Antidepressant agent. Selectively inhibits the reuptake of serotonin, which leads to an increase in its concentration in the synaptic cleft, amplification and prolongation of action at postsynaptic receptors. Boosting serotonergic transmission, for negative feedback mechanism inhibits fluoxetine exchange neurotransmitter. With prolonged use of fluoxetine inhibits the activity of 5-HT1 receptors. Has little effect on the reuptake of norepinephrine and dopamine. It has no direct action on serotonin, m-cholinergic, H1-histamine and alpha-adrenergic receptors.
Unlike most antidepressants do not cause a decrease in the activity of postsynaptic beta-adrenergic receptors.
Effective with endogenous depression and obsessive-compulsive disorders. It improves mood, reduces stress, anxiety and feelings of fear, eliminates dysphoria. Has anorectic effect, can cause weight loss. It does not cause orthostatic hypotension, sedation, nekardiotoksichen. Stable clinical effect occurs within 1-2 weeks of treatment.
1 capsule contains:
Actives – fluoxetine hydrochloride 22.36 mg per mg of fluoxetine 20.00;
Excipients – corn starch, lactose monohydrate (milk sugar), magnesium stearate;
Capsules Hard gelatin № 3, including: gelatine, titanium dioxide, indigo carmine.
– depression of various etiology;
– bulimia nervosa;
– obsessive-compulsive disorder.
– simultaneous reception of monoamine oxidase inhibitors (MAO) and for 14 days after their withdrawal;
– simultaneous reception thioridazine (and within 5 weeks after discontinuation of fluoxetine), pimozide;
– liver failure;
– renal failure (creatinine clearance less than 10 mL / min);
– atony of the bladder;
– closure glaucoma;
– prostatic hyperplasia;
– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
– up to age 18 years.
Suicide risk: in depression there is a possibility of suicide attempts, which may persist until the onset of stable remission. Individual cases of suicidal thoughts and suicidal behavior have been described against the background of treatment with fluoxetine or shortly after its closure, similar to the effect of other drugs close pharmacological action (antidepressants). Careful monitoring of patients at risk. Physicians should convince patients to immediately report any thoughts and feelings that cause anxiety.
Epileptic seizures: as in the case of other antidepressants, fluoxetine should be used with caution in patients who have previously observed seizures.
Hyponatremia: there were cases hyponatremia (in some cases in the serum sodium concentration was less software mmol / l). Basically similar cases occurred in elderly patients and in patients treated with diuretics, due to a decrease in circulating blood volume.
Glycemic control: patients with diabetes during fluoxetine treatment of hypoglycemia was observed, and after discontinuation of the drug developed hyperglycemia. At the beginning or after the end of treatment with fluoxetine may require an adjustment of dose of insulin and / or hypoglycemic agents for oral administration.
Hepatic / renal failure: fluoxetine undergoes extensive metabolism in the liver and excreted by the kidneys. Patients with severe liver function impairment is recommended to prescribe a lower dose of fluoxetine or to prescribe a drug through the day. With fluoxetine at 20 mg / day for two months, patients with severe renal function (creatinine clearance < 10 ml / min) requiring hemodialysis showed no differences concentration of fluoxetine and norfluoxetine plasma from healthy persons having normal kidney function.
Body as a Whole: autonomic symptoms (dry mouth, sweating and vasodilation, chills), hypersensitivity (itching, skin rash, urticaria, anaphylactic reactions, vasculitis, reaction such as serum, angioedema), serotonin syndrome (characterized by a complex clinical manifestations of mental status changes and neuromuscular activity in combination with impaired autonomic nervous system), photosensitivity, erythema multiforme exudative).
Cardiovascular system: palpitations, arrhythmia.
Digestive System: gastrointestinal disorders (diarrhea, nausea, vomiting, dysphagia, dyspepsia, taste perversion), a very rare idiosyncratic hepatitis.
Endocrine system: abnormal secretion of antidiuretic hormone.
Blood and lymphatic system: ecchymosis.
Errors of Metabolism and Nutrition: loss of body weight.
Musculoskeletal system: arthritis, bone pain, bursitis, leg cramps, arthritis, myasthenia, myopathy, osteomyelitis, osteoporosis, rheumatoid arthritis.
Nervous system: abnormal movement / tremor (twitching, ataxia, Bucco-glosalny Syndrome, myoclonus, tremor), anorexia, anxiety and its symptoms (palpitations, restlessness, nervousness, agitation), dizziness, fatigue (somnolence, asthenia), impaired concentration process and thinking (including depersonalization), manic rastrojstva, sleep disorders (abnormal dreams, insomnia), seizures.
Respiratory system: yawning.
Senses: visual disturbances (blurred vision, mydriasis).
Genitourinary system: urinary disorders (including change in the frequency of urination), priapism / prolonged erection, sexual dysfunction (decreased libido, delayed or absence of ejaculation, anorgasmia, impotence).
How to accept, acceptance rate and dosage
Depression. initial recommended dose is 20 mg / day 1 times. If necessary, increase the dose of 20 mg / day weekly. The maximum daily dose of 80 mg in 2-3 doses.
Bulimia. The recommended dose is 60 mg / day in 3 divided doses.
Obsessive-Compulsive Disorder. recommended dose is 20-60 mg / day.
