Cephalexin

CEPHALEXIN- cephalexin powder, for suspension
Rebel Distributors Corp

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Cephalexin for Oral Suspension, USP and other antibacterial drugs, Cephalexin for Oral Suspension, USP should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

DESCRIPTION

Cephalexin, USP is a semisynthetic cephalosporin antibiotic intended for oral administration. It is 7-(D-α-Amino-α-phenylacetamido)-3-methyl-3-cephem-4-carboxylic acid monohydrate. Cephalexin has the molecular formula C16 H17 N3 O4 S•H2 O and the molecular weight is 365.41.

Cephalexin has the following structural formula:

mjbivjb
(click image for full-size original)

The nucleus of cephalexin is related to that of other cephalosporin antibiotics. The compound is a zwitterion; i.e., the molecule contains both a basic and an acidic group. The isoelectric point of cephalexin in water is approximately 4.5 to 5.

The crystalline form of cephalexin which is available is a monohydrate. It is a white crystalline solid having a bitter taste. Solubility in water is low at room temperature; 1 or 2 mg/mL may be dissolved readily, but higher concentrations are obtained with increasing difficulty.

The cephalosporins differ from penicillins in the structure of the bicyclic ring system. Cephalexin has a D- phenylglycyl group as substituent at the 7-amino position and an unsubstituted methyl group at the 3-position.

Cephalexin for Oral Suspension, USP is a white to off white granular powder with characteristic flavor, and gives orange colored viscous suspension after reconstitution with water.

After mixing, each 5 mL of Cephalexin for Oral Suspension, USP, will contain cephalexin monohydrate equivalent to 125 mg (360 micro mol) or 250 mg (720 micro mol) of anhydrous cephalexin. The suspensions also contains the following inactive ingredients: colloidal silicon dioxide, FD&C Yellow No.6, tutti-frutti flavor, orange flavor, sodium lauryl sulphate, sucrose and xanthan gum.

CLINICAL PHARMACOLOGY

Human Pharmacology:

Cephalexin is acid stable and may be given without regard to meals. It is rapidly absorbed after oral administration. Following doses of 250 mg, 500 mg, and 1 g, average peak serum levels of approximately 9, 18, and 32 mcg/mL respectively were obtained at 1 hour. Measurable levels were present 6 hours after administration. Cephalexin is excreted in the urine by glomerular filtration and tubular secretion. Studies showed that over 90% of the drug was excreted unchanged in the urine within 8 hours. During this period, peak urine concentrations following the 250-mg, 500-mg, and 1-g doses were approximately 1000, 2200, and 5000 mcg/mL respectively.

Microbiology:

In vitro tests demonstrate that the cephalosporins are bactericidal because of their inhibition of cell-wall synthesis. Cephalexin has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section.

Aerobes, Gram-positive:

Staphylococcus aureus (including penicillinase-producing strains)

Streptococcus pneumoniae (penicillin-susceptible strains)

Streptococcus pyogenes

Aerobes, Gram-negative:

Escherichia coli

Haemophilus influenzae

Klebsiella pneumoniae

Moraxella (Branhamella) catarrhalis

Proteus mirabilis

Note – Methicillin-resistant staphylococci and most strains of enterococci (Enterococcus faecalis [formerly Streptococcus faecalis ]) are resistant to cephalosporins, including cephalexin. It is not active against most strains of Enterobacter spp., Morganella morganii, and Proteus vulgaris. It has no activity against Pseudomonas spp. or Acinetobacter calcoaceticus. Penicillin — resistant Streptococcus pneumoniae is usually cross-resistant to beta-lactam antibiotics.

Susceptibility Tests

Dilution Techniques:

Quantitative methods are used to determine antimicrobial minimal inhibitory concentrations (MIC’s). These MIC’s provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MIC’s should be determined using a standardized procedure. Standardized procedures are based on a dilution method1-3 (broth or agar) or equivalent with standardized inoculum concentrations and standardized concentrations of cephalothin powder. The MIC values should be interpreted according to the following criteria:

MIC (mcg/mL) Interpretation
≤8 Susceptible (S)
16 Intermediate (I)
≥32 Resistant (R)

A report of “Susceptible” indicates that the pathogen is likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where high dosage of drug can be used. This category also provides a buffer zone which prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the pathogen is not likely to be inhibited if the antimicrobial compound in the blood reaches the concentrations usually achievable; other therapy should be selected.

Standardized susceptibility test procedures require the use of laboratory control microorganisms to control the technical aspects of the laboratory procedures. Standard cephalothin powder should provide the following MIC values:

Microorganism MIC (mcg/mL)
E. coli ATCC 25922 4-16
S. aureus ATCC 29213 0.12-0.5
Diffusion Techniques:

Quantitative methods that require measurement of zone diameters also provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. One such standardized procedure2,3 requires the use of standardized inoculum concentrations. This procedure uses paper disks impregnated with 30-mcg cephalothin to test the susceptibility of microorganisms to cephalexin.

Reports from the laboratory providing results of the standard single-disk susceptibility test with a 30-mcg cephalothin disk should be interpreted according to the following criteria:

Zone Diameter (mm) Interpretation
≥18 Susceptible (S)
15-17 Intermediate (I)
≤14 Resistant (R)

Interpretation should be as stated above for results using dilution techniques. Interpretation involves correlation of the diameter obtained in the disk test with the MIC for cephalexin.

As with standard dilution techniques, diffusion methods require the use of laboratory control microorganisms that are used to control the technical aspects of the laboratory procedures. For the diffusion technique, the 30-mcg cephalothin disk should provide the following zone diameters in these laboratory test quality control strains:

Microorganism Zone Diameter (mm)
E. coli ATCC 25922 15-21
S. aureus ATCC 25923 29-37
Page 1 of 4 1 2 3 4

All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.

This site is provided for educational and informational purposes only, in accordance with our Terms of Use, and is not intended as a substitute for the advice of a medical doctor, nurse, nurse practitioner or other qualified health professional.

Privacy Policy | Copyright © 2024. All Rights Reserved.