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(External links: added link to mechanism of action of olanzapine)
 
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[[Image:Olanzapine.png|170px|Olanzapine chemical structure]]<br/>
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[[Image:Olanzapine.png|170px|Olanzapine chemical structure]]<br />
 
''Olanzapine''
 
''Olanzapine''
 
|-
 
|-
| align="center" colspan="2" | ''2-methyl-4-(4-methyl-1-piperazinyl)-<BR>10''H''-thieno[2,3-''b''][1,5]benzodiazepine''
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| align="center" colspan="2" | ''2-methyl-4-(4-methyl-1-piperazinyl)-<br />10''H''-thieno[2,3-''b''][1,5]benzodiazepine''
 
|- align="center" style="border-bottom: 3px solid gray"
 
|- align="center" style="border-bottom: 3px solid gray"
| '''[[CAS number]]''' <br/> 132539-06-1
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| '''[[CAS number]]'''<br />132539-06-1
| '''[[ATC code]]''' <br/> [[ATC code N05|N05]]AH03
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| '''[[ATC code]]'''<br />[[ATC code N05|N05]]AH03
 
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| bgcolor="#eeeeee" | [[Chemical formula]]
 
| bgcolor="#eeeeee" | [[Chemical formula]]
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| bgcolor="#ddeeff" | ?
 
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| bgcolor="#eeeeee" | [[Pregnancy category (pharmaceutical)|Pregnancy category]]
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| bgcolor="#eeeeee" | [[Pregnancy category (pharmaceutical)|Pregnancy category]]
 
| bgcolor="#ddeeff" | ?
 
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| bgcolor="#eeeeee" | Routes of administration
 
| bgcolor="#eeeeee" | Routes of administration
 
| bgcolor="#ddeeff" | ?
 
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'''Olanzapine''' (sold as '''Zyprexa'''®, '''Zydis®''', or in combination with [[fluoxetine]], as '''Symbyax'''®) was the second [[atypical antipsychotic]] to gain FDA approval and has become one of the most commonly used [[atypical antipsychotic]]s. Olanzapine has been [[FDA]] approved for the treatment of [[schizophrenia]], acute [[mania]] in [[bipolar disorder]], agitation associated with schizophrenia and bipolar disorder, and as maintenance treatment in [[bipolar disorder]]. Olanzapine is manufactured and marketed by the [[pharmaceutical company]] [[Eli Lilly and Company]]. It is available as a pill that comes in the strengths of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, and 20 mg. It is also available as Zydis orally disintegrating tables in the strengths of 5 mg, 10 mg, 15 mg, and 20 mg.
+
'''Olanzapine''' (sold as '''Zyprexa'''®, '''Zydis®''', or in combination with [[fluoxetine]], as '''Symbyax'''®) was the second [[atypical antipsychotic]] to gain FDA approval and has become one of the most commonly used [[atypical antipsychotic]]s. Olanzapine has been [[FDA]] approved for the treatment of [[schizophrenia]], acute [[mania]] in [[bipolar disorder]], agitation associated with schizophrenia and bipolar disorder, and as maintenance treatment in [[bipolar disorder]]. Olanzapine is manufactured and marketed by the [[pharmaceutical company]] [[Eli Lilly and Company]]. It is available as a pill that comes in the strengths of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, and 20 mg. It is also available as Zydis orally disintegrating tables in the strengths of 5 mg, 10 mg, 15 mg, and 20 mg.
   
 
Olanzapine can also be used to treat anxiety. In particular, unlike benzodiazapenes, antipsychotics are non-addictive. Some psychiatrists have also been known to prescribe it to eating disorder patients, due both to its mood stabilising effects and tendency to increase weight.
 
Olanzapine can also be used to treat anxiety. In particular, unlike benzodiazapenes, antipsychotics are non-addictive. Some psychiatrists have also been known to prescribe it to eating disorder patients, due both to its mood stabilising effects and tendency to increase weight.
   
 
==Pharmacology==
 
==Pharmacology==
Olanzapine is structurally similar to [[clozapine]], and is classified as a [[thienobenzodiazepine]]. Olanzapine has a high affinity for [[dopamine receptor|dopamine]] and [[serotonin receptor|serotonin]] receptors. Like most atypical antipsychotics compared to the older typical ones, Olanzapine has a lower affinity for [[histamine receptor|histamine]], [[Muscarinic acetylcholine receptor|cholinergic muscarinic]] and [[alpha-adrenergic receptor|alpha adrenergic]] receptors. The mechanism of action of olanzapine is unknown, however it is theorized that olanzapine's antipsychotic activity is mediated primarily by antagonism at [[dopamine]] receptors, specifically D2. [[Serotonin]] antagonism may also play a role in the effectiveness of olanzapine, but the significance of [[5-HT2A]] antagonism is debated among researchers. Antagonism at muscarinic, histaminic and alpha adrenergic receptors likely explains some of the side effects of olanzapine, such as [[anticholinergic]] effects, weight gain, [[sedation]] and [[orthostatic hypotension]].
+
Olanzapine is structurally similar to [[clozapine]], and is classified as a [[thienobenzodiazepine]]. Olanzapine has a high affinity for [[dopamine receptor|dopamine]] and [[serotonin receptor|serotonin]] receptors. Like most atypical antipsychotics compared to the older typical ones, Olanzapine has a lower affinity for [[histamine receptor|histamine]], [[Muscarinic acetylcholine receptor|cholinergic muscarinic]] and [[alpha-adrenergic receptor|alpha adrenergic]] receptors. The mechanism of action of olanzapine is unknown, however it is theorized that olanzapine's antipsychotic activity is mediated primarily by antagonism at [[dopamine]] receptors, specifically D2. [[Serotonin]] antagonism may also play a role in the effectiveness of olanzapine, but the significance of [[5-HT2A]] antagonism is debated among researchers. Antagonism at muscarinic, histaminic and alpha adrenergic receptors likely explains some of the side effects of olanzapine, such as [[anticholinergic]] effects, weight gain, [[sedation]] and [[orthostatic hypotension]].
   
 
==Pharmacokinetics==
 
==Pharmacokinetics==
Olanzapine displays linear kinetics. Its elimination half-life ranges from 21 to 54 hours. Steady state plasma concentrations are achieved in about a week. Olanzapine undergoes extensive [[first pass metabolism]] and [[bioavailability]] is not affected by food.
+
Olanzapine displays linear kinetics. Its elimination half-life ranges from 21 to 54 hours. Steady state plasma concentrations are achieved in about a week. Olanzapine undergoes extensive [[first pass metabolism]] and [[bioavailability]] is not affected by food.
   
 
==Metabolism==
 
==Metabolism==
Olanzapine is metabolized by the [[Cytochrome P450]] system isoenzymes 1A2 and 2D6 (minor pathway). Drug metabolism may be increased or decreased by agents that induce (e.g. cigarette smoke) or inhibit (e.g. fluvoxamine or ciprofloxacin) CYP1A2 activity respectively.
+
Olanzapine is metabolized by the [[Cytochrome P450]] system isoenzymes 1A2 and 2D6 (minor pathway). Drug metabolism may be increased or decreased by agents that induce (e.g. cigarette smoke) or inhibit (e.g. fluvoxamine or ciprofloxacin) CYP1A2 activity respectively.
   
 
==Adverse events==
 
==Adverse events==
Adverse events reported in the package insert for olanzapine include dry mouth, [[dizziness]], [[sedation]], [[insomnia]], [[orthostatic hypotension]], [[akathisia]], and [[obesity|weight gain]]. Olanzapine is reported to cause [[extrapyramidal symptom]]s, [[tardive dyskinesia]] and [[neuroleptic malignant syndrome]], although at a much reduced rate when compared to the classical antipsychotics.
+
Adverse events reported in the package insert for olanzapine include dry mouth, [[dizziness]], [[sedation]], [[insomnia]], [[orthostatic hypotension]], [[akathisia]], and [[obesity|weight gain]]. Olanzapine is reported to cause [[extrapyramidal symptom]]s, [[tardive dyskinesia]] and [[neuroleptic malignant syndrome]], although at a much reduced rate when compared to the classical antipsychotics.
   
Recently the FDA required the manufacturers of all atypical antipsychotics to include a warning about the risk of [[hyperglycemia]] and [[diabetes]] with atypical antipsychotics. Additionally there are some case reports of olanzapine-induced [[diabetic ketoacidosis]]. There is data showing that olanzapine can decrease insulin sensitivity. In addition, increased [[triglyceride]] levels may also be an issue with olanzapine. Impaired glucose metabolism, high triglycerides, and obesity have been shown to be constituents of the [[metabolic syndrome]] and may increase the risk of [[cardiovascular disease]]. The data suggests that olanzapine may be more likely to cause adverse metabolic effects than some of the other atypical antipsychotics.
+
Recently the FDA required the manufacturers of all atypical antipsychotics to include a warning about the risk of [[hyperglycemia]] and [[diabetes]] with atypical antipsychotics. Additionally there are some case reports of olanzapine-induced [[diabetic ketoacidosis]]. There is data showing that olanzapine can decrease insulin sensitivity. In addition, increased [[triglyceride]] levels may also be an issue with olanzapine. Impaired glucose metabolism, high triglycerides, and obesity have been shown to be constituents of the [[metabolic syndrome]] and may increase the risk of [[cardiovascular disease]]. The data suggests that olanzapine may be more likely to cause adverse metabolic effects than some of the other atypical antipsychotics.
   
 
Citing an increased risk of [[stroke]], in [[2004]] the Committee for the Safety of Medicines (CSM) in the UK issued a warning that olanzapine and [[risperidone]], both atypical antipsychotic medications, should not be given to elderly patients with [[dementia]].
 
Citing an increased risk of [[stroke]], in [[2004]] the Committee for the Safety of Medicines (CSM) in the UK issued a warning that olanzapine and [[risperidone]], both atypical antipsychotic medications, should not be given to elderly patients with [[dementia]].
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* Duggan and others, "[http://www.cochrane.org/cochrane/revabstr/AB001359.htm Olanzapine for schizophrenia (Cochrane Review)]", [[The Cochrane Library]], 2005.
 
* Duggan and others, "[http://www.cochrane.org/cochrane/revabstr/AB001359.htm Olanzapine for schizophrenia (Cochrane Review)]", [[The Cochrane Library]], 2005.
 
* [http://www.zyprexa.com/ Zyprexa] - manufacturer's site
 
* [http://www.zyprexa.com/ Zyprexa] - manufacturer's site
  +
* [http://psychopharmacologyinstitute.com/antipsychotics/olanzapine/mechanism-action-pharmacodynamics-olanzapine/ Mechanism of Action of Olanzapine]
 
* [http://www.olanzapine.com/ Olanzapine.com] - promotional site
 
* [http://www.olanzapine.com/ Olanzapine.com] - promotional site
 
* [http://pi.lilly.com/us/zyprexa-pi.pdf Package Insert] (PDF)
 
* [http://pi.lilly.com/us/zyprexa-pi.pdf Package Insert] (PDF)
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<!--Categories-->
 
<!--Categories-->
[[Category:Atypical antipsychotics]]
 
   
 
<!--Other languages-->
 
<!--Other languages-->
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[[zh:奥氮平]]
 
[[zh:奥氮平]]
 
{{enWP|Olanzapine}}
 
{{enWP|Olanzapine}}
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[[Category:Atypical antipsychotics]]

Latest revision as of 15:42, November 9, 2013

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Olanzapine
Olanzapine

2-methyl-4-(4-methyl-1-piperazinyl)-
10
H-thieno[2,3-b][1,5]benzodiazepine
CAS number
132539-06-1
ATC code
N05AH03
Chemical formula C17H20N4S
Molecular weight 312.439
Bioavailability  ?
Metabolism  ?
Elimination half-life 21-54h
Excretion  ?
Pregnancy category  ?
Legal status  ?
Routes of administration  ?

