Names and pronunciation
(a-sen′a-peen) Saphris, Secuado
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Drug reference
(a-sen′a-peen) Saphris, Secuado
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Func. class.: Antipsychotic, atypical; DOPamine-serotonin antagonist
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Chem. class.: Dibenzapine
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ACTION: Unknown; may be mediated through both DOPamine type 2 (D2) and serotonin type 2 (5-HT2A) antagonism
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USES: Bipolar 1 disorder, schizophrenia
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CONTRAINDICATIONS: Breast- feeding, hypersensitivity Precautions: Pregnancy, children, geri- atric patients, cardiac/renal/hepatic dis- ease, breast cancer, Parkinson’s disease, dementia, seizure disorder, CNS depres- sion, agranulocytosis, QT prolongation, torsades de pointes, suicidal ideation, substance abuse, diabetes mellitus
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Black Box Warning: Increased mortality in elderly patients with dementia-related psychosis Black Box Warning: Mental status before initial administration; watch for suicidal thoughts and behaviors; dementia and death may occur among elderly patients • Affect, orientation, LOC, reflexes, gait, coordination, sleep pattern disturbances • B/P standing and lying; also pulse, respi- rations; take these during initial treatment; establish baseline before starting treatment; report drops of 30 mm Hg; watch for ECG changes; QT prolongation may occur • Dizziness, faintness, palpitations, tachycardia on rising • EPS, including akathisia, tardive dys- kinesia (bizarre movements of the jaw, mouth, tongue, extremities), pseudopar- kinsonism (rigidity, tremors, pill rolling, shuffling gait) • Neuroleptic malignant syndrome: hyperthermia, increased CPK, altered mental status, muscle rigidity • Weight, thyroid function studies, serum prolactin, lipid profile, serum electrolytes, creatinine, pregnancy test, neurologic function, LFTs, glycosylated hemoglobin A1c, CBC, blood glucose, AIMS assessment baseline and periodically • 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 a long time • Beers: avoid use in older adults; high risk of delirium, CVA, worsening parkinso- nian symptoms, increased CNS effects; may use in schizophrenia, bipolar disor- der, or as antiemetic in chemotherapy Black Box Warning: To report suicidal thoughts/behaviors, dementia immediately • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; identify if pregnancy is planned or suspected; if pregnant, register at National Preg- nancy Registry for Atypical Antipsychotics (866-961-2388)
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SIDE EFFECTS CNS: EPS, pseudoparkinsonism, akathi sia, dystonia, tardive dyskinesia; drows iness, insomnia, agitation, anxiety, headache, seizures, neuroleptic malignant syndrome, dizziness, suicidal ideation CV: Orthostatic hypotension, tachycardia; QT prolongation ENDO: Hyperglycemia GI: Nausea, vomiting, oral hypoesthesia/ paresthesia (SL) HEMA: Agranulocytosis, anemia, leukopenia INTEG: Serious allergic reactions (ana- phylaxis, angioedema)
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INTERACTIONS Increase: sedation—other CNS depres- sants, alcohol Increase: EPS—CYP2D6 inhibitors/sub- strates (SSRIs) Increase: serotonin syndrome—SSRIs Increase: Seizure risk—buPROPion Increase: EPS—other antipsychotics Increase: asenapine excretion— carBAMazepine Increase: QT prolongation—class IA/III antidysrhythmics, some phenothiazines, β-agonists, local anesthetics, tricyclics, haloperidol, methadone, chloroquine, clarithromycin, droperidol, erythromycin, pentamidine; avoid concurrent use Decrease: asenapine action—CYP2D6 inducers (carBAMazepine, barbiturates, phenytoins, rifAMPin) Drug/Herb Increase: CNS depression—kava Increase: EPS—betel palm, kava Drug/Lab Test Increase: prolactin levels, glucose, cho- lesterol, LFTs, lipids, triglycerides Decrease: sodium
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TREATMENT OF OVERDOSE: Lavage if orally ingested; provide airway; do not induce vomiting A HIGH ALERT
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DOSAGE AND ROUTES Schizophrenia • Adult: SL 5 mg bid, may increase to 10 mg bid after 1 wk, max 20 mg/day Acute mania/mixed episodes (bipo- lar 1 disorder, monotherapy) • Adult: SL 10 mg bid, may decrease to 5 mg bid as needed, max 20 mg/day; with lithium or valproate 5 mg bid, may increase to 10 mg bid • Child 10-17 yr: SL 2.5 mg bid, may increase after 3 days to 5 mg bid, then after 3 more days 10 mg bid can be tolerated
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Available forms: SL tablet 2.5, 5, 10 mg; transdermal 3.8 mg/24 hr, 5.7 mg/24 hr, 7.6 mg/24 hr
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Administer: • Anticholinergic agent to be used for EPS • Store in tight, light-resistant container • SL tablet: remove tablet; place tablet under tongue; after it dissolves, swallow; advise patient not to chew, crush, swal- low tablets; not to eat, drink for 10 min Transdermal • Open when ready to use, apply patch to clean, dry skin on hip, upper arm, upper back, abdomen; use for 24 hr
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Assess:
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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 oc- cur; to rise from sitting or lying position gradually • To avoid hot tubs, hot showers, tub baths; hypotension may occur • To avoid abrupt withdrawal of this product; EPS may result; product should be withdrawn slowly • To avoid OTC preparations (cough, hay fever, cold) unless approved by pre- scriber; serious product interactions may occur; to avoid use of alcohol, opioids, increased drowsiness may occur • That weight gain is common • How to take prescribed product • To avoid hazardous activities if drowsy, dizzy • About compliance with product regimen • That heat stroke may occur in hot weather; to take extra precautions to stay cool • To notify provider if history of diabetes in patient or family; if so, blood sugar should be checked before starting this product
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PHARMACOKINETICS Extensively metabolized by the liver by CYP3A4/UGTA14, protein binding 95%, peak 0.5-1.5 hr, half-life 24 hr, excreted urine 50%, feces 40% (metabolites)
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• Adult: SL 5 mg bid, may increase to 10 mg bid after 1 wk, max 20 mg/day Acute mania/mixed episodes (bipo- lar 1 disorder, monotherapy)
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• Adult: SL 10 mg bid, may decrease to 5 mg bid as needed, max 20 mg/day; with lithium or valproate 5 mg bid, may increase to 10 mg bid
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• Child 10-17 yr: SL 2.5 mg bid, may increase after 3 days to 5 mg bid, then after 3 more days 10 mg bid can be tolerated
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