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Long-Acting Antipsychotic Injections Depot Antipsychotic injections Active Ingredient Brand name Peak levels Duration of action Steady state Flupentixol dec. Depixol® 7-10 days 3-4 weeks 10-12 weeks Fluphenazine dec. Modecate® 6-48 hours 1-3 weeks 6-12 weeks Haloperidol dec. Haldol® 3-9 days 6 weeks 10-12 weeks Pipothiazine palmit. Piportil® 9-10 days 4-6 weeks 8-12 weeks Zuclopenthixol dec. Clopixol® 4-9 days 2-4 weeks 10-12 weeks Test Doses •Depot antipsychotic injections are long acting injections so side-effects are likely to be long lived •Test with low initial dose to assess likely side-effects and tolerability to the oil used to formulate the injection. •Write test dose in the right place of chart…. •Depot injections are rarely associated with anaphylaxis, but it is recommended that the first and second doses are given in a clinic where adrenaline is available. Maintenance Doses •Start with low doses •Use lowest effective dose •Use longest possible recommended interval to reduce the number of potentially painful injections •As it takes longer for depot injections to reach steady state blood levels, allow sufficient time to elapse before changing doses How Is Risperdal Consta ® Different to Other Depots? •Encapsulated micro-spheres. •The drug is not stable in the solution. •Dose can not be assured if part vials are administered. •Administer only full vials. •Long Teflon® coated needle to ensure IM administration. •It requires refrigeration. If out of fridge for 20 min shelf life is reduced to 7 days. •Allow to warm to room temperature 20 min prior to injection. •Can be administered into the deltoid site Paliperidone – potential benefits & convenience •No cold chain •Reduced wastage •Prefilled syringe •No reconstitution •Monthly injection •Frees up valuable nursing resource •Patient preference? •No need for oral supplementation •More acceptable for patients? •No post-injection monitoring Paliperidone – dosing & indication • Broad dose range • 50, 75, 100, 150 mg (~ 25, 37.5, 50, 75 mg Risperidone LAI) • Small volume of injection • 0.5, 0.75, 1.0, 1.5 mL • Deltoid and gluteal administration • Deltoid quicker steady state (see later) • Greater patient choice • “Normalisation” of injection process Paliperidone – efficacy, safety & tolerability • Tmax 13 days • gradual increase in plasma levels • Half-life 25-49 days (dose dependant) • No sudden drop-off in plasma levels • Aqueous injection • Less risk of hypersensitivity, nodules, pain? • Early onset of action • Efficacy seen from Day 8 • Limited hepatic metabolism • Low risk of CYP450 drug-drug interactions Paliperidone – Deltoid vs Gluteal profile Deltoid administration – higher Cmax and AUCτ, but similar tmax and AUC∞ 1. Xeplion® EU SmPC; 2. Cleton et al. Poster no. PI-75 presented at ASCPT: Orlando, April 2–5, 2008 INITIATION REGIMEN Day 1 150 mg eq. Deltoid Day 8 +/- 2 days 100 mg eq. Deltoid MAINTENANCE REGIMEN (1 month after 2nd initiation dose) 1 month later +/- 7 days 1 month later +/- 7 days 75 mg eq. (recommended*) 75 mg eq. (recommended*) Deltoid/gluteal† Deltoid/gluteal† Dose range** Dose range** 25–150 mg eq. Deltoid/gluteal† 25–150 mg eq. Deltoid/gluteal† *Recommended monthly dose **Some patients may benefit from lower or higher doses based on individual patient tolerability and/or efficacy. Patients who are overweight or obese may require doses in the upper range †A switch from gluteal to deltoid (and vice versa) should be considered in the event of injection site pain (if discomfort is not well tolerated).It is also recommended to alternate between Xeplion® EU SmPC; Gopal et al. Curr Med Res Opin 2010;26:377–387 left and right sides Xeplion®: Product summary Risperdal Consta Xeplion® 2 weekly injection Monthly injection Requires cold storage No cold chain 3 weeks delay Fast Onset Oral Supplementation No oral Supplementation 3 available doses 4 available doses 19 Steps to Inject Inject and go