Universal reference book for medicines
Name of the drug: NEBIDO ® (NEBIDO ® )

Active substance: testosterone

Type: Androgenic drug - depot form

Manufacturer: BAYER PHARMA (Germany)
Composition, form of production and packaging
The solution for the / m introduction is
transparent, oily, with a yellowish tinge.

1 ml of 1 amp.

testosterone undecanoate 250 mg 1 g

Excipients: benzyl benzoate - 2 g, purified castor oil (for parenteral administration) - 1.18 g.

4 ml ampoules from amber glass type I (1) - packs of cardboard with glued holder.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Androgen.
Testosterone undecanoate is an ester of natural androgen, testosterone. The active form, testosterone, is formed as a result of the cleavage of the side chain.
Testosterone is a male sex hormone possessing the entire spectrum of biological activity necessary for the formation and maintenance of androgenic functions.
It is synthesized mainly in testicles and, to a lesser extent, in the adrenal cortex. Provides the formation of male characteristics during intrauterine development, in early childhood; in the period of puberty - the development of male genital organs and secondary sexual characteristics. Subsequently, testosterone provides maintenance of the male phenotype and androgen-dependent functions (for example, spermatogenesis, sex glands).
Insufficient secretion of testosterone leads to male hypogonadism, which is characterized by low concentrations of testosterone in the serum.
Symptoms associated with male hypogonadism include, but are not limited to, erectile dysfunction, decreased sexual desire, fatigue, depressed moods, lack, underdevelopment or regression of secondary sexual characteristics, and an increased risk of osteoporosis. Exogenous androgens are prescribed to increase inadequate levels of endogenous testosterone and reduce symptoms of hypogonadism.
Depending on the target organ, the action of testosterone is mainly androgenic (for example, the prostate gland, seminal vesicles, epididymis) or protein-anabolic (muscle, bone, hematopoietic system, kidney, liver).

The action of testosterone in some organs is manifested after the peripheral conversion of testosterone to estradiol, which then binds to estrogen receptors in the nuclei of target cells (for example, the pituitary, adipose tissue, brain, bones and testicular cells of Leydig).

In men suffering from hypogonadism, the use of androgens reduces the body fat mass, increases the body's lean body mass, and also prevents the loss of bone tissue.Androgens can improve sexual function, and also have a positive psychotropic effect, improving mood.

PHARMACOKINETICS

Suction

After an injection of an oil solution of testosterone, undecanoate is gradually released from the depot and almost completely cleaved by serum esterases to testosterone and undecanoic acid.
An increase in serum testosterone concentrations relative to the baseline may be determined the day after the injection.
Distribution

In two separate studies, mean C max testosterone, 24 nmol / L and 45 nmol / L, were determined respectively 14 and 7 days after a single IM injection of testosterone undecanoate at a dose of 1 g to men with hypogonadism.
In the male serum, binding to proteins (GSPA and albumin) is about 98%. Only the free fraction of testosterone is considered biologically active. After IV infusion of testosterone, the elderly V d was about 1 l / kg.
After repeated I / m injections of testosterone undecanoate at a dose of 1 g to men with hypogonadism, at intervals between injections at 10 weeks, C ss was achieved between 3 and 5 injections.
The mean values ​​of the maximum C ss and the minimum C ss of testosterone were about 42 and 17 nmol / L, respectively. T 1/2 testosterone is about 90 days, which corresponds to the release rate of the substance from the depot.
Metabolism

Testosterone, formed from testosterone undecanoate as a result of cleavage of the ester bond, is metabolized and excreted from the body in the same ways as endogenous testosterone.
Undecanoic acid is metabolized by p-oxidation in the same way as other aliphatic carboxylic acids.
Excretion

Testosterone is significantly metabolized in the liver and beyond.
After the administration of labeled testosterone, about 90% of radioactivity is detected in the urine as glucuronide and sulfate acid conjugates, and 6% after passage of the enterohepatic circulation is detected in the stool. Urine-specific foods include androsterone and etiocholanolone.
INDICATIONS

- Insufficiency of testosterone in primary and secondary hypogonadism in men (testosterone-replacement therapy).

