Introduction
Uzedy (risperidone) is a long-acting subcutaneous antipsychotic injection approved by the FDA in 2023 for the treatment of schizophrenia in adults. It utilizes a novel drug delivery technology called SteadyTeq, which provides sustained release of risperidone over extended periods, potentially improving treatment adherence and reducing dosing frequency compared to traditional oral antipsychotics.
Mechanism of Action
Uzedy contains risperidone, an atypical antipsychotic that exerts its therapeutic effects through antagonism of dopamine D₂ and serotonin 5-HT₂A receptors. The SteadyTeq delivery system forms a biodegradable matrix upon subcutaneous injection that gradually releases risperidone over time, maintaining stable plasma concentrations. Additional pharmacological activity includes antagonism of α₁-adrenergic and histamine H₁ receptors.
Indications
- Treatment of schizophrenia in adults
- Maintenance treatment of schizophrenia in patients who require extended therapy
Dosage and Administration
Available strengths: 50 mg, 75 mg, 100 mg, and 125 mg subcutaneous injections Recommended dosing: Administered subcutaneously every once monthly or once every two months based on individual patient needs and response Administration:- Inject subcutaneously in the abdomen or thigh
- Rotate injection sites
- Allow the syringe to reach room temperature for 15 minutes before administration
- Do not massage the injection site
- Renal impairment: Use caution in patients with severe renal impairment
- Hepatic impairment: Use caution in patients with hepatic impairment
- Elderly: Consider lower doses due to increased sensitivity
- Pediatric: Safety and effectiveness not established
Pharmacokinetics
Absorption: Following subcutaneous administration, risperidone is released gradually from the SteadyTeq matrix with peak concentrations achieved within 4-8 days Distribution: Volume of distribution is 1-2 L/kg; 90% protein bound (primarily to albumin and α₁-acid glycoprotein) Metabolism: Extensive hepatic metabolism via CYP2D6 to 9-hydroxyrisperidone (active metabolite) Elimination: Terminal half-life approximately 20 hours (risperidone) and 30 hours (9-hydroxyrisperidone); excreted primarily in urine (70%) and feces (14%)Contraindications
- Hypersensitivity to risperidone or any component of the formulation
- History of neuroleptic malignant syndrome with risperidone
- Concomitant use with strong CYP3A4 inducers (e.g., carbamazepine, rifampin)
Warnings and Precautions
Boxed Warning:- Increased mortality in elderly patients with dementia-related psychosis
- Not approved for dementia-related psychosis
- Cerebrovascular adverse events in elderly patients with dementia
- Neuroleptic malignant syndrome (NMS)
- Tardive dyskinesia
- Metabolic changes (hyperglycemia, dyslipidemia, weight gain)
- Hyperprolactinemia
- Orthostatic hypotension and syncope
- Falls
- Leukopenia, neutropenia, and agranulocytosis
- Seizures
- Cognitive and motor impairment
- Dysphagia
- Priapism
- Body temperature regulation disruption
Drug Interactions
Significant interactions:- Strong CYP3A4 inducers: May decrease risperidone concentrations (contraindicated)
- Strong CYP2D6 inhibitors: May increase risperidone concentrations (reduce dose)
- Centrally-acting drugs: Additive CNS depression with alcohol, benzodiazepines, opioids
- Antihypertensive agents: Enhanced hypotensive effects
- Levodopa and dopamine agonists: May antagonize effects
Adverse Effects
Common (≥5%):- Weight gain
- Somnolence/sedation
- Akathisia
- Parkinsonism
- Headache
- Anxiety
- Nasopharyngitis
- Injection site reactions
- Neuroleptic malignant syndrome
- Tardive dyskinesia
- Metabolic syndrome
- Hyperprolactinemia
- Orthostatic hypotension
- Seizures
- Blood dyscrasias
Monitoring Parameters
- Efficacy: Psychiatric symptoms, CGI scores
- Metabolic: Weight, BMI, blood glucose, lipid profile
- Neurological: EPS symptoms, tardive dyskinesia assessment
- Cardiovascular: Blood pressure (especially orthostatic changes)
- Hematologic: CBC in patients with pre-existing low WBC
- Prolactin: Levels if clinical symptoms suggest hyperprolactinemia
- Injection sites: For reactions or nodules
Patient Education
- Importance of adherence to treatment schedule
- Do not stop treatment abruptly without consulting healthcare provider
- Report any unusual movements, muscle stiffness, or fever immediately
- Monitor for weight gain and maintain healthy lifestyle
- Avoid alcohol during treatment
- Be cautious when driving or operating machinery until response is known
- Rise slowly from sitting/lying position to prevent dizziness
- Report any signs of infection (fever, sore throat)
- Inform all healthcare providers about Uzedy treatment
- Keep appointment for regular monitoring visits
References
1. FDA Approval Package: Uzedy (risperidone) extended-release injectable suspension. 2023. 2. Correll CU, et al. Efficacy and safety of once-monthly risperidone ISM in schizophrenia: A double-blind, randomized, controlled study. J Clin Psychiatry. 2021;82(5):20m13774. 3. Risperidone package insert. Teva Pharmaceuticals. 4. Kane JM, et al. Long-acting injectable antipsychotics: recommendations for clinicians. CNS Spectr. 2020;25(2):170-178. 5. Keepers GA, et al. The American Psychiatric Association Practice Guideline for the Treatment of Patients With Schizophrenia. Am J Psychiatry. 2020;177(9):868-872. 6. Leucht S, et al. Comparative efficacy and tolerability of 32 oral antipsychotics for the acute treatment of adults with multi-episode schizophrenia: a systematic review and network meta-analysis. Lancet. 2019;394(10202):939-951.
Note: This information is intended for educational purposes only and should not replace professional medical advice. Always consult with a qualified healthcare provider for personalized medical guidance.