1 capsule contains: Active ingredient: fluoxetine (in the form of hydrochloride) 20 mg.
Selectively blocks the reverse neuronal seizure of serotonin (5-hydroxytryptamine) in the synapses of neurons of the central nervous system. Inhibition of serotonin reuptake leads to an increase in the concentration of this neurotransmitter in the synaptic cleft, enhances and prolongs its action on postsynaptic receptor sites. It has a low affinity for α1, α2, and β-adrenergic, serotonin, dopaminergic, H1-histaminic, muscarinic, and isotropic, H. It improves mood, reduces tension, anxiety and fear, eliminates dysphoria, causes a decrease in appetite. It causes the reduction of obsessive-compulsive disorders. Does not cause orthostatic hypotension, sedation, is not cardiotoxic. Persistent clinical effect occurs after 1-2 weeks of treatment.
When ingested, the drug is well absorbed from the gastrointestinal tract. Eating does not affect the bioavailability of the drug. Cmax in plasma is reached after 6-8 hours. The drug binds well to plasma proteins - about 95% (including albumin and alpha 1-acid glycoprotein), accumulates well in tissues. The distribution of the drug is high, easily penetrates the blood-brain barrier, is excreted in breast milk (up to 25% of plasma concentration). It is metabolized in the liver by CYP2D6 isoenzyme by demethylation to the active metabolite of norfluoxetine. Metabolites are excreted by the kidneys (80%) and the intestine (15% ) mainly in the form of glucuronides. T1 / 2 fluoxetine after reaching the equilibrium concentration in plasma is 4-6 days, with a single dose - 1-4 days, T1 / 2 norfluoxetine - 4-16 days, which causes a significant cumulation of the active forms and long-term presence in the body (5-6 weeks) after discontinuation of the drug. In patients with cirrhosis, the T1 / 2 liver is 3–4 times longer.
Depression of various origins. Nervous bulimia. Obsessive-compulsive disorders (obsessive-compulsive disorder).
Hypersensitivity. The use of MAO inhibitors (in the previous 2 weeks). Hepatic and renal failure (creatinine clearance less than 10ml / min). Epilepsy and convulsive states (in history). Suicidal mood. Diabetes mellitus. Bladder atony. Closed-angle glaucoma. Prostate hypertrophy. Pregnancy. Breastfeeding. With care: Children age (safety and efficacy not established). myocardium, including in history. Cirrhosis of the liver. Older age. In case of cardiovascular diseases. Insufficiency of the liver and / or kidneys
With care: diabetes, epilepsy (including in history), excessive weight loss, Parkinson's disease, suicidal mood.
Use during pregnancy and lactation
Contraindicated during pregnancy and lactation.
Dosage and administration
Inside Persistent clinical effect is achieved after 2-3 weeks of treatment, supportive therapy can last up to 6 months. Depression: 20 mg 1 time per day in the morning. If necessary, after 3-4 weeks the dose can be increased to 20 mg 2 times a day (morning and evening). The maximum daily dose is 80 mg 1-2 times a day. Bulimic neurosis: up to 60 mg / day. Obsessive frustration: 20-60 mg / day.
CNS dizziness, headache, sleep disturbances, fatigue, asthenia, tremor, agitation, motor agitation, increased suicidal tendencies, anxiety, mania or hypomania. From the gastrointestinal tract, decreased appetite, taste disturbance, nausea, vomiting, dry mouth or hypersity, diarrhea. Allergic reactions in the form of skin rash, itching, urticaria, myalgia, arthralgia, fever. From the urogenital system, urinary incontinence or urinary retention, dysmenorrhea, vaginitis, reduction of elibido, dysfunction of men (slowed and ejaculation). Other increased sweating, tachycardia, impaired visual acuity, weight loss, systemic disorders of the lungs, kidneys or liver, vasculitis.
Symptoms: nausea, vomiting, arousal, motor restlessness, convulsive disorders, impaired function of the cardiovascular system. Treatment: specific antagonists of fluoxetine were not found. Symptomatic therapy, gastric lavage, the appointment of activated carbon, in convulsions, the appointment of tranquilizers, the maintenance of breathing, cardiac activity.
Interaction with other drugs
You can not use the drug simultaneously with MAO inhibitors, as it is possible the development of serotonin syndrome (hyperthermia, chills, increased sweating, myoclonus, hyperreflexia, tremor, diarrhea, impaired motor coordination, autonomic lability, agitation, delirium and coma). Tryptophan strengthens serotonergic drugs of the drug increased agitation, motor anxiety, disorders of the gastrointestinal tract). When used with drugs containing Hypericum perforatum (Hypericum perforatum), mustache may occur ylene serotonergic effects, increased unwanted effektov.Povyshaet plasma concentration of phenytoin, tricyclic antidepressants, maprotiline, trazodone twice (to be 50% lower dose of these drugs while the use of fluoxetine) .Usilivaet effects of alprazolam, diazepam, ethanol, hypoglycemic drugs Simultaneous intake of fluoxetine with alcohol or with centrally acting drugs that inhibit the function of the central nervous system enhances their effect and increases the risk of developing side effects. effects. Medicines containing lithium should be used with caution because of the possible increase in the concentration of lithium and the risk of toxic effects. On the background of electroconvulsive therapy, prolonged convulsive seizures may develop. When used simultaneously with drugs with a high degree of protein binding, especially with anticoagulants and digitoxin, it is possible to increase the plasma concentration of free (unbound) drugs and increase the risk of developing adverse clear effects.
Patients with concomitant diabetes may develop hypoglycemia during therapy with fluoxetine and hyperglycemia after its withdrawal. Therefore, the dose of insulin and / or any other hypoglycemic agents should be adjusted. Patients should be under the supervision of a physician before significant improvement in the treatment of diabetes mellitus. Anorexigenic effects should be considered when treating patients with a body weight deficit (progressive loss of body weight is possible). The interval between the end of therapy with MAO inhibitors and the start of treatment with fluoxetine should be at least 14 days ; between the end of treatment with fluoxetine and the start of therapy with MAO inhibitors - at least 5 weeks. In liver diseases and in the elderly, treatment should begin with 1/2 the dose. In children,adolescents and young people (under 24 years) with depression, other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing fluoxetine or any antidepressants in children, adolescents and young people (under 24 years old), the risk of suicide should be correlated with the benefits of their use. In short-term studies, the risk of suicide was not increased in people over 24 years of age, while in people over 65 years of age it was somewhat reduced. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for the purpose of early detection of abnormalities or behavioral changes, as well as suicidal tendencies. Effect on ability to drive vehicles and control mechanisms requiring increased attention and speed of mental and motor reactions.