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, prevents its reuptake in platelets. It improves mood, relieves tension, a feeling of anxiety, eliminates irritability and hostility towards others.

Recommended for use in depression, accompanied by a feeling of fear, eating disorder (bulimia), mental disorders, as well as in cases of ineffectiveness of other drugs with anti-depressive effects.

Clinico-pharmacological group

Antidepressant, propylamine derivative.

Terms of sale from pharmacies

You can buy by prescription.

Price

How much does fluoxetine cost in pharmacies? The average price in 2018 is at the level of 90 rubles.

Composition and release form

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

The drug 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 of 7 capsules, 2, 3, 5 or 10 blisters of 10 capsules or 1 bank in a pack).

The structure of 1 capsule includes:

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

Pharmacological effect

The drug is a derivative of propylamine. Pharmacological action is the partial suppression of serotonin reuptake. As a result, there is an increase in the concentration of the drug in the synaptic cleft and enhancement of its action.

The active substance of the drug eliminates 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 within a week or two.

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

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

The level of ability to bind with proteins is 94%. The process of metabolization 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 prolonged use of fluoxetine, this period is 5-6 days.

The drug is excreted mainly by the kidneys: in an unchanged condition it is 11.6%, in the form of fluoxetine glucuronide - 7.4%, other compounds - 46%, in the form of hippuric acid - 20%. When kidney malfunction, the process of excretion of metabolites slows down significantly. When conducting dialysis drug is not displayed at all. This is due to the huge volume of distribution and a high degree of binding to plasma proteins.

The efficacy 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 selective inhibition of the reverse blocking of serotonin at the sites of transmission of neurotransmitters. The drug is able to have thymoanaleptic and stimulating effect. After a single dose, the feeling of anxiety and fear diminishes, but the drug does not have a full sedative effect.

Indications for use

Fluoxetine can only be used on the advice of a doctor if the following indications are met:

  • depressive conditions of various origins;
  • bulimic neurosis;
  • obsessive compulsive disorders.

Contraindications

According to the instructions Fluoxetine is contraindicated in the following cases:

  • Individual intolerance to the drug;
  • Atony of the bladder;
  • Angle-closure glaucoma;
  • Severe hepatic or renal failure;
  • Treatment with MAO inhibitors;
  • Pregnancy and lactation;
  • Increased suicidal tendency;
  • Prostatic hypertrophy.

The use of fluoxetine in patients with Parkinson's syndrome, epilepsy, diabetes, or severe exhaustion requires special care.

Appointment during pregnancy and lactation

The safety of the drug in pregnant women has been little studied, the results of individual published epidemiological studies are controversial. In some random and cohort studies, no increase in the likelihood of congenital developmental anomalies has been identified.

A prospective study conducted by ENTIS suggests an increase in the likelihood of congenital anomalies in the structure of large vessels or the heart in children whose mothers took Fluoxetine in the 1st trimester of pregnancy, compared to children whose mothers did not receive this drug.

It was not possible to establish a reliable relationship between the administration of the drug in early pregnancy and the formation of malformations in the fetus. The specific group of CAS anomalies was also not determined.

The use of SSRIs in the last weeks of pregnancy contributes to the development of complications in newborns, in particular, an increase in the duration of mechanical ventilation and tube feeding and the duration of hospitalization.

There are references to 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.

These pathological conditions may be a consequence of the syndrome of cancellation of SSRIs or a manifestation of their toxic effects.

Dosage and method of use

As indicated in the instructions for use Fluoxetine capsules are intended for ingestion, regardless of the meal. They are not chewed and washed down with plenty of water. The dosage regimen and dosage depend on medical indications:

  • Obsessive compulsive disorder - the recommended therapeutic dosage is 20-60 mg per day.
  • Bulimic neurosis - Fluoxetine capsules are used in a dosage of 60 mg, divided into 2-3 doses during the day.
  • Depression of various origins - 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 does not develop earlier than 1-2 weeks after the start of a course of therapy.

The need to reduce the dosage for elderly patients is usually not, provided the normal functional activity of the liver or kidneys. The duration of the course of therapy the doctor sets individually.

Cancellation syndrome

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

The risk of withdrawal is influenced by several factors (including the duration of the course of therapy and the rate of dose reduction). Most often, patients complain of dizziness, sensory disturbances (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, the withdrawal syndrome resolves itself within two weeks, but in some cases its manifestations may be longer (from 2 to 3 months or more). Cancellation of fluoxetine should take place gradually, taking into account the patient's condition (usually this process takes 1-2 weeks).

Suicidal risks while taking fluoxetine

In patients with depression increases the likelihood of committing suicidal attempts (may be relevant until the onset of persistent remission). As with other antidepressants, on 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 carefully monitor the at-risk patients and convince them of the need to immediately inform the doctor of any unpleasant feelings and thoughts that cause anxiety.

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

before the start of therapy - more severe course of depression, the presence of thoughts about death;
during the period of therapy - the development of insomnia, the worsening of depression.
One of the risk factors for treatment with fluoxetine was the development of severe psychomotor arousal (for example, panic, akathisia, agitation).

The occurrence or the presence of these conditions before or during treatment is a reason to enhance the clinical control or correction of the 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, dyspepsia.
  • On the part of the musculoskeletal system, the appearance of muscle twitches is possible.
  • On the part of the senses, when taking Fluoxetine systematically, the side effect of the drug may be manifested by blurred vision.
  • From the side of the central nervous system: sleep disturbance, headaches, anxiety, drowsiness, nervousness, dizziness, agitation, tremor, hyperactivity, attention or coordination disorder, ataxia, lethargy.
  • Since the cardiovascular system: hot flashes, hypotension, atrial flutter, vasculitis.
  • From the genitourinary and reproductive system: frequent urination, decreased libido, erectile dysfunction, impaired ejaculation, gynecological bleeding.
  • Metabolism: hypoglycemia, increased sweating, hyponatremia.
  • On the part of the skin: polymorphic skin rash, hyperhidrosis, a tendency to bruise, pruritus, cold sweat, alopecia, urticaria, ecchymosis.

