Haloperidol decanoate

Across the sites, an average of 15% of inpatients received depot antipsychotic drugs (Sim etal, 2004b). This was most common in Singapore (75%) followed by Taiwan (20%), Japan and China (6%). The depot antipsychotic drugs used were fluphenazine decanoate, flupenthixol decanoate, zuclopenthixol decanoate, haloperidol decanoate, pipothiazine palmitate, and fluphenazine enanthate. 

Intramuscular (IM) Into skeletal muscle. This route is used to deliver depot antipsychotic drugs like fluphenazine and haloperidol decanoate, which are used in the treatment of schizophrenia. 

Depot antipsychotics (e.g., haloperidol decanoate, fluphenazine decanoate, and risperidone long-acting injection) can be used for maintenance therapy of bipolar disorder with noncompliance or treatment resistance. 

For haloperidol decanoate, an esterified formulation in sesame seed oil, a factor of 10 to 15 times the oral daily dose is commonly recommended, rounding up to the nearest 50-mg interval, administered IM in a once-monthly dose with oral haloperidol overlap for 1 month. 

A number of prodrugs in clinical use are esters of fatty acids. For example, haloperidol decanoate is of interest in slow-release preparations. This compound was hydrolyzed by such hydrolases as purified carboxylesterase but was reported to be stable in human blood or plasma and in a variety of rat tissue homogenates [107], The source of this apparent lack of reactivity was competitive binding to blood and tissue proteins. In other words, protein binding sequesters this very lipophilic prodrug and prevents enzymatic hydrolysis, thereby slowing its activation and prolonging its in vivo effects. 

K. Nambu, H. Miyazaki, Y. Nakanishi, Y. Oh-e, Y. Matsunaga, M. Hashimoto, Enzymatic Hydrolysis of Haloperidol Decanoate and Its Inhibition by Proteins , Biochem. Pharmacol. 1987, 36, 1715-1722. 

Haloperidol decanoate (Haldol Decanoate) Antipsychotic Inj 50,100 mg/mL 25-100 mg IM q4 weel long acting. Reduce dose in elderly extrapyramidal symptoms, alpha-blocking effects, high doses may prolong QT interval. 

Psychotic disorder- For the treatment of psychotic disorders (eg, schizophrenia). Haloperidol decanoate is for patients who require prolonged parenteral antipsychotic therapy. 

Haloperidol decanoate injection - Individualize dosage and provide close clinical supervision during initiation and stabilization of therapy. The recommended interval between doses is monthly or every 4 weeks. However, variation in patient response may dictate a need for adjustment of the dosing interval as well as the dose. To determine the minimum effective dose, begin with lower initial doses and adjust the dose upward as needed. 

Initial dosage The initial dose should not exceed 100 mg regardless of previous antipsychotic dose requirements. If the conversion requires more than 100 mg of haloperidol decanoate as an initial dose, administer that dose in 2 injections (maximum of 100 mg initially followed by the balance in 3 to 7 days). 

Among the difficulties in pharmacological treatment is the frequent non-compliance. The biggest determinant of compliance is the quality of a patient s relationship with his doctor. But a further way to handle the issue has involved the development of long acting products (depot neuroleptics), even though their effectiveness in the absolute or compared to oral preparations has not been adequately explored. The most commonly used depot agents are fluphenazine and haloperidol decanoate (see David et al., 2004). 

Quraishi S, David A. Depot haloperidol decanoate for schizophrenia. Cochrane Database Syst Rev 1999. Issue 4. 

T. Sassa, T. Suhara, H. Ikehira, T. Obata, F. Girard, S. Tanada, Y. Okubo, 19F-magnetic resonance spectroscopy and chemical shift imaging for schizophrenic patients using haloperidol decanoate. Psychiatry Clin. Neurosci. 56 (2002) 637-642. 

A high risk of relapse is inherent to schizophrenic psychoses. A relapse is often triggered by emotional stress. It is very important to prevent a relapse by either maintaining low-dose oral medication or by switching to a depot antipsychotic. In some cases, this cannot be avoided. Especially when compliance is a problem, a depot medication may help to keep the patient free of psychotic symptoms. Frequently used depot antipsy-chotics are haloperidol-decanoate, fluphenazine-decanoate, and fluspirilene, which are given in relatively low dosages (see Table 41.4). In EOS, relapse prevention is more important than in adulthood, as the majority of patients have not yet finished school or started a professional career. 

Clinically, haloperidol decanoate has been administered to hundreds of chronic schizophrenic patients in several open studies to determine its efficacy, pharmacokinetics, safety, and adverse effects. The trials ranged from 4 months to 2 years, with dosages ranging from 25 to 500 mg given once every 4 weeks. The results of these studies have consistently shown that depot haloperidol ... 

