Cefepime hydrochloride is a parenteral "fourth-" generation Cephalosporin antibiotic. It has an expanded spectrum of activity against gram-positive and gramnegative microbes as compared to the third-generation cephalosporins. In addition, pathogens resistant to other cephalosporins may be eradicated by Cefepime.
The chemical structure of cefepime allows it to bind to penicillin-binding proteins and to penetrate through the outer membrane of gram-negative bacteria more rapidly than most cephalosporins. Cefepime is also more stable to ß-lactamase hydrolysis, making for an enhanced resistance pattern, especially with gram-negative bacteria. Cefepime is indicated for use in uncomplicated and complicated urinary tract infections, uncomplicated skin and skin structure infections, and moderate to severe pneumonia. Amikacin is an aminoglycoside used to treat different types of bacterial infections.
Amikacin works by binding to the bacterial 30S ribosomal subunit, causing misreading of mRNA and leaving the bacterium unable to synthesize proteins vital to its growth. Cefepime and Amikacin, combination of these two different antibiotics act synergistically to provide total solution against multi resistant bacteria like P.aeruginosa, Acinetobacter spp and methicilin resistant S.aureus. Of these two antibiotics one is protein synthesis inhibiting antibiotic and another is non-protein synthesis inhibiting antibiotic. Combination of these two antibiotics have lesser nephrotoxicity as compared to other combinations. They are administered as a single composition parentally.
Our organization - Venus Remedies is in grant of a patent for this drug combination as a single compound which can be administered parentally. Extended-spectrum -lactamase (ESBL) production is one of the main mechanisms of resistance to lactam antibiotics among the strains of the family Enterobacteriaceae. The therapeutic choices in infections caused by such strains remain limited because of cross-resistance. In such cases combination of the above mentioned antibiotics provide a solution.
Bactericidal activity against wide range of organisms including multi resistant bacteria, better efficacy and safety, lesser dose than the individual antibiotics, least nephrotoxicity when compared to other combinations of aminoglycosides and cephalosporins, minimization in development of resistance, reduction in hospitalization time, reduction in treatment cost to patient Protein synthesis inhibiting antibiotic means an agent that disrupts the bacterial ribosome cycle through which polypeptide chain initiation and elongation is normally effected.
Amikacin in the above combination is a protein synthesis inhibiting antibiotic. Other examples of Protein synthesis inhibiting antibiotics are aminoglycosides such as gentamycin, kanamycin, netilmicin, streptomycin, tobramycin, macrolides such as erythromycin, lincomycin, tetracyclines like tetracycline, doxycycline, chlortetracycline and minocycline, oxazolidinones such as linezolid, fusidic acid and chloramphenicol.
Non protein synthesis inhibiting antibiotic means antibiotics other than protein synthesis inhibiting antibiotics. The second antibiotic used in the combination i.e., cefepime belongs to this class. Other examples of this class include penicillins, cephalosporins, carbapenems like imipenem and meropenem, quinolones such as ciprofloxacin, moxifloxacin and levofloxacin This antibiotic combination further consists of stabilizing agent such as L-arginine which stabilizes two non compatible antibiotics as a single product.
The amount of amikacin present is 400mg to 600mg, cefepime in an amount of 2g to 4g and arginine in the amount of 600mg to 1.2 gm. It exists as a dry powder form along with stabilizing agent which is reconstituted before injection with a suitable solvent. This product is preferably twice a day product depending on the patient condition and severity of infection, wherein the administration of the antibiotic product is a concentrate which is diluted before administration in suitable infusions.
The combination dosage form after reconstitution is a sterile, colorless to light straw colored solution with the pH of the solution in the range from about 3.5 to 6.The average period of treatment with this combination is 9 to 10 days and is successful in more than 95% patients. The combination is provided in a sealed container such as transparent glass vial capped with appropriate halogenated stopper and seal, and is used for reconstitution for intramuscular or intravenous administration for the treatment of acute or serious bacterial infections.