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

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. It is a weak antagonist of muscarinic, histamine H1, and adrenergic a1 a2 receptor has little effect on the reuptake of dopamine. Promotes mood improvement, reduces feelings of fear and tension, eliminates dysphoria, causes a decrease in appetite. Does not cause sedation. It causes a reduction in obsessive-compulsive disorders. When taken in moderate therapeutic doses, it practically does not affect the function of the cardiovascular system.

Pharmacokinetics:

When ingested, the drug is well absorbed from the gastrointestinal tract (up to 95% of the dose taken),application with food slightly inhibits the 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 94.5%. 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 creatinine klirens is 94-704 ml / min, norfluoxetine - 60-336 ml / min. Renal insufficiency does not have a significant effect on the rate of excretion of fluoxetine. About 12% of the drug is excreted through the gastrointestinal tract. The half-life (T1 / 2) of fluoxetine is about 2-3 days, norfluoxetine is 7-9 days. In patients with deficiency of liver function, T1 / 2 fluoxetine and norfluoxetine is prolonged. The drug is excreted in breast milk (up to 25% of the concentration in the blood serum).

Indications:

Use strictly according to the doctor's prescription!

Depression of various genesis.

Obsessive-compulsive disorder (OCD).

Bulimic neurosis.

Contraindications:

Hypersensitivity to fluoxetine and other components of the drug;
simultaneous administration with monoamine oxidase inhibitors (MAO); within 14 days after the abolition of MAO inhibitors of irreversible action;
simultaneous administration with thioridazine (and within 5 weeks after the abolition of fluoxetine), pimozide;
lactation period;
children under 18 years of age (safety and efficacy not established).

Carefully:

diabetes mellitus, convulsive disorders (including history), Parkinson's disease, suicidal mood, excessive weight loss, cardiovascular diseases, impaired liver function, manic conditions in the anamnesis, simultaneous use with tryptophan.

Pregnancy and lactation:

Do not use during pregnancy (safety of the drug during pregnancy is not established).

The drug is excreted into breast milk, so during the therapy it is necessary to stop breastfeeding.

Dosing and Administration:

Inside, in the morning, regardless of food intake.

Depression of various genesis:

The initial dose is 20 mg once a day.If necessary, the dose can be increased to 40-60 mg / day, divided into 2-3 doses. The maximum daily dose is 80 mg. The therapeutic effect of the drug is established 3-4 weeks after the start of treatment, in some patients it can be achieved later.

In elderly patients, the recommended daily dose is 60 mg. Obsessive-compulsive disorder (ROC):

The initial dose is 20 mg 1 time per day. If necessary, the dose can be gradually increased to 60 mg / day, divided into 2-3 doses.

Bulimic neurosis:

The drug is used in a daily dose of 60 mg divided into 2-3 doses.

In patients with impaired liver function, lower doses are recommended and the interval between phases taken is 2 days).

There is no data on the need for dose changes for the elderly.

Side effects:

On the part of the organs of hematopoiesis and lymphatic system: rarely - leukopenia. Metabolic and nutritional disorders: rarely - reversible hyponatremia (<110 mmol / l) (more often in elderly patients, with diuretic therapy).

From the central (CNS) and peripheral nervous system: very often - headache,insomnia, tremor, vertigo, dizziness, paresthesia, emotional lability, anxiety, nightmares; very rarely - convulsions (more often on the background of electroconvulsive therapy), extrapyramidal symptoms (against Parkinson's disease), manic disorders, increased suicidal tendencies, increased fatigue,

From the senses: very often - a violation of visual acuity.

From the cardiovascular system: very often - palpitations, pain in the chest; often - arterial hyper / hypotension, syncope.

From the organs of respiration, thorax and mediastinum: rarely - shortness of breath.

On the part of the digestive system: very often - nausea, dry mouth, decreased appetite, taste perversion, vomiting, diarrhea, constipation, abdominal pain, weight loss; infrequently - increased activity of "liver" enzymes, dysphagia; rarely - a violation of the liver (including jaundice).

Allergic reactions: very often - itching; often - anaphylactoid reactions (including bronchospasm, Quincke's edema, urticaria); rarely - in the form of skin rash, itching, chills, leukocytosis, fever, pain in the muscles and joints, dyspnea, (against the background of allergic reactions possible use of antihistamine and steroid drugs),

From the side of the musculoskeletal system: very often - muscle weakness.

Other: very often - fatigue, sweating, a feeling of "hot flashes" to the skin of the face. On the part of the genitourinary system: urinary incontinence or retention, dysmenorrhea, vaginitis, sexual dysfunction in men (delayed ejaculation), impotence, decreased libido.

Overdose:

Symptoms: agitation, motor anxiety, fever, mania, seizures, heart rhythm disturbances, tachycardia, nausea, vomiting, diarrhea, sweating, myoclonus, hyperreflexia. In severe cases, there are possible: impaired consciousness to coma, shallow breathing, arterial hypotension.

Treatment: a specific antidote is unknown. Symptomatic therapy, gastric lavage with the appointment of activated charcoal, with convulsions - diazepam, maintaining breathing, cardiac activity, body temperature.

Interaction:

Fluoxetine should not be administered simultaneously with MAO inhibitors and for at least 14 days after discontinuation of treatment with MAO inhibitors of irreversible action; it is possible to administer fluoxetine the next day after discontinuation of treatment with MAO inhibitors of reversible action (for example, moclobemide). After the abolition of fluoxetine and the beginning of treatment with MAO inhibitors, there should be an interval of at least 5 weeks. If long-term fluoxetine treatment was used and / or the drug was used in high doses, then this interval should be increased. Among patients who had previously taken fluoxetine, and started taking MAO inhibitors through a shorter interval, there were cases of the development of serotonin syndrome (manifestations of which may be similar to malignant neuroleptic syndrome (NSA), up to a lethal outcome. Cyproheptadine or dantrolene may reduce the severity of symptoms. With the simultaneous use of selective inhibitors of reverse neuronal seizure of serotonin and

MAO inhibitors appear: hyperthermia, rigidity, convulsions, myoclonus, lability in the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion, which in some cases can go to a delirious condition or to whom.

Tryptophan enhances the serotonergic properties of fluoxetine (increased anxiety, motor anxiety, gastrointestinal disorders).

Simultaneous reception of fluoxetine with alcohol or with drugs of central action, which cause depression of the central nervous system, enhances their effect.

Fluoxetine blocks the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin (diphenin), 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. it is possible to increase it.

Fluoxetine enhances the effect of hypoglycemic drugs and anticoagulants. Fluoxetine strongly binds to plasma proteins. Therefore, when the drug is prescribed against the background of the use of another drug that binds firmly to plasma proteins, changes in the plasma concentrations of both drugs and an increased risk of developing adverse effects are possible.

Against the background of electroconvulsive therapy in rare cases, the development of prolonged convulsive seizures.

After the drug is withdrawn, its therapeutic concentration in the blood serum may persist for several (3-5) weeks. Consider the long-term T1 / 2 fluoxetine and its active metabolite norfluoxetine and, in this connection, the possibility of drug interaction.

Simultaneous reception of fluoxetine and St. John's wort (Hypericum perforatum) increases the risk of side effects.

Special instructions:

If skin rashes or other possible allergic reactions occur, the etiology of which can not be determined, fluoxetine should be withdrawn.

In patients with diabetes mellitus, the development of .hyperglycemia during fluoxetine and hyperglycaemia after its cancellation is possible. It is recommended to control the concentration of glucose in the blood and correct the dose of insulin or hypoglycemic drugs.

In cardiovascular diseases, the drug should be administered under the strict supervision of the therapist.

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

The risk of committing suicide is inherent in depression and can persist until a significant improvement in the condition occurs spontaneously or as a result of ongoing therapy. Careful observation of patients on antidepressant medication is necessary, especially at the beginning of treatment because of the possibility of clinical deterioration and / or the appearance of suicidal manifestations (thoughts and behavior). This precaution should be followed in the treatment of other mental disorders due to the possibility of simultaneous development of depression.

In a number of cases, in the treatment of SSRIs with antidepressants (selective serotonin reuptake inhibitors), there has been an increased risk of developing suicidal thoughts and behavior in children, adolescents and young people younger than 24 years compared with placebo.

Effect on the ability to drive transp. cf. and fur:

The intake of fluoxetine can adversely affect the performance of work that requires a high rate of mental and physical reactions (control of mechanical vehicles, mechanisms, work at height, etc.)

Form release / dosage:

Capsules 20 mg.

Packaging:

For 7 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3 contour squares, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

List B.

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:

2 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003164 / 01

Date of registration:31.08.2009

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Fluoxetine-OBL (Fluoxetine-OBL)