Kissling et al. (27,9) evaluated both fluphenazine and haloperidol decanoate in a 6-month double-blind study involving 31 schizophrenic patients. These authors found both were equally effective in preventing relapse, with a slight advantage for haloperidol decanoate as reflected by fewer adverse effect-related dropouts and a decreased need for antiparkinsonian medications with this latter agent. Wistedt ( 280) compared fluphenazine decanoate with haloperidol decanoate in a double-blind... 

Fluphenazine decanoate may cause more acute EPS than haloperidol decanoate due to a phenomenon known as dose dumping. Here, a small amount of depot formulation is released into the systemic circulation shortly after an injection. There may be a tendency for haloperidol to be more effective for a subset of schizophrenic symptoms, less depressogenic, and slightly less likely to exacerbate extrapyramidal symptoms. These effects, however, are not large, may not be clinically significant, and are not consistently evident in all studies. 

Zissis NP, Psaras M, Lyketsos G. Haloperidol decanoate, a new long-acting antipsychotic, in chronic schizophrenics double-blind comparison with placebo. Curr Ther Res 1982 31 650-655. 

Nair NPV, Suranyi-Cadotte B, Schwartz G, et al. A clinical trial comparing intramuscular haloperidol decanoate and oral haloperidol in chronic schizophrenic patients efficacy, safety, and dosage equivalence. J Clin Psychopharmacol 1986 6(suppl 1) 30S-37S. 

Deberdt R, Elens P, Berghmans W, et al. Intramuscular haloperidol decanoate for neuroleptic maintenance therapy. Efficacy, dosage schedule and plasma levels. An open multicenter study. 

Reyntjens AJM, Heykants JJP, Woestenborghs RJH, et al. Pharmacokinetics of haloperidol decanoate. A 2-year follow-up. Int Pharmacopsychiatry 1982 17 238-246. 

Gelders YG, Reyntjens AJM, Ash CW, et al. 12-month study of haloperidol decanoate in chronic schizophrenic patients. I nt Pharmacopsychiatry 1982 17 247-254. 

Suy E, Woestenborghs R, Heykants J. Bioavailability and clinical effect of two different concentrations of haloperidol decanoate. Curr Ther Res 1982 31 982-991. 

Youssef HA. A one-year study of haloperidol decanoate in schizophrenic patients. Curr Ther Res 1982 31 976-981. 

Bucci L, Marini S. Haloperidol decanoate in chronic schizophrenic patients. Curr Ther Res 1985 37 1091-1097. 

Kane JM. Dosage strategies with long-acting injectable neuroleptics, including haloperidol decanoate. J Clin Psychopharmacol 1986 6(suppl) 20S-23S. 

Kissling W, Moller HJ, Walter K, et al. Double-blind comparison of haloperidol decanoate and fluphenazine decanoate effectiveness, adverse effects, dosage and serum levels during a six months treatment for relapse prevention. Pharmacopsychiatry 1985 18 240-245. 

Wistedt B, Persson T, Hellbom E. A clinical double-blind comparison between haloperidol decanoate and fluphenazine decanoate. Curr Ther Res 1984 35 804-814. 

Chouinard G, Annable L, Campbell W, et al. A double-blind, controlled clinical trial of haloperidol decanoate and fluphenazine decanoate in the maintenance treatment of schizophrenia. Psychopharmacol Bull 1984 20 108-109. 

Well-tolerated parenteral forms of the high-potency older drugs haloperidol and fluphenazine are available for rapid initiation of treatment as well as for maintenance treatment in noncompliant patients. Since the parenterally administered drugs may have much greater bioavailability than the oral forms, doses should be only a fraction of what might be given orally, and the manufacturer s literature should be consulted. Fluphenazine decanoate and haloperidol decanoate are suitable for long-term parenteral maintenance therapy in patients who cannot or will not take oral medication. 

A 58-year-old schizophrenic woman who had taken haloperidol decanoate 125 mg every 2 weeks had a mildly raised prolactin concentration (505 mIU/1 upper limit of the reference range 450 mlU/hter). Dual X-ray absorptiometry showed osteopenia in her spine and hips. She began taking alendronic acid 5 mg/ day and absorptiometry at 1 year showed that her spine and hip had improved by 7% and 9%, although her prolactin concentrations remained mildly raised. 

Nyberg S, Farde L, Halldin C, Dahl M-L, Bertilsson L. D2 dopamine receptor occupancy during low-dose treatment with haloperidol decanoate. Am J Psychiatry 1995 152 173-178. 

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