Профлузак®

General characteristics. Structure:

Active ingredient: 0,02 g of fluoxetine.

Excipients: cellulose microcrystallic, silicon dioxide colloid (aerosil), magnesium stearate.

Structure of the capsule: gelatin, titanium dioxide.

Pharmacological properties:

Pharmacodynamics. Selectively blocks the return neyronalny serotonin reuptake (5HT) in synapses of neurons of the central nervous system (CNS). 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 H1, adrenergic a1 and a2 of receptors, influences the return capture of dopamine a little. Promotes improvement of mood, reduces sensation of fear and tension. Eliminates a dysphoria, causes a loss of appetite. Does not cause sedation. Causes a reduction of obsessivno-compulsive frustration.

At reception in average therapeutic doses also other systems practically do not influence functions cardiovascular. The lasting clinical effect occurs in 1-2 weeks.

Pharmacokinetics. At intake drug is well soaked up from digestive tract (to 95% of the accepted dose), use with food slightly slows down absorption of a floksetin. The maximum concentration in a blood plasma is reached in 6-8 hours and makes 15-55 ng/ml. 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 94,5% (including albumine and an alfa1-glycoprotein).

Both enantiomeric forms of fluoxetine of an ekvieffektivna, but S-fluoxetine are removed more slowly and prevails over a R-form at equilibrium concentration (Css). In a liver enantiomer are metabolized by demethylation to an active metabolite of a norfluoksetin and a number of not identified metabolites. Metabolites are removed by kidneys (80%) and with a fecal masses (15%), is preferential in the form of glucuronides. The size of clearance of fluoxetine makes 94-704 ml/min., a norfluoksetin of 60-336 ml/min.

The elimination half-life (T1/2) of fluoxetine makes 1-4 days at a single dose and 4-6 days at achievement of Css. T1/2 of a norfluoksetin — 4-16 days in both cases that causes cumulation of active forms, slow achievement of their equilibrium level in plasma and long presence at an organism after cancellation. At a renal failure the speed of removal of medicine considerably does not change. At patients with cirrhosis of T1/2 of fluoxetine and a norfluoksetin it is extended by 3-4 times. Drug is emitted with breast milk (to 25% of concentration in blood serum).

Indications to use:

• Depressions of various etiology.
• Nervous bulimia.
• Obsessivno-kompulsivnoye frustration.

Route of administration and doses:

Drug is accepted inside. At depressions 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, but no more, than to 80 mg/days.

At bulimia drug is used in a daily dose of 60 mg divided into 2-3 receptions. At persuasive states — 20-60 mg/days. Maintenance dose of 20 mg/days. A course of treatment — 3-4 weeks.

At patients of advanced age the recommended 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 at its cancellation — a hyperglycemia. In this regard the dose of insulin and/or any other hypoglycemic means applied inside has to be corrected. Before considerable improvement in treatment patients have to be under observation of the doctor.

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 with half doses.

During treatment it is necessary to abstain from reception of ethanol and occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.

Side effects:

From TsNS: mania or hypomania, strengthening of suicide tendencies, alarm, headache, dizziness, tremor, irritability, sleep disorder, adynamy.

From digestive tract: a loss of appetite, nausea, dryness in a mouth, the increased salivation, diarrhea.

Allergic reactions: skin rash, small tortoiseshell.

Others: the increased sweating, weight loss, decrease in a libido, system disturbances from lungs, kidneys or a liver, vasculites.

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 a serotonergic syndrome which symptoms can be confusion of consciousness, a hypomaniacal state, motive concern, agitation, spasms, a dysarthtia, hypertensive crisis, a fever, a tremor, nausea, vomiting, diarrhea is possible.
• Fluoxetine strengthens effect of alcohol, the hypoglycemic drugs and drugs of the central action causing TsNS function oppression.
• Fluoxetine blocks metabolism of tricyclic and tetracyclic antidepressive means, Trazodonum, carbamazepine, diazepam, a metoprolol, terfenadin, Phenytoinum that leads to increase in their concentration in blood serum, strengthening their action and increasing the frequency of complications; at simultaneous use of tricyclic antidepressants it is necessary to reduce their dose twice.
• The combined use of fluoxetine and salts of lithium demands careful control of concentration of lithium in blood since its change is possible (as towards increase, and decrease).
• At simultaneous use with the medicines possessing high extent of linkng with proteins, especially with anticoagulants and digitoxin increase in concentration in plasma of free (untied) drugs and increase in risk of development of adverse effects is possible.

Contraindications:

• Hypersensitivity to drug.
• A concomitant use with MAO inhibitors.
• Breastfeeding period.
• Pregnancy.
• Heavy renal failures and liver (clearance of creatinine less than 10 ml/min.)
• Suicide mood.

With care. A diabetes mellitus, an epileptic syndrome of various genesis and epilepsy (including in the anamnesis), Parkinson's disease, the compensated renal and/or liver failure, a cachexia.

Overdose:

Symptoms: agitation, motive concern, 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:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. It is not necessary to accept drug after the expiry date specified on packaging. A period of validity - 2 years 6 months.

Issue conditions:

According to the recipe

Packaging:

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