Haloperidol decanoate

Haloperidol decanoate 50 and Haloperidol decanoate 100 are indicated for the treatment of patients with schizophrenia who require prolonged parenteral antipsychotic therapy.

of haloperidol for the treatment of schizophrenia is unclear. However, its efficacy could be mediated through its activity as an antagonist at central dopamine type 2 receptors. Haloperidol also binds to alpha-1 adrenergic receptors, but with lower affinity, and displays minimal binding to muscarinic cholinergic and histaminergic (H 1 ) receptors. Administration of haloperidol decanoate in sesame oil results in slow and sustained release of haloperidol. The plasma concentrations of haloperidol gradually rise, reaching a peak at about 6 days after the injection, and falling thereafter, with an apparent half-life of about 3 weeks. Steady state plasma concentrations are achieved within 2 to 4 months in patient receiving monthly injections.

Haloperidol decanoate 50 and Haloperidol decanoate 100 should be administered by deep intramuscular injection. A 21 gauge needle is recommended. The maximum volume per injection site should not exceed 3 mL. DO NOT ADMINISTER INTRAVENOUSLY. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Haloperidol decanoate 50 and Haloperidol decanoate 100 are intended for use in schizophrenic patients who require prolonged parenteral antipsychotic therapy. These patients must be previously stabilized on antipsychotic medication before considering a conversion to haloperidol decanoate.

Since the pharmacologic and clinical actions of Haloperidol decanoate 50 and Haloperidol decanoate 100 are attributed to haloperidol as the active medication, Contraindications, Warnings, and additional information are those of haloperidol, modified only to reflect the prolonged action. Haloperidol is contraindicated in patients with: Severe toxic central nervous system depression or comatose states from any cause. Hypersensitivity to this drug – hypersensitivity reactions have included anaphylactic reaction and angioedema. Parkinson's disease. Dementia with Lewy bodies.

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. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. 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. Haloperidol decanoate is not approved for the treatment of patients with dementia-related psychosis. Cardiovascular Effects Cases of sudden death, QTc interval-prolongation, and Torsades de Pointes have been reported in patients receiving haloperidol.

The following adverse reactions are discussed in more detail in other sections of the labeling: WARNINGS, Increased mortality in Elderly Patients with Dementia-Related Psychosis WARNINGS, Cardiovascular Effects WARNINGS, Tardive Dyskinesia WARNINGS, Neuroleptic Malignant Syndrome WARNINGS, Hypersensitivity Reactions WARNINGS, Falls WARNINGS, Combined Use of Haloperidol and Lithium WARNINGS, General PRECAUTIONS, Leukopenia, Neutropenia, and Agranulocytosis PRECAUTIONS, Other PRECAUTIONS, Usage in Pregnancy Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug, and may not reflect the rates observed in practice.

Drug-drug interactions can be pharmacodynamic (combined pharmacologic effects) or pharmacokinetic (alteration of plasma levels). The risks of using haloperidol in combination with other drugs have been evaluated as described below. Pharmacodynamic Interactions Since QTc interval-prolongation has been observed during haloperidol treatment, caution is advised when prescribing to a patient with QT-prolongation conditions or to patients receiving medications known to prolong the QTc-interval. Examples include (but are not limited to): Class 1A antiarrhythmics (e.g., procainamide, quinidine, disopyramide), Class 3 antiarrhythmics (e.g., amiodarone, sotalol), and other drugs such as citalopram, erythromycin, levofloxacin, methadone, and ziprasidone.

Store at controlled room temperature (15°–30° C, 59°–86° F). Do not refrigerate or freeze. Protect from light.