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enanthate testosterone

enanthate testosterone

Enanthate testosterone – a semisynthetic cephalosporin antibiotic III generation broad-spectrum.The bactericidal activity of enanthate testosterone due to suppression of the synthesis of cell membranes.Enanthate testosterone – a derivative of the basic penicillin nucleus. It is an irreversible inhibitor of beta-lactamases, which are released by microorganisms resistant to beta-lactam antibiotics; prevents degradation of penicillins and cephalosporins by the action of beta-lactamase-resistant microorganisms; binding to penicillin binding proteins, exhibits synergism when applied simultaneously with penicillins and cephalosporins.

Enanthate testosterone has no clinically significant antibacterial activity (with the exception of Neisseriaceae and Acinetobacter spp.). Sulbactam interacts with certain proteins penitsillin¬svyazyvayuschimi, so the combination of enanthate testosterone + [sulbactam] often has a more pronounced effect on the sensitive strains than one enanthate testosterone.

The combination of enanthate testosterone + [sulbactam] is active against all organisms sensitive to enanthate testosterone, and acts synergistically (reduced to 4 times the minimum inhibitory concentration (MIC) of the combination compared with enanthate testosterone).

It is active against the following microorganisms:

Gram-negative aerobes: of Acinetobacter lwoffii, of Acinetobacter anitratus *, the Aeromonas hydrophila, of Alcaligenes faecalis, of Alcaligenes odorans, of Borrelia burgdorferi, Capnocytophaga spp, Citrobacter diversus, Citrobacter freundii **, of Escherichia coli, of Enterobacter aerogenes *, of Enterobacter cloacae *, of Enterobacter spp *,.. Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae , Hafnia alvei, Klebssiella oxytoca, Klebssiella pneumoniae **, Moraxella catarrhalis, Moraxella osloensis, Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris *, Proteus penneri *, Pseudomonas fluorences *, Pseudomonas spp., Providencia spp., including Providencia rettgeri *, Salmonella spp. (netifoidnye), Salmonella typhi, Serratia spp. *, including Serratia marcescens *, Shigella spp., Vibrio spp., Yersinia spp., Including Yersinia enterocolitica.

* Some isolates of these species are resistant to enanthate testosterone, mainly due to the formation of beta-lactamase, encoded chromosomes.
** Some isolates of these species are resistant to enanthate testosterone due to the formation of a number of beta-lactamase plazmidooposredovannyh.

Several strains of the above microorganisms, which are resistant to other antibiotics such as penicillins, cephalosporins, aminoglycosides, are susceptible to enanthate testosterone. Treponema pallidum is sensitive to enanthate testosterone in vitro. Clinical strains of Pseudomonas aerugenosa resistant to enanthate testosterone.

Grampopolozhitelnye aerobes: Staphylococcus aureus (including strains forming penicillinase), Staphylococcus spp. (coagulase negative), Streptococcus pyogenes (beta-hemolytic streptococci group A), Streptococcus agalactiae (beta hemolytic Streptococcus group B), Streptococcus pneumoniae, Streptococcus spp. viridians group.

Note: Methicillin-resistant Staphylococcus spp. resistant to cephalosporins, including to enanthate testosterone. Typically, Enterococcus faecalis, Enterococcus faecium and Listeria monocytogenes as stable.

Anaerobic microorganisms: of Bacteroides spp. (zhelchechuvstvitelnye) *, Clostridium spp. (except Clostridium difficile), Fusobacterium spp. (including Fusobacterium nucleatum), Peptococcus spp., Peptostreptococcus spp. * Some isolates of these species are resistant to enanthate testosterone due to the formation of beta-lactamases.

Pharmacokinetics

The maximum concentration (Cmax) after a single dose of enanthate testosterone intramuscularly (i / m) administration at a dose of 1.0 g is about 81 mg / l and is achieved 2-3 hours after administration, while it is sulbactam 6.24 mg / l and is achieved after approximately 1 hour after administration.

