Active substanceFluoxetineFluoxetine
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  • Dosage form: & nbspcapsules
    Composition:
    Active substance:
    fluoxetine hydrochloride 11.2 mg, equivalent to 10 mg fluoxetine; fluoxetine hydrochloride 22.4 mg, equivalent to 20 mg fluoxetine;
    Auxiliary substances: lactose monohydrate (milk sugar) 30.8 mg / 61.6 mg, microcrystalline cellulose 16.1 mg / 32.2 mg, silicon dioxide colloid (aerosil) 0.15 mg / 0.30 mg, magnesium stearate 0 , 6 mg / 1.2 mg, talc 1.15 mg / 2.30 mg;
    the composition of the capsule with a dosage of 10 mg: gelatin 36.44 mg, titanium dioxide 1.52 mg, indigocarmine 0.04 mg;
    the composition of the capsule with a dosage of 20 mg: gelatin 36.44 mg, titanium dioxide 1.52 mg, dye azorubin 0.03 mg, dye crimson (Ponso 4R) 0.01 mg, dye blue. patent 0.05 mg and dye diamond black 0.06 mg.

    Description:
    Hard gelatin capsules. For a dosage of 10 mg: with a white body and a blue lid; for a dosage of 20 mg: with a body of white color and a lid of blue color. The contents of capsules are white or almost white powder.

    Pharmacotherapeutic group:antidepressant
    ATX: & nbsp

    N.06.A.B.03   Fluoxetine

    Pharmacodynamics:
    Antidepressant group selective serotonin reuptake inhibitors.
    Has a timoanaleptic and stimulating effect.
    Pharmacodynamics. Selectively blocks the reverse neuronal capture of serotonin (5HT) in the synapses of neurons of the central nervous system. Inhibition of reuptake of serotonin leads to an increase in the concentration of this neurotransmitter in the synaptic cleft, enhances and prolongs its effect on postsynaptic receptor sites. Increasing serotonergic transmission, by the mechanism of negative membrane communication fluoxetine inhibits neuromediator metabolism.With prolonged use fluoxetine inhibits the activity of 5-HT1-receptors. Poorly affects the re-uptake of norepinephrine and dopamine. It has no direct effect on serotonin, m-cholinergic, H1-histamine and alpha-adrenergic receptors. Unlike most antidepressants, there is no decrease in activity of postsynaptic beta-adrenergic receptors.
    Effective with endogenous depression and obsessive-compulsive disorders. Has an anorexigenic effect, can cause weight loss. Does not cause orthostatic hypotension, sedation, non-cardiotoxic. A persistent clinical effect occurs after 1 to 2 weeks of treatment.

    Pharmacokinetics:When ingested, the drug is well absorbed from the gastrointestinal tract (up to 95% of the dose taken), use with food slightly inhibits absorption of fluoxetine. The maximum concentration in the blood plasma is reached after 6-8 hours. Bioavailability of fluoxetine after ingestion is more than 60%. The drug is well accumulated in tissues, easily penetrates the blood-brain barrier, binding to plasma proteins is more than 90%.Metabolised in the liver by demethylation to the active metabolite of norfluoxetine and a number of unidentified metabolites. It is excreted by the kidneys in the form of metabolites (80%) and intestine (15%), mainly in the form of glucuronides. The half-life of fluoxetine after reaching the equilibrium concentration in the blood plasma is about 4-6 days. The half-life of the active metabolite of norfluxetine for a single dose and after reaching the equilibrium concentration in the blood plasma is from 4 to 16 days. In patients with liver failure, the half-life of fluoxetine and norfluoxetine is prolonged
    Indications:
    Depression of various genesis.
    Obsessive-compulsive disorder
    Bulimic neurosis.

    Contraindications:
    • Hypersensitivity to the drug.
    • Simultaneous reception with monoamine oxidase MAO inhibitors (and within 14 days after their cancellation),
    • Simultaneous reception of thioridazine (and within 5 weeks after the abolition of fluoxetine), pimozide.
    • Pregnancy.
    • Breastfeeding period.
    • Severe renal impairment (creatinine clearance less than 10 ml / min).
    • Liver failure.
    • Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.
    • Age to 18 years.

    Carefully:
    Suicidal risk: with depression, there is a possibility of suicide attempts, which can persist until the onset of stable remission. Separate cases of suicidal thoughts and suicidal behavior are described against the background of therapy or soon after its termination, similar to the action of other drugs of close pharmacological action (antidepressants). Careful monitoring of patients at risk is necessary. Physicians should convince patients to immediately report any thoughts and feelings of concern.
    Epileptic seizures: Flouxetin should be administered with caution to patients who have had epileptic seizures.
    Hyponatremia: cases of hyponatremia have been reported. In most cases, such cases were observed in elderly patients and in patients taking diuretics, due to a decrease in the volume of circulating blood.
    Diabetes mellitus: glycemic control in diabetics during the treatment with fluoxetine showed hypoglycemia, after the withdrawal of the drug, hyperglycemia developed.At the beginning or after treatment with fluoxetine, you may need to adjust the dosages of insulin and / or hypoglycemic drugs for oral administration. Renal / hepatic insufficiency: fluoxetine is metabolized in the liver and excreted by the kidneys and through the gastrointestinal tract. Patients with severe impairment of liver function are recommended to prescribe lower doses of fluoxetine, or to prescribe the drug every other day. When taking fluoxetine at a dose of 20 mg / day for two months, there was no difference in fluoxetine concentrations and
    norfluoxetine in the blood plasma of healthy individuals with normal kidney function and patients with severe renal dysfunction (creatinine clearance 10 ml / min) in need of hemodialysis.

    Dosing and Administration:
    The drug is taken orally, at any time, regardless of food intake.
    Depressive state
    The initial dose is 20 mg once a day in the morning, regardless of food intake. If necessary, the dose can be increased to 40-60 mg / day, divided into 2-3 receptions (20 mg / day weekly). The maximum daily dose is 80 mg in 2 to 3 doses.
    The clinical effect develops 1 to 2 weeks after the start of treatment, in some patients it can be achieved later.
    Obsessive-compulsive disorders:
    The recommended dose is 20-60 mg per day.
    Bulimic neurosis
    The drug is used in a daily dose of 60 mg, divided into 2-3 doses.
    The use of the drug by patients of different ages
    There are no data on dose changes depending on age. Begin the treatment of elderly patients with a dose of 20 mg / day.
    Accompanying illnesses
    Assign fluoxetine patients with impaired hepatic or renal function are recommended with the use of low doses and lengthening the interval between doses (see the section "With caution").

    Side effects:
    When fluoxetine is used, as in the case of the use of drugs of the group of selective serotonin reuptake inhibitors, the following undesirable effects are noted.
    From the side of the cardiovascular system
    Often (> 1% - <10%): atrial flutter, hot flashes (hot flushes).
    Infrequently (> 0,1% - <1%): hypotension.
    Rarely (<0.1%): vasculitis, vasolilation.
    From the side of the digestive system Very often (> 10%) diarrhea, nausea.
    Often (> 1% - <10%): dry mouth, indigestion, vomiting.
    Infrequently (> 0.1% - <1%): dysphagia, a taste perversion.
    Rarely (<0.1%): pain along the esophagus.
    From the hepatobiliary system Rarely (<0.1%): idiosyncratic hepatitis.
    From the immune system:
    Very rarely (<0.1%): anaphylactic reactions, serum sickness.
    Metabolic and nutritional disorders
    Often (> 1% - <10%): anorexia (including weight loss) of the body.
    From the musculoskeletal system infrequently (> 0.1% - <1%): muscle twitching.
    From the side of the central nervous system
    Very often (> 10%): headache.
    Often (> 1% - <10%): attention disturbance, dizziness, lethargy, drowsiness (including hypertonia, sedation), tremor.
    Infrequently (> 0.1% - <1%): psychomotor agitation, hyperactivity, ataxia, impaired coordination, bruxism, dyskinesia, myoclonus.
    Rarely (<0.1%): bucco-glossal syndrome, seizures, serotonin syndrome.
    Mental disorders
    Very often (> 10%): insomnia (including early morning awakening, primary and secondary insomnia).
    Often (> 1% - <10%): unusual dreams (including nightmares), nervousness, tension, decreased libido (including lack of libido), euphoria, sleep disorder.
    Infrequently (> 0,1% - <1%): depersonalization, hypertension, violation of orgasm (including anorgasmia), impaired thinking.
    Rarely (<0.1%): manic disorders.
    From the skin
    Often (> 1% - <10%): hyperhidrosis, itchy skin, polymorphous skin rash, urticaria. Infrequently ((> 0,1% - <1%): ecchymosis, tendency to bruising, alopecia, cold sweat.
    Rarely (<0.1%): angioedema, photosensitivity reactions.
    From the sense organs
    Often (> 1% - <10%): blurred vision.
    Infrequently ((> 0,1% - <1%): mydriasis.
    From the genitourinary system
    Often (> 1% - <10%): frequent urination (including pollakiuria), ejaculation disorder (including lack of ejaculation, dysfunctional ejaculation, early ejaculation, ejaculation delay, retrograde ejaculation), erectile dysfunction, gynecological bleeding (including bleeding from the cervix, dysfunctional uterine bleeding, bleeding from the genital tract, menometrorrhagia, menorrhagia, metrorrhagia, polymenorrhoea, postmenopausal bleeding, uterine bleeding, vaginal bleeding).
    Infrequently (> 0.1% - <1%): dysuria.
    Rarely (<0.1%): sexual dysfunction, priapism.
    Post-marketing messages
    From the side of the endocrine system, cases of an antidiuretic hormone deficiency were noted.
    These side effects often occur at the beginning of fluoxetine therapy or with an increase in the dose of the drug.

    Overdose:
    Symptoms: psychomotor agitation, convulsive attacks, drowsiness, heart rhythm disturbances, tachycardia, nausea, vomiting.
    Other serious symptoms of fluoxetine overdose (both with isolated fluoxetine intake and simultaneous admission with other drugs) included coma, delirium, QT interval prolongation and ventricular tachyarrhythmia, including fibrillation-ventricular flutter and cardiac arrest, lowering blood pressure, fainting, mania, pyrexia, stupor and a condition similar to malignant neuroleptic syndrome
    Treatment: specific antagonists to fluoxetine have not been found. Symptomatic therapy, gastric lavage with the appointment of activated charcoal, with convulsions - diazepam, maintaining breathing, cardiac activity, body temperature.

    Interaction:
    Fluoxetine and its main metabolite, norfluoxetine, have long half-lives,that must be taken into account when combining fluoxetine with other drugs, as well as when replacing it with another antidepressant.
    Do not use the drug simultaneously with monoamine oxidase (MAO) inhibitors, including antidepressants - MAO inhibitors; furozolidone, procarbazine, seleggins, as well as tryptophan (a precursor of serotonin), since it is possible to develop a serotonergic syndrome manifested in confusion, hypomania, psychomotor agitation, convulsions, dysarthria, hypertensive crises, chills, tremor, nausea, vomiting, diarrhea.
    After using MAO inhibitors, administration of fluoxetine is allowed no earlier than 14 days. Do not use MAO inhibitors earlier than 5 weeks after fluoxetine withdrawal.
    Simultaneous reception of drugs metabolized with the participation of the isoenzyme CYP2D6 (carbamazepine, diazepam, propafenone) with fluoxetine should be administered with minimal therapeutic doses. Fluoxetine blocks the metabolism of tricyclic and tetracyclic antidepressant drugs trazodone, metoprolol, terfenadine, which leads to an increase in their concentration in the blood serum, enhancing their effect and increasing the incidence of complications.
    In patients who regularly took maintenance doses of phenytoin, plasma phenytoin concentrations increased significantly and symptoms of phenytoin intoxication appeared (nystagmus, diplopia, ataxia and CNS depression) after the onset of concomitant fluoxetine treatment.
    The combined use of fluoxetine and lithium salts requires careful monitoring of the concentration of lithium in the blood. it is possible to increase it.
    Fluoxetine enhances the action of hypoglycemic drugs.
    When used simultaneously with drugs that have a high degree of binding to proteins, especially with anticoagulants and digitoxin, it is possible to increase plasma concentrations of free (unbound) drugs and increase the risk of developing adverse effects.

    Special instructions:
    It requires careful monitoring of patients with suicidal tendencies, especially at the beginning of treatment. The highest risk of suicide in patients who have previously taken other antidepressants, and patients who have excessive fatigue, hypersomnia or motor anxiety in the presence of fluoxetine.Before the onset of significant improvement in treatment, such patients should be under the supervision of a physician.
    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 other antidepressants in children, adolescents and young people (under 24 years of age), the risk of suicide and the benefits of using them should be correlated. In short-term studies in people over 24 years of age, the risk of suicide did not increase, but in people older than 65 years, it declined slightly. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of abnormalities or behavioral changes, as well as suicidal tendencies.
    Against the background of electroconvulsive therapy, it is possible to develop long-term epileptic seizures.
    The interval between the end of therapy with monoamine oxidase inhibitors (MAO) and the initiation of fluoxetine treatment should be at least 14 days; between the end of fluoxetine treatment and the initiation of therapy with MAO inhibitors - at least 5 weeks.
    After the drug is withdrawn, its therapeutic concentration in the blood serum may persist for several weeks.
    Patients with diabetes mellitus may develop hypoglycemia during fluoxetine and hyperglycaemia therapy after withdrawal. At the beginning or after treatment with fluoxetine, you may need to adjust the dosages of insulin and / or hypoglycemic drugs for oral administration.
    In the treatment of patients with body weight deficiency, anorexigenic effects should be considered (a progressive loss of body weight is possible).
    When taking fluoxetine, you should refrain from drinking alcohol, since the drug enhances the effect of alcohol.

    Effect on the ability to drive transp. cf. and fur:Taking fluoxetine can adversely affect the performance of work that requires a high rate of mental and physical reactions (management of mechanical vehicles, mechanisms, work at height, etc.).
    Form release / dosage:Capsules of 10 mg and 20 mg each.
    Packaging:10 capsules per package. 1, 2, 3, 4 or 5 packs of cell contour along with the instruction for use are placed in a pack of cardboard.
    Storage conditions:
    In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:
    3 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002375
    Date of registration:02.12.2011
    The owner of the registration certificate:ALSI Pharma, ZAO ALSI Pharma, ZAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp20.10.2015
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