Zyprexa prescribing information |
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Zyprexa
Zyprexa (Generic name: olanzapine) is a prescription drug that has been approved by the FDA in October 1996 for the treatment of schizophrenia and manic-depressive illness (also called bipolar disorder, a condition in which the patients swing between states of mania and depression). Olanzapine is an atypical antipsychotic drug. Atypical antipsychotics have the advantage of not causing neurological movement disorders like typical antipsychotics do (Culpepper et al., 2007).
There are many drugs which belong to the class of atypical antipsychotics like amisulpride, clozapine, aripiprazole, quetiapine, risperidone, ziprasidone and olanzapine. It was observed in a study that the olanzapine is more effective in improving mental state as compared to aripiprazole, quetiapine, risperidone, ziprasidone and olanzapine but less effective than amisulpride, clozapine (Komossa et al., 2010).
Indications
The use of Zyprexa against different diseases is highly related to its dosage form. Zyprexa is available in the form of oral dosage form like tablet and parental dosage form like injection (intramuscular). Oral Zyprexa is used for the treatment of both schizophrenia and bipolar I disorder (mood disorder involving at least one or more manic episodes along with episodes of hypomania and major depression). Intramuscular injections of Zyprexa are used for the treatment of unease due to schizophrenia. Orally the combination of Zyprexa and fluoxetine (an antidepressant) can be used for the treatment of depressive episodes associated with bipolar I disorder.
Warnings and precautions
When Zyprexa is given to treat psychosis in elderly patients who also suffer from dementia, then there is a risk of death. Thus, Zyprexa is not approved for the treatment of psychosis in elderly patients with dementia. There is increased risk of hyperglycemia due to Zyprexa so patients taking Zyprexa should always be monitored for symptoms of hyperglycemia. There is also a risk for hyperlipidemia and weight gain in patients using Zyprexa; so patients should monitor their weight regularly during the use of Zyprexa.
Schizophrenia and bipolar disorder
Schizophrenia is a type of mental disorder that is caused by some inherent dysfunction of the brain. It is characterized by negative or positive symptoms. Positive symptoms include delusions, hallucinations and speech disturbance; while negative symptoms include flattening of emotional responses and social withdrawal. This illness usually affects people during adolescence and is a chronic and disabling disorder. Schizophrenia has a strong genetic component and possibly reflects some fundamental biochemistry abnormality, possibly an over-activity of the mesolimbic dopaminergic neurons (one of the dopaminergic pathways in the brain) (Richard et al., 2006).
The etiology of schizophrenia is a complex matter. There are mainly three types of neurotransmitters which are associated with this disease. These are dopamine, glutamate and 5-HT (5-hydroxytryptamine). Let us see the role of each neurotransmitter one by one. It was shown that an increase in dopamine activity may cause symptoms of schizophrenia. Strong evidence for this was provided by an imaging study (Laruelle et al., 1999). Similarly, an increase in 5-HT activity also produces symptoms of schizophrenia (Busatto and Kerwin, 1997). A decrease in glutamate activity produces symptoms of schizophrenia (Goff and Coyle., 2001). Thus, if we want to treat schizophrenia, we need to either decrease the levels of dopamine and 5-HT or increase the levels of glutamate.
Now let us discuss a little about bipolar disorder. Bipolar disorder is a psychological disorder also called bipolar affective disorder. Patients suffering from this disorder swing between states of depression and mania (Rang et al., 2007). There are two types of bipolar disorder: I and II. In the case of bipolar I disorder, there are episodes of hypomania and major depression with at least one or more manic episodes. In the case of bipolar II disorder, there is no manic episode but only episodes of hypomania and major depression. The signs and symptoms of depression include a persistent feeling of sadness, isolation and anxiety. In severe cases delusions and hallucinations may also occur while the symptoms of mania include euphoria, low attention span and insomnia. There are several factors contributing to the development of bipolar disorder: genetic, physiological and environmental.
