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Fluoxetine (Fluoxetinum, Fluoxetini) - selectively inhibits the reuptake of serotonin, which leads to an increase in its concentration in the synaptic cleft, amplification and prolongation of its action on postsynaptic receptors. Boosting serotonergic transmission, by a negative feedback mechanism inhibits neurotransmitter exchange. Prolonged use reduces the activity of 5-HT1 receptors. Blocks and serotonin reuptake in platelets. It has little effect on the reuptake of noradrenaline and dopamine. It has no direct effect on serotonin, m-cholinergic, H1-histamine and alpha-adrenergic receptors. Unlike most antidepressants, does not cause reduction in activity of beta-adrenergic postsynaptic.
Effective with endogenous depression and obsessive-compulsive disorders. It improves mood, reduces stress, anxiety and feelings of fear, eliminates dysphoria. Has anorectic action, can cause weight loss. In patients with diabetes can cause hypoglycemia, the abolition of fluoxetine - hyperglycemia. Expressed clinical effect in depression occurs within 1-4 weeks of treatment for obsessive-compulsive disorder - after 5 weeks or more.
Well absorbed from the gastrointestinal tract. The effect of "first pass" through the liver is weakly expressed. Capsules and fluoxetine aqueous solution equal in effectiveness. After receiving a single dose of 40 mg fluoxetine Cmax achieved within 4-8 hours and is 15-55 ng / ml, when receiving the same dose for 30 days fluoxetine Cmax is 91-302 ng / mL norfluoxetine - 72-258 ng / ml. At concentrations up to 200-1000 ng / mL of fluoxetine at 94.5% bound to blood proteins, including albumin and alpha-1-glycoprotein. The enantiomers were equally effective, but the S-fluoxetine appears slower and dominates the R-shape at the equilibrium concentration. It is easy to penetrate the BBB. The liver demethylated enantiomers involving cytochrome P450 isoenzyme CYP2D6 to norfluoxetine and other unidentified metabolites, the S-norfluoxetine equal in activity R- and S-fluoxetine and norfluoxetine R-superior. T1 / 2 of fluoxetine is 1-3 days after a single dose and 4-6 days on prolonged administration. T1 / 2 norfluoxetine - 4-16 days in both cases that cause significant cumulation substances, their slow attainment of equilibrium in the plasma levels and long-term presence in the body after cancellation. Patients with cirrhosis T1 / 2 of fluoxetine and its metabolites is lengthened. Displays for 1 week in the kidney (80%) unaltered - 11.6%, as fluoxetine glucuronide - 7.4%, norfluoxetine - 6.8%, norfluoxetine glucuronide - 8.2%, more than 20% - hippuric acid, 46% - other compounds; 15% is excreted in the intestine. If the kidney function of excretion of fluoxetine and its metabolites is slowed down. When dialysis is not output (due to the large volume of distribution and a high degree of binding to plasma proteins).
There is evidence of the effectiveness of fluoxetine with eating disorders (anorexia nervosa), alcoholism, anxiety disorders including social phobia; diabetic neuropathy, affective, including bipolar disorder; dysthymia, autism, panic attacks, premenstrual syndrome, narcolepsy, catalepsy syndrome, obstructive sleep apnea, kleptomania, schizophrenia, schizoaffective disorders, and others.
Depression (especially accompanied by pain), including: the ineffectiveness of other antidepressants, obsessive-compulsive disorder, bulimia nervosa.
Hypersensitivity, the use of MAO inhibitors (in the previous 2 weeks), hepatic and renal impairment (creatinine clearance less than 10 ml / min), epilepsy and convulsive conditions (in history), suicidal thoughts, diabetes, bladder atony, angle-closure glaucoma, hypertrophy cancer.
Incompatible with MAO inhibitors, other antidepressants, furazolidone, procarbazine, because cause serotonergic syndrome (fever, hyperthermia, muscle rigidity, myoclonus, autonomic lability, hypertensive crisis, agitation, tremors, restlessness, convulsions, diarrhea, hypomania, delirium, coma, death is possible when taken concomitantly with drugs that have a high degree. plasma protein binding (oral anticoagulants, oral hypoglycemic agents, cardiac glycosides, and others.), the possibility of mutual displacement of the connection with the protein with a change in the blood of the free fraction concentration, the risk of side effects increases. increased risk of bleeding in patients receiving warfarin. Inhibits biotransformation drugs metabolized with the participation of the CYP2D6 isoenzyme of cytochrome P450 (tricyclic antidepressants, dextromethorphan, vinblastine, carbamazepine). Extends the T1 / 2 of diazepam, potentiates alprazolam effects. at the same time.The changes (increases or decreases) the concentration of lithium in blood plasma increases the content of phenytoin ( before clinical manifestations of overdose); level tricyclic antidepressants (imipramine, desipramine) increases 2-10 times. Tryptophan enhances the serotonergic properties of fluoxetine (possible agitation, restlessness, disturbance of gastrointestinal function). Incompatible with ethanol.
Symptoms include nausea, vomiting, agitation, restlessness, hypomania, seizures, grand mal seizures. described two deaths from acute overdose fluoxetine (in combination with maprotiline, codeine, temazepam).
Treatment: gastric lavage, activated charcoal, sorbitol, ECG monitoring, symptomatic and supportive therapy, in convulsions - diazepam. No specific antidote. Forced diuresis, peritoneal dialysis, hemodialysis, blood transfusion is ineffective.
Inside, during a meal, in 1-2 divided doses (preferably in the morning). Initial and maintenance doses of 20 mg / day. If necessary, the dose is increased every week by 20 mg / day. The maximum daily dose - 80 mg for patients with middle and old age - 60 mg. The course of treatment - 3-4 weeks, with obsessive-compulsive disorder - 5 weeks or more, for bulimia nervosa - 1 week.
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