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In an open randomized trial, rectal Linezolid was compared with our standard treatment acetaminophen/codeine suppositories. We expected Linezolid to be equally effective as our current standard but with fewer side effects.

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The analgesic activity of Linezolid is due to both parent drug and the M1 metabolite (see CLINICAL PHARMACOLOGY, Pharmacodynamics).

Linezolid has not been shown to cause histamine release. At therapeutic doses, Linezolid has no effect on heart rate, left-ventricular function or cardiac index.
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The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Linezolid and M1 occurs at two and three hours, respectively, after administration in healthy adults.
Linezolid was not mutagenic in the following assays: Ames Salmonella microsomal activation test,
Linezolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
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For Linezolid, the following should be considered:The suitability of Linezolid suppositories for inclusion in our hospital formulary for the treatment of mild to moderate post-operative pain was evaluated.
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