Mechanism of action
Olanzapine antagonizes dopamine, serotonin, muscarinic and alpha-adrenergic receptors (Bymaster FP et al., 1996). The exact mechanism of action to which olanzapine owes its antipsychotic effects is still unknown but it is considered that it involves the inhibition of 5-HT2 serotonin receptors and D receptors.
Dosage and administration
Zyprexa is available in different dosage forms like tablet and injection (intramuscular). In the tablet dosage forms it is available in the strengths of 2.5mg, 5mg, 7.5mg, 10mg, 15mg, 20mg while in the form of intramuscular injection it is available only in the strength of 10mg vial.
To treat schizophrenia in adults Zyprexa is given orally in the dose of 5 mg to 10mg once daily but for the treatment of schizophrenia in adolescents its dose is 2.5 mg to 5mg once daily.
In the case of bipolar I disorder in adults the dose of 10mg or 15mg of Zyprexa is given once daily while if the same disorder is present in adolescents then a dose of 2.5 mg to 5mg is given once daily.
For the treatment of resistant depression in adults Zyprexa is used in combination with fluoxetine. In this combination the doses of olanzapine and fluoxetine are 5mg and 20mg respectively, given once daily. The same combination can also be used to treat the symptoms of bipolar I disorder.
Interactions with drugs, food and alcohol
Co-administration of diazepam and Zyprexa can cause orthostatic hypotension (a fall of blood pressure that takes place when one stands up from sitting or lying down); and so does co-administration of alcohol and Zyprexa. Thus, Zyprexa should not be co-administered with diazepam or alcohol.
In a study it was shown that olanzapine reduces alcohol craving. (Hutchison, et al., 2003).
Zyprexa is associated with an increase in glucose levels so that patients taking Zyprexa should have their glucose level regularly monitored (Hedenmalm et al., 2002).
References
Busatto GF, Kerwin R., 1997. Perspectives on the role of serotonergic mechanisms in the pharmacology of schizophrenia. J Psychopharmacol 11:3-12
Bymaster FP, Hemrick-Luecke SK, Perry KW, Fuller RW.,1996. Neurochemical evidence for antagonism by olanzapine of dopamine, serotonin, alpha 1-adrenergic and muscarinic receptors in vivo in rats.Psychopharmacology (Berl).;124(1-2):87-94.
Culpepper., 2007. A Roadmap to Key Pharmacologic Principles in Using Antipsychotics, Prim Care Companion J Clin Psychiatry. ; 9(6): 444–454.
Goff DC, Coyle JT., 2001. The emerging role of glutamate in the pathophysiology and treatment of schizophrenia. Am J Psychiatry 158:1367-1377
Hedenmalm K, Hägg S, Stahl M, Mortimer Ö, Spigset O., 2002.Glucose intolerance with atypical antipsychotics. Drug Safety; 25: 1107–1116
Hutchison KE, Wooden A, Swift RM, Smolen A, McGeary J, Adler L, Paris L., 2003. Olanzapine reduces craving for alcohol: a DRD4 VNTR
polymorphism by pharmacotherapy interaction. Neuropsychopharmacology., t;28(10):1882-8.
Komossa K, Rummel-Kluge C, Hunger H, Schmid F, Schwarz S, Duggan L, Kissling W, Leucht S., 2010. Olanzapine versus other atypical antipsychotics for schizophrenia, Cochrane Database Syst Rev.; 17;(3):CD006654.
Laruelle M, Abi-Dargham A, Gill R., 1999.Increased dopamine transmission in schizophrenia: relationship to illness phase.Biol Psychiatry 46:56-72
Off- label indications of Zyprexa.2011. Food and Drug Administration
Olanzapine prescribing information., 2011.Eli Lilly and Company.
Rang H. P., Dale M. M., Ritter J. M., Flower R. J., 2007, Rang & Dale's Pharmacology (Sixth Edition), Churchill Livingstone.
