Nebido refers to the slow preparations of the male hormone testosterone, which, after oil intramuscular injection, slowly dissolve, maintaining a constant concentration of the hormone in the blood.
Androgen is in the medicine in the form of undecanoic acid ester, which breaks down in the body under the influence of the esterase enzyme into free testosterone and undecanoic acid.
The main reason for the use of testosterone Nebido is primary or secondary hypogonadism, leading to androgen deficiency.
The drug is also prescribed for the following diseasesresulting from a lack of testosterone in the body:
- male menopause
- delayed puberty and development in young men,
- male infertility with impaired spermatogenesis,
The main contraindication is individual intolerance, which can be expressed:
- frequent urge to cough,
- dyspnea - a failure of the respiratory rhythm, accompanied by a feeling of lack of air,
- excessive sweating
- chest pain
- dizziness and tachycardia.
It is forbidden to use Nebido with the following diseases:
- carcinoma of the prostate or mammary glands of androgen-dependent nature,
- hypercalcemia, which is the precursor of malignant tumors,
- liver tumors in the present tense or history.
After Nebido injection, caution should be exercised in patients with apnea (periodic falling of the airways in a dream, leading to temporary respiratory arrest).
Mode of application
The drug is produced by the German company Bayer Schering AG in ampoules or in glass bottles of dark glass of 4 ml, which contains 1 g of the main active substance. This is a single dose.
The medicine is injected into the body only intramuscularly. As a rule, in the buttock.
The main condition for injection is to avoid getting the needle into the blood vessel. It is fraught with thromboembolism of the lungs.
An injection is made as follows:
- open the ampoule or bottle,
- take medicine into a syringe,
- treat the injection site with alcohol to disinfect,
- the needle with the syringe is held perpendicular to the injection site,
- after the needle enters the muscle, the piston is pulled towards itself. If blood appeared in the syringe, then this means that the needle entered the vessel, the medicine cannot be administered at this point. In the absence of blood in the syringe, a very slow injection of the drug begins.
An injection should be done only in a specialized clinic.
After the injection, it is not recommended to immediately get up to avoid dizziness and fainting.
Then, within one and a half to two hours, the patient should be under the supervision of specialists to control overall well-being. Short-term possible at this time:
- bouts of weakness
- heart palpitations and pain behind the sternum,
- coughing fit.
As a rule, all these symptoms quickly disappear.
The level of testosterone undecanoate Nebido in blood plasma begins to rise the very next day after administration of the drug in the muscle, reaching a maximum value after 30 days. Then the level of male hormone reaches a plateau up to 65-70 days, after which it begins to decline slowly.
The application scheme of Nebido therefore implies one intramuscular injection with a content of the main active ingredient of 1 g, which is repeated every three months.
Treatment with Nebido suggests that the patient has a lack of testosterone in the body. Therefore, he needs to do an analysis on the content of this hormone every time before an injection, as well as on the 7th, 14th and 30th day after it.
The injection of the drug should be done immediately after opening the ampoule or vial in order to avoid ether oxidation in contact with atmospheric oxygen and under the influence of light.
Advantages and disadvantages of the drug
The main advantage of the drug is its effectiveness. Also, the advantages include:
- gradual impact, due to which the man’s body has time to reorganize to a new state
- dosed action. The quantity is calculated very accurately, overdose is excluded,
- pharmacological purity of the drug.
The main disadvantage of Nebido is its substitution effect, that is, with prolonged use, the body ceases to synthesize testosterone on its own. Also disadvantages include:
- high price,
- impossibility of independent use,
- the presence of a significant number of contraindications,
- possible development of side effects.
But with an organic lack of testosterone in the body of a man Nebido is one of the best treatment options.
A complete analogue of Nebido is a drug manufactured in the Netherlands, called Andriol. It also contains testosterone in the form of undecanoic acid ester. The difference is only in the dosage form. Andriol is available in tablet form.
Also, the analogues of Nebido include:
- Sustanon-250, made in Holland. The tool contains a complex of four testosterone esters.
