A recent meta-analysis of the efficacy and tolerance of 15 antipsychotic drugs APDs found that it had the highest propensity for causing weight gain out of the 15 APD compared with a SMD of 0. Several patient groups are at a heightened risk of side effects from olanzapine and antipsychotics in general. Olanzapine may produce non-trivial high blood sugar in people with diabetes mellitus. Likewise, the elderly are at a greater risk of falls and accidental injury. Young males appear to be at heightened risk of dystonic reactions, although these are relatively rare with olanzapine.
Most antipsychotics, including olanzapine, may disrupt the body's natural thermoregulatory systems, thus permitting excursions to dangerous levels when situations exposure to heat, strenuous exercise occur. Other side effects include galactorrhea , amenorrhea , gynecomastia , and erectile dysfunction impotence. Olanzapine is used therapeutically to treat serious mental illness.
Occasionally, it can have the opposite effect and provoke serious paradoxical reactions in a small subgroup of people, causing unusual changes in personality, thoughts, or behavior; hallucinations and excessive thoughts about suicide have also been linked to olanzapine use. The US Food and Drug Administration requires all atypical antipsychotics to include a warning about the risk of developing hyperglycemia and diabetes , both of which are factors in the metabolic syndrome.
These effects may be related to the drugs' ability to induce weight gain, although there are some reports of metabolic changes in the absence of weight gain. Of all the atypical antipsychotics, olanzapine is one of the most likely to induce weight gain based on various measures. There are some case reports of olanzapine-induced diabetic ketoacidosis. Despite weight gain, a large multi-center randomized National Institute of Mental Health study found that olanzapine was better at controlling symptoms because patients were more likely to remain on olanzapine than the other drugs. Olanzapine has demonstrated carcinogenic effects in multiple studies when exposed chronically to female mice and rats, but not male mice and rats.
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The tumors found were in either the liver or mammary glands of the animals. The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse. There is tentative evidence that discontinuation of antipsychotics can result in psychosis. Symptoms of an overdose include tachycardia , agitation , dysarthria , decreased consciousness, and coma.
Drugs or agents that increase the activity of the enzyme CYP1A2 , notably tobacco smoke, may significantly increase hepatic first-pass clearance of olanzapine; conversely, drugs which inhibit CYP1A2 activity examples: ciprofloxacin , fluvoxamine may reduce olanzapine clearance. Olanzapine has a higher affinity for 5-HT 2A serotonin receptors than D 2 dopamine receptors, which is a common property of most atypical antipsychotics, aside from the benzamide antipsychotics such as amisulpride along with the non-benzamides aripiprazole , brexpiprazole , blonanserin , cariprazine , melperone and perospirone.
Olanzapine had the highest affinity of any second-generation antipsychotic towards the P-glycoprotein in one in vitro study. The mediation of olanzapine in the central nervous system by P-GP means that any other substance or drug which interacts with P-GP increases the risk for toxic accumulations of both olanzapine and the other drug.
Olanzapine is a potent antagonist of the muscarinic M 3 receptor,  which may underlie its diabetogenic side effects. The mode of action of olanzapine's antipsychotic activity is unknown. It may involve antagonism of dopamine and serotonin receptors.
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Antagonism of dopamine receptors is associated with extrapyramidal effects such as tardive dyskinesia TD , and with therapeutic effects. Antagonism of muscarinic acetylcholine receptors is associated with anticholinergic side effects such as dry mouth and constipation, in addition it may suppress or reduce the emergence of extrapyramidal effects for the duration of treatment, however it offers no protection against the development of tardive dyskinesia.
In common with other second generation atypical antipsychotics, olanzapine poses a relatively low risk of extrapyramidal side effects including TD, due to its higher affinity for the 5HT 2A receptor over the D 2 receptor. Antagonizing H 1 histamine receptors causes sedation and may cause weight gain, although antagonistic actions at serotonin 5-HT 2C and dopamine D 2 receptors have also been associated with weight gain and appetite stimulation.
The drug became generic in Eli Lilly has faced many lawsuits from people who claimed they developed diabetes or other diseases after taking Zyprexa, as well as by various governmental entities, insurance companies, and others. Lilly produced a large number of documents as part of the discovery phase of this litigation, which started in ; the documents were ruled to be confidential by a judge and placed under seal , and later themselves became the subject of litigation.
A December New York Times article based on leaked company documents concluded that the company had engaged in a deliberate effort to downplay olanzapine's side effects. In September Judge Weinstein issued an order to make public Lilly's internal documents about the drug in a different suit brought by insurance companies, pension funds, and other payors. Olanzapine is generic and is available under many trade names worldwide. Olanzapine is marketed in a number of countries, with tablets ranging from 2.
Zyprexa and generic olanzapine is available as an orally-disintegrating "wafer" which rapidly dissolves in saliva.
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It is also available in 10 milligram vials for intramuscular injection. Olanzapine has been studied as an antiemetic , particularly for the control of chemotherapy-induced nausea and vomiting CINV. In general, olanzapine appears to be about as effective as aprepitant for the prevention of CINV, though there are some concerns for its use in this population. For example, concomitant use of metoclopramide or haloperidol increases the risk for extrapyramidal symptoms EPS. Otherwise, olanzapine appears to be fairly well tolerated for this indication, with somnolence being the most common side effect.
Olanzapine has been considered as part of an early psychosis approach for schizophrenia. Olanzapine was effective for treating the prodromal symptoms, but was associated with significant weight gain. From Wikipedia, the free encyclopedia. IUPAC name. Interactive image. See also: List of adverse effects of olanzapine. Drug Metabolism and Disposition. September Clin Pharmacokinetics.
Clinical Pharmacokinetics. TGA eBusiness Services. Sandoz Pty Ltd. Retrieved 26 November Medscape Reference. Retrieved 24 December The Maudsley Prescribing Guidelines in Psychiatry 12th ed. London, U K: Wiley-Blackwell. Centers for Medicare and Medicaid Services. Retrieved 22 December Retrieved 25 November Donald A. Address: Donald A. Malone, Jr. ABSTRACT Although antidepressant drugs do not differ much in their efficacy rates, the particular characteristics of one drug may make it a better choice in a given patient.
This article provides insight into the art of prescribing antidepressants in primary care, with recommendations for prescribing for patients with chronic pain, sexual dysfunction, anxiety, chronic fatigue syndrome, fibromyalgia, severe insomnia, old age, diabetes, and heart problems. With the variety of drugs available for treating depression, choosing one can be daunting. Different agents have characteristics that may make them a better choice for different types of patients, but even so, treating any kind of mental illness often requires an element of trial and error.
Primary care providers are on the frontline of treating mental illness, often evaluating patients before they are seen by a psychiatrist. The purpose of this article is to provide insight into the art of prescribing antidepressants in the primary care setting. We will discuss common patient presentations, including depressed patients without other medical comorbidities as well as those with common comorbidities, with our recommendations for first-line treatment. We hope our recommendations will help you to navigate the uncertainty more confidently, resulting in more efficient and tailored treatment for your patients.
For example, elevation of liver enzymes may preclude the use of duloxetine. Tests should include:. Electrocardiography may also be useful, as some antidepressants can prolong the QT interval or elevate the blood levels of other drugs with this effect. There are several classes of antidepressants, and each class has a number of agents.
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