Description
Latin name
Fluanxol
release form
film-coated tablets
Packing
100 pcs.
Pharmacological action of
Fluconazole – antifungal.
Pharmacodynamics
Antifungal agent, has a highly specific effect, inhibiting the activity of fungal enzymes dependent on cytochrome P450. It blocks the conversion of lanosterol of fungal cells into a membrane lipid – ergosterol increases the permeability of the cell membrane, disrupts its growth and replication.
Fluconazole, being highly selective for cytochrome P450 fungi, practically does not inhibit these enzymes in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, it inhibits cytochrome P450-dependent oxidative processes in human liver microsomes to a lesser extent). It does not have antiadrogenic activity.
Active in opportunistic mycoses, incl. caused by Candida spp. (including generalized forms of candidiasis against the background of immunosuppression),mi of plasma is about 99%. With intramuscular injection of a solution for injection, Css is achieved after 3 months of use of the drug.
Flupentixol and cis (Z) -flupentixol slightly penetrate the placental barrier, excreted in small amounts with breast milk.
Metabolism
Metabolites do not have antipsychotic activity.
Excretion of
With an intramuscular injection 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.
Flupentixol metabolites do not have antipsychotic activity. They are excreted mainly with feces and, partially, with urine. T1 / 2 is approximately 35 hours.
Pharmacokinetically, a dose of Fluanxole 40 mg when administered intramuscularly once every 2 weeks is equivalent to a dose of Fluanxol 10 mg / day when taken orally for 2 weeks.
Indications
For use of the drug 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 acute reactions srdl situationally-related anxiety disorders and states of emotional stress in which a sedative / hypnotic effect is not required (especially if you suspect that the patient is predisposed to abuse of tranquilizers).
For the use of the drug in doses of 3 mg / day or more
– psychotic conditions with a predominance of hallucinations, paranoid delusions and impaired thinking, also accompanied by apathy, anergy and autism.
Contraindications – CNS depression
– acute alcohol intoxication
– acute intoxication barbiturates
– acute intoxication opioid analgesics
– coma
– pathological changes
blood – bone marrow depression
– pheochromocytoma
– collapse
– pregnancy
– lactation ( breastfeeding)
– children’s age
– hypersensitivity to the antipsychotics of the thioxanthene structure.
Patients in a state of agitation or hyperactivity should not be prescribed fluanxol in insufficiently high doses (up to 3 mg).
Use during pregnancy and lactation
Use of Fluanxole during pregnancy and lactation (breastfeeding) is possible only if the intended benefit of the therapy for the mother outweighs the potential risk to the fetus.
In newborns whose mothers took antipsychotics in the third trimester of pregnancy or during childbirth, signs of intoxication may be observed, such as lethargy, tremors, excessive irritability. In addition, such newborns have a low Apgar score.
During treatment with fluanxol, breastfeeding is allowed if clinically recognized as necessary. In such cases, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.
Composition
1 coated tablet contains:
active substance:
flupentixol dihydrochloride, which corresponds to 5 mg flupentixol.
excipients:
lactose monohydrate,
potato starch,
gelatin,
talc,
magnesium stearate.
shell:
gelatin,
sucrose,
sucrose powder,
iron oxide yellow (E172).
Dosage and administration
For the treatment of depressive and anxiety disorders, the initial dose of the drug for oral administration 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 can be increased to 2 mg / day.
The daily dose of 2 mg to 3 mg should be divided into several doses. In the absence of a therapeutic effect when using Fluanxole in a maximum dose of 3 mg / day for 1 week, the drug should be discontinued.
In the treatment of psychotic conditions, the dose is set individually, depending on the condition of the patient. 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 1 time / day in the morning.
Side effects
The incidence of side effects and their severity are most pronounced at the beginning of treatment, decrease as therapy continues.
From the nervous system: drowsiness, dizziness, headache, tremor, akathisia, parkinsonism, hypokinesia, dystonia infrequently – impaired attention, extrapyramidal disorders (mainly muscle rigidity and hyperkinesis), dyskinesia, amnesia, convulsive disorders, tardive dystonia.
From the side of mental activity: insomnia, nervousness, agitation infrequently – decreased libido, depression, confusion.
From the cardiovascular system: infrequently – palpitations, orthostatic hypotension.
From the hemopoietic organs: rarely – granulocytopenia, agranulocytosis (more likely between 4 and 10 weeks of treatment), leukopenia, hemolytic anemia.
From the side of the organs of vision: violation of accommodation, clouding of the cornea and / or lens with possible visual impairment infrequently – oculogyric crisis.
From the digestive system: dry mouth, digestive disorders (including constipation, diarrhea, dyspepsia, nausea), increased salivation, vomiting, cholestatic jaundice (more likely between 2 and 4 weeks of treatment).
Metabolic and nutritional disorders: infrequently – decreased appetite, increased appetite.
From the respiratory system: infrequently – shortness of breath.
From the endocrine system: dysmenorrhea, gynecomastia, diabetes mellitus, decreased potency, changes in carbohydrate metabolism, hot flashes.
From the urinary system: infrequently – urinary retention, painful urination.
Allergic reactions: infrequently – itching, dermatitis, skin rash, photosensitivity, increased sweating.
Disorders of the musculoskeletal system and connective tissue: infrequently – arthralgia.
From the reproductive system: infrequently – erectile dysfunction, galactorrhea.
On the part of the body as a whole: weakness, asthenia infrequently – weight gain.
There is evidence of the development of malignant antipsychotic syndrome (ZNS). The main symptoms of ZNS are hyperthermia, muscle rigidity and impaired consciousness in combination with autonomic nervous system dysfunction (labile blood pressure, tachycardia, increased sweating). In addition to the immediate cessation of antipsychotic administration, the use of general supportive measures and symptomatic treatment is imperative.
Patients on long-term treatment may develop tardive dyskinesia. Antiparkinsonian drugs do not eliminate its symptoms and may exacerbate them. Dose reduction or, if possible, discontinuation of treatment is recommended.
With persistent akathisia, benzodiazepines or propranolol may be useful.
There are few reports of the development of minor transient changes in the performance of liver function tests.
When taking flupentixol, the following side effects were also reported when taking other antipsychotics: in rare cases, prolongation of the QT interval, ventricular (ventricular) arrhythmia – ventricular fibrillation, ventricular tachycardia, sudden death and the development of paroxysms of ventricular tachycardia (Torsade de Pointes).
Drug Interaction
When used with Fluanxol, it may enhance the sedative effect of ethanol, barbiturates and other CNS depressant agents.
Fluanxol should not be used with guanetidine and agents with a similar effect, since neuroleptics may weaken their hypotensive effects.
When used with Fluanxol, it can reduce the effectiveness of levodopa and other adrenergic agents.
When fluanxol is co-administered with metoclopramide and piperazine, the risk of extrapyramidal disorders increases.
Fluanxol should not be mixed with other injectable fluids.
Overdose
Symptoms: drowsiness, hyper- or hypothermia, extrapyramidal disorders, seizures, hypotension, shock, coma are possible.
Treatment: conduct symptomatic and supportive therapy. In case of taking the drug inside it is necessary to wash the stomach as soon as possible, it is recommended to take sorbent.
Steps should be taken to support the activities of the respiratory and cardiovascular systems. Adrenaline (epinephrine) should not be used because this can lead to a subsequent decrease in blood pressure.
Seizures can be stopped with diazepam and extrapyramidal symptoms with biperiden.
Storage conditions
Store at a temperature not exceeding 30 ° C.
Expiration
3 years.
Active substances
Flupentyksol
dosage form
dosage form
tablets