DOSING MODE

Injection of Nebido ® in a dose of 1 g of testosterone undecanoate (1 ampoule) is performed once every 10-14 weeks.
At this injection frequency, a sufficient level of testosterone is maintained, and no cumulation of the substance takes place.
The drug is given in / m immediately after opening the ampoule.
Injections should be made very slowly. Nebido ® can only be entered strictly in / m. Care must be taken to ensure that the product does not enter the blood vessel.
Before starting treatment, determine the amount of testosterone in the serum.
The first interval between injections can be reduced, but should be at least 6 weeks. C ssat this dose is achieved quickly.
At the end of the interval between injections, it is recommended to measure testosterone concentration in serum.
If its level is lower than normal, this fact may indicate a need to reduce the interval between injections. At high concentrations, the feasibility of increasing this interval should be considered. The interval between injections should remain within the recommended range of 10-14 weeks.
Because clinical studies have not been conducted in men under the age of 18, Nebido® is not intended for children and adolescents.

Available limited data do not indicate the need for dose adjustment in elderly patients .

Studies of the use of the drug in patients with impaired liver function were not performed.

Studies of the use of the drug in patients with renal insufficiency have not been conducted.

SIDE EFFECT

Most often: acne, pain at the injection site.

The table below lists unwanted reactions grouped according to the classes of organ systems according to the MedRA terminology.
The frequency of occurrence is determined from the data of clinical trials and is classified as follows: often (from 1/100 to <1/10) and infrequently (from 1/1000 to <1/100).
Undesirable reactions were recorded during 6 clinical trials (in total - 422 patients).
The association of these undesirable reactions with the use of Nebido ® is considered, at least, possible.
Table.
Relative frequency of occurrence of patients with adverse reactions according to the MedRA classification, determined on the basis of the aggregate data of 6 clinical trials, n = 422 (100%)
Often Often

On the part of the blood and lymphatic system

Polycythemia Increase in hematocrit Increase in the number of red blood cells Increase in hemoglobin

From the immune system

Hypersensitivity

From the side of metabolism and nutrition

Increase in body weight Increase in appetite Increase in glycosylated hemoglobin level Hypercholesterolemia Increase in triglyceride level in blood Increase in cholesterol level in the blood

From the side of the psyche

Depression Emotional disturbances Insomnia Anxiety Aggressiveness Irritability

From the nervous system

Headache Migraine Tremor

From the side of the cardiovascular system

Tides Violation of the function of the cardiovascular system Hypertension Increased blood pressure Dizziness

On the part of the respiratory system, the organs of the thorax and the mediastinum

Bronchitis Sinusitis Cough Shortness of breath Snoring Dysphonia

From the digestive system

Diarrhea Nausea

From the liver and biliary tract

Deviations of functional liver tests, incl.
increased ACT activity
From the skin and subcutaneous tissues

Acne Alopecia Erythema Rash Papular rash Itching Dryness of the skin

From the musculoskeletal system and connective tissue

Arthralgia Pain in the limbs Muscle spasms Muscle tension Myalgia Musculoskeletal rigidity Increased activity of CK in the blood

From the urinary system

Decrease in urine output Urine retention Disorders of urinary tract function Nicturia Dysuria

From the side of the reproductive system

Increase in PSA level Pathological results of examination of the prostate Benign prostatic hyperplasia Intraepithelial neoplasia of the prostate Prostatic gland Prostatitis Imbalance of the prostate gland Increase of the libido Decrease of the libido Pain in the testicles Pain in the mammary gland Breast in the mammary gland Gynecomastia Increase of the level of estradiol Increase of the level of free testosterone in the blood Increase testosterone level in the blood

General reactions

Increased fatigue Asthenia Hyperhidrosis Night sweats

Local Reactions

Pain, discomfort, itching, swelling, bruising, irritation at the injection site.

The pulmonary embolism of the pulmonary artery with oil solutions can rarely lead to the appearance of a number of signs and symptoms, such as coughing, shortness of breath, malaise, hyperhidrosis, chest pain, dizziness, paresthesia or fainting.
These reactions can develop during or immediately after injection and are reversible. In clinical trials, as well as in the postmarketing period, rare cases (? 1/10 000 and <1/1000 injections) of pulmonary artery pulmonary microembolism were recorded.
After Nebido ® injections, there are reports of anaphylactic reactions.

Along with the above undesirable reactions against the background of treatment with testosterone-containing medications, nervousness, aggression, sleep apnea, various skin reactions (including seborrhea), increased erections, and also isolated cases of jaundice development have been reported.

Therapy with drugs high in testosterone usually causes a reversible cessation or reduction of spermatogenesis, which leads to a decrease in the size of the testicles.

Testosterone-replacement therapy for hypogonadism in rare cases can cause persistent painful erections (priapism).

Long-term or high-dose therapy with testosterone can sometimes lead to increased frequency of fluid retention in the body and edema.

