testosterone does not cause development of testicles: it reduces pituitary secretion of gonadotrophins.
Effects of testosterone on some target organs are shown after peripheral transformation of testosterone to oestradiol which then contacts estrogenic receptors in kernels of cells of target organs (such as hypophysis, fatty tissue, a brain, bones and testicular cells of Leydiga).

Pharmacokinetics. Extent of absorption of testosterone through skin varies within 9–14% of the put dose.

After dermal absorption testosterone comes to a system blood stream in rather constant concentration during a 24-hour cycle.
Concentration of testosterone increase in serum from the first hour after drug use, reaching constant value from the second day of treatment. Daily fluctuations of concentration of testosterone have the same amplitude, as well as the changes of content of endogenous testosterone observed in circadian rhythms. At an outside way of administration of drug, thus, it is possible to avoid the distribution peaks in blood arising at an injection route of administration
Contrary to peroral therapy by androgens, external use of drug does not cause increase in concentration of steroids in a liver above physiological norms. Use of 5 g of Androgel causes average increase in concentration of testosterone in plasma approximately on 2,5 ng/ml (8,7 nmol/l).
After the treatment termination concentration of testosterone begins to decrease approximately in 24 h after the last reception. Concentration is returned to initial level approximately in 72–96 h after reception of the last dose.
The main active metabolites of testosterone are dihydrotestosterone and oestradiol.
Androgel is excreted generally with urine and with a stake in the form of the conjugated testosterone metabolites.

Indications to use:

Replacement therapy at insufficiency of testosterone.

Route of administration and doses:

Outwardly, at the same time, it is preferable in the morning. Gel is applied on the clean, dry, unimpaired skin of shoulders and/or a stomach.

The recommended dose — 5 g of gel (50 mg of testosterone), once a day. The individual day dose can be adjusted by the doctor depending on clinical and laboratory indicators at patients, but should not exceed 10 g of gel a day. Correction of the mode of dosing has to be carried out gradually, 2,5 g of gel a day.

After opening of a bag it is necessary to apply immediately on skin all its contents and to distribute a thin layer. It is not obligatory to rub it in skin. It is necessary to allow to dry within, at least, 3–5 min. before clothing. After putting gel it is necessary to wash up hands water with soap.

It is not necessary to apply gel on area of chest glands and genitalias since the high content of alcohol in drug can cause local irritation.

Constant concentration of testosterone in plasma is reached approximately for the second day of treatment by Androgel. For correction of a dose of testosterone it is necessary to define concentration of testosterone in serum in the morning, before drug use, with the day before yesterday after an initiation of treatment (within one week). The dosage can be reduced if the content of testosterone in plasma is increased. If concentration low, a dose it is possible to increase to 10 g of gel a day (no more).

Features of use:

Androgel it is necessary to use only at the insufficiency of testosterone which is followed by such clinical manifestations as regression of secondary sexual characteristics, change of a structure of a body, an adynamy, decrease in a libido, erectile dysfunction, etc.

Before an initiation of treatment other possible reasons which are the cornerstone of the above described symptoms have to be excluded.

Now there are no accurate norms on the levels of testosterone dependent on age. But it must be kept in mind that physiological levels of serumal testosterone decrease with age.

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

Androgel is not used for treatment of male infertility or erectile dysfunction which reason is not connected with insufficiency of testosterone.

Before purpose of testosterone all patients have to undergo inspection to exclude risk of existence of a prostate cancer since androgens can accelerate a progression of a subclinical prostate cancer and benign hyperplasia of a prostate. Careful and regular observation of a condition of a prostate (a manual rectal research, definition of prostatospetsifichesky antigen (DOG) in serum) and chest glands has to be carried out, at least, once a year, and at elderly patients and patients from risk group (with clinical or family factors) — it is regular, 2 times a year.

It is necessary to be careful when using Androgel's at patients with malignant new growths because of danger of a hypercalcemia (and the accompanying hypercalcuria) owing to metastasises in a bone. At these patients it is recommended to control concentration of calcium in serum.

At the patients having a heavy heart, liver or renal failure, treatment by Androgel can cause the complications which are characterized by hypostases with congestive heart failure or without it. In this case treatment has to be immediately stopped. Besides, therapy by diuretics can be required.

Androgel it is necessary to appoint with care the patient with an ischemic heart disease.

Testosterone can cause increase in the ABP and therefore Androgel it is necessary to appoint with care the patient with arterial hypertension.

At the patients accepting androgens during the long period in addition to laboratory control of concentration of testosterone, it is periodically necessary to check the following laboratory indicators: hemoglobin, a hematocrit (for identification of a polycythemia) and functional trials of a liver.

Androgel with care has to be used at patients with epilepsy and migraine as these states can be aggravated.

