What is the central nervous system (CNS) penetration of Teicoplanin?

CNS Penetration of Teicoplanin

Teicoplanin has extremely poor CNS penetration when administered intravenously, with CSF levels consistently below 1 μg/mL even with inflamed meninges, making it unsuitable for systemic treatment of CNS infections. 1, 2, 3

Pharmacokinetic Profile for CNS Infections

Intravenous Administration

• Teicoplanin achieves negligible CSF concentrations (<1 μg/mL) after standard IV dosing, regardless of meningeal inflammation status 1, 2
• This poor penetration occurs despite therapeutic serum levels, as teicoplanin is 90% protein-bound and does not effectively cross the blood-brain barrier 3
• The drug's high protein binding and molecular characteristics prevent adequate CNS penetration even when the blood-brain barrier is disrupted by infection 3

Intraventricular Administration

• Direct intraventricular administration achieves therapeutic CSF levels of 12.5-38 μg/mL, which are sustained and bactericidal 1, 2
• Dosing regimens that have proven effective include:
  • Adults: 20 mg daily or 20 mg every other day intraventricularly 1
  • Infants: 5 mg daily intraventricularly 1, 2
• The alternate-day schedule (20 mg every 48 hours) is as effective as daily administration due to prolonged CSF half-life 1
• CSF sterilization occurs after an average of 4.4 days with intraventricular therapy 1

Clinical Implications for CNS Staphylococcal Infections

Treatment Approach

• For CNS shunt infections or ventriculitis caused by staphylococci, intraventricular teicoplanin combined with shunt removal is the appropriate strategy 1, 2
• Vancomycin remains the guideline-recommended first-line agent for MRSA CNS infections, with CSF penetration of 1-5% (uninflamed to inflamed meninges) and concentrations of 2-6 μg/mL 4
• Linezolid is superior for CNS infections with 66% CSF penetration and levels of 7-10 μg/mL, making it a preferred alternative when IV therapy alone is used 4, 5

Critical Pitfalls

• Never rely on IV teicoplanin alone for CNS infections—multiple case reports document treatment failures when IV administration was used without intraventricular supplementation 1, 2
• The combination of IV teicoplanin with rifampin (which achieves 22% CSF penetration) may improve outcomes but still requires consideration of alternative agents 4
• Surgical intervention (shunt removal, abscess drainage) must be performed whenever possible, as antimicrobial therapy alone has poor outcomes for device-related CNS infections 4, 6

Comparative Context with Other Antibiotics

Teicoplanin's CNS penetration is significantly worse than vancomycin (1-5% penetration), linezolid (66% penetration), and TMP-SMX (13-63% penetration) 4, 5. This positions teicoplanin as unsuitable for systemic treatment of CNS infections unless administered directly into the CSF compartment 1, 2, 3.