Universal reference book for medicines
Product name: IMIPENEM AND CILASTATIN SPENSER (IMIPENEM AND CILASTATIN SPENSER)

Active substance: cilastatin, imipenem

Type: Carbapenem Group Antibiotic

Manufacturer: SPENSER PHARMA UK (UK) manufactured by COOPER PHARMA (India)
Composition, form of production and packaging
Powder for solution preparation for
intravenous administration 1 fl.

imipenem 500 mg

cilastatin sodium 500 mg

Vials (1) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Beta-lactam antibiotic of broad spectrum of action.
Suppresses the synthesis of the bacterial cell wall and has a bactericidal effect against a wide range of gram-positive and gram-negative microorganisms, aerobic and anaerobic.
Imipenem - a derivative of tienamycin, belongs to the group of carbapenems.

Cilastatin sodium inhibits dehydropeptidase, an enzyme that metabolizes imipenem in the kidneys, which significantly increases the concentration of unchanged imipenem in the urinary tract.
Cilastatin does not have its own antibacterial activity, does not inhibit? -lactamase bacteria.
The drug is active against Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus faecalis and Bacteroides fragilis.
Resistant to destruction by bacterial β-lactamase, which makes it effective against many microorganisms, such as Pseudomonas aeruginosa, Serratia spp. and Enterobacter spp., which are resistant to most beta-lactam antibiotics. The antibacterial spectrum includes virtually all clinically relevant pathogens.
It is active against gram-negative aerobic bacteria: Achromobacter spp., Acinetobacter spp.
(formerly Mima-Herellea), Aeromonas hydrophila, Alcaligenes spp., Bordetella bronchicanis, Bordetella bronchiseptica, Bordetella pertussis, Brucella melitensis, Campylobacter spp., Capnocytophaga spp., Citrobacter spp. (including Citrobacter diversus, Citrobacter freundii), Eikenella corrodens, Enterobacter spp. (including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (including strains forming beta-lactamase), Haemophilus parainfluenzae, Hafnia alvei, Klebsiella spp (inc. Klebsiella oxytoca, Klebsiella ozaenae, Klebsiella pneumoniae), Moraxella spp., Morganella morganii (formerly Proteus morganii), Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Yersinia spp. (formerly Pasteurella), incl. Yersinia multocida, Yersinia enterocolitica, Yersinia pseudotuberculosis; Plesiomonas shigelloides, Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp.(including Providencia alcalifaciens, Providencia rettgeri (formerly Proteus rettgeri), Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa, Pseudomonas fluorescens, Pseudomonas pseudomallei, Pseudomonas putida, Pseudomonas stutzeri), Salmonella spp. (including Salmonella typhi), Serratia spp.(including Serratia marcescens, Serratia proteamaculans), Shigella spp; (including penicillinase-producing strains), Staphylococcus epidermidis (including penicillinase-producing strains), Staphylococcus saprophyticus, Streptococcus (Staphylococcus epidermidis), Staphylococcus epidermidis (including strains forming penicillinase), Staphylococcus epidermidis (including strains forming penicillinase), Staphylococcus epidermidis, Staphylococcus epidermidis agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus group C, Streptococcus group G, greening streptococci including alpha and gamma-hemolytic strains); Gram-negative anaerobic bacteria: Bacteroides spp. (including Bacteroides distasonis, Bacteroides fragilis, Prevotella melaninogenica (formerly Bacteroides melaninogenicus), Bacteroides ovatus, Bacteroides thetaiotaomicronron, Bacteroides uniformis, Bacteroides vulgatus), Bilophila wadsworthia, Fusobacterium spp incl. (Fusobacterium necrophorum, Fusobacterium nucleatum), Porphyromonas asaccharolytica (formerly Bacteroides asaccharolyticus), Prevotella bivia (formerly Bacteroides bivius), Prevotella disiens (formerly Bacteroides disiens), Prevotella intermedia (formerly Bacteroides intermedius), Veillonella spp .; Gram-positive anaerobic bacteria: Actinomyces spp., Bifidobacterium spp., Clostridium spp. (including Clostridium perfringens), Eubacter spp., Lactobacillus spp., Microaerophilic streptococcus, Mobiluncus spp., Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp. (including Propionibacterium acne); other microorganisms: Mycobacterium fortuitum, Mycobacterium smegmatis.
Some Staphylococcus spp.
(resistant to methicillin), Streptococcus spp. (Group D), Stenotrophomonas maltophilia, Enterococcus faecium and some strains of Pseudomonas cepacia are insensitive to imipenem. Effective against many infections caused by bacteria, resistant to cephalosporins, aminoglycosides, penicillins. In vitro acts synergistically with aminoglycosides against some strains of Pseudomonas aeruginosa.
PHARMACOKINETICS

