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Clozaril or clozapine, one of first new drugs designed for treating schizophrenia in over 20 years, was introduced in 1975 (1989 in United States) by Novartis Pharmaceuticals Corporation and is mostly used in Europe. Symptoms such as hallucinations, delusions, blunted affect, and hostility are successfully addressed with this synthesized antipsychotic pharmaceutical, which is also marketed as leponex.

View a second image of crystallized clozaril.

A yellow, crystalline powder that is very slightly soluble in water, clozapine binds to dopamine receptors in the limbic system of the brain of the patient while avoiding extrapyramidal side effects. Dopamine plays a role in a loss of touch with reality, attention deficit disorder (ADD), drug addictions, and moods. Clozaril also is an antagonist to the adrenergic (weight gain, moodiness, arousal, startle response), cholinergic (memory), histaminergic (sleep and weight gain), and serotonergic (depression, anxiety, panic, aggression) receptors of the central nervous system. Thus, the largely genetic illnesses of schizophrenia and bipolar disorder are treated via medication by changing the brain's biochemistry. Upon elimination via urine and feces, only trace amounts of the unchanged drug are detectable, with the clozapine being almost completely metabolized. An aminoacridine derivative, clozaril impedes dominant alpha waves and promotes delta and theta activity in the brain.

Clinical trials with Alzheimer's patients show some promise, but there are serious side effects associated with this medication including seizures, blood pressure loss, agranulocytosis (reduced white blood cell count), and accelerated heart rate. Because of the sometimes life-threatening associated risks, including heart inflammation (myocarditis), this antipsychotic is usually only prescribed to severely ill schizophrenics who fail to respond to standard drug therapies. An interesting effect of taking clozaril is that rapid eye movement sleep occurs almost immediately after falling asleep and may occupy almost 85 percent of the total sleep time. Reportedly, clozapine is not addictive nor does the drug create a "high" for the patient. As with any prescription drugs, potential patients and their guardians must consult with their physicians and pharmacists before beginning clozaril therapy and weigh the potential risks against the probable benefits.

Contributing Authors

Omar Alvarado, Thomas J. Fellers and Michael W. Davidson - National High Magnetic Field Laboratory, 1800 East Paul Dirac Dr., The Florida State University, Tallahassee, Florida, 32310.



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