Trade names
Apo-Fluoxetine. Bioksetin. Depreks. Deprenon. Portal. Prodep. Prozac. Profluzak. Flokset. Fluval. Fluksonil. Flunat. Fluoxetine. Flyudak. Frameks.
Subgroup
Selective serotonin inhibitors reverse the seizure.
Action
Pharmacological Effects - antidepressive. Promotes the improvement of mood, reduces anxiety and stress, eliminates dysphoria. It is sedative effect. Persistent clinical effect occurs within 1-2 weeks of treatment.
Mechanism of Action
The mechanism of action is related to selective blockade of reverse neuronal capture of serotonin in the central nervous system. Fluoxetine is a weak antagonist of choline-, adreno-and gistaminovyh receptors. Unlike most antidepressants, Fluoxetine, apparently, does not cause decline in functional activity postsinapticheskih b-adrenoretseptorov.Pri admission to secondary therapeutic doses virtually no effect on the function of the cardiovascular and other systems.
Pharmacokinetics
After a single injection 40 mg into the Cmax in plasma observed after 6-8 h and is 15-55 ng / ml. The capsules and aqueous solution of the drug bioequivalent, eating does not affect the bioavailability. At concentrations up to 1000 ng / ml Fluoxetine to 94.5% associated with blood proteins, including albumin and alfa1-glycoprotein. Both enantiomeric forms ekvieffektivny, but S-Fluoxetine displayed slower and dominates over the R-form, with the equilibrium concentration. In the liver enantiomers demetiliruyutsya to norfluoksetina. T1 / 2 Fluoxetine is 1-3 days after a single application and 4-6 days after reaching the equilibrium concentration. T1 / 2 norfluoksetina - 4-16 days in both cases, causing significant cumulation of reactive, slow achievement of equilibrium levels in plasma and prolonged presence in the body after the repeal. In patients with hepatic cirrhosis T1 / 2 extended by 3-4 times.
Indications
* Depression
* Obsessive-compulsive state
* Bulimia, anorexia
Contraindications
Glaucoma, urinary bladder atony, severe violations of kidney function, benign prostate hyperplasia, the simultaneous appointment of MAO inhibitors, spastic syndrome of different genesis, epilepsy, pregnancy, lactation, hypersensitivity to Fluoxetine.
Side Effects
Anxiety, nervousness, lethargy, insomnia, rapid fatigue, headache, dizziness, tremors, convulsive status, reduction of libido, anorexia, weight loss, nausea, vomiting, dyspepsia, dry mouth, diarrhea, increased salivation, rash, urticaria, which is often accompanied by systemic violations of the lung, kidney or liver vaskulity.
Interaction
If you are applying Fluoxetine with drugs which have a depressing effect on the central nervous system, as well as possibly significant increase in ethanol depressant actions in the CNS, as well as increasing the chance of seizures.
When applied simultaneously with drugs that possess a high degree of binding to proteins, especially with anticoagulants or digitoksinom may increase the concentration in the blood plasma of free (unbound) drugs and increased risk of adverse effects, with medication lithium - may increase the concentration of lithium, and development of toxic effects; with phenytoin - increasing its concentration in blood plasma and the development of toxic effects, with tryptophanyl - may strengthen the agitation, motor disturbance, misconduct by ZHKT.
When applied simultaneously with MAO inhibitors (eg selegiline or moklobemidom), due to increased content of serotonin and the suppression of a seizure, there is a significant increase in the number of serotonin in the synapse - serotoninovy syndrome "in which there are hyperthermia, muscle rigidity, mioklonus, as well as manifestations of mental instability and physiological state of the body until death.
Dosing and Administration in Adults
Inside. When depression - 20 mg in the morning to rise no more than 80 mg in 2-3 reception, with bulimia - 60 mg in 3 admission, with obsessive-compulsive states - 20-60 mg / day.
Pregnancy and lactation
Not applicable.
Overdosage
Symptoms: nausea, vomiting, central nervous system excitation, gipomaniya, convulsions.
Treatment: induction of vomiting or gastric lavage, the appointment of activated charcoal, symptomatic and supportive therapy.
Cautions
With great care used in patients with disorders of liver and kidney function, with a history of seizures, cardio-vascular diseases. Patients with diabetes may change in the level of glucose in the blood, which requires correction gipoglikemicheskih drug dosing regime. When using a weakened patients receiving Fluoxetine increases the likelihood of development of epileptic seizures. If you are applying Fluoxetine and Electro-therapy may develop prolonged epileptic seizures. Fluoxetine can be applied not earlier than 14 days after the lifting of MAO inhibitors. The period after the abolition of Fluoxetine prior to the start of therapy MAO inhibitors should not be less than 5 weeks. Patients older require correction dosing regime. Safety Fluoxetine application in children has not been established. During the period of treatment to avoid alcohol. Impact on ability to driving a car, and management arrangements in the period of treatment should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
