Цефамабол®

General characteristics. Structure:

Active ingredient: 1,0 g of a tsefamandol of a nafat (and recalculation on цифамандол). Excipient: sodium carbonate.

Pharmacological properties:

Pharmacodynamics. The Tsefalosporinovy antibiotic of the II generation for parenteral use. Works bakteritsidno (breaks synthesis of a cell wall of microorganisms). Has a broad spectrum of activity. It is highly active concerning gram-positive microorganisms - Staphylococcus aureus (including the strains which are producing and not producing a penicillinase), Staphylococcus epidermidis, Streptococcus spp (including beta and hemolitic strains of a serogroup And (Streptococcus pyogenes), Streptococcus pneumoniae; gram-negative microorganisms - Escherichia coli, Klebsiella spp., Enterobacter spp., Haemophilus influenzae, Providencia rettgeri, Morganella morganii, Proteus mirabilis, Proteus vulgaris; anaerobic microorganisms - gram-positive and gram-negative cocci (including Peptococcus, Peptostreptococcus), gram-positive sticks (including Clostridium spp.), gram-negative sticks (including Fusobacterium spp, Bacteroides spp.). It is steady against action beta лактамаз. It is not active concerning different types of Pseudomonas, the majority of strains of Enterococcus spp. (т.ч. Enterococcus faecalis), Enterobacter cloacae, Bacteroides fragilis, metitsillinorezistentny strains of Staphylococcus spp., Serratia spp.i Listeria monocytogenes Has disulfiramopodobny effect.

Pharmacokinetics. After intramuscular introduction of 0,5 or 1,0 g (in oil) time of achievement of the maximum concentration (TCmax) - 30 - 120 min., the size of the maximum concentration (Cmax) makes 13 and 25 mkg/ml respectively. After intravenous (in/in) introductions of 1, 2 or 3 g in 10 min. Cmax makes 139, 240 and 533 mkg/ml and remains at the therapeutic level during 6 h. Therapeutic concentration is reached in pleural and joint liquids, bile and bones. Does not kumulirut. The period to a floor of removal (Т½) later in/in - 30-35 min., after 60 min. in oil. It is removed by kidneys in not changed look (for 8 h 65-85% are removed and provides high concentration of drug in urine). After introduction in oil of 0,5 and 1,0 g the content in urine makes 254 and 1357 mkg/ml respectively; at in introduction of 1 and 2 g - 750 and 1380 mkg/ml respectively. At the chronic renal failure (CRF) removal is slowed down. At the patients who are on a hemodialysis Т½ increases to 6 h.

Indications to use:

Respiratory infections (community-acquired pneumonia), infection of ENT organs (sinusitis, average otitis), intraabdominal infections (peritonitises of various localization), urological (pyelonephritises) and gynecologic infections, infections of skin, soft tissues and joints, postoperative infection of various localization. It is applied to an antibiotikoprofilaktika of surgical infections.

Route of administration and doses:

The drug is administered intramusculary or intravenously. For intramuscular introduction drug (0,5 g or 1,0 g) is dissolved in 3 ml of water for injections or in 3 ml of 0,9% of solution of sodium of chloride. For intravenous jet administration drug is dissolved at the rate of 1 g of drug in 10 ml of water for injections or in 10 ml of 0,9% of solution of sodium of chloride. For intravenous drop administration dissolved as it is described above, drug mix from 5%-10% solution of a dextrose or 0,9% chloride sodium solution. The adult appoint 0,5 g - to 1 g there are each 4-8 hours. At infections of skin and soft tissues appoint 0,5 g each 6 hours; for treatment of uncomplicated community-acquired pneumonia on 0,5-1 g each 6 hours; at uncomplicated infections of urinary tract – to 0,5 g there are each 8 hours; at the complicated infections of urinary tract – 1 g each 8 h. For therapy of heavy and life-threatening infections enter 2 g each 4-6 hours (the maximum daily dose should not exceed 12 g).

At the infections caused by a beta and hemolitic streptococcus, it is necessary to continue treatment not less than 10 days. For prevention of postoperative infectious complications Tsefamabol enter in/in in a dose of 1 g or 2 g together with premedication or an introduction anesthesia, but not earlier than for an hour prior to operation. If necessary, continue introduction in the mode to 1 g or 2 g there are each 6 hours during 24-48 h.

