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Cerebrospinal fluid concentrations of aqueous procaine penicillin G in the neonate
Insights
Intramuscular aqueous procaine penicillin G achieved therapeutic penicillin levels in neonatal serum and cerebrospinal fluid (CSF). This antibiotic provides spirocheticidal activity in the CSF for at least 24 hours.
Area of Science:
- Pharmacology
- Neonatal Medicine
- Infectious Diseases
Background:
- Neonatal infections require effective antibiotic penetration into the central nervous system.
- Penicillin G is a crucial antibiotic for treating various bacterial infections.
Purpose of the Study:
- To evaluate the pharmacokinetic profile of aqueous procaine penicillin G in neonates.
- To determine if intramuscular administration achieves therapeutic cerebrospinal fluid (CSF) concentrations for treating infections like syphilis.
Main Methods:
- Simultaneous serum and CSF samples were collected from 25 neonates after intramuscular injection of aqueous procaine penicillin G (50,000 units/kg).
- Penicillin concentrations were measured in serum and CSF over a 24-hour period.
Main Results:
- Penicillin activity was detected in all serum and CSF samples.
- Peak serum levels (17.1 +/- 6.3 µg/ml) were observed at 4 hours; peak CSF levels (0.70 +/- 0.35 µg/ml) at 12 hours.
- CSF penicillin levels remained above the spirocheticidal threshold (≥0.03 µg/ml) for at least 24 hours.
Conclusions:
- Intramuscular aqueous procaine penicillin G achieves adequate and sustained CSF concentrations in neonates.
- This dosing regimen is effective in maintaining spirocheticidal levels in the CSF for at least 24 hours, supporting its use in treating neonatal infections.
Abstract:
Simultaneous serum and CSF samples were obtained following the intramuscular administration of 50,000 units/kg of aqueous procaine penicillin G in 25 neonates. Penicillin activity was detected in the sera and CSF of all patients. Peak serum levels were noted at four hours (mean +/- SEM, 17.1 +/- 6.3 micrograms/ml). Peak CSF levels were noted at 12 hours (0.70 +/- 0.35 microgram/ml). The serum level at 24 hours was 2.1 +/- 0.98 microgram/ml (range, 0.2 to 5.8 micrograms/ml); the CSF level at 24 hours was 0.12 +/- 0.05 micrograms/ml (range, 0.03 to 0.27 microgram/ml). These results demonstrate that spirocheticidal levels (greater than or equal to 0.03 microgram/ml) are achieved for at least 24 hours in the CSF following the intramuscular administration of aqueous procaine penicillin G in neonates.