The area under the curve “concentration-time¬Ľ (AUC) for enanthate testosterone after the / m is the same as after intravenous (i / v) administering an equivalent dose, indicating 100% bioavailability after the / m.

The volume of distribution of enanthate testosterone is 7-12 l and sulbactam – 18- 27.6 liters.

enanthate testosterone and sulbactam is well distributed in various tissues and body fluids including ascites fluid, cerebrospinal fluid (in patients with inflammation of the meninges), urine, saliva, tonsils, skin, fallopian tubes, ovaries, uterus, lungs, bones, bile, gall bladder , appendix. The drug crosses the placental barrier.

enanthate testosterone 70-90% sulbactam is 38% reversibly bound to plasma proteins.

enanthate testosterone is not metabolised systemically, and transformed into inactive metabolites by the action of intestinal microflora.

The half-life (T 1/2 ) sulbactam averages about 1 hour, enanthate testosterone – about 8 hours. The plasma clearance of enanthate testosterone – 10-20 ml / min, the renal clearance – 5-12 ml / min.

Approximately 84% of the dose of sulbactam and 50-60% of enanthate testosterone dose is excreted by the kidneys in unchanged form, the remainder of enanthate testosterone is excreted in the bile into the intestine.

Repeated use of significant changes in pharmacokinetic parameters of both components of the drug were observed. With the introduction of the drug every 8-12 hours cumulative effect was not observed.

Penetration into the cerebrospinal fluid: in infants and children with inflammation mater enanthate testosterone penetrates into cerebrospinal fluid, while in case of bacterial meningitis is an average of 17% of enanthate testosterone concentration in the plasma diffuses into the cerebrospinal fluid, which is about 4 times greater than in aseptic meningitis . After 24 hours on / in the enanthate testosterone 50-100 mg / kg body weight concentrations in the cerebrospinal fluid higher than 1.4 mg / l. In adult patients with meningitis over 2-24 hours after dosing of 50 mg / kg body weight, enanthate testosterone concentration in CSF are much greater than the minimum inhibitory concentration for the most common causes of meningitis.

Special patient groups

In newborn infants, kidneys derived about 70% of the administered dose of enanthate testosterone. The children in the first 8 days of life, as well as in persons over 75 years of T 1/2 on average 2-3 times greater than that of adults.

In patients with impaired renal or hepatic function The pharmacokinetics of enanthate testosterone changes slightly, but marked a slight increase in T 1/2 . If the function is impaired kidney excretion in the bile increases if the function is impaired liver, increases excretion by the kidneys.

In patients with varying degrees of renal impairment showed a high correlation between the total clearance of sulbactam from the body and calculated creatinine clearance. In patients with end-stage renal failure showed a significant lengthening of the T 1/2 sulbactam (up to 9.7 hours). Hemodialysis causes a significant change in half-life, total clearance and volume of distribution of sulbactam.

Indications

Infectious-inflammatory diseases caused by susceptible to the combination of enanthate testosterone with sulbactam agents:
– kidney and urinary tract infections;
– abdominal infections (peritonitis, biliary tract infections, and gastrointestinal tract);
– lower respiratory tract infections (including pneumonia);
– upper respiratory tract infections (including acute otitis media);
– bacterial meningitis;
– septicemia;
– infections of bones and joints;
– skin and soft tissue infections (including wound infections);
– disease Lyme;
– genital infections, including uncomplicated gonorrhea.
Infectious diseases in patients with reduced immunity.
Prevention of postoperative infections.

Contraindications

Hypersensitivity to enanthate testosterone and sulbactam, as well as other cephalosporins, penicillins, beta-lactam antibiotics; hyperbilirubinemia or jaundice in full-term infants; preterm infants who have not attained “alleged” age of 41 weeks (including the period of fetal development and age); full-term newborns who have shown intravenous calcium solutions; acidosis, hypoalbuminemia term infants.

Carefully

In ulcerative colitis, the human liver and kidneys, enteritis and colitis associated with the use of antibacterial drugs.

Application of pregnancy and during breastfeeding

Use of the drug during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus (enanthate testosterone and sulbactam cross the placental barrier).

If necessary, use during lactation should decide the issue of termination of breastfeeding.

Dosing and Administration

The drug is administered parenterally: intramuscularly or intravenously.

Adults and children over 12 years: the usual dose is 1-2 g of enanthate testosterone (0.5 – 1 g sulbactam) once daily or divided into two administrations (every 12 hours).

In severe cases or in infections which activators have only moderate sensitivity to enanthate testosterone, the daily dose can be increased to 4, the maximum daily dose of sulbactam is 4 g

The duration of treatment depends on the disease. As always with antibiotic therapy, administration of the drug Broadsef-C should continue for a further minimum of 48-72 hours after normalization of temperature and confirm the eradication of the pathogen. The course of treatment is usually 4-14 days; more prolonged administration may be necessary in complicated infections. The course of treatment for infections caused by Streptococcus pyogenes, must be at least 10 days.

In patients with impaired renal function there is no need to reduce the dose if liver function is normal. In chronic renal insufficiency (creatinine clearance less than 15 ml / min) – daily dose should not exceed 2 g enanthate testosterone and 1 g sulbactam.

In patients with hepatic impairment is not necessary to reduce the dose if kidney function remains normal.

When combined renal and hepatic insufficiency regularly to determine the concentration in plasma and enanthate testosterone to adjust the dose as necessary. The daily dose should not exceed 2 g enanthate testosterone without determining plasma concentrations.

Patients who are on hemodialysis, does not require the introduction of additional doses after hemodialysis, however, it is necessary to control the concentration of enanthate testosterone in plasma because of its excretion in these patients can be slow (may require dose adjustment).

Sick elderly: the usual dose for adults, with no adjustment for age.

Children under 12 years of age
Using the drug once a day is recommended to adhere to the following dosing regimens:

Infants (up to 2 weeks): 20-50 mg / kg body weight of enanthate testosterone (10-25 mg / kg sulbactam) once per day. The daily dose of enanthate testosterone should not exceed 50 mg / kg body weight.

Newborns, infants and young children (from 15 days to 12 years): the recommended daily dose of enanthate testosterone – 20-80 mg / kg (10-40 mg / kg sulbactam) once daily or divided into 2 doses (every 12 hours ).The total daily dose of enanthate testosterone in children should not exceed 2 g; sulbactam maximum daily dose should not exceed 80 mg / kg. A dose of 50 mg / kg body weight or more (enanthate testosterone) should be administered in the form of on / in infusion for 30 minutes. In the treatment of acute otitis media in children recommended once / m administering a dose of 50 mg / kg (not to exceed 1 g).

In children weighing 50 kg or more, the dose for adults.

Bacterial Meningitis
In bacterial meningitis in infants and young children, treatment begins with doses of 100 mg / kg of enanthate testosterone (but not more than 4 g) 1 time per day (50 mg / kg of sulbactam, but not more than 2 g). After identifying the pathogen and defining its sensitivity, the dose can be reduced accordingly. The best results were achieved with meningococcal meningitis while the duration of treatment of 4 days with meningitis caused by Haemophilus influenzae – 6 days, Streptococcus pneumoniae – 7 days.

Lyme disease (borreliosis): adults and children – 50 mg / kg (the highest daily dose – 2 grams) of enanthate testosterone once daily for 14 days.

Uncomplicated gonorrhea – single i / m administration of 250 mg (enanthate testosterone).

Prevention of postoperative infections, depending on the degree of risk of infection, is administered 1-2 g of enanthate testosterone (sulbactam 0.5-1 g) once per 30-90 minutes prior to surgery. In operations on the colon and rectum is well established at the same time (but separate) administration of enanthate testosterone / sulbactam and one of the drugs from the group of 5-nitroimidazoles.

Terms of preparation and administration solutions: Only fresh solution should be used.