CONTRAINDICATIONS

- androgen-dependent carcinoma of the prostate;

- androgen-dependent breast carcinoma in men;

- hypercalcemia associated with malignant tumors;

- Liver tumors at present or in the anamnesis;

- Hypersensitivity to the active substance or any of the auxiliary components of the drug.

Nebido ® is not used in women.

With caution should be used in patients with the syndrome of apnea.

PREGNANCY AND LACTATION

Nebido ® is not used in women.

APPLICATION FOR FUNCTIONS OF THE LIVER

Studies of the use of the drug in patients with renal insufficiency have not been conducted.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in tumors of the liver at present or in the anamnesis.

Studies of the use of the drug in patients with impaired liver function were not performed.

APPLICATION FOR CHILDREN

Clinical trials Nebido involving children or adolescents under the age of 18 has not been carried out to date.

The use of testosterone for the treatment of children, along with masculinization, can cause the growth and maturation of bone tissue to accelerate, as well as premature closure of the epiphyseal growth zone, which will result in a decrease in the final growth.
The appearance of common acne


APPLICATION IN ELDERLY PATIENTS

With the use of androgens in the treatment of elderly patients, the risk of developing prostatic hyperplasia may increase.
Despite the lack of evidence that androgens can cause prostate carcinoma, they can contribute to the growth of the existing carcinoma. Therefore, before starting treatment with drugs containing testosterone, prostate cancer should be excluded.
SPECIAL INSTRUCTIONS

With the use of androgens in the treatment of elderly patients, the risk of developing prostatic hyperplasia may increase.
Despite the lack of evidence that androgens can cause prostate carcinoma, they can contribute to the growth of the existing carcinoma. Therefore, before starting treatment with drugs containing testosterone, prostate cancer should be excluded.
As a preventive measure, regular examinations of the prostate gland are recommended.

Patients on long-term androgen therapy are advised to periodically monitor hemoglobin and hematocrit to identify cases of polycythemia.

Against the background of the use of sex steroids, which include testosterone, benign and, more rarely, malignant liver tumors that could lead to intraabdominal bleeding have been observed.
If the background of treatment with Nebido ® develops severe pain in the upper abdomen, liver is enlarged, or signs of intra-abdominal bleeding are present, then in case of differential diagnosis, the probability of having a liver tumor should be taken into account.
Caution should be exercised in patients prone to edema, as androgen therapy may delay the excretion of sodium ions.

The existing sleep apnea syndrome may worsen.

Androgens are not used to enhance muscle development in healthy subjects, nor to increase physical ability.

Substitution testosterone therapy can reversibly reduce spermatogenesis.

Like all oil solutions, Nebido ® should be injected / m and very slowly to avoid pulmonary artery microembolism with an oil solution of the drug that can manifest itself with symptoms such as coughing, shortness of breath, malaise, hyperhidrosis, chest pain, dizziness, paresthesia or fainting.
These reactions can develop during or immediately after injection and are reversible. Treatment, as a rule, supporting, for example, the introduction of additional oxygen.
Use in Pediatrics

Nebido ® is not intended for use in children and adolescents, because clinical studies of the drug with children and adolescents under the age of 18 years have not been conducted.

The use of testosterone for the treatment of children, along with masculinization, can cause the growth and maturation of bone tissue to accelerate, as well as the premature closure of the epiphyseal growth zone, which will result in a decrease in the final growth.
Perhaps the appearance of common acne.
Impact on the ability to drive vehicles and manage mechanisms

Nebido ® does not affect the ability to drive and work with mechanisms that require increased attention.

Safety data from preclinical studies

The use of Nebido ® can lead to virilization of the female fetus at some stages of development.
However, the results of studies for embryotoxic and, in particular, teratogenic effects, do not indicate the likelihood of further deterioration in organ development.
OVERDOSE

In case of overdose, special therapeutic measures are not required, except for temporary discontinuation of therapy or dose reduction.

DRUG INTERACTION

Drugs affecting testosterone

Possible interaction with drugs that induce microsomal enzymes (eg, barbiturates), which can lead to an increase in testosterone clearance.

Influence of androgens on other drugs

Androgens can cause an increase in the concentration of oxyphenbutazone in the serum.

Testosterone and its derivatives can increase the activity of oral anticoagulants, which may lead to the need for dose adjustment.
Regardless of this fact, as a general rule, one should always observe the restrictions regarding I / m injections to patients with acquired or hereditary blood clotting disorders.
Under the influence of androgens, hypoglycemic effects of insulin may increase.
You may need to reduce the dose of hypoglycemic drug.
Since compatibility studies have not been conducted, this drug should not be confused with other drugs.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 5 years.
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