Drug name
Last update: Jul 2026Risperidone
Developer(s)
Drug information
Risperidone
RISPERDAL CONSTA®, PERSERIS®, RYKINDO®, UZEDY®
Small molecule
Not provided
Risperidone LAI is an atypical antipsychotic indicated for schizophrenia and maintenance treatment of Bipolar I Disorder. It acts via dopamine D₂ and serotonin 5-HT₂ receptor antagonism. The apparent half-life for risperidone + hydroxyrisperidone is 3–6 days, and clearance is 13.7 L/h (in extensive metabolisers) and 3.3 L/h (in poor metabolisers). Following intramuscular injection, risperidone is released gradually, with therapeutic levels sustained for up to 6 weeks. It is metabolised hepatically via CYP2D6 to active 9-hydroxyrisperidone. Common adverse effects include extrapyramidal symptoms, weight gain, and hyperprolactinemia. Clinical trials demonstrate efficacy in reducing relapse rates in schizophrenia and bipolar disorder, with a favourable safety profile under monitored use.
Risperidone microsphere LAI formulation is approved in 54 countries including Canada, United States, European Union countries, UAE, Switzerland, Brazil, Chile, China, Russia, Hong Kong, Malaysia, India, New Zealand, Australia, Israel, Philippines, Saudi Arabia, South Africa, Taiwan, Thailand, the United Kingdom, South Korea, Turkey, Japan, United Arab Emirates, Argentina and Mexico.
Risperdal Consta (12.5 mg, 25 mg, 37.5 mg, and 50 mg) has received marketing authorization from multiple regulatory agencies, including Health Canada, the U.S. FDA, and authorities such as DOH, Swissmedic, ANVISA, ISP, NMPA, MINZDRAV, NPRA, CDSCO, MedSafe, TGA, MOH, FDA Philippines, SFDA, SAHPRA, TFDA, THAI FDA, MHRA, MFDS, TMMDA, PMDA, MOHAP, ANMAT, and COFEPRIS. In addition, approvals have been granted by European national agencies such as CBG, AGES, FAMHP, ANMDMR, SUKL (Czechia), SUKL (Slovakia), DMA, IMA, FIMEA, ANSM, BFARM, EOF, NNGYK, and HPRA. Other European authorities have also provided authorization. However, the European Medicines Agency (EMA) has issued only a positive opinion following a referral from BFARM (Germany), rather than granting centralized approval.
Therapeutic area(s)
- Mental Health Disorders (incl. schizophrenia, bipolar disorders, Schiz. Aff. Dis.) : "incl. schizophrenia"
- Treatment
Administration route
Oral, Subcutaneous, Intramuscular
Associated long-acting platforms
Polymer-based particles, Microspheres
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
- Administered by a community health worker
- Every 2 weeks
Dosage
12.5 mg; 25 mg; 37.5 mg; 50 mg powder for injection
50 mg IM every 2 weeks
1. Initial Treatment Dose for Schizophrenia & Bipolar: • Administer 25 mg intramuscularly (IM) every 2 weeks. 2. Dose Adjustment for Non-Responders: • If inadequate response at 25 mg, consider increasing to 37.5 mg or 50 mg IM every 2 weeks. • Do not exceed 50 mg every 2 weeks. 3. Special Populations (Renal or Hepatic Impairment): • Initiate treatment at a reduced dose of 12.5 mg IM every 2 weeks. 4. Previously Treated Patients: • Previous antipsychotics should be continued for 3 weeks after the first injection of risperidone LAI to ensure that therapeutic concentrations are maintained until the main release phase of risperidone from the injection site has begun
Risperidone LAI must be reconstituted only in the diluent supplied in the dose pack and must be administered with only the appropriate needle supplied in the dose pack for gluteal (2-inch needle) or deltoid (1-inch needle) administration. All components are required for administration. Do not substitute any components of the dose pack. To ensure that the intended dose of risperidone is delivered, the full contents from the vial must be administered. Administration of partial contents may not deliver the intended dose of risperidone.
Associated compounds, formulations and regimens
Not provided
Associated technologies
CompareLYNX
In-situ Microimplants
Additional information
Developer(s)
J&J / Janssen
Janssen Pharmaceuticals is a subsidiary company of Johnson & Johnson headquartered in Beerse, Belgium. They focus on manufacturing and developing pharmaceutical products for use in areas such as, Immunology, Infectious Diseases & Vaccines, Pulmonary Hypertension, Cardiovascular & Metabolism, Oncology, and Neuroscience.
Alkermes
Alkermes, Inc. is the U.S. R&D and manufacturing arm of Alkermes plc, a fully integrated, global biopharmaceutical company. The company focuses on developing innovative medicines for serious psychiatric and neurological disorders.
Drug structure
Scale-up and manufacturing prospects
Not provided
Static Mixer: Cole Parmer L04667-14. Gear Pumps: Cole Parmer L07149-04, L07002-16. Quench Tank: 55 L capacity. Sieves: 25 µm and 180 µm stainless steel mesh. Lyophilizer: Pilot-scale, ramped cycle (max 30°C, 50 h). Gamma Irradiator: Co-60 source.
Risperidone microspheres are synthesized by dissolving PLGA (75:25 lactide:glycolide) in ethyl acetate and benzyl alcohol, then adding risperidone base. This organic phase is emulsified with an aqueous phase containing 1% polyvinyl alcohol using a static mixer. The emulsion is quenched in chilled water with buffer, stirred for solvent removal, sieved (25–180 µm), washed, and dried. Optional steps include lyophilization and gamma sterilization for stability and sterility, ensuring controlled release for 14–60 days.
1. Laser Diffraction Analyzer 2. Scanning Electron Microscope (SEM) 3. High-Performance Liquid Chromatography (HPLC) 4. UV-Vis Spectrophotometer 5. Gas Chromatography (GC) 6. Differential Scanning Calorimetry (DSC) 7. Thermogravimetric Analysis (TGA)
Excipients & delivery device(s)
Not provided
The list of excipients used is: 1. Polysorbate 20 2. Sodium carboxymethyl cellulose 3. Disodium hydrogen phosphate dihydrate 4. Citric acid anhydrous 5. Sodium chloride 6. Sodium hydroxide 7. Water for injection
Not provided
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
Not provided
Not provided
Not provided
Microparticles
The invention provides a process for the preparation of biodegradable biocompatible microparticles, said process comprising: contacting microparticles comprising a biodegradable biocompatible polymer matrix containing an active (e.g. pharmaceutical or diagnostic) agent and an organic solvent with an aqueous solvent system whereby the content of said organic solvent in said particles is reduced to 2 % or less of the weight of said particles, said solvent system being such as to satisfy at least one of the conditions (a) that it is at an elevated temperature (e.g. from 25 to 40 °C) during at least part of the time that it is in contact with said particles, and (b) that it comprises water and water-miscible solvent for said organic solvent; and recovering said particles from said aqueous solv
WO1997041837A2
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Alkermes Controlled Therapeutics Inc
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Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
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WO1995013814A1
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Janssen Pharmaceutica N.V.
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