CEFADROXIL TABLETS, USP AND CEFADROXIL CAPSULES, USP
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Cefadroxil Tablets and Cefadroxil Capsules and other antibacterial drugs, Cefadroxil Tablets and Cefadroxil Capsules should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Cefadroxil , USP (hemihydrate) is a semisynthetic cephalosporin antibiotic intended for oral administration. It is white to off-white crystalline powder. It is slightly soluble in water and it is acid-stable. It is chemically designated as 5-Thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylic acid, 7-[[amino (4-hydroxyphenyl) acetyl] amino]-3- methyl-8-oxo-, hemihydrate, [6R-[6α, 7β (R*)]]-. It has the formula C16H17N3O5S•½ H2O and the molecular weight of 372.39. It has the following structural formula:
Each film coated tablet for oral administration contains Cefadroxil hemihydrate equivalent to 1 gram cefadroxil. In addition, each tablet contains the following inactive ingredients: croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, monosodium citrate, polyethylene glycol, talc and titanium dioxide.
Each capsule for oral administration contains Cefadroxil hemihydrate equivalent to 500 mg cefadroxil. In addition, each capsule contains the following inactive ingredients: magnesium stearate and pregelatinized starch.
The capsule shell also contains D&C yellow no. 10, FD&C blue no. 1, FD&C red no. 40, gelatin and titanium dioxide.
The imprinting ink also contains D&C yellow no. 10 aluminum lake, FD&C blue no. 1 aluminum lake, FD&C blue no. 2 aluminum lake, FD&C red no. 40 aluminum lake, pharmaceutical glaze, propylene glycol and synthetic black iron oxide.
Cefadroxil is rapidly absorbed after oral administration. Following single doses of 500 and 1000 mg, average peak serum concentrations were approximately 16 and 28 mcg/mL, respectively. Measurable levels were present 12 hours after administration. Over 90% of the drug is excreted unchanged in the urine within 24 hours. Peak urine concentrations are approximately 1800 mcg/mL during the period following a single 500 mg oral dose. Increases in dosage generally produce a proportionate increase in cefadroxil urinary concentration. The urine antibiotic concentration, following a 1-g dose, was maintained well above the MIC of susceptible urinary pathogens for 20 to 22 hours.
In vitro tests demonstrate that the cephalosporins are bactericidal because of their inhibition of cell-wall synthesis. Cefadroxil has been shown to be active against the following organisms both in vitro and in clinical infections (see INDICATIONS AND USAGE):
Staphylococci, including penicillinase-producing strains
Streptococcus (Diplococcus) pneumoniae
Moraxella (Branhamella) catarrhalis
Note: Most strains of Enterococcus faecalis (formerly Streptococcus faecalis) and Enterococcus faecium (formerly Streptococcus faecium) are resistant to cefadroxil. It is not active against most strains of Enterobacter species, Morganella morganii (formerly Proteus morganii), and P. vulgaris. It has no activity against Pseudomonas species and Acinetobacter calcoaceticus (formerly Mima and Herella species).
Susceptibility tests: Diffusion techniques
The use of antibiotic disk susceptibility test methods which measure zone diameter give an accurate estimation of antibiotic susceptibility. One such standard procedure1 which has been recommended for use with disks to test susceptibility of organisms to cefadroxil uses the cephalosporin class (cephalothin) disk. Interpretation involves the correlation of the diameters obtained in the disk test with the minimum inhibitory concentration (MIC) for cefadroxil.
Reports from the laboratory giving 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||(S) Susceptible|
|15 to 17||(I) Intermediate|
|≤ 14||(R) Resistant|
A report of “Susceptible” indicates that the pathogen is likely to be inhibited by generally achievable blood levels. A report of “intermediate susceptibility” suggests that the organism would be susceptible if high dosage is used or if the infection is confined to tissue and fluids (e.g., urine) in which high antibiotic levels are attained. A report of “Resistant” indicates that achievable concentrations of the antibiotic are unlikely to be inhibitory and other therapy should be selected.
Standardized procedures require the use of laboratory control organisms. The 30 mcg cephalothin disk should give the following zone diameters:
| Organism || Zone Diameter (mm) |
| Staphylococcus aureus ATCC 25923||29 to 37|
| Escherichia coli ATCC 2 5922||17 to 22|
When using the NCCLS agar dilution or broth dilution (including microdilution) method2 or equivalent, a bacterial isolate may be considered susceptible if the MIC (minimum inhibitory concentration) value for cephalothin is 8 mcg/mL or less. Organisms are considered resistant if the MIC is 32 mcg/mL or greater. Organisms with an MIC value of less than 32 mcg/mL but greater than 8 mcg/mL are intermediate.
As with standard diffusion methods, dilution procedures require the use of laboratory control organisms. Standard cephalothin powder should give MIC values in the range of 0.12 mcg/mL and 0.5 mcg/mL for Staphylococcus aureus ATCC 29213. For Escherichia coli ATCC 25922, the MIC range should be between 4 mcg/mL and 16 mcg/mL. For Streptococcus faecalis ATCC 29212, the MIC range should be between 8 and 32 mcg/mL.