23.06.2020

Haloperidol decanoate, solution for intramuscular administration (ampoules). Haloperidol decanoate - instructions, use, indications, contraindications, action Cautions for use

Dosage form: solution for intramuscular administration (oil) Compound:

Active substance: 70.52 mg of haloperidol decanoate (corresponding to 50 mg of haloperidol) per 1 ml.

Excipients: benzyl alcohol - 15.00 mg, sesame oil - up to 1.00 ml.

Description:

Yellow or greenish-yellow, transparent solution.

Pharmacotherapeutic group:Antipsychotic (neuroleptic) ATX:

N.05.A.D.01 Haloperidol

Pharmacodynamics:

Haloperidol decanoate is an ester of haloperidol and decanoic acid. When administered intramuscularly, slow hydrolysis releases haloperidol, which then enters the blood circulation.

Haloperidol decanoate is a butyrophenone-derived antipsychotic. is a pronounced antagonist of central dopamine receptors and is a strong antipsychotic.

It has a pronounced calming effect during psychomotor agitation, and is effective against mania and other agitations.

The limbic activity of the drug manifests itself in a sedative effect and is effective as an additional remedy for chronic pain.

Effects on the basal ganglions cause extrapyramidal side effects (dystonia, akathisia, parkinsonism).

In socially withdrawn patients, social behavior is normalized.

Severe peripheral antidopamine activity is accompanied by the development of nausea and vomiting (irritation of chemoreceptors), relaxation of the gastrointestinal sphincter and increased release of prolactin (blocks the prolactin-inhibiting factor in the adenohypophysis).

Pharmacokinetics:

The plasma concentration of haloperidol released from haloperidol decanoate depot after intramuscular injection reaches its maximum after 3-9 days. The half-life is about 3 weeks. With regular monthly administration, the saturation stage in plasma is reached after 2-4 months. Pharmacokinetics when administered intramuscularly is dose-dependent. At doses below 450 mg, there is a direct relationship between the dose and plasma concentration of haloperidol.

To achieve a therapeutic effect, 4 - 20-25 mg/l plasma concentration of haloperidol is required. easily penetrates the blood-brain barrier. 92% binds to blood proteins and is excreted in feces (60%) and urine (40%), where ~ 1% is unchanged.

Indications:

Treatment of chronic schizophrenia and other psychoses, especially when treatment with rapid-acting haloperidol has been effective and an effective, moderately sedative antipsychotic is needed.

Other disorders of mental activity and behavior that occur with psychomotor agitation and require long-term treatment.

Contraindications:

Hypersensitivity to any of the components of the drug.

Coma.

Central nervous system depression caused by drugs or alcohol.

Parkinson's disease.

Damage to the basal ganglia.

Childhood.

Carefully:

Decompensated cardiovascular diseases (including angina pectoris, intracardiac conduction disorders, prolongation of the Q-T interval or a predisposition to this - hypokalemia, simultaneous use of other drugs that can cause prolongation of the Q-T interval), epilepsy, angle-closure glaucoma, hepatic and /or renal failure, hyperthyroidism (with symptoms of thyrotoxicosis), pulmonary-cardiac and respiratory failure (including in COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Pregnancy and lactation:

Studies involving a large number of patients indicate that haloperidol decanoate does not cause a significant increase in the incidence of malformations. In a few isolated cases, congenital malformations have been observed when haloperidol decanoate was used concomitantly with other drugs during fetal development.

Prescribing haloperidol decanoate during pregnancy is possible only if the treatment will bring more benefit than harm to the fetus.

Haloperidol decanoate passes into breast milk. When treating with haloperidol decanoate, the benefit of treatment should clearly prevail over the possible harm. In some cases, the development of extrapyramidal symptoms in infants was observed when the drug was taken by a nursing mother.

Directions for use and dosage:

Intended exclusively for adults, exclusively for intramuscular administration! Do not administer intravenously!

For adults : Patients on long-term treatment with oral antipsychotics (mainly haloperidol) may be advised to switch to depot injections. The dose should be adjusted on an individual basis due to significant individual differences in response. Dose selection should be carried out under strict medical supervision of the patient. The choice of the initial dose is carried out taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times higher than the dose of oral haloperidol, which usually corresponds to 25-75 mg of haloperidol decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.

Depending on the effect, the dose can be increased stepwise, by 50 mg, until the optimal effect is obtained. Typically the maintenance dose corresponds to 20 times the daily dose of oral haloperidol. If symptoms of the underlying disease recur during dose titration, treatment with haloperidol decanoate can be supplemented with oral haloperidol.

Typically, injections are given every 4 weeks, however, due to large individual differences in effectiveness, more frequent use of the drug may be required.

Elderly patients and patients with oligophrenia A lower initial dose is recommended, such as 12.5-25 mg every 4 weeks. In the future, depending on the effect, the dose may be increased.

Side effects:

Side effects that develop during treatment with haloperidol decanoate are due to the action of haloperidol.

Local reactions associated with the injection may also develop.

From the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), restlessness, anxiety, agitation, fears, akathisia, euphoria or depression, lethargy, epileptic attacks, development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, incl. tardive dyskinesia (smacking and wrinkling of the lips, puffing out of the cheeks, rapid and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), tardive dystonia (frequent blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled bending movements of the neck, torso , arms and legs) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness).

From the SSS side: when used in high doses - decreased blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (extension of the Q-T interval, signs of flutter and ventricular fibrillation).

From the digestive system: when used in high doses - loss of appetite, dry mouth, hyposalivation, nausea, vomiting, diarrhea or constipation, impaired liver function, up to the development of jaundice.

From the hematopoietic organs: rarely - temporary leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

From the genitourinary system: urinary retention (with prostatic hyperplasia), peripheral edema, pain in the mammary glands, gynecomastia, hyperprolactinemia, menstrual irregularities, decreased potency, increased libido, priapism.

From the senses: cataracts, retinopathy, blurred vision.

Allergic reactions: maculopapular and acne-like skin changes, photosensitivity, rarely - bronchospasm, laryngospasm.

Laboratory indicators: hyponatremia, hyper- or hypoglycemia.

Others: alopecia, weight gain.

Overdose:

The use of depot injections of haloperidol decanoate is associated with a lower risk of overdose than oral haloperidol. The symptoms of an overdose of haloperidol decanoate and haloperidol are the same. If an overdose is suspected, the long duration of action of haloperidol decanoate should be taken into account.

Symptoms : development of known pharmacological effects and side effects in a more pronounced form.

Symptoms that pose the greatest danger: extrapyramidal reactions, decreased blood pressure, sedation. Extrapyramidal reactions manifest themselves in the form of muscle rigidity and general or localized tremor. More often it is possible to increase blood pressure than to decrease it. In exceptional cases, the development of a coma with respiratory suppression and arterial hypotension, turning into a shock-like state. Possible prolongation of the QT interval with the development of ventricular arrhythmias.

Treatment : There is no specific antidote. The airway of a comatose patient is ensured using an oropharyngeal or endotracheal tube; if respiratory depression occurs, artificial ventilation may be required. Vital functions and ECG are monitored until it is completely normalized, severe arrhythmias are treated with appropriate antiarrhythmic drugs, in case of low blood pressure and circulatory arrest - intravenous administration of fluid, plasma or concentrated albumin and dopamine, or norepinephrine as a vasopressor. The administration of epinephrine is unacceptable, because as a result of interaction with haloperidol, decanoate can cause a significant increase in blood pressure, requiring immediate correction. For severe extrapyramidal symptoms, administration of antiparkinsonian drugs with anticholinergic action for several weeks (symptoms may return after discontinuation of these drugs!).

Interaction:

Increases the severity of the inhibitory effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotics, and agents for general anesthesia.

Enhances the effect of peripheral m-anticholinergic drugs and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from alpha-adrenergic neurons and suppression of its uptake by these neurons).

It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, thereby increasing (mutually) their sedative effect and toxicity.

When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of grand mal seizures.

Reduces the effect of anticonvulsants (lowering the seizure threshold with haloperidol).

Weakens the vasoconstrictor effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of alpha-adrenergic receptors by haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure).

Reduces the effect of antiparkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system).

Changes (may increase or decrease) the effect of anticoagulants.

Reduces the effect of bromocriptine (dose adjustment may be required).

When used with methyldopa, it increases the risk of developing mental disorders (including disorientation in space, slowdown and difficulty in thinking processes).

Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psychostimulant effect (blockade of alpha-adrenergic receptors by haloperidol).

Anticholinergic, antihistamine (first generation) and antiparkinsonian drugs can enhance the m-anticholinergic effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).

Long-term administration of carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in plasma.

In combination with Li + drugs (especially in high doses), encephalopathy may develop (can cause irreversible neurointoxication) and increased echetrapyramidal symptoms.

When taken simultaneously with fluoxetine, the risk of developing side effects from the central nervous system, especially extrapyramidal reactions, increases.

When used simultaneously with drugs that cause extrapyramidal reactions, it increases the frequency and severity of estrapyramidal disorders.

Drinking strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.

Special instructions:

In several cases, sudden death occurred in psychiatric patients receiving antipsychotic drugs. If you are predisposed to QT prolongation (QT syndrome, hypokalemia, taking medications that prolong QT), caution should be exercised during treatment with haloperidol decanoate due to the risk of QT prolongation.

Treatment should begin with oral haloperidol and only then proceed to injections of haloperidol decanoate to identify unexpected adverse reactions.

If liver function is impaired, caution must be exercised, because the drug is metabolized in the liver.

With long-term treatment, regular monitoring of liver function and blood counts is necessary.

In isolated cases, haloperidol decanoate has caused convulsions. Treatment of patients with epilepsy or in conditions predisposing to convulsions (eg, head trauma, alcohol withdrawal) requires caution.

Thyroxine increases the toxicity of haloperidol decanoate. Treatment of patients suffering from hyperthyroidism with haloperidol decanoate is permissible only with appropriate thyreostatic treatment.

In the simultaneous presence of depression and psychosis or when depression is dominant, haloperidol decanoate is prescribed together with antidepressants.

When antiparkinsonian therapy is carried out simultaneously, after completion of treatment with haloperidol decanoate, it should be continued for several more weeks in view of faster elimination of antiparkinsonian drugs.

The drug Haloperidol decanoate is an oil solution for intramuscular administration, therefore it is prohibited to administer intravenously!

In the future, the degree of prohibition is determined based on the individual reaction of the patient. During treatment with haloperidol decanoate, it is prohibited to drink alcohol.

At the beginning of treatment with the drug and, especially, during the use of high doses, a sedative effect of varying severity may occur with a decrease in attention, which can be aggravated by alcohol intake.

Caution must be exercised when performing heavy physical work or taking a hot bath (heat stroke may develop due to suppression of central and peripheral thermoregulation in the hypothalamus).

During treatment, you should not take “anti-cold” over-the-counter drugs (anticholinergic effects and the risk of heat stroke may increase).

Exposed skin should be protected from excess solar radiation due to the increased risk of photosensitivity.

Treatment is stopped gradually to avoid withdrawal syndrome.

Impact on the ability to drive vehicles. Wed and fur.:

During the initial period of treatment with haloperidol decanoate, it is prohibited to drive a car and perform work associated with an increased risk of injury and/or requiring concentration.

Release form/dosage:Solution for intramuscular administration (oil). Package:

1 ml of the drug in a dark glass ampoule of hydrolytic class I with a breaking point.

5 ampoules in a plastic tray.

1 plastic pallet along with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 °C, in a place protected from light.

Keep out of the reach of children.

Best before date:

Use before the expiration date indicated on the package.

Conditions for dispensing from pharmacies:

Description of the drug Haloperidol decanoate
Composition of the drug Haloperidol decanoate
Indications for the drug Haloperidol decanoate
Storage conditions for the drug Haloperidol decanoate
Shelf life of the drug Haloperidol decanoate

Release form, composition and packaging

solution for injection oily 50 mg/1 ml: amp. 5 pieces.
Reg. No.: RK-LS-5-No. 010234 dated 09/06/2012 - Valid

Excipients: benzyl alcohol, sesame oil.

1 ml - dark glass ampoules (5) - cardboard packs.

Description of active ingredients drug HALOPERIDOL DECANOATE. The scientific information provided is general and cannot be used to make a decision about the possibility of using a particular drug. Update date: 01/14/2006

pharmachologic effect

Antipsychotic drug (neuroleptic), butyrophenone derivative. It has a pronounced antipsychotic effect due to the blockade of depolarization or a decrease in the degree of excitation of dopamine neurons (reduced release) and blockade of postsynaptic dopamine D 2 receptors in the mesolimbic and mesocortical structures of the brain.

It has a moderate sedative effect due to the blockade of α-adrenergic receptors of the reticular formation of the brain stem; pronounced antiemetic effect due to blockade of dopamine D 2 receptors in the trigger zone of the vomiting center; hypothermic effect and galactorrhea caused by blockade of dopamine receptors in the hypothalamus.

Long-term use is accompanied by changes in endocrine status; in the anterior lobe of the pituitary gland, the production of prolactin increases and the production of gonadotropic hormones decreases.

Blockade of dopamine receptors in the dopamine pathways of the substantia nigra striata promotes the development of extrapyramidal motor reactions; blockade of dopamine receptors in the tuberoinfundibular system causes a decrease in the release of GH.

It has virtually no anticholinergic effect.

Eliminates persistent personality changes, delusions, hallucinations, mania, and increases interest in the environment. Effective in patients resistant to other antipsychotics. Has some activating effect. In hyperactive children, it eliminates excessive motor activity and behavioral disorders (impulsivity, difficulty concentrating, aggressiveness).

Unlike haloperidol, haloperidol decanoate is characterized by a prolonged action.

Pharmacokinetics

When taken orally, it is absorbed from the gastrointestinal tract by 60%. Cmax in plasma when taken orally is achieved after 3-6 hours, with intramuscular administration - after 10-20 minutes, with intramuscular administration of haloperidol decanoate - 3-9 days. Subject to first pass effect through the liver.

Protein binding is 92%. V d at equilibrium concentration is 18 l/kg. Actively metabolized in the liver with the participation of isoenzymes CYP2D6, CYP3A3, CYP3A5, CYP3A7. It is an inhibitor of the CYP2D6 isoenzyme. There are no active metabolites.

Easily penetrates histohematic barriers, including the BBB. Excreted in breast milk.

T1/2 when administered orally - 24 hours, with intramuscular administration - 21 hours, with intravenous administration - 14 hours. Haloperidol decanoate is excreted within 3 weeks.

Excreted by the kidneys - 40% and with bile through the intestines - 15%.

Indications for use

Acute and chronic psychotic disorders (including schizophrenia, manic-depressive, epileptic, alcoholic psychoses), psychomotor agitation of various origins, delusions and hallucinations of various origins, Huntington's chorea, mental retardation, agitated depression, behavioral disorders in old age and childhood ( including hyperreactivity in children and childhood autism), psychosomatic disorders, Tourette's disease, stuttering, long-term and treatment-resistant vomiting and hiccups, prevention and treatment of nausea and vomiting during chemotherapy.

Dosage regimen

When taken orally for adults, the initial dose is 0.5-5 mg 2-3 times / day, for elderly patients - 0.5-2 mg 2-3 times / day. Further, depending on the patient’s response to treatment, the dose is gradually increased in most cases to 5-10 mg/day. High doses (more than 40 mg/day) are used in rare cases, for a short time and in the absence of concomitant diseases. For children - 25-75 mcg/kg/day in 2-3 doses.

When administered intramuscularly to adults, the initial single dose is 1-10 mg, the interval between repeated injections is 1-8 hours; when using the depot form, the dose is 50-300 mg once every 4 weeks.

For intravenous administration, a single dose is 0.5-50 mg, the frequency of administration and the dose for repeated administration depend on the indications and clinical situation.

Maximum doses: when taken orally for adults - 100 mg/day;

IM - 100 mg/day, when using the depot form - 300 mg/month.

Side effects

From the side of the central nervous system: headache, insomnia, anxiety, feelings of anxiety and fear, euphoria, agitation, drowsiness (especially at the beginning of treatment), akathisia, depression or euphoria, lethargy, epileptic attack, development of a paradoxical reaction (exacerbation of psychosis, hallucinations);

with long-term treatment - extrapyramidal disorders (including tardive dyskinesia, tardive dystonia and NMS).

From the cardiovascular system: when used in high doses - arterial hypotension, tachycardia, arrhythmia, ECG changes (increased QT interval, signs of ventricular flutter and fibrillation).

From the digestive system: when used in high doses - loss of appetite, dry mouth, hyposalivation, nausea, vomiting, constipation or diarrhea, liver dysfunction, including the development of jaundice.

From the hematopoietic system: rarely - mild and temporary leukopenia, leukocytosis, agranulocytosis, slight erythropenia and a tendency to monocytosis.

From the endocrine system: gynecomastia, pain in the mammary glands, hyperprolactinemia, menstrual irregularities, decreased potency, increased libido, priapism.

From the side of metabolism: hyper- and hypoglycemia, hyponatremia;

increased sweating, peripheral edema, weight gain.

From the side of the organ of vision: impaired visual acuity, cataracts, retinopathy, accommodation disorders.

Allergic reactions: rarely - skin rash, bronchospasm, laryngospasm, hyperpyrexia.

Dermatological reactions: maculopapular and acne-like skin changes;

rarely - photosensitivity, alopecia.

Effects due to cholinergic action: dry mouth, hyposalivation, urinary retention, constipation.

Contraindications for use

Diseases of the central nervous system, accompanied by symptoms of extrapyramidal disorders, depression, hysteria, coma of various etiologies; severe toxic depression of the central nervous system caused by drugs. Pregnancy, lactation. Children under 3 years of age. Hypersensitivity to haloperidol and other butyrophenone derivatives.

Use during pregnancy and breastfeeding

Haloperidol is contraindicated during pregnancy and lactation.

IN experimental studies in some cases, teratogenic and fetotoxic effects were detected. Haloperidol is excreted in breast milk. Concentrations of haloperidol in breast milk have been shown to be sufficient to cause sedation and impaired motor function in the infant.

Use in elderly patients

special instructions

Use with caution in cardiovascular diseases with symptoms of decompensation, myocardial conduction disorders, an increase in the QT interval or the risk of an increase in the QT interval (including hypokalemia, simultaneous use with drugs that can increase the QT interval); for epilepsy; angle-closure glaucoma; liver and/or kidney failure; with thyrotoxicosis; pulmonary-cardiac and respiratory failure (including with COPD and acute infectious diseases); with prostatic hyperplasia with urinary retention; for chronic alcoholism; simultaneously with anticoagulants.

If tardive dyskinesia develops, it is necessary to gradually reduce the dose of haloperidol and prescribe another drug.

There are reports of the possibility of symptoms of diabetes insipidus, exacerbation of glaucoma, and a tendency (with long-term treatment) to the development of lymphomonocytosis during haloperidol therapy.

Elderly patients usually require a lower initial dose and a more gradual dose titration. This group of patients is characterized by a high probability of developing extrapyramidal disorders. Close monitoring of the patient is recommended to identify early signs of tardive dyskinesia.

During treatment with antipsychotics, the development of NMS is possible at any time, but most often it occurs soon after the start of therapy or after transferring a patient from one antipsychotic drug to another, during combination treatment with another psychotropic drug, or after increasing the dose.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

During the period of use of haloperidol, you should refrain from engaging in potentially hazardous activities that require increased attention and high speed of psychomotor reactions.

Drug interactions

When used simultaneously with drugs that have a depressant effect on the central nervous system, ethanol may increase central nervous system depression, respiratory depression and hypotensive effects.

With the simultaneous use of drugs that cause extrapyramidal reactions, the frequency and severity of extrapyramidal effects may increase.

With the simultaneous use of drugs with anticholinergic activity, the anticholinergic effects may be enhanced.

When used simultaneously with anticonvulsants, it is possible to change the type and/or frequency of epileptiform seizures, as well as reduce the concentration of haloperidol in the blood plasma; with tricyclic antidepressants (including desipramine) - the metabolism of tricyclic antidepressants decreases, the risk of developing seizures increases.

With simultaneous use, haloperidol potentiates the effect of antihypertensive drugs.

When used simultaneously with beta-blockers (including propranolol), severe arterial hypotension is possible. With the simultaneous use of haloperidol and propranolol, a case of severe arterial hypotension and cardiac arrest has been described.

With simultaneous use, a decrease in the effect of indirect anticoagulants is observed.

When used simultaneously with lithium salts, the development of more pronounced extrapyramidal symptoms is possible due to increased blockade of dopamine receptors, and when used in high doses, irreversible intoxication and severe encephalopathy are possible.

When used simultaneously with venlafaxine, it is possible to increase the concentration of haloperidol in the blood plasma; with guanethidine - it is possible to reduce the hypotensive effect of guanethidine; with isoniazid - there are reports of increased concentrations of isoniazid in the blood plasma; with imipenem - there are reports of transient arterial hypertension.

When used simultaneously with indomethacin, drowsiness and confusion are possible.

When used simultaneously with carbamazepine, which is an inducer of microsomal liver enzymes, it is possible to increase the rate of metabolism of haloperidol. Haloperidol may increase plasma concentrations of carbamazepine. Symptoms of neurotoxicity may occur.

With simultaneous use, the therapeutic effect of levodopa and pergolide may be reduced due to blockade of dopamine receptors by haloperidol.

When used simultaneously with methyldopa, sedation, depression, dementia, confusion, and dizziness are possible; with morphine - myoclonus may develop; with rifampicin, phenytoin, phenobarbital - a decrease in the concentration of haloperidol in the blood plasma is possible.

When used concomitantly with fluvoxamine, there are limited reports of a possible increase in the concentration of haloperidol in the blood plasma, which is accompanied by toxic effects.

When used simultaneously with fluoxetine, the development of extrapyramidal symptoms and dystonia is possible; with quinidine - an increase in the concentration of haloperidol in the blood plasma; with cisapride - prolongation of the QT interval on the ECG.

When used simultaneously with epinephrine, it is possible to “pervert” the pressor effect of epinephrine, and as a result of this, the development of severe arterial hypotension and tachycardia.

solution for intramuscular administration, oily 50 mg/ml; dark glass ampoule 1 ml, cardboard pack 5; No. P N015065/01, 2009-05-13 from Gedeon Richter (Hungary)

Latin name

Haloperidol decanoate

Active substance

Haloperidol*(Haloperidolum)

ATX:

N05AD01 Haloperidol

Pharmacological group

Neuroleptics

Nosological classification (ICD-10)

F20 Schizophrenia
F29 Non-organic psychosis, unspecified
F91 Behavioral disorders
R41.8.0* Intellectual-mnestic disorders
R45.1 Restlessness and agitation

Release form

Solution for intramuscular administration, oily, 50 mg/ml. In a dark glass ampoule of I hydrolytic class with a breaking point, 1 ml. 5 pcs in a plastic tray. 1 plastic pallet in a cardboard box.

Compound

pharmachologic effect

pharmachologic effect- antipsychotic, neuroleptic, antiemetic.

Indications of the drug

Psychomotor agitation of various origins (manic state, mental retardation, psychopathy, schizophrenia, chronic alcoholism), delusions and hallucinations (paranoid states, acute psychosis), Gilles de la Tourette syndrome, Huntington's chorea, psychosomatic disorders, behavioral disorders in old age and childhood, stuttering , long-lasting and treatment-resistant vomiting and hiccups. For haloperidol decanoate: schizophrenia (maintenance therapy).

Contraindications

Hypersensitivity, severe toxic depression of the central nervous system or coma caused by taking drugs; diseases of the central nervous system accompanied by pyramidal and extrapyramidal symptoms (including Parkinson's disease), epilepsy (the convulsive threshold may decrease), severe depressive disorders (symptoms may worsen), cardiovascular diseases with decompensation symptoms, pregnancy, breastfeeding, age up to 3 years.

Directions for use and doses

V/m, in the gluteal region.

Intended exclusively for adults, exclusively for intramuscular administration. Do not administer IV.

Doses exceeding 3 ml should be avoided to avoid an unpleasant feeling of fullness at the injection site.

Use during pregnancy and breastfeeding

Contraindicated during pregnancy.

During treatment, you should stop breastfeeding (passes into breast milk).

Side effects

From the nervous system and sensory organs: akathisia, dystonic extrapyramidal disorders (including spasms of the muscles of the face, neck and back, tic-like movements or jerks, weakness in the arms and legs), parkinsonian extrapyramidal disorders (including difficulty speaking and swallowing, mask-like face, shuffling gait, hand tremors and fingers), headache, insomnia, drowsiness, restlessness, anxiety, agitation, agitation, euphoria or depression, lethargy, epileptic seizures, confusion, exacerbation of psychosis and hallucinations, tardive dyskinesia (see “Precautions”); visual impairment (including visual acuity), cataracts, retinopathy.

From the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, arterial hypotension/hypertension, QT interval prolongation, ventricular arrhythmia, ECG changes; There have been reports of cases of sudden death, prolongation of the QT interval and torsade de pointes (TdP) (see Precautions); transient leukopenia and leukocytosis, erythropenia, anemia, agranulocytosis.

From the respiratory system: laryngospasm, bronchospasm.

From the gastrointestinal tract: anorexia, constipation/diarrhea, hypersalivation, nausea, vomiting, dry mouth, liver dysfunction, obstructive jaundice.

From the genitourinary system: engorgement of the mammary glands, unusual secretion of milk, mastalgia, gynecomastia, menstrual irregularities, urinary retention, impotence, increased libido, priapism.

From the skin: maculopapular and acne-like skin changes, photosensitivity, alopecia.

Others: neuroleptic malignant syndrome, accompanied by hyperthermia, muscle rigidity, loss of consciousness; hyperprolactinemia, sweating, hyperglycemia/hypoglycemia, hyponatremia.

Precautionary measures

Increased mortality in older patients with dementia-associated psychosis. According to Food and Drug Administration (FDA) 1, Antipsychotic drugs increase mortality in elderly patients when treating psychosis associated with dementia. An analysis of 17 placebo-controlled studies (lasting 10 weeks) in patients taking atypical antipsychotic drugs revealed an increase in drug-associated mortality by 1.6–1.7 times compared with patients receiving placebo. In typical 10-week controlled studies, the percentage of drug-attributable mortality was about 4.5%, compared with 2.6% in the placebo group. Although the causes of death varied, most were related to cardiovascular problems (such as heart failure, sudden death) or pneumonia. Observational studies suggest that, like atypical antipsychotics, treatment with traditional antipsychotics may also be associated with increased mortality.

Tardive dyskinesia. As with other antipsychotics, haloperidol is associated with the development of tardive dyskinesia, a syndrome characterized by involuntary movements (may occur in some patients with long-term treatment or occur after drug therapy has been discontinued). The risk of developing tardive dyskinesia is higher in older patients during high-dose therapy, especially in women. Symptoms are persistent and, in some patients, irreversible: rhythmic involuntary movements of the tongue, face, mouth and jaw (for example, protrusion of the tongue, puffing out of the cheeks, puckering of the lips, uncontrolled chewing movements), sometimes they can be accompanied by involuntary movements of the limbs and torso. If tardive dyskinesia develops, discontinuation of the drug is recommended.

Dystonic extrapyramidal disorders are most common in children and young adults and at the beginning of treatment; may subside within 24–48 hours after stopping haloperidol. Parkinsonian extrapyramidal effects more often develop in older people and are detected in the first few days of treatment or during long-term therapy.

Cardiovascular effects. Cases of sudden death, QT interval prolongation and torsades de pointes have been reported in patients receiving haloperidol. Caution should be exercised when treating patients with predisposition factors to prolongation of the QT interval, incl. electrolyte imbalance (especially hypokalemia and hypomagnesemia), simultaneous use of drugs that prolong the QT interval. When treating with haloperidol, it is necessary to regularly monitor the ECG, blood count, and evaluate the level of liver enzymes. During therapy, patients must refrain from engaging in potentially hazardous activities that require increased attention and rapid mental and motor reactions.

Storage conditions for the drug Haloperidol decanoate

In a place protected from light, at a temperature of 15–30 °C.

Keep out of the reach of children.

Solution, 50 mg/ml:

Active substance: haloperidol decanoate 70.52 mg (corresponds to 50 mg of haloperidol);
Excipients;
benzyl alcohol - 15 mg;
sesame oil - up to 1 ml.

In a dark glass ampoule of I hydrolytic class with a breaking point, 1 ml. 5 pcs in a plastic tray. 1 plastic pallet in a cardboard box.

Description of the dosage form

Oily solution for intramuscular administration.

pharmachologic effect

Haloperidol decanoate is an ester of haloperidol and decanoic acid. When administered intramuscularly, slow hydrolysis releases haloperidol, which then enters the systemic circulation. Haloperidol decanoate is a butyrophenone-derived antipsychotic. Haloperidol is a strong antagonist of central dopamine receptors and is a strong neuroleptic.

Haloperidol is highly effective in the treatment of hallucinations and delusions, due to the direct blockade of central dopamine receptors (probably acts on mesocortical and limbic structures), and affects the basal ganglia (nigrostria). It has a pronounced calming effect during psychomotor agitation, and is effective against mania and other agitations.

The limbic activity of the drug manifests itself in a sedative effect; effective as an additional remedy for chronic pain.

Impact on the basal ganglia causes extrapyramidal reactions (dystonia, akathisia, parkinsonism).

In socially withdrawn patients, social behavior is normalized.

Severe peripheral antidopamine activity is accompanied by the development of nausea and vomiting (irritation of chemoreceptors), relaxation of the gastroduodenal sphincter and increased release of prolactin (blocks the prolactin-inhibiting factor in the adenohypophysis).

Pharmacokinetics

Absorption and distribution.

The Cmax of haloperidol released from the haloperidol depot after intramuscular injection is reached after 3-9 days. With regular monthly administration, the saturation stage in plasma is reached after 2-4 months. Pharmacokinetics with intramuscular administration is dose-dependent. At doses below 450 mg, there is a direct relationship between the dose and plasma concentration of haloperidol. To achieve a therapeutic effect, a plasma concentration of haloperidol of 20-25 mcg/l is required.

Haloperidol easily penetrates the BBB. Plasma protein binding - 92%.

Excretion.

T1/2 about 3 weeks. Excreted through the intestines (60%) and kidneys (40%, including 1% unchanged).

Instructions

IM, in the gluteal region.

Intended exclusively for adults, exclusively for intramuscular administration. Do not administer i.v.

Doses exceeding 3 ml should be avoided to avoid an unpleasant feeling of fullness at the injection site.

Indications for use: Haloperidol decanoate

Chronic schizophrenia and other psychoses, especially when treatment with rapid-acting haloperidol has been effective and an effective, moderately sedative antipsychotic is needed.

Other disorders of mental activity and behavior that occur with psychomotor agitation and require long-term treatment.

Contraindications for use of Haloperidol decanoate

Coma;
CNS depression caused by drugs or alcohol;
Parkinson's disease;
damage to the basal ganglia;
hypersensitivity to the components of the drug.

With caution: decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disorders, prolongation of the QT interval or a predisposition to this - hypokalemia, simultaneous use of other drugs that can cause prolongation of the QT interval), epilepsy, angle-closure glaucoma, liver and/or renal failure, hyperthyroidism (with symptoms of thyrotoxicosis), pulmonary-cardiac and respiratory failure (including in COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Haloperidol decanoate Use in pregnancy and children

Prescribing the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

Haloperidol Decanoate is excreted in breast milk. Prescribing the drug during breastfeeding is possible only if the expected benefit to the mother outweighs the potential risk to the baby. In some cases, the development of extrapyramidal symptoms in infants was observed when the drug was taken by a nursing mother.

Contraindicated for children.

Haloperidol decanoate Side effects

Side effects that develop during treatment with Haloperidol Decanoate are due to the action of haloperidol.

It is possible to develop local reactions associated with intramuscular administration of the drug.

From the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, agitation, fears, akathisia, euphoria or depression, lethargy, epileptic attacks, development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, incl. tardive dyskinesia (smacking and wrinkling of the lips, puffing out of the cheeks, rapid and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), tardive dystonia (frequent blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled bending movements of the neck, torso , arms and legs) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness).

From the cardiovascular system: when used in high doses - decreased blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (prolongation of the QT interval, signs of flutter and ventricular fibrillation).

From the digestive system: when used in high doses - loss of appetite, dry mouth, hyposalivation, nausea, vomiting, diarrhea or constipation, impaired liver function, up to the development of jaundice.

From the hematopoietic system: rarely - transient leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.

From the urinary system: urinary retention (with prostatic hyperplasia), peripheral edema.

From the reproductive system and mammary gland: pain in the mammary glands, gynecomastia, hyperprolactinemia, menstrual irregularities, decreased potency, increased libido, priapism.

From the organ of vision: cataracts, retinopathy, blurred vision.

Metabolism: hyperglycemia, hypoglycemia, hyponatremia.

From the skin and subcutaneous tissues: maculopapular and acne-like skin changes, photosensitivity.

Allergic reactions: rarely - bronchospasm, laryngospasm.

Other: alopecia, weight gain.

Drug interactions

Increases the severity of the depressant effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotics, and general anesthesia.

Enhances the effect of peripheral m-anticholinergic drugs and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from α-adrenergic neurons and suppression of its uptake by these neurons).

It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, thereby increasing (mutually) their sedative effect and toxicity.

When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of grand mal seizures.

Reduces the effect of anticonvulsants (lowering the seizure threshold with haloperidol).

Weakens the vasoconstrictor effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of α-adrenergic receptors by haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure).

Reduces the effect of antiparkinsonian drugs (antagonistic effect on dopaminergic structures of the central nervous system).

Changes (may increase or decrease) the effect of anticoagulants.

Reduces the effect of bromocriptine (dose adjustment may be required).

When used with methyldopa, it increases the risk of developing mental disorders (including disorientation in space, slowing down and difficulty thinking).

Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psychostimulant effect (blockade of α-adrenergic receptors by haloperidol).

Anticholinergic, antihistamine (1st generation) and antiparkinsonian drugs can enhance the m-anticholinergic effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required).

Long-term use of carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in plasma.

In combination with lithium preparations (especially in high doses), the development of encephalopathy (can cause irreversible neurointoxication) and increased extrapyramidal symptoms is possible.

When taken simultaneously with fluoxetine, the risk of developing side effects from the central nervous system, especially extrapyramidal reactions, increases.

When used simultaneously with drugs that cause extrapyramidal reactions, it increases the frequency and severity of extrapyramidal disorders.

Drinking strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.

Dosage of Haloperidol decanoate

Adults: Patients on long-term treatment with oral antipsychotics (mainly haloperidol) may be advised to switch to depot injections. The dose should be adjusted on an individual basis due to significant individual differences in response. Dose selection should be carried out under strict medical supervision of the patient. The choice of the initial dose is carried out taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during previous treatment.

At the beginning of treatment, it is recommended to prescribe doses 10-15 times higher than the dose of oral haloperidol every 4 weeks, which usually corresponds to 25-75 mg of haloperidol decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.

Depending on the effect, the dose can be increased stepwise by 50 mg until the optimal effect is obtained. Typically the maintenance dose corresponds to 20 times the daily dose of oral haloperidol. If symptoms of the underlying disease return during dose titration, treatment with haloperidol decanoate can be supplemented with oral haloperidol. Typically, injections are given every 4 weeks, but due to large individual differences in effectiveness, more frequent use of the drug may be required.

Overdose

The use of depot injections of the drug Haloperidol Decanoate is associated with a lower risk of overdose than oral administration of haloperidol. Symptoms of an overdose of Haloperidol Decanoate and haloperidol are the same. If an overdose is suspected, the longer action of the former should be taken into account.

Symptoms: development of known pharmacological effects and side effects in a more pronounced form. The most dangerous symptoms are extrapyramidal reactions, decreased blood pressure, and sedation. Extrapyramidal reactions manifest themselves in the form of muscle rigidity and general or localized tremor. More often it is possible to increase blood pressure rather than decrease it. In exceptional cases, the development of a coma with respiratory depression and arterial hypotension, turning into a shock-like state. Possible prolongation of the QT interval with the development of ventricular arrhythmias.

Treatment: there is no specific antidote. Airway patency during the development of a coma is ensured using an oropharyngeal or endotracheal tube; in case of respiratory depression, mechanical ventilation may be required. Monitor vital functions and ECG (until it is completely normalized), treat severe arrhythmias with appropriate antiarrhythmic drugs; with reduced blood pressure and circulatory arrest - intravenous administration of fluid, plasma or concentrated albumin and dopamine or norepinephrine as a vasopressor. The administration of epinephrine is unacceptable, because as a result of interaction with the drug Haloperidol Decanoate, blood pressure may increase significantly, which will require immediate correction. For severe extrapyramidal symptoms, administration of antiparkinsonian drugs with anticholinergic action for several weeks (symptoms may return after discontinuation of these drugs).

Precautionary measures

In several cases, sudden death occurred in psychiatric patients receiving antipsychotic drugs.

If you are predisposed to prolongation of the QT interval (long QT syndrome, hypokalemia, use of drugs that prolong the QT interval), caution should be exercised during treatment due to the risk of prolongation of the QT interval.

Treatment should begin with oral haloperidol and only then proceed to injections of the drug Haloperidol Decanoate to identify unexpected adverse reactions.

If liver function is impaired, caution must be exercised, because the drug is metabolized in the liver.

With long-term treatment, regular monitoring of liver function and blood counts is necessary.

In isolated cases, Haloperidol Decanoate has caused convulsions. Treatment of patients with epilepsy and conditions predisposing to seizures (eg, head trauma, alcohol withdrawal) requires caution.

Thyroxine increases the toxicity of the drug. Treatment with Haloperidol Decanoate in patients suffering from hyperthyroidism is permissible only with appropriate thyreostatic treatment.

In case of simultaneous presence of depression and psychosis or in case of dominance of depression, Haloperidol Decanoate is prescribed together with antidepressants.

When antiparkinsonian therapy is carried out simultaneously after the end of treatment with Haloperidol Decanoate, it should be continued for several more weeks due to the faster elimination of antiparkinsonian drugs.

The drug Haloperidol Decanoate is an oil solution for intramuscular administration, therefore it is prohibited to administer it intravenously.

During treatment with the drug, it is prohibited to drink alcohol. In the future, the degree of prohibition is determined based on the individual reaction of the patient.

At the beginning of treatment with the drug and especially when used in high doses, a sedative effect of varying severity may occur with a decrease in attention, which can be aggravated by alcohol intake.

Caution must be exercised when performing heavy physical work or taking a hot bath (heat stroke may develop due to suppression of central and peripheral thermoregulation in the hypothalamus).

During treatment, you should not take “anti-cold” over-the-counter medications (anticholinergic effects and the risk of heat stroke may increase).

Exposed skin should be protected from excess solar radiation due to the increased risk of photosensitivity.

Treatment is stopped gradually to avoid withdrawal syndrome.

Influence on the ability to drive vehicles and operate machinery.

At the beginning of treatment with Haloperidol Decanoate, it is prohibited to drive a car or perform work associated with an increased risk of injury and/or requiring increased concentration.

Haloperidol decanoate is an antipsychotic drug intended for the treatment of psychotic disorders. According to its molecular structure, it is an ester of haloperidol and decanoic (capric) acid. It is a derivative of the aromatic ketone butyrophenone. Shows antagonism to central transmembrane metabotropic dopamine receptors. Thanks to the direct blocking of the latter, the drug is effective in eliminating hallucinations and delusions. Causes pronounced sedation with motor restlessness (from fussiness to destructive actions), including those accompanied by speech excitement (verbalism, shouting of phrases, words, individual sounds). Effective for manic syndrome and any form of motor restlessness that occurs with strong emotional arousal. Activity in relation to the limbic system is manifested in the ability to cause pronounced sedation. Can be taken as an adjuvant for chronic pain syndrome. Impact on the basal ganglia can provoke neuroleptic extrapyramidal disorders. It facilitates adaptation in society for persons with social behavior disorders. Blockade of peripheral dopamine receptors can cause vomiting (including productive ones), decreased tone of the lower esophageal sphincter and increased secretion of prolactin. The peak concentration of the active substance in the blood after intramuscular administration is observed in the time range from 3 to 9 days. The half-life is approximately three weeks. Elimination from the body is carried out together with feces (2/3 of the administered dose) and urine (1/3 of the administered dose). The drug is not used in pediatric practice. It is administered by injection and exclusively intramuscularly. The optimal injection site is the gluteal muscle. The maximum recommended volume for a single injection is 3 ml: otherwise, if it is exceeded, discomfort at the injection site (a feeling of fullness) is possible. Persons who have been taking tableted haloperidol for a long time can be transferred to treatment with injectable haloperidol in depot form - Haloperidol decanoate.

The dosage is selected individually for each specific patient under strict medical supervision, because reactions to taking the drug can vary widely. When selecting the initial dose, the symptoms of the disease, the severity of its course, and previously taken doses of haloperidol or other antipsychotics are taken into account. Depending on the therapeutic response, the dosage can be increased stepwise in increments of 50 mg until the desired effect is achieved. As a rule, the dosage of Haloperidol decanoate for maintenance therapy is identical to twenty times the dosage of oral haloperidol. If signs of the underlying pathology return during the dosage selection stage, haloperidol decanoate can be combined with oral haloperidol. In most cases, the frequency of administration of the drug is set once a month, however, due to the different severity of the therapeutic response, more frequent use of the drug is possible. Elderly people should be prescribed a more gentle dose of the drug. The medical literature describes cases of sudden deaths in psychiatric patients taking antipsychotics. If haloperidol is prescribed for the first time, it is recommended to start treatment with the oral form, and only then introduce Haloperidol Decanoate into the treatment regimen. This is done to identify unexpected side effects. Considering that metabolic transformations of the drug occur in the liver, if the functioning of this organ is impaired, special care should be taken when using Haloperidol decanoate. With a long course of medication, regular medical monitoring of liver function parameters is indicated. The thyroid hormone thyroxine increases the toxicity of Haloperidol decanoate. While using the drug, you should completely avoid the consumption of alcoholic beverages.

Pharmacology

Antipsychotic drug. Haloperidol decanoate is an ester of haloperidol and decanoic acid. When administered intramuscularly, slow hydrolysis releases haloperidol, which then enters the systemic circulation. Haloperidol decanoate is a butyrophenone-derived antipsychotic. Haloperidol is a strong antagonist of central dopamine receptors and is a strong neuroleptic.

The limbic activity of the drug manifests itself in a sedative effect; effective as an additional remedy for chronic pain.

Impact on the basal ganglia causes extrapyramidal reactions (dystonia, akathisia, parkinsonism).

In socially withdrawn patients, social behavior is normalized.

Pharmacokinetics

Suction and distribution

Haloperidol easily penetrates the BBB. Plasma protein binding - 92%.

Removal

T 1/2 about 3 weeks. Excreted through the intestines (60%) and kidneys (40%, including 1% unchanged).

Release form

The solution for intramuscular administration (oil) is transparent, yellow or greenish-yellow.

Excipients: benzyl alcohol - 15 mg, sesame oil - up to 1 ml.

1 ml - dark glass ampoules (5) - plastic trays (1) - cardboard packs.

Dosage

The drug is intended exclusively for adults, for intramuscular administration only. Do not administer the drug intravenously.

Patients on long-term treatment with oral antipsychotics (mainly haloperidol) may be advised to switch to depot injections. The dose should be adjusted individually due to significant differences in response to treatment between patients. Dose selection should be carried out under strict medical supervision of the patient. The choice of the initial dose is carried out taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times higher than the dose of haloperidol for oral administration, which usually corresponds to 25-75 mg of Haloperidol Decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.

Depending on the effect, the dose can be increased stepwise, by 50 mg, until the optimal effect is obtained. Typically, the maintenance dose corresponds to 20 times the daily oral dose of haloperidol. If the symptoms of the underlying disease return during the dose selection period, treatment with Haloperidol Decanoate can be supplemented with haloperidol for oral administration.

Injections are usually given every 4 weeks, but due to large individual differences in effectiveness, more frequent use may be required.

For elderly patients and patients with mental retardation, a lower initial dose is recommended, for example, 12.5-25 mg every 4 weeks. In the future, depending on the effect, the dose may be increased.

Overdose

Interaction