Olanzapine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Espanzapin, Olanzapin, Olanzespin, Zalasta, Zypadhera, Zyprexa; Belgium: Zyprexa; Bulgaria: Olanzapine; Cyprus: Olanzapine, Zalasta, Zyprexa; Czech Republic: Lapozan, Olanzapin, Olanzapine, Olipazix, Parnassan, Zalasta, Zypadhera, Zyprexa; Denmark: Zypadhera, Zyprexa; Estonia: Olansapiin, Olanzapin, Olanzapine, Ozapex, Parnassan, Solazin, Zalasta, Zolafren, Zypadhera, Zyprexa; Finland: Olanzapin, Olanzapine, Solazin, Zalasta, Zolafren, Zypadhera, Zyprexa; France: Medizanoro, Olanpha, Olanzapine, Orolanpha, Orozapinol, Zapinol, Zolacta, Zyprexa; Germany: Olanzapin, Zalasta, Zyprexa; Greece: Caprilon-Lavipharm, Lapenza, Niolib, Olanzapin, Olanzapine, Olapine, Zalasta, Zalepin, Zolafren, Zoxil, Zypadhera, Zyprexa; Hungary: Olanzapin, Olasyn, Olipazix, Olzin, Parnassan, Synza, Zalasta, Zesprone, Zoiros; Ireland: Olanzapine, Olazax, Olstadryn, Zalasta, Zypadhera, Zyprexa; Italy: Zyprexa; Latvia: Olanzapine, Zalasta, Zyprexa; Lithuania: Lapozan, Olanzapin, Olzin, Ozapex, Parnassan, Solazin, Zolafren; Luxembourg: Olanzapine, Zalasta, Zyprexa; Malta: Olanzapine, Zalasta, Zyprexa; Netherlands: Olanzapine; Poland: Lanzapin, Olanzapin, Olanzapina, Olanzapine, Olanzomer; Portugal: Decolan, Fordep, Olanzapina, Olanzapine, Olanzaran, Olapin, Olasyn, Synza, Zalasta, Ziprodec, Zolafren, Zypadhera, Zyprexa; Romania: Lapozan, Olanzapina, Olanzapine, Olipazix, Olstadryn, Parnassan, Zalasta, Zypadhera, Zyprexa; Slovakia: Lapozan, Olanzapin, Olanzapine, Olazax, Olipazix, Parnassan, Zalasta, Zypadhera, Zyprexa; Slovenia: Olanzapin, Zapilux, Zolrix; Spain: Arenbil, Olanzapina, Olapin, Zapris, Zolafren, Zyprexa; Sweden: Olanzapin, Olanzapine, Olanzafloc, Zalasta, Zapilux, Zypadhera, Zyprexa; UK: Zypadhera, Zyprexa.

North America

Canada: Olanzapine, Zyprexa; USA: Olanzapine, Zyprexa.

Latin America

Argentina: Apsico, Midax, Zyprexa; Brazil: Zyprexa; Mexico: Zyprexa.

Asia

Japan: Zyprexa.

Drug combinations

Olanzapine and Fluoxetine

Chemistry

Olanzapine: C~17~H~20~N~4~S. Mw: 312.43. (1) 10H-Thieno[2,3-b][1,5]benzodiazepine, 2-methyl-4-(4-methyl-1-piperazinyl)-; (2) 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine. CAS-132539-06-1 (1992).

Pharmacologic Category

Atypical Antipsychotics. Antimanic Agents. (ATC-Code: N05AH03).

Mechanism of action

A second-generation thienobenzodiazepine antipsychotic which displays potent antagonism of serotonin 5-HT~2A~ and 5-HT~2C~, dopamine D~1-4~, histamine H~1~ and α~1~-adrenergic receptors. Olanzapine shows moderate antagonism of 5-HT~3~ and muscarinic M~1-5~ receptors, and weak binding to GABA-A, BZD, and β-adrenergic receptors. Although precise mechanism of action in schizophrenia and bipolar disorder is unknown, efficacy of olanzapine is thought to be mediated through combined antagonism of dopamine and serotonin type 2 receptor sites.

Therapeutic use

Manifestations of schizophrenia. Acute or mixed mania episodes associated with bipolar I disorder (as monotherapy or in combination with lithium or valproate). Maintenance treatment of bipolar disorder. Acute agitation (schizophrenia or bipolar mania).

Pregnancy and lactiation implications

No evidence of teratogenicity in animal studies. There are no adequate studies in pregnant women. Enters breast milk (not recommended in nursing women).

Unlabeled use

Psychosis/schizophrenia in children or adolescents. Chronic pain. Prevention of chemotherapy-associated delayed nausea or vomiting. Psychosis/agitation related to Alzheimer’s dementia.

Contraindications

Hypersensitivity to olanzapine or any component of the formulation.

Warnings and precautions

May alter cardiac conduction (life-threatening arrhythmias occurred). May cause anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention). Antipsychotic use associated with esophageal dysmotility and aspiration (caution in risk of pneumonia). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of dystonia may be greater with increased doses, use of conventional antipsychotics, males, and younger patients). Atypical antipsychotics associated with development of hyperglycemia (greater association with hyperglycemia than other atypical antipsychotics; caution in diabetes or other disorders of glucose regulation). Use may be associated with neuroleptic malignant syndrome (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension. May be moderate to highly sedating. Possibility of suicide attempt inherent in psychotic illness or bipolar disorder (use with caution in high-risk patients during initiation of therapy). Impaired core body temperature regulation may occur. Significant weight gain (>7% of baseline weight) observed with antipsychotic therapy; incidence varies with product. Elderly patients with dementia-related psychosis treated with atypical antipsychotics are at increased risk of death compared to placebo (increased incidence of cerebrovascular adverse events reported in elderly patients with dementia-related psychosis; olanzapine not approved for this indication). Use with caution in narrow-angle glaucoma (condition may be exacerbated by cholinergic blockade), in hepatic disease or impairment, in myasthenia gravis (condition may be exacerbated by cholinergic blockade), in Parkinson’s disease (may be more sensitive to adverse effects), in breast cancer or other prolactin-dependent tumors (elevates prolactin levels), in renal disease, and in risk of seizures. Elderly patients may be at increased risk of seizures due to increased prevalence of predisposing factors. Olanzapine levels may be lower in patients who smoke.

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