Nebido Injection 250mg / ml amp 4ml 1 piece

Description

Composition
Active substance:
1 ampoule or vial (4 ml) contains: active substance testosterone undecanoate – 1000.0 mg ,.
Excipients:
Benzyl Benzoate – 2000.0 mg, castor oil refined for parenteral administration – 1180.0 mg.
Description:
The clear oily solution with a yellowish tinge.
Product form:
A solution for intramuscular injection of 250 mg / ml.
Ampoules: 4 ml of the preparation in the vial of amber glass type I.
Vials: 4 mL of the preparation in the vial of dark glass type I, with rubber stopper, aluminum cap with run-plastic lid.
1 ampoule or vial with instructions for use in a cardboard bundle c glued cardboard holder.
Contraindications
Nebido® The drug should not be used in the presence androgenozavisimoy prostate carcinoma or mammary glands in males; hypercalcemia accompanying malignant tumors; liver tumors at the present time or history; hypersensitivity to active substance or any of the auxiliary components of the preparation.
Nebido® The drug should not be used in women.
With care – in patients with sleep apnea syndrome; in hypertensive men – in patients with severe hepatic, renal and heart failure, coronary artery disease, symptoms of edema; – in patients with epilepsy; – in patients with migraine; – in patients with thrombophilia.
Indications
Testosterone deficiency in primary and secondary hypogonadism in men (testosterone replacement therapy).
Interaction with other drugs
With drugs that induce hepatic microsomal enzymes
Possible interactions with drugs that induce microsomal enzymes (e.g., barbiturates), which may lead to an increase in testosterone clearance.
With oxyphenbutazone.
It reported an increase in serum concentrations of oxyphenbutazone.
With indirect oral anticoagulants.
Testosterone and its derivatives can enhance pharmacological effects of indirect oral anticoagulants, coumarin derivatives that may lead to the need to adjust dosages.
Regardless of these data, as a general rule always necessary to consider the risk of bleeding when administered intramuscularly to patients with acquired or inherited bleeding disorders. Patients receiving therapy with indirect oral anticoagulants should be closely monitored: the regular determination of the concentration of prothrombin, and the international normalized ratio (INR), especially at the beginning and end of the testosterone therapy.
With hypoglycemic drugs.
Androgens may enhance the hypoglycemic effect of insulin. It may be necessary to reduce the dose of hypoglycemic medication.
With other drugs.
While the use of ACTH (adrenocorticotropic hormone) and corticosteroids increase the risk of edema.
Since compatibility studies have been conducted, do not mix the drug with other drugs.
Influence the results of certain lab tests.
Androgens can reduce the concentration of thyroxine binding globulin, resulting in a reduction of total T4 and T3 and T4 increased absorption (binding test resin). However, the concentration of free thyroid hormones remain unchanged, and the clinical data of thyroid dysfunction is not.
Overdose
No specific therapeutic measures, except for the temporary cessation of therapy or reduce the dose, an overdose is not required.
pharmachologic effect
Pharmacological group:
Androgen.
Pharmacodynamics:
Testosterone undecanoate is an ester of the natural androgen, testosterone. The active form, testosterone, is formed by the cleavage of the side chain.
Testosterone is the most important androgen in men and is synthesized mainly by the testes and, to a lesser extent by the adrenal cortex.
Testosterone is responsible for the formation of male characteristics during fetal development in early childhood and puberty, and subsequently for maintenance androgenozavisimyh male phenotype and functions (e.g., spermatogenesis, gonads). Inadequate secretion of testosterone results in male hypogonadism, which is characterized by low concentrations of testosterone in the serum. Symptoms associated with male hypogonadism, among other things, include erectile dysfunction, decreased libido, fatigue, depressed mood, lack, underdevelopment or regression of secondary sexual characteristics, as well as an increased risk of osteoporosis. Exogenous Androgens are assigned in order to improve insufficient levels of endogenous testosterone and reduce symptoms of hypogonadism.
