Fluanxol oil solution intramuscularly 20 mg ml 1 ml N10
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Active ingredients
Flupentixol
Release form
Solution
Composition
1 ml of cis (Z) -flupentixol decanoate 20 mg. Excipients: triglycerides with medium chains.
Pharmacological effect
Antipsychotic agent (neuroleptic), a derivative of thioxanthene with a pronounced antipsychotic, activating and anxiolytic action. The antipsychotic action of neuroleptics is associated with the blockade of dopamine receptors, but, perhaps, with the blockade of serotonin 5-HT receptors. Fluanxol reduces the main symptoms of psychosis, incl. hallucinations, paranoid delusions and thinking disorders. The antipsychotic effect of Fluanxol begins to manifest when the drug is used orally at a dose of 3 mg / day; the intensity of the action increases with increasing dose as with ingestion and with i / m administration. Fluanxol has disinhibiting (anti-antacistic and activating) properties, as well as weakens secondary mood disorders, which activates patients with depressive symptoms, increases their communicability and facilitates social adaptation. In small and medium doses (up to 25 mg / day when taken orally and up to 100 mg intramuscularly 1 time every 2 weeks), the drug does not have a sedative effect, but in high doses it can cause a nonspecific sedation. When administered in small doses (up to 3 mg / day), the drug has an antidepressant effect. Fluanxol solution for i / m injection of oil is intended for depot injection, being the deposited form of flupentixol. In this dosage form, the drug has a significantly longer duration of action than Fluanxol in the form of pills, and allows continuous antipsychotic therapy, which is especially important for the treatment of patients who do not follow medical prescriptions. The use of Fluanxol in the form of a solution for i / m administration prevents frequent recurrences associated with the voluntary interruption of treatment by patients while taking the drug inside. Fluanksola injections can be performed at intervals of 2-4 weeks.
Pharmacokinetics
Absorption: After oral ingestion, Cmax of flupentixol in plasma is reached in 3-6 hours. Bioavailability is about 40%. After i / m administration of cis (Z) -flupentixol, decanoate is subjected to enzymatic cleavage into the active component of cis (Z) -flupentixol and decanoic acid. Cmax of cis (Z) -flupentixol in serum is reached by the end of the first week after injection. Distribution: The apparent Vd is about 14.1 l / kg. Plasma protein binding is about 99%.With the / m injection of Css injection for injections is achieved after 3 months of use of the drug. Flupentiksol and cis (Z) -flupentixol slightly penetrate the placental barrier, in small quantities are excreted in breast milk. Metabolism: Metabolites do not possess neuroleptic activity. Withdrawal: With i / m administration of the injection solution, the serum concentration curve decreases exponentially with a T1 / 2 of about 3 weeks, which reflects the rate of release of flupentixol from the depot. Metabolites flupentiksola not possess antipsychotic activity. Excreted mainly in the feces and, in part, with the urine. T1 / 2 is about 35 hours. A pharmacokinetic dose of Fluanxol 40 mg when given i / m once every 2 weeks is equivalent to Fluansol 10 mg / day when taken orally for 2 weeks.
Indications
For oral administration in doses up to 3 mg / day - mild to moderate depression with anxiety, asthenia and lack of initiative - chronic neurotic disorders with anxiety, depression and apathy - psychosomatic disorders with asthenic reactions. For oral administration at a dose of 3 mg / day or more - schizophrenia and schizophrenia-like psychosis with a predominance of hallucinatory symptoms, delusions, thinking disorders, also accompanied by apathy, anergy, decreased mood and autism. For intramuscular administration, schizophrenia and other psychotic states occurring with hallucinations, delusions and thinking disorders, accompanied by apathy, anergy, decreased mood and autism.
Contraindications
- vascular collapse - depression of consciousness of any origin (including caused by alcohol, barbiturates or opioid analgesics) - coma - childhood and adolescence under 18 years old - hypersensitivity to the components of the drug - hypersensitivity to phenothiazines - hereditary intolerance to galactose and / or fructose deficiency of lactase lapp deficiency of sucrase and isomaltase, impaired absorption of glucose and galactose (when taking pills). To be used with care in patients with organic brain diseases, convulsive disorders, incl. with epilepsy (as a result of lowering the threshold of convulsive readiness, an increase in seizures is possible) with severe hepatic insufficiency with hypokalemia, hypomagnesia and cardiovascular diseases in history (risk of transient reduction in blood pressure), includingwith prolonged QT interval, bradycardia less than 50 beats / min, with recent acute myocardial infarction, with uncompensated heart failure, and with arrhythmias, risk factors for the development of stroke by glaucoma (and a predisposition to it) with gastric ulcer and duodenal ulcer, and with a predisposition to it with gastric ulcer and duodenal ulcer with a risk of developing insult to glaucoma (with a predisposition to it) with gastric ulcer and duodenal ulcer, and with a predisposition to it with gastric ulcer and duodenal ulcer with a risk of developing insult to glaucoma (with a predisposition to it) with gastric ulcer and duodenal ulcer, and with a predisposition to it with gastric ulcer and duodenal ulcer with a risk of developing insult to glaucoma (with a predisposition to it) action on the central nervous system) with pheochromocytoma with leukopenia and respiratory disorders associated with acute infectious diseases, bronchial asthma or pulmonary emphysema in Parkinson’s disease (increased extra pyramidal effects) with urinary retention, benign prostatic hyperplasia with clinical symptoms (urinary retention risk) with Reye's syndrome (increased risk of hepatotoxicity) in pregnancy, lactation (breastfeeding). It is not recommended to prescribe Fluanxol in a dose of up to 25 mg / day to patients in a state of psychomotor agitation, since the activating effect of Fluanxol in small doses (when administered orally up to 3 mg / day or when i / m administration of 10-20 mg 1 time every 2 weeks) can lead to an exacerbation of these symptoms.
Use during pregnancy and lactation
Use of Fluanxol during pregnancy and lactation (breastfeeding) is possible only in cases where the intended benefit of therapy for the mother outweighs the potential risk to the fetus. Newborns whose mothers took antipsychotics in the third trimester of pregnancy or during childbirth may show signs of intoxication, such as lethargy, tremor, excessive irritability. In addition, these newborns have a low Apgar score. Breast-feeding is allowed during treatment with Fluanxol if this is deemed clinically necessary. In such cases, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.
Dosage and administration
For oral administration in a dose of up to 3 mg / day With mild to moderate depression with anxiety, asthenia and lack of initiative; chronic neurotic disorders with anxiety, depression, and apathy; psychosomatic disorders with asthenic reactions, the initial dose of the drug is 1 mg 1 time / day in the morning or 500 mcg 2 times / day. In the absence of a satisfactory therapeutic effect after 1 week, the dose may be increased to 2 mg / day.The daily dose, comprising from 2 mg to 3 mg, should be divided into several doses. For elderly patients, the recommended daily dose is 0.5-1.5 mg. The therapeutic effect usually occurs within 2-3 days. If at reception of the maximum dose of 3 mg / day the effect is not observed within a week, then the drug should be canceled. For oral administration in a dose of 3 mg / day or more. When treating psychotic conditions, the dose is set individually, depending on the patient's condition. At the beginning of treatment, it is recommended to use the drug in low doses, which then, depending on the patient's response to treatment, quickly increase to achieve the optimal clinical effect. The initial daily dose is 3-15 mg in 2-3 doses. If necessary, the dose can be increased to 20-30 mg / day. The maximum daily dose is 40 mg. For maintenance therapy, the drug is used in a dose of 5-20 mg / day. For intramuscular administration. The solution for intramuscular injection is introduced deep intramuscularly into the upper outer quadrant of the buttock. It is not recommended to inject into other muscles. If the required volume of the solution exceeds 2 ml, it is recommended to divide it into 2 parts and make 2 injections. The drug in the form of a solution for i / m injection of 20 mg / ml is usually administered in a dose of 20-40 mg (1-2 ml) every 2-4 weeks. Some patients may need higher doses or shorter intervals between injections. With exacerbation or acute recurrence of the disease, it may be necessary to administer the drug in a dose of up to 400 mg at one time at intervals of 2 or even 1 week. Switching from Fluanxol for oral administration to intramuscular injection. Daily dose (mg) of the oral preparation x 4 = single dose (mg) of the solution for intramuscular injection every 2 weeks. At the same time, during the 1st week after the 1st injection, the drug should be continued to be taken orally, but in a reduced dose. Subsequent doses and intervals between injections are set in accordance with the clinical effect. The maximum dose Fluanksola with the / m introduction is 400 mg simultaneously with an interval between injections in 1 week. Patients who are transferred from therapy with depo-forms of other drugs should receive Fluanxol taking into account the following ratios: 40 mg of flupentixol decanoate is equivalent to 25 mg of flufenazine decanoate, 200 mg of suklopentyxol decanoate or 50 mg of haloperidol decanoate.
Side effects
Nervous system disorders: drowsiness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia, speech disorders, depression, insomnia, nervousness, agitation; sometimes - dizziness, attention disorders, extrapyramidal disorders (mainly muscular rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, aggression, decreased libido, confusion; rarely - late dystonia. It should be borne in mind that when using neuroleptics, including flupentiksol, in rare cases, the development of the NNS. The main symptoms of ZNS are: hyperthermia, muscle rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, increased sweating). When these symptoms appear, an urgent withdrawal of the neuroleptic and the appointment of symptomatic and supportive therapy is necessary. With prolonged drug treatment may develop tardive dyskinesia. Anti-Parkinsonian drugs do not eliminate its symptoms and may aggravate them. A dose reduction or, if possible, discontinuation of treatment is recommended. Benzodiazepines or propranolol may be effective in persisting actatisia. In the first few days after the injection and in the early stages of treatment, motility disorders may occur. In most cases, such effects are controlled by dose reduction and / or anti-Parkinsonian drugs. However, the routine use of anti-parkinsonian drugs for the prevention of side effects is not recommended. Transient insomnia or anxiety can be observed especially if patients have previously taken neuroleptics with a sedative effect. Since the cardiovascular system: sometimes - orthostatic hypotension, tachycardia; in rare cases (like when taking other antipsychotics) - prolongation of the QT interval, ventricular arrhythmia (ventricular fibrillation, ventricular tachycardia, development of paroxysmal ventricular tachycardia of the "pirouette" type, sudden death). On the part of the blood system: rarely - granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia. On the part of the organ of vision: disturbance of accommodation, corneal clouding and / or lens with possible visual impairment; sometimes - oculogy crisis, accommodation paresis. On the part of the digestive system: dry mouth, digestive disorders (includingconstipation, diarrhea, dyspepsia, nausea), increased salivation, dysphagia, vomiting, cholestatic jaundice (more likely between 2 and 4 weeks of treatment), loss of appetite; in isolated cases - slight transient changes in the functional liver function tests. On the part of the endocrine system: galactorrhea, gynecomastia, dysmenorrhea, impotence, decreased libido, increased appetite, weight gain, hot flashes, changes in carbohydrate metabolism. On the part of the urinary system: sometimes - urinary retention, painful urination. From the musculoskeletal system: sometimes - arthralgia. On the part of the reproductive system: sometimes - erectile dysfunction. Allergic reactions: sometimes - itching, skin rash, dermatitis, photosensitivity, increased sweating. Local reactions: rarely - erythema, swelling, inflammation or abscess. Others: weakness, asthenia.
Overdose
Symptoms: drowsiness, hyper- or hypothermia, extrapyramidal disorders, convulsions, shock, coma are possible. When taken simultaneously with drugs that affect cardiac activity, ECG changes, prolongation of the QT interval, ventricular arrhythmias, incl. arrhythmia type "pirouette", cardiac arrest. Treatment: conduct symptomatic and supportive therapy. In the case of taking the drug inside it is necessary to wash the stomach as soon as possible, it is recommended to take a sorbent. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use epinephrine (adrenaline), because this can lead to a subsequent decrease in blood pressure. Spasms can be stopped by diazepam, and extrapyramidal symptoms - biperidenom.
Interaction with other drugs
With simultaneous use Fluanxol may enhance the sedative effect of ethanol, barbiturates and other means that have a inhibitory effect on the central nervous system. Fluanxol should not be used in conjunction with guanethidine and agents with a similar effect, because antipsychotics can weaken their hypotensive action. Tricyclic antidepressants and neuroleptics (including Fluanksol) mutually inhibit metabolism. The simultaneous use of neuroleptics and lithium increases the risk of neurotoxicity.With simultaneous use Fluanxol can reduce the effectiveness of levodopa and the action of adrenergic agents. With simultaneous use of Fluanxol with metoclopramide and piperazine increases the risk of extrapyramidal disorders. Prolongation of the QT interval, characteristic of antipsychotic therapy, may increase while taking drugs that have the same effect, including antiarrhythmics IA and III classes (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and antibiotics of the quinolone series (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), cisapride, lithium preparations. It is necessary to avoid simultaneous administration of Fluanxol and the listed drugs. With simultaneous use with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of flupentixol or flupentixol decanoate in the blood plasma, the risk of prolongation of the QT interval and the occurrence of life-threatening arrhythmias may increase. Pharmaceutical interaction Fluanxol in the form of a solution for i / m injection should not be mixed with deposited forms based on sesame oil, because this may have a significant effect on the pharmacokinetics of the drugs administered.
special instructions
In the case of prior treatment with neuroleptics or tranquilizers with a sedative effect, their intake should be stopped gradually. With long-term therapy, especially with the use of Fluanxol in high doses, it is necessary to carefully monitor and periodically assess the condition of patients in order to timely adjust the maintenance dose. With the concomitant treatment of diabetes, the prescription of Fluanxole may require correction of the insulin dose. Influence on the ability to drive motor vehicles and control mechanisms During the period of treatment, the patient should avoid practicing potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.