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Thioridazine ( Mellaril or Melleril ) is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. The branded product was withdrawn worldwide in 2005 because it caused severe cardiac arrhythmias. However, generic versions are still available in the US.
2 Side effects
6 Antibiotic activity
8 External links
Thioridazine was voluntarily discontinued by its manufacturer, Novartis, worldwide because it caused severe cardiac arrhythmias.
Its primary use in medicine was the treatment of schizophrenia.
For further information see: Phenothiazine
Thioridazine prolongs the QTc interval in a dose-dependent manner.
Thioridazine has the following binding profile:
Binding affinity (K i [nM])
Binding affinity of Mesoridazine (K i [nM])
Binding affinity of Sulforidazine (K i [nM])
The ratio of 5-HT2A to D2 receptor binding is believed to dictate whether or not most antipsychotics are atypical or typical. In thioridazine’s case its ratio of 5-HT2A to D2 receptor binding is below the level that’s believed to be required for atypicality despite its relatively low extrapyramidal side effect liability in practice.
Believed to play a role in the weight gain-promoting effects of antipsychotics.
Likely the receptor responsible for the orthostatic hypotension known to occur in individuals on thioridazine.
This receptor is believed to be the chief receptor responsible for the anticholinergic side effects of thioridazine (e.g. dry mouth, constipation, blurred vision, etc.). Likely plays a role in thioridazine’s low extrapyramidal side effect liability as anticholinergic drugs such as benzatropine are routinely given to treat extrapyramidal side effects resulting from antipsychotic treatment.
Believed to be the receptor responsible for the therapeutic effects of antipsychotics.
Likely involved in thioridazine’s cardiac effects.
Likely responsible for the sedating effects of thioridazine.
Regulates the release of hydrochloric acid into the stomach.
Note: The Binding affinities given are towards cloned human receptors unless otherwise specified
HB — Human brain receptor
RC — Cloned rat receptor
ND — No data
Thioridazine is a racemic compound with two enantiomers, both of which are metabolized, according to Eap et al., by CYP2D6 into ( S )- and ( R )-thioridazine-2-sulfoxide, better known as mesoridazine,
The manufacturer Novartis /Sandoz/Wander of the brands of thioridazine, Mellaril in the USA and Canada and Melleril in Europe, discontinued the drug worldwide in June 2005.
This section needs expansion. You can help by adding to it. (November 2015)
Thioridazine is known to kill XDR-TB
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