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Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

author:Critical Medicine

Author: Liu Yujuan

Source: Neurology Channel of the Medical Community

Bacterial meningitis is a severe, acute infectious disease caused by bacterial invasion of the meninges and is usually the most common central system infection.

When choosing antimicrobial therapy, it is important to grasp the penetration of the drug into the cerebrospinal fluid. The penetration of the drug is related to the lipid solubility, ionization degree, molecular weight and protein binding rate of the drug. The following is a summary of the permeability of different types of antimicrobial drugs to normal and inflammatory cerebrospinal fluid (CSF) and the key points of treatment.

01

Penicillins

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!
  • Most of the penicillins have poor permeability to normal cerebrospinal fluid, and the permeability of inflammatory cerebrospinal fluid is improved, and penicillin and ampicillin can be used to treat Neisseria meningitidis in the treatment.
  • Ampicillin can be used to treat Listeria monocytogenes and Haemophilus influenzae.
  • Oxacillin can be used to treat methicillin-susceptible staphylococci.

02

Cephalosporins/cephamycins

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

Like penicillin, cephalosporins are poorly permeable to the normal blood-brain barrier, and third- and fourth-generation cephalosporins can permeate inflammatory cerebrospinal fluid.

Ceftriaxone or cefotaxime are used to treat bacterial meningitis caused by Streptococcus pneumoniae, Haemophilus haemogenes, Klebsiella, and Escherichia coli.

The combination of ceftazidime and aminoglycosides can treat central infections caused by Pseudomonas aeruginosa.

03

Anti-MRSA antibiotics

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

Vancomycin has good permeability to inflammatory cerebrospinal fluid and can be combined with ceftriaxone to treat central infections caused by penicillin-resistant Streptococcus pneumoniae; In combination with fosfomycin for the treatment of central infections caused by methicillin-resistant staphylococci.

04

Carbapenems

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

Imipenem is not used for the treatment of central nervous system infections because it is prone to adverse reactions (convulsions) of the central nervous system.

Meropenem is permeable to inflammatory cerebrospinal fluid and can be used to treat multidrug-resistant gram-negative bacilli and severe central infections with a mixture of aerobic and anaerobic.

Carbapenems are time-dependent antibiotics, and an appropriate extension of the infusion time (e.g., meropenem to 3 hours) can improve efficacy.

05

Quinolones

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

Moxifloxacin can be used to treat central infection with penicillin-resistant Streptococcus pneumoniae; Ciprofloxacin plus aminoglycosides can be used to treat infections caused by Pseudomonas aeruginosa.

06

Macrolides and tetracyclines

Both macrolides and tetracyclines have poor permeability to normal and inflammatory cerebrospinal fluids.

07

Aminoglycosides

Amikacin and gentamicin, which are among the aminoglycosides, can penetrate inflammatory cerebrospinal fluid and can be used in combination with other drugs to treat central infections caused by Pseudomonas aeruginosa, or by intrathecal injection.

08

Sulfonamides

Sulfamethoxazole (SMZ)/trimethoprim (TMP), sulfamethoxazole, sulfamethoxazole, sulfamethoxazole, and sulfadiazine can penetrate the blood-brain barrier, and cerebrospinal fluid concentrations can reach 80%-90% of the blood concentration when the meninges are purulent and inflamed.

09 Miscellaneous

Metronidazole and tinidazole have good penetration of the normal meninges, and the cerebrospinal fluid concentration in inflammatory meninges is 90% of the plasma concentration. It can be used in combination with other drugs for the treatment of brain abscess.

Fosfomycin can penetrate the blood-brain barrier and can reach more than 50% of the blood concentration during inflammation.

10

Summary

Summary of antimicrobial drugs that can enter cerebrospinal fluid (dry goods)!

In general, the treatment of central nervous system infections begins with a smear of cerebrospinal fluid, culture, and blood culture before antimicrobial therapy, and a susceptibility test. Empirical treatment should be carried out as early as possible before the results of culture and drug susceptibility are available, and antiseptic drugs that can easily penetrate the blood-brain barrier should be used.

Bibliography:

1. Guidelines for the Use of Antimicrobial Drugs 2015

2. Clinical Therapeutics - Infectious Diseases

3. Pharmacopoeia of the People's Republic of China - Instructions for Clinical Use

4. Clinical Anti-Infective-Therapeutics

5. Expert Consensus on the Clinical Application of Antimicrobial Pharmacokinetics/Pharmacodynamics Theory (2018)

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