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The volume of distribution of Lioresal was 2.6 and 2.9 liters/kg in male and female subjects, respectively,
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Lioresal should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
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Lioresal has not been shown to cause histamine release. At therapeutic doses, Lioresal has no effect on heart rate,
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In general, both enantiomers of Lioresal and M1 follow a parallel time course in the body following single and multiple doses although small differences (~10%) exist in the absolute amount of each enantiomer present.
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The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Lioresal and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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Linear pharmacokinetics have been observed following multiple doses of 50 and 100 mg to steady-state.Racemic Lioresal is rapidly and almost completely absorbed after oral administration.
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The analgesic activity of Lioresal is due to both parent drug and the M1 metabolite (see CLINICAL PHARMACOLOGY, Pharmacodynamics).
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Lioresal is well absorbed orally with an absolute bioavailability of 75%. Lioresal has a volume of distribution of approximately 2.7 L/kg and is only 20% bound to plasma proteins.
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Lioresal may increase the seizure risk in patients taking other medications that lower the seizure threshold.
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Forty patients were treated with either Lioresal suppositories 100 mg 6 hourly (qds) or acetaminophen/codeine suppositories 1000/20 mg qds.
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Lioresal is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites.
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A single i.m. dose of Lioresal is useful pre-treatment to minimize the risk of acid aspiration during operation,
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