Efipim

General characteristics. Structure:

Active ingredient: 1 g of a tsefepim (in the form of a hydrochloride) in 1 bottle.

Excipients: L-arginine.

Pharmacological properties:

Pharmacodynamics. Efipim is a tsefalosporinovy antibiotic of the IV generation. Efipim acts bakteritsidno by inhibition of synthesis of mukopeptid of a cell wall of bacteria in a mitosis phase. Efipim is highly steady against hydrolysis by the majority beta лактамаз, has small affinity concerning the beta laktamaz coded by chromosomal genes and quickly gets into gram-negative bacterial cells. Possesses a broad spectrum of activity concerning gram-positive and gram-negative bacteria, strains, resistant to aminoglycosides or tsefalosporinovy antibiotics of the III generation. Efipim is active in the relation:

Indications to use:

— infections of lower parts of respiratory tracts (including pneumonia and bronchitis);

— the infections of urinary tract (as complicated and uncomplicated);

— infections of skin and soft tissues;

— intraabdominal infections (including peritonitis and infections of bilious ways);

— gynecologic infections;

— septicaemia;

— neytropenichesky fever (as empirical therapy);

— bacterial meningitis at children;

— prevention of infections when carrying out band surgeries.

Route of administration and doses:

The dose and way of introduction are established depending on sensitivity of the activator, weight of an infection, and also from a condition of function of kidneys of the patient. In/in a way of introduction it is preferable to patients with heavy or life-threatening infections, especially at threat of shock.

To adults and children with body weight more than 40 kg at normal function of kidneys appoint drug in the following doses.

Severity of a disease	Single dose	Interval between introductions
infections of urinary tract easy and moderate severity	0.5-1 in/in or in oil	each 12 h
other infections easy and moderate severity	1 g in/in or in oil	each 12 h
heavy infections	2 g in/in	each 12 h
life-threatening infections	2 g in/in	each 8 h

 

For prevention of possible infections when carrying out surgeries in 60 min. prior to operation the drug is administered in a dose 2 g in/in within 30 min. After the end of introduction in addition appoint metronidazole in/in in a dose of 500 mg. Solutions of metronidazole should not be entered along with drug Efipim. The infusional system before administration of metronidazole should be washed out. During long (more than 12 h) surgeries in 12 h after the first dose repeated introduction of an equal dose of drug of Efipims is recommended by the subsequent administration of metronidazole.

For children aged from 2 months the maximum dose should not exceed the recommended dose for adults. The average dose for children with body weight to 40 kg at the complicated or uncomplicated infections of urinary tract (including pyelonephritis), uncomplicated infections of skin and soft tissues, pneumonia, empirical treatment of neytropenichesky fever makes 50 mg/kg each 12 h.

To patients with neytropenichesky fever and bacterial meningitis drug is appointed on 50 mg/kg by each 8 h. The average duration of therapy makes 7-10 days. At heavy infections more long treatment can be required.

At patients with renal failures (KK less than 30 ml/min.) correction of the mode of a drug dosing is necessary. The initial dose of Efipim has to be same, as well as for patients with normal function of kidneys. Maintenance doses of drug define depending on KK values:

Clearance of creatinine (ml/min.)	The recommended doses
	2 g each 8 h	2 g each 12 h	1 g each 12 h
> 30	the average dose, corrections is not required
10-30	1 g each 12 h	1 g each 24 h	500 mg each 24 h
<10	1 g each 24 h	500 mg each 24 h	250 mg each 24 h

At a hemodialysis for 3 h from an organism about 68% of total quantity of Efipim are removed. At the end of each session it is necessary to enter the repeated dose equal to an initial dose. At the patients who are on continuous out-patient peritoneal dialysis to apply Efipimmozhno in the average recommended doses, i.e. 500 mg, 1 g or 2 g depending on weight of an infection, with an interval between introductions of a single dose of 48 h.

The same changes of the mode of dosing, as well as the adult as Efipim's pharmacokinetics at adults and children has similar character are recommended to children with renal failures.

Rules of preparation of solutions for parenteral administration. For preparation of solution for in/in introductions powder for injections in a bottle is dissolved in 5 ml or 10 ml of sterile water for injections, by 5% solution of glucose or 0.9% chloride sodium solution as it is specified in the table. In/in struyno Efipimvvodyat within 3-5 min. For introduction through system for in/in injections the prepared solution is combined with other solutions for in/in injections and entered within not less than 30 min. Solutions of drug of Efipimv of concentration from 1 to 40 mg/ml are compatible to the following solutions for parenteral administration: 0.9% chloride sodium solution for injections, 5% or 10% glucose solutions for injections, solution of 5% of glucose and 0.9% of sodium of chloride for injections, Ringer's solution with a lactate and 5% dextrose solution for injections. For preparation of solution for introduction in oil, powder for injections in a bottle is dissolved in sterile water for injections, by 5% glucose solution for injections or 0.9% chloride sodium solution for injections, bacteriostatic water for injections with paraben or benzyl alcohol, in 0.5% or 1% hydrochloride lidocaine solution as it is specified in the table:

