Haloperidol decanoate solution intramuscularly 50mg 1ml N5
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Description
Solution Haloperidol Decanoate for intramuscular injection is an antipsychotic drug. Haloperidol decanoate is an ester of haloperidol and decanoic acid. When administered intramuscularly, during slow hydrolysis, haloperidol is released, which then enters the systemic circulation. Haloperidol is highly effective in treating hallucinations and delusions, due to the direct blockade of central dopamine receptors (probably acting on mesocortical and limbic structures), affects the basal ganglia (nigrostria). It has a pronounced sedative effect in case of psychomotor agitation, is effective in mania and other agitations.
Active ingredients
Haloperidol
Release form
Solution
Composition
Active ingredient: haloperidol decanoate. Excipients: benzyl alcohol, sesame oil.
Pharmacological effect
Antipsychotic drug. Haloperidol decanoate is an ester of haloperidol and decanoic acid. When i / m administration during slow hydrolysis, haloperidol is released, which then enters the systemic circulation. Haloperidol decanoate is a neuroleptic-derived butyrophenone. Haloperidol is a pronounced antagonist of central dopamine receptors and is considered a strong neuroleptic. Haloperidol is highly effective in treating hallucinations and delusions, due to the direct blockade of central dopamine receptors (probably acting on mesocortical and limbic structures), affects the basal ganglia (nigrostria). It has a pronounced sedative effect in case of psychomotor agitation, is effective in mania and other agitations. The limbic activity of the drug is manifested 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 isolated 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 prolactin inhibitory factor in the adenohypophysis).
Pharmacokinetics
Suction and distribution. Cmax of haloperidol released from the depot of haloperidol after intramuscular injection is achieved after 3-9 days. With regular monthly administration, the plasma saturation stage is reached in 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, a plasma concentration of haloperidol of 20–25 mcg / L is necessary. Haloperidol easily penetrates the BBB. Plasma protein binding - 92%. Inference. T1 / 2 about 3 weeks. Excreted through the intestines (60%) and the kidneys (40%, including 1% unchanged).
Indications
Chronic schizophrenia and other psychosis, especially when treatment with quick-acting haloperidol was effective and necessary effective neuroleptic moderately sedative, other mental disorders and behaviors occurring with psychomotor agitation and requiring long-term treatment.
Contraindications
Coma, CNS depression caused by drugs or alcohol, Parkinson’s disease, damage to the basal ganglia, children’s age, hypersensitivity to the drug’s components.
Precautionary measures
The drug should be prescribed with caution in decompensated diseases of the cardiovascular system (including angina pectoris, impaired intracardiac conduction, prolongation of the QT interval or susceptibility to this - hypokalemia, simultaneous use of other drugs that may cause prolongation of the QT 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 in ektsionnyh disease), prostatic hyperplasia with urinary retention, alcoholism.
Use during pregnancy and lactation
Studies conducted with the involvement of a large number of patients indicate that Haloperidol Decanoate does not cause a significant increase in the incidence 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. Prescribing a drug during pregnancy is possible only when the intended benefit to the mother outweighs the potential risk to the fetus.Haloperidol Decanoate is excreted in breast milk. Prescription drug during breastfeeding is possible only in the case when the intended benefits to the mother outweigh the potential risk to the infant. In some cases, babies experienced extrapyramidal symptoms when the drug was taken by a nursing mother.
Dosage and administration
The drug is intended exclusively for adults, only for intramuscular administration. It is forbidden to administer the drug intravenously. Haloperidol Decanoate is recommended to be administered in the gluteal region. Administration in doses greater than 3 ml should be avoided to avoid the unpleasant feeling of distention at the injection site. Patients undergoing long-term treatment with oral antipsychotics (mainly haloperidol) may be advised to switch to depot injections. The dose should be selected individually due to the significant differences in responses to treatment in different patients. Selection of the dose 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 administered during the previous treatment. At the beginning of treatment, every 4 weeks, it is recommended to prescribe a dose, 10-15 times higher than the dose of haloperidol for intravenous administration, 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 increased in steps, 50 mg each, until the optimum effect is obtained. A maintenance dose usually corresponds to a 20-fold daily oral dose of haloperidol. If you resume the symptoms of the underlying disease during the dose selection period, treatment with Haloperidol Decanoate can be supplemented with haloperidol for oral administration. Typically, injections are given every 4 weeks, but because of large individual differences in efficacy, more frequent use of the drug may be required. Older patients and patients with oligophrenia are recommended a lower initial dose, for example, 12.5–25 mg every 4 weeks. In the future, depending on the effect of the dose can be increased.
Side effects
Side effects that develop during treatment with the drug Haloperidol Decanoate are due to the action of haloperidol. On the part of the nervous system: headache, insomnia or drowsiness (especially at the beginning of treatment), anxiety, anxiety, agitation, fears, akathisia, euphoria or depression, lethargy, epileptic seizures, the development of a paradoxical reaction - exacerbation of psychosis and hallucinations, with prolonged treatment - extrapyramidal disorders, including tardive dyskinesia (smacking and puckering of the lips, puffing up of the cheeks, fast and worm-like movements of the tongue, uncontrolled chewing movements, uncontrolled movements of the arms and legs), late dystonia (frequent blinking or eyelid spasms, unusual facial expression or body position, uncontrollable flexing movements of the neck, body , hands and feet) and neuroleptic malignant syndrome (difficulty or rapid breathing, tachycardia, arrhythmia, hyperthermia, increased or decreased blood pressure, increased sweating, urinary incontinence, rigidity l muscle, seizures, loss of consciousness). Since the cardiovascular system: when used in high doses - lowering blood pressure, orthostatic hypotension, arrhythmias, tachycardia, ECG changes (lengthening of the QT interval, signs of trembling and ventricular fibrillation). On the part of the digestive system: when used in high doses - loss of appetite, dry mouth, hypo-salivation, nausea, vomiting, diarrhea or constipation, abnormal 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. On the part of the urinary system: urinary retention (with prostatic hyperplasia), peripheral edema. On the part of the reproductive system and the 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. Metabolism: hyperglycemia, hypoglycemia, hyponatremia. From the side of skin and subcutaneous tissues: maculopapular and acne-like skin changes, photosensitization. Allergic reactions: rarely - bronchospasm, laryngism.Other: alopecia, weight gain.
Overdose
The use of depot injections of the drug Haloperidol Decanoate is associated with a lower risk of overdose than taking oral haloperidol. Symptoms of an overdose of the drug Haloperidol Decanoate and haloperidol are the same. If an overdose is suspected, the longer duration of the first should be considered. Symptoms: the development of known pharmacological effects and side effects in a more pronounced form. The most dangerous symptoms are extrapyramidal reactions, decrease in blood pressure, sedation. Extrapyramidal reactions are manifested in the form of muscle rigidity and general or localized tremor. More often it is possible to increase blood pressure, rather than lowering. In exceptional cases - the development of a comatose state with respiratory depression and arterial hypotension, turning into a shock-like. Possible prolongation of the QT interval with the development of ventricular arrhythmias. Treatment: there is no specific antidote. The airway during the development of a comatose state is provided with an oropharyngeal or endotracheal probe, and respiratory depression may be required for respiratory depression. Vital functions and ECG are monitored (until it is fully normalized), treatment of severe arrhythmias with appropriate antiarrhythmic agents, with reduced blood pressure and circulatory arrest - by intravenous fluids, 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 may significantly increase, which will require immediate correction. For severe extrapyramidal symptoms, the introduction of antiparkinsonian anticholinergic agents for several weeks (renewal of symptoms may be possible after discontinuation of these drugs).
Interaction with other drugs
Increases the severity of the inhibitory effect on the central nervous system of ethanol, tricyclic antidepressants, opioid analgesics, barbiturates and sleeping pills, drugs for general anesthesia. Enhances the action of peripheral m-cholinoblockers and most antihypertensive drugs (reduces the effect of guanethidine due to its displacement from α-adrenergic neurons and the suppression of its capture by these neurons). It inhibits the metabolism of tricyclic antidepressants and MAO inhibitors, while their sedative effect and toxicity increase (mutually).When used simultaneously with bupropion, it reduces the epileptic threshold and increases the risk of large epileptic seizures. Reduces the effect of anticonvulsants (reduction of the seizure threshold by haloperidol). It weakens the vasoconstrictor action of dopamine, phenylephrine, norepinephrine, ephedrine and epinephrine (blockade of α-adrenoreceptors with haloperidol, which can lead to a distortion of the action of epinephrine and a paradoxical decrease in blood pressure). Reduces the effect of anti-parkinsonian 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 (may require dose adjustment). When used with methyldopa, it increases the risk of developing mental disorders (including disorientation in space, slowing down and difficulty of thinking processes). Amphetamines reduce the antipsychotic effect of haloperidol, which, in turn, reduces their psychostimulating effect (haloperidol blocking of α-adrenoreceptors). Anticholinergic, antihistamine (1st generation) and anti-Parkinsonian drugs can enhance the m-anticholinergic blocking effect of haloperidol and reduce its antipsychotic effect (dose adjustment may be required). Prolonged use of carbamazepine, barbiturates and other inducers of microsomal oxidation reduces the concentration of haloperidol in the plasma. In combination with lithium preparations (especially in high doses), encephalopathy may develop (it may cause irreversible neurointoxication) and reinforcement of extrapyramidal symptoms. When taken simultaneously with fluoxetine, the risk of side effects from the central nervous system, especially extrapyramidal reactions, increases. 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.
special instructions
In several cases, psychiatric patients who received antipsychotic drugs experienced sudden death. In case of predisposition to prolongation of the QT interval (prolongation of the QT interval, hypokalemia, use of drugs prolonging the QT interval), care should be taken during treatment because of the risk of prolongation of the QT interval.Treatment should begin with the use of oral haloperidol and only then proceed to the injection of the drug Haloperidol Decanoate to detect unforeseen adverse reactions. When abnormal liver function, be careful, because drug metabolism is carried out in the liver. With prolonged treatment requires regular monitoring of liver function and blood picture. In isolated cases, Haloperidol Decanoate caused convulsions. Treatment of patients with epilepsy and conditions that predispose to seizures (for example, a head injury, alcohol withdrawal) requires caution. Thyroxin enhances the toxicity of the drug. Treatment with Haloperidol Decanoate for patients suffering from hyperthyroidism is permissible only with appropriate thyreostatic 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 termination of treatment with Haloperidol Decanoate, it should be continued for several more weeks due to more rapid elimination of anti-Parkinsonian drugs. The drug Haloperidol Decanoate is an oil solution for the / m injection, therefore it is forbidden to enter it in / in. During treatment with a drug it is forbidden to drink alcohol. In the future, the degree of prohibition is determined on the basis of the individual response of the patient. At the beginning of drug treatment, 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 doing hard physical work, taking a hot bath (thermal shock may develop due to suppression of central and peripheral thermoregulation in the hypothalamus). During treatment, one should not take "anti-cold" non-prescription drugs (possibly increased anticholinergic effects and the risk of heat stroke). Open skin should be protected from excessive solar radiation due to increased risk of photosensitivity.Treatment is stopped gradually to prevent the onset of withdrawal. Effect on the ability to drive vehicles and control mechanisms: at the beginning 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 increased concentration.