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Although Doxepin is known to exhibit a local anaesthetic effect, how Doxepin exerts this effect is not understood fully.
Doxepin is administered as a racemate and both [-] and [+] forms of both Doxepin and M1 are detected in the circulation.
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The binding of Doxepin to human plasma proteins is approximately 20%,
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Doxepin was evaluated in peri- and post-natal studies in rats.

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Doxepin 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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In general, both enantiomers of Doxepin 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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1 Dosing may be increased to 100 mg every four to six hours, but the daily dosage should not exceed 400 mg 1 and should be limited to 250 to 300 mg .
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Breast-feeding�Doxepin passes into breast milk and may cause unwanted effects in nursing babies.
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Doxepin was not mutagenic in the following assays:
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Intramuscular (i.m.) Doxepin increases gastric pH during anaesthesia similar to famotidine.
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which may affect the therapeutic response (see PRECAUTIONS - Drug Interactions).
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