To the patients who are exposed to Cesarean section, 1-2 g of Tsefamabol are entered directly before operation or at once after crossclamping of an umbilical cord. To patients on a hemodialysis each 12 h intravenously or intramusculary enter 1 g (if intramuscular introduction is used, then after end of a hemodialysis in addition enter 1/3-1/2 doses). For prevention of postoperative infectious complications in 30-60 min. prior to intervention by the adult enter - 1-2 g, to children - 50-100 mg on 1 kg, with the subsequent use of the same doses during 24-48 h. To patients with renal failures the mode of dosing is set taking into account values of clearance of creatinine. After an initial dose of 1-2 g (depending on weight of an infection) appoint the following maintenance doses: The clearance of creatinine (ml/min.) Heavy infections Medium-weight infections of 50-80 2 g    or to 1,5 g is each 6 hours each 4 hours 0,75-1,5 g each 6 hours 25-50 1,5 g every the 6th hour or to 2 g there are each 8 hours 0,75-1,5 g each 8 hours of 10-25 1 g each 6 hours or to 1,25 g there are each 8 hours 0,5-1 g each 8 hours of 2-10 0,67 g each 8 hours or to 1 g there are each 12 hours 0,5-0,75g each 12 hours Less than 2 0,5 g each 8 hours or 0,75 g each 12 hours 0,25-0,5 g each 12 hours to Children are more senior enter at the rate of 50-100 mg/kg/days 1 month; the daily dose is divided into 3-6 bucketed introductions of 4-8 hours. At heavy infections the daily dose can be increased to 150 mg/kg/days, but not exceed 12 g. For prevention of postoperative infectious complications enter in the same mode, as at adults, at the rate of 50-100 mg/kg in bucketed days between introductions of 6 hours solution Preparation. For use in oil 1 g of powder dissolve in 3 ml of water for injections or 3 ml of isotonic solution of sodium of chloride. Enter deeply into a buttock. For in/in jet introductions Tsefamabol dissolve at the rate of 1 g of drug in 10 ml of water for injections or 10 ml of isotonic solution of sodium of chloride. Enter slowly intravenously from 3 to 5 minutes. For in/in drop of introduction the drug (prepared as it is described above) dissolve in 5-10% solution of glucose or isotonic solution of sodium of chloride. Time introduction from 10 to 30 minutes.

Features of use:

The patients who had allergic reactions to penicillin in the anamnesis can have hypersensitivity to tsefalosporinovy antibiotics. During treatment tsefamandoly are possible: false positive forward reaction of Koombs, false positive reaction of urine to glucose, proteinuria. The elderly and weakened patients with deficit of vitamin K have an increased risk of development of a prothrombinopenia with bleeding or without it (in these cases administration of vitamin K is shown). During treatment it is necessary to abstain from ethanol reception - the effects similar to action of Disulfiramum are possible (face reddening, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, decrease in the ABP, tachycardia, short wind). Freshly cooked solution is good for use during 24 h at its storage at the room temperature, and during 96 h - at storage in the refrigerator. Researches about influence on speed of response were not conducted. Considering possible developing of dizziness and encephalopathy, it is necessary to be careful when driving vehicles and difficult mechanisms. When developing diarrhea during treatment by drug it is necessary to exclude psevdomembrazny colitis. If the diagnosis of psevdomembrazny colitis is confirmed, it is necessary to stop administration of drug immediately.

Side effects:

Allergic reactions: a small tortoiseshell, a fever or fever, rash, an itch, it is rare - a bronchospasm, an eosinophilia, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease), a Quincke's disease, an acute anaphylaxis. From the alimentary system: nausea, vomiting, diarrhea or a lock, dysbacteriosis, an abnormal liver function (increase in activity of "hepatic" transaminases, an alkaline phosphatase, a hyperbilirubinemia, cholestatic jaundice, hepatitis), it is rare - stomatitis, a glossitis, a pseudomembranous coloenteritis. From bodies of a hemopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolitic anemia. From an urinary system: an azotemia, increase in content of urea in blood, a giperkreatininemiya, a renal failure. From a nervous system: headache, dizziness. Local reactions: phlebitis, morbidity on the vein course, morbidity and infiltrate in the place in oil of introduction. Others: superinfection.

Interaction with other medicines:

The aminoglycosides, "loopback" diuretics, drugs reducing canalicular secretion increase nephrotoxicity. It is incompatible with ethanol (inhibits an atsetaldegidrogenaza), disulfiramopodobny reactions (an abdominal pain, a dermahemia of the person, a headache, a lowering of arterial pressure, nausea, vomiting, heartbeat, the increased sweating) develop. In solution pharmaceutical it is incompatible with aminoglycosides.

Contraindications:

Hypersensitivity (including to cephalosporins, penicillin, karbapenema), early children's age (up to 1 month). With care: a renal failure, pseudomembranous colitis (in the anamnesis). Use of drug during the periods of pregnancy and a lactation is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit. In need of purpose of a tsefamandol in the period of a lactation it is necessary to stop breastfeeding.

Overdose:

Symptoms: spasms (especially at patients with HPN). Treatment: symptomatic therapy, including diazepam and shortly operating barbiturates, in hard cases - a hemodialysis.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store drug in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 1,0 g of active agent in glass bottles with a capacity of 10 ml. On 1 or 5 bottles in a cardboard pack together with the instruction on a medical use. On 1 or 5 bottles in a blister strip packaging complete with solvent (water for injections). Each planimetric packaging in a cardboard pack together with the instruction on a medical use. On 1 bottle complete with solvent in a pack cardboard without planimetric packaging. Put one application instruction in a pack. On 50 bottles place in a box cardboard with 1-5 application instructions (for hospitals).