Antimicrobial activity

Resembles closely that of cefalexin

Pharmacokinetics

Oral absorption: >90% Cmax 250 mg oral: c. 9 mg/L after 1.2 h 500 mg oral: c. 18 mg/L after 1.2 h Plasma half-life: 1–1.5 h Plasma protein binding : 20% Absorption is little affected by administration with food. Distribution is similar to that of cefalexin. It is eliminated unchanged by glomerular filtration and tubular secretion; 90% of the dose appears in the urine over 24 h, most in the first 6 h, producing concentrations exceeding 500 mg/L.

Pharmacology

Cefadroxil has a broad spectrum of antimicrobial action; it is active with respect to Grampositive and Gram-negative microorganisms. Like all of the other drugs described above, it acts as a bactericide by disrupting the process of restoring the membranes of bacteria. Synonyms of this drug are bidocef, cefadril, duracef, ultracef, and others.

Side effects

Side effects described are those common to oral cephalosporins.

Synthesis

Cefadroxil, [6R-[6α,7β(R)]]-3-methyl-8-oxo-7-[[amino(4-hydroxyphenyl) acetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (32.1.2.14), is an analog of cephalexin and differs only in the presence of a hydroxyl group in the fourth position of the phenyl ring of phenylglycine, and is synthesized by a scheme analogous to the scheme of cephradin synthesis.

Veterinary Drugs and Treatments

Cefadroxil is approved for oral therapy in treating susceptible infections of the skin, soft tissue, and genitourinary tract in dogs and cats. The veterinary oral tablets have been discontinued (in the USA), but human-labeled oral capsules and tablets are still available.

in vitro

the inhibitory activity of Cefadroxil was similar to that of cephalexin and cephradine when tested against 602 clinical isolates on mueller-hinton medium. in the oral treatment of experimental infections of mice, cefadroxil was more effective than cephalexin against streptococcus pyogenes, and comparably effective against streptococcus pneumoniae, staphylococcus aureus, and several gram-negative species [1].

in vivo

in mice, oral administration of cefadroxil at doses ranging from 25 to 100 mg/kg attained peak concentrations in the blood. higher peak levels were noted with cefadroxil than with cephalexin at a dose of 200 mg/kg [1].

Drug interactions

Potentially hazardous interactions with other drugs Anticoagulants: effects of coumarins may be enhanced.

Metabolism

More than 90% of a dose of cefadroxil may be excreted unchanged in the urine within 24 hours by glomerular filtration and tubular secretion.

references

[1] buck r e, price k e. cefadroxil, a new broad-spectrum cephalosporin[j]. antimicrobial agents and chemotherapy, 1977, 11(2): 324-330.[2] gerber m a, randolph m f, chanatry j, et al. once daily therapy for streptococcal pharyngitis with cefadroxil[j]. the journal of pediatrics, 1986, 109(3): 531-537.

Brand Name(s) in US

Veterinary: Cefa-Tabs, Cefa-Drops? Human dosage form: Duricef and generic

Definition

ChEBI: The hydrate that is the monohydrate of the cephalosporin cefadroxil.

Brand name

Duricef (Bristol-Myers Squibb); Ultracef (Bristol Labs).