- Omnadren -250 (Poland), also containing four ethers, but different from Sustanon-250.
- Androgel (Belgium) - produced in the form of a gel for external use. The drug contains pure testosterone.
But the most worthy and effective replacement for Nebido can be considered only Andriol, which also has a prolonged and dosed effect.
Feasible side effects
The development of side effects is possible in cases of:
- Individual intolerance (diarrhea, disruption of the heart muscle and respiratory rhythm failure, persistent pain behind the sternum).
In this case, you should wait until the termination of the drug, and then, with the help of a doctor, choose another drug to increase testosterone. Restructuring of the body systems to a new state (the appearance of acne, rash, joint pain, dizziness, headache and discomfort during urination).
After 7-10 days, the condition, as a rule, is normalized, all unpleasant symptoms change to good health and vitality.
After prolonged hormone replacement therapy, antiestrogen drugs - Anastrazole, Proviron, etc. can be recommended.
Can I get a prescription?
Nebido can be purchased in the pharmacy network only by prescription. To get it, you can contact:
- to the doctor endocrinologist at the place of residence,
- to the andrologist in any specialized clinic.
After collecting an anamnesis and a general examination, the doctor will give a referral to a blood test to determine the level of total testosterone in the blood. If the male hormone indicator is below normal, then the doctor will prescribe a prescription for Nebido in the absence of contraindications from the patient’s health.
The use of funds in bodybuilding
It is not recommended to use nebido for building muscle mass with a normal level of testosterone in the blood. The reasons for this are as follows:
- The intake of male hormone from an external source inhibits the body's production of endogenous androgen by the testes and adrenal glands. This leads to increased estrogen production, which can lead to gynecomastia, the formation of seals in the testicles and prostate gland.
- Violation of the natural hormonal balance can lead to emotional instability, neurosis, insomnia, which can adversely affect the training process.
The use of Nebido in bodybuilding can be justified only with a deficiency of testosterone after long intensive training once, under the supervision of a doctor.
Nebido - is a powerful, potent medicine of prolonged exposure. The drug is indispensable for testosterone deficiency in the body of a man caused by insufficient testicular function. It can be used only on the recommendation of a doctor in the absence of contraindications.
NEBIDO INFORMATION INFORMATION (TESTOSTERONE)
Common name: Testosterone (As Undecanoate)
Brand Name: Nebido®
Dose: 250 mg / ml
The form: Injection Solution (IM)
Packaging: 4 ml ampoule
Manufacturer: Bayer Pharma AG
Nebido® belongs to the group of male sex hormones - androgens. The drug is available in the form of an oil solution for parenteral administration. One ampoule with a volume of 4 ml contains 1000 mg of testosterone undecanoate. After intramuscular injection, Nebido® accumulates in muscle tissue. Slowly released from the depot, the drug produces a clinical effect. Testosterone, once in the bloodstream, has an androgenic effect on the testes, prostate gland, seminal vesicles, and also activates the synthetic function, enhances protein production in the liver, potentiates bone mineralization and muscle growth, and increases bone marrow function.
PRINCIPLE OF ACTION OF THE DRUG
Nebido® is prescribed to male patients with primary and secondary hypogonadism. Hypogonadism is a clinical syndrome caused by androgen deficiency - the inability of the testicles to produce enough testosterone and semen (or both components at the same time).
In addition to sexual and reproductive functions, testosterone regulates the functioning of skeletal muscles, mineralization of bone tissue, stimulates the production of energy, and is a regulator of positive mood. Hypogonadism develops as a result of violations of one or more levels in the chain of hypothalamic-pituitary-gonadal endocrine regulation. Primary hypogonadism can develop in men at any age. It is associated with a decrease in the function of the glandular tissue of the testicles due to disorders developing in the testicles themselves. Late (age-related) hypogonadism is caused by a violation of hypothalamic-pituitary regulation and is associated with age-related changes; it is characterized by a decrease in serum testosterone levels below 10–35 nmol / l (300–1000 ng / dl).
