Biomaterial Database

Pharmacokinetics and tissue penetration of orally administered pefloxacin. 1987

J M Webberley, and J M Andrews, and J P Ashby, and A McLeod, and R Wise

Department of Medical Microbiology, Dudley Road Hospital, Birmingham, UK.

The pharmacokinetics of the quinolone pefloxacin were determined following a 400 mg oral dose given to each of six male volunteers. Concentrations were determined in serum and urine by high-performance liquid chromatography, and in cantharidin-induced inflammatory fluid by a microbiological assay. The mean peak serum level of 6.6 micrograms/ml was attained rapidly 0.8 h after administration. The mean serum elimination half-life was 11.6 h. Inflammatory fluid was penetrated quickly with a mean peak level of 3.9 micrograms/ml occurring at 2.4 h. Pefloxacin was excreted in the urine as the parent compound and its two metabolites, norfloxacin and pefloxacin N-oxide (24 h urinary recovery being 8.0%, 12.0% and 13.1% respectively of the dose). This study suggests that a twice or possibly once daily dosage may be sufficient to treat systemic infections caused by susceptible pathogens. Once daily dosing should be sufficient for urinary tract infections.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009643	Norfloxacin	A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.	AM-0715,AM-715,MK-0366,MK-366,MK0366,MK366,Noroxin,AM 0715,AM 715,AM0715,MK 0366,MK 366
D001768	Blister	Visible accumulations of fluid within or beneath the epidermis.	Bulla,Vesication,Bleb,Bullae,Bullous Lesion,Blebs,Blisters,Bullous Lesions,Lesion, Bullous,Lesions, Bullous,Vesications
D006207	Half-Life	The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity.	Halflife,Half Life,Half-Lifes,Halflifes
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284	Administration, Oral	The giving of drugs, chemicals, or other substances by mouth.	Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000328	Adult	A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available.	Adults
D000890	Anti-Infective Agents	Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.	Anti-Infective Agent,Anti-Microbial Agent,Antimicrobial Agent,Microbicide,Microbicides,Anti-Microbial Agents,Antiinfective Agents,Antimicrobial Agents,Agent, Anti-Infective,Agent, Anti-Microbial,Agent, Antimicrobial,Agents, Anti-Infective,Agents, Anti-Microbial,Agents, Antiinfective,Agents, Antimicrobial,Anti Infective Agent,Anti Infective Agents,Anti Microbial Agent,Anti Microbial Agents
D014018	Tissue Distribution	Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.	Distribution, Tissue,Distributions, Tissue,Tissue Distributions
D015366	Pefloxacin	A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.	2589 R.B.,Abactal,Peflacine,Pefloxacin Mesylate,Pefloxacin Mesylate Dihydrate,Pefloxacine,Silver Pefloxacin,Dihydrate, Pefloxacin Mesylate,Mesylate Dihydrate, Pefloxacin,Mesylate, Pefloxacin,Pefloxacin, Silver,R.B., 2589