FLUOXETINE of 10 mg

General characteristics. Structure:

Active ingredient: fluoxetine a hydrochloride - 11,18 mg or 22,36 mg,

in terms of fluoxetine – 10,00 mg or 20,00 mg.

Excipients: lactoses monohydrate (sugar milk) – 82,42 mg or 71,24 mg, potato starch – 24,00 mg or 24,00 mg, magnesium stearate – 1,20 mg or 1,20 mg, silicon dioxide colloid (aerosil) – 1,20 mg or 1,20 mg.

Structure of capsules: for a dosage of 10 mg – the case: gelatin, titanium E 171 dioxide; lid: gelatin, titanium E 171 dioxide, dye quinolinic yellow E 104;

for a dosage of 20 mg – the case: gelatin, titanium E 171 dioxide; lid: gelatin, titanium E 171 dioxide.

 Description.

Solid gelatin capsules No. 3 opaque white color with a lid of yellow color (for a dosage of 10 mg) or opaque white color with a lid of white color (for a dosage of 20 mg). Contents of capsules – powder of color, white or white with a yellow shade.

Pharmacological properties:

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

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. _H1, adrenergic _α1 is a weak antagonist muskarinovy, histamine and _α2 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. Insufficiency of kidneys does not exert noticeable impact on fluoxetine removal speed. 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 hepatic unsufficiency 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 genesis.

- Obsessivno-kompulsivnye frustration.

- Bulimic neurosis.

Route of administration and doses:

Drug is accepted inside.

The initial dose makes 20 mg 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 - 80 mg.

The clinical effect develops 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 bulimic neurosis drug is used in a daily dose of 60 mg divided into 2-3 receptions.

At patients of advanced age the recommended daily dose makes 20 mg. At patients with abnormal liver functions and kidneys, and also with low body weight use of lower doses and lengthening of an interval between receptions is recommended.

Duration of reception is defined by the attending physician and can last for several years.

Features of use:

There are messages on developing of skin rash, anaphylactic reactions and the progressing system disturbances with involvement in pathological process of skin, lungs, a liver, kidneys for the patients accepting fluoxetine. At emergence of skin rash or other possible allergic reactions which etiology cannot be defined reception of fluoxetine should be cancelled.

In the researches in vitro and on animals the evidence of carcinogenicity is not obtained.

Safety and efficiency of use of fluoxetine for children are not established.

When using drug флуокситен elderly patients the dose of drug has to be reduced twice. Also the dose should be reduced twice at the broken function of a liver and kidneys.

At patients with a diabetes mellitus development of a hypoglycemia is possible during therapy by fluoxetine and a hyperglycemia after its cancellation. At the beginning and after the end of treatment by fluoxetine correction of doses of insulin and/or hypoglycemic drugs for intake can be required.

Against the background of performing electroconvulsive therapy development of long epileptic seizures is possible.

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

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

During treatment fluoxetine does not allow reception of alcoholic beverages.

Careful observation of patients with suicide bents, especially in an initiation of treatment is required. More persons are subject to risk of a suicide is younger
24 years.

Influence on ability to driving of motor transport and to control of mechanisms.

During treatment by Fluoxetine it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the central nervous system: hypomania or mania, strengthening of suicide tendencies, alarm, acrimony, agitation, dizziness, headache, tremor, sleeplessness or drowsiness, asthenic frustration.

From digestive tract: a loss of appetite, taste disturbances, 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).

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

Seldom meet: allergic reactions in the form of skin rash, a small tortoiseshell, an itch, a fever, fervescence, muscle and joints pain (use of antihistaminic and steroid drugs is possible); the increased sweating, a hyponatremia, tachycardia, visual acuity disturbance, 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:

It is impossible to use drug along with MAO inhibitors, including antidepressants - MAO inhibitors; furasolidone, Procarbazinum, selegiliny, and also tryptophane (the predecessor of serotonin) as development of the serotonergic syndrome which is shown in confusion of consciousness, a hypomaniacal state, psychomotor excitement, spasms, a dysarthtia, hypertensive crises, a fever, tremor, nausea, vomiting, diarrhea 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.

The concomitant use of fluoxetine with alcohol or with the drugs of the central action causing oppression of function of the central nervous system strengthens their effect.

Fluoxetine blocks metabolism of tricyclic and tetracyclic antidepressive means, Trazodonum, carbamazepine, diazepam, a metoprolol, terfenadin, Phenytoinum (dipheninum) that leads to increase in their concentration in blood serum, strengthening their action and increasing the frequency of complications.

Combined use of fluoxetine and salts of lithium demands careful control of concentration of lithium in blood as its increase is possible.

Fluoxetine strengthens effect of hypoglycemic drugs. 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:

- Children and teenagers up to 18 years.

- Hypersensitivity to drug.

- A concomitant use with monoamine oxidase inhibitors (MAO).

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

- Breastfeeding period.

- Pregnancy.

Overdose:

Symptoms: psychomotor excitement, convulsive attacks, 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:

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 10 capsules in a blister strip packaging. On 2, 3 or 5 blister strip packagings together with the application instruction in a pack from a cardboard.