CILAVIL 500mg/500mg 

CILAVIL 500mg/500mg

Imipenem/Cilastatin (Cilavil^®)

Description

(Imipenem and Cilastatin for Injection) is a potent broad spectrum antibacterial agent for intravenous administration.

Clinical pharmacology

(Imipenem and Cilastatin for Injection) is a sterile formulation of imipenem (a thienamycin antibiotic) and cilastatin sodium (the inhibitor of the renal dipeptidase, dehydropeptidase I), with sodium bicarbonate added as a buffer.

The bactericidal activity of imipenem results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B.

Imipenem has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases produced by gram-negative and gram-positive bacteria. It is a potent inhibitor of beta-lactamases from certain gram-negative bacteria which are inherently resistant to most beta-lactam antibiotics, e.g., Pseudomonas aeruginosa, Serratia spp., and Enterobacter spp.

Antibacterial activity

Imipenem has in vitro activity against a wide range of gram-positive and gram- negative organisms. It has a high degree of stability in the presence of beta-lactamases, including penicillinases and cephalosporinases produced by grm-negative and gram- positive bacteria. It is a potent inhibitor of β- lactamases from certan gram-negative bacteria resistant to many beta-lactam antibiotics (eg, pseudomonas aeruginosa, Serratia sp., Enterobacter sp.).

In vitro, imipenem is active against most strains of clinical isolates in the following microorganisms: Gram-positive aerobes; streptococcus; gram-negative aerobes; gram-positive anaerobes; gram-negative anaerobes.

In viro tests show imipenem to act synergistically with aminoglycoside antibiotics against some isolates of Pseudomonas aerugnosa.

Pharmacokinetics

Oral absorption -

Presystemic metabolism -

Plasma half – life

(Each component) 1 h

Mean

- Imipenem 91±7.0 min

- Cilastatin 69±15 min

Volume of distribution 14.4 L

Plasma protein binding

- Imipenem 20%

- Cilastatin 40%

Indication

1- Lower respiratory tract infections.

2- Skin and skin-structure infections.

3- Urinary tract infections.

4- Bacterial septicemia.

5- Bone & joint infections.

6- Gynecologic infections.

7- Intra-abdominal infections.

8- Endocarditis.

9- Polymicrobic infections.

Contraindication

Imipenem I.V. is contraindicated in patients who have shown hypersensitivity to any component of this product.

Precaution

· While Imipenem/Cilastatin has the characteristic low toxicity of the beta-lactam group of antibiotics, periodically assess organ system functions, including renal, hepatic, and hematopoietic, during prolonged therapy.

· For patients on hemodialysis, Imipenem/Cilasatin is recommended only when the benefit outweighs the potential risk of seizures.

· Close adherence to the recommended dosage and dosage schedules is urged, especially in patients with known factors that predispose to convulsive activity.

· Use caution when administering to patients with a history of penicillin allergy due o a possible cross-sensitivity to Imipenem/ Cilastatin.

· As with other antibiotics, prolong use of Imipenem/Cilastatin may result in overgrowth of nonsusceptible organisms.

Pregnancy

Pregnancy category C.

There are no adequate and well – controlled studies in pregnant women. Therefore Imipenem should be used during pregnancy only if clearly needed.

Breast feeding

It is not known whether this drug is excreted in breast milk. Caution should be exercised when it is administered to a nursing woman.

Dosage

Usual adult dose

Intravenous Dosage Schedule for Adults with Normal Renal Function and Body Weight >/=70 kg

Imipenem-Cilastatin IV Dosing Schedule for Adults with Normal Renal Function
Type or severity of infection	Fully susceptible organismsª	Total daily dose	Moderately susceptible organisms, primarily some strains of P.aeruginosa	Total daily dose
Mild	250 mg every 6 h	1 g	500 mg every 6 h	2g
Moderate	500 mg every 8 h or 500 mg every 6 h	1.5 or 2 g	500 mg every 6 h or 1 g every 8 h	2 or 3 g
Severe,life     threatening	500 mg every 6 h	2g	1 g every 8 h or 1 g every 6 h	3 or 4 g
Uncomplicated UTI	250 mg every 6 h	1g	250 mg every 6 h	1g
Complicated UTI	500 mg every 6 h	2g	500 mg