PIRSUE STERILE SOLUTION
Overview
Chemical Names
(2S-cis)-METHYL 7-CHLORO-6,7,8-TRIDEOXY-6-[[(4-ETHYL-2-PIPERIDINYL)CARBONY]AMINO]-1-THIO-l-threo-alpha-D-GALACTOOCTOPYRANOSIDE MONOHYDROCHLORIDE, HYDRATE
Synonyms
PIRSUE STERILE SOLUTION; PNU-57930E
Functional Class
Veterinary Drug
ANTIMICROBIAL_AGENT
ANTIMICROBIAL_AGENT
Evaluations
Evaluation year: 2004
ADI:0–8 µg/kg bw/d
ADI:
0–8 µg/kg bw/d
Comments:
The Committee noted that pirlimycin belongs to the class of lincosamide antibiotics that are known to be associated with perturbation of the gastrointestinal microflora following administration in humans. The ADI based on MIC data was considered to be extremely conservative considering the findings in a hamster model of pseudomembranous colitis and in humans. Therefore, the Committee established a microbiological ADI of 0–8 µg/kg bw/d on the basis of the NOEL for gastrointestinal effects in humans of 50 mg (0.83 mg/kg bw for a 60-kg adult) and a safety factor of 100, rounded to one significant figure.
MRL Comment:
MRLs (expressed as pirlimycin) in cattle: Muscle, fat, and milk: 0.1 mg/kg; liver: 1 mg/kg; kidney: 0.4 mg/kg
Intake:
0.305 mg/p/d TMDI (64% of ADI)
Meeting:
62
Report:
Tox Monograph:
Residues:
Toxicological study
Pivotal Study:
Clinical study (Brown et al., 1983; Gerard et al., 1982): Five males received single oral doses of pirlimycin hydrochloride at 50, 125, 250 and 500 mg in capsules. The doses were administered in escalating order, with 7 days between treatments. Five men were given placebo capsules containing starch. Soft stools were noted frequently in one treated man. Clostridium difficile was found in stool samples of 2-5 men/dose the week after treatment at all doses versus one control subject. The Committee considered the dose level of 50 mg (0.83 mg/kg bw for a 60-kg adult) to be without significant effect on gut flora in this study.
Animal Specie:
Human
Effect:
Clostridium difficile in stool
NOEL:
50 mg
Point of departure:
50 mg