Tiotixene, or thiothixene, sold under the brand name Navane among others, is a

typical antipsychotic Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics ma ...

of the

thioxanthene Thioxanthene is a chemical compound in which the oxygen atom in xanthene is replaced with a sulfur atom. It is also related to phenothiazine. Several of its derivatives are used as typical antipsychotics in the treatment of schizophrenia and othe ...

class which is related to chlorprothixene and is used in the treatment of psychoses like

schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...

and bipolar mania. It was introduced in the

United States The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territori ...

in 1967 by

Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer ...

. Tiotixene is also related to thioproperazine and pipotiazine, members of the

phenothiazine Phenothiazine, abbreviated PTZ, is an organic compound that has the formula S(C6H4)2NH and is related to the thiazine-class of heterocyclic compounds. Derivatives of phenothiazine are highly bioactive and have widespread use and rich history. T ...

class.

Pharmacology

Pharmacodynamics

Tiotixene acts primarily as a highly potent antagonist of the dopamine D₂ and D₃ receptors (subnanomolar affinity). It is also an antagonist of the

histamine Histamine is an organic nitrogenous compound involved in local immune responses, as well as regulating physiological functions in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Since histamine was discovered ...

H₁, α₁-adrenergic, and serotonin 5-HT₇ receptors (low nanomolar affinity), as well as of various other receptors to a much lesser extent (lower affinity). It does not have any

anticholinergic Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system. These agents inhibit the parasympathetic nervous sys ...

activity. Antagonism of the D₂ receptor is thought to be responsible for the antipsychotic effects of tiotixene.

History

Tiotixene was introduced in 1967.

Chemistry

Tiotixene is a member of the

class of antipsychotics. Analogues include chlorprothixene,

clopenthixol Clopenthixol (Sordinol), also known as clopentixol, is a typical antipsychotic drug of the thioxanthene class. It was introduced by Lundbeck in 1961. Clopenthixol is a mixture of '' cis'' and ''trans'' isomers. Zuclopenthixol, the pure ''cis' ...

flupentixol Flupentixol (INN), also known as flupenthixol (former BAN), marketed under brand names such as Depixol and Fluanxol is a typical antipsychotic drug of the thioxanthene class. It was introduced in 1965 by Lundbeck. In addition to single drug pre ...

, and

zuclopenthixol Zuclopenthixol (brand names Cisordinol, Clopixol and others), also known as zuclopentixol, is a medication used to treat schizophrenia and other psychoses. It is classed, pharmacologically, as a typical antipsychotic. Chemically it is a thioxanth ...

References

{{Tricyclics 5-HT7 antagonists Alpha-1 blockers Antihistamines D2 antagonists D3 antagonists H1 receptor antagonists Piperazines Sulfonamides Dimethylamino compounds Thioxanthene antipsychotics