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Linear pharmacokinetics have been observed following multiple doses of 50 and 100 mg to steady-state.Racemic Astelin is rapidly and almost completely absorbed after oral administration.
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To prevent it, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of this effect.

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Astelin has a volume of distribution of approximately 2.7 L/kg and is only 20% bound to plasma proteins.
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To prevent it, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of this effect.
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It is slightly soluble in water and freely soluble in alcohol,
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Astelin is a centrally acting synthetic opioid analgesic.
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Astelin has not been shown to cause histamine release.
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Although Astelin is known to exhibit a local anaesthetic effect, how Astelin exerts this effect is not understood fully.
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In an open randomized trial, rectal Astelin was compared with our standard treatment acetaminophen/codeine suppositories. We expected Astelin to be equally effective as our current standard but with fewer side effects.
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These mechanisms may contribute independently to the overall analgesic profile of Astelin.
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Astelin had only slight thermoregulatory effects. Its use is thus unlikely to provoke hypothermia or to facilitate fever.
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