Symptoms of hypogonadism are individual. Hormonal insufficiency in late hypogonadism resembles the symptoms of aging, and therefore this condition is often not diagnosed. To eliminate hypofunction of the gonads, exogenous hormonal agents are used - derivatives of testosterone. Nebido® is prescribed for insufficient production of androgens, when the following clinical manifestations develop:
- decreased sexual desire (libido) and erectile dysfunction,
- difficulty reaching orgasm
- increased fatigue and drowsiness, decreased overall tone and energy,
- depression, anxiety, irritability,
- decreased attention span and memory function,
- decrease in muscle mass, strength and endurance,
- excessive sweating, mainly at night,
- pubic, trunk and face hair loss,
- insulin resistance
- decreased bone mineralization.
Men with low testosterone levels are also at increased risk of cardiovascular disease, diabetes and metabolic syndrome, osteoporosis.
|Intramuscular solution||1 amp (fl.) 4 ml|
|testosterone undecanoate||1000.0 mg|
|Excipients: benzyl benzoate - 2000.0 mg, purified castor oil for parenteral administration - 1180.0 mg|
Nebido® is an intramuscular depot preparation containing testosterone undecanoate, and for this reason there is no primary passage effect. After an intramuscular injection of an oil solution of testosterone undecanoate, it is gradually released from the depot and is almost completely cleaved by serum esterases into testosterone and undecanoic acid. An increase in serum concentrations of testosterone relative to baseline can be determined the very next day after injection.
After the first intramuscular injection of 1000 mg of testosterone undecanoate to men with hypogonadism, the average maximum concentration of testosterone was 38 nmol / L (11ng / ml) after 7 days. The second injection was carried out 6 weeks after the first, and maximum concentrations of testosterone of about 50 nmol / L (15ng / ml) were achieved. The standard interval of administration at 10 weeks was maintained during three subsequent administrations; equilibrium concentrations were achieved between the 3rd and 5th administration. The average values of Cmax and Cmin upon reaching the equilibrium concentration of testosterone were about 37 (11 ng / ml) and 16 nmol / l (5 ng / ml), respectively. The median inter- and intra-individual variability (coefficient of variation in%) of the minimum Cmin was 22% (range: 9-28%) and 34% (range: 25-48%), respectively.
In male blood serum, about 98% of circulating testosterone binds to sex hormone-binding globulin and albumin. Only the free fraction of testosterone is considered biologically active. After intravenous infusion of testosterone in older men, the apparent volume of distribution was determined at a level of approximately 1.0 L / kg.
Testosterone, formed from testosterone undecanoate as a result of cleavage of the ether bond, is metabolized and excreted from the body in the same ways as endogenous testosterone. Undecanoic acid is metabolized by -oxidation in the same way as other aliphatic carboxylic acids. The main active metabolites of testosterone are estradiol and dihydrotestosterone.
Testosterone undergoes significant metabolism in the liver and beyond. After the use of radiolabeled testosterone, about 90% of the radioactivity is observed in the urine in the form of glucuronide and sulfate conjugates, and 6% after passage of the intestinal-hepatic circulation is found in feces. Urinary products include androsterone and etiocholanolone. After intramuscular administration of the drug, the rate of release of the substance from the depot was characterized by a half-life of 90 + 40 days.
Testosterone undecanoate is a natural androgen ester, testosterone. The active form, testosterone, is formed as a result of the splitting of the side chain. Testosterone is the most important androgen in the male body and is synthesized mainly in the testes and, to a lesser extent, in the adrenal cortex. Testosterone is responsible for the formation of male signs during prenatal development, in early childhood, as well as during puberty, and subsequently for maintaining the male phenotype and androgen-dependent functions (e.g., spermatogenesis, additional sex glands). It also performs functions, in particular, in the skin, muscles, kidneys, liver, bone marrow and central nervous system.
