Haloperidol decanoate when it starts to work. Haloperidol decanoate instructions for use, contraindications, side effects, reviews. Instructions for use and dosage

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

Latin name

Haloperidol decanoate

Active substance

Haloperidol*(Haloperidolum)

ATH:

N05AD01 Haloperidol

Pharmacological group

Antipsychotics

Nosological classification (ICD-10)

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

Release form

Oil solution for intramuscular injection, 50 mg/ml. In a dark glass ampoule of hydrolytic class I with a break point of 1 ml. In a plastic pallet, 5 pcs. 1 plastic pallet in a carton.

Compound

pharmachologic effect

Indications of the drug

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

Contraindications

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

Dosage and administration

V/m , in the gluteal region.

It is intended exclusively for adults, exclusively for intramuscular injection. It is forbidden to enter in / in.

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

Use during pregnancy and lactation

Contraindicated in pregnancy.

At the time of treatment should stop breastfeeding (penetrates into breast milk).

Side effects

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

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia, arterial hypotension/hypertension, prolongation of the QT interval, ventricular arrhythmia, ECG changes; there are reports of cases of sudden death, prolongation of the QT interval and pirouette-type heart rhythm disturbances (see "Precautions"); transient leukopenia and leukocytosis, erythropenia, anemia, agranulocytosis.

From the respiratory system: laryngospasm, bronchospasm.

From the digestive tract: anorexia, constipation / diarrhea, hypersalivation, nausea, vomiting, dry mouth, abnormal liver function, obstructive jaundice.

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

From the side of 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 in the treatment of psychosis on the background of 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 trials, drug-associated mortality was about 4.5% versus 2.6% in the placebo group. Although the causes of death varied, the majority were related to cardiovascular problems (such as heart failure, sudden death) or pneumonia. Observational studies suggest that, like atypical antipsychotics, treatment with conventional antipsychotics may also be associated with increased mortality.

Tardive dyskinesia. As with other antipsychotics, haloperidol has been associated with the development of tardive dyskinesia, a syndrome characterized by involuntary movements (may appear in some patients during long-term treatment or occur after drug therapy has been discontinued). The risk of developing tardive dyskinesia is higher in elderly patients with high doses, especially in women. Symptoms are persistent and, in some patients, irreversible: rhythmic involuntary movements of the tongue, face, mouth, and jaw (eg, protrusion of the tongue, pouting of the cheeks, wrinkling of the lips, uncontrolled chewing movements), sometimes they may be accompanied by involuntary movements of the limbs and trunk. With the development of tardive dyskinesia, drug withdrawal is recommended.

Dystonic extrapyramidal disorders are most common in children and young people, and also at the beginning of treatment; may subside within 24 to 48 hours after discontinuation of haloperidol. Parkinsonian extrapyramidal effects are more likely to develop in the elderly 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 treated with haloperidol. Caution should be exercised in the treatment of patients with predisposition factors for prolongation of the QT interval, incl. electrolyte imbalance (especially hypokalemia and hypomagnesemia), simultaneous administration of drugs that prolong the QT interval. When treating with haloperidol, it is necessary to regularly monitor the ECG, blood counts, and evaluate the level of liver enzymes. During therapy, patients should refrain from engaging in potentially hazardous activities that require increased attention, rapid mental and motor reactions.

Storage conditions of 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 ingredient: haloperidol decanoate 70.52 mg (equivalent to 50 mg haloperidol);
• Excipients;
• benzyl alcohol - 15 mg;
• sesame oil - up to 1 ml.

In a dark glass ampoule of hydrolytic class I with a break point of 1 ml. In a plastic pallet, 5 pcs. 1 plastic pallet in a carton.

Description of the dosage form

Oily solution for intramuscular injection.

pharmachologic effect

Haloperidol decanoate is an ester of haloperidol and decanoic acid. With the / m administration during slow hydrolysis, haloperidol is released, which then enters the systemic circulation. Haloperidol decanoate is a neuroleptic derivative of butyrophenone. Haloperidol is a pronounced antagonist of the central dopamine receptors and belongs to strong antipsychotics.

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), affects the basal ganglia (nigrostria). It has a pronounced calming effect in psychomotor agitation, effective in mania and other agitations.

Limbic activity of the drug is manifested in a sedative effect; effective as an adjunct in chronic pain.

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

In socially closed patients, social behavior is normalized.

Pronounced 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.

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 i / m administration is dose-dependent. At doses below 450 mg, there is a direct relationship between the dose and the plasma concentration of haloperidol. To achieve a therapeutic effect, the concentration of haloperidol in plasma is 20-25 μg / l.

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

Withdrawal.

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

Instruction

In / m, in the gluteal region.

It is intended exclusively for adults, exclusively for intramuscular injection. It is forbidden to enter in / in.

Doses greater than 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 rapid-acting haloperidol treatment has been effective and an effective, moderately sedating antipsychotic is needed.

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

Contraindications to the 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 disturbances, 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, hepatic and / or renal failure, hyperthyroidism (with symptoms of thyrotoxicosis), pulmonary heart and respiratory failure (including 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 intended benefit to the mother outweighs the potential risk to the fetus.

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

Contraindicated in children.

Haloperidol decanoate side effects

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

Perhaps the development of local reactions associated with the / m 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 seizures, development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, incl. tardive dyskinesia (lip smacking and wrinkling, puffing out of the cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), tardive dystonia (increased blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled twisting movements of the neck, torso , hands and feet) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increase or decrease in blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness).

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

On the part of 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.

On the part of 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 disorders, decreased potency, increased libido, priapism.

On the part of the organ of vision: cataract, retinopathy, blurred vision.

From the side of metabolism: hyperglycemia, hypoglycemia, hyponatremia.

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

Allergic reactions: rarely - bronchospasm, laryngospasm.

Other: alopecia, weight gain.

drug interaction

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

Enhances the effect of peripheral m-anticholinergics 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, while increasing (mutually) their sedative effect and toxicity.

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

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

Weakens the vasoconstrictive effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of α-adrenergic receptors by haloperidol, which can lead to a perversion of the action of epinephrine and to 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 in thinking processes).

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 increase 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 plasma concentrations of haloperidol.

In combination with lithium preparations (especially in high doses), encephalopathy may develop (may cause irreversible neurointoxication) and increase in extrapyramidal 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 extrapyramidal disorders.

The use of 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 selected 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 neuroleptics prescribed during previous treatment.

At the beginning of treatment, every 4 weeks it is recommended to prescribe doses 10-15 times 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 in steps of 50 mg, until the optimal effect is obtained. Typically, the maintenance dose corresponds to 20 times the daily dose of oral haloperidol. With the resumption of symptoms of the underlying disease during the period of dose selection, treatment with haloperidol decanoate can be supplemented with oral haloperidol. Usually injections are administered every 4 weeks, however, 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 haloperidol. Symptoms of an overdose of the drug Haloperidol Decanoate and haloperidol are the same. If an overdose is suspected, the longer action of the former should be taken into account.

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

Treatment: There is no specific antidote. The patency of the respiratory tract during the development of a coma is provided with the help of an oropharyngeal or endotracheal probe, with respiratory depression, mechanical ventilation may be required. Carry out monitoring of vital functions and ECG (until it is completely normalized), treatment of severe arrhythmias with appropriate antiarrhythmic drugs; with reduced blood pressure and circulatory arrest - in / in the introduction of liquid, plasma or concentrated albumin and dopamine or norepinephrine as a vasopressor. The introduction 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. In severe extrapyramidal symptoms, the introduction of antiparkinsonian anticholinergic drugs for several weeks (possible resumption of symptoms after discontinuation of these drugs).

Precautionary measures

In several cases, psychiatric patients treated with antipsychotics have experienced sudden death.

In case of a predisposition to prolongation of the QT interval (long QT interval 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 move on to injections of the drug Haloperidol Decanoate to detect unforeseen adverse reactions.

In case of impaired liver function, care must be taken, because. drug metabolism is carried out in the liver.

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

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

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

With the simultaneous presence of depression and psychosis or with the dominance of depression, Haloperidol Decanoate is prescribed together with antidepressants.

With simultaneous anti-Parkinsonian therapy after the end of treatment with Haloperidol Decanoate, it should be continued for a few more weeks due to faster elimination of anti-Parkinsonian drugs.

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

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

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

Care must be taken when performing heavy physical work, 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 "cough" over-the-counter drugs (possibly increased anticholinergic effects and the risk of heat stroke).

Exposed skin should be protected from excessive solar radiation due to an increased risk of photosensitivity.

Treatment is stopped gradually to avoid the occurrence of a withdrawal syndrome.

Influence on the ability to drive vehicles and control mechanisms.

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

Antipsychotic drug (neuroleptic), a derivative of butyrophenone.
Drug: HALOPERIDOL DECANOATE
The active substance of the drug: haloperidol
ATX encoding: N05AD01
CFG: Antipsychotic drug (neuroleptic)
Registration number: P No. 015065/01
Date of registration: 21.10.05
The owner of the reg. Credit: GEDEON RICHTER Ltd. (Hungary)

Release form Haloperidol decanoate, drug packaging and composition.

Solution for i / m administration (oily) is transparent, yellow or greenish-yellow in color.

1 ml
haloperidol decanoate
70.52 mg
which corresponds to the content of haloperidol
50 mg

Excipients: benzyl alcohol, sesame oil.

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

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is provided only for familiarization with the drug, you should consult a doctor about the possibility of using it.

Pharmacological action Haloperidol decanoate

Antipsychotic drug (neuroleptic), a derivative of butyrophenone. It has a pronounced antipsychotic effect due to the blockade of depolarization or a decrease in the degree of excitation of dopamine neurons (decrease in release) and blockade of postsynaptic dopamine D2 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 D2 receptors of the trigger zone of the vomiting center; hypothermic effect and galactorrhea due to blockade of dopamine receptors in the hypothalamus.

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

Blockade of dopamine receptors in the dopamine pathways of the black-striped substance contributes to the development of extrapyramidal motor reactions; blockade of dopamine receptors in the tuberoinfundibular system causes a decrease in the release of growth hormone.

Virtually no anticholinergic action.

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

In contrast to haloperidol, haloperidol decanoate is characterized by a prolonged action.

Pharmacokinetics of the drug.

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

Protein binding is 92%. Vd at equilibrium concentration - 18 l / kg. It is 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 through histohematic barriers, including the BBB. Excreted in breast milk

T1 / 2 when taken orally - 24 hours, with intramuscular injection - 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 the elderly and childhood ( including hyperreactivity in children and childhood autism), psychosomatic disorders, Tourette's disease, stuttering, long-term and therapy-resistant vomiting and hiccups, prevention and treatment of nausea and vomiting during chemotherapy.

Dosage and method of application of the drug.

When administered 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 1 time in 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 the clinical situation.

Maximum doses: when taken orally for adults - 100 mg / day; i / m - 100 mg / day, when using the depot form - 300 mg / month.

Side effects of Haloperidol decanoate:

From the side of the central nervous system: headache, insomnia, anxiety, anxiety and fear, euphoria, agitation, drowsiness (especially at the beginning of treatment), akathisia, depression or euphoria, lethargy, epilepsy attack, development of a paradoxical reaction (exacerbation of psychosis, hallucinations); with long-term treatment - extrapyramidal disorders (including tardive dyskinesia, tardive dystonia and neuroleptic malignant syndrome).

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

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

On the part of 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 disorders, decreased potency, increased libido, priapism.

From the side of metabolism: hyper- and hypoglycemia, hyponatremia; increased sweating, peripheral edema, weight gain.

On the part of the organ of vision: visual acuity disorders, cataracts, retinopathy, accommodation disorders.

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

Dermatological reactions: maculo-papular and acne-like skin changes; rarely - photosensitivity, alopecia.

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

Contraindications to the drug:

CNS diseases, accompanied by symptoms of extrapyramidal disorders, depression, hysteria, coma of various etiologies; severe toxic CNS depression caused by drugs. Pregnancy, lactation. Children's age up to 3 years. Hypersensitivity to haloperidol and other butyrophenone derivatives.

Use during pregnancy and lactation.

Haloperidol is contraindicated during pregnancy and lactation.

In experimental studies, in some cases, teratogenic and fetotoxic effects were found. Haloperidol is excreted in breast milk. It has been shown that concentrations of haloperidol in breast milk are sufficient to cause sedation and impaired motor functions in an infant.

Special instructions for the use of haloperidol decanoate.

Use with caution in cardiovascular diseases with decompensation phenomena, 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); with epilepsy; angle-closure glaucoma; hepatic and / or renal failure; with thyrotoxicosis; pulmonary heart and respiratory failure (including COPD and acute infectious diseases); with prostatic hyperplasia with urinary retention; with chronic alcoholism; along with anticoagulants.

In the event of tardive dyskinesia, 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 contingent of patients is characterized by a high probability of developing extrapyramidal disorders. Careful monitoring of the patient is recommended to detect early signs of tardive dyskinesia.

Against the background of treatment with antipsychotics, the development of neuroleptic malignant syndrome is possible at any time, but most often it occurs shortly after the start of therapy or after the patient is transferred from one antipsychotic agent to another, during combined treatment with another psychotropic drug or after increasing the dose.

Avoid drinking alcohol during treatment.

Influence on the ability to drive vehicles and control mechanisms

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

Interaction of Haloperidol decanoate with other drugs.

With simultaneous use with drugs that have a depressant effect on the central nervous system, with ethanol, it is possible to increase the depression of the central nervous system, respiratory depression and hypotensive action.

With the simultaneous use of drugs that cause extrapyramidal reactions, it is possible to increase the frequency and severity of extrapyramidal effects.

With the simultaneous use of drugs with anticholinergic activity, it is possible to increase anticholinergic effects.

With simultaneous use with anticonvulsants, it is possible to change the type and / or frequency of epileptiform seizures, as well as a decrease in the concentration of haloperidol in the blood plasma; with tricyclic antidepressants (including desipramine) - the metabolism of tricyclic antidepressants decreases, the risk of convulsions increases.

With the simultaneous use of haloperidol potentiates the action of antihypertensive drugs.

With simultaneous use 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.

With simultaneous use with lithium salts, more pronounced extrapyramidal symptoms may develop due to increased blockade of dopamine receptors, and when used in high doses, irreversible intoxication and severe encephalopathy are possible.

With simultaneous use with venlafaxine, an increase in the concentration of haloperidol in the blood plasma is possible; with guanethidine - it is possible to reduce the hypotensive effect of guanethidine; with isoniazid - there are reports of an increase in the concentration of isoniazid in the blood plasma; with imipenem - there are reports of transient arterial hypertension.

With simultaneous use with indomethacin, drowsiness and confusion are possible.

With simultaneous use 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. Possible manifestation of symptoms of neurotoxicity.

With simultaneous use, it is possible to reduce the therapeutic effect of levodopa, pergolide due to blockade of dopamine receptors by haloperidol.

With simultaneous use with methyldopa, a sedative effect, depression, dementia, confusion, dizziness are possible; with morphine - the development of myoclonus is possible; with rifampicin, phenytoin, phenobarbital - a decrease in the concentration of haloperidol in the blood plasma is possible.

With simultaneous use with fluvoxamine, there are limited reports of a possible increase in the concentration of haloperidol in the blood plasma, which is accompanied by a toxic effect.

With simultaneous use with fluoxetine, extrapyramidal symptoms and dystonia may develop; with quinidine - an increase in the concentration of haloperidol in the blood plasma; with cisapride - prolongation of the QT interval on the ECG.

With simultaneous use with epinephrine, a “perversion” of the pressor action of epinephrine is possible, and as a result of this, the development of severe arterial hypotension and tachycardia.

Country of origin

Product group

Antipsychotic drug (neuroleptic)

Release form

• 1 ml - dark glass ampoules (5) - contour plastic packaging (1) - cardboard packs. 1 ml - dark glass ampoules (5) - contour plastic packaging (1) - cardboard packs.

Description of the dosage form

• Solution for intramuscular injection oily transparent, yellow or greenish-yellow color

pharmachologic effect

Pharmacokinetics

Special conditions

Compound

• haloperidol decanoate 70.52 mg, which corresponds to the content of haloperidol 50 mg Excipients: benzyl alcohol, sesame oil.

Haloperidol decanoate indications for use

• - chronic schizophrenia and other psychoses, especially when rapid-acting haloperidol treatment has been effective and an effective antipsychotic with moderate sedation is needed; - other disorders of mental activity and behavior that occur with psychomotor agitation and require long-term treatment.

Haloperidol decanoate contraindications

• - coma; - depression of the central nervous system caused by drugs or alcohol; - Parkinson's disease; - damage to the basal ganglia; - childhood; - Hypersensitivity to the components of the drug. With caution: decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disturbances, 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 kidney failure, hyperthyroidism (with manifestations of thyrotoxicosis), pulmonary heart and respiratory failure (including COPD and acute infectious diseases), prostatic hyperplasia with urinary retention, alcoholism.

Haloperidol decanoate dosage

• 50 mg 50 mg/ml

Haloperidol decanoate side effects

• Side effects that develop during treatment are due to the action of haloperidol. From the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, agitation, fears, akathisia, euphoria or depression, lethargy, epileptic seizures, development of a paradoxical reaction - exacerbation of psychosis and hallucinations; with long-term treatment - extrapyramidal disorders, incl. tardive dyskinesia (lip smacking and wrinkling, puffing out of the cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), tardive dystonia (increased blinking or spasms of the eyelids, unusual facial expression or body position, uncontrolled twisting movements of the neck, torso , hands and feet) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increase or decrease in blood pressure, increased sweating, urinary incontinence, muscle rigidity, epileptic seizures, loss of consciousness). From the side of the cardiovascular system: when used in high doses - a decrease in blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (prolongation of the QT interval, signs of flutter and ventricular fibrillation). On the part of 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.

drug interaction

Storage conditions

• keep away from children
• store in a place protected from light

Haloperidol decanoate is an antipsychotic. It can be attributed to a derivative form of butyrophenone. It is able to have a pronounced antipsychotic effect. This happens due to the blockade of depolarization or a decrease in the degree of excitation of dopamine neurons. This medication is widely used for mental disorders.

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ATX code

N05AD01 Haloperidol

Active ingredients

Haloperidol

Pharmacological group

Antipsychotic (neuroleptic)

pharmachologic effect

Antiemetics

Antipsychotic drugs

Antipsychotic drugs

Indications for use Haloperidol decanoate

Indications for the use of Haloperidol decanoate are that the drug is used for severe schizophrenia. It is prescribed as maintenance therapy. Especially in those cases where ordinary haloperidol was previously used as a therapeutic action.

This form of medication is enhanced and is able to support a person during periods of severe seizures. It is impossible to completely get rid of the disease, but to partially improve the patient's condition completely.

The medication is prescribed in cases where a person suffers from severe mental disorders. Often they are accompanied by hallucinations, increased aggression and excitability.

The drug is one of the long-acting antipsychotics. It is able to have a powerful antipsychotic effect and a moderate sedative effect. He can block dopamine receptors in the central nervous system. Haloperidol decanoate is able to have analgesic, anticonvulsant, antiemetic and antihistamine effects.

Release form

The release form is represented by tablets of white and almost white color. They have a rounded shape with a chamfer. The smell is practically absent. On one side of the tablet there is an engraving "I|I". The tablet contains 1.5 mg of haloperidol. Auxiliary substances of the drug are corn starch, gelatin, lactose, potato starch and talc.

The solution for intravenous and intramuscular administration is colorless or slightly yellowish. One ampoule contains 5 mg of the active substance. Lactic acid and water act as auxiliary components.

The clinical and pharmacological group of the drug is a neuroleptic. The tool is effective in both cases. It has a positive effect, both in the form of tablets and a solution for administration. In this case, it is worth deciding on your own which form of release to give preference to.

It is important to familiarize yourself with the main characteristics of the drug. This will allow you to determine whether a remedy is suitable or not and to understand when a fake is in front of a person. How to use the medication Haloperidol decanoate should be decided by the attending physician.

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Pharmacodynamics

The pharmacodynamics of the drug is represented by the fact that it is one of the long-acting antipsychotics. It is able to have a pronounced antipsychotic effect. In addition, the drug helps to calm down and has good sedative properties.

The drug actively blocks dopamine receptors, which are located in the central nervous system. The drug is able to have a powerful antiemetic effect. It also eliminates heat and constricts blood vessels.

This medication can be attributed to those that have a wide effect. After all, it helps not only to alleviate the condition of a person, but also to save him from unpleasant symptoms caused by mental disorders.

For the drug to really help, you need to use it correctly. Otherwise, the situation may worsen significantly. Therefore, consulting a doctor is a necessary measure. To take Haloperidol decanoate, you need to know enough about this medication and, most importantly, to use it correctly.

Pharmacokinetics

The pharmacokinetics of the drug is that it reaches the full equilibrium concentration only after 2-3 months. In this case, the drug must be re-introduced.

Haloperidol decanoate is one of the neuroleptics that have a prolonged action. Due to its active components, it has a pronounced antipsychotic effect. The person begins to feel relief after a short time. The main thing is to constantly support the patient with medication.

The possibility of blocking dopamine receptors in the central nervous system leads to the fact that the drug can have a pronounced antiemetic effect. In addition, it has antipyretic, antihistamine, analgesic and anticonvulsant functions. This is enough to make a person feel better.

Periodic attacks bring a lot of inconvenience to the patient and the people around him. Therefore, it is necessary to take Haloperidol Decanoate, it will help to transfer these processes much easier.

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Use of haloperidol decanoate during pregnancy

The use of haloperidol decanoate during pregnancy is not acceptable. The fact is that such exposure can adversely affect the development of the fetus. It is especially dangerous to take the remedy in the early stages of pregnancy. The mother's body is significantly weakened, the immune system does not perform protective functions. This is a favorable environment for the penetration of various infections.

Therefore, the use of strong drugs is prohibited. This can make the situation worse. If a woman needs to take medicine during pregnancy, a doctor's consultation is needed.

During lactation, it is recommended to cancel the use of the drug. After all, together with milk, the active components can penetrate the baby's body. In the first months of life, this is simply an unacceptable intervention. This can lead to the development of health problems that are irreversible. Reception Haloperidol decanoate should be carried out under the supervision of a physician. But still, it is recommended to find an alternative way to solve the problem.

Contraindications

Contraindications to the use of Haloperidol Decanoate are the presence of certain health problems. So, they include neurological diseases, which may be accompanied by pyramidal and extrapyramidal symptoms.

The risk group includes pregnant women and young mothers who are breastfeeding. The penetration of active components into the body during this period is unacceptable.

These factors should be taken into account when taking medication. In some cases, by adjusting the dose, it turns out to continue or start using the medication. But this is possible only in exceptional moments.

You should not neglect the basic rules. After all, an independent increase in the dose, taking the medicine when it is prohibited can lead to the development of serious problems. That is why a person suffering from mental disorders should use Haloperidol Decanoate under someone else's guidance. This can save his life and protect him from wrong actions.

Side effects of haloperidol decanoate

Side effects of Haloperidol decanoate are represented by various manifestations from the central nervous system. She suffers mostly. So, the appearance of extrapyramidal disorders is possible. They manifest themselves in the form of increased muscle tone, akinesia and tremor.

The appearance of tardive dyskinesia is not excluded, it occurs only against the background of prolonged use of the drug. A pronounced sedative effect is also among the side effects. Severe depression may develop.

Other negative effects include a reversible increase in serum prolactin. This usually occurs when taking a large amount of medication. This factor will change for the better on its own.

If you do everything as written in the instructions, and do not take the drug in high doses, then there can be no side effects. In this case, the medicine will have the necessary effect and will not harm the body. Therefore, consultation regarding Haloperidol Decanoate is the main criterion.

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Dosage and administration

To achieve the correct effect, it is important to know the method of administration and dosage of Haloperidol Decanoate. So, the medicine is administered orally and intramuscularly. The duration of treatment depends on the individual characteristics of the organism and how the disease progresses.

The dosage is chosen in a similar way. When calculating this moment, it is necessary to take into account the doses of the drug itself and other medicines that are used as an additional remedy. It is desirable that the combination is the same. Much depends on which drug was taken before Haloperidol decanoate. After all, most likely the concentration of the previous drug in the blood plasma is still preserved.

This agent is administered at a dose of 50-200 mg once every 4 weeks. This is a drug that is designed to maintain a person's condition, after timely therapy. It does not need to be taken constantly. But, again, a lot depends on the condition of the person. In general, Haloperidol decanoate is able to help, but not completely solve the problem.

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Overdose

Does an overdose of Haloperidol Decanoate occur and what causes it? It's just that this phenomenon never occurs. Most likely, the situation is in an increase in the dose or improper administration of the drug.

The main symptoms of overdose are the manifestation of muscle rigidity and local tremor. In some cases, arterial hypotension manifests itself, sometimes arterial hypertension and drowsiness. With an extremely complex overdose, a coma, shock and respiratory depression may develop.

Treatment is carried out on the basis of the ventilator procedure. To improve blood circulation, it is necessary to inject plasma, albumin solution and norepinephrine intravenously.

Adrenaline in this case can not be taken! This can lead to serious problems. To reduce the severity of extrapyramidal disorders, it is worth using antiparkinsonian drugs for several weeks. This will remove all the unpleasant symptoms that Haloperidol Decanoate can cause.

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Interactions with other drugs

Naturally, interactions with other drugs are possible, but for this you need to know some rules. So, it is not recommended to use Haloperidol decanoate together with antihypertensive drugs. This can lead to increased action of the latter.