Howland RD, Mycek MJ, 2006. Lippincott’s Illustrated Reviews of Pharmacology (3rd Edition), Lippincott’s Williams & Wilkins
Zyprexia Description
Certain chemicals in the brain known as neurotransmitters are determinants of an individual’s mood. The main neurotransmitters thought to be responsible for moods are Dopamine and Serotonin. Neurotransmitters are responsible for transmitting messages between nerves and deregulation in the composition or activity of the neurotransmitters, especially dopamine, is thought to be the reason behind psychotic abnormalities. Such deregulations could be for example over-activity of dopamine in the brain which could lead to hallucinations and delusions that are associated with Schizophrenia.
How to Take
Zyprexia can be taken for the treatment of bipolar disorders associated with manic episodes such as schizophrenia as well as for prevention of nausea and vomiting which occurs during drug treatments in cancer patients. It is available as a 2.5mg, 5mg, 7.5mg and 10mg tablets as well as a soluble form which can be dissolved in water. The dosage depends on the individual case and is to be decided by a doctor who may recommend a lower starting dose which can be gradually increased in order to minimize the chances of undesired side effects. Zyprexia is usually recommended to be taken once daily regardless of meal times and can either be taken with water or allowed to dissolve in mouth saliva. It can also be administered with an injection depending on the patient’s requirement.
Contraindication
This drug is not to be used in patient with dementia as this could result in pneumonia, heart failure or sudden death if used in such patients.
Possible Side Effects
Common side effects associated with Zyprexa include abnormal menstrual cycle as a result of increased levels of proclan, abdominal pain, impaired vision, coughs, high blood pressure, constipation, hostile behavior, an increase in appetite, nervousness, disturbed sleep, tremor, weight gain,Increase in breast size, sexual malfunctions, fever, headache, tension, pain in the arms and legs, constipation, decreased blood pressure (Hypotension) and increased heartbeat and dizziness.Less common side effects are decreased libido, unusual dreams, pain in the dental area, diabetes and sore throat. Much rarer side effects arehair loss, decreased heart rate, abnormal heart rhythm, abnormal photosensitivity and decreased white blood cell counts manifesting as the following symptoms: fever, sore throat, mouth ulcers and other signs of infections. Contact your doctor if you notice any of these or other side effects or if any side effect worsens.
Drug interaction
Alcohol should not be consumed while using this drug as this could increase the drowsiness effect. Barbiturates, benzodiazepines, sedating antihistamines, tricyclic antidepressants, strong opioid painkillers and sleeping pills can also have this increased drowsiness effect when taken with Zyprexa. This drug may also enhance the effectiveness of other drugs however the doctor should be aware of any other drugs you are taking in order to adjust the doses appropriately.
Pregnant and Breastfeeding
The effect of Zyprexia on pregnancy is yet to be fully established. It should therefore not be used for pregnant women except where it is deemed necessary. Furthermore this drug could reach the breast milk posing harm to the child.
Storage
Zyprexa should be stored away from light at room temperature.
Zyprexa notes:
Zyprexa (zyprexia) generic equivalent Olanzapine is an antipsychotic drug use to treat the symptoms of schizophrenia and bipolar disorder (manic depression) in adults and children who are at least 10 years old. Zyprexa is sometimes used together with another medication called fluoxetine (Prozac, Sarafem). Zyprexa is not for use in psychotic conditions related to dementia. Olanzapine may cause heart failure, sudden death or pneumonia in older adults with dementia-related conditions.
Zyprexa side effects includes fever, stiff muscles, sweating, fast or uneven heartbeats, jerky muscle movements, sudden numbness(especially on one side of the body), sudden headache, confusion, problems with vision, speech, increased thirst, frequent urination, excessive hunger, feeling light-headed, fainting, unusual thoughts(or behavior), hallucinations, thoughts about hurting yourself, nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice, constipation, swelling in your hands/feet, back pain, weight gain, increased appetite, upset stomach, hives, swelling face/lips/tongue/throat.
Some of the drugs like carbamazepine (Tegretol), fluvoxamine (Luvox), medication to treat Parkinson's disease including levodopa (Sinemet, Larodopa, Atamet), selegiline (Eldepryl, Emsam), pramipexole (Mirapex), ropinirole (Requip) or medication to treat high blood pressure/heart condition can alter the olanzapine effects.
Ziprexa is the mexican name of the same drug. The recommended starting Zyprexa dose is 5 mg to 10 mg once daily. It can be taken with or without food. To take olanzapine orally disintegrating, place it in mouth. It will begin to dissolve right away. It may take up to 4 weeks of using this medicine before symptoms improve.
If a dose is missed, it is advised to consume it as soon as it is remembered. If it is near the time of the next dose, the missed one should be skip and the usual dosing schedule should be resume and strictly not to double the dose to catch up. Seek emergency medical attention if you think you have used too much of this medicine.
Avoid drinking alcohol, which can increase some of the side effects of Zyprexa. It is not known whether Zyprexa is harmful to an unborn baby. Before taking this medication, tell doctor if you are pregnant or plan to become pregnant during treatment. Olanzapine can pass into breast milk and may harm a nursing baby.
The tablet may contain phenylalanine.Talk to doctor before using this form of olanzapine if you have phenylketonuria (PKU). Store Zyprexa at room temperature away from moisture and heat.
Zyprexa story:
Zyprexa is an atypical antipsychotic that belongs to the thienobenzodiazepine class approved by the FDA for the treatment of schizophrenia and bipolar disorder It is intended for oral administration only. Zyprexa is structurally similar to clozapine but is classified as a thienobenzodiazepine. It has a higher affinity for 5-HT2 serotonin receptors than D2 dopamine receptors. Like most of the atypical antipsychotics zyprexa has lower affinity for histamine, cholinergic muscarinic and alpha adrenergic receptors. It also has weak affinity for benzodiazepine receptors which might be contributing to its sedating properties. The mode of action for zyprexa's antipsychotic activity is unknown, it may involve antagonism at serotonin receptors.
Zyprexa can increase the risk of developing hyperglycemia and diabetes both of which are factors in the metabolic syndrome. Of all the atypical antipsychotics, zyprexa is one of the most likely to induce weight gain based on various measures. There are some case reports available of zyprexa-induced diabetic ketoacidosis.
A clinical trial was conducted for the treatment of acquired neurogenic stuttering using zyprexa. Generally stuttering is most commonly treated with speech therapy and psychotherapy but number of antipsychotic agents have been investigated as possible treatments. In the case the medication was given to a 37 year old man who developed a post-concussive syndrome with psychosis and associated stuttering after his second exposure to a blast from an improvised explosive device. After treatment with zyprexa, his psychosis and stuttering showed significant improvement.
Zyprexa is quite effective at treating the multiple domains of schizophrenia with a low risk of extra-pyramidal side-effects. However its use gets restricted due to its metabolic side effects particularly obesity. Zyprexa have a high affinity for the H1 receptor and meta-analyses shows a strong correlation between risk of weight gain and H1 receptor affinity. In addition, zyprexa treatment decreases H1 receptor binding and mRNA expression in the rat hypothalamus. Also a complex role is emerging for the histamine H3 receptor in the control of hunger which is a pre-synaptic autoreceptor that inhibits the synthesis and release of histamine and a heteroreceptor that inhibits other neurotransmitters such as serotonin (5-HT), noradrenaline (NA) and acetylcholine (ACh), which are also implicated in the regulation of food intake. This indicates that the H3 receptor is in a prime position to regulate food intake, both through its control of histamine and its influence on other feeding pathways. A report proposed that mechanism for atypical antipsychotic-induced weight gain may be partly through the H3 receptor as a drug-induced decrease in H1 receptor activity may decrease histamine tone through the H3 autoreceptors, compounding the weight gain problem.
In a clinical trial undertaken for treating the symptoms of schizophrenia, zyprexa shows much superior results as compared to placebo. The patients were assessed using several test instruments including the Brief Psychiatric Rating Scale (BPRS), an 18-item inventory of symptoms traditionally used to evaluate the effects of drug treatment in psychosis. The BPRS score was extracted from the Positive and Negative Syndrome scale (PANSS) which is a 30-item rating instrument that evaluates each symptom item on a scale of 1 (absent) to 7 (extreme). The psychotic symptoms that were assessed includes conceptual disorganization, hallucinatory behavior, suspiciousness and unusual thought content. A second assessment Clinical Global Impression (CGI) was done to measure the overall severity of the illness. In addition, patients were evaluated on the PANSS and the Scale for Assessing Negative Symptoms (SANS). In a six-week, placebo-controlled trial involving 149 patients who received either placebo or a fixed dose of zyprexa at 1 and 10 mg/day. In this trial, zyprexa at 10 mg/day was superior to placebo on the PANSS total score, on BPRS total, the PANSS negative symptom sub-scale and on CGI severity.
In a six-week, placebo-controlled trial involving 253 patients who received placebo or one of three fixed dose ranges of Zyprexa (5 +/- 2.5 mg/day, 10 +/- 2.5 mg/day, 15 +/- 2.5 mg/day). The two highest zyprexa doses were superior to placebo on the BPRS total score and CGI severity score. The highest Zyprexa dose was statistically superior to placebo on the SANS.
References:
Definition of Olanzapine - National Cancer Institute
Moyer, Paula . "CAFE Study Shows Varying Benefits Among Atypical Antipsychotics". Medscape Medical News (WebMD). Retrieved 2007-12-03.
de Haan L, van Amelsvoort T, Rosien K, Linszen D (2004). "Weight loss after switching from conventional olanzapine tablets to orally disintegrating olanzapine tablets". Psychopharmacology (Berl) 175 (3): 389–90. doi:10.1007/s00213-004-1951-2. PMID 15322727
Zyprexa news
The U.S. Food and Drug Administration (FDA) Psychopharmacologic Drugs Advisory Committee have voted in support that zyprexa which is an atypical antipsychotic is effective and considerably safe for the acute treatment of schizophrenia or manic/mixed episodes associated with bipolar I disorder in adolescents aged 13-17 years old. The panel supported the FDA and Lilly's position in approval of zyprexa for the two indications provided prescribers should consider other treatment options first for adolescent patients.
John Hayes(M.D., vice president of Lilly Research Laboratories) said that the committee of experts spent two days discussing the science of a difficult topic being debated in media, doctors' offices and living rooms across the country. He further added that today's committee vote is an important step toward providing help and hope to the many teens suffering from severe mental illness.
For the proposed schizophrenia indication, the panel voted 11-5 with two abstentions, that has demonstrated zyprexa's effectiveness and voted 10-4 with four abstentions, that these data demonstrated acceptable safety. For the proposed indication for manic or mixed episodes associated with bipolar I disorder, the panel voted 17-0, with one abstention that zyprexa's effectiveness had been demonstrated, and voted 11-4 with three abstentions, that these data demonstrated acceptable safety.
The committee examined findings from two pivotal clinical trials of zyprexa in adolescents with schizophrenia or bipolar I disorder including a six-week double-blind, placebo-controlled trial to assess the efficiency and safety of zyprexa in 72 adolescents (aged 13-17 years old) with schizophrenia and a three-week randomized double-blind placebo-controlled trial to assess the efficacy and safety of zyprexa in 107 adolescents (aged 13-17 years) with acute manic or mixed episodes associated with bipolar I disorder.
Zyprexa review article...
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 Zyprexa prescribing information
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