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Ceftriaxone is an antibiotic from the group of third-generation cephalosporin for parenteral administration. It has bactericidal activity against many gram-negative and gram-positive bacteria. Ceftriaxone resistant to beta-lactamases. It is also active against strains resistant to other cephalosporins. High sensitivity to ceftriaxone have the following strains: Streptococcus viridans, Streptococcus pneumoniae, Staphylococcus aureus, S.epidermidis, testosterone suspensiontestosterone suspension Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitides, Haemophilus ducreyi, Yersinia pestis, Borellia burdorferi, Treponema pallidum, Serratia marcescens, Peptostreptococcus spp., Proteus mirabilis, Proteus vulgaris. Types Enterobacteriacieae (Escherichia coli, Salmonella spp. , Shigella spp., Citrobacter spp., Morganella morganii, Klebsiella spp., Enterobacter spp., Providencia spp. ) is also susceptible to ceftriaxone, other than strains that produce beta-lactamase. Ceftriaxone is not effective against Acinetobacter spp., P. aeruginosa, Campylobacter jejuni, Bacterioides fragilis, Clostridium difficile, Listeria monocytogenes, Enterococcus fecalis, and methicillin-resistant staphylococci. mycoplasmas, mycobacteria chlamydia and resistant to cephalosporins. Due to the long half-life (about 8 hours), the drug can be administered once a day. Ceftriaxone well absorbed when intramuscularly administered and reaches high concentrations in serum. The bioavailability of the drug is 100%. Ceftriaxone quickly penetrates the tissue fluid and characterized by a high volume of distribution in many tissues and fluids of the body. Meningitis in children, including babies, ceftriaxone penetrates into cerebrospinal fluid in inflammation meningeal membranes, while its concentration in CSF is 17% of the plasma concentration. In adult patients after 2-24 hours after administration of a single dose of 50 mg / kg body weight ceftriaxone concentration in the cerebrospinal fluid higher than the minimum inhibitory concentration for the most common causes of meningitis. Because of the long half-life (mean 8 hours in children during the first 8 days of life, as well as in patients older than 75 years – twice as much), ceftriaxone concentration 24 hours after administration is higher than the MIC for most organisms that cause a variety of infections. Approximately 50 – 60% of the injected ceftriaxone is excreted unchanged by the kidneys, the rest – through the liver. In newborns kidneys derived about 70% of the drug.

Indications
Lendatsin used to treat infections caused by bacteria susceptible to ceftriaxone, including the following:

infections of the upper and lower respiratory tract

  • infections in otorhinolaryngology
  • septicemia
  • endocarditis
  • bacterial meningitis
  • abdominal infections (peritonitis, inflammatory diseases of the gastrointestinal tract, biliary tract)
  • urinary tract infections
  • reproductive tract infections, including gonorrhea and chancroid
  • Infection of bone, joints, soft tissue, skin and wound infections
  • typhoid fever, invasive salmonellosis, shigellosis
  • Lyme disease
  • febrile neutropenia in patients with malignancies.Contraindications
    Ceftriaxone is contraindicated in patients with known allergy to cephalosporins.Precautions
    Ceftriaxone should not be administered to newborns with hyperbilirubinemia.
    Ceftriaxone should be used with caution in patients with known hypersensitivity to penicillins because of possible cross-allergenicity.
    Ceftriaxone should be given with caution to persons with combined pochechno- liver failure, gallbladder disease and gastro-intestinal diseases in history.

    Pregnancy and lactation
    Ceftriaxone should be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus.
    Ceftriaxone in low concentrations into breast milk. If necessary, the appointment during lactation should stop breastfeeding for a period of treatment.

    Dosage and administration
    Ceftriaxone may be administered intramuscularly, intravenously or as a slow intravenous infusion, continuing for at least 30 minutes.

    Adults and children over 12 years
    The usual dose is 1-2 g of ceftriaxone once daily or divided into two doses (every 12 hours). The maximum daily dose was 4 g (2 g administered as an intravenous infusion over 30 minutes with a 12-hour intervals).
    To avoid local reactions at intramuscular testosterone suspensiontestosterone suspension injection should be alternated injections into the left and right buttock.
    For the treatment of uncomplicated gonorrhea in men and women recommended single intramuscular dose of 250 mg of ceftriaxone.