Insufficient secretion of testosterone leads to male hypogonadism, which is characterized by low concentrations of testosterone in the blood serum. Symptoms associated with male hypogonadism include, but are not limited to, erectile dysfunction, decreased sex drive, fatigue, depressive moods, the absence, underdevelopment, or regression of secondary sexual characteristics, as well as an increased risk of osteoporosis, an increase in visceral fat mass, and a decrease in lean body mass. and muscle strength.
Nebido® is prescribed to increase insufficient levels of endogenous testosterone and reduce symptoms of hypogonadism.
Depending on the target organ, the nature of the action of testosterone is mainly androgenic (for example, in the prostate, seminal vesicles, epididymis) or protein-anabolic (in muscles, bones, hematopoietic system, kidneys, liver). The effect of testosterone in some organs appears after the peripheral conversion of testosterone to estradiol, which then binds to estrogen receptors in the nuclei of target cells (e.g., pituitary gland, adipose tissue, brain, bones, and testicular Leydig cells).
In men with hypogonadism, the use of Nebido® reduces the body fat mass, increases lean body mass, and also prevents bone loss. The drug can improve sexual function, as well as have a positive psychotropic effect by improving mood.
Pharmacodynamics and pharmacokinetics
Testosterone Undecanoate is an ether of natural testosterone.
Testosterone It is a sex hormone in men, possessing all types of biological activity necessary for maintaining and forming androgenic functions. It is formed in the testicles and in the adrenal cortex. Provides the formation of male characteristics during fetal development and in childhood, in adolescence - the development of secondary and primary sexual characteristics. The rest of the time it serves to maintain androgen-dependent functions and the male phenotype.
Insufficient biosynthesis testosterone leads to hypogonadismmanifesting erectile dysfunctionfatigue, weakening of sexual desire, depressive moods, reverse development of secondary sexual characteristics, osteoporosis.
Nature of the impacttestosterone depending on the target organ, it can be androgenic or protein-anabolic. Act testosterone in a number of organs manifests itself after transformation testosterone in estradiol.
In men with hypogonadismuse androgen reduces the amount of adipose tissue, increases lean body weight, stops bone regression. Androgens able to enhance sexual function and have a positive psychotropic effect.
After intramuscular injection testosterone undecanoate it is slowly released from the depot and completely cleaved esterasesserum onundecanoic acid and testosterone. Increased concentration of free testosterone can be fixed the very next day.
The onset of maximum concentration is 10-14 days. Protein binding in the serum of a man reaches 98%. The half-life of testosterone is about 90 days, which approaches its release rate from the depot.
Metabolized and excreted in the same way as natural testosterone. It undergoes a significant transformation in the liver and in other tissues. It is excreted in the urine in the form of conjugates and through the intestines.
- Most common acne and pain in the area of administration.
- Reactions from blood: polycythemiaincrease hematocrit, erythrocytosis, level increase hemoglobin.
- Reactions from immunity: development is possible reactionshypersensitivity.
- Reactions from metabolism: increase in body weight, increased appetite, hypercholesterolemiaincreasing concentration glycosylated hemoglobinlevel increase triglycerides in plasma.
- Reactions from psycheaggressiveness depression, anxiety, insomniairritability.
- Reactions from nervous activity: migraine, headache, tremor.
- Reactions from blood circulation: pressure increase, hypertensiontides dizziness.
- Reactions from breathing: snoring bronchitiscough sinusitis, dyspnea, dysphonia.
- Reactions from digestion: nausea diarrheachanges in liver counts.
- Reactions from skin: alopecia, acne, erythema, papular rash, rash, dry skin, itching.
- Reactions from musculoskeletal system: pain in the limbs, arthralgia, muscle spasms, myalgiamuscle tension, increased activity creatine phosphokinase, rigidity.
- Reactions from genitourinary sphere: urinary retention, decreased urine output, nocturia, dysuria,increase in content prostate specific antigen, prostate adenomapathological results of a study of the prostate gland, prostate intraepithelial neoplasiaprostate tightening, increase or decrease libido, prostatitis, pain in the testicles or in the mammary gland, increased content estradiol, gynecomastiaincreasing content testosterone in blood.
