Names and pronunciation
(zi-praz′ih-dohn) Geodon, Zeldox
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Drug reference
(zi-praz′ih-dohn) Geodon, Zeldox
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Func. class.: Antipsychotic/neuroleptic
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Chem. class.: Benzisoxazole derivative
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ACTION: Unknown; may be mediated through both dopamine type 2 (D2) and serotonin type 2 (5-HT2) antagonism
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USES: Schizophrenia, acute agitation, acute psychosis, bipolar disorder, mania, psychotic depression
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CONTRAINDICATIONS: Breast feeding, hypersensitivity, acute MI, heart failure, QT prolongation, breast feeding, drugs that increase QT interval Precautions: Pregnancy, children, geri atric patients, cardiac/renal/hepatic dis ease, breast cancer, diabetes, seizure dis orders, AV block, CNS depression, abrupt discontinuation, agranulocytosis, ambient temperature increase, suicidal ideation, torsades de pointes, strenuous exercise, diuretics, diarrhea
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Black Box Warning: Increased mortality in geriatric patients with dementia-related psychosis Black Box Warning: Assess geriatric pa- tient with dementia closely; heart failure, sudden death have occurred; this prod- uct is not approved for the treatment of dementia-related psychosis in the elderly • DRESS: Assess for rash, fever, swollen lymph nodes, product should be discon- Z tinued • Steven’s Johnson Syndrome: rash with fever, aches, blisters, swelling of face, discontinue product immediately • Seizures: Seizures in those with sei- zure disorders, provide seizure precau- tions, seizure threshold is lowered • Assess for metabolic syndrome (hy perglycemia, hypertension, increased cholesterol/lipids, increased BMI/ab dominal obesity) • Watch for suicidal thoughts/behaviors • Bilirubin, CBC, LFTs, fasting blood glu cose, cholesterol profile; potassium, magnesium when taken with loop/thia zide diuretics monthly, not to be used with electrolyte abnormalities • B/P standing and lying; also pulse, respirations; take these q4hr during ini tial treatment; establish baseline before starting treatment; report drops of 30 mm Hg; watch for ECG changes; QT prolongation may occur; discontinue product if QTc >500 msec • Dizziness, faintness, palpitations, tachycardia on rising, may be serious dysrthmia • EPS, including akathisia (inability to sit still, no pattern to movements), tar dive dyskinesia (bizarre movements of the jaw, mouth, tongue, extremities), pseudoparkinsonism (rigidity, tremors, pill rolling, shuffling gait) • Neuroleptic malignant syndrome, serotonin syndrome: hyperthermia, in- creased CPK, altered mental status, mus- cle rigidity • Constipation, urinary retention daily; if these occur, increase bulk and water in diet or stool softener • Fall risk assessment, supervised am bulation until patient is stabilized on medication; do not involve patient in strenuous exercise program because fainting is possible; patient should not stand still for a long time • Beers: avoid use in older adults except for schizophrenia, bipolar disorder, or short term as an antiemetic during che motherapy; increased risk of stroke and cognitive decline • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may cause EPS in the neonate, enroll pregnant women in the Atypical Antipsychotic Pregnancy Registry, 1-866-961-2388; avoid breastfeeding, excretion unknown
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SIDE EFFECTS CNS: EPS, pseudoparkinsonism, akathi- sia, dystonia, tardive dyskinesia; drowsi- ness, insomnia, agitation, anxiety, head- ache, seizures, neuroleptic malignant syndrome, dizziness, tremors, facial droop CV: Orthostatic hypotension, tachycardia, prolonged QT/QTc, hypertension, sudden death, heart failure (geriatric patients), tor- sades de pointes HEMA: Agranulocytosis EENT: Blurred vision, diplopia ENDO: Hypoglycemia GI: Nausea, vomiting, anorexia, consti- pation, jaundice, weight gain, diarrhea, dry mouth, abdominal pain GU: Priapism INTEG: Rash, injection-site pain, sweating, DRESS, Steven’s Johnson Syndrome photosensitivity RESP: Infection, cough
