Fluoxetine

General characteristics. Structure:

Active agent: fluoxetine a hydrochloride of 22.36 mg (in terms of fluoxetine of 20 mg)

Pharmacological properties:

Pharmacodynamics. Antidepressive means, selective serotonin reuptake inhibitor. Improves mood, reduces tension, uneasiness and sensation of fear, eliminates a dysphoria. Does not cause orthostatic hypotension, sedation, некардиотоксичен. The lasting clinical effect occurs in 1-2 weeks of treatment.

Pharmacokinetics. Absorption - high, TCmax after intake of 40 mg - 6-8 h, Cmax value - 15-55 ng/ml. Capsules and aqueous solution of drug of a bioekvivalentna, meal does not influence bioavailability. Communication with proteins of plasma - 94.5% (including albumine and an alfa1-glycoprotein). Distribution volume - high, easily gets through GEB. Both enantiomeric forms of an ekvieffektivna, but S-fluoxetine are removed more slowly and prevails over a R-form at Css. In a liver enantiomer are metabolized to an active metabolite - a norfluoksetin. Metabolites are removed by kidneys (80%) and with a fecal masses (15%), is preferential in the form of glucuronides. Is inhibitor of isoenzymes CYP2C19, CYP3A2, CYP3A3, CYP3A5 and CYP3A7. Fluoxetine T1/2 - 1-4 days at a single dose and 4-6 days - after achievement of Css. T1/2 of a norfluoksetin at a single dose and after achievement of Css - 4-16 days that causes considerable cumulation of active forms, slow achievement of their Css in plasma and long presence at an organism after cancellation. At patients with cirrhosis of T1/2 it is extended by 3-4 times.

Indications to use:

Depressions (irrespective of extent of depressive frustration - weak, moderate, heavy), bulimia, anorexia, alcoholism, persuasive states

Route of administration and doses:

Inside, at a depression an initial dose - 20 mg/days of 1 times, in the morning; if necessary weekly the dose is increased by 20 mg/days. The maximum daily dose - 80 mg in 2-3 receptions. At bulimia and for elderly patients - 60 mg in 3 receptions, at persuasive states - 20-60 mg/days. A maintenance therapy - 20 mg/days. A course of treatment - 3-4 weeks.

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 reception of ethanol and occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions. 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 1/2 doses.

Side effects:

From a nervous system: dizziness, a headache, drowsiness or sleeplessness, slackness, increased fatigue, an adynamy, a tremor, agitation, uneasiness, suicide bent (inherent to the patient with depressive frustration), a mania or a hypomania.

From the alimentary system: a loss of appetite, dryness in a mouth or hypersalivation, nausea, 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:

Strengthens effects of an alprazolam, diazepam, ethanol and hypoglycemic HP. 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). 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 a GIT). MAO inhibitors increase risk of development of a serotoninovy syndrome (a hyperthermia, a fever, the increased sweating, a myoclonus, a hyperreflexia, a tremor, diarrhea, lacks of coordination of movements, vegetative lability, excitement, nonsense and a coma). The HP exerting the oppressing impact on TsNS increase risk of development of side effects and strengthening of the oppressing action on TsNS. At simultaneous use with the HP possessing high extent of linkng with proteins, especially with anticoagulants and digitoxin increase in a koytsentration in plasma of free (untied) HP and increase in risk of development of adverse effects is possible.

Contraindications:

Hypersensitivity, HPN (KK less than 10 ml/min.), the expressed liver failure, a suicide mood, a concomitant use of MAO inhibitors (in the previous 2 weeks), pregnancy, the lactation period.

Overdose:

Symptoms: nausea, vomiting, condition of excitement, spasm. Treatment: a gastric lavage, purpose of absorbent carbon, at spasms - anxiolytic HP (tranquilizers), symptomatic therapy.

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.

Issue conditions:

According to the recipe

Packaging:

capsules of 20 mg (banks polymeric, planimetric strip packagings).