Quetiapine was developed in 1985 by scientists at AstraZeneca (formerly Zeneca)
Pharmaceuticals. It received official US Food and Drug Administration approval in September 1997 and approval in Germany in 2000. Since then,
quetiapine has been used in the treatment of severe
mental illness in approximately 70 countries including Canada, most Western European countries, and Japan.
Quetiapine is a dibenzothiazepine derivative with a relatively broad receptor binding profile. It has major affinity to cerebral serotonergic (5HT(2A)), histaminergic (H1), and dopaminergic D(1) and D(2) receptors, moderate affinity to alpha(1)- und alpha(2)-adrenergic receptors, and minor affinity to muscarinergic M1 receptors; it demonstrates a substantial selectivity for the limbic system. This receptor occupancy profile with relatively higher affinity for the 5HT(2A) receptor compared with the D(2) receptor is in part responsible for the
antipsychotic characteristics and low incidence of extrapyramidal side-effects of
quetiapine. The efficacy of
quetiapine in reducing positive and negative symptoms of
schizophrenia has been proven in several clinical trials with placebo-controlled comparators.
Quetiapine has also demonstrated robust efficacy for treatment of cognitive, anxious-depressive, and aggressive symptoms in
schizophrenia. Long-term trials show sustained tolerability for a broad spectrum of symptoms.
Quetiapine has also proven efficacy and tolerability in the treatment of moderate to severe
manic episodes, and in the treatment of juveniles with oppositional-defiant or
conduct disorders, and in the geriatric
dementia population. Recent data indicate that
quetiapine may also be effective in the treatment of bipolar depressive symptoms without increasing the risk of triggering
manic episodes, and in
borderline personality disorder. In comparison with other
antipsychotics,
quetiapine has a favorable side-effect profile. In clinical trials only small insignificant prolongations of the QT interval were observed.
Weight-gain liabilities and new-onset metabolic side-effects occupy a middle-ground among newer
antipsychotics. As a result of its good efficacy and tolerability profile
quetiapine has become well established in the treatment of
schizophrenia and
manic episodes.