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Updated: Sep 13, 2026

Biosensor for Detection of Antibiotic Resistant Staphylococcus Bacteria
Published on: May 8, 2013
Pharmacology of methicillin
Abstract:
The pharmacology of a new antibiotic methicillin, 6(2:6-dimethoxybenzamido)-penicillanic acid, which is effective against staphylococci resistant to penicillin G, has been investigated. It is free from acute and chronic toxic effects, except that some pain may be caused following intramuscular injection. It is poorly absorbed orally, but after intramuscular injection the concentrations in the serum and in tissues are very similar to those found with penicillin G. It is excreted by the kidneys both by renal tubular secretion and glomerular filtration. It is also excreted in the bile in very high concentrations, the ratio of concentration in the bile to the blood being approximately 2.5 times that of penicillin G. From a study of the metabolism of the drug it is calculated that 75% is eliminated unchanged in the urine and that the remainder is probably destroyed after the excretion into the intestine via the bile.
Insights
Methicillin, a new antibiotic effective against penicillin-resistant staphylococci, shows favorable pharmacology. It has minimal toxicity and similar serum/tissue concentrations to penicillin G after intramuscular injection.
Area of Science:
- Pharmacology
- Microbiology
- Drug Metabolism
Background:
- Penicillin G resistance in Staphylococcus is a growing clinical concern.
- Development of novel antibiotics is crucial for combating resistant bacterial strains.
Purpose of the Study:
- To investigate the pharmacology of methicillin, a new antibiotic.
- To assess methicillin's efficacy against penicillin-resistant staphylococci.
Main Methods:
- Pharmacological investigation of methicillin.
- Assessment of toxicity, absorption, distribution, and excretion.
- Metabolism studies.
Main Results:
- Methicillin is effective against penicillin G-resistant staphylococci.
- It exhibits minimal acute and chronic toxicity, with minor injection site pain.
- Oral absorption is poor, but intramuscular injection yields serum and tissue concentrations comparable to penicillin G.
- Renal excretion occurs via tubular secretion and glomerular filtration.
- Biliary excretion is high, with a bile-to-blood concentration ratio 2.5 times that of penicillin G.
- Approximately 75% of methicillin is eliminated unchanged in urine; the remainder is likely degraded after biliary excretion.
Conclusions:
- Methicillin demonstrates a promising pharmacological profile for treating infections caused by penicillin-resistant staphylococci.
- Its excretion pathways and metabolic fate are characterized, supporting its clinical utility.
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