    Children under 12 years of age
    The recommended daily dose is 50-75 mg / kg of body weight once a day, or divided into 2 doses.
    The total daily dose should not exceed 2 g Newborns: The recommended dose is 20-50 mg / kg body weight by slow intravenous infusion. in bacterial meningitis in infants and children up to 12 years of ceftriaxone administered at a dose of 100 mg / kg / day of body weight (but not more than 4 g / day.), duration of the course of 7-14 days.

    Intramuscular administration of
    250 mg of ceftriaxone dissolved in 2 ml and 1 g – 3.5 ml 1% lidocaine. The solution is injected deep into the gluteal muscle. It is recommended to be administered not more than 1 g in each buttock.
    A solution of lidocaine in any case not be administered intravenously.

    Intravenous administration of
    250 mg of ceftriaxone dissolved in 5 ml and 1 g – 10 ml water for injection. The solution was slowly administered into the vein for 2-4 minutes.

    An intravenous infusion of
    2 g of ceftriaxone dissolved in 40 ml of the appropriate infusion solution containing no calcium (0.45% or 0.9% sodium chloride, 2.5%, 5% or 10% glucose, levulose 5%, 6% dextran on glucose). The duration of infusion for at least 30 minutes.

    Side effects
    : As with other cephalosporins, the treatment with ceftriaxone following side effects may occur
    gastrointestinal disorders (diarrhea, nausea, vomiting, flatulence, stomatitis, rarely – pseudomembranous colitis),
    allergic reactions (swelling, pruritus, urticaria, allergic dermatitis, rarely – fever, anaphylaxis (bronchospasm, hypotension), exudative erythema multiforme;
    haematological disorders (thrombocytosis, eosinophilia, leukopenia, thrombocytopenia, hemolytic anemia) with the urinary system – oliguria,
    the central nervous system – headache, dizziness.
    Local reactions (painful seal, phlebitis) can occur at the site of injection.
    Laboratory indicators: reduction in prothrombin time, increased activity of “liver” transaminases, increases in serum creatinine, hyperbilirubinemia.
    Side effects are usually mild and do not require discontinuation of therapy.

    Overdose
    Clinical signs of overdose are: nausea, vomiting, diarrhea, confusion, convulsions.
    No specific antidote. Treatment is symptomatic.
    Hemodialysis is ineffective.

    Interaction with other medicines
    Ceftriaxone must not be mixed with solutions of other antimicrobial agents or infusion fluids other than given in the section “Dosage and method of administration.” Ceftriaxone must not be mixed with solutions containing calcium.
    When concomitant administration of cephalosporins and cyclosporine levels in blood plasma and the latest toxicity may be increased.
    With the simultaneous use of NSAIDs and other inhibitors of platelet aggregation increases the likelihood of bleeding.
    Diclofenac stimulates secretion into bile and reduces total clearance in the urine.
    acetazolamide increases the concentration of ceftriaxone in the stomach contents.
    Do not interact with probenecid.

    Cautions Prolonged treatment should be monitored blood count. Patients with impaired synthesis of vitamin K or low stockpiles (eg, liver diseases and malnutrition) may require monitoring of hematologic and coagulation parameters during treatment. Ceftriaxone changes the results of the determination of glucose in urine using copper reduction reaction (Klinitest), but does not affect the results of the glucose oxidase test. Blackout by ultrasound, the corresponding deposits of ceftriaxone should not be mistaken for gallstones. Similar deposits of ceftriaxone in the gallbladder observed frequently, but they are usually asymptomatic and disappear spontaneously. In testosterone suspensiontestosterone suspension patients with mild renal impairment is not necessary to reduce the dosage of ceftriaxone, provided normal liver function. In the case of severe renal insufficiency (creatinine clearance 10 mL / min or less) should adjust the dose. in patients with impaired hepatic function there is no need to reduce the dosage of ceftriaxone, provided normal kidney function.in the case of simultaneous severe violations of liver and kidney function should be to reduce the dose of ceftriaxone 2 times and implement control of its concentration in blood plasma. For patients older group dose adjustment is required. As with other antibiotic treatment, there is a risk of superinfection resistant microorganisms; pseudomembranous colitis is rare.

    Data on the effect of ceftriaxone on ability to drive and do not have the mechanisms.

    Product form
    Powder for solution for intramuscular and intravenous administration of 250 mg in bottles; 1, 5 or 10 bottles in a carton box together with instruction for medical use;
    Powder for solution for intramuscular and intravenous administration of 1 g vials; 1, 5, 10 or 50 bottles in a carton box together with instruction for medical use;
    Powder for solution for infusion 2 g vials; 1, 5 or 10 bottles in a carton box with instruction on the medical application.

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