Composition, form of production and packaging
Capsules 1 caps.
fluoxetine (in the form of hydrochloride) 20 mg
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
Selectively blocks the reverse neuronal capture of serotonin (5HT) in the synapses of neurons of the central nervous system. Inhibition of the reuptake of serotonin leads to an increase in the concentration of this neurotransmitter in the synaptic cleft, enhances and prolongs its effect on postsipaptic receptor sites. In therapeutic doses, fluoxetine blocks the seizure of serotonin by human platelets. Is a weak antagonist of muscarinic, histamine H 1 , adrenergic? 1 and? 2 receptors, has little effect on re-uptake of dopamine. Promotes mood improvement, reduces feelings of fear and tension, eliminates dysphoria, causes a decrease in appetite. Does not cause sedation. It causes a reduction in obsessive-compulsive disorders. When taken in moderate therapeutic doses, it practically does not affect the function of the cardiovascular and other systems. A persistent clinical effect occurs in 1-2 weeks.
When ingested, the drug is well absorbed from the digestive tract (up to 95% of the dose taken), use with food slightly inhibits absorption of fluoxetine. C max in blood plasma reaches 6-8 hours and is 15-55 ng / ml. Bioavailability of fluoxetine after ingestion is more than 60%. The drug is well accumulated in tissues, easily penetrates the blood-brain barrier, binding to plasma proteins is 94.5% (including albumin and alpha-1-glycoprotein). Both enantiomeric forms of fluoxetine are equivalent, but S-fluoxetine is more slowly excreted and predominates over the R-form at C ss .
In the liver, enantiomers are metabolized by demethylation to the active metabolite of norfluoxetine and a number of unidentified metabolites. Metabolites are excreted by the kidneys (80%) and with fecal masses (15%), mainly in the form of glucuronides. The value of clearance of fluoxetine is 94-704 ml / min, norfluoxetine 60-336 ml / min. T 1/2 fluoxetine is 1-4 days for a single dose and 4-6 days for C ss , T 1/2 of norfluoxetine for 4-16 days in both cases, which causes the cumulation of the active forms, the slow achievement of their equilibrium level in the plasma, and the prolonged presence in the organism after cancellation. With renal failure, the rate of excretion of the drug does not change noticeably. In patients with liver cirrhosis T 1/2 Fluoxetine and norfluoxetine is extended 3-4 times. The drug is excreted in breast milk (up to 25% of the concentration in the blood serum).
- Depression of various etiologies;
- Bulimia nervosa;
- obsessive-compulsive disorder.
The drug is taken orally.
With depression, the initial dose is 20 mg 1 time / day in the morning, regardless of food intake. If necessary, the dose may be increased, but not more than up to 80 mg / day.
With bulimia, the drug is used in a daily dose of 60 mg divided into 2-3 doses.
For obsessive conditions - 20-60 mg / day. Supportive dose of 20 mg / day. The course of treatment is 3-4 weeks,
In elderly patients, the recommended daily dose is 20 mg. In patients with impaired liver and kidney function , lower doses and lengthening of the interval between doses are recommended.
From the side of the central nervous system: mania or hypomania, increased suicidal tendencies, tripod, headache, dizziness, tremor, irritability, sleep disorders, asthenia.
From the gastrointestinal tract: decreased appetite, nausea, dry mouth, increased salivation, diarrhea.
Allergic reactions: skin rash, hives.
Other: increased sweating, weight loss, decreased libido, systemic disorders of the lungs, kidneys or liver, vasculitis.
- simultaneous administration with MAO inhibitors;
- the period of breastfeeding;
- severe violations of the kidney and liver (CC less than 10 ml / min);
- Suicidal mood;
- Hypersensitivity to the drug.
With caution: diabetes mellitus, epileptic syndrome of various genesis and epilepsy (including in the anamnesis), Parkinson's disease, compensated renal and / or liver failure, cachexia.
PREGNANCY AND LACTATION
Contraindicated during pregnancy and during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe violations of kidney function (QC less than 10 ml / min).
With caution: compensated renal failure. Patients with impaired renal function are recommended to use lower doses and lengthen the interval between doses.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
With caution: compensated hepatic insufficiency. In patients with impaired hepatic function, lower doses and lengthening of the interval between doses are recommended.
APPLICATION IN ELDERLY PATIENTS
In old age, treatment should begin with half the doses.
In elderly patients, the recommended daily dose is 20 mg.
In the treatment of patients with body weight deficiency, anorexigenic effects should be considered (a progressive loss of body weight is possible).
In patients with diabetes, the administration of fluoxetine increases the risk of developing hypoglycemia, and when it is canceled, hyperglycemia. In this regard, the dose of insulin and / or any other hypoglycemic agents used orally should be adjusted. Before the onset of significant improvement in treatment, patients should be under the supervision of a physician.
The interval between the end of therapy with MAO inhibitors and the initiation of treatment with fluoxetine should be at least 14 days; between the end of treatment with fluoxetype and the initiation of therapy with MAO inhibitors - at least 5 weeks.
With liver disease and in old age, treatment should begin with half the doses. During treatment should refrain from taking ethanol and practicing potentially dangerous activities that require increased attention and speed of mental and motor reactions.
Symptoms: agitation, motor anxiety, convulsive seizures, heart rhythm disturbances, tachycardia, nausea, vomiting.
Treatment: specific antagonists to fluoxetine have not been found. Symptomatic therapy, gastric lavage with the appointment of activated charcoal, convulsions - diazepam, maintenance of breathing, cardiac activity, body temperature.
It is impossible to apply the drug simultaneously with MAO inhibitors, including antidepressants - MAO inhibitors, furazolidone, procarbazip, selegiline, as well as tryptophan (a precursor of serotonin), since the development of a serotonergic syndrome is possible. Symptoms may include confusion, hypomania, motor anxiety, agitation, convulsions, dysarthria, hypertensive crisis, chills, tremor, nausea, vomiting, diarrhea.
Fluoxetine enhances the effect of alcohol, hypoglycemic drugs and central-action drugs that cause depression of the central nervous system.
Fluoxetine blocks the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, cherfenadine, phenytoin, which leads to an increase in serum concentrations, increasing their effect and increasing the frequency of complications; with the simultaneous use of tricyclic antidepressants it is necessary to reduce their dose by 2 times.
The combined use of fluoxetine and lithium salts requires careful monitoring of the concentration of lithium in the blood. it is possible to change it (both upward and downward).
When used simultaneously with drugs that have a high degree of binding to proteins, especially with anticoagulants and digitoxin, it is possible to increase plasma concentrations of free (unbound) drugs and increase the risk of developing adverse effects.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
List B. In a dry, the dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 2 years 6 months.