Depending on the target organ character action of testosterone is mainly androgenic (e.g., prostate, seminal vesicles, epididymis) or protein-anabolic (muscle, bone, blood system, kidney, liver).
Actions of testosterone in some organs are shown after peripheral conversion of testosterone to estradiol, which then binds to the estrogen receptor in the nuclei of target cells (e.g., the pituitary, adipose tissue, brain, bone and testicular leydigovskih cells).
In men suffering from hypogonadism, androgen use reduces the mass of body fat, increase lean body mass and prevent bone loss. Androgens may improve sexual function, as well as have a positive impact by improving psychotropic mood.
Pharmacokinetics:
Suction.
Preparation Nebido® represents intramuscular depot formulation containing testosterone undecanoate. For this reason, there is no effect of the first passage. After intramuscular injection of an oil solution of testosterone undecanoate it is gradually released from the depot and is almost completely cleaved by esterases in the serum testosterone and undecanoic acid. The increase in serum testosterone concentrations in relation to baseline values ​​can be determined on the next day after the injection.
Distribution.
In two separate studies mean maximum testosterone concentration of 24 and 45 nmol / l, determined, respectively, at 14 and 7 days after single intramuscular injection of 1000 mg of testosterone undecanoate men suffering from hypogonadism. Postmaksimalnye testosterone levels declined, while the half-life was about 53 days.
About 98% of circulating testosterone is bound to serum albumin and to SHBG. It is considered to be biologically active only the free fraction of testosterone.
After intravenous administration of testosterone elderly men apparent volume distribution was determined at approximately 1.0 L / kg.
Metabolism
Testosterone is produced from testosterone undecanoate as a result of splitting the ester bond, metabolized and excreted by the same pathways that endogenous testosterone. Undecanoic acid is metabolized by beta-oxidation as well as other aliphatic carboxylic acids.
Withdrawal.
Testosterone undergoes considerable metabolism in the liver and beyond. After administration of testosterone labeled about 90% of the radioactivity is determined in urine as glucuronide and sulfate conjugates of acid, and 6% after passing kishechnopechenochnoy circulation is found in the faeces. Defined in the urine products include androsterone and etioholanolon.
The equilibrium concentration.
After repeated intramuscular injections of 1000 mg of testosterone undecanoate men suffering from hypogonadism, with the interval between injections in the 10 weeks, the equilibrium concentration achieved between the 3rd and 5th injections. The average maximum and average minimum testosterone concentration at steady state is about 42 and 17 nmol / L, respectively. Postmaksimalnye testosterone serum levels declined with a half-life of about 90 days, which corresponds to the rate of release of a substance from the depot.
Conditions of supply of pharmacies
On prescription.
side effects
The most commonly in the treatment of drug Nebido® observed undesirable effects such as acne and pain at the injection site.
The frequency of occurrence of HP determined in clinical trials, and is classified as follows: very often> 1/10, often> 1/100 to 1/1000 to 1/10000 to
From the blood and lymphatic system: often-polycythemia; infrequently-elevated hematocrit, an increase in the number of red blood cells, elevated levels of hemoglobin.
Immune system: Infrequent-hypersensitivity.
On the part of metabolism and nutrition: often, weight gain; infrequently, increased appetite, increased content of glycosylated hemoglobin, hypercholesterolemia, elevated blood triglyceride levels, increase. the concentration of cholesterol in the blood
Mental disorders: rarely, depression, disturbances in the emotional sphere, insomnia, anxiety, aggressiveness, irritability.
From the nervous system: Infrequent, headache, migraine, tremor.
With the cardiovascular system: often-tides; infrequently-dysfunction of the cardiovascular system, increased blood pressure, increased blood pressure and dizziness.
The respiratory system, thorax and mediastinum: Infrequent, bronchitis, sinusitis, cough, shortness of breath, snoring, dysphonia.
