Pharmacokinetics of Phenoxymethylpenicillin in Volunteers

Abstract

Pharmacokinetics of phenoxymethylpenicillin was studied in 12 healthy volunteers. They received four different single oral dose sizes. At all dose levels (0.4, 1, 2 and 3 g) phenoxymethylpenicillin was rapidly absorbed, usually with serum peaks within 0.75 h. The mean maximal serum peaks ( ± SD) were 6.1 ± 2.0, 15.0 ± 4.3, 26.3 ± 10.0 and 35.5 ± 10.8 mg/l after 0.4, 1, 2 and 3 g, respectively. The relationship between the mean peak serum concentrations and the doses was nonlinear (p < 0.001). The mean areas under the serum concentrations vs. time curve (AUC) increased almost linearly with increasing doses, and the deviation from linearity was not significant (p < 0.05). Very low penicillin concentrations were obtained in saliva. The urinary excretion during 10 h was 37–43% of the doses given. The pharmacokinetic results indicated that phenoxymethyl penicillin in the present formulation is rapidly and well absorbed up to as high doses as 3 g. The tablet formulations used were better absorbed than previous ones. The percent of absorption was relatively lower with the highest doses, but this probably has only minor therapeutic consequences.

Pharmacokinetics of phenoxymethyl penicillin (penicillin V) in calves

“…The coadministration of the drug with probenecid, which blocks the transport mechanism responsible for tubular secretion of penicillins (Mandell & Sande, 1980), was effective in elevating and prolonging serum antibiotic concentrations during the first 4 h after treatment only (Table 111). A similar temporary effect of probenecid on serum phenoxymethyl penicillin concentrations was noted in human volunteers (Josefsson & Bergan, 1982) and in the dog (Anderson et al, 1956).…”

Exploring the Pharmacokinetics of Phenoxymethylpenicillin (Penicillin-V) in Adults: A Healthy Volunteer Study

“…This study provides a base PK model for oral penicillin-V developed using rich PK data from 10 healthy volunteers. It adds to historical clinical trial data, which are now >20 years old [ 8 , 12 , 13 ]. In this study, we observed that penicillin-V was 77% plasma protein bound and had a free serum t1/2 of 55 minutes, in keeping with published product characteristics [ 12 ].…”

“…It adds to historical clinical trial data, which are now >20 years old [ 8 , 12 , 13 ]. In this study, we observed that penicillin-V was 77% plasma protein bound and had a free serum t1/2 of 55 minutes, in keeping with published product characteristics [ 12 ]. This is something that has rarely been demonstrated beyond pediatric populations and will support the planning of large population dosing studies in adults.…”

Use of Anthrax Vaccine in the United States: Recommendations of the Advisory Committee on Immunization Practices (ACIP)

“…Because oral amoxicillin has better pharmacokinetics than equivalent doses of oral penicillin V, oral amoxicillin may be used with a less frequent dosing interval, potentially improving adherence to therapy (218)(219)(220)(221)(222). Compared with oral penicillin, oral amoxicillin has greater pulmonary penetration and is able to maintain a higher concentration above MIC in the target tissues (e.g., pulmonary-associated lymph nodes, tissues, and secretions) for a greater portion of the dosing interval (223)(224)(225)(226)(227).…”