Metabolism of Penicillins to Penicilloic Acids and 6-Aminopenicillanic Acid in Man and Its Significance in Assessing Penicillin Absorption
TLDR
It is important to take into account the penicilloic acid content of urine when estimating total absorption of a penicillin, as increased stability in the body as well as slower renal clearance can lead to high concentrations in the serum.Abstract:
Penicillins can be metabolized to penicilloic acids in man, the extent being dependent on the penicillin structure. In the phenoxy penicillin series, phenoxymethyl penicillin was found to be particularly unstable, but the higher homologues were more stable. In the isoxazolyl series, oxacillin was unstable, and progressive insertion of halogen in the phenyl ring increased stability. Ampicillin and amoxycillin showed some instability, ampicillin possibly being the more stable. After intramuscular administration, carbenicillin was very stable in the body, ampicillin was fairly stable, and benzyl penicillin was unstable. It is important to take into account the penicilloic acid content of urine when estimating total absorption of a penicillin. Increased stability in the body as well as slower renal clearance can lead to high concentrations in the serum. Penicilloic acids seemed to be more slowly cleared from the body than penicillins. The liver is probably the site of inactivation.read more
Citations
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Pharmaceuticals in the Environment—A Human Risk?
TL;DR: Human risk as a consequence of exposure via the environment has been addressed and assessed and results indicate a negligible human risk connected to the environmental exposure for these substances.
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Determination of penicillin G and its degradation products in a penicillin production wastewater treatment plant and the receiving river
TL;DR: An analytical method was developed for the simultaneous detection of PEN G and five degradation products using liquid chromatography-electrospray ionization mass spectrometry (LC-ESI/MS), which revealed the fate of penicillin G in the wastewater from a P EN G production facility and the receiving river.
Journal ArticleDOI
Enzyme Immunoassays for the Detection of Infectious Antigens in Body Fluids: Current Limitations and Future Prospects
TL;DR: Standard enzyme immunoassay techniques are not sufficiently sensitive for the measurement of some antigens from other viruses, bacteria, and parasites in concentrations that commonly occur in body fluids during the course of infectious diseases.
Journal ArticleDOI
Tobramycin: A Review of its Antibacterial and Pharmacokinetic Properties and Therapeutic Use
TL;DR: Tobramycin is a new aminoglycoside antibiotic with a broad antibacterial spectrum in vitro, and pharmacokinetic properties similar to those for gentamicin, and appears to offer no clear advantages over gentamicIn against sensitive organisms it is indicated in infection caused by strains of P. aeruginosa.
Book ChapterDOI
Microbial Penicillin Acylases
Erick Vandamme,J.P. Voets +1 more
TL;DR: The chapter examines methods to isolate and purify penicillin acylases and to stabilize these enzyme preparations, and describes the reaction of cysteine and related compounds with penicillins, resulting in a loss of antibacterial activity.
References
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Journal ArticleDOI
Amoxycillin: a new semi-synthetic penicillin.
TL;DR: The new penicillin was bactericidal in activity, as with other penicillins, and its antibacterial activity was not reduced in the presence of serum.
Journal ArticleDOI
Clinical Pharmacology of Carbenicillin Compared with Other Penicillins
TL;DR: The mechanisms responsible for the high levels of the drug in the blood are elucidated, comparisons with other penicillins are made, and dosage regimens that are appropriate for various therapeutic purposes are considered.
Journal ArticleDOI
Mechanisms Responsible for the Blood Level Differences of Isoxazolyl Penicillins: Oxacillin, Cloxacillin, and Dicloxacillin
TL;DR: With continuous intravenous infusions plasma levels of dicloxacillin sodium monohydrate were much higher, and the calculated plasma half-life was much longer, than for cloxacisin monohydrate sodium and oxacillin Sodium.