Fluoxetine

General characteristics. Structure:

Active ingredient: 11,2 mg or 22,4 mg of fluoxetine of a hydrochloride that 10 mg or 20 mg of fluoxetine are equivalent.

Excipients: lactoses monohydrate (sugar milk), cellulose microcrystallic, silicon dioxide colloid (aerosil), magnesium stearate, talc.

Structure of the capsule on 10 mg of fluoxetine: gelatin, titanium dioxide, indigo carmine.

Structure of the capsule on 20 mg of fluoxetine: gelatin, titanium dioxide, dyes: azoruby, crimson (понсо 4R), blue patent, diamond black.

Fluoxetine has the normalizing effect on a nervous system. At reception of this drug the mood increases, the feeling of fear, depression decreases, working capacity increases, the patient becomes less dependent on negative emotions. Fluoxetine eliminates morbid conditions of spiteful irritability.

At such action on a nervous system, the fact that fluoxetine does not cause sedation is very important: block, drowsiness; does not exert a negative impact on heart and vessels.

Fluoxetine helps to win against a depression, chronic alarming states, fear; it is appointed at a premenstrual dysphoria (strong changes of mood in the last days of a menstrual cycle); it is effective at persuasive states. Drug significantly reduces appetite and is used for treatment of nervous bulimia (sharp strengthening of appetite and an overeating because of nerves).

Fluoxetine belongs to antidepressants of new generation with good tolerance, high safety in case of overdoses, low toxicity, lack of a withdrawal. As it was already told, you should not expect effect of administration of drug at once – it will be shown gradually, improving quality of life and confidence in it.

Pharmacological properties:

Antidepressant of group of selective serotonin reuptake inhibitors.

Pharmacodynamics. Selectively blocks the return neyronalny serotonin reuptake (5-gidroksitriptamin) in synapses of neurons of the central nervous system. The inhibition of the return serotonin reuptake leads to increase in concentration of this neurotransmitter in a synaptic gap, strengthens and prolongs its action on postsynaptic receptor sites. H1 - to histamine, muskarinovy and Gamkergichesky receptors has low affinity to α1, α2 and β adrenergic, serotoninovy, dofaminergichesky. Promotes improvement of mood, reduces tension, uneasiness and sensation of fear, eliminates a dysphoria, causes a loss of appetite. Causes a reduction of obsessivno-compulsive frustration. Does not cause orthostatic hypotension, sedation, not кардиотоксичен.

The lasting clinical effect occurs in 1-2 weeks of treatment.

Pharmacokinetics. At intake drug is well soaked up from digestive tract. Meal does not influence bioavailability of drug. The maximum concentration in a blood plasma is reached in 6-8 hours. Fluoxetine well contacts proteins of plasma - about 95% (including albumine and an alfa1-acid glycoprotein), well collect in fabrics. Fluoxetine distribution volume – high, easily gets through a blood-brain barrier, is allocated with breast milk (to 25% of concentration in plasma). It is metabolized in a liver by CYP2D6 isoenzyme by demethylation to an active metabolite of a norfluoksetin. Metabolites are removed by kidneys (80%) and intestines (15%) is preferential in the form of glucuronides. The fluoxetine elimination half-life after achievement of equilibrium concentration in plasma makes 4-6 days, at a single dose – 1-4 days, an elimination half-life of a norfluoksetin – 4-16 days that causes considerable cumulation of active forms and long presence at an organism (5-6 weeks) after drug withdrawal. At patients with cirrhosis the elimination half-life is extended by 3-4 times.

Indications to use:

• Depressions of various genesis;

• Obsessivno-kompulsivnye frustration;

• Bulimic neurosis;

• Premenstrual dysphoria.

Drug is used strictly on doctor's orders!

Route of administration and doses:

Drug is accepted inside.

At a depression the initial dose makes 20 mg of fluoxetine of 1 times a day in the first half of day, irrespective of meal. If necessary the dose can be increased to 40 – 60 mg/days divided into 2-3 receptions. The maximum daily dose makes 80 mg.

At obsessivno-kompuljsivny frustration: the recommended dose makes 20 – 60 mg a day.

At bulimic neurosis and for elderly patients drug is used in a daily dose of 60 mg divided into 2-3 receptions.

At premenstrual dysphoric frustration the recommended dose makes 20 mg/days.

The patient with a renal and liver failure, and also with low body weight it is recommended to begin use with lower doses — on 10 mg of fluoxetine a day and lengthening of an interval between receptions.

Duration of reception is defined by the attending physician, as a rule, not less than 3-4 weeks and can last for several years.

Features of use:

At patients with the accompanying diabetes mellitus development of a hypoglycemia is possible during therapy by fluoxetine and a hyperglycemia after its cancellation. Therefore the dose of insulin and/or any other hypoglycemic means has to be corrected. Before considerable improvement in treatment of a diabetes mellitus patients have to be under observation of the doctor.

At treatment of patients with deficit of body weight it is necessary to consider anorexigenic effects (the progressing loss of body weight is possible).

The interval between the end of therapy by MAO inhibitors and an initiation of treatment fluoxetine has to make at least 14 days; between the end of treatment by fluoxetine and the beginning of therapy by MAO inhibitors – not less than 5 weeks.

At diseases of a liver and at advanced age treatment should be begun about ½ doses.

At children, teenagers and young people (24 years are younger) with a depression, etc. mental disturbances antidepressants, in comparison with placebo, increase risk of emergence of suicide thoughts and suicide behavior. Therefore at purpose of fluoxetine or any other antidepressants at this category of patients it is necessary to correlate risk of a suicide and advantage of their use. In short-term researches at people 24 years are more senior the risk of a suicide did not increase, and at people 65 years are more senior decreased a little. Any depressive frustration in itself increases risk of a suicide. During treatment by antidepressants for all patients observation for the purpose of early identification of suicide bents has to be established.

At development, against the background of reception of fluoxetine, convulsive attacks drug should be cancelled.

After drug withdrawal its therapeutic concentration in blood serum can remain within several weeks.

During treatment by fluoxetine it is necessary to refrain from alcohol intake and occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions (control of mechanical vehicles, mechanisms, work at height, etc.).

Side effects:

From the central nervous system (CNS): dizziness, headache, sleep disorders, increased fatigue, adynamy, tremor, agitation, motive excitement, strengthening of suicide tendencies, uneasiness, mania or hypomania.

From digestive tract: a loss of appetite, taste disturbance, nausea, vomiting, dryness in a mouth or hypersalivation, diarrhea.

From urinogenital system: an incontience or an ischuria, a dysmenorrhea, a vaginitis, decrease in a libido, disturbance of sexual function at men (delay of an ejaculation).

Allergic reactions in the form of skin rash, a small tortoiseshell, an itch, fever, muscle and joints pain.

Others: the increased sweating, tachycardia, visual acuity disturbance, weight loss, system disturbances from lungs, kidneys or a liver, vasculites.

The specified side effects arise at the beginning of therapy by fluoxetine or at increase in a dose of drug more often.

Interaction with other medicines:

It is impossible to use drug along with inhibitors of a monoaminooxidase (MAO) (for example, with selegiliny, Procarbazinum, furasolidone, etc.), including antidepressants - MAO inhibitors; and also tryptophane (the predecessor of serotonin) as development of the serotonergic syndrome which is shown in a hyperthermia, a fever, the increased sweating, vegetative lability, a myoclonus, a hyperreflexia, a tremor, diarrhea, a lack of coordination of movements, excitement, nonsense and a coma is possible.

At use with the drugs containing the St. John's Wort made a hole (Hypericum perforatum) there can be strengthening of serotonergic effect, strengthening of undesirable effects.

Fluoxetine increases in plasma concentration of Phenytoinum (dipheninum), tricyclic antidepressive means, Maprotilinum, Trazodonum twice (it is necessary to lower by 50% a dose of these drugs at simultaneous use with fluoxetine).

Strengthens effects of an alprazolam, diazepam, ethanol, hypoglycemic medicines.

The concomitant use of fluoxetine with alcohol or with drugs of the central action, the TsNS functions causing oppression, strengthens their effect and increases risk of development of side effects.

The medicines containing lithium (Li+) should be applied with care because of possible increase in concentration of lithium (Li+) and risk of development of toxic effects.

Against the background of performing electroconvulsive therapy development of long convulsive attacks is possible.

At simultaneous use with the drugs possessing high extent of linkng with proteins, especially with anticoagulants and digitoxin increase in concentration in plasma of available (untied) medicines and increase in risk of development of adverse effects is possible.

Contraindications:

• Hypersensitivity to drug;

• A concomitant use of monoamine oxidase inhibitors (MAO) and within 14 days after their cancellation, thioridazine, Pimozidum;

• Lactation period;

• Pregnancy;

• Heavy renal failures (clearance of creatinine less than 10 ml/min.) and liver;

• Bladder atony;

• Children's age up to 18 years (efficiency and safety is not established);

• Due to the content in monohydrate lactose drug (milk sugar) patients with rare hereditary diseases, such as intolerance of a galactose, deficit of lactase or glyukozo-galaktozny malabsorption should not accept drug.

With care. Drug is used with care at a diabetes mellitus, epilepsy (including in the anamnesis), excessive weight loss, Parkinson's disease, a suicide mood.

Overdose:

Symptoms: nausea, vomiting, condition of psychomotor excitement, motive concern, convulsive frustration, dysfunction of cardiovascular system.

Treatment: specific antagonists to fluoxetine are not found. Symptomatic therapy, a gastric lavage, purpose of absorbent carbon is carried out, at spasms — purpose of tranquilizers, maintenance of breath, cordial activity.

Storage conditions:

Capsules on 10 mg or on 20 mg. On 10 capsules in a planimetric strip packaging. 1, 2, 3, 4 or 5 planimetric strip packagings together with the application instruction place in a pack from a cardboard.

Issue conditions:

According to the recipe

Packaging:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after the date specified on packaging.