Fluoxetine

Fluoxetine is an antidepressant that belongs to the group of selective inhibitors. This tool is prescribed for obsessive and depressive states.

Increases the amount of serotonin in the brain, thereby prolonging its stimulating effect on the nervous system. Increases the transmission of serotonin, does not allow its re-uptake in platelets. It increases mood, relieves tension, sensation of anxiety, eliminates irritability and dislike of the environment.

Recommended for use in depressive states, accompanied by a sense of fear, eating disorders (bulimia), mental disorders, as well as in cases of ineffectiveness of other drugs with antidepressant effect.

Clinical and pharmacological group

Antidepressant, a derivative of propylamine.

Terms of sale from pharmacies

Can buyby prescription.

Price

How much does Fluoxetine cost in pharmacies? The average price in 2018 is at the level of90 rubles.

Composition and form of release

Fluoxetine is available in the form of hard gelatin capsules of 10 or 20 mg. Capsules have a white body and white (10 mg) or a green (20 mg) cap. Inside are white or white with a yellowish tinge of granules and powder.

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The preparation is packaged in blisters (5 or 10 capsules) or polymer cans (20, 30, 50 or 100 capsules) and packed in cardboard packs (2 or 4 blisters for 7 capsules, 2, 3, 5 or 10 blisters for 10 capsules or 1 can in a pack).

The composition of 1 capsule includes:

active ingredient: fluoxetine - 10 or 20 mg;
auxiliary substances: povidone, lactose monohydrate, potato starch, calcium stearate;
composition of the shell: water, titanium dioxide, gelatin; additionally for capsules 20 mg - indigocarmine, iron oxide yellow.

Pharmacological effect

The drug is a derivative of propylamine. The pharmacological action consists in partial suppression of the reuptake of serotonin. As a result, the concentration of the drug in the synaptic cleft increases and its effect increases.

The active substance of the medicine removes anhedonia, reduces tension, anxiety and feelings of fear. Fluoxetine does not have a toxic effect on the human body and does not provoke the appearance of orthostatic hypotension. The desired therapeutic effect occurs in one to two weeks.

The drug has a minimal effect on the metabolism of acetylcholine, dopamine and norepinephrine. Especially effective in obsessive-compulsive disorders and endogenous depression. After intake, dysphoria is eliminated and the mood improves. The pronounced therapeutic effect with depression is observed after 2-4 weeks of admission, and with compulsive disorders - after 5 weeks.

The drug is well absorbed from the digestive tract. At the first passage through the liver, all components undergo a weak metabolic process. The process of taking food does not affect the degree of absorption, but slows its speed. The highest degree of saturation of the drug in blood plasma is achieved after six to eight hours after its use. In this case, the medication should be continuous (for several weeks).

The level of ability to bind to proteins is 94%. The process of metabolism takes place in the liver in the form of demethylation, with the formation of norfluoxetine (the main active metabolite). The half-life of the drug is 2-3 days after a single dose. With long-term use of fluoxetine, this period is 5-6 days.

The medication is excreted mainly by the kidneys: 11.6% in the unmodified state, 7.4% in the form of fluoxetine glucuronide, 46% in other compounds, 20% in the form of hippuric acid. With improper functioning of the kidneys, the process of excretion of metabolites is significantly slowed down. When the dialysis is performed, the drug is not taken out at all. This is due to the huge volume of distribution and the high degree of binding to plasma proteins.

The effectiveness of the drug was noted even with such disorders as: anorexia nervosa and diabetic neuropathy.

The mechanism of action of the drug is based on the selective inhibition of reverse blocking of serotonin at the sites of neurotransmitter transmission. The drug is able to have a timoanaleptic and stimulating effect. After a single dose, the feeling of anxiety and fear decreases, but the drug does not have a complete soothing effect.

Indications for use

Fluoxetine can be used only on the advice of a doctor in the case of the following indications for admission:

depressive states of various origin;
bulimic neuroses;
obsessive-compulsive disorders.

Contraindications

According to the instructions, fluoxetine is contraindicated in the following cases:

Individual intolerance to the drug;
Atony of the bladder;
Closed-angle glaucoma;
Pronounced hepatic or renal insufficiency;
Treatment with MAO inhibitors;
Pregnancy and lactation;
Increased propensity to suicide;
Hypertrophy of the prostate.

The use of fluoxetine in patients with Parkinson's syndrome, epilepsy, diabetes mellitus, or severe exhaustion requires extreme caution.

Intended use for pregnancy and lactation

The safety of the drug in pregnant women is poorly understood, the results of individual published epidemiological studies are contradictory. In some random and cohort studies, there was no increase in the likelihood of congenital developmental abnormalities.

The prospective study conducted by ENTIS allows us to talk about an increase in the likelihood of developing congenital anomalies in the structure of large vessels or heart in children whose mothers took fluoxetine in the 1st trimester of pregnancy, compared with children whose mothers did not receive this drug.

It was not possible to establish a reliable relationship between the use of the drug in the early stages of pregnancy and the formation of malformations in the fetus. The specific group of CCC abnormalities was also not determined.

The use of SSRIs in the last weeks of pregnancy contributes to the development of complications in newborns, in particular, the prolongation of the duration of ventilation and probe nutrition and the duration of hospitalization.

There are mentions of the development of apnea, respiratory distress syndrome, seizures, hypoglycemia, lability of body temperature and blood pressure, tremor, hyperreflexia, vomiting, cyanosis, difficulties with adequate nutrition, constant crying, excitability, nervous irritability.

The listed pathological conditions can be a consequence of the syndrome of withdrawal of SSRIs or the manifestation of their toxic effects.

Dosage and route of administration

As indicated in the instructions for use, capsules of Fluoxetine are intended for ingestion regardless of food. They are not chewed and washed down with enough water. The mode of taking the drug and the dosage depend on the medical indications:

Obsessive-compulsive disorder - the recommended therapeutic dosage is 20-60 mg per day.
Bulimic neurosis - capsules Fluoxetine is used in a dosage of 60 mg divided into 2-3 doses during the day.
Depression of different origin - the initial dosage is 20 mg (1 tablet) 1 time per day, preferably before lunch. If necessary, it increases to 40-60 mg per day and is divided into 2-3 doses. The maximum daily dose should not exceed 80 mg. The therapeutic effect develops not earlier than 1-2 weeks after the start of the course of therapy.

There is usually no need to reduce dosage for elderly patients, provided normal functional activity of the liver or kidneys. The doctor sets the duration of the therapy course individually.

The withdrawal syndrome

In many cases, with the cessation of fluoxetine treatment (especially when the drug is abruptly withdrawn), withdrawal symptoms are noted. The results of clinical studies indicate that about 60% of patients with the withdrawal of therapy developed various side effects. These data are valid for both the fluoxetine group and the placebo group: in the first case, 17% of the events were severe, in the second case, 12%.

Several factors influence the risk of withdrawal syndrome (including the duration of the course of therapy and the rate of dose reduction). Most often, patients complain of dizziness, sensory disorders (including paresthesia), asthenia, agitation, anxiety, sleep disturbances (including deep sleep and insomnia), nausea, vomiting, headaches, tremors. Usually, these episodes have mild or moderate severity, but in some patients they are more pronounced.

In most cases, withdrawal syndrome passes independently for two weeks, but in some cases, its manifestations may be longer (2 to 3 months or more). The abolition of fluoxetine should be gradual in view of the patient's condition (usually this process takes 1-2 weeks).

Suicidal risks associated with taking fluoxetine

In patients with depression, the likelihood of committing suicidal attempts (may be actual until the onset of stable remission) increases. As with the use of other antidepressants, against the background of fluoxetine therapy, or shortly after its completion, there were isolated cases of suicidal thoughts and behavior. That is why it is necessary to ensure close monitoring of patients belonging to the risk group and to convince them in the need to immediately inform the doctor about any unpleasant feelings and thoughts that cause anxiety.

Studies involving adult patients with major depressive disorder allowed the following risk factors for suicide in both groups (taking fluoxetine and placebo):

before the start of therapy - a more severe course of depression, the presence of thoughts about death;
in the period of therapy - the development of insomnia, weighting depression.
One of the risk factors in the treatment of fluoxetine was the development of severe psychomotor agitation (eg, panic, akathisia, agitation).

The emergence or presence of these conditions before or during treatment is a reason for strengthening clinical control or correction of treatment.

Adverse Reactions

The use of fluoxetine can cause the following side effects:

On the part of the digestive system: dry mouth, nausea, diarrhea, vomiting, indigestion.
From the side of the musculoskeletal system, there may be muscle twitching.
On the part of the sensory organs with the systematic administration of fluoxetine, the side effect of the drug may be manifested by blurred vision.
From the side of the central nervous system: sleep disorders, headaches, anxiety, drowsiness, nervousness, dizziness, psychomotor excitation, tremor, hyperactivity, attention or coordination impairment, ataxia, lethargy.
From the cardiovascular system: hot flushes, hypotension, atrial flutter, vasculitis.
From the genitourinary and reproductive system: frequent urination, decreased libido, erectile dysfunction, ejaculation, gynecological bleeding.
On the part of metabolism: hypoglycemia, increased sweating, hyponatremia.
On the part of the skin: a polymorphous skin rash, hyperhidrosis, a tendency to bruising, itching, cold sweat, alopecia, urticaria, ecchymosis.

It is also possible to increase body temperature, shortness of breath, pain in the muscles and joints. When applying fluoxetine, the side effects of the drug often require its withdrawal.

Overdose

In case of accidental or deliberate admission of a large dose of fluoxetine, the patient needs urgent medical attention. There is no specific antidote, therefore, symptomatic treatment is performed. To accelerate the removal of the drug from the body, the stomach is washed and sorbents are given inside.

special instructions

Before you start using the drug, read the special instructions:

During the treatment period, do not drink alcohol.
Older patients need a correction of the dosing regimen.
The safety of fluoxetine in children is not established.
With special care apply in patients with impaired liver and kidney function, with epileptic seizures in history, cardiovascular diseases.
In patients with diabetes, blood glucose levels may change, which requires correction of the dosage regimen for hypoglycemic drugs. When used in weakened patients with fluoxetine, the likelihood of epileptic seizures increases.
With the simultaneous use of fluoxetine and electroconvulsive therapy, it is possible to develop prolonged epileptic seizures.
Fluoxetine can be used no earlier than 14 days after the abolition of MAO inhibitors. The period after the abolition of fluoxetine before initiating therapy with MAO inhibitors should be at least 5 weeks.

Compatibility with other drugs

When using the drug, it is necessary to take into account the interaction with other drugs:

There have been reports of increased effects of warfarin when used concomitantly with fluoxetine.
When used simultaneously with haloperidol, fluphenazine, maprotiline, metoclopramide, perphenazine, pericyazine, pimozide, risperidone, sulpiride, trifluoperazine, cases development of extrapyramidal symptoms and dystonia; with dextromethorphan - the case of hallucinations development is described; with digoxin - a case of increasing the concentration of digoxin in the blood plasma.
With simultaneous use with lithium salts, it is possible to increase or decrease the concentration of lithium in blood plasma.
With simultaneous use, it is possible to increase the concentration of imipramine or desipramine in blood plasma 2-10 times (may persist for 3 weeks after fluoxetine cancellation).
When used simultaneously with drugs that exert a depressant effect on the central nervous system, with ethanol possibly a significant increase in the inhibitory effect on the central nervous system, as well as an increased likelihood of seizures.
When used simultaneously with MAO inhibitors, furazolidone, procarbazine, tryptophan, the development of serotonin syndrome (confusion, hypomaniacal state, motor anxiety, agitation, convulsions, dysarthria, hypertensive crisis, chills, tremor, nausea, vomiting, diarrhea).
With simultaneous use of fluoxetine inhibits the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin, which leads to an increase in their concentration in the blood serum, enhancing their therapeutic and side effects.
With simultaneous use, it is possible to suppress the biotransformation of drugs metabolized with the participation of the CYP2D6 isoenzyme.
When used simultaneously with hypoglycemic agents, it is possible to intensify their action.
With simultaneous use with propofol, a case is described in which spontaneous movements were observed; with phenylpropanolamine - described a case in which there was dizziness, weight loss, hyperactivity.
With simultaneous use, it is possible to enhance the effects of flecainide, mexiletine, propafenone, thioridazine, zuclopentixol.

Reviews

We offer you to read reviews of people who used Fluoxetine:

Eugene. In the past six months, I worked very hard, I did not have time and energy to rest. Then came such apathy and fatigue that it was not fruitful to work, I simply could not do anything. The mood was constantly at zero, nothing pleased. The familiar doctor advised me to take Fluoxetine. A month later, it became a little easier. Now I drink these pills for the 3rd month. Gradually, the mood and everything else is getting better. I'm satisfied.
Eve. Saw Fluoxetine, in principle, it suits me. The only thing - in the first weeks of taking the medicine began to notice a slight trembling of the hands, as a side effect, probably. But a month later it all passed. And the price of these pills is quite good, which can not but rejoice.
Tatyana. Stunning remedy for stress. Personally, I need only one capsule in order to calm down, as it should. But do not abuse them. I once drank 3 tablets and I was just put to sleep. And I slept long enough, and when the state woke up it was bad: my head ached, my appetite zero, no desire to do anything. So I replaced fluoxetine with regular herbal tea for a while.

Reviews of doctors about fluoxetine for weight loss are unequivocal: you can use a medicine to fight excess pounds only if the cause of weight gain is a mental disorder. When excess weight is the result of depression caused by stress or overeating, the drug for 2-3 weeks allows you to completely get rid of bouts of gluttony and for the first month to remove up to 5 kg.

Reviews losing weight about Fluoxetine (Lannacher, OZONE, etc.) allow you to conclude that to reduce weight on this drug can far from all: someone's appetite disappears completely (down to disgust in food), for someone it remains the same. However, in most cases the remedy has serious side effects: many people who took it noted a decrease in the sexual attraction and deterioration of sexual life, a sense of inhibition, severe pain, drowsiness, increased aggression, the appearance of suicidal thoughts. In addition, for many of the debilitated drugs, the need to stop driving and drinking alcohol, and the fact that fluoxetine is highly addictive.

Summarizing reviews, the following conclusions can be drawn: Fluoxetine is primarily a cure for depression and can only be taken if there is evidence and only under the supervision of a doctor.

Analogues

Structural analogs for the active substance:

Apo Fluoxetine;
Depres;
Depenone;
Portal;
Prodep;
Prozac;
Profluzak;
Floxet;
Fluval;
Fluxonil;
Flunisan;
Fluoxetine HEXAL;
Fluoxetine Lannacher;
Fluoxetine Nycomed;
Fluoxetine OBL;
Fluoxetine Canon;
Fluoxetine hydrochloride;
Framex.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

The shelf life of capsules Fluoxetine is 3 years. The drug should be stored in its original undamaged original packaging, dark, dry, inaccessible to children at an air temperature of no more than + 25 ° C.