Data on increase in risk of development of an apnoea in a dream at the patients with a hypogonadism receiving treatment by testosterone esters, especially at what had risk factors, such as obesity and chronic respiratory diseases were published.

At achievement of normal concentration of testosterone in a blood plasma at the patients receiving androgens increase in sensitivity to insulin is possible.

Some clinical symptoms — irritability, nervousness, increase in body weight, long or frequent erections — can indicate the excessive influence of an androgen demanding correction of a dosage.

At development in the patient of heavy local reaction treatment has to be reconsidered and, in case of need, is stopped.

When using Androgel's at athletes it must be kept in mind that testosterone can give positive reaction in anti-doping tests.

Potential transfer of testosterone

At Androgel's appointment it is necessary to inform the patient on security measures.

To guarantee safety of the sexual partner, the patient should observe an interval between Androgel's use and sexual intercourse, or to put on the t-shirt covering gel sites of application during the contact period or to take a shower before sexual intercourse.

Not less than 6 h between putting gel and acceptance of a bathtub or shower are preferable to observe an interval. However accidental acceptance of a shower during from 1 to 6 h after putting gel has no significant effect on treatment.

It is recommended to observe the following precautionary measures:

For the patient: to wash up hands with soap after putting gel;

to close the field of putting gel clothes after gel dries;

to take a shower before any situation at which the contact with other person is inevitable.

For the persons which are not accepting Androgel: in case of hit on Androgel's skin, it is necessary to wash out as soon as possible water with soap this site of skin;

it is necessary to report to the doctor about emergence and development of such signs of a giperandrogenization as an acne or change of usual growth of hair.

In case of pregnancy of the partner the patient needs to observe precautionary measures attentively. Pregnant women have to avoid any contact of drug with skin, otherwise it is necessary to wash out immediately the place of contact by water with soap.

At contact with children it is recommended to wear the t-shirt covering a gel site of application to avoid risk of contact of skin of children with drug.

Androgel should not appoint patients who will not be able to observe security guidelines (for example a heavy alcoholism, toxicomania, heavy mental disorders).

Drug does not influence ability to driving and other mechanisms.

Side effects:

(5 g of gel a day) skin reactions were the most frequent undesirable effects at use in the recommended dose: reaction on site drawings, erythema, acne, xeroderma.

During clinical tests of Androgel in isolated cases the following undesirable effects were noted:

The general: changes of results of laboratory tests (polycythemia, decrease in level of lipids), headache.

From urinogenital system: changes of a prostate, gynecomastia, mastodynia.

From the central and peripheral nervous system: dizziness, paresthesia, amnesia, hyperesthesia, changes of mood.

From cardiovascular system: increase in the ABP.

From a GIT: diarrhea.

From skin and its appendages: alopecia.

At purpose of high dosages development of the following clinical symptoms is possible: irritability, nervousness, increase in body weight, long or frequent erections. These states demand dose adjustment.

The gynecomastia often occurs at the patients receiving treatment concerning a hypogonadism.

Drug contains alcohol therefore at its frequent drawing on skin the irritation and dryness can appear.

Interaction with other medicines:

Strengthens effect of peroral anticoagulants by modification of synthesis of factors of coagulation in a liver and competitive inhibition of linkng with proteins of plasma (it is necessary to be careful at joint appointment). It is recommended to control PV. The patients receiving peroral anticoagulants demand frequent control, especially at the beginning and/or at the end of a course of treatment androgens.

Joint purpose of testosterone and AKTG or corticosteroids can increase risk of emergence of hypostases. At co-administration, especially the patients having heart diseases, kidneys or a liver should be careful.

Impact on laboratory tests: androgens can reduce the level of tiroksinsvyazyvayushchy globulin, leading to reduction of serumal concentration of T4 and to increase in sensitivity to T3 and T4. Levels of free hormones of a thyroid gland, however, remain invariable, and at the same time there are no clinical manifestations of a hypothyroidism.

Contraindications:

Hypersensitivity to testosterone or other components of drug;
carcinoma of chest gland or prostate cancer or suspicion on their existence.

Experience of use of Androgel for women and children is absent.
With care:
- malignant new growths (because of danger of a hypercalcemia and a hypercalcuria);
- heavy heart, liver or renal failure;
- Ischemic heart disease, arterial hypertension;
- epilepsy, migraine.

Overdose:

Overdose cases at Androgel's use are not recorded.

Only one case of overdose after use of testosterone entered injektsionno is described. It the patient had a stroke with high concentration of testosterone in plasma — 114 ng/ml (the 395th nmol/l).

However it is improbable that similar concentration of testosterone in plasma can be reached when putting drug on skin.

Storage conditions:

At a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Androgel, gel for external use of 1%; a package (bag) from aluminum foil laminated 2.5 g, a pack of cardboard 10 or 30 pieces.