C max imipenem with iv administration at a dose of 250, 500 or 1000 mg for 20 minutes - 14-24, 21-58 and 41-83 μg / ml, respectively.
C max cilastatin with iv administration at a dose of 250, 500 or 1000 mg for 20 minutes - 15-25, 31-49 and 56-80 mcg / ml. Binding to plasma proteins imipenem - 20%, cilastatin - 40%.Quickly and well distributed in most tissues and body fluids. The highest concentrations are achieved in pleural effusion, peritoneal and interstitial fluids and reproductive organs. In low concentrations it is found in the cerebrospinal fluid. V d in adults is 0.23-0.31 l / kg, in children 2-12 years - 0.7 l / kg, in newborns - 0.4-0.5 l / kg.
Blocking tubular secretion of imipenem with cilastatin results in inhibition of its renal metabolism and accumulation in the urine in unchanged form.
Cilastatin is metabolized to the N-acetyl compound. With iv introduction of T 1/2 imipenem and cilastatin in adults - 1 h, in children 2-12 years - 1-1.2 h, in newborns T 1/2imipenem - 1.7-2.4 h, cilastatin - 3.8-8.4 h; when renal function T 1/2 imipenem is broken down - 2.9-4 hours, cilastatin - 13.3-17.1 hours. It is mainly excreted by the kidneys (70-76% for 10 hours) by glomerular filtration (2/3) and active tubular secretion (1 / 3); 1-2% is excreted through the gastrointestinal tract and 20-25% - by the extrarenal route (the mechanism is unknown).
Quickly and effectively (73-90%) is excreted by hemodialysis (as a result of a 3-hour session of intermittent hemofiltration, 75% of the dose is removed).

INDICATIONS

Infectious-inflammatory diseases caused by sensitive microorganisms (polymicrobial or mixed aerobic-anaerobic infections):

- infections of the lower respiratory tract;

- urinary tract infections;

- intra-abdominal infections;

- skin and soft tissue infections;

- infections of bones and joints;

- peritonitis;

- sepsis;

- endocarditis;

- inflammatory diseases of the pelvic organs.

Prevention of postoperative complications.

DOSING MODE

In / in the drip.

The following doses are calculated for a body weight of 70 kg and more and a creatinine clearance (CC) of 70 ml / min / 1.73 m2 and more .
For patients with SC less than 70 ml / min / 1.73 m2 and / or less body weight , the dose should be proportionally reduced.
The average therapeutic dose of adults on intravenous administration is 1-2 g / day, divided into 3-4 injections;
the maximum daily dose is 4 g or 50 mg / kg, depending on the toga, which dose will be lower.
Patients with mild infection severity - 250 mg 4 times / day, medium degree - 500 mg 3 times / day or 1 g 2 times / day, severe - 500 mg 4 times / day, with aninfection endangering the patient's life - 1 g 3-4 times / day.
Every 250-500 mg is administered intravenously for 20-30 minutes, and every 1 g for 40-60 minutes.
For the prevention of postoperative infections - 1 g during introductory anesthesia and 1 g in 3 hours. In the case of surgical intervention with a high risk of infection (surgery on the colon and rectum), 500 mg are additionally administered at 8 and 16 hours after general anesthesia.

Maximum daily doses for intravenous administration in patients with renal insufficiency, depending on the degree of infection severity and CK values ​​(ml / min / 1.73 m 2):

- for a mild course of infection and CC 41-70 ml / min - 250 mg after 8 hours, CC 21-40 ml / min - 250 mg after 12 hours, CC 6-20 ml / min - 250 mg after 12 hours ;

- for infection of medium severity and CK 41-70 ml / min - 250 mg after 6 hours, CC 21-40 ml / min - 250 mg after 8 hours, CC 6-20 ml / min - 250 mg after 12 hours ;

- In severe (high-sensitivity strains) and CC 41-70 ml / min - 500 mg every 8 hours, CC 21-40 ml / min - 250 mg after 6 hours, KK 6-20 ml / min - 250 mg after 12 hours;

- In severe cases (moderately sensitive strains, including Pseudomonas aeruginosa) and CC 41-70 ml / min - 500 mg every 6 hours, CC 21-40 ml / min - 500 mg after 8 hours, CC 6 -20 ml / min - 500 mg every 12 hours;

- In severe life-threatening infections, and CC 41-70 ml / min - 750 mg every 8 hours, CC 21-40 ml / min - 500 mg after 6 hours, KK 6-20 ml / min - 500 mg after 12 hours.

