HaloperidolHaloperidol is an antipsychotic medication that is available as an oral preparation as well as intravenous and intramuscular injections. The free action is only 7. The main mode of hepatic clearance is through glucuronidation, reduction fefect oxidation mediated by CYP3A4. Excretion is biliary, meaning the drug leaves the body in the haldol im peak effect and urine. The half-life is between 14 and 26 hours for intravenous preparations, 21 hours for intramuscular preparations and between 14 and hqldol hours for oral preparations. One injectable preparation is the long-acting decanoate ester which is used to treat schizophrenia and related conditions in patients who have had difficulty adhering to other medication plans. This can happen if patients have a winstrol depot orally understanding hsldol their illness or because they forget to take their tablets.
Geriatric patients with dementia-related psychosis treated with antipsychotic agents are at an increased risk of death. Analyses of 17 placebo-controlled trials in geriatric patients mainly receiving atypical antipsychotic agents revealed an approximate 1. Most fatalities appeared to result from cardiovascular-related events e. Observational studies suggest that conventional or first-generation antipsychotic agents also may increase mortality in such patients.
Antipsychotic agents, including haloperidol, are not approved for the treatment of dementia-related psychosis. Butyrophenone derivative; a b c d e conventional prototypical, first-generation antipsychotic agent. Antipsychotic agents are used for all phases of schizophrenia, including acute psychotic episodes as well for long-term stabilization and to minimize risk of relapse.
Patients who do not respond to or tolerate one drug may be successfully treated with an agent from a different class or with a different adverse effect profile. APA considers certain atypical second-generation antipsychotic agents first-line for the acute phase of schizophrenia, principally because of the decreased risk of adverse extrapyramidal effects and tardive dyskinesia, with the understanding that the relative advantages, disadvantages, and cost-effectiveness of atypical antipsychotic agents compared with first-generation antipsychotic agents remain controversial.
Conventional antipsychotic agents may be considered first-line in patients with acute psychotic episodes who have been treated successfully in the past with, or who prefer, conventional agents. Long-acting haloperidol decanoate ester used principally for prolonged antipsychotic therapy e. May be used concomitantly with a stimulant for tic disorders e.
Manufacturers recommend reserving for severe behavioral problems or ADHD, only after failure of psychotherapy or drug therapy other than antipsychotics. Avoid skin contact with haloperidol lactate oral solution and injection, since contact dermatitis has occurred rarely. Haloperidol or haloperidol lactate: Administer orally 2 or 3 times daily. Administer by deep IM injection into the gluteal region using a gauge needle, usually at monthly intervals; maximum volume should not exceed 3 mL per IM injection site.
Administer IM at intervals based on patient response; may administer as often as every hour, although 4- to 8-hour intervals may be satisfactory.
IM administration of haloperidol decanoate or lactate in pediatric patients is not recommended by the manufacturers. ECG monitoring is recommended whenever haloperidol is administered IV. Available as the base, decanoate decanoic acid ester , and lactate salt; dosage is expressed in terms of haloperidol.
There is considerable interindividual variation in optimum dosage requirements; carefully adjust dosage according to individual requirements and response, using the lowest possible effective dosage. Children 3—12 years of age weighing 15—40 kg: Severely disturbed psychotic children may require higher initial dosages.
During prolonged maintenance therapy, keep dosage at the lowest possible effective level; once an adequate response has been achieved, gradually reduce dosage and make subsequent adjustments according to patient response and tolerance. Once an adequate response is achieved, gradually reduce dosage and make subsequent adjustments according to patient response and tolerance. Nonpsychotic or hyperactive behavioral problems in children may be acute, and short-term administration may be adequate.
APA recommends 5—20 mg daily in all patients with schizophrenia. To achieve prompt control, higher initial dosages may be necessary in some patients. Initially, 3—5 mg 2 or 3 times daily. To achieve prompt control, higher initial dosages may be required in some patients. Patients who remain severely disturbed or inadequately controlled may require dosage adjustment.