It may also increase body temperature, shortness of breath, pain in muscles and joints. When using Fluoxetine, the side effects of the drug often require its discontinuation.

Overdose

When accidentally or deliberately taking a large dose of fluoxetine, the patient needs urgent medical attention. There is no specific antidote, therefore symptomatic treatment is carried out. To speed up the elimination of the drug from the body, gastric lavage is performed and sorbents are given inside.

Special instructions

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

  1. During the period of treatment to prevent the use of alcohol.
  2. Elderly patients require correction dosing regimen.
  3. The safety of fluoxetine in children has not been established.
  4. With extreme caution used in patients with impaired liver and kidney function, with epileptic seizures in history, cardiovascular diseases.
  5. In patients with diabetes mellitus, a change in blood glucose level is possible, which requires correction of the dosage regimen of hypoglycemic drugs. When used in weakened patients while taking fluoxetine, the likelihood of developing epileptic seizures increases.
  6. With the simultaneous use of fluoxetine and electroconvulsive therapy may develop prolonged epileptic seizures.
  7. Fluoxetine can be applied no earlier than 14 days after discontinuation of MAO inhibitors. The period after discontinuation of fluoxetine before initiating therapy with MAO inhibitors should be at least 5 weeks.

Compatibility with other drugs

When using the drug, you must consider the interaction with other drugs:

  1. There are reports of increased effects of warfarin when it is used simultaneously with fluoxetine.
  2. With simultaneous use with haloperidol, fluphenazine, maprotilin, metoclopramide, perphenazine, peritsiazina, pimozide, risperidone, sulpiride, trifluoperazin, the development of extrapyramidal symptoms and dystonia are described; with dextromethorphan - described the case of the development of hallucinations; with digoxin - a case of increasing the concentration of digoxin in the blood plasma.
  3. With simultaneous use with lithium salts may increase or decrease the concentration of lithium in the blood plasma.
  4. With simultaneous use may increase the concentration of imipramine or desipramine in the blood plasma by 2-10 times (may persist for 3 weeks after discontinuation of fluoxetine).
  5. With simultaneous use with drugs that have a depressant effect on the central nervous system, ethanol may significantly enhance the inhibitory effect on the central nervous system, as well as increase the likelihood of seizures.
  6. With simultaneous use with MAO inhibitors, furazolidone, procarbazine, tryptophan, serotonin syndrome may develop (confusion, hypomania, motor anxiety, agitation, convulsions, dysarthria, hypertensive crisis, chills, tremor, nausea, vomiting, diarrhea).
  7. 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 serum, enhancing their therapeutic and side effects.
  8. With simultaneous use, it is possible to suppress the biotransformation of drugs metabolized with the participation of the CYP2D6 isoenzyme.
  9. With simultaneous use with hypoglycemic agents may enhance their action.
  10. When applied simultaneously with propofol, a case has been described in which spontaneous movements were observed; with phenylpropanolamine - described a case in which there was dizziness, weight loss, hyperactivity.
  11. With simultaneous use may enhance the effects of flekainida, meksiletina, propafenone, thioridazine, zuclopentyxol.

Reviews

We offer to read the reviews of people who used fluoxetine:

  1. Eugene. In the past six months, he worked very hard, there was no time and energy left for rest.Then there was such apathy and fatigue that it was impossible to work fruitfully, I just could not do anything. The mood was constantly at zero, nothing pleased. A familiar doctor advised me of Fluoxetine. After a month of reception it became a little easier. Now I am taking these pills for the 3rd month. Gradually, the mood and everything else is getting better. I am pleased.
  2. Eve. Fluoxetine saw, in principle, it suits me. The only time - in the first weeks of taking the medicine, I 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 tablets is quite good, which can not but rejoice.
  3. Tatyana. A terrific remedy for stress. Personally, one capsule is enough for me to calm down as it should. But do not abuse it. I once drank 3 tablets and I just put it to sleep. And I slept long enough, but when I woke up I was in a bad state: my head was aching, zero appetite, no desire to do anything. Therefore, I replaced fluoxetine with regular herbal tea for a while.

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

Reviews of losing weight about Fluoxetine (Lannaher, OZONE, etc.) allow us to conclude that not everyone is able to lose weight on this drug: someone has no appetite at all (up to aversion in food), someone has it the same. However, in most cases, the tool has quite serious side effects: many people who have taken it have noted a decrease in sexual attraction and deterioration of sex life, a feeling of lethargy, severe pain, drowsiness, increased aggression, and the appearance of suicidal thoughts. In addition, for many slimming minuses, the need to give up driving and drinking alcohol, as well as the fact that Fluoxetine is highly addictive, has become necessary.

Summarizing the reviews, we can draw the following conclusions: Fluoxetine is primarily a cure for depression and can be taken only if there are indications and only under the supervision of a physician.

Analogs

Structural analogues of the active substance:

  • Apo Fluoxetine;
  • Deprex;
  • Deprenon;
  • Portal;
  • Prodep;
  • Prozac;
  • Profluzak;
  • Floxet;
  • Fluwal;
  • Fluxonil;
  • Flunisan;
  • Fluoxetine Hexal;
  • Fluoxetine Lannaher;
  • Fluoxetine Nycomed;
  • Fluoxetine OBL;
  • Fluoxetine Canon;
  • Fluoxetine hydrochloride;
  • