Thioridazine

(RS) -10 - [2 - (1- methylpiperidin- 2-yl ) ethyl ]-2- methylsulfanylphenothiazin (IUPAC)

• C21H26N2S2 (thioridazine )
• C21H27N2S2Cl (hydrochloride)

• 50-52-2 (thioridazine )
• 130-61-0 (hydrochloride)

N05AC02

White to off- white powder

Antipsychotics

• 370.57 g · mol -1 (thioridazine )
• 407.05 g.mol -1 (hydrochloride)

• 72-74 ° C (thioridazine )
• 158-160 ° C ( hydrochloride)

230 ° C (thioridazine, 2.66 Pa)

• Insoluble in water
• Slightly soluble in dichloromethane and methanol
• Soluble in ethanol

Hydrochloride

Attention

• 995 mg · kg -1 ( LD50, Rat, oral, thioridazine )
• 385 mg · kg -1 ( LD50, Mouse, oral, thioridazine )
• 1060 mg · kg -1 ( LD50, Rat, oral, hydrochloride)
• 360 mg · kg -1 ( LD50, Mouse, oral, hydrochloride)

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Thioridazine is a drug from the group of neuroleptics ( antipsychotics ).

The chemical compound is one of the phenothiazines, and is used in the form of the racemate.

Thioridazine was patented in 1966 by Sandoz and was by this company under the trade name Melleril ®. At present it is still available as a generic. The drug is mainly used as better water-soluble hydrochloride or tartrate.

Because QTc prolongation (see QT syndrome) has taken the largest manufacturer Novartis Melleril ® in the U.S. and in Europe from the market.

In India, thioridazine has recently been successfully used in several small studies against extremely resistant strains of Mycobacterium tuberculosis (XDR - TB). Larger clinical trials are planned.

Pharmacological properties

Thioridazine shows a strong blockade of

• α1 -adrenoceptors

And in each case a moderate blockade of

• Dopamine D2
• Serotonin 5 -HT2A
• Histamine H1
• And muscarinic acetylcholine M1 receptor.

A similar spectrum of activity such as thioridazine has quetiapine.