Olanzapine (sold as Zyprexa®, Zydis®, or in combination with fluoxetine, as Symbyax®) was the second atypical antipsychotic to gain FDA approval and has become one of the most commonly used atypical antipsychotics. Olanzapine has been FDA approved for the treatment of schizophrenia, acute mania in bipolar disorder, agitation associated with schizophrenia and bipolar disorder, and as maintenance treatment in bipolar disorder. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company. It is available as a pill that comes in the strengths of 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, and 20 mg. It is also available as Zydis orally disintegrating tables in the strengths of 5 mg, 10 mg, 15 mg, and 20 mg.

Olanzapine can also be used to treat anxiety. In particular, unlike benzodiazapenes, antipsychotics are non-addictive. Some psychiatrists have also been known to prescribe it to eating disorder patients, due both to its mood stabilising effects and tendency to increase weight.

PharmacologyEdit

Olanzapine is structurally similar to clozapine, and is classified as a thienobenzodiazepine. Olanzapine has a high affinity for dopamine and serotonin receptors. Like most atypical antipsychotics compared to the older typical ones, Olanzapine has a lower affinity for histamine, cholinergic muscarinic and alpha adrenergic receptors. The mechanism of action of olanzapine is unknown, however it is theorized that olanzapine's antipsychotic activity is mediated primarily by antagonism at dopamine receptors, specifically D2. Serotonin antagonism may also play a role in the effectiveness of olanzapine, but the significance of 5-HT2A antagonism is debated among researchers. Antagonism at muscarinic, histaminic and alpha adrenergic receptors likely explains some of the side effects of olanzapine, such as anticholinergic effects, weight gain, sedation and orthostatic hypotension.

PharmacokineticsEdit

Olanzapine displays linear kinetics. Its elimination half-life ranges from 21 to 54 hours. Steady state plasma concentrations are achieved in about a week. Olanzapine undergoes extensive first pass metabolism and bioavailability is not affected by food.

MetabolismEdit

Olanzapine is metabolized by the Cytochrome P450 system isoenzymes 1A2 and 2D6 (minor pathway). Drug metabolism may be increased or decreased by agents that induce (e.g. cigarette smoke) or inhibit (e.g. fluvoxamine or ciprofloxacin) CYP1A2 activity respectively.

Adverse eventsEdit

Adverse events reported in the package insert for olanzapine include dry mouth, dizziness, sedation, insomnia, orthostatic hypotension, akathisia, and weight gain. Olanzapine is reported to cause extrapyramidal symptoms, tardive dyskinesia and neuroleptic malignant syndrome, although at a much reduced rate when compared to the classical antipsychotics.

Recently the FDA required the manufacturers of all atypical antipsychotics to include a warning about the risk of hyperglycemia and diabetes with atypical antipsychotics. Additionally there are some case reports of olanzapine-induced diabetic ketoacidosis. There is data showing that olanzapine can decrease insulin sensitivity. In addition, increased triglyceride levels may also be an issue with olanzapine. Impaired glucose metabolism, high triglycerides, and obesity have been shown to be constituents of the metabolic syndrome and may increase the risk of cardiovascular disease. The data suggests that olanzapine may be more likely to cause adverse metabolic effects than some of the other atypical antipsychotics.

Citing an increased risk of stroke, in 2004 the Committee for the Safety of Medicines (CSM) in the UK issued a warning that olanzapine and risperidone, both atypical antipsychotic medications, should not be given to elderly patients with dementia.

Finally, Olanzapine causes severe tiredness and hence may cause severe mental and physical retardation.

The results of a large, random-design study funded by NIH's National Institute of Mental Health (NIMH) were published in September 2005. The 18-month study, which involved 1,400 participants at 57 sites around the country, found that "patients on olanzapine also experienced substantially more weight gain and metabolic changes associated with an increased risk of diabetes than those participants taking the other drugs." [1]

External links Edit



fr:Olanzapinenl:Zyprexa ru:Оланзапин sv:Olanzapin zh:奥氮平

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