Fluoxetine - instructions for use, dose, side effects, contraindications

Active ingredient: fluoxetine hydrochloride - 0.02236 g (in terms of fluoxetine - 0.02 g) Excipients: sugar milk (lactose) - 0.17334 g potato starch - 0.032 g magnesium stearate - 0.0023 g Content of the capsule contents - 0.230 g Capsules: titanium dioxide, dye quinoline yellow (yellow quinoline), dye sunset yellow (yellow sunset), methyl parahydroxybenzoate (methyl hydroxybenzoate), propyl parahydroxybenzoate (propylhydroxybenzoate), acetic acid, gelatin.

Description:Capsules number 3 of yellow color.The contents of the capsule powder are white or white with a yellowish hue.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.03 Fluoxetine

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. In therapeutic doses fluoxetine blocking the seizure of serotonin by human platelets. Is a weak antagonist of muscarinic, histamine HI, adrenergic alpha 1 and alpha 2 receptors, has little effect on re-uptake of dopamine. It causes a reduction in obsessive compulsive disorders, as well as a decrease in appetite, which can lead to a decrease in body weight. Does not cause sedation. When taken in moderate therapeutic doses, it practically does not affect the function of the cardiovascular and other systems.

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, the amount of clearance of fluoxetine is 94-704 ml / min, norfluoxetine 60-336 ml / min. Kidney deficiency has no significant effect on the rate of fluoxetine removal. About 12% of the drug is released through the gastrointestinal tract. The half-life of fluoxetine is about 2-3 days, norfluoxetine is 7-9 days. In patients with liver failure, the half-life of fluoxetine and norfluoxetine is prolonged. The drug is excreted in breast milk (up to 25% of the concentration in the blood serum).

Indications:

Depression of various genesis.

Obsessive-compulsive disorder

Bulimic neurosis.

Contraindications:

Hypersensitivity to the drug.

Simultaneous reception with monoamine oxidase inhibitors (MAO).

Severe renal function impairment (creatinine clearance less than 10 ml / min) and liver.

Breastfeeding period.

Pregnancy.

Carefully:

With care diabetes mellitus, convulsive syndrome of various genesis and epilepsy (including in the anamnesis), Parkinson's disease, compensated renal and / or hepatic insufficiency, excessive weight loss, suicidal mood.

Dosing and Administration:

The drug is taken orally.

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. The maximum daily dose is 80 mg.

The clinical effect develops 1-4 weeks after the start of treatment, in some patients it can be achieved later.

Obsessive-compulsive disorder: The recommended dose is 20-60 mg per day. With bulimic neurosis, the drug is used in a daily dose of 60 mg divided into 2-3 doses.

In elderly patients, the recommended daily dose is 20 mg.

In patients with impaired liver and kidney function, the use of lower doses and the lengthening of the interval between doses is recommended.

Side effects:

From the side of the central nervous system: hypomania or mania, increased suicidal tendencies, anxiety, increased irritability, agitation, dizziness, headache, tremor, insomnia or drowsiness, asthenic disorders.

On the part of the gastrointestinal tract: decreased appetite, impaired taste, nausea, vomiting, dry mouth or hypersalivation, diarrhea.

From the genitourinary system: urinary incontinence or retention, dysmenorrhea, vaginitis, decreased libido, sexual dysfunction in men (delayed ejaculation).

When developing, against the background of taking fluoxetine, seizures, the drug should be discarded.

Rarely occur: allergic reactions in the form of skin rashes, hives, itching, chills, fever, pain in the muscles and joints (possibly using antihistamines and steroid drugs); increased sweating, hyponatremia, tachycardia, visual acuity, vasculitis.

Perhaps the development of anorexia and weight loss.

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 seizures, heart rhythm disturbances, tachycardia, nausea, vomiting.

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:

It is impossible to apply the drug simultaneously with MAO inhibitors, including antidepressants - MAO inhibitors; furozolidone, procarbazine, selegiline, 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 fluoxetine with alcohol or with drugs of central action, causing oppression of the central nervous system, enhances their effect.

Fluoxetine blocks the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin (diphenine), which leads to an increase in serum concentrations, increasing their effect and increasing the incidence of complications.

The combined use of fluoxetine and lithium salts requires careful monitoring of the concentration of lithium in the blood, as it may be increased.

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:

Patients with diabetes mellitus may develop hypoglycemia during fluoxetine and hyperglycaemia therapy after withdrawal.

Against the background of electroconvulsive therapy, it is possible to develop long-term epileptic seizures.

In the treatment of patients with body weight deficiency, anorexigenic effects should be considered (a progressive loss of body weight is possible).

After the drug is withdrawn, its therapeutic concentration in the blood serum may persist for several weeks.

During the treatment with fluoxetine, alcoholic beverages are not allowed.

Taking fluoxetine can adversely affect the performance of the work,requiring high speed of mental and physical reactions (control of mechanical vehicles, mechanisms, work at height, etc.)

The interval between the end of therapy with MAO inhibitors and the initiation of treatment with fluoxetine should be at least 14 days; between the end of treatment with fluoxetine and the onset of therapy with MAO inhibitors - at least 5 weeks.

With liver diseases and in old age, treatment should be started with 1/2 dose.

Form release / dosage:

Capsules 20 mg.

Packaging:

10 capsules are packed in a contour mesh box made of polyvinyl chloride film and foil of aluminum printed lacquered. For 1, 2 or 3 contour packagings together with the instructions for use are placed in a cardboard box.

Packing for hospitals. 100, 200, 300, 400 or 500 contour-cell packs with instructions for use are placed in cardboard boxes.

For 500, 1000 or 2000 capsules are packed in polymer cans with lids made of polymer materials. For 1, 2, 3, 4, 5 or 6 cans with instructions for use are put in boxes of cardboard.

Storage conditions:

List B. In dry sheltered from light, out of reach of children, at a temperature of no higher than 25 ° C.

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

Terms of leave from pharmacies:On prescription

Registration number:P N003923 / 01

Date of registration:25.05.2010

The owner of the registration certificate:ZIO-HEALTH, JSC ZIO-HEALTH, JSC Russia

Manufacturer: & nbsp

ZIO-HEALTH, JSC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Fluoxetine (Fluoxetine )