Patients with SC less than 5 ml / min are prescribed only if hemodialysis is performed every 48 hours, followed by 12 hours after the end of the procedure.

At present, there is insufficient data on the dosage regimen for preoperative prophylaxis of patients with SC less than 70 ml / min / 1.73 sq.m.

Children with a body weight of 40 kg and more - the same dose as an adult.

Children older than 3 months and with a body weight of less than 40 kg - 15 mg / kg 4 times / day;
the maximum daily dose is 2 g.
To prepare the infusion solution, 100 ml of solvent (0.9% sodium chloride solution, 5% aqueous dextrose solution, 10% aqueous dextrose solution, 5% dextrose solution and 0.9% sodium chloride) are added to the vial.
The concentration of imipenem in the resulting solution is 5 mg / ml.
SIDE EFFECT

From the nervous system: myoclonia, mental disorders, hallucinations, confusion, epileptic seizures, paresthesia.

From the urinary system: oliguria, anuria, polyuria, acute renal failure (rarely).

From the gastrointestinal tract: nausea, vomiting, diarrhea, pseudomembranous enterocolitis, hepatitis (rarely).

From the hematopoiesis and hemostasis system: eosinophilia, leukopenia, neutropenia, agranulocytosis.
thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis. basophilia, decreased hemoglobin, prolonged prothrombin time.
Laboratory indicators: increased activity of hepatic transaminases and alkaline phosphatase, hyperbilirubinemia.
hypercreatininaemia, increased urea nitrogen concentration, direct positive Coombs test.
Allergic reactions: skin rash, itching, urticaria, multiforme exudative erythema (including Stevens-Jopson's syndrome), angioedema, toxic epidermal necrolysis (rare), exfoliative dermatitis (rarely), fever, anaphylactic reactions.

Local reactions: thrombophlebitis.

Other: candidiasis, a taste disorder.

CONTRAINDICATIONS

- Pregnancy;

- lactation period;

- early childhood (up to 3 months);

- in children with impaired renal function (serum creatinine concentration more than 2 mg / dL);

- Hypersensitivity to the components of the drug, to carbapenems and other beta-lactam antibiotics.

With caution

Diseases of the central nervous system, gastrointestinal tract (including in the anamnesis), elderly age.

PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy and lactation.

APPLICATION FOR CHILDREN

Children with a body weight of 40 kg and more - the same dose as an adult.

Children older than 3 months and with a body weight of less than 40 kg - 15 mg / kg 4 times / day;
the maximum daily dose is 2 g.
Contraindicated:

- early childhood (up to 3 months);

- in children with impaired renal function (serum creatinine concentration more than 2 mg / dL).

APPLICATION IN ELDERLY PATIENTS

It should be borne in mind that elderly patients are likely to have age-related renal dysfunction, which may require a dose reduction.

SPECIAL INSTRUCTIONS

Not recommended for the treatment of meningitis.
Stains urine in a reddish color.
The dosage form for intravenous administration should not be used for in / m and vice versa.
Before the start of therapy, a thorough anamnesis should be made about the previous allergic reactions to beta-lactam antibiotics.
People who have a history of GIT disease (especially colitis), there is an increased risk of developing pseudomembranous enterocolitis.

Therapy with antiepileptic drugs in patients with brain injuries or seizures in the history should continue throughout the treatment period with the drug (to avoid side effects from the CNS).

It should be borne in mind that elderly patients are likely to have age-related renal dysfunction, which may require a dose reduction.

OVERDOSE

Symptoms: may increase the side effects.

There is no specific information on the treatment of drug overdose.
Imipenem and cilastatin undergo hemodialysis. However, the effectiveness of this procedure with an overdose of the drug is unknown.
DRUG INTERACTION

Pharmaceutically incompatible with the salt of lactic acid, other antibacterial drugs.

With simultaneous use with penicillins and csphalosporins, a cross allergy is possible;
shows antagonism towards other beta-lactam antibiotics (penicillins, cephalosporins and monobactams).
Ganciclovir increases the risk of developing generalized seizures.

Drugs that block tubular secretion, slightly increase the concentration in the plasma and T 1/2 imipenem (if high concentrations of imipenem are required, it is not recommended to use these medicines at the same time).

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