Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/779
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Haldol Decanoate (Injection)
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dailymed-instance:dosage |
HALDOL Decanoate 50 and HALDOL 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. HALDOL
Decanoate 50 and HALDOL Decanoate 100 are intended for use in schizophrenic
patients who require prolonged parenteral antipsychotic therapy. These patients
should be previously stabilized on antipsychotic medication before considering
a conversion to haloperidol decanoate. Furthermore, it is recommended that
patients being considered for haloperidol decanoate therapy have been treated
with, and tolerate well, short-acting HALDOL (haloperidol) in order to reduce
the possibility of an unexpected adverse sensitivity to haloperidol. Close
clinical supervision is required during the initial period of dose adjustment
in order to minimize the risk of overdosage or reappearance of psychotic symptoms
before the next injection. During dose adjustment or episodes of exacerbation
of symptoms of schizophrenia, haloperidol decanoate therapy can be supplemented
with short-acting forms of haloperidol. The dose of
HALDOL Decanoate 50 or HALDOL Decanoate 100 should be expressed in terms of
its haloperidol content. The starting dose of haloperidol decanoate should
be based on the patient's age, clinical history, physical condition, and response
to previous antipsychotic therapy. The preferred approach to determining the
minimum effective dose is to begin with lower initial doses and to adjust
the dose upward as needed. For patients previously maintained on low doses
of antipsychotics (e.g. up to the equivalent of 10 mg/day oral haloperidol),
it is recommended that the initial dose of haloperidol decanoate be 10���15
times the previous daily dose in oral haloperidol equivalents; limited clinical
experience suggests that lower initial doses may be adequate.<br/>Initial Therapy: Conversion from oral haloperidol to haloperidol decanoate
can be achieved by using an initial dose of haloperidol decanoate that is
10 to 20 times the previous daily dose in oral haloperidol equivalents. In
patients who are elderly, debilitated, or stable on low doses of oral haloperidol
(e.g. up to the equivalent of 10 mg/day oral haloperidol), a range of 10 to
15 times the previous daily dose in oral haloperidol equivalents is appropriate
for initial conversion. In patients previously maintained
on higher doses of antipsychotics for whom a low dose approach risks recurrence
of psychiatric decompensation and in patients whose long-term use of haloperidol
has resulted in a tolerance to the drug, 20 times the previous daily dose
in oral haloperidol equivalents should be considered for initial conversion,
with downward titration on succeeding injections. The
initial dose of haloperidol decanoate should not exceed 100 mg regardless
of previous antipsychotic dose requirements. If, therefore, conversion requires
more than 100 mg of haloperidol decanoate as an initial dose, that dose should
be administered in two injections, i.e. a maximum of 100 mg initially followed
by the balance in 3 to 7 days.<br/>Maintenance Therapy: The maintenance dosage of haloperidol decanoate must be individualized
with titration upward or downward based on therapeutic response. The usual
maintenance range is 10 to 15 times the previous daily dose in oral haloperidol
equivalents dependent on the clinical response of the patient. Close clinical supervision is required during initiation
and stabilization of haloperidol decanoate therapy. Haloperidol decanoate
is usually administered 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 . Clinical
experience with haloperidol decanoate at doses greater than 450 mg per month
has been limited.
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dailymed-instance:descripti... |
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: 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.
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dailymed-instance:clinicalP... |
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.
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dailymed-instance:contraind... |
Since the pharmacologic and clinical actions of HALDOL Decanoate
50 and HALDOL Decanoate 100 are attributed to HALDOL (haloperidol) as the
active medication, CONTRAINDICATIONS, WARNINGS, and additional information
are those of HALDOL, modified only to reflect the prolonged action. HALDOL
is contraindicated in severe toxic central nervous system depression or comatose
states from any cause and in individuals who are hypersensitive to this drug
or have Parkinson's disease.
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dailymed-instance:supply |
HALDOL (haloperidol) Decanoate 50 for IM
injection, 50 mg haloperidol as 70.52 mg per mL haloperidol decanoate���NDC
0045-0253, 10��1 mL ampuls and 3��1 mL ampuls. HALDOL (haloperidol)
Decanoate 100 for IM injection, 100 mg haloperidol as 141.04 mg per mL haloperidol
decanoate���NDC 0045-0254, 5��1 mL ampuls. Store
at controlled room temperature (15�����30��C, 59�����86��F). Do not refrigerate or freeze. Protect from light.
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dailymed-instance:precautio... |
HALDOL Decanoate 50 and HALDOL Decanoate 100 should be administered
cautiously to patients: If concomitant antiparkinson medication is required, it
may have to be continued after HALDOL Decanoate 50 or HALDOL Decanoate 100
is discontinued because of the prolonged action of haloperidol decanoate.
If both drugs are discontinued simultaneously, extrapyramidal symptoms may
occur. The physician should keep in mind the possible increase in intraocular
pressure when anticholinergic drugs, including antiparkinson agents, are administered
concomitantly with haloperidol decanoate. In patients
with thyrotoxicosis who are also receiving antipsychotic medication, including
haloperidol decanoate, severe neurotoxicity (rigidity, inability to walk or
talk) may occur. When HALDOL is used to control mania
in bipolar disorders, there may be a rapid mood swing to depression.<br/>Information for Patients: Haloperidol decanoate may impair the mental and/or physical
abilities required for the performance of hazardous tasks such as operating
machinery or driving a motor vehicle. The ambulatory patient should be warned
accordingly. The use of alcohol with this drug should
be avoided due to possible additive effects and hypotension.<br/>Drug Interactions: An encephalopathic syndrome (characterized by weakness, lethargy,
fever, tremulousness and confusion, extrapyramidal symptoms, leukocytosis,
elevated serum enzymes, BUN, and FBS) followed by irreversible brain damage
has occurred in a few patients treated with lithium plus HALDOL. A causal
relationship between these events and the concomitant administration of lithium
and HALDOL has not been established; however, patients receiving such combined
therapy should be monitored closely for early evidence of neurological toxicity
and treatment discontinued promptly if such signs appear. As
with other antipsychotic agents, it should be noted that HALDOL may be capable
of potentiating CNS depressants such as anesthetics, opiates, and alcohol. In
a study of 12 schizophrenic patients coadministered oral haloperidol and rifampin,
plasma haloperidol levels were decreased by a mean of 70% and mean scores
on the Brief Psychiatric Rating Scale were increased from baseline. In 5 other
schizophrenic patients treated with oral haloperidol and rifampin, discontinuation
of rifampin produced a mean 3.3-fold increase in haloperidol concentrations.
Thus, careful monitoring of clinical status is warranted when rifampin is
administered or discontinued in haloperidol-treated patients.<br/>Carcinogenesis, Mutagenesis, and Impairment
of Fertility: No mutagenic potential of haloperidol decanoate was found
in the Ames Salmonella microsomal activation assay. Negative or inconsistent
positive findings have been obtained in in vitro
and in vivo studies of
effects of short-acting haloperidol on chromosome structure and number. The
available cytogenetic evidence is considered too inconsistent to be conclusive
at this time. Carcinogenicity studies using oral haloperidol
were conducted in Wistar rats (dosed at up to 5 mg/kg daily for 24 months)
and in Albino Swiss mice (dosed at up to 5 mg/kg daily for 18 months). In
the rat study survival was less than optimal in all dose groups, reducing
the number of rats at risk for developing tumors. However, although a relatively
greater number of rats survived to the end of the study in high-dose male
and female groups, these animals did not have a greater incidence of tumors
than control animals. Therefore, although not optimal, this study does suggest
the absence of a haloperidol related increase in the incidence of neoplasia
in rats at doses up to 20 times the usual daily human dose for chronic or
resistant patients. In female mice at 5 and 20 times
the highest initial daily dose for chronic or resistant patients, there was
a statistically significant increase in mammary gland neoplasia and total
tumor incidence; at 20 times the same daily dose there was a statistically
significant increase in pituitary gland neoplasia. In male mice, no statistically
significant differences in incidences of total tumorsor specific tumor types
were noted. Antipsychotic drugs elevate prolactin levels;
the elevation persists during chronic administration. Tissue culture experiments
indicate that approximately one-third of human breast cancers are prolactin
dependent in vitro, a factor of potential
importance if the prescription of these drugs is contemplated in a patient
with a previously detected breast cancer. Although disturbances such as galactorrhea,
amenorrhea, gynecomastia, and impotence have been reported, the clinical significance
of elevated serum prolactin levels is unknown for most patients. An
increase in mammary neoplasms has been found in rodents after chronic administration
of antipsychotic drugs. Neither clinical studies nor epidemiologic studies
conducted to date, however, have shown an association between chronic administration
of these drugs and mammary tumorigenesis; the available evidence is considered
too limited to be conclusive at this time.<br/>Usage in Pregnancy: Pregnancy Category C. Rodents given up to 3 times the usual
maximum human dose of haloperidol decanoate showed an increase in incidence
of resorption, fetal mortality, and pup mortality. No fetal abnormalities
were observed. Cleft palate has been observed in mice
given oral haloperidol at 15 times the usual maximum human dose. Cleft palate
in mice appears to be a nonspecific response to stress or nutritional imbalance
as well as to a variety of drugs, and there is no evidence to relate this
phenomenon to predictable human risk for most of these agents. There
are no adequate and well-controlled studies in pregnant women. There are reports,
however, of cases of limb malformations observed following maternal use of
HALDOL along with other drugs which have suspected teratogenic potential during
the first trimester of pregnancy. Causal relationships were not established
with these cases. Since such experience does not exclude the possibility of
fetal damage due to HALDOL, haloperidol decanoate should be used during pregnancy
or in women likely to become pregnant only if the benefit clearly justifies
a potential risk to the fetus.<br/>Nursing Mothers: Since haloperidol is excreted in human breast milk, infants
should not be nursed during drug treatment with haloperidol decanoate.<br/>Pediatric Use: Safety and effectiveness of haloperidol decanoate in children
have not been established.<br/>Geriatric Use: Clinical studies of haloperidol did not include sufficient
numbers of subjects aged 65 and over to determine whether they respond differently
from younger subjects. Other reported clinical experience has not consistently
identified differences in responses between the elderly and younger patients.
However, the prevalence of tardive dyskinesia appears to be highest among
the elderly, especially elderly women (see WARNINGS,
Tardive dyskinesia). Also, the pharmacokinetics of haloperidol
in geriatric patients generally warrants the use of lower doses .
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dailymed-instance:overdosag... |
While overdosage is less likely to occur with a parenteral
than with an oral medication, information pertaining to HALDOL (haloperidol)
is presented, modified only to reflect the extended duration of action of
haloperidol decanoate.<br/>Manifestations: In general, the symptoms of overdosage would be an exaggeration
of known pharmacologic effects and adverse reactions, the most prominent of
which would be: 1) severe extrapyramidal reactions, 2) hypotension, or 3)
sedation. The patient would appear comatose with respiratory depression and
hypotension which could be severe enough to produce a shock-like state. The
extrapyramidal reactions would be manifested by muscular weakness or rigidity
and a generalized or localized tremor, as demonstrated by the akinetic or
agitans types, respectively. With accidental overdosage, hypertension rather
than hypotension occurred in a two-year old child. The risk of ECG changes
associated with torsade de pointes should be considered. (For
further information regarding torsade de pointes, please refer to ADVERSE REACTIONS.)<br/>Treatment: Since there is no specific antidote, treatment is primarily
supportive. A patent airway must be established by use of an oropharyngeal
airway or endotracheal tube or, in prolonged cases of coma, by tracheostomy.
Respiratory depression may be counteracted by artificial respiration and mechanical
respirators. Hypotension and circulatory collapse may be counteracted by use
of intravenous fluids, plasma, or concentrated albumin, and vasopressor agents
such as metaraminol, phenylephrine and norepinephrine. Epinephrine should
not be used. In case of severe extrapyramidal reactions, antiparkinson medication
should be administered, and should be continued for several weeks, and then
withdrawn gradually as extrapyramidal symptoms may emerge. ECG and vital signs
should be monitored especially for signs of Q-T prolongation or dysrhythmias
and monitoring should continue until the ECG is normal. Severe arrhythmias
should be treated with appropriate anti-arrhythmic measures.
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dailymed-instance:genericMe... |
Haloperidol Decanoate
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dailymed-instance:fullName |
Haldol Decanoate (Injection)
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dailymed-instance:adverseRe... |
Adverse reactions following the administration of HALDOL
Decanoate 50 or HALDOL Decanoate 100 are those of HALDOL (haloperidol). Since
vast experience has accumulated with HALDOL, the adverse reactions are reported
for that compound as well as for haloperidol decanoate. As with all injectable
medications, local tissue reactions have been reported with haloperidol decanoate.<br/>Cardiovascular Effects: Tachycardia, hypotension, and hypertension have been reported.
QT prolongation and/or ventricular arrhythmias have also been reported, in
addition to ECG pattern changes compatible with the polymorphous configuration
of torsade de pointes, and may occur more frequently with high doses and in
predisposed patients (see WARNINGS and PRECAUTIONS). Cases
of sudden and unexpected death have been reported in association with the
administration of HALDOL. The nature of the evidence makes it impossible to
determine definitively what role, if any, HALDOL played in the outcome of
the reported cases. The possibility that HALDOL caused death cannot, ofcourse,
be excluded, but it is to be kept in mind that sudden and unexpected death
may occur in psychotic patients when they go untreated or when they are treated
with other antipsychotic drugs.<br/>CNS Effects:<br/>Extrapyramidal Symptoms (EPS): EPS during the administration of HALDOL (haloperidol) have
been reported frequently, often during the first few days of treatment. EPS
can be categorized generally as Parkinson-like symptoms, akathisia, or dystonia
(including opisthotonos and oculogyric crisis). While all can occur at relatively
low doses, they occur more frequently and with greater severity at higher
doses. The symptoms may be controlled with dose reductions or administration
of antiparkinson drugs such as benztropine mesylate USP or trihexyphenidyl
hydrochloride USP. It should be noted that persistent EPS have been reported;
the drug may have to be discontinued in such cases.<br/>Dystonia: Class Effect: Symptoms
of dystonia, prolonged abnormal contractions of muscle groups, may occur in
susceptible individuals during the first few days of treatment. Dystonic symptoms
include: spasm of the neck muscles, sometimes progressing to tightness of
the throat, swallowing difficulty, difficulty breathing, and/or protrusion
of the tongue. While these symptoms can occur at low doses, they occur more
frequently and with greater severity with high potency and at higher doses
of first generation antipsychotic drugs. An elevated risk of acute dystonia
is observed in males and younger age groups.<br/>Withdrawal Emergent Neurological Signs: Generally, patients receiving short-term therapy experience
no problems with abrupt discontinuation of antipsychotic drugs. However, some
patients on maintenance treatment experience transient dyskinetic signs after
abrupt withdrawal. In certain of these cases the dyskinetic movements are
indistinguishable from the syndrome described below under "Tardive Dyskinesia"
except for duration. Although the long-acting properties of haloperidol decanoate
provide gradual withdrawal, it is not known whether gradual withdrawal of
antipsychotic drugs will reduce the rate of occurrence of withdrawal emergent
neurological signs.<br/>Tardive Dyskinesia: As with all antipsychotic agents HALDOL has been associated
with persistent dyskinesias. Tardive dyskinesia, a syndrome consisting of
potentially irreversible, involuntary, dyskinetic movements, may appear in
some patients on long-term therapy with haloperidol decanoate or may occur
after drug therapy has been discontinued. The risk appears to be greater in
elderly patients on high-dose therapy, especially females. The symptoms are
persistent and in some patients appear irreversible. The syndrome is characterized
by rhythmical involuntary movements of tongue, face, mouth or jaw (e.g., protrusion
of tongue, puffing of cheeks, puckering of mouth, chewing movements). Sometimes
these may be accompanied by involuntary movements of extremities and the trunk. There
is no known effective treatment for tardive dyskinesia; antiparkinson agents
usually do not alleviate the symptoms of this syndrome. It is suggested that
all antipsychotic agents be discontinued if these symptoms appear. Should
it be necessary to reinstitute treatment, or increase the dosage of the agent,
or switch to a different antipsychotic agent, this syndrome may be masked. It
has been reported that fine vermicular movement of the tongue may be an early
sign of tardive dyskinesia and if the medication is stopped at that time the
full syndrome may not develop.<br/>Tardive Dystonia: Tardive dystonia, not associated with the above syndrome,
has also been reported. Tardive dystonia is characterized by delayed onset
of choreic or dystonic movements, is often persistent, and has the potential
of becoming irreversible.<br/>Other CNS Effects: Insomnia, restlessness, anxiety, euphoria, agitation, drowsiness,
depression, lethargy, headache, confusion, vertigo, grand mal seizures, exacerbation
of psychotic symptoms including hallucinations, and catatonic-like behavioral
states which may be responsive to drug withdrawal and/or treatment with anticholinergic
drugs.<br/>Body as a Whole: Neuroleptic malignant syndrome (NMS), hyperpyrexia and heat
stroke have been reported with HALDOL. (See WARNINGS
for further information concerning NMS.)<br/>Hematologic Effects: Reports have appeared citing the occurrence of mild and usually
transient leukopenia and leukocytosis, minimal decreases in red blood cell
counts, anemia, or a tendency toward lymphomonocytosis. Agranulocytosis has
rarely been reported to have occurred with the use of HALDOL, and then only
in association with other medication.<br/>Liver Effects: Impaired liver function and/or jaundice have been reported.<br/>Dermatologic Reactions: Maculopapular and acneiform skin reactions and isolated cases
of photosensitivity and loss of hair.<br/>Endocrine Disorders: Lactation, breast engorgement, mastalgia, menstrual irregularities,
gynecomastia, impotence, increased libido, hyperglycemia, hypoglycemia and
hyponatremia.<br/>Gastrointestinal Effects: Anorexia, constipation, diarrhea, hypersalivation, dyspepsia,
nausea and vomiting.<br/>Autonomic Reactions: Dry mouth, blurred vision, urinary retention, diaphoresis
and priapism.<br/>Respiratory Effects: Laryngospasm, bronchospasm and increased depth of respiration.<br/>Special Senses: Cataracts, retinopathy and visual disturbances.<br/>Postmarketing Events: Hyperammonemia has been reported in a 5 1 /2 year old child
with citrullinemia, an inherited disorder of ammonia excretion, following
treatment with HALDOL.
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dailymed-instance:indicatio... |
HALDOL Decanoate 50 and HALDOL Decanoate 100 are indicated
for the treatment of schizophrenic patients who require prolonged parenteral
antipsychotic therapy.
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dailymed-instance:name |
Haldol Decanoate
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