Clinical experience suggests that higher-dosage regimens i. Initially, manufacturers recommend 3—5 mg 2 or 3 times daily. May consider for patients requiring prolonged antipsychotic therapy e. Patients stabilized on low daily oral dosages up to 10 mg daily , or geriatric or debilitated patients.
Usually, administer at monthly intervals i. Observe closely during dosage titration to minimize risk of overdosage or emergence of psychotic manifestations prior to next dose; if supplemental antipsychotic therapy is necessary during periods of dosage titration or for control of acute exacerbations of psychotic manifestations, use a short-acting haloperidol preparation.
Initially, 2—5 mg as a single dose for prompt control in patients with moderately severe to very severe symptoms. Use total parenteral dosage during preceding 24 hours for initial approximation of total daily oral dosage required; since this dosage is only an initial estimate, closely monitor patients being switched to oral therapy, particularly for efficacy, sedation, and adverse effects, for first several days following initiation of oral therapy.
Increase or decrease subsequent oral dosage according to patient tolerance and therapeutic response, using lowest possible effective dosage. During prolonged maintenance therapy, keep dosage at lowest effective level. Patients who remain inadequately controlled may require dosage adjustment. Dosages up to mg daily may be required in some patients to achieve optimal response.
Optimum dosage not established. Although single IV doses up to 50 mg or total daily dosages of mg have been reported, must consider risk of adverse effects, particularly prolongation of the QT interval and torsades de pointes. Some evidence suggests that risk of torsades de pointes increases at total daily dosages of 35—50 mg or more. In patients requiring multiple IV injections of the drug to control delirium e. Determine ECG at baseline and periodically or continuously thereafter, paying special attention to possible prolongation of the QT interval; reduce dosage or discontinue drug if clinically important QT prolongation e.
In geriatric or debilitated patients, lower dosages may be required than those in younger adults; optimal response is usually obtained with more gradual dosage adjustments.
Severe toxic CNS depression or comatose states from any cause. Increased risk of death with use of either conventional first-generation or atypical second-generation antipsychotics in geriatric patients with dementia-related psychosis.
Antipsychotic agents, including haloperidol, are not FDA labeled for the treatment of dementia-related psychosis. Sudden death, QT-interval prolongation, and torsades de pointes reported in patients receiving haloperidol.
Although these effects have been reported in the absence of predisposing factors, use haloperidol with particular caution in patients with other conditions that prolong the QT interval, including electrolyte imbalance particularly hypokalemia and hypomagnesemia , underlying cardiac abnormalities, hypothyroidism, and familial long QT syndrome, as well as in those concurrently receiving other drugs known to prolong the QT interval.
Tardive dyskinesia, a syndrome of potentially irreversible, involuntary, dyskinetic movements, reported with use of antipsychotic agents, including haloperidol. Reserve long-term antipsychotic treatment for patients with chronic illness known to be responsive to antipsychotic agents, and for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate. APA recommends assessing patients receiving first-generation antipsychotic agents for abnormal involuntary movements every 6 months; for patients at increased risk for tardive dyskinesia, assess every 3 months.
Neuroleptic malignant syndrome NMS , a potentially fatal syndrome characterized by hyperpyrexia, muscle rigidity, altered mental status, and autonomic instability, reported with antipsychotic agents, including haloperidol. Immediately discontinue therapy and initiate supportive and symptomatic therapy if NMS occurs.
Hyperpyrexia and heat stroke not associated with NMS also reported. Cases of limb malformations in offspring of women given haloperidol concurrently with other potentially teratogenic drugs during first trimester of pregnancy reported; causal relationship not established. Use during pregnancy or in women likely to become pregnant only when potential benefits justify possible risks to fetus.
Acute encephalopathic syndrome reported occasionally in patients receiving lithium and an antipsychotic agent concurrently, especially when high serum lithium concentrations were present. Bronchopneumonia, sometimes fatal, reported with use of antipsychotic agents, including haloperidol. Ocular changes reported in patients receiving chemically related drugs, although not reported with haloperidol.
