Imipenem + Cilastatin - instructions for use, dose, side effects, contraindications

A complex preparation consisting of two elements: imipenem and cilastatin sodium in a ratio of 1: 1; retains a high activity against groups of Gram-positive aerobic cocci that are insensitive to other antibiotics (cephalothin, cefotaxime, moxalactam, cefoxitin, ceftazidime, cefamandol and ceftriaxone): Staphylococcus aureus, Streptococcus faecalis; gram-negative - Enterobacter spp., Serratia spp., Pseudomonas aeruginosa and others, resistant to the action of most β-lactam antibiotics, as well as anaerobes (Bacteroides fragilis).

Imipenem

Has bactericidal action due to inhibition of bacterial cell wall synthesis. Violates the synthesis of peptidoglycan - a biopolymer, the main component of the bacterial cell wall. It inhibits the peptidoglycan transpeptidase, inhibits the activity of the endogenous inhibitor, which leads to activation of murein hydrolase, which cleaves peptidoglycan. Effective against fissile bacteria, in the walls of which the synthesis of peptidoglycan occurs.

Cilastatin

Inhibits dehydropeptidase, which takes part in the metabolism of imipenem in the kidneys, due to which the concentration of the drug increases in the urinary tract. Do not inhibit β-lactamase bacteria - does not have its own antibacterial activity.

Pharmacokinetics:

Imipenem

After intramuscular injection, the bioavailability is 95%, the maximum concentration in the blood plasma is reached after 20 minutes. The connection with plasma proteins is 20%. Penetrates through the blood-brain barrier.

The highest concentrations are achieved in peritoneal and interstitial fluids, pleural effusion and reproductive organs. Cilastatin blocks the tubular secretion of imipenem, which leads to inhibition of its renal metabolism.

The elimination half-life is 1 hour. Elimination of the kidneys for 10 hours in unchanged form.

Cilastatin

After intramuscular injection, the bioavailability is 95%, the maximum concentration in the blood plasma is reached after 20 minutes. The connection with plasma proteins is 40%.

Half-life is 2-3 hours. Elimination of the kidneys for 10 hours in unchanged form.

The drug is removed during hemodialysis.

Indications:

It is used to treat infectious diseases caused by pathogens sensitive to the drug: bone and connective tissue, skin and subcutaneous tissue, lower respiratory tract, septicemia, peritonitis, urinary tract infections.

ICD-10

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A41 Other septicemia

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J20-J22.J20 Acute bronchitis

X.J40-J47.J40 Bronchitis, not specified as acute or chronic

X.J40-J47.J42 Chronic bronchitis, unspecified

XIV.N70-N77.N73.3 Acute pelvic peritonitis in women

XI.K65-K67.K65.0 Acute peritonitis

XI.K35-K38.K35.1 Acute appendicitis with peritoneal abscess

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K83.0 Cholangitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M00-M03.M00 Pyogenic arthritis

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N15.1 Abscess of kidney and adrenal tissue

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N70 Salpingitis and oophoritis

XIV.N70-N77.N71.0 Acute inflammatory disease of the uterus

XIV.N70-N77.N71.1 Chronic inflammatory disease of the uterus

XIV.N70-N77.N72 Inflammatory disease of the cervix

XIV.N70-N77.N73.0 Acute parametritis and pelvic cellulite

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:

Individual intolerance to β-lactam antibiotics: penicillins and cephalosporins,children's age up to 3 months.

Carefully:

Pseudomembranous colitis, diseases of the central nervous system, imbalance of electrolytes or fluids, severe liver damage.

Pregnancy and lactation:

Recommendations for FDA - category C. It is used in pregnancy for vital indications, during application it is necessary to stop lactation, as the drug penetrates into breast milk.

Dosing and Administration:

Use in children

- from body weight of 40 kg apply the same dose as for adults;

- with a body weight of less than 40 kg, the dose is applied at a rate of 15 mg / kg at 6-hour intervals.

The total daily dose should not exceed 2 g.

It is not used to treat meningitis.

Adults

Intramuscularly deep 1-2% solution of lidocaine with a preliminary skin test for tolerability, 500-750 mg every 12 hours.

The highest daily dose: 1.5 g.

The highest single dose: 750 mg.

Side effects:

Central and peripheral nervous system: encephalopathy, myoclonia, paresthesia, headache, hallucinations, tremor.

Respiratory system: shortness of breath, hyperventilation.

Hemopoietic system: thrombocytopenia, eosinophilia, leukopenia, an increase in prothrombin index and coagulation time.

The cardiovascular system: tachycardia, palpitations.

Digestive system: nausea, vomiting, diarrhea, increased activity of hepatic enzymes, hepatic or cholestatic jaundice, intestinal dysbacteriosis.

urinary system: polyuria, oliguria, proteinuria, cylindruria, rarely - acute renal failure.

Sense organs: a change in taste, a decrease in hearing.

Dermatological reactions: local reactions - compaction at the injection site, candidiasis dermatitis, vulvovaginitis.

Allergic reactions.

Overdose:

Nausea, vomiting, diarrhea, neuromuscular excitability, convulsive attacks.

Treatment is symptomatic, hemodialysis.

Interaction:

Reduces the level of valproic acid in the blood plasma, which can lead to sudden seizures.

With simultaneous use with ganciclovir, the risk of developing generalized seizures increases.

Special instructions:

Before applying imipenem, a skin test is required for sensitivity, in view of the high likelihood of polyvalent allergy in persons with hypersensitivity to penicillins and cephalosporins.

With intramuscular injection, you need to make sure that the drug does not enter the blood vessel.

Instructions

Imipenem + Cilastatin (Imipenemum + Cilastatinum)