Expiration date: 04/2026
Pharmachologic effect:
Fluoxetine has an antidepressant, anorexigenic effect. Selectively blocking the reuptake of serotonin (5-HT) neurotransmission in the central nervous system neurons.
Pharmacokinetics:
If ingestion is well absorbed from the gastrointestinal tract (up to 95% of the dose), the use of food slows the absorption of fluoxetine significantly. Cmax plasma levels achieved after 6-8 hours. The bioavailability after oral administration of fluoxetine is more than 60%. The drug was well accumulates in the tissues, easily penetrates through the BBB. Binding to plasma proteins - more than 90%. It is metabolized in the liver by demethylation to the active metabolite norfluoxetine and a number of unidentified metabolites. Report the news, Cl fluoxetine - 94-704 ml / min, norfluoxetine - 60-336 ml / min. renal insufficiency did not have a noticeable effect on the rate of excretion of fluoxetine. About 12% of the drug is released through the digestive tract. T1 / 2 of fluoxetine - about 2-3 days, norfluoxetine - 7-9 days. Patients with liver failure T1 / 2 of fluoxetine and norfluoxetine lengthened. The drug is excreted in breast milk (25% of the serum concentration).
Description of the pharmacological actions:
Inhibition of reuptake of serotonin leads to increasing the concentration of the neurotransmitter in the synaptic cleft, amplifies and prolong its effect on post-synaptic receptor sites. At therapeutic doses fluoxetine blocks the uptake of serotonin human platelets. He is a weak antagonist of muscarinic, histamine H1, and adrenergic & alpha- & alpha2-receptors, has little effect on the reuptake of dopamine. It causes reduction of obsessive-compulsive disorders, and anorexia, which may lead to weight loss. It does not cause sedation. When taken in high therapeutic doses, has practically no effect on the function of the cardiovascular and other systems.
Testimony:
Depression different genesis, obsessive-compulsive disorders, neurosis bulimic.
Contraindications:
Hypersensitivity to the drug, concomitant use with MAO inhibitors, severe renal impairment (Cl creatinine <10 ml / min) and liver, pregnancy, breastfeeding.
With care - diabetes, convulsions and epilepsy of various origins (including history), Parkinson's disease, compensated renal and / or hepatic insufficiency, excessive weight loss, suicidal thoughts.
Application of pregnancy and breastfeeding:
Contraindicated during pregnancy. At the time of treatment should stop breastfeeding.
Side effect:
CNS: hypomania or mania, increased suicidal tendencies, anxiety, irritability, agitation, dizziness, headache, tremor, sleepiness or insomnia, asthenic disorders. With the development in patients receiving fluoxetine seizures drug should be discontinued.
On the part of the digestive tract: loss of appetite, taste disturbance, nausea, vomiting, dry mouth or hypersalivation and diarrhea. Perhaps anorexia development and weight loss.
From the urogenital system: incontinence or urinary retention, dysmenorrhea, vaginitis, decreased libido, sexual dysfunction in men (delayed ejaculation).
Other: rarely - allergic reactions such as skin rash, hives, itching, chills, fever, pain in muscles and joints (use of antihistamines and steroids), increased sweating, hyponatremia, tachycardia, disturbance of the visual acuity, vasculitis.
These side effects often occur at the beginning or fluoxetine with increasing dose.
Drug Interactions:
Incompatible with MAO inhibitors, other antidepressants, furazolidone, procarbazine, selegiline, and tryptophan (a precursor of serotonin), as may develop serotonin syndrome, manifesting confusion, hypomania, agitation, seizures, dysarthria, hypertensive crisis, chills, tremors, nausea, vomiting, diarrhea.
Simultaneous administration of fluoxetine with alcohol or drugs with central action, causing inhibition of the central nervous system, enhances their effect.
Fluoxetine metabolism blocking tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin (diphenylhydantoin), which leads to an increase in their concentration in the serum, amplifying their effects and increasing the incidence of complications.
Combined use of fluoxetine and lithium salts requires close monitoring of the concentration of lithium in the blood, because it may increase.
Fluoxetine increases the effects of hypoglycemic agents.
In an application with drugs, possessing a high degree of protein binding, especially with anticoagulants and digitoxin, may increase the plasma concentration of free (unbound) drug and increase the risk of adverse effects.
Dosage and administration:
Inside, regardless of meals. Initial dose - 20 mg 1 time per day in the morning, if necessary, the dose may be increased to 40-60 mg / day, divided into 2-3 doses. The maximum daily dose - 80 mg.
The clinical effect develops within 1-4 weeks after initiation of treatment, some patients it may be achieved later.
Obsessive-Compulsive Disorder: The recommended dose - 20-60 mg / day. When bulimic neurosis - 60 mg / day, divided into 2-3 doses.
Elderly patients daily dose - 20 mg.
In patients with impaired hepatic and renal function is recommended to use lower doses and lengthening of the interval between doses.
Overdose:
Symptoms: agitation, seizures, irregular heartbeat, tachycardia, nausea, vomiting.
Treatment: specific antagonists to fluoxetine were found. Symptomatic therapy, gastric lavage with the appointment of activated charcoal, in convulsions - diazepam, maintenance of respiration, cardiac activity, body temperature.
Special instructions:
Patients with diabetes may develop hypoglycemia during therapy with fluoxetine and hyperglycaemia after its cancellation. Against the background of electroconvulsive therapy may develop prolonged seizures. In the treatment of patients with deficiency of body weight should be considered anorectic effects (possible progressive loss of body weight). After discontinuation of its therapeutic serum concentrations may persist for several weeks. During treatment with fluoxetine intake of alcoholic beverages is not allowed. Fluoxetine may adversely affect the performance of work requiring a high rate of mental and physical reactions (drive motor vehicles, machinery, working at heights, etc.). The interval between the end and the beginning of therapy MAO inhibitors fluoxetine treatment should be at least 14 days between the end and the beginning of treatment with fluoxetine therapy MAO inhibitors - not less than 5 weeks. When liver disease and old age should begin treatment with a dose of 1/2.
