Tsilapenem

General characteristics. Structure:

Active ingredients: 250 mg or 500 mg of an imipenem of monohydrate (in terms of imipeny), 250 mg or 500 mg of a tsilastatin of sodium salt (in terms of циластатин) in the form of mix of an imipenem and a tsilastatin of sodium salt.

Pharmacological properties:

Pharmacodynamics. Tsilapenem – an antibiotic of a broad spectrum of activity. Suppresses synthesis of a cell wall of bacteria and has bactericidal effect concerning a wide range of microorganisms. The antibacterial range includes practically all clinically significant pathogenic microorganisms. It is effective against many infections caused by the bacteria steady against cephalosporins, aminoglycosides, penicillin.

Indications to use:

Intra belly infections, infections of lower parts of respiratory tracts, urinogenital system, bones and joints, skin and soft tissues, bodies of a small pelvis, sepsis, bacterial endocarditis, prevention of postoperative infections, multi-infections, intrahospital infections, etc.

Route of administration and doses:

The drug is administered intravenously, kapelno. The dosage form for introduction in oil should not be used for in/in infusions and vice versa. Doses are calculated the doctor proceeding from the body weight of the patient and a condition of function of kidneys. In/in a way of introduction it is more preferable to use at the initial stages of therapy of bacterial sepsis, endocarditis, etc. heavy and life-threatening infections, including infections of lower parts of the respiratory tracts caused by Pseudomonas aeruginosa and in case of heavy complications.

Average therapeutic dose for adults at in introduction - 1-2 g/days, divided into 3-4 introductions; the maximum daily dose - 4 g or 50 mg/kg depending on what dose will be smaller. The patient with easy severity of an infection - on 250 mg 4 times a day, average degree - 500 mg 3 times a day or 1 g 2 times a day, heavy degree - 500 mg 4 times a day, at an infection, life-threatening the patient, - 1 g 3-4 times a day. Each 250-500 mg enter in/in within 20-30 min., and each 1 g - within 40-60 min. For prevention of postoperative infections - 1 g during introduction anesthesia and 1 g - in 3 h. In case of surgical intervention with a high risk of development of an infection (operation on thick and a rectum) in addition enter on 500 mg in 8 and 16 h after the general anesthesia.

For preparation of infusion solution add 100 ml of solvent to a bottle (0.9% NaCl solution, 5% aqueous solution of a dextrose, 10% aqueous solution of a dextrose, solution of 5% of a dextrose and 0.9% of NaCl, etc.). Average therapeutic dose for adults at in introduction - 1-2 g/days, divided into 3-4 introductions; the maximum daily dose - 4 g or 50 mg/kg depending on what dose will be smaller. The patient with easy severity of an infection - on 250 mg 4 times a day, average degree - 500 mg 3 times a day or 1 g 2 times a day, heavy degree - 500 mg 4 times a day, at an infection, life-threatening the patient, - 1 g 3-4 times a day. Each 250-500 mg enter in/in within 20-30 min., and each 1 g - within 40-60 min. For prevention of postoperative infections - 1 g during introduction anesthesia and 1 g - in 3 h. In case of surgical intervention with a high risk of development of an infection (operation on thick and a rectum) in addition enter on 500 mg in 8 and 16 h after the general anesthesia. For prevention of postoperative infections at adults - on 1 g at introduction anesthesia and repeatedly in 3 h; at surgical interventions with a high risk (on thick and a rectum) - in addition enter on 500 mg in 8 and 16 h after the beginning of the general anesthesia.

To children with the body weight of 40 kg and more - the same doses, as the adult; with body weight less than 40 kg - 15 mg/kg 4 times a day; the maximum daily dose - 2 g.

The maximum daily doses for in/in introductions at patients are calculated the doctor depending on severity of an infection and expressiveness of a renal failure with a renal failure. 

Features of use:

During pregnancy drug is used only according to "vital" indications when the expected advantage of treatment justifies potential risk for a fruit.

It is unknown whether this drug with maternal milk is emitted. For treatment it is necessary to stop breastfeeding.

Precautionary measures. It is not recommended for treatment of meningitis. Paints urine in reddish color. At the persons having in digestive tract diseases (especially colitis), the increased risk of development of a pseudomembranous coloenteritis is noted. Therapy by antiepileptic medicines at patients with brain injuries or attacks in the anamnesis has to continue the entire period of treatment by drug. At elderly patients existence of age renal failures is probable that can demand dose adjustment by the attending physician.

Side effects:

From a nervous system: myoclonia, mental disturbances, hallucinations, confusion of consciousness, epileptic seizures, paresthesias.

From an urinary system: oliguria, anury, polyuria, acute renal failure (seldom).

From the alimentary system: nausea, vomiting, diarrhea, pseudomembranous coloenteritis, hepatitis (seldom).

From bodies of a hemopoiesis and system of a hemostasis: eosinophilia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis, basophilia, decrease in Hb, lengthening of a prothrombin time, positive reaction of Koombs.

Laboratory indicators: increase in activity of "hepatic" transaminases and ShchF, hyperbilirubinemia, giperkreatininemiya, increase in concentration of an urea nitrogen; direct positive test of Koombs.

Allergic reactions: skin rash, itch, small tortoiseshell, multiformny exudative erythema (including Stephens-Johnson's syndrome), Quincke's disease, toxic epidermal necrolysis (seldom), exfoliative dermatitis (seldom), fever, anaphylactic reactions.

Local reactions: a dermahemia, painful infiltrate in an injection site, thrombophlebitis.

Others: candidiasis, taste disturbance.

Interaction with other medicines:

Pharmaceutical it is incompatible with salt of lactic acid, other antibacterial medicines.

At simultaneous use with penicillin and cephalosporins the cross allergy is possible; shows antagonism in relation to others beta лактамным to antibiotics (penicillin, cephalosporins and monobaktama).

Gantsiklovir increases risk of development of generalized spasms.

The medicines blocking canalicular secretion slightly increase concentration in plasma and T1/2 of an imipenem (if high concentration of an imipenem are required, it is not recommended to apply these HP at the same time).

Contraindications:

Hypersensitivity (including to karbapenema, etc. beta лактамным to antibiotics), pregnancy (only according to "vital" indications), early children's age (up to 3 months); children have a heavy renal failure (concentration of serumal creatinine more than 2 mg/dl). For suspension at the injection in oil prepared with hydrochloride lidocaine use as solvent - hypersensitivity to local anesthetics of amide structure (shock, disturbance of endocardiac conductivity). With care apply at TsNS diseases, in the period of a lactation, at advanced age.

Overdose:

Specific symptoms are absent. At overdose by drug strengthening of side effect is possible. There is no special information on overdose treatment tsilapenemy. Tsilapenem is exposed to a hemodialysis. However efficiency of this procedure at overdose is unknown.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for infusions of 0,25 g and 0,5 g in bottles.