- Local reactions: discomfort, pain, itching, hematoma, edemairritation in the area of administration.
- General reactions: hyperhidrosisfatigue asthenia, sweating.
Microembolism with oily solutions of the pulmonary artery can in very rare cases cause shortness of breath, cough, malaise,chest pain, hyperhidrosis, paresthesia, dizziness, fainting. These reactions are reversible.
High Testosterone Therapy Causes a Reversible Decrease spermatogenesis and a decrease in the testicles, as well as swelling.
Instructions for use (Method and dosage)
The instruction on Nebido recommends making one injection of the drug in a dose of 1 gram (1 ampoule) every 3-4 months. At the indicated injection frequency, an adequate level is maintained. testosterone and no cumulation of the substance is observed.
Nebido is administered strictly intramuscularly immediately after opening the ampoule. The introduction should be made as slowly as possible. It is necessary to ensure that the drug does not end up in a blood vessel.
Content should also be defined. testosterone in the blood before starting therapy. The first interval between injections is usually shortened, but is not less than 6 weeks.
At the end of each break between injections, it is advised to measure the content testosterone in blood. These values can be corrected by changing the interval between administrations.
Androgens may cause an increase in content oxyphenbutazone in serum.
Reception with activating drugs microsomal enzymes (barbiturates)causes an increase in clearance testosterone.
Testosterone able to enhance effects oral anticoagulants.
Under influence androgen likely gainhypoglycemic actions insulin.
Persons on long-term therapy androgens, it is advised to periodically monitor the level hemoglobin and hematocrit.
Using androgenfor the treatment of the elderly it is possible to increase the risk of prostatic hyperplasia. Also androgens can contribute to the development of existing prostate carcinomas.
Against the background of use testosterone in extremely rare cases, malignant and benign liver tumors were detected that could lead to intra-abdominal bleeding. If the liver enlarges during treatment with the drug, severe pains appear in the upper abdomen or symptoms of intra-abdominal bleeding, then cancer of the liver should be excluded.
Sleep Apnea Syndromewhile taking the drug may increase.
Androgens should not be used to enhance muscle growth in healthy individuals and to increase physical abilities.
Replacement treatment testosterone may temporarily lower spermatogenesis.
The drug does not change the ability to control mobile mechanisms.
Special security measures
The injection should be visually tested before use. Only clean solutions that do not contain visible particles are allowed. This medicine is intended for single use only. Any unused drug residues must be disposed of in accordance with local regulations.
Instructions for working with ampoules with a tip that breaks off, and a break point:
Thanks to the previously applied notch under the colored dot on the ampoule, there is no need to file the tip of the ampoule. Before opening the ampoule, make sure that the entire solution has moved from the top of the ampoule to the bottom. Opening the ampoule with both hands. Holding the bottom of the ampoule with one hand, with the other hand, break off the top of the ampoule, starting from the indicated point.
Vials are intended solely for single use of the drug.
According to the American Association of Clinical Endocrinologists and the American College of Endocrinologists for 2016, the overall prevalence of obesity in the adult population is 71%. At the same time, 50–80% of obese men have testosterone deficiency. The most common concomitant pathology among the obese population is type II diabetes (about half of all men with type II diabetes have hypogonadism).
The clinical guidelines of the American Association of Clinical Endocrinologists (AACE) and the American College of Endocrinologists (ACE) for 2016 noted:
- All men with a waist circumference of ≥102 cm or in the presence of obesity (BMI ≥30 kg / m²) are subject to examination to exclude hypogonadism. For this, a thorough history is taken, a physical examination, determination of the level of testosterone in the blood serum. Also, all men with hypogonadism should be evaluated for overweight or obesity.
- All men with type II diabetes should be tested to rule out testosterone deficiency.
- Treatment for hypogonadism in men with increased waist circumference or obesity should include weight loss therapy. Weight loss of more than 5–10% is necessary to normalize serum testosterone levels.
- Men with hypogonadism and obesity who are not seeking fertility can be considered as applicants for Nebido® treatment. Testosterone therapy in these patients leads to weight loss, decreased waist circumference, improved metabolic parameters of glucose, HbA 1C, and lipid profile.
According to clinical studies in 2016, long-term testosterone therapy (for up to 10 years) is safe and steadily improves the cardiovascular system, lipid profile, glycemic profile, normalizes blood pressure, heart rate, and cardiac output fraction.
The drug Nebido can be used exclusively in cases of confirmed (hypo- or hypergonadotropic) hypogonadism and only after preliminary exclusion of other possible causes that may be due to existing symptoms. Testosterone deficiency should be clearly manifested clinically (a decrease in the severity of secondary sexual characteristics, changes in body structure, asthenia, a decrease in sexual desire, erectile dysfunction) and be confirmed by two separate measurements of the level of testosterone in the blood.
With extreme caution, testosterone should be used in patients with arterial hypertension, epilepsy or migraine, diabetes mellitus, since these diseases can worsen.
With excessive sexual stimulation, the drug must be discontinued.
The experience of using Nebido in patients over the age of 65 is insignificant. There is no single point of view regarding the age norms of testosterone levels. However, it should be borne in mind that with age, the physiological level of testosterone in serum decreases.
Before starting therapy with testosterone, all patients must undergo a thorough medical examination to exclude existing prostate cancer. In patients receiving testosterone treatment, it is necessary to regularly and thoroughly check the status of the prostate and mammary glands using generally accepted research methods (digital rectal examination, monitoring of serum specific prostate antigen (PSA) level) at least once a year or 2 times a year for elderly patients and special categories of patients (with clinical or hereditary risk factors).
In addition to laboratory monitoring of testosterone concentrations in patients undergoing long-term androgen therapy, it is also necessary to regularly determine the following parameters: hemoglobin, hematocrit and functional liver tests (see section “Adverse reactions”).
Through the variability of laboratory parameters, all measurements of testosterone levels are recommended in one laboratory.
Androgens can accelerate the development of subclinical prostate cancer and benign prostatic hyperplasia.
Caution should be used in applying Nebido to patients with cancer with a risk of developing hypercalcemia (and the associated hypercalciuria) caused by bone metastases. It is recommended that you regularly monitor serum calcium levels in these patients. Cases of benign and malignant liver tumors have been reported in individuals taking hormonal substances, in particular androgenic compounds. If a man who is receiving Nebido treatment has severe pain in the upper abdomen, an enlarged liver, or there are signs of intra-abdominal bleeding, with a differential diagnosis, it is necessary to exclude a possible tumor of the liver.
In patients with severe heart, liver or kidney failure or coronary heart disease, testosterone therapy can cause severe complications, characterized by edema, which may or may not be associated with congestive heart failure. In this case, it is necessary to immediately stop the therapy. Studies to study the efficacy and safety of the drug with the participation of patients with impaired renal or hepatic function have not been conducted. According to testosterone replacement therapy, such patients should be treated with caution.
Caution must be exercised in patients who are prone to edema, since treatment with androgen group drugs can lead to an increase in sodium retention (see section “Adverse Reactions”).
Existing sleep apnea syndrome may worsen.
Following the appointment of Nebido, there were reports of suspected anaphylactic reactions.
According to the basic rules, it is necessary to comply with the conditions for performing intramuscular injections in patients with acquired or congenital bleeding disorders.
Caution should be used in applying Nebido to patients with epilepsy or migraine, due to the possible worsening of these conditions.
In patients who receive androgens and in the achieved normal levels of testosterone in blood plasma after replacement therapy with testosterone, an increase in insulin sensitivity may be observed.
Certain clinical symptoms, such as irritability, nervousness, weight gain, persistent or frequent erections may indicate an overdose of androgen and require dose adjustment.
If symptoms of hyperandrogenism persist or recover during therapy in the recommended dosage regimens, the use of Nebido should be temporarily discontinued.
Like injections of all oil solutions, injections of Nebido should be carried out accurately and very slowly (within 2 minutes) intramuscularly.