On the part of the gastrointestinal tract: rarely, diarrhea, nausea.
Of the liver and biliary tract: rare-deviation “liver” tests, increased activity aspartataminotrasferazy (AST).
Skin and subcutaneous tissue disorders: acne often; infrequently, alopecia, erythema, rash, maculopapular rash, pruritus, dry skin.
On the part of the musculoskeletal and connective tissue disorders: uncommon, arthralgia, pain in limbs, muscle spasms, muscle tension, myalgias, skeletal muscle rigidity, increased creatine kinase activity in the blood.
The kidneys and the urinary tract: rare-reduction urine volume, urinary retention, impaired urinary function, nocturia, dysuria.
On the part of genitals and mammary glands: the often-increasing prostate-specific antigen level, pathologic results of the examination of the prostate, benign prostatic hyperplasia; infrequently-prostatic intraepithelial neoplasia, seal, prostatitis, impaired function of the prostate gland, increase libido, decreased libido, pain in the testicles, breast pain, induration in the mammary gland, gynecomastia, increased concentrations of estradiol, increase free testosterone concentration in the serum blood, increasing the concentration of testosterone in the blood serum.
General disorders and the site of injection: often, different kinds of injection site reactions (pain, discomfort, itching, swelling, bruising, irritation at the injection site); infrequently, fatigue, asthenia, hyperhidrosis, night sweats.
Microembolisms pulmonary artery oily solutions can in rare cases lead to the emergence of a number of signs and symptoms, such as cough, dyspnea, malaise, hyperhydrosis, chest pain, dizziness, paraesthesia, or syncope. These reactions may develop during injection or immediately after it, and are reversible. In clinical trials, as well as in the post-marketing period, recorded rare (> 1/10000, and
There are reports of anaphylactic reactions following injection Nebido® drug.
Along with the above adverse reactions during treatment with drugs testosteronsoderzhaschimi reported nervousness, aggression, sleep apnea, various skin reactions (including seborrhea), hair growth enhancing, frequent erections, as well as rare cases of jaundice development.
drug therapy high testosterone usually causes reversible reduction or cessation of spermatogenesis, which reduces the size of the testicles.
Testosterone replacement therapy of hypogonadism can in rare cases cause persistent painful erection (priapism).
Prolonged or vysokodozirovannaya testosterone therapy can sometimes lead to increased incidence of fluid retention and edema.
special instructions
In the application of androgen risk of prostatic hyperplasia may be increased in elderly patients. Despite the lack of data that androgens can cause carcinoma of the prostate, they can promote the growth of existing carcinomas. Before starting treatment with preparations containing testosterone, to exclude prostate carcinoma. As a precaution it is recommended to have regular prostate examinations.
In order to eliminate benign hyperplasia and subclinical prostate cancer recommend that the digital rectal examination of the prostate and determination of the concentration of prostate-specific antigen (PSA) at least 1 time per year, and in elderly patients and patients with cancer risk factors for prostate cancer (the presence of family history, etc.) – not less than 2 -x once a year.
In patients on long-term androgen therapy is recommended regular determination of hematocrit and hemoglobin in order to detect cases of polycythemia (see. Section “Side effects”), as well as liver enzymes and lipid profile. The therapy is recommended for laboratory examinations in the same laboratory.
As a general rule you must always take into account the risk of hemorrhage following intramuscular injection of the drug in patients with acquired or inherited bleeding disorders. It reported that testosterone and its derivatives can enhance pharmacological effects of indirect oral anticoagulants, coumarin derivatives (see. See “The interaction with other drugs”).
Testosterone should be used with caution in patients with thrombophilia, as in post-marketing studies have been reported cases of thrombosis during therapy with testosterone preparations in these patients.
Against the background of sex hormone drugs, which include testosterone, observed benign and malignant tumors of the liver, which can lead to intra-abdominal haemorrhage.
