Index
It is a medication used to treat schizophrenia and acute manic episodes associated with bipolar disorder.
Olanzapine belongs to a class of medications, this class includes clozapine (Clozaril), risperidone (Risperdal), aripiprazole (Abilify), and ziprasidone (Geodon), known as atypical antipsychotics.
The exact mechanism of action of Olanzapine is not known. It can work by blocking the receptors of several neurotransmitters (chemicals that the nerves use to communicate with each other) in the brain. It binds to the receptors alpha-1, dopamine, histamine H-1, muscarinic, and serotonin type 2 (5-HT2).
The Food and Drug Administration approved Olanzapine in 1996.
Distribution and class names:
- Marca: Zyprexa, Zyprexa Relprevv, Zyprexa Zydis.
- Generic name : Olanzapine.
- Drug Class: Antipsychotics, 2nd Generation; Antimanic agents.
Applications
Olanzapine treats certain mental/mood conditions (such as schizophrenia and bipolar disorder). It can also be used in combination with other medications to treat depression .
This medication can help decrease hallucinations and help you think more clearly and positively about yourself, feel less agitated, and take a more active part in daily life.
Olanzapine is a type of medicine known as an atypical antipsychotic. It works in the brain, where it affects the activity of several neurotransmitters, particularly dopamine and serotonin (also known as 5HT).
Neurotransmitters are chemicals stored in nerve cells and participate in the transmission of messages between nerve cells.
Dopamine and serotonin are neurotransmitters known for their participation in regulating mood, behavior, thinking, and perception, among other things.
The psychotic illness seems to be caused by alterations in the activity of neurotransmitters (mainly dopamine) in the brain.
It is known that schizophrenia is associated with an overactivity of dopamine in the brain, which may be responsible for the delusions and hallucinations that are a hallmark of this disease.
Olanzapine works by blocking the brain receptors in which dopamine acts. This prevents excessive dopamine activity and thus helps control the symptoms of schizophrenia and mania.
Olanzapine improves symptoms such as:
- Hallucinations (hearing, seeing, or feeling things not there).
- Disturbed thoughts (such as having wrong beliefs or feeling unusually suspicious or paranoid).
- I was feeling depressed, anxious, agitated, hostile, or unusually excited, lacking emotion.
What are Olanzapine preparations available?
- Tablets: 2.5mg, 5mg, 7.5mg, 10mg, 15mg, 20mg.
- Tablets (which disintegrate orally): 5mg, 10mg, 15mg, 20mg.
- Injection (immediate release): vial of 10mg.
- Extended release powder suspension for injection: 210mg, 300mg and 405mg.
Doses available for adults
Dosage forms for adults and strengths.
Dosage in tablets and tablets that disintegrate orally:
- 2.5mg, 5mg, 7.5mg, 10mg, 15mg, 20mg.
Intramuscular (IM) injection, short-acting:
- 10mg.
Intramuscular injection (IM), prolonged-release suspension:
- 210mg / bottle, 300mg / bottle, 405mg / bottle.
Available doses of Olanzapine for children and adolescents
Pediatric dosage forms and Strengths.
Dosage in tablets:
- 2.5mg, 5mg, 7.5mg, 10mg, 15mg, 20mg.
Tablets, which are disintegrated orally:
- 5mg, 10mg, 15mg, 20mg.
Dosing considerations:
Schizophrenia in adults
Doses are taken orally:
- Tablets of 5mg – 10mg per day initially; if necessary, increments of 5 mg per day can be given at intervals greater than one week.
- Maintenance: 10mg – 20mg per day; It should not exceed 20mg per day.
Intramuscular injection, prolonged-release:
Dosage recommended by your doctor, based on oral dosage:
- Oral dose 10mg per day: Administer an intramuscular injection of 210mg every two weeks or an intramuscular injection of 405mg every four weeks for the first eight weeks, then 150mg every two weeks or 300mg every 4 weeks.
- Oral dose 15mg per day: Administer an intramuscular injection of 300mg every two weeks for the first eight weeks, then 210mg every 2 weeks or 405mg every 4 weeks.
- 20mg oral dose per day: Administer an intramuscular injection of 300mg every 2 weeks for the first eight weeks, then 300mg every 2 weeks.
Schizophrenia in children:
Less than 13 years: Safety and efficacy not established.
