Olanzapine
Olanzapine is a drug used to treat certain forms of schizophrenia.
Olanzapine (presentation: Zyprexa® or in combination with fluoxetine as Symbyax®) was the second atypical antipsychotic to gain FDA approval U.S. and became one of the atypical antipsychotics commonly used. Olanzapine was approved by the F.D.A. Americans to treat schizophrenia, the delusions of manic bipolar disorder, agitation associated with schizophrenia and bipolar disorder (also known as bipolar disorder) as well as basic treatment of bipolar disorder. Olanzapine, under the trade name Zyprexa is manufactured and marketed by the pharmaceutical company Eli Lilly since 1996.
Pharmacology
Olanzapine is structurally similar to clozapine and is classified as thiénobenzodiazépine. Olanzapine has high affinity for dopamine receptors and serotonin. Like most atypical antipsychotics compared to typical old the same way, olanzapine has a lower affinity for histamine receptors, muscarinic acetylcholine (muscarinic cholinergic receptors) and also alpha-adrenergic receptors.
The principle of action of olanzapine is unknown, although it theorizes that the antipsychotic activity of olanzapine that is due primarily to an antagonism at the dopamine receptors, specifically D2. Antagonism of serotonin might also play a role in the effectiveness of olanzapine, but the significance of the 5-HT2A antagonism is debated by the international research community. Antagonism located at muscarinic receptors, histamine and alpha-adrenergic receptors appears to explain some of the side effects or drug reactions (side effects) of olanzapine, aspects such as anticholinergics, the tendency to overweight (diabetes iatrogenic?), Sedation and orthostatic hypotension.
Pharmacokinetics
Olanzapine exhibits linear kinetics. Its elimination has a half-life of 21 to 54 hours, averaging 37 hours and a half or a little more than a half day and full [two hours longer than thirty-six hours (36 h + 1 h 30 min in mean always)]. The plasma concentrations at rest are obtained after approximately one week. Olanzapine undergoes metabolism premier organic and availability is not affected by food intake.
Pharmacodynamics
In addition to the antagonistic action anti-dopamine or anti-serotonergic, anti-muscarinic and anti-histamine, perhaps, one effect is or appears to be the reduction of acetylcholine (this would be an anticholinergic).
Clinical trials
Dr. David Healy, Psychopharmacologist, internationally recognized expert, noted that the rate of suicide deaths and suicide attempts related to Zyprexa that occurred during clinical trials of pre-marketing was "the highest of all Psychotropic drugs in history".
Facts related companies
Counterfeit
In Belgium, May 25, 2007, a circular of the SCM (service control drugs) announced that the Federal Agency for Medicines and Health Products (depending on the FPS Health) and they themselves had been informed by the Eli Lilly Benelux identified in Britain three counterfeit batches of Zyprexa 10 mg tablets, French presentation, which had been shipped to Britain to parallel importers. The lot numbers of these counterfeit products were identical to the lots marketed in France by Lilly France.
Judicial controversies
Between 2005 and 2007, many trials of American users are brought to the firm Lilly on the grounds of insufficient information related to side effects, particularly about the effect on metabolism (obesity, diabetes) that are induced by the drug. In the U.S., the firm has been fined a record 1.4 billion dollars for encouraging the prescription of its product outside guidance set (particularly for the purpose of sedation).
Read also Bipolar Disorder
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