Fluoxetine

General characteristics. Structure:

Capsules of 10 mg. Each capsule contains
Active agent: fluoxetine a hydrochloride of 11,2 mg in terms of fluoxetine of 10 mg.

Excipients: cellulose microcrystallic - 153,0 mg, starch prezhelatinizirovanny - 14,3 mg, magnesium mg stearate-1,5.

Structure of the capsule of 10 mg: titanium dioxide, indigo carmine, dye ferrous oxide yellow, gelatin.

Capsules of 20 mg. Each capsule contains
Active agent: fluoxetine a hydrochloride of 22,4 mg in terms of fluoxetine of 20 mg.

Excipients: cellulose microcrystallic - 141,8 mg, starch prezhelatinizirovanny - 14,3 mg, magnesium stearate - 1,5 mg.

Structure of the capsule of 20 mg: titanium dioxide, indigo carmine, dye ferrous oxide yellow, dye quinolinic yellow, dye azoruby, dye blue patent, dye diamond black, gelatin.

Pharmacological properties:

Antidepressant of group of selective serotonin reuptake inhibitors. Possesses a timoanaleptichesky and promoting effect.

Pharmacodynamics. Selectively blocks the return neyronalny serotonin reuptake (5HT) 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. In therapeutic doses fluoxetine blocks serotonin reuptake by thrombocytes of the person. Is a weak antagonist of muskarinovy, histamine Ng adrenergic and, and and, receptors, influences the return capture of dopamine a little. Causes a reduction of obsessivno-compulsive frustration, and also a loss of appetite that can lead to decrease in body weight. Does not cause sedation. At reception in average therapeutic doses also other systems practically do not influence functions cardiovascular.

Pharmacokinetics. At intake drug is well soaked up from digestive tract (to 95% of the accepted dose), use with food slightly slows down fluoxetine absorption. The maximum concentration in a blood plasma are reached in 6-8 hours. Bioavailability of fluoxetine after intake makes more than 60%. Drug well collects in fabrics, easily gets through a blood-brain barrier, linkng with proteins of a blood plasma makes more than 90%. It is metabolized in a liver by demethylation to an active metabolite of a norfluoksetin and a number of not identified metabolites. It is removed by kidneys, the size of clearance of fluoxetine makes 94-704 ml/min., a norfluoksetin of 60-336 ml/min. About 12% of drug are allocated through digestive tract. The elimination half-life of fluoxetine makes about 2-3 days, a norfluoksetin — 7-9 days. Patients with a liver failure have an elimination half-life of fluoxetine and a norfluoksetin is extended. Drug is emitted with breast milk (to 25% of concentration in blood serum).

Indications to use:

— Depressions of various etiology.
— Obsessivno-kompulsivnye frustration.
— Bulimic neurosis.
— Premenstrual dysphoric frustration.

Route of administration and doses:

Drug is accepted inside. Depression. The initial dose makes 20 mg of 1 times a day in the first half of day, irrespective of meal. If necessary and portability, the dose can be increased to 40-60 mg a day (on 20 mg a week) divided into 2-3 receptions. The maximum daily dose — 80 mg. The therapeutic effect of drug is established in 1-4 weeks after an initiation of treatment, at some patients it can be reached later. Obsessivno-kompulsivnye frustration — the recommended dose makes 20-60 mg a day. At nervous bulimia the recommended dose makes 60 mg a day divided into 2-3 receptions.
Premenstrual dysphoric frustration: the recommended dose makes 20 mg a day. At patients of advanced age the recommended initial daily dose makes 20 mg.
At patients with abnormal liver functions and kidneys use of lower doses and lengthening of an interval between receptions is recommended.

Features of use:

At treatment of patients with deficit of body weight it is necessary to consider anorexigenic effects (the progressing loss of body weight is possible). At patients with a diabetes mellitus purpose of fluoxetine increases risk of development of a hypoglycemia and hyperglycemia — at its cancellation. In this regard the dose of insulin and/or any other hypoglycemic HP applied inside has to be corrected. Before considerable improvement in treatment patients have to be under observation of the doctor.
During treatment it is necessary to abstain from alcohol intake and occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.
After use of MAO inhibitors appointment of fluoxetine is allowed not earlier than 14 days. It is not necessary to apply MAO inhibitors and/or thioridazine earlier, than in 5 weeks after fluoxetine cancellation.
At development, against the background of reception of fluoxetine, convulsive attacks drug should be cancelled. At diseases of a liver and at advanced age treatment should be begun with the minimum doses.

Side effects:

- From the central nervous system: strengthening of suicide tendencies, alarm, headache, tremor, agitation, acrimony, sleep disorder, dizziness, drowsiness, asthenic frustration, reduction of a libido, maniacal and convulsive frustration.
- 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, sexual dysfunction at men (the slowed-down ejaculation).
- Seldom allergic reactions in the form of skin rash, an itch, a fever, a small tortoiseshell, fervescence, muscle and joints pain (use of antihistaminic and steroid drugs is possible), a hyponatremia, orthostatic hypotonia, tachycardia, visual acuity disturbance meet.
- Other: the increased sweating, tachycardia, system disturbances from lungs, kidneys or a liver, vasculites.
Development of anorexia and degrowth of a body is possible.
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:

Strengthens effects of an alprazolam, diazepam, alcohol and the hypoglycemic medicines (M).
Increases in plasma concentration of Phenytoinum, tricyclic antidepressants, Maprotilinum, Trazodonum twice (it is necessary to lower by 50% a dose of tricyclic antidepressants at simultaneous use).
Increase in concentration of lithium — risk of development of toxic effects of lithium is possible. These HP should be applied along with care, frequent definition of concentration of lithium in blood serum is recommended.
Against the background of performing electroconvulsive therapy development of long epileptic seizures is possible.
Tryptophane increases serotonergic properties of fluoxetine (strengthening of agitation, motive concern, disturbances from digestive tract).
MAO inhibitors increase risk of development of a seroto-ninovy syndrome (a hyperthermia, a fever, the increased sweating, a myoclonus, a hyperreflexia, a tremor, diarrhea, lacks of coordination of movements, vegetative lability, psychomotor excitement, crazy frustration, oppression of consciousness up to a coma). The HP exerting the oppressing impact on the central nervous system increase risk of development of side effects and strengthening of the oppressing action on the central nervous system. At simultaneous use with the HP possessing high extent of linkng with proteins, especially with anticoagulants and digitoxin increase in concentration in plasma of free (untied) HP and increase in risk of development of adverse effects is possible. Fluoxetine strengthens effect of hypoglycemic drugs and anticoagulants.

Contraindications:

Hypersensitivity, concomitant use of MAO inhibitors (and within 14 days after their cancellation), thioridazine (and during 5 weeks after fluoxetine cancellation), Pimozidum, heavy renal failures (clearance of creatinine less than 10 ml/min.) and a liver, pregnancy, the lactation period, age up to 18 years.

With CARE. A diabetes mellitus, epilepsy, convulsive frustration (including in the anamnesis), a suicide mood.

Overdose:

Symptoms: agitation, maniacal and convulsive frustration, disturbances of a cordial rhythm, tachycardia, nausea, vomiting.
Treatment: specific antagonists to fluoxetine are not found. Symptomatic therapy, a gastric lavage with purpose of absorbent carbon is carried out, at spasms — diazepam, maintenance of breath, cordial activity, body temperature.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules of 10 mg and 20 mg.
On 7,10,14 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 7,10,14, 20, 28, 30, 40, 50 or 100 capsules in a container polymeric for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.