All readings. The recommended dose may be reduced or increased. Dosages greater than 80 mg / day not been systematically studied.
Age. There are no data on the need to change the dose depending on the age.
Eating. Fluoxetine can be taken at any time, regardless of the meal.
Associated diseases and / or concomitant therapy. in patients with impaired liver function, concomitant diseases, or taking other drugs, the dose should be reduced and to reduce the frequency of administration.
In a dry, dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.
Fluoxetine and its major metabolite norfluoxetine have long half-lives that must be considered in combination with other drugs fluoxetine, as well as its replacement with another antidepressant.
Phenytoin. They were identified changes in the blood concentration of phenytoin in the combination with fluoxetine. In some cases, we observed symptoms of intoxication. Increasing the dose of phenytoin or fluoxetine during their simultaneous appointment should be made with caution and under the control of the dynamics of clinical status.
Serotonergic drugs. Simultaneous treatment with serotonergic drugs (e.g., tramadol and triptans) enhances the probability of serotonin syndrome. Simultaneous treatment with triptans also contributes to increase the likelihood of developing coronary vasoconstriction and hypertension.
Benzodiazepines. With simultaneous use of fluoxetine and benzodiazepines may increase the half-life period of the past. In a joint reception of alprazolam and fluoxetine showed an increase in the blood concentration of alprazolam and strengthening of its sedative action.
Lithium and tryptophan. Known cases of development of serotonin syndrome while taking selective serotonin reuptake inhibitors (SSRIs) and lithium, or tryptophan, and therefore the co-administration of fluoxetine with these drugs should be done with caution. When simultaneous administration of fluoxetine and lithium needs more frequent and careful monitoring of the clinical condition.
Drugs metabolized with isoenzyme CYP2D6 (propafenone, carbamazepine, tricyclic antidepressants). Note that fluoxetine metabolism (as tricyclic antidepressants and selective serotonergic antidepressants) is carried out with the participation liver cytochromes CYP2D6 isoenzyme system. Simultaneous administration of drugs, the main of which is by biotransformation metabolism involving SYP2D6 isoenzyme, and having a small therapeutic dose interval (such as propafenone, carbamazepine, tricyclic antidepressants), should be conducted using the minimum therapeutic dose. The foregoing also applies in the case if it took less than 5 weeks after discontinuation of fluoxetine.
Indirect anticoagulants and other agents affecting the blood clotting system (non-steroidal anti-inflammatory agents, acetylsalicylic acid). It is known to change anticoagulant actions (on laboratory parameters and / or clinical manifestations) without any common characteristic trend, but with probability amplification bleeding while receiving oral anticoagulants, and fluoxetine. The functional state of the blood coagulation system in patients receiving warfarin should be closely monitored when starting or stopping fluoxetine.
Electroconvulsive therapy (ECT). There are rare reports of an increase in the duration of seizures in patients on fluoxetine receiving ECT and, in this connection, it is recommended to be careful.
Alcohol. In experimental studies, fluoxetine did not contribute to an increase in the concentration of alcohol in the blood, as well as enhance the effects of alcohol. However, the concomitant use of SSRIs and alcohol is not recommended.
Funds on the basis of the plant Hypericum perforatum. As applied to other SSRIs may develop pharmacodynamic interaction between fluoxetine and means based on plant Hypericum perforatum, which may lead to increased unwanted actions.
In the treatment of patients with deficiency of body weight should be considered anorectic effects of fluoxetine (possible progressive loss of body weight).
In patients with diabetes mellitus appointment fluoxetine increases the risk of hypoglycemia; with its abolition – hyperglycemia. In this regard, the dose of insulin and / or any other hypoglycemic drugs used in, should be adjusted. Patients should be under a doctor’s supervision.
The interval between the end of therapy, monoamine oxidase inhibitors and MAO starting treatment with fluoxetine must be at least 14 days; between the end and the beginning of treatment with fluoxetine therapy MAO inhibitors – at least 5 weeks.
It requires careful monitoring of patients with suicidal tendencies, especially early in treatment. The highest risk of suicide in patients previously treated with other antidepressants, and patients during therapy with fluoxetine is noted excessive fatigue, hypersomnia, or restlessness.
In carrying out ECT in patients receiving fluoxetine may be prolonged epileptic seizures.
During the treatment should refrain from drinking alcohol and classes of potentially hazardous activities that require attention and speed of mental and motor responses.
In children, adolescents and young adults (under 24 years) with depression and other mental disorders antidepressants compared to placebo increased the risk of suicidal thoughts or suicidal behavior. Therefore, the appointment of fluoxetine or any other antidepressant in children, adolescents and young adults (under 24 years) should be related to the risk of suicide and the use of their applications. In short-term studies in people older than 24 years, the risk of suicide did not increase, and people older than 65 years is somewhat reduced. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants of all patients should be monitored for early detection of faults or changes in behavior and suicidal tendencies.
It reported the occurrence of skin rashes, anaphylactic reactions, and progressive systemic disorders, sometimes with involvement in serious pathological process of the skin, kidney, liver and lung in patients treated with fluoxetine. When a skin rashes or other possible allergic reactions, the etiology of which can not be determined, fluoxetine reception should be canceled.