Names and pronunciation
(oh-lanz′a-peen) ZyPREXA, ZyPREXA Relprevv, ZyPREXA Zydis
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Individual generic drug information
Extracted information for OLANZapine only.
(oh-lanz′a-peen) ZyPREXA, ZyPREXA Relprevv, ZyPREXA Zydis
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Func. class.: Antipsychotic (1st generation), neuroleptic
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Chem. class.: Thienobenzodiazepine
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Do not confuse: OLANZapine/olsalazine ZyPREXA/CeleXA/ZyrTEC /Zestril/Zolpidem
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ACTION: May mediate antipsychotic activity by both DOPamine and serotonin type 2 (5-HT2) antagonists; may antago- nize muscarinic receptors, histaminic (H1)- and α-adrenergic receptors
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USES: Schizophrenia, acute manic O episodes with bipolar disorder, acute agi- tation
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Unlabeled uses: Chemotherapy-related breakthrough nausea, vomiting
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Extracted information for OLANZapine only.
CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, geriatric patients, hypertension, cardiac/ renal/hepatic disease, diabetes, agranu- locytosis, abrupt discontinuation, Asian patients, closed-angle glaucoma, coma, leukopenia, QT prolongation, tar- dive dyskinesia, torsades de pointes, sui- cidal ideation, stroke history, TIA
Source page 975
Black Box Warning: Increased mortality in elderly patients with dementia-related psychosis, postinjection delirium/seda- tion syndrome Black Box Warning: Available only through restricted distribution program (Zyprexa Relprevv Patient Care Program, 877-772-9390) due to postinjection de- lirium/sedation syndrome; given at a facil- ity with emergency services; continuous observation; monitor for 3 hr after injection • Use gloves to prepare; irritating to skin • Use deep IM gluteal inj only • Use only diluent provided in kit; give q2-4wk using 19-G, 1.5-inch needle in kit; for obese patients, use 19-G, 2-inch or larger needle Black Box Warning: Increase: respiratory depression—opioids Decrease: OLANZapine levels—CYP1A2 inducers: carBAMazepine, omeprazole, rifAMPin Decrease: antiparkinson activity— levodopa, bromocriptine, other DOPa- mine agonists Drug/Lab Test Increase: LFTs, prolactin, CPK Drug/Herb Increase: toxicity—kava Decrease: olanzapine effect—St. John’s wort; avoid concurrent use Black Box Warning: Postinjection de- lirium/sedation syndrome (ZyPREXA Relprevv): monitor continuously for ≥3 hr after injection; patient must be accom- panied when leaving: assess for seda- tion, coma, delirium, EPS, slurred speech, altered gait, aggression, dizziness, weak- ness, hypertension, seizures; before leav- ing, confirm that patient is alert, oriented, and free of any other symptoms • Mental status: assess orientation, af- fect, LOC, reflexes, coordination, sleep pattern disturbances, mood, behavior, presence of hallucinations and type be- fore initial administration, monthly; EPS, including akathisia (inability to sit still, no pattern to movements), tardive dyski- nesia (bizarre movements of jaw, mouth, tongue, extremities), pseudoparkinson- ism (rigidity, tremors, pill rolling, shuf- fling gait), suicidal thoughts, behaviors • Renal status: I&O ratio; palpate blad- der if low urinary output occurs; urinary retention may be cause, especially in geri- atric patients; urinalysis recommended before, during prolonged therapy • Bilirubin, CBC, LFTs • B/P sitting, standing, lying: take pulse, respirations during initial treatment; establish baseline before starting treat- ment; report drops of 30 mm Hg; obtain baseline ECG • Dizziness, faintness, palpitations, tachycardia on rising Black Box Warning: Geriatric patients O for serious reactions: fatal pneumonia, heart failure, stroke leading to death (IM); do not use in dementia-related psychosis • Neuroleptic malignant syndrome: hy- perpyrexia, muscle rigidity, increased CPK, altered mental status, acute dystonia (cheek chewing, swallowing, eyes, pill rolling), stop drug immediately • EPS: May occur after long-term use • Hyperthermia: Monitor for excessive heat, worse with exercising • Constipation, urinary retention daily; increase bulk, water in diet • Weight gain, hyperglycemia, metabolic changes in diabetic patients • Supervised ambulation until patient stabilized on medication; do not involve patient in strenuous exercise program because fainting is possible; patient should not stand still for long periods • Hyperglycemia: increased in diabetic patient, monitor FBS baseline and peri- odically • Metabolic syndrome: large weight gain, increased B/P, FBS, cholesterol, and triglycerides, BMI • DRESS: may be fatal; fever, hepatitis, cutaneous reactions, eosinophilia, nephri- tis, pneumonia, myocarditis, discontinue immediately • Beers: avoid in older adults except for schizophrenia, bipolar disorder, or short-term use as an antiemetic during chemotherapy; increased risk of stroke • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may cause EPS in infant if used in 3rd trimester; those pregnant should enroll women in the National Pregnancy Registry for Atypi- cal Antipsychotics, 1-866-961-2388; ex- creted in breast milk, avoid breastfeeding Black Box Warning: About postinjection delirium/sedation syndrome: all symp- toms, not to drive or engage in hazardous activities after injection on that day • To use good oral hygiene; frequent rinsing of mouth; sugarless gum, hard candy, ice chips for dry mouth • To avoid hazardous activities until product response is determined • That orthostatic hypotension occurs often; to rise from sitting or lying position gradually • To avoid hot tubs, hot showers, tub baths because hypotension may occur • To avoid abrupt withdrawal of this product because EPS may result; product should be withdrawn slowly • To avoid OTC preparations (cough, hay fever, cold) unless approved by pre- scriber because serious product interac- tions may occur; to avoid use with alco- hol, CNS depressants, opioids because increased drowsiness may occur • Suicidal thoughts, behaviors: report immediately suicidal thoughts/behaviors • That in hot weather, heat stroke may occur; to take extra precautions to stay cool • To take PO without regard to food, how to use ODT • To notify prescriber if pregnancy is planned or suspected; not to breastfeed