When the therapy drug Nebido® severe pain in the upper abdomen, or signs of liver enlargement intraabdominal bleeding in the differential diagnosis should take into account the probability of the presence of liver tumor.
Caution should be exercised in patients who are prone to edema, for example, in the case of severe cardiac, hepatic or renal insufficiency or ischemic heart disease. Use of testosterone may cause sodium and water retention. In case of severe complications characterized by edema with or without congestive heart failure, therapy should be discontinued immediately (see. Section “Side effects”).
Nebido® drug should be used with caution in men with hypertension because testosterone may cause increased blood pressure.
Nebido® drug should be used with caution in patients with epilepsy and migraine, as the possible worsening of these diseases.
Use of the drug in boys and young adolescents under the age of 18 years is contraindicated due to a lack of data on the efficacy and safety of testosterone use in this age group.
Existing sleep apnea may be exacerbated during sleep.
Androgens are used to enhance muscle development in healthy subjects as well as for increasing physical ability.
Guidelines for drug administration: injection Nebido® preparation should be done very slowly (over 2 minutes).
Nebido® drug should be administered only intramuscularly (deep into the gluteal muscle).
The concentration of testosterone must be checked regularly throughout the treatment period (considering the physiological decrease of testosterone concentration with age). When testosterone replacement therapy requires an individual adjustment of the frequency of injection (see. The section “Method of administration and dose”).
There are reports of anaphylactic reactions following injection Nebido® drug.
fertility
Testosterone replacement therapy may reversibly reduce spermatogenesis (see. Section “Side effects”).
Effects on ability to drive vehicles and moving machinery.
Nebido® The drug has no effect on ability to drive and moving mechanisms that require attention.
Storage conditions
At temperatures above 25 ° C.
Keep out of the reach of children!.
Dosing and Administration
Nebido® Injection formulation (1 vial or vial contained 1000 mg of testosterone undecanoate) is done once at 10 – 14 weeks. At this frequency is provided by maintaining a sufficient injection of testosterone and there is no accumulation of the substance.
The contents of ampoules or vials should be administered intramuscularly immediately after opening. Injection should be done very slowly (about 2 minutes). A drug
Небидо® можно вводить только строго внутримышечно. Необходимо тщательно следить за тем, чтобы вводимое вещество не попало в сосуд.
Для флакона: после снятия пластмассовой крышки не снимайте резиновую пробку, обкатанную алюминиевым колпачком.
Начало лечения.
Перед началом лечения следует определить величину содержания тестостерона в сыворотке крови. Первый интервал между инъекциями может быть сокращен, но он должен составлять не менее 6 недель. Равновесная концентрация при такой дозе достигается быстро.
Индивидуальная корректировка лечения.
В конце интервала между инъекциями рекомендуется измерять концентрацию тестостерона в сыворотке крови. Если его концентрация ниже нормальных показателей, то это может свидетельствовать о необходимости сокращения интервала между инъекциями.
При высоких концентрациях следует рассмотреть вопрос о целесообразности увеличения данного интервала. Интервал между инъекциями должен оставаться в пределах рекомендуемого диапазона 10 – 14 недель.
Особые категории пациентов.
Дети и подростки.
Препарат Небидо® не предназначен для применения у детей и подростков, поскольку для него не проводились клинические исследования у мужчин в возрасте до 18 лет (см. раздел «Особые указания»).
Elderly patients
Имеющиеся ограниченные данные не указывают на необходимость корректировки дозы у пациентов пожилого возраста (см. раздел «Особые указания»).
Patients with impaired liver function.
Никаких официальных исследований у пациентов с нарушениями функции печени не проводилось. Использование препарата Небидо® противопоказано у мужчин с опухолями печени в настоящее время или в анамнезе (см. раздел «Противопоказания»).
Пациенты с почечной недостаточностью.
Никаких официальных исследований у пациентов с почечной недостаточностью не проводилось.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist