Composition, form of production and packaging
Solution for the / m introduction (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 - 15 mg, sesame oil - up to 1 ml.
1 ml - dark glass ampoules (5) - plastic pallets (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Antipsychotic drug. Haloperidol decanoate is the ester of haloperidol and decanoic acid. With the / m introduction in the course of slow hydrolysis, haloperidol is released, which then enters the systemic circulation. Haloperidol decanoate refers to neuroleptic derivatives of butyrophenone. Haloperidol is a pronounced antagonist of central dopamine receptors and refers to strong neuroleptics.
Haloperidol is highly effective in the treatment of hallucinations and delusions, due to the direct blockade of central dopamine receptors (probably acting on the mesocortical and limbic structures), affects the basal ganglia (nigrostri). Has a pronounced soothing effect in psychomotor agitation, is effective in mania and other agitations.
Limbic activity of the drug is manifested in a sedative effect; is effective as an additional remedy for chronic pain.
Exposure to the basal ganglia causes extrapyramidal reactions (dystonia, akathisia, parkinsonism).
In socially closed patients, social behavior is normalized.
The expressed peripheral antidopaminovaya 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
Suction and distribution
C max of haloperidol released from the depot of haloperidol after a / m injection is achieved after 3-9 days. With regular monthly administration, the saturation stage in plasma is achieved after 2-4 months. Pharmacokinetics with the / m introduction is dose-dependent. At doses below 450 mg, there is a direct relationship between dose and plasma concentration of haloperidol. To achieve a therapeutic effect, the concentration of haloperidol in plasma is 20-25 Ојg / l.
Haloperidol easily penetrates the BBB. Binding to plasma proteins - 92%.
Excretion
T 1/2 about 3 weeks. It is excreted through the intestine (60%) and kidneys (40%, including 1% unchanged).
INDICATIONS
- Chronic schizophrenia and other psychoses, especially when treatment with haloperidol fast action was effective and an effective neuroleptic of moderately sedative action is needed;
- Other disorders of mental activity and behavior that occur with psychomotor agitation and require long-term treatment.
DOSING MODE
The drug is intended exclusively for adults , only for the / m introduction. Do not administer the drug iv.
Haloperidol Decanoate is recommended to enter the gluteal region. Avoid administration at doses in excess of 3 ml to avoid unpleasant feelings of raspiraniya at the injection site.
Patients on long-term treatment with oral antipsychotics (mainly haloperidol) may be recommended to switch to depot injections. The dose should be selected individually due to significant differences in the response to treatment in different patients. Dose selection should be carried out with strict medical supervision of the patient. The choice of the initial dose is made taking into account the symptoms of the disease, its severity, the dose of haloperidol or other antipsychotics prescribed during the previous treatment.
At the beginning of treatment every 4 weeks, it is recommended to prescribe doses 10-15 times higher than haloperidol for intake, which usually corresponds to 25-75 mg of the drug Haloperidol Decanoate (0.5-1.5 ml). The maximum initial dose should not exceed 100 mg.
Depending on the effect, the dose can be stepped up, 50 mg, until the optimal effect is obtained. Usually, the maintenance dose corresponds to a 20-fold daily dose of haloperidol for oral administration. When the symptoms of the underlying disease recur in the period of dose selection, treatment with the drug Haloperidol Decanoate can be supplemented with haloperidol for oral administration.
Usually injections are administered every 4 weeks, however, due to large individual differences in efficacy, a more frequent use of the drug may be required.
Older patients and patients with oligophrenia are recommended a smaller initial dose, for example, 12.5-25 mg every 4 weeks. Further, depending on the effect, the dose can be increased.
SIDE EFFECT
The side effects that develop during treatment with the drug Haloperidol Decanoate are due to the action of haloperidol.
From the side of the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, arousal, fears, akathisia, euphoria or depression, lethargy, epileptic seizures, development of paradoxical reaction - exacerbation of psychosis and hallucinations; with prolonged treatment - extrapyramidal disorders, incl. late dyskinesia (smacking lips and lips, inflating cheeks, fast and wormlike movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the hands and feet), late dystonia (rapid blinking or spasms of the eyelids, unusual facial expression or position of the body, uncontrollable curving movements of the neck, trunk , hands and feet) and malignant neuroleptic syndrome (shortness or rapid breathing, tachycardia, arrhythmia, hyperthermia, increase or decrease in blood pressure, increased sweating, incontinence, rigidity muscle, epileptic seizures, loss of consciousness).
From the side of the cardiovascular system: when used in high doses - reduced blood pressure, orthostatic hypotension, arrhythmias, tachycardia, changes in the ECG (prolongation of the QT interval, signs of flutter and fibrillation of the ventricles).
On the part of the digestive system: when used in high doses - decreased appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, impaired liver function, until the development of jaundice.
From the hemopoietic system: rarely - transient leukopenia or leukocytosis, agranulocytosis, erythropenia and a tendency to monocytosis.
From the urinary system: urinary retention (with prostatic hyperplasia), peripheral edema.
On the part of the reproductive system and the breast: pain in the mammary glands, gynecomastia, hyperprolactinaemia, menstrual cycle disorder, decreased potency, increased libido, priapism.
From the side of the organ of vision: cataract, retinopathy, blurred vision.
From the metabolism: hyperglycemia, hypoglycemia, hyponatremia.
From the skin and subcutaneous tissues: maculopapular and acne-like skin changes, photosensitization.
Allergic reactions: rarely - bronchospasm, laryngospasm.
Other: alopecia, weight gain.
CONTRAINDICATIONS
- a coma;
- depression of the central nervous system caused by drugs or alcohol;
- Parkinson's disease;
- defeat of the basal ganglia;
- childhood;
- Hypersensitivity to the components of the drug.
With caution , the drug should be prescribed for decompensated diseases of the cardiovascular system (including angina pectoris, intracardiac conduction disorders, prolongation of the QT interval or predisposition to it - hypokalemia, simultaneous use of other drugs that can cause prolongation of the QT interval), epilepsy, closed-angle glaucoma, hepatic and / or renal failure, hyperthyroidism (with thyrotoxicosis), pulmonary-cardiac and respiratory failure (including COPD and acute infections ektsionnyh disease), prostatic hyperplasia with urinary retention, alcoholism.
PREGNANCY AND LACTATION
Studies conducted with the involvement of a large number of patients suggest that Haloperidol Decanoate does not cause a significant increase in the frequency of malformations. In several isolated cases, congenital malformations were observed with the use of Haloperidol Decanoate simultaneously with other drugs during the period of fetal development. The purpose of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
Haloperidol Decanoate is excreted in breast milk. The purpose of the drug during breastfeeding is possible only if the intended benefit to the mother exceeds the potential risk for the baby. In some cases, infants have developed extrapyramidal symptoms when taking the drug as a nursing mother.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug should be administered with caution to patients with renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug should be administered with caution to patients with hepatic insufficiency.
Caution is necessary when liver function is impaired. the metabolism of the drug is carried out in the liver.
APPLICATION FOR CHILDREN
The drug is contraindicated in childhood.
APPLICATION IN ELDERLY PATIENTS
Elderly patients are recommended a smaller initial dose, for example, at 12.5-25 mg every 4 weeks. Further, depending on the effect, the dose can be increased.
SPECIAL INSTRUCTIONS
In a few cases, psychiatric patients who received antipsychotics suddenly experienced sudden death.
In case of a predisposition to prolong the QT interval (QT interval prolongation syndrome, hypokalemia, use of drugs prolonging the QT interval), care should be taken during treatment because of the risk of prolonging the QT interval.
Treatment should begin with the use of oral haloperidol and only then proceed to injections of the drug Haloperidol Decanoate to detect unforeseen side reactions.
Caution is necessary when liver function is impaired. the metabolism of the drug is carried out in the liver.
With prolonged treatment, regular monitoring of liver function and blood picture is necessary.
In isolated cases, Haloperidol Decanoate caused seizures. Treatment of patients with epilepsy and conditions predisposing to convulsions (eg, head trauma, alcohol withdrawal), requires caution.
Thyroxine increases the toxicity of the drug. Treatment with the drug Haloperidol Decanoate patients suffering from hyperthyroidism is permissible only with the appropriate thyreostatic treatment.
With the simultaneous presence of depression and psychosis, or when depression dominates, Haloperidol Decanoate is prescribed along with antidepressants.
With simultaneous antiparkinsonian therapy after the end of treatment with the drug Haloperidol Decanoate, it should be continued for a few more weeks due to faster elimination of antiparkinsonian drugs.
The drug Haloperidol Decanoate is an oily solution for the / m administration, so it is forbidden to inject it IV.
During treatment, the drug is prohibited from drinking 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 application in high doses, a sedative effect of varying severity may appear with a decrease in attention, which can be aggravated by the intake of alcohol.
Care must be taken when performing heavy physical work, taking a hot bath (it is possible to develop a heat stroke due to the suppression of central and peripheral thermoregulation in the hypothalamus).
During treatment, do not take "cold" non-prescription drugs (possibly increasing the anticholinergic effects and the risk of heat stroke).
Protect open areas of the skin from excessive sunlight due to the increased risk of photosensitivity.
Treatment is stopped gradually to avoid the occurrence of withdrawal syndrome.
Impact on the ability to drive vehicles and manage mechanisms
At the beginning of treatment with the drug Haloperidol Decanoate, it is forbidden to drive and perform work associated with an increased risk of injury and / or requiring increased concentration of attention.
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 you suspect an overdose, consider the longer lasting effect of the first.
Symptoms: the development of known pharmacological effects and side effects in a more pronounced form. Symptoms that present the greatest danger are extrapyramidal reactions, a decrease in blood pressure, a sedative effect. Extrapyramidal reactions are manifested in the form of rigidity of muscles and general or localized tremor. It is often possible to raise blood pressure, rather than decrease. In exceptional cases - the development of a coma with respiratory depression and arterial hypotension, which turns into a shock-like one. Possible prolongation of the QT interval with the development of ventricular arrhythmias.
Treatment: there is no specific antidote. The passage of the airways in the development of a coma is ensured by an oropharyngeal or endotracheal probe, respiratory depression may require mechanical ventilation. Monitor the vital functions and ECG (until it is fully normalized), treat severe arrhythmias with appropriate antiarrhythmic drugs; with reduced blood pressure and stopping blood circulation - intravenous fluid, 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 AD can significantly increase, which will require immediate correction. With severe extrapyramidal symptoms - the introduction of antiparkinsonian anticholinergic agents for several weeks (possibly the resumption of symptoms after the withdrawal of these drugs).
DRUG INTERACTION
Increases the severity of the inhibitory effect on CNS ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and hypnotics, funds for general anesthesia.
Strengthens the action of peripheral m-holinoblokatorov and most antihypertensives (reduces the effect of guanetidine due to its displacement from? -adrenergic neurons and suppression of its capture by these neurons).
It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, while their (mutually) sedative effect and toxicity increase.
With simultaneous use with bupropion reduces the epileptic threshold and increases the risk of major epileptic seizures.
Reduces the effect of anticonvulsants (reducing the convulsive threshold with haloperidol).
Weaken the vasoconstrictive effect of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of ОІ-adrenoreceptors 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 increases the risk of developing mental disorders (including disorientation in space, slowing and hindering thinking processes).
Amphetamines reduce the antipsychotic effect of haloperidol, which in turn reduces their psycho-stimulating effect (haloperidol-ОІ-adrenoreceptor blockade).
Anticholinergic, antihistamine (1 generation) and anti-Parkinsonian drugs can enhance the m-cholinoblock 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 an increase in extrapyramidal symptoms.
With simultaneous administration with fluoxetine, the risk of side effects from the central nervous system increases, especially extrapyramidal reactions.
With simultaneous use with drugs that cause extrapyramidal reactions, increases the frequency and severity of extrapyramidal disorders.
The use of strong tea or coffee (especially in large quantities) reduces the effect of haloperidol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light and inaccessible to children at a temperature of no higher than 25 В° C. Shelf life - 5 years.
