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Cimetidine, but not oxmetidine, penetrates into the cerebrospinal fluid after a single intravenous dose.
Author(s) -
Jonsson KA,
Eriksson SE,
Kagevi I,
Norlander B,
Bodemar G,
Walan A
Publication year - 1982
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1982.tb02042.x
Subject(s) - cimetidine , cerebrospinal fluid , lumbar puncture , histamine , histamine h2 receptor , antagonist , medicine , chemistry , anesthesia , pharmacology , receptor
1 Thirty‐six patients with various neurological diseases or symptoms received single intravenous doses of either cimetidine 400 mg (n = 19) or oxmetidine 200 mg (n = 17), 15 or 60 min before a diagnostic lumbar puncture. 2 In the 15 min CSF samples concentrations of cimetidine were detectable but not measurable in 5 and non‐detectable in 3 patients. 3 In the 60 min CSF samples the concentrations of cimetidine were detectable in all 11 patients and were measurable in 8 of these patients with a mean +/‐ s.e. mean of 0.12 +/‐ 0.01 microgram/ml. These CSF concentrations were correlated to simultaneously measured plasma concentrations (P less than 0.01). The mean ratio CSF/plasma concentration was 0.03. 4 No detectable concentrations of oxmetidine were found either in the 15 min (n = 9) or in the 60 min (n = 8) liquor samples. 5 Cimetidine penetrates the blood‐drain barrier slowly and not freely after a single dose. Our data suggest that the new histamine H2‐ receptor antagonist oxmetidine does not cross this barrier.