SECUADO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SECUADO (SECUADO).
SECUADO (asenapine) is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors, as well as dopamine D2, D3, and D4 receptors. It also exhibits moderate affinity for histamine H1 and alpha2-adrenergic receptors, and low affinity for alpha1 and muscarinic receptors. The therapeutic effect in schizophrenia and bipolar disorder is primarily mediated through antagonism at D2 and 5-HT2A receptors.
| Metabolism | Asenapine is primarily metabolized by direct glucuronidation via UGT1A4 and oxidative metabolism via CYP1A2. Minor contributions from CYP2D6 and CYP3A4. The major metabolite is asenapine N-glucuronide. |
| Excretion | Primarily renal: 50-80% as unchanged drug; biliary/fecal: <15%. |
| Half-life | Terminal elimination half-life: 20-24 hours; steady-state achieved within 5 days. |
| Protein binding | Approximately 94-97% bound to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 7 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Transdermal: approximately 80% relative to subcutaneous administration. |
| Onset of Action | Transdermal: 4-6 hours for detectable plasma levels; clinical antipsychotic effect within 1-2 weeks. |
| Duration of Action | Once-daily application; clinical effect maintained over 24 hours; apply every 24 hours. |
Adults: 3.8 mg/24 hours applied transdermally once daily; initially 3.8 mg/24 hours, may titrate to 5.7 mg/24 hours, 7.6 mg/24 hours, or 11.4 mg/24 hours based on tolerability and efficacy. Maximum dose: 11.4 mg/24 hours.
| Dosage form | SYSTEM |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min), use with caution; experience limited and lower maintenance doses may be needed. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). For moderate impairment (Child-Pugh class B), use with caution; maximum dose 7.6 mg/24 hours. For mild impairment (Child-Pugh class A), no dose adjustment needed. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. No specific weight-based guidelines available. |
| Geriatric use | Elderly patients with dementia-related psychosis are at increased risk of death; not approved for this use. In elderly patients without dementia, start at 3.8 mg/24 hours and titrate slowly; monitor for orthostatic hypotension, sedation, and extrapyramidal symptoms. Renal function commonly decreases with age, consider lower maintenance doses. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SECUADO (SECUADO).
| Breastfeeding | Asenapine is excreted in breast milk; M/P ratio unknown. Limited data. Consider developmental and health benefits of breastfeeding alongside mother's need for drug and potential adverse effects on infant. Monitor infant for sedation, poor feeding, and extrapyramidal symptoms. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Limited data, but antipsychotics may increase risk of congenital malformations, particularly cardiac defects. Second and third trimesters: Risk of extrapyramidal symptoms and/or withdrawal symptoms in neonates exposed during the third trimester. No specific data for SECUADO (asenapine transdermal); based on asenapine oral data. |
■ FDA Black Box Warning
WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. SECUADO is not approved for the treatment of patients with dementia-related psychosis.
| Serious Effects |
["Hypersensitivity to asenapine or any components of the transdermal system","Severe hepatic impairment (Child-Pugh C)"]
| Precautions | ["Cerebrovascular adverse events in elderly patients with dementia-related psychosis","Neuroleptic malignant syndrome (NMS)","Tardive dyskinesia","Metabolic changes including hyperglycemia, dyslipidemia, and weight gain","QT prolongation","Leukopenia, neutropenia, and agranulocytosis","Somnolence and sedation","Orthostatic hypotension and syncope","Seizures","Potential for abuse and dependence","Dysphagia","Hyperprolactinemia","Body temperature dysregulation"] |
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| Fetal Monitoring | Monitor maternal weight, glucose, lipids, and prolactin levels. Monitor fetal growth via ultrasound if significant weight gain or metabolic changes. Neonatal monitoring for extrapyramidal symptoms and withdrawal after delivery. |
| Fertility Effects | Asenapine may increase prolactin levels, potentially causing galactorrhea, amenorrhea, and reversible fertility impairment. Clinical significance unknown; monitor for reproductive function changes. |