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SIDE EFFECTS CNS: EPS (pseudoparkinsonism, akathi- sia, dystonia, tardive dyskinesia), seizures, headache, neuroleptic malignant syn- drome (rare), agitation, nervousness, hos- tility, dizziness, hypertonia, tremor, euphoria, confusion, drowsiness, fatigue, abnormal gait, insomnia, fever, suicidal thoughts CV: Hypotension, tachycardia, chest pain, heart failure, sudden death (geriat- ric patients, IM), orthostatic hypotension, peripheral edema ENDO: Increased prolactin levels, hypo/ hyperglycemia GI: Dry mouth, nausea, vomiting, appe- tite, dyspepsia, anorexia, constipation, abdominal pain, weight gain, jaundice, hepatitis GU: Urinary retention, urinary frequency, enuresis, impotence, amenorrhea, gyne- comastia, breast engorgement, premen- strual syndrome HEMA: Neutropenia, agranulocytosis, leukopenia INTEG: Rash MISC: Peripheral edema, accidental injury, hypertonia, hyperlipidemia MS: Joint pain, twitching RESP: Cough, pharyngitis; fatal pneu- monia (geriatric patients, IM)
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INTERACTIONS Increase: sedation—other CNS depressants, alcohol, barbiturate anesthetics, antihista- mines, sedatives/hypnotics, antidepressants Increase: OLANZapine levels—CYP1A2 inhibitors (fluvoxaMINE) Increase: hypotension—antihyperten- sives, alcohol, diazePAM Increase: anticholinergic effects— anticholinergics
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TREATMENT OF OVERDOSE: Lavage if orally ingested; provide airway; do not induce vomiting or use EPINEPHrine HIGH ALERT
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Extracted information for OLANZapine only.
DOSAGE AND ROUTES Schizophrenia • Adult: PO 5-10 mg/day initially, may increase dosage by 5 mg at ≥1 wk intervals, max 20 mg/day; ORALLY DIS- INTEGRATING tabs: daily, open blister pack, place tab on tongue, let disintegrate, swallow; ext rel inj (Zyprexa Relprevv) IM 150-300 mg q2wk or 405 mg q4wk • Geriatric/debilitated: PO 5 mg/day, may increase cautiously at 1-wk intervals, max 20 mg/day • Adolescent: PO 2.5 or 5 mg/day, tar- get 10 mg/day, max 20 mg Acute mania or mixed episodes as- sociated with bipolar I disorder • Adult: PO 10-15 mg/day, may increase dose after >24 hr by 5 mg, max 20 mg/day • Adolescent: PO 2.5 or 5 mg/day, target 10 mg/day, max 20 mg/day Acute agitation associated with schizophrenia, bipolar I mania • Adult: IM (reg rel) 10 mg once • Geriatric: IM (reg rel) 2.5-5 mg once Chemotherapy nausea/vomiting prophylaxis (unlabeled) • Adult: 10 mg on day of chemotherapy, then 10 mg on day 2 ,3, 4 with dexa- methasone and palonosetron day 1; breakthrough nausea/vomiting 10 mg daily × 3 days
Source pages 975, 976
Available forms: Tab 2.5, 5, 7.5, 10, 15, 20 mg; orally disintegrating tabs 5, 10, 15, 20 mg (ZyPREXA Zydis); powder for inj 10 mg; ext rel powder for susp for inj 210, 300, 405 mg base/vial (ZyPREXA Relprevv)
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Administer: • Decreased dose in geriatric patients PO route • With full glass of water, milk, food to decrease GI upset, may give without re- gard to food • Store in tight, light-resistant container • Orally disintegrating tabs: open blis- ter pack; place tab on tongue until dis- solved; swallow; no water needed; do not break, crush, chew • Keep recumbent if dizziness occurs IM route (ZyPREXA intramuscular) • Inspect for particulate, discoloration before use; if present, do not use • Dissolve contents of vials with 2.1 mL sterile water for inj (5 mg/mL); use im- mediately • Do not use IV or subcut • Inject slowly, deep into muscle mass • Keep recumbent if dizziness occurs IM route (ZyPREXA Relprevv)
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Extracted information for OLANZapine only.
Assess:
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Evaluate: • Therapeutic response: decrease in emotional excitement, hallucinations, de- lusion, paranoia, reorganization of pat- terns of thought, speech
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CLINICAL CONSIDERATIONS
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Patient and caregiver information:
Source page 978
Extracted information for OLANZapine only.
PHARMACOKINETICS Well absorbed (60%), metabolized by liver, glucuronidation/oxidation by CYP1A2 and CYP2D6; excreted in urine (57%), feces (30%); 93% bound to plasma proteins; half-life 21-54 hr, extended in geriatric patients; clearance decreased in women, increased in smok- ers, peak PO 6 hr, IM 15-45 min, IM ext rel 7 days
Source page 977
Filter the extracted dose blocks for this individual drug.
Schizophrenia
• Adolescent: PO 2.5 or 5 mg/day, tar- get 10 mg/day, max 20 mg Acute mania or mixed episodes as- sociated with bipolar I disorder
Candidate age grouping · source pages 975, 976
Schizophrenia
• Adolescent: PO 2.5 or 5 mg/day, target 10 mg/day, max 20 mg/day Acute agitation associated with schizophrenia, bipolar I mania
Candidate age grouping · source pages 975, 976