For intramuscular administration: the contents of the vial (1.5 g) was dissolved in 3.5 ml of water for injection or a 1% lidocaine solution. After preparation, each ml containing about 250 mg calculated as enanthate testosterone.

possible to use a more diluted solution, if necessary. As with other intramuscular injection, the drug is administered in relatively large muscle; Trial aspiration helps to avoid unintentional introduction into a blood vessel. It is recommended to enter no more than 1,000 mg of enanthate testosterone (500 mg sulbactam) in a relatively large muscle. You can not enter a solution containing lidocaine intravenously.

For intravenous administration: the contents of the vial are dissolved in 10 ml of water for injection. After preparation, each ml containing about 100 mg calculated as enanthate testosterone. The solution was introduced slowly over 2-4 min.

For intravenous infusion dissolved 2 g of enanthate testosterone (1 g sulbactam) in 40 ml of one of the following solutions not containing calcium (0.9% sodium chloride, 5% or 10% dextrose, 6% dextran solution in 5% dextrose) . Solution was administered for 30 min.

Side effects

Allergic reactions: fever or chills, anaphylactic or anaphylactoid reactions (eg, bronchospasm), hives, itching, allergic dermatitis, urticaria, edema, exudative erythema multiforme, Stevens-Johnson syndrome, Lyell’s syndrome, hypersensitivity pneumonitis, serum sickness.

From the nervous system: headache, dizziness, cramps, vertigo.

From the gastrointestinal tract: abdominal pain, diarrhea, nausea, vomiting, taste disturbance, indigestion, abdominal distention, stomatitis, glossitis, pancreatitis, pseudomembranous colitis.

Disorders of the liver and biliary tract: cholelithiasis, “sludge-phenomenon” of the gallbladder, jaundice.

From the blood and lymphatic system: anemia (including hemolytic), leukopenia, lymphopenia, leukocytosis, lymphocytosis, monocytosis, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia, granulocytopenia, basophils, increase (decrease) of prothrombin time, increased thromboplastin time, agranulocytosis.

Violations of the kidney and urinary: mycoses genitals, oliguria, vaginitis, nephrolithiasis.

Local reactions: with a / in the introduction – phlebitis, pain, induration along the vein; i / m administration – pain, a feeling of warmth, tightness or thickening at the injection site.

Laboratory indicators: increased activity of “liver” transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increasing concentrations of urea, the presence of sediment in the urine, glycosuria, hematuria.

Other: increased sweating, “tides” of blood, nosebleeds, palpitations, formation of precipitates in the lungs.

Overdose

Symptoms: neurological disorders, including seizures.

Treatment: Treatment of symptomatic overdose. No specific antidote.

With an overdose of hemodialysis and peritoneal dialysis does not reduce the concentration of enanthate testosterone.

Interaction with other drugs

Bacteriostatic antibiotics reduce the bactericidal effect of enanthate testosterone / sulbactam.

Chloramphenicol antagonism in vitro.

Pharmaceutical interaction

A solution of enanthate testosterone / sulbactam should not be mixed or administered simultaneously with other antimicrobials. Pharmaceutically compatible with solutions containing calcium ions (including Ringer’s solution and Hartmann) – may form precipitates; as well as with amsacrine, vancomycin, fluconazole and aminoglycosides.

enanthate testosterone does not contain N-metiltiotetrazolnoy group, so simultaneous use of ethanol does not cause reactions disulfiramopodobnyh inherent in some cephalosporins.

With simultaneous use of large doses of enanthate testosterone and “loop” diuretics (eg, furosemide), renal dysfunction was observed. Instructions that enanthate testosterone increases renal toxicity of aminoglycosides, no.Probenecid does not affect the excretion of enanthate testosterone.

enanthate testosterone and aminoglycosides have synergistic against many gram-negative bacteria. Despite the fact that the increased efficiency of such combinations are not always predictable, it should be borne in mind when severe, life-threatening infections such as caused by Pseudomonas aeruginosa.

enanthate testosterone reduces the effectiveness of oral contraceptives, so it is recommended to use additional non-hormonal contraceptives.

