olanzapine (Rx) - Zyprexa, Zyprexa Relprevv, more..Zyprexa Zydis

Dosing Forms & Strengths

Schizophrenia

Bipolar Mania

Monotherapy: 10-15 mg PO qD initially

Adjunct with lithium or valproate: 10 mg PO qD initially

Dosage adjustments, if necessary, at intervals >24 hr

Maintenance: 5-20 mg PO qD

No more than 20 mg qD

Monotherapy or combine with lithium or valproate

Schizophrenia or Bipolar-Related Agitation

10 mg IM (consider 5-7.5 mg for geriatric or if circumstances warrant)

May administer subsequent IM doses up to 10 mg, 2 hr after 1st dose and 4hr after 2nd dose

Maximum: 30 mg/day IM

Use Zyprexa IntraMuscular (short-acting)

Geriatric Dosing

Not approved for dementia-related psychosis because of increased risk of cardiovascular or infectious related deaths (see Black Box Warnings)

Consider lower starting dose for elderly patients

Other Information

See also combo with fluoxetine (Symbyax)

Administration

IM: Zyprexa IntraMuscular (short-acting) and Zyprexa Relprevv (long-acting) NOT interchangeable!

Zyprexa Relprevv: reconstitute with supplied diluent: 210 mg vial in 1.3 mL; 300 mg in 1.8 mL and 405 mg in 2.3 mL

Zyprexa Relprevv: deep in gluteal muscle

Zyprexa IntraMuscular: dissolve in 2.1 mL SWI to yield 5 mg/mL soln; inject deep and slow within 1 hr of reconstitution

Do NOT use lorazepam injection for reconstitution

Do NOT mix with haloperidol or diazepam in syringe

Dosing Forms & Strengths

Bipolar I Disorder (Manic or Mixed Episodes)

<13 years: Safety and efficacy not established

Adolescents: 2.5-5 mg PO qD initially; target dose is 10 mg/day; adjust by dose increments/decrements of 2.5-5 mg

Dosage range: 2.5-20 mg/day

Schizophrenia

<13 years: Safety and efficacy not established

Adolescents (13-17 years): 2.5-5 mg PO qD initially; target dose is 10 mg/day; adjust by dose increments/decrements of 2.5-5 mg

Dosage range: 2.5-20 mg/day

Other Information

Weight gain and hyperlipidemia: Consider increased potential (in adolescents as compared with adults) for weight gain and hyperlipidemia; clinicians should consider the potential long-term risks when prescribing to adolescents, and in many cases this may lead them to consider prescribing other drugs first in adolescents

Comprehensive treatment program in pediatric patients: olanzapine indicated as an integral part of a total treatment program for pediatric patients with schizophrenia and bipolar disorder that may include other measures (eg, psychological, educational, social)

Other Indications & Uses

Off-label for stuttering: 1.25-2.5 mg PO hs

>10%

Weight gain (5-40%, dose dependent)

Hypertriglyceridemia (up to 39%)

Hypercholesterolemia (up to 39%)

Somnolence (6-39%, dose dependent)

Extrapyramidal symptoms (15-32%, dose dependent)

Xerostomia (9-22%)

Weakness (2-20%)

Dizziness (4-18%)

Accidental injury (12%)

Insomnia (12%)

Elevated ALT (5-12%)

Constipation (9-11%)

Dyspepsia (7-11%)

Hyperprolactinemia

Hyperglycemia

<1%

Syncope

Sudden cardiac death

Hyperglycemia

Diabetic coma with ketoacidosis

Diabetic ketoacidosis

Acute hemorrhagic pancreatitis

Venous thromboembolism

Immune hypersensitivity reaction

Cerebrovascular disease

Seizure (0.9% ), status epilepticus

Suicidal intent (0.1% to 1% )

Pulmonary embolism

Death

NMS, tardive dyskinesia

Black Box Warnings

Elderly patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials; deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature

Not approved for the treatment of patients with dementia-related psychosis

Patients are at risk for severe sedation (including coma) and/or delirium after each injection and must be observed for at least 3 hr in a registered facility with ready access to emergency response services

Because of this risk, olanzapine is only available only through a restricted distribution program

Contraindications

Documented hypersensitivity

Breastfeeding

Cautions

Increased risk of hyperglycemia and diabetes; in some cases, hyperglycemia concomitant with use of atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death

Monitor blood glucose of high-risk pts

Irreversible, involuntary, dyskinetic movements may develop with antipsychotic drugs; although prevalence appears to be highest among elderly individuals, especially elderly women

Neuroleptic malignant syndrome has been reported

Increased potential for weight gain

May induce orthostatic hypotension associated with dizziness, tachycardia, bradycardia and, in some patients, syncope, especially during the initial dose-titration period, probably reflecting its alpha-1-adrenergic antagonistic properties

Do not reconstitute with lorazepam inj; do not mix with diazepam or haloperidol in syringe

FDA Warning regarding off-label use for dementia in elderly (see Black Box Warnings)

Caution in narrow-angle glaucoma, cardiovascular disease, cerebrovascular disease, prostatic hypertrophy, seizure disorders, hypovolemia, and dehydration; hyperglycemia may occur and in some cases be extreme, resulting in ketoacidosis, hyperosmolar coma, or death; administration of more than one IM injection is associated with substantial orthostatic hypotension (33%), maintain patient in recumbent position and monitor blood pressure before repeating IM doses

Prolactinemia: Changes from normal to high prolactin levels observed in controlled studies; incidence 30%

Mechanism of Action

Acts upon several types of neurotransmitter receptors