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Forty patients were treated with either Lioresal suppositories 100 mg 6 hourly.
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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 rarely be habit forming. Lioresal should be avoided in patients with a history of opiate addiction or hypersensitivity to opiate medications.
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Lioresal has not been shown to cause histamine release. At therapeutic doses, Lioresal has no effect on heart rate, left-ventricular function or cardiac index.
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Lioresal may not work as well and may require higher doses to obtain the same effect as when originally taken. This is known as TOLERANCE.
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Lioresal can impair thinking and the physical abilities required for driving or operating machinery. Lioresal should be avoided in patients intoxicated with alcohol,
Talk with your doctor if Lioresal stops working well. Do not take more than prescribed.Some people who use Lioresal for a long time without a break may develop a physical need to continue taking it.
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Lioresal was not mutagenic in the following assays: Ames Salmonella microsomal activation test,
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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Lioresal may rarely be habit forming. Lioresal should be avoided in patients with a history of opiate addiction or hypersensitivity to opiate medications.
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