HALDOL DECANOATE- haloperidol decanoate injection
Janssen Pharmaceuticals, Inc.
For IM Injection Only
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. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. HALDOL Decanoate is not approved for the treatment of patients with dementia-related psychosis (see WARNINGS).
DESCRIPTION
Haloperidol decanoate is the decanoate ester of the butyrophenone, HALDOL (haloperidol). It has a markedly extended duration of effect. It is available in sesame oil in sterile form for intramuscular (IM) injection. The structural formula of haloperidol decanoate, 4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]-4 piperidinyl decanoate, is:
Chemical Structure
(click image for full-size original)
Haloperidol decanoate is almost insoluble in water (0.01 mg/mL), but is soluble in most organic solvents.
Each mL of HALDOL Decanoate 50 for IM injection contains 50 mg haloperidol (present as haloperidol decanoate 70.52 mg) in a sesame oil vehicle, with 1.2% (w/v) benzyl alcohol as a preservative.
Each mL of HALDOL Decanoate 100 for IM injection contains 100 mg haloperidol (present as haloperidol decanoate 141.04 mg) in a sesame oil vehicle, with 1.2% (w/v) benzyl alcohol as a preservative.
CLINICAL PHARMACOLOGY
HALDOL Decanoate 50 and HALDOL Decanoate 100 are the long-acting forms of HALDOL (haloperidol). The basic effects of haloperidol decanoate are no different from those of HALDOL with the exception of duration of action. Haloperidol blocks the effects of dopamine and increases its turnover rate; however, the precise mechanism of action is unknown.
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 after the third or fourth dose. The relationship between dose of haloperidol decanoate and plasma haloperidol concentration is roughly linear for doses below 450 mg. It should be noted, however, that the pharmacokinetics of haloperidol decanoate following intramuscular injections can be quite variable between subjects.
Haldol Decanoate Indications and Usage
HALDOL Decanoate 50 and HALDOL Decanoate 100 are indicated for the treatment of schizophrenic patients who require prolonged parenteral antipsychotic therapy.