The usual dose of maintenance therapy, for example, the appointment of additional oxygen therapy.
Androgens should not be used to enhance muscle development in healthy subjects, as well as to increase physical abilities.When using Nebido, possible positive results of doping control. The health consequences of using Nebido as a dope are unpredictable, the possibility of a serious threat to health is not ruled out (see section “Adverse reactions”).
MODE OF APPLICATION
Nebido® is used parenterally. The drug is administered intramuscularly slowly, after checking for the absence of a needle in the lumen of the vessel.
Nebido® oily solution is prohibited for intravenous use!
The dose of the drug is calculated individually, depending on the degree of hypogonadism and the concentration of testosterone in the serum of peripheral blood. Typically, the contents of the ampoule (4 ml of solution) is administered once 1 time in 10-14 weeks. Such a dosage allows you to maintain the necessary level of male sex hormones in the blood without their excessive deposition in the body.
With intravascular administration of the drug, a formidable complication is possible - fatty embolism of the pulmonary arteries. When using high doses of the drug, inhibition of spermatogenesis and testicular hypotrophy are periodically observed, in elderly patients, the risk of developing benign prostatic tissue hyperplasia is increased.
During Nebido® therapy, painful discomfort in the testicles is sometimes observed, while the level of PSA, free and bound testosterone in the blood serum can increase.
Intramuscular administration of Nebido® may cause local reactions in the form of soreness, skin rashes at the injection site. Allergic reactions to the components of the drug, as well as dryness, peeling and itching of the skin may be noted.
Among the undesirable effects when using Nebido® are increased appetite and weight gain, increased levels of AST, cholesterol, LDL and triglycerides in the blood serum. From the side of the central nervous system, the appearance of a cephalgic syndrome, migraine attacks, soreness and tremor of the muscles of the extremities, emotional lability. Vascular reactions in the form of a feeling of heat, redness of the face, fluctuations in blood pressure indicators are less commonly observed. The drug activates hematopoiesis, in connection with which hyperproduction of all hematopoietic bone marrow growths can be noted, which is expressed by polycythemia, an increased content of hemoglobin in peripheral blood.
The drug is contraindicated for use in women and boys under 18 years of age. Nebido® should not be prescribed to patients with prostate cancer and breast carcinoma, the presence of tumor-like liver diseases.
The drug is not recommended for use as an anabolic agent during sports with the goal of hypertrophic muscle growth.
WHERE COULD I BUY?
You can buy Nebido in Moscow in pharmacies according to the prescription prescribed by the doctor. The signature is necessary for the correct selection of the dose and the optimal frequency of administration of the drug. At the same time, the price of Nebido in a pharmacy can vary significantly, depending on the place of residence. Sometimes it’s impossible to buy Nebido at a pharmacy, especially in remote regions. In central pharmacies, it is also not always available. You can buy Nebido by ordering it at an online pharmacy. The cost of testosterone in this case can be 10-15% lower than the retail price. In order to buy Nebido with delivery and protect yourself from unscrupulous sellers, you should place an order with cash on delivery. To buy testosterone in Moscow online, you must sequentially enter the words “buy nebido 1000 mg in Moscow” in the browser’s search line, find the online pharmacy using the links provided and place an order. To select the optimal price of the drug Nebido, you can use the phrase "nebido 1000 mg discount price." The operational logistics of drug delivery through online resources allows you to buy Nebido in Moscow quickly enough and at the best price.
For undesirable effects associated with the use of androgens, see "Features of use."
Common side effects that occur with Nebido are acne and pain at the injection site.
Table 1 shows the adverse reactions associated with the use of Nebido according to MedDRA by organ system class (MedDRA SOCs, version 11.0) *. The following adverse reactions recorded during clinical trials using the drug are distributed according to the frequency of occurrence according to the following gradation: often (≥1 / 100, 1 Skin rashes, including nodular
2 Muscle Disorders: muscle cramps, muscle tension and myalgia
In rare cases, pulmonary microembolism with oily solution can lead to the development of signs and symptoms such as coughing, shortness of breath, general malaise, hyperhidrosis, chest pain, dizziness, anxiety, paresthesia, or fainting.
Shelf life 5 years.
TREATMENT OF OTHER FORMS OF DISEASES
The drug can be used as an adjuvant for the comprehensive medical correction of male infertility, as well as to stimulate the synthetic function of the liver in debilitated patients after severe surgical interventions, burn disease, sepsis and other pathological conditions. In this case, the drug is prescribed for a short time, the dosage is selected individually. In this case, testosterone treatment is not in the nature of replacement therapy and is carried out exclusively under the supervision of a doctor.
ANALOGUES, SUBSTITUTES, GENERICS
Available on the pharmaceutical market androgens for replacement therapy are presented in the table.
|Trade name||Active substance|
|Metadren, Androral, Glosso-Sterandril, Hormal, Madiol, Malogen||Methyltestosterone|
|Andriol, Nouveau||Testosterone undecanoate|
|Agovirin, Androfort, Androlin, Andronat, Homesterone, Malestron, Oreton F, Prenandren, Sterandril||Testosterone propionate|
|Testenat, Testosterone Depot||Testosterone Enanthate + Testosterone Propionate|
|Sustanon-250, Omnadren-250||Testosterone - solution in oil for injection (combined mixture of esters)|
NEBIDO: INSTRUCTIONS FOR USE
Before you start using the drug Nebido® (testosterone), you must read the instructions for use of the drug. The drug has a number of side effects and contraindications, which must be considered when using it. A full description of Nebido®, as well as information on the pharmacological properties and clinical effects of the drug are indicated in the annotation.
Suction. Nebido ® is an intramuscular depot preparation containing testosterone undecanoate. For this reason, the effect of the first passage is absent. After a / m injection of an oil solution of testosterone undecanoate, it is gradually released from the depot and is almost completely cleaved by serum esterases into testosterone and undecanoic acid. An increase in serum concentrations of testosterone relative to baseline can be determined the very next day after injection.
Distribution. In two separate studies, the mean Cmax testosterone, comprising 24 and 45 nmol / l, were determined, respectively, 14 and 7 days after a single IM injection of 1000 mg of testosterone undecanoate in men suffering from hypogonadism. Postmaximal testosterone levels decreased, with T1/2 was approximately 53 days.
About 98% of circulating testosterone binds in the blood serum to sex steroid-binding globulin and albumin. Only the free fraction of testosterone is considered biologically active. After iv administration of testosterone to older men, apparent Vd measured at approximately 1 l / kg.
Metabolism. Testosterone, formed from testosterone undecanoate as a result of cleavage of the ether bond, is metabolized and excreted from the body in the same ways as endogenous testosterone. Undecanoic acid is metabolized by β-oxidation in the same way as other aliphatic carboxylic acids.
Breeding. Testosterone undergoes significant metabolism in the liver and beyond. After the administration of labeled testosterone, about 90% of the radioactivity is determined in the urine in the form of glucuronide and sulfate acid conjugates, and 6% after passage of the intestinal-hepatic circulation is found in feces. Urinary products include androsterone and etiocholanolone.
Equilibrium concentration. After repeated i / m injections of 1000 mg of testosterone undecanoate to men suffering from hypogonadism, at an interval between injections of 10 weeks, an equilibrium concentration was reached between the 3rd and 5th injections. The average values of Cmax and Cmin testosterone in equilibrium were about 42 and 17 nmol / L, respectively. Postmaximal serum testosterone levels decreased with T1/2 equal to approximately 90 days, which corresponds to the rate of release of the substance from the depot.
Solution for intramuscular injection, 250 mg / ml.
Ampoules. 4 ml of the drug in an amber glass ampoule of type I.
Bottles. 4 ml of the drug in a bottle of dark glass type I, with a rubber stopper, rolled in an aluminum cap with a plastic cap.
At 1 amp. or fl. placed in a cardboard box with glued cardboard holder.