- 13 years – 17 years: initially 2.5mg – 5mg per day orally.
- Target dose: 10mg per day.
- Adjust by increments / decrements of 2.5mg – 5mg; Dosing range, 2.5mg – 20mg per day.
Bipolar mania in adults:
Indicated for acute maintenance treatment of manic or mixed episodes associated with bipolar disorder 1, it can be used as monotherapy or in combination with lithium or valproate to treat manic or mixed episodes associated with bipolar disorder.
- Monotherapy: 10mg – 15mg / day orally initially.
- I am attached to lithium or valproate: 10 mg/day orally initially.
- Maintenance: 5mg – 20mg / day orally; It should not exceed 20mg / day.
Depression in bipolar disorder.
I indicated depressive episodes associated with bipolar I disorder in combination with fluoxetine.
- Use in conjunction with fluoxetine.
- 5mg in the afternoon; adjusted to a range of 5mg – 12.5 mg/day; it can be increased up to 20 mg/day in resistant depression .
Dosing considerations:
- Dose adjustments, if necessary, should be made at intervals more significant than 24 hours.
Schizophrenia or agitation related to bipolar disorder in adults:
- Intramuscular injection of 10mg of fast action.
- Consider 5mg – 7.5mg for geriatric patients or if circumstances justify it.
- Subsequent intramuscular injections of up to 10mg may be administered 2 hours after the 1st dose and 4 hours after the 2nd dose; It should not exceed 30 mg/day.
Bipolar disorder I (manic or mixed episodes) in children:
Less than 13 years: Safety and efficacy not established.
- 13 years – 17 years: 2.5mg – 5mg / day orally initially.
- Ideal dose, 10mg / day.
- Adjustment by increments / decrements of 2.5mg – 5mg.
- Dosage range, 2.5mg – 20mg / day.
Stuttering (unusual indication) in children:
Children twelve years of age or younger.
- Tablets of 1.25mg orally at bedtime for four weeks, then 2.5mg tablets before bedtime.
Children over twelve years of age
- Tablets of 2.5mg orally at bedtime for four weeks, then Tablets of 5mg before bedtime.
Modifications of doses:
Renal insufficiency: it is not necessary to adjust the dose.
Hepatic insufficiency: it may be required to change the amount with caution.
Administration of the medication
Administration of an intramuscular injection:
- The preparations of a prolonged-release and prolonged-release intramuscular injection are not interchangeable.
- Short-acting: dissolve in 2.1ml of SWI to solve 5 mg/ml; Inject deeply and slowly within 1 hour of reconstitution.
- Prolonged-release: reconstitute with the supplied diluent (210mg in 1.3ml, vial of 300mg in 1.8ml, vial of 405mg in 2.3ml); Inject deeply into the gluteal muscle.
- Do not use lorazepam injection for reconstitution, and do not mix with haloperidol or diazepam in a syringe.
Considerations of geriatric dosage:
It is not approved for psychosis related to dementia due to an increased risk of cardiovascular mortality or infection.
Think of a minimum initial dose.
Schizophrenia:
- Tablets of 2.5mg – 5mg / day taken orally initially.
Intramuscular injection of prolonged-release: 150mg every four weeks in patients weakened or predisposed to episodes of hypotension; not studied in patients with renal or hepatic insufficiency; requires administration of deep intramuscular injection (muscle mass in older adults may be sufficient)
Schizophrenia or agitation related to bipolar disorder:
Short-acting intramuscular injection:
- 5mg; consider 2.5mg if the patient is predisposed to hypotensive reactions.
How long has Olanzapine taken effect?
It may take a few weeks to take Olanzapine to develop to its maximum effect, but some people find that it begins to help during the first week.
Your doctor will want to check your progress during this time and may wish to increase your dose if necessary.
Treatment with Olanzapine is usually long-term, and it is essential to continue taking it every day, as directed by your doctor, even once you start to feel better.
Stopping the treatment can cause a relapse, so you should only stop taking the medication if your doctor recommends it.
What are the side effects associated with the use of Olanzapine?
Side effects of Olanzapine include:
- Dizziness / low blood pressure when standing up.
- Weight gain, dose-dependent.
- High levels of triglycerides in the blood.
- High levels of cholesterol.
