Tseftum

General characteristics. Structure:

1 bottle contains a ceftazidime for injections sterile (sterile mix of a ceftazidime of pentahydrate and sodium of a carbonate) in terms of a ceftazidime of 1,0 g.

Pharmacological properties:

Pharmacodynamics. The ceftazidime belongs to tsefalosporinovy antibiotics of the III generation. Has bactericidal effect due to damage of a cell wall of bacteria (acetylates membrane-bound transpeptidases, breaking the cross stitching of peptidoglikan necessary for ensuring durability and rigidity of a cell wall). Possesses a wide range of antimicrobic action. Various gram-positive are sensitive to drug: Staphylococcus aureus (strains sensitive to Methicillinum), St.epidermidis (strains sensitive to Methicillinum), Micrococcus spp., Streptococcus pneumoniae, Str.pyogenes, Str.agalactiae, Str.mitis, Streptococcus spp. (excepting Streptococcus faecalis), gram-negative: Aeromonas spp., Citrobacter spp., Enterobacter spp., Escherichia coli, H.influenzae, H.parainfluenzae, Klebsiella spp. (including K.pneumoniae), Morganella morganii, Providencia rettgeri, Providencia spp., Neisseria gonorrhoeae, N.miningitidis, Pasteurella multocida, Proteus mirabilis, P.vulgaris, Salmonella spp., Serratia spp. (including Serratia marcescens), Shigella spp., Yersinia spp. (including Yersinia enterocolitica), Acinetobacter spp. and anaerobic bacteria: Bacteroides spp. (many strains of Bacteroides fragilis are resistant), Clostridium perfringers, Fusobacterium spp. Peptococcus spp., Peptostreptococcus, Propionibacterium spp. Drug is steady against beta lactamelements of gram-positive and gram-negative bacteria.

Pharmacokinetics. At intramuscular and intravenous administration of a ceftazidime high concentration of drug in a blood plasma is quickly reached (in 5 - 10 min. after intravenous and in 30 - 45 min. after intramuscular introduction). Cmax after intravenous administration is reached in 20 - 30 min. and makes from 42 to 170 mkg/ml (depending on a dose). Therapeutic concentration of active agent in a blood plasma remain 8 - 12 hours depending on a dose and a way of administration of drug. The ceftazidime contacts proteins of plasma less, than for 10%. Easily gets into a phlegm, into fabrics (including a bone tissue) and liquids (synovial, pleural, peritoneal) an organism, through a placental barrier. Badly gets through a blood-brain barrier, in a small amount gets into breast milk. At an inflammation of a meninx the ceftazidime is found in therapeutic concentration in cerebrospinal fluid. It is not metabolized. The ceftazidime preferential (80 - 90%) by kidneys in not changed look within 24 hours is removed. The elimination half-life of drug makes 2 hours. At a renal failure the dose of drug is reduced as its elimination half-life (2,2 hours) is extended.

Indications to use:

Tseftum is effective at treatment of the infections caused by microorganisms, sensitive to drug:
- at heavy infections (a septicaemia, bacteremia, peritonitis, meningitis, infections at patients with reduced immunity; infections at the patients who are in intensive care units);
- at respiratory infections (including infections of lungs and a mucoviscidosis);
- at infections of an ear, nose, throat;
- at infections of urinary tract;
- at infections of skin and soft tissues;
- at infections of digestive tract, biliary tract, an abdominal cavity;
- at infections of bones and joints;
- at infections of bodies of a small pelvis;
- at the infections connected with a hemodialysis and peritoneal dialysis.

Route of administration and doses:

Drug is used intramusculary and intravenously. The dose is established individually, depending on the activator, by weights of a course of a disease, age of the patient, his body weight, function of kidneys.
Solutions are prepared just before introduction. For intramuscular introduction dissolve 1,0 g of drug in 3 ml of solvent (sterile water for injections or 0,5 - 1,0% lidocaine solution), enter deeply into areas of an upper outside quadrant of a big gluteus or in the field of a lateral part of a hip. For intravenous jet administration dissolve 1,0 g of drug in 10 ml of water for injections. Solution is entered slowly within 3 - 5 minutes. For intravenous drop administration drug in addition part in 150 - 400 ml 5% - a leg of solution of glucose or isotonic solution of sodium of chloride. Solution is entered slowly within 1,5 - 2 hours. Solution of drug can be entered directly into a vein or into a tube of infusional system. Tseftum in the form of powder is in a bottle under the lowered pressure. At dissolution of powder carbon dioxide is emitted (in the form of small bubbles) and pressure in a bottle increases. Therefore for the purpose of simplification of use it is recommended to observe the following method of preparation of solution for intramuscular or intravenous bolyusny administration:
1. To insert the hypodermic needle through a cover of a bottle and to enter the recommended amount of solvent.
2. To take out the hypodermic needle and to stir up a bottle within 1 - 2 minutes that transparent solution turned out.
3. To turn a bottle. At completely entered piston of the syringe to insert a needle into a bottle cover so that the needle completely was in solution and to gather all solution in the syringe (the needle has to be in solution).
To newborns and babies aged up to 2 months drug is appointed in a daily dose
25 - 50 mg/kg in 2 receptions. To children 2 months drug are more senior appoint in a daily dose 50 - 100 mg/kg in 2 - 3 receptions. To children with reduced immunity at heavy infections appoint up to 150 mg/kg (at most 6 g a day); frequency rate of reception - 3 times a day. To children 12 years are more senior and the adult at the majority of infections appoint 1 g each 8 hours or on 2 g each 12 hours.
At a severe disease, especially at patients with reduced immunity, including patients with a neutropenia, it is necessary to appoint 2 g in each 8 or 12 hours or on 3 g each 12 hours. The maximum daily dose - 6 g. If necessary it is possible to increase a single dose by 50% or to increase the frequency of administration of drug, but in this case it is necessary to control Tseftum's level in blood serum, concentration of drug at the same time should not exceed 40 mg/l. The adult with a mucoviscidosis and at infections of the lungs caused by pseudo-monads appoint Tseftum in a dose 100 - 150 mg/kg a day in 3 receptions. At infections of urinary tract drug is appointed for 0,5 - 1,0 by each 12 hours. The dosing mode for patients with renal failures is set depending on values of clearance of creatinine. The initial dose makes 1 g.
The maintenance doses recommended for adults:
Clearance of creatinine (ml/min.)            dosing Mode
50 - To 31                                             1 g  there are each 12 hours
30 - To 16                                               1 g  there are each 24 hours
15 -                                                To 5 500 mg there are each 24 hours
                                            to less than 5 500 mg there are each 48 hours
After each session of a hemodialysis enter maintenance doses of drug according to the stated above table. At peritoneal dialysis, in addition to intravenous administration, Tseftum it is possible to include in dialysis solution (125 - 250 mg on 2 l of dialysis solution). For the adults with a renal failure who are on a continuous hemodialysis with use of the arteriovenous shunt and for the patients who are on haemo filtering of high speed in intensive care unit, the recommended dose makes 1 g a day daily (in one or several receptions). For the patients who are on haemo filtering of low speed appoint the doses recommended at a renal failure.
To patients of advanced age, in view of the lowered clearance of drug at acute diseases, Tseftum in a dose is recommended to appoint no more than 3 g a day, especially to patients 80 years are more senior.

Features of use:

With care it is necessary to use drug for treatment of newborn children. Before therapy using Tseftum it is necessary to exclude existence at the patient of hypersensitivity to antibiotics from group of cephalosporins, penicillin and to other drugs. At development of allergic reaction on Tseftum drug should be cancelled immediately. At a renal failure of a dose of Tseftum reduce according to degree of a renal failure. Prolonged use of drug can lead to increase in growth of insensitive microorganisms (Candida, Enterococci), at the same time the termination of treatment or performing the corresponding therapy can be required.

Side effects:

There can be allergic reactions (rash, fever, an itch, an eosinophilia; very seldom - a bronchospasm, a lowering of arterial pressure, a Quincke's disease), a digestive disturbance (nausea, vomiting, diarrhea, abdominal pains, it is rare - stomatitis, colitis), neurologic frustration (a headache, dizziness, paresthesias, disturbance of flavoring feelings; patients with a renal failure at the wrong selection have doses - a tremor, spasms, encephalopathy), is very rare - a leukopenia, a neutropenia, thrombocytopenia, a lymphocytosis. The effects caused by biological effect: superinfection (candidiasis, including mucous membrane of a vagina). Local reactions: phlebitis or thrombophlebitis at intravenous administration, morbidity in the place of an intramuscular injection.

Interaction with other medicines:

If necessary for strengthening of antibacterial activity concerning Pseudomonas aeruginosa, perhaps combined use of Tseftum with aminoglycosides (gentamycin, amikacin). At the same time, for reduction of toxic effect, it is necessary to administer the drugs separately as on an injection site (at intramuscular injections), and on time (with an interval not less, than 1 hour). Use in combination with broncholitic, mucolytic drugs, immunomodulators is possible. In case of simultaneous use of Tseftum and chloramphenicol it is necessary to pay attention to possible antagonistic action. Simultaneous introduction of Tseftum (in high doses) and nephrotoxic drugs can make an adverse effect on function of kidneys.

Contraindications:

Hypersensitivity to tsefalosporinovy antibiotics, pregnancy (especially 1 trimester), feeding by a breast (for the period of treatment stop).

Overdose:

Symptoms: a headache, dizziness, paresthesias, in hard cases - generalized spasms, encephalopathy, a coma. Treatment: maintenance of vital signs, a hemodialysis, at development of spasms - antikonvulsant. At development of reactions of hypersensitivity use of adrenaline, a hydrocortisone, antihistaminic drugs and holding other urgent actions is shown.

Storage conditions:

To store in the place protected from light at a temperature not above 20 °C. A period of validity – 2 years. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1,0 g in bottles. On 10 bottles in a pack.