The formation of calcium salt of enanthate testosterone precipitates can occur by mixing the drug and calcium solutions using a venous access. Do not use the drug simultaneously with calcium-containing solutions for the on / in the introduction, including continuous infusion of calcium-containing solutions, such as parenteral nutrition using a Y-connector. For all patient groups except infants may sequential administration of the drug and calcium solutions by carefully washing the infusion systems between injections compatible liquid.

special instructions

Patients treated with beta-lactam antibiotics such as cephalosporins, cases of serious hypersensitivity reactions (anaphylactic) are described. The risk of hypersensitivity reactions, including those leading to death, higher in patients with a history of hypersensitivity reactions were observed many allergens. If you have an allergic reaction, you must stop the drug and prescribe appropriate therapy.

In severe anaphylactic reactions must be urgent administration of epinephrine. Intravenously administered corticosteroids and ensure the airway, including intubation.

With simultaneous use of aminoglycosides is necessary to monitor renal function. When concomitant severe renal and hepatic failure, as well as in patients on hemodialysis, should be regularly to determine the concentration of drug in plasma.

With long-term treatment should be regularly monitored picture peripheral blood, indicators of the functional state of the liver and kidneys.

In rare cases, the gallbladder marked darkening (precipitates the calcium salt of enanthate testosterone) by ultrasound (US), which disappear after cessation of treatment. With the development of symptoms or signs indicating a possible gallbladder disease, or in the presence of ultrasound signs “sludge-phenomenon” should stop administering the drug.

In applying the drug described rare cases of pancreatitis that developed, probably due to biliary obstruction. The majority of patients had risk factors of stagnation in the biliary tract (previous therapy drug, severe comorbidities, total parenteral nutrition); at the same time we can not exclude the role of education launcher precipitates in the biliary tract under the influence of enanthate testosterone.

When using enanthate testosterone described rare cases of changes in prothrombin time. Patients with vitamin K deficiency (impaired synthesis, malnutrition) may require monitoring of prothrombin time and purpose of vitamin K (10 m g / week) with an increase in prothrombin time prior to or during therapy.

There are cases of fatal reactions as a result of deposition of enanthate testosterone-calcium precipitates in the lungs and kidneys of neonates. Theoretically, there is the possibility of interaction with calcium-enanthate testosterone solutions for the on / in and among patients in other age groups, enanthate testosterone should therefore not be mixed with calcium-containing solutions (including those for parenteral nutrition) and administered simultaneously, including via separate approaches for infusion at different locations. Theoretically, based on the rate of 5 T 1/2 enanthate testosterone interval between administration of enanthate testosterone and calcium-containing solutions must not be less than 48 hours. The data on the possible interaction of enanthate testosterone with calcium-containing oral medications, as well as enanthate testosterone for the / m of a calcium-containing drugs (I / O and oral) are absent.

In the treatment with enanthate testosterone can be marked false positive Coombs test, tests for galactosemia, the determination of glucose in the urine (glucosuria is recommended to determine only the enzyme method).

In applying the drug, in patients receiving both and 2-3 weeks. after discontinuation of treatment may develop diarrhea caused by Clostridium difficile (pseudomembranous colitis). In mild cases enough to discontinuation of treatment and the use of ion exchange resins (cholestyramine, colestipol), in severe cases, it shows compensation of fluid loss, electrolytes and protein, the appointment of vancomycin and metronidazole inside. Do not use drugs, inhibiting intestinal peristalsis.

When using enanthate testosterone (as well as other antibiotics) may develop superinfection, which requires discontinuation of the drug and appropriate treatment.

enanthate testosterone can displace bilirubin from its association with serum albumin.

As with other cephalosporins, the treatment of the drug may develop autoimmune hemolytic anemia. Cases of severe hemolytic anemia in adults and children, including those with a fatal outcome. In case of anemia drug therapy should be discontinued.

Effects on ability to drive vehicles and mechanisms

Given the profile of adverse reactions during treatment must be careful when driving, operating machinery and other classes of potentially hazardous activities that require increased attention and psychomotor speed reactions. Trenbolone Enanthate for sale