- Drowsiness is dependent on the dose.
- Extrapyramidal (EPS) symptoms, dose-dependent (muscle spasms, erratic movements, slow movements).
- Dry mouth.
- Weakness.
- Dizziness.
- Accidental injuries
- Insomnia.
- High level of alanine aminotransferase (ALT).
- Constipation.
- Indigestion.
- High blood sugar
- Temblor.
- Weakness.
- Restlessness.
- Parkinsonism reactions.
This document does not contain all possible side effects, and others may occur.
For example, various movement disorders can also occur with Olanzapine and extrapyramidal effects (sudden, often erratic, involuntary movements of the head, neck, arms, body, or eyes).
The dyskinesia late (involuntary movements of the mouth, tongue, jaw, or eyelids) can also occur in 1 of every 100 patients receiving Olanzapine. Some cases can be irreversible.
The probability of developing tardive dyskinesia increases with prolonged treatment.
There may be an increased risk of high blood sugar levels and diabetes with Olanzapine and the other antipsychotic medications in its class.
Patients should be tested during treatment to detect high blood sugar levels.
In addition, people with risk factors for diabetes, including obesity or a family history of diabetes, should have their blood sugar levels fasted before starting treatment and periodically throughout the treatment to detect the onset of the disease. Diabetes.
Any patient who develops symptoms that suggest diabetes during treatment should be tested for diabetes.
Interactions
Severe interactions:
No severe reactions are known from the use of Olanzapine. Powerful interactions with Olanzapine include:
- Apomorphine.
- Bromocriptine.
- Carolina.
- Dopamine
- Fluvoxamine.
- Levodopa.
- Lisuride.
- Mefloquine.
- Methyldopa .
- Ondansetron.
- Pefloxacin.
- Pramipexole.
- Ropinirole.
- Sodium oxybate
- Umeclidinium bromide / inhaled vilanterol.
- Inhaled vilanterol / fluticasone furoate.
Moderate interactions:
Olanzapine has known moderate interactions with at least 293 different medications.
Mild interactions:
- Brimonidine.
- Chasteberry.
- Ethanol.
- Eucalyptus.
- Omeprazole.
- Ruxolitinib.
- Wise.
Warnings and precautions
Warnings:
Not approved for psychosis related to dementia; Elderly patients with dementia-related psychosis who are treated with antipsychotic medications have an increased risk of death.
Patients are at risk of severe sedation (including coma) or delirium after each injection. They should be observed for at least 3 hours in a registered facility with easy access to emergency response services.
Do not take Zyprexa, Zyprexa Relprevv, or Zyprexa Zydis if you are allergic to Olanzapine or any of the ingredients in this medicine.
Keep out of the reach of children. Get medical help or contact a Poison Control Center immediately in case of overdose.
Precautions
Increased risk of hyperglycemia and diabetes; in some cases, hyperglycemia concomitant with atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death.
Control blood glucose in high-risk patients.
Irreversible and involuntary dyskinetic movements can be developed with antipsychotic drugs; the prevalence seems to be higher among the elderly, especially older women. Discontinue if it is clinically appropriate.
It can cause anticholinergic effects, including ileus paralytic, urinary retention, xerostomia, hyperplasia, and Benign prostatic and visual problems.
Reported neutropenia, leucopenia, and agranulocytosis; suspend treatment at the first sign of blood dyscrasias or if the absolute neutrophil count is less than 1000 / mm³.
Cerebrovascular effects were reported, including stroke and transient ischemic attack that resulted in death.
More significant potential for weight gain; Patients should receive regular weight control.
Appropriate clinical monitoring is recommended, including the fasting blood lipid test at the beginning and periodically during treatment.
The increase in prolactin levels can manifest as abnormal menstruation, sexual dysfunction, and enlargement of the breasts.
Do not reconstitute with lorazepam injection; Do not mix with diazepam or haloperidol in a syringe.
In narrow-angle glaucoma, cardiovascular disease, cerebrovascular disease, prostatic hypertrophy, hypovolemia, and dehydration can cause hyperglycemia and, in some cases, can be extreme, resulting in ketoacidosis, hyperosmolar coma, or death.
Intramuscular injection of more than one injection is associated with substantial orthostatic hypotension (33%); Keep the patient in a reclined position and check the blood pressure before intramuscular injection doses.
