Nebido - Instructions For Use Of The Drug, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Nebido

Nebido: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Nebido

ATX code: G03BA03

Active ingredient: testosterone (testosterone)

Producer: Bayer AG (Germany)

Description and photo update: 2019-20-08

Nebido is an androgenic drug used for testosterone replacement therapy.

Release form and composition

Nebido is available in the form of a solution for intramuscular administration: oily, transparent, with a yellowish tinge (4 ml in amber glass ampoules or type I dark glass vials, 1 ampoule or bottle in a cardboard box with a glued holder).

The composition of 4 ml (1 ampoule or 1 bottle) of the solution includes:

• Active ingredient: testosterone undecanoate - 1 g;
• Auxiliary components: benzyl benzoate - 2 g, purified castor oil - 1.18 g.

Pharmacological properties

Pharmacodynamics

The active substance of Nebido is testosterone undecanoate, an ester of the natural male hormone testosterone, the active form of which is formed as a result of the splitting of the side chain.

Testosterone is the most important androgen in the male body, synthesized primarily in the testicles and, to a lesser extent, in the adrenal cortex. During the period of intrauterine formation and development of the fetus, in early childhood, during puberty, the hormone is responsible for male characteristics, later - for maintaining the male phenotype, as well as androgen-dependent functioning of the body (gonads, spermatogenesis). Inadequate testosterone production can cause male hypogonadism, which is characterized by low serum testosterone levels. The consequence of male hypogonadism, among other symptoms, is considered erectile dysfunction, decreased libido, increased fatigue, depression, increased risk of osteoporosis, as well as the absence, underdevelopment or regression of secondary (external) sexual characteristics. Exogenous androgens are used when it is necessary to increase endogenous testosterone when it is deficient to relieve symptoms of hypogonadism.

The nature of the action of testosterone, depending on the target organ, is often androgenic (seminal vesicles, prostate gland, epididymis), but it is protein-anabolic (muscle mass, hematopoietic system, bones, liver, kidneys).

In some organs, the action of the hormone manifests itself after its peripheral transformation into estradiol, which subsequently binds to estrogen receptors in the nuclei of target cells, such as the pituitary gland, adipose tissue, brain, bones, Leydig cells.

The use of androgens in hypogonadal men has been shown to reduce body fat mass, increase lean body mass, and prevent bone loss. Male sex hormones can improve sexual function and have positive psychotropic effects through improved mood.

Pharmacokinetics

• absorption: as a result of intramuscular injection of Nebido oil solution, testosterone undecanoate is released from the depot gradually, almost completely split by serum esterases into undecanoic acid and testosterone. An increase in serum testosterone levels after injection relative to baseline levels can be determined the very next day;
• distribution: according to independent studies in men with hypogonadism, the average values of the maximum plasma concentration (C _max) of testosterone after a single intramuscular injection of testosterone undecanoate at a dose of 1 g were 45 nmol / L after 1 week, and 24 nmol / L after 2 weeks. Up to 98% of the exogenous hormone binds to plasma proteins (mainly albumin and globulin that connects sex hormones). It is believed that only the free fraction of testosterone has biological activity. The apparent volume of distribution (V _d) due to intravenous infusion of testosterone in elderly men reached 1 L / kg. Stationary plasma concentration (C _ss) of testosterone after repeated intramuscular injections of 1 g of testosterone undecanoate in patients with hypogonadism was achieved in the interval from the 3rd to the 5th injection with the frequency of Nebido being administered once every 10 weeks. The average indicator of the maximum C _ss value of testosterone was about 42 nmol / L, the minimum - 17 nmol / L. T _1/2 (half-life) of testosterone is approximately 90 days, which corresponds to the rate of its release from the depot;
• Metabolism: Exogenous testosterone resulting from the cleavage of the ester bond from testosterone undecanoate is metabolized and excreted from the body using the same pathways as endogenous hormone. The metabolism of undecanoic acid occurs, as in other aliphatic carboxylic acids, by means of p-oxidation;
• excretion: Significantly metabolized in and outside the liver. After the introduction of labeled testosterone, up to 90% of radioactivity is determined in the urine in the form of glucuronide and sulfate acid conjugates, up to 6% is found in the feces after passing the intestinal-hepatic circulation. Urine metabolites contain androsterone and etiocholanolone.

Indications for use

According to the instructions, Nebido is prescribed for men with testosterone deficiency in primary and secondary hypogonadism (testosterone replacement therapy).