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INTERACTIONS Increase: respiratory depression-opioids, avoid concurrent use Increase: Ziprasidone level-CYP3A4 in- hibitors (Ketoconazole, itraconazole); dose may need to be reduced Increase: QT prolongation—class IA/III antidysrhythmics, some phenothiazines, β-agonists, local anesthetics, tricyclics, haloperidol, methadone, chloroquine, clarithromycin, droperidol, erythromycin, pentamidine, moxifloxacin Increase: sedation—other CNS depres sants, alcohol Increase: hypotension—antihypertensives, monitor B/P Increase: serotonin syndrome, neuroleptic malignant syndrome—SSRIs, SNRIs Decrease: ziprasidone effect—carba- mazepine, may need ziprasidone dose increased Drug/Lab Increase: lipids, glucose Decrease: WBCs
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TREATMENT OF OVERDOSE: Lavage if orally ingested; provide airway; do not induce vomiting HIGH ALERT
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DOSAGE AND ROUTES Schizophrenia • Adult: PO 20 mg bid with food, ad just dosage every 2 days upward to max of 80 mg bid; IM 10-20 mg; may give 10 mg q2hr; doses of 20 mg may be given q4hr; max 40 mg/day (acute epi sodes) Acute mania/mixed episodes bipolar disorder • Adult: PO 20-40 mg bid with food; in crease ≥q2days as needed maintenance as adjunct to lithium/valproate 40-80 mg bid
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Available forms: Caps 20, 40, 60, 80 mg; inj 20 mg/mL (after reconstituting) single-dose vials
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Administer: PO route • Take cap whole and with food, with plenty of fluid at same time of day • Reduced dose in geriatric patients • Anticholinergic agent to be used for EPS • Store in tight, light-resistant container IM route • Add 1.2 mL sterile water for inj to vial; shake vigorously until dissolved; do not admix; give only IM; give deeply in large muscle; do not use if particulates are pres ent, keep patient recumbent for 30 min af ter injection • Do not give over 3 consecutive days, switch to PO as soon as possible • Store injection at room temperature, protect from light, after reconstituting may be stored at room temperature × 24 hr, 7 days refrigerated
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Assess: • Mental status before initial administra tion, AIMS assessment
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Evaluate: • Therapeutic response: decrease in emotional excitement, hallucinations, de lusions, paranoia; reorganization of pat terns of thought, speech
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That orthostatic hypotension may occur; to rise from sitting or lying position gradually • To avoid hot tubs, hot showers, tub baths because hypotension may occur • To avoid tanning beds, excessive sun light, photosensitivity may occur • To avoid abrupt withdrawal of product because EPS may result; that product should be withdrawn slowly • To avoid OTC preparations (cough, hay fever, cold), herbals, supplements unless approved by prescriber because serious product interactions may occur; to avoid use with alcohol because increased drowsiness may occur • To avoid hazardous activities if drowsy or dizzy • To report impaired vision, tremors, muscle twitching, diarrhea • That results may take up to 6 wk • To notify prescriber if pregnancy is planned or suspected or if breastfeeding • To report immediately mouth sores, rash, swollen face/mouth/eyes, swollen lymph nodes • To take with food; not to break, crush, or chew capsules • Not to use opioids with benzodiaze pines, other CNS depressants; to seek emergency services for dizziness, severe sleepiness, change in breathing • That continuing follow-up exams will be needed • In hot weather, that heat stroke may occur; to take extra precautions to stay cool, take adequate liquids
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PHARMACOKINETICS IM: Peak 60 min PO: Peak 6-8 hr, extensively metabolized by liver to major active metabolite, plasma protein binding 99%, half-life 7 hr
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• Adult: PO 20 mg bid with food, ad just dosage every 2 days upward to max of 80 mg bid; IM 10-20 mg; may give 10 mg q2hr; doses of 20 mg may be given q4hr; max 40 mg/day (acute epi sodes) Acute mania/mixed episodes bipolar disorder
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• Adult: PO 20-40 mg bid with food; in crease ≥q2days as needed maintenance as adjunct to lithium/valproate 40-80 mg bid
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