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Dose escalation safety and tolerance study of the N-methyl-Daspartate antagonist dextromethorphan in

Dose escalation safety and tolerance study of the N-methyl-Daspartate antagonist dextromethorphan in

  1. machineelf368
    Steinberg et al. 1996

     Experimental studies have shown that dextromethorphan, a noncompetitive N-methyl-D-aspartate antagonist is neuroprotective
    in experimental models of ischemic cerebral injury. The authors studied the safety and tolerability of oral dextromethorphan
    (DM) in humans, and correlated serum levels of this drug with cerebrospinal fluid (CSF) and brain levels.
    Neurosurgical patients undergoing intracranial surgery or endovascular procedures were given ascending doses of oral DM
    prior to and 24 hours after surgery. Serum, CSF, and brain levels of DM and its active metabolite, dextrorphan, were measured.
    One hundred eighty-one patients received a total of 212 courses of DM treatment in dose ranges of 0.8 to 9.64
    mg/kg. Serum DM levels correlated highly with CSF and brain DM levels. Brain levels were 68-fold higher than serum
    levels, whereas CSF levels were fourfold lower than serum levels. The maximum DM levels attained were 1514 ng/ml
    (serum), 118 ng/ml (CSF), and 92,700 ng/g (brain). The maximum dextrorphan levels were 501 ng/ml (serum), 167 ng/ml
    (CSF), and 6840 ng/g (brain). In 11 patients, brain and plasma levels of DM were comparable to levels that have been
    shown to be neuroprotective in animal studies. Frequent side effects occurring at neuroprotective levels of DM included
    nystagmus (64%), nausea and vomiting (27%), distorted vision (27%), feeling “drunk” (27%), ataxia (27%), and dizziness
    (27%). All symptoms were reversible and no patient suffered severe adverse reactions. This study demonstrates that potentially
    neuroprotective doses of DM can be administered safely to neurosurgical patients. Brain and CSF levels of DM can
    be estimated from serum levels of the drug. Side effects, even at the highest levels, proved to be tolerable and reversible.
    Administration of DM to patients at risk for cerebral injury should be further explored.