Contraindications

• Liver tumors (if indicated in history or currently);
• Androgen-dependent carcinoma of the mammary or prostate glands;
• Hypercalcemia accompanying malignant tumors;
• Age up to 18 years (due to the lack of the necessary data to assess the effectiveness and safety of the drug);
• Hypersensitivity to Nebido components.

Caution requires the appointment of Nebido in apnea syndrome.

Women should not use the drug.

Instructions for use of Nebido: method and dosage

Nebido is injected intramuscularly (do not allow the substance to enter the blood vessel), immediately after opening the package.

To maintain a sufficient level of testosterone (without cumulation of the substance), Nebido is administered once every 10-14 weeks at a dose of 1 g (contents of 1 ampoule or 1 bottle).

Before starting therapy, it is necessary to determine the value of testosterone in serum. The first interval between injections can be shortened, but it should not be less than 6 weeks. At a dose of 1 g, C _ss (steady-state concentration of the substance in the blood) is reached quickly.

At the end of the interval between Nebido injections, it is recommended to measure the serum testosterone concentration. Further therapy is adjusted depending on this indicator - at a level below normal values, it may be necessary to shorten the interval between injections, and vice versa. In this case, the interval should remain within the recommended range (10-14 weeks).

No dose adjustment is required for elderly patients.

Side effects

Most often, during the use of Nebido, the development of disorders such as pain at the injection site and acne was noted.

Side effects that occur during therapy (from? 1/100 to <1/10 - often, from? 1/1000 to <1/100 - infrequently):

• Cardiovascular system: often - hot flashes; infrequently - increased blood pressure, dysfunction of the cardiovascular system, hypertension, dizziness;
• Nervous system: infrequently - headache, tremor, migraine;
• Digestive system: infrequently - nausea, diarrhea;
• Lymphatic system and blood: often - polycythemia; infrequently - an increase in the number of erythrocytes and hemoglobin levels, an increase in hematocrit;
• Immune system: infrequently - hypersensitivity;
• Biliary tract and liver: infrequently - increased activity of aspartate aminotransferase, abnormalities in the "liver" tests;
• Urinary tract and kidneys: infrequently - dysfunction of the urinary tract, decreased urine output, dysuria, urinary retention, nocturia;
• Connective and musculoskeletal tissue: infrequently - pain in the limbs, arthralgia, musculoskeletal rigidity, muscle spasms, myalgia, muscle tension, increased activity of creatine phosphokinase in the blood;
• Breasts and genitals: often - benign prostatic hyperplasia, pathological results of examination of the prostate gland, increased levels of prostate-specific antigen; infrequently - prostatitis, intraepithelial neoplasia of the prostate, pain in the testicles, induration of the prostate gland, dysfunction of the prostate gland, increase or decrease in libido, gynecomastia, pain and induration in the mammary gland, increased levels of estradiol, testosterone and free testosterone in the blood;
• Subcutaneous tissue and skin: often - acne; infrequently - itching, dry skin, rash, alopecia, papular rash, erythema;
• Nutrition and metabolism: often - weight gain; infrequently - hypercholesterolemia, increased appetite, increased levels of triglycerides and cholesterol in the blood, as well as glycosylated hemoglobin;
• Organs of the mediastinum and chest, respiratory system: infrequently - sinusitis, bronchitis, dysphonia, cough, snoring, shortness of breath;
• Mind: infrequently - aggressiveness, depression, insomnia, disturbances in the emotional sphere, anxiety, irritability;
• Violations at the injection site and general disorders: often - various reactions at the injection site (in the form of pain, discomfort, itching, edema, hematoma, irritation at the injection site of Nebido); infrequently - asthenia, fatigue, night sweats, hyperhidrosis.

In rare cases, with microembolism of the pulmonary artery with oil solutions, the appearance of cough, shortness of breath, malaise, hyperhidrosis, chest pain, dizziness, paresthesia, or fainting may occur. As a rule, these disorders, developing during the injection or immediately after it, are reversible. During clinical and post-marketing studies, rare cases of fatty microembolism of the pulmonary artery were recorded.

There is evidence of the development of anaphylactic reactions after Nebido injections.

In addition, there is information about the development of nervousness, aggression, increased erections, sleep apnea, various skin reactions (including seborrhea), as well as isolated cases of jaundice.

Therapy with drugs containing high doses of testosterone, as a rule, leads to a reversible cessation or reduction of spermatogenesis and, accordingly, a decrease in testicular size. In rare cases, testosterone replacement therapy for hypogonadism can lead to persistent painful erections (priapism).

During high-dose or prolonged testosterone therapy, edema and an increase in fluid retention in the body can sometimes develop.

Overdose

Unintentional excess of the recommended dose requires a temporary cessation of the course or a reduction in the dose of Nebido. No other special therapeutic measures are required.

special instructions

Patients undergoing long-term androgen therapy should periodically check their hematocrit and hemoglobin levels to detect cases of polycythemia.

In elderly patients, the use of Nebido may increase the risk of prostatic hyperplasia. Also, the drug can promote the growth of an existing carcinoma, and therefore it is recommended to exclude it before prescribing treatment.

In rare cases, during the use of sex steroids, including testosterone, the development of benign liver tumors was noted, even less often - malignant ones, which can lead to the development of intra-abdominal bleeding. If there is severe pain in the upper abdomen, an enlarged liver, or symptoms of intra-abdominal bleeding, the likelihood of a liver tumor should not be excluded during differential diagnosis.

Patients prone to edema need to be careful when using Nebido, since treatment with androgens can lead to a delay in the excretion of sodium ions.

The use of testosterone in the treatment of patients under 18 years of age, along with masculinization, can lead to accelerated growth and maturation of bone tissue, as well as premature closure of the growth zone of the pineal gland and, accordingly, a decrease in the final growth.

When using Nebido, you need to consider the likelihood of developing the following conditions:

• The appearance of common acne;
• Strengthening existing sleep apnea syndrome;
• Decreased spermatogenesis (reversible).

Androgens should not be used to enhance performance and muscle development in healthy men.

To avoid pulmonary embolism (main symptoms: hyperhidrosis, cough, fainting, shortness of breath, paresthesia, malaise, dizziness, chest pain), Nebido should be administered slowly. With its development, supportive treatment is indicated, for example, additional oxygen is prescribed.

Taking Nebido can lead to virilization of a female fetus at some stages of development, however, there is no evidence of the risk of additional deterioration in organ development.

Influence on the ability to drive vehicles and complex mechanisms

Nebido does not adversely affect cognitive and psychophysical functions, due to which, during therapy, patients can drive vehicles and perform other potentially dangerous types of work.

Application during pregnancy and lactation

Nebido is not used to treat women.

Pediatric use

Due to the fact that so far, clinical trials of Nebido with the participation of children or adolescents under 18 years old have not been carried out, the drug is not used in pediatrics.

With impaired renal function

There are no data from formal studies of the use of Nebido in renal failure.

For violations of liver function

The use of Nebido is contraindicated in patients with current or history of liver tumors.

There are no data from official studies of the use of testosterone in liver failure.

Use in the elderly

Elderly patients should be prescribed Nebido with caution, since exogenous androgens may increase their risk of developing prostate adenoma.

Drug interactions

When Nebido is used in combination with certain drugs / substances, the following effects may be observed:

• Barbiturates and other enzyme inducers: increase in testosterone clearance;
• Oxyphenbutazone: an increase in its concentration in the blood serum;
• Oral anticoagulants: an increase in their activity (dose adjustment may be required; restrictions on intramuscular injections should always be observed in patients with hereditary or acquired bleeding disorders);
• Medicines with a hypoglycemic effect: an increase in the hypoglycemic effect of insulin (a decrease in the dose of a hypoglycemic agent may be required).

Due to the lack of data on compatibility, Nebido should not be mixed with other drugs.

Analogs

Analogs of Nebido are: Testosterone Propionate, Andriol, Androgel, Andriol TC, Sustanon 250, Omnadren 250.

Terms and conditions of storage

Keep out of reach of children at temperatures up to 25 ° C.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Nebido

According to reviews, Nebido is a very effective drug with a dosed action that quickly increases testosterone levels. Nebido's advantages are also noted for its dosing regimen, prolonged and less aggressive (fewer peaks) action.

Everyone considers the high price of the drug to be a disadvantage. A few reviews indicate such adverse reactions at the injection site, such as burning and pain.

Price for Nebido in pharmacies

The approximate price of Nebido (solution for intramuscular injection of 250 mg / ml) for 1 ampoule of 4 ml is from 4730 to 5470 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!