Use with caution in patients with known allergies or with a history of allergic reactions to drugs. Possible risk of seizures; may lower seizure threshold.
Possible impairment of ability to perform activities requiring mental alertness or physical coordination e. Possible additive effects or potentiated action when used with alcohol or other CNS depressants. Extrapyramidal symptoms occur frequently; if concomitant therapy with an antiparkinsonian drug is necessary to manage extrapyramidal symptoms, it may be necessary to continue the antiparkinsonian drug for a period of time after haloperidol discontinuance to prevent emergence of these symptoms.
If used to control mania in patients with bipolar disorder, there may be a rapid mood swing to depression. Possible transient dyskinetic signs after abrupt withdrawal in some patients receiving maintenance therapy; in some cases, dyskinetic movements are indistinguishable from tardive dyskinesia except for duration.
Elevated prolactin concentrations possible; may persist during long-term therapy. Although disturbances such as galactorrhea, amenorrhea, gynecomastia, and impotence have been reported, clinical importance of elevated prolactin concentrations for most patients has not been established. Use with caution in patients with previously diagnosed breast cancer, since in vitro tests indicate that about one-third of such tumors are prolactin dependent.
Decreased serum cholesterol concentrations reported in patients receiving chemically related agents. Leukopenia and neutropenia temporally related to antipsychotic agents, including haloperidol, reported. Possible risk factors for leukopenia and neutropenia include preexisting low WBC count and a history of drug-induced leukopenia or neutropenia. Carefully monitor patients with clinically significant neutropenia for fever or other signs and symptoms of infection and treat promptly if observed.
Safety and efficacy of IM administration of haloperidol decanoate or lactate not established in pediatric patients. Hyperammonemia reported during postmarketing surveillance in a 5. Prevalence of tardive dyskinesia appears to be highest among geriatric patients, particularly geriatric women. Pharmacokinetics of haloperidol in geriatric patients generally warrant use of reduced dosages. Geriatric patients with dementia-related psychosis treated with either conventional or atypical antipsychotic agents are at an increased risk of death.
QT-interval prolongation and torsades de pointes reported; patients receiving higher than recommended dosages of any haloperidol preparation and those receiving the drug IV appear to be at higher risk.
Increases in intraocular pressure may occur in patients receiving anticholinergic drugs, including antiparkinsonian agents, concurrently with haloperidol a b c d e. Antagonism of anticoagulant activity of phenindione no longer commercially available in US reported in 1 patient b c d e. Possible additive effects or potentiated action of other CNS depressants a b c d e. An acute encephalopathic syndrome occasionally has occurred, especially when high serum lithium concentrations were present a b c d e.
Observe patients receiving combined therapy for evidence of adverse neurologic effects; promptly discontinue if such signs or symptoms appear a b d e. Clinical importance of this possible interaction not determined; carefully observe patients for adverse psychiatric symptoms if used concurrently a.
Following discontinuance of rifampin in other schizophrenic patients treated with oral haloperidol, mean haloperidol concentrations increased 3.
Careful monitoring of clinical status and appropriate dosage adjustment warranted whenever rifampin is initiated or discontinued in patients stabilized on haloperidol Well absorbed from GI tract following oral administration, but appears to undergo first-pass metabolism in the liver. Following IM administration of haloperidol lactate, peak plasma haloperidol concentrations occur within 10—20 minutes.
Following IM administration of haloperidol decanoate, plasma haloperidol concentrations are usually evident within 1 day and peak concentrations generally occur within about 6—7 days range: Following IM administration of haloperidol lactate, peak pharmacologic action occurs within 30—45 minutes; in acutely agitated patients, control of psychotic manifestations may become apparent within 30—60 minutes, with substantial improvement often occurring within 2—3 hours.
Esterification of haloperidol results in slow and gradual release of haloperidol decanoate from fatty tissues, thus prolonging duration of action; administration of the ester in a sesame oil vehicle further delays rate of release.