In controlled studies, changes in average to high prolactin levels were observed (incidence, 30%).
Be cautious in patients at risk of pneumonia; it can cause esophageal dysmotility and aspiration.
Be careful with strenuous exercise, dehydration, exposure to heat, and medications with anticholinergic effects; a deteriorated central body temperature regulation may occur.
Doctors who prescribe to adolescents should consider the possible long-term risks, which in many cases may lead them to prescribe other medications first in this population.
Pharmacological reactions with eosinophilia and systemic symptoms (DRESS) were reported with exposure to Olanzapine.
Pharmacological reaction with eosinophilia and systemic symptoms can occur with a skin reaction (rash or exfoliative dermatitis), eosinophilia, fever, and lymphadenopathy with systemic complications such as hepatitis nephritis, pneumonitis, myocarditis, and pericarditis.
The pharmacological reaction with eosinophilia and systemic symptoms is sometimes fatal; suspend Olanzapine if you suspect a drug reaction with eosinophilia and systemic symptoms.
If the patient requires treatment with antipsychotic drugs after recovering from the neuroleptic malignant syndrome, the possible reintroduction of pharmacological therapy should be carefully considered.
The patient must be carefully monitored since neuroleptic malignant syndrome has been reported.
It can impair judgment, thinking, and motor skills; Be careful when operating machinery.
Olanzapine is indicated as an integral part of the comprehensive treatment program for pediatric patients with schizophrenia and bipolar disorder, which may include other measures (e.g., psychological, educational, social) as well.
Olanzapine in pregnancy and lactation
During pregnancy, use Olanzapine with caution; there are no adequate studies of Olanzapine in pregnant women. Olanzapine should only be given to pregnant women if the benefits justify the unknown risks.
Studies in animals show risk studies, and in humans, there are no studies available, or studies were not conducted.
Neonates exposed to antipsychotic medications during the third trimester of pregnancy are at risk of developing extrapyramidal symptoms (EPS) or withdrawal symptoms after delivery.
These complications vary in severity, some are self-limiting, and others require support from the intensive care unit and prolonged hospitalization.
Olanzapine enters breast milk; It is recommended that nursing mothers do not use Olanzapine.
How should I keep Olanzapine stored?
The tablets should be kept at room temperature, 20 ° C – 25 ° C (68 ° F – 77 ° F). The suspension is stored at room temperature, not to exceed 30 ° C (86 ° F).
Oral disintegration tablets:
- Store at room temperature, 68 ° F – 77 ° F (20 ° C – 25 ° C).
- Preserve light and moisture.
Intramuscular, short-acting injection:
- Before reconstitution: store at room temperature, 68 ° C – 77 ° F (20 ° C – 25 ° C).
- Reconstituted flask: store at room temperature, 68 ° C – 77 ° F (20 ° C – 25 ° C).
- Discard any unused portion of the reconstituted bottle.
- Protect from light, do not freeze.
Intramuscular injection, prolonged-release:
- Before reconstitution: Store at room temperature not to exceed 30 ° C (86 ° F).
- Suspended solution: Store at room temperature for up to 24 hours if necessary.
Shake immediately before removing the product. Administer directly once the suspension is drawn to the syringe.
Summary
Olanzapine (Zyprexa, Zydis, Zyprexa Relprevv) is a medication prescribed to treat schizophrenia associated with bipolar disorder and some types of depression.
It helps control moderate to severe manic episodes of manic depression (bipolar affective disorder).
If your manic episode improves with olanzapine treatment, your doctor may suggest that you continue taking it as a mood stabilizer. This can help prevent future episodes of mania or depression.
Olanzapine is not licensed for use in children under 18 years of age. However, specialists can sometimes prescribe it to treat schizophrenia or mania in children 12 to 18 years of age.
Most people take Olanzapine orally, either as standard tablets or tablets that dissolve in the tongue. For people with schizophrenia, it can also be given as a long-acting “long-acting” injection that lasts two or four weeks.
Olanzapine is a generic medicine that comes in standard tablets and tablets that dissolve in the tongue. Olanzapine is also available under several brands, which include:
- Zalasta tablets and orodispersible tablets.
- Zyprexa tablets.
The Olanzapine deposit injection is available under the brand name ZypAdhera.