Powder for injections	Solution volume for cultivations (ml)	Volume of received solution (ml)	Concentration In Efipy (mg/ml)
In/in introduction: 500 mg / фл. 1000 mg / фл.	5	5.6	100
	10	11.3	100
Introduction in oil: 500 mg / фл. 1000 mg / фл.	1.3	1.8	280
	2.4	3.6	280

The prepared drug solution for in/in and injections in oil is stable during 24 h at the room temperature, 7 days at storage in the refrigerator (2-8 °C).

Features of use:

Use at pregnancy and feeding by a breast. Use of drug during pregnancy is possible only under observation of the doctor and is justified only when the estimated advantage for mother exceeds potential risk for a fruit. Efipim is allocated with breast milk in very low concentration. However in the period of a lactation it is necessary to use drug with care.

Use for children. ротивопоказан at children's age up to 2 months. Use for children is more senior than 2 months perhaps according to the dosing mode.

Special instructions. For identification of a microorganism activator and definition of sensitivity to Efipim it is necessary to carry out the corresponding tests. At Efipim's appointment patients who are in group of the increased risk of developing of an infection at the expense of the mixed аэробно / anaerobic microflora (including in cases when one of activators is Bacteroides fragilis) before identification of the activator are recommended to appoint along with Efipim drug, active concerning anaerobe bacterias. Efipim with care appoint to patients with any forms of an allergy, especially at allergic reactions to medicines in the anamnesis. At emergence of allergic reactions against the background of therapy by Efipim it should be cancelled. At serious reactions of immediate hypersensitivity use of adrenaline and other forms of urgentny treatment can be required. At emergence of diarrhea against the background of treatment by Efipim it is necessary to consider a possibility of development of pseudomembranous colitis. Easy forms of colitis can independently pass after the termination of administration of drug; moderate or hard cases can demand special treatment. At Efipim's use (as well as other antibiotics) development of superinfection is possible that demands drug withdrawal and purpose of the corresponding treatment.

Influence on ability to driving of motor transport and to control of mechanisms. Does not influence.

Side effects:

Often: rash, diarrhea.

Infrequently: an itch, urticaria, fever, nausea, vomiting, oral cavity candidiasis, phlebitis or thrombophlebitis, pain and an inflammation in the place in oil or in/in an injection.

Seldom: the increased or lowered maintenance of some types of leukocytes, a neutropenia, thrombocytopenia, changes of coagulability of blood, a headache, paresthesia, reversible encephalopathy (changes of attention and consciousness, development of a coma, a hallucination, a myoclonus, spasms is possible) and/or heavy renal dysfunction, is more often at too high dose of a tsefepim at patients with an impaired renal function, especially at patients of advanced age. Usually symptoms of a neurotoxicity are reversible and are resolved after the therapy termination tsefepimy and/or a hemodialysis - moderately expressed and temporary increase in activity of some enzymes of a liver (AST-ALT)

Very seldom: the heavy anaphylaxis (acute anaphylaxis), abdominal pains, colitis, especially pseudomembranous colitis, ulcers in oral cavities, an agranulocytosis, confusion of consciousness, dizziness, spasms, a dysgeusia, tinnit, arterial hypotension, vasodilatation, decrease in concentration of calcium in blood, a swelling and morbidity of joints, a vaginitis.

Interaction with other medicines:

At simultaneous administration of solution of Efipim (as well as most of others beta лактамных antibiotics) with solutions of metronidazole, Vancomycinum, gentamycin, sulfate Tobramycinum perhaps pharmaceutical interaction. At Efipim's appointment with the listed drugs it is necessary to enter each antibiotic separately.

With extra care it is necessary to apply Efipim with aminoglycosides, furosemide and other loopback diuretics as increase nefro-and ototoxicity is possible at their combined use.

Contraindications:

— hypersensitivity to Efipimuili to L-arginine, and also to tsefalosporinovy antibiotics, penicillin or another beta лактамным to antibiotics;

— at administration of drug in oil it is necessary to consider contraindications to lidocaine (solvent);

— children's age up to 2 months.

Overdose:

Symptoms: at considerable overdose encephalopathy symptoms are possible.

Treatment: in cases of considerable exceeding of the recommended doses, especially at patients with renal failures, the hemodialysis is shown.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature below 25 °C. Period of storage 2 years.

Issue conditions:

According to the recipe

Packaging:

Bottles glass (1) - boxes cardboard.