Fluoxetine capsules 20 mg 30 pcs
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Active ingredients
Fluoxetine
Release form
Capsules
Composition
The composition and the form of Fluoxetine capsules: 1 capsule contains 10 or 20 mg fluoxetine.
Pharmacological effect
Pharmacological action - antidepressant, anorexigenic.
Pharmacokinetics
Selectively inhibits the reuptake of serotonin, which leads to an increase in its concentration in the synaptic cleft, enhancement and prolongation of its action on postsynaptic receptors. By increasing serotonergic transmission, a negative feedback mechanism inhibits the neurotransmitter metabolism. With prolonged use reduces the activity of 5-HT1 receptors. It also blocks the reuptake of serotonin in platelets. It has little effect on the reuptake of norepinephrine and dopamine. It has no direct effect on serotonin, m-cholinergic, H1-histamine and alpha-adrenergic receptors. Unlike most antidepressants, does not cause a decrease in the activity of postsynaptic beta-adrenergic receptors. It is effective in endogenous depressions and obsessive-compulsive disorders. It improves mood, reduces tension, anxiety and fear, eliminates dysphoria. It has anorexigenic effects and may cause weight loss. In patients with diabetes mellitus, it can cause hypoglycemia, with the withdrawal of fluoxetine - hyperglycemia. A pronounced clinical effect in depression occurs after 1-4 weeks of treatment, with obsessive-compulsive disorders - after 5 weeks or more. Well absorbed from the digestive tract. The effect of "first pass" through the liver is mild. Capsules and an aqueous solution of fluoxetine are equivalent in effectiveness. After a single dose of 40 mg of Cmax, fluoxetine is reached in 4–8 hours and amounts to 15–55 ng / ml, when taken in the same dose for 30 days, Cmax of fluoxetine is 91–302 ng / ml, norfluoxetine - 72–258 ng / ml. At concentrations up to 200–1000 ng / ml, 94.5% binds to blood proteins, including albumin and alpha1-glycoprotein. Enantiomers are equally effective, but S-fluoxetine is eliminated more slowly and prevails over the R-form at an equilibrium concentration. Easily penetrates the BBB. In the liver, enantiomers demethylate with the participation of the cytochrome P450 isoenzyme CYP2D6 to norfluoxetine and other unidentified metabolites, and S-norfluoxetin is equal in activity to R- and S-fluoxetine and exceeds R-norfluoxetine. T1 / 2 fluoxetine is 1-3 days after a single dose and 4-6 days with long-term administration.T1 / 2 of norfluoxetine - 4–16 days in both cases, which causes a significant accumulation of substances, the slow achievement of their equilibrium level in the plasma and the long presence in the body after withdrawal. In patients with cirrhosis of the liver, T1 / 2 fluoxetine and its metabolites are lengthened. Excreted within 1 week mainly by the kidneys (80%): unchanged - 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 by the intestines. In the event of impaired renal function, the elimination of fluoxetine and its metabolites slows down. During dialysis is not displayed (due to the large volume of distribution and a high degree of binding to plasma proteins). There is evidence of the effectiveness of fluoxetine in eating disorders (anorexia nervosa), alcoholism, anxiety disorders, including social phobia; diabetic neuropathy, affective, incl. bipolar disorders; dysthymia, autism, panic attacks, premenstrual syndrome, narcolepsy, catalepsy, obstructive sleep apnea syndrome, kleptomania, schizophrenia, schizoaffective disorders, etc.
Indications
Depression (regardless of the degree of depressive disorder, mild, moderate, severe), bulimia, anorexia, alcoholism, obsessive-compulsive disorder.
Contraindications
Atony of the bladder. Severe renal dysfunction. Simultaneous administration of MAO inhibitors. Glaucoma. Adenoma of the prostate gland. Congestive syndrome of various genesis. Epilepsy. Pregnancy. Lactation (breastfeeding). Increased sensitivity to the drug
Precautionary measures
Be wary to appoint in old age, with cardiovascular diseases, liver and / or kidney function failure. Careful observation of patients with suicidal tendencies, especially at the beginning of treatment, is required. The risk of suicide is greatest in patients who have previously taken other antidepressants, and patients who have excessive fatigue, hypersomnia, or motor restlessness during treatment with fluoxetine. When treating patients with low body mass, the anorexigenic properties of fluoxetine should be considered. When conducting electroconvulsive therapy with fluoxetine, prolonged epileptic seizures may occur.The interval between the withdrawal of MAO inhibitors and the start of fluoxetine should be more than 2 weeks, and between the withdrawal of fluoxetine and the intake of MAO inhibitors - at least 5 weeks. Be careful with drivers of vehicles and people whose activities require increased concentration of attention and quickness of psychomotor reactions. Alcohol should be avoided during treatment.
Use during pregnancy and lactation
When pregnancy should be prescribed only in case of emergency. When fluoxetine is used during pregnancy, an increased risk of preterm birth, developmental abnormalities and low adaptation of newborns (including difficulty in breathing, cyanosis, excitability) are noted.
Dosage and administration
In depressions of various origins, the initial dose of Fluoxetine 20 mg 1 time / day in the first half of the day. If necessary, the dose of the drug may be increased. The maximum daily dose is 80 mg in 2-3 doses. With bulimia and for elderly patients, the drug is prescribed 20 mg 3 times / day, with obsessive conditions - 20-60 mg / day. Maintenance therapy - 20 mg / day. The course of treatment is 3-4 weeks.
Side effects
On the part of the central nervous system, headache, nervousness, sleep disturbance, increased anxiety, increased fatigue. On the side of the gastrointestinal tract, nausea, diarrhea, dry mouth, vomiting, loss of appetite. feeling hot, hyponatremia.
Overdose
Symptoms: nausea, vomiting, agitation, anxiety, hypomania, convulsions, major epileptic seizures. Two deaths from acute overdose of fluoxetine (in combination with maprotiline, codeine, temazepam) have been described. Treatment: gastric lavage, taking activated carbon, sorbitol, ECG monitoring, symptomatic and supportive therapy, with seizures - diazepam. There is no specific antidote. Forced diuresis, peritoneal dialysis, hemodialysis, blood transfusion are ineffective.
Interaction with other drugs
Incompatible with MAO inhibitors, other antidepressants, furazolidone, procarbazine, because causes serotonergic syndrome (chills, hyperthermia, muscle rigidity, myoclonus, vegetative lability, hypertensive crisis, agitation, tremor, motor restlessness, convulsions, diarrhea, hypomania, delirium, coma; fatal outcome.When taken concurrently with drugs with a high degree of binding to plasma proteins (oral anticoagulants, oral hypoglycemic agents, cardiac glycosides, etc.), the risk of developing side effects of the free fraction in the blood may increase. The risk of bleeding increases while taking warfarin. It inhibits the biotransformation of drugs metabolized by the CYP2D6 isoenzyme of cytochrome P450 (tricyclic antidepressants, dextromethorphan, etc.). Extends T1 / 2 diazepam, potentiates the effects of alprazolam. When taken simultaneously, it changes (increases or decreases) the concentration of lithium in the blood plasma, increases the content of phenytoin (before the clinical manifestations of its overdose); the level of tricyclic antidepressants (imipramine, desipramine) increases 2-10 times. Tryptophan increases the serotonergic properties of fluoxetine (possible agitation, anxiety, gastrointestinal dysfunction). Incompatible with ethanol.
special instructions
In patients with diabetes mellitus, hypoglycemia may develop during therapy with fluoxetine and hyperglycemia after its withdrawal. On the background of electroconvulsive therapy, the development of prolonged epileptic seizures is possible. After the use of MAO inhibitors, fluoxetine can be prescribed not earlier than 14 days. MAO and / or thioridazine inhibitors should not be used earlier than 5 weeks after discontinuing fluoxetine. With the development, against the background of fluoxetine, convulsive seizures, the drug should be canceled. When treating patients with a body mass deficiency, anorexigenic effects should be taken into account (progressive loss of body weight is possible). After discontinuation of the drug, its therapeutic serum concentration may persist for several weeks. During treatment with fluoxetine, alcohol is not allowed. Reception of fluoxetine may adversely affect the performance of work that requires a high rate of mental and physical reactions (control of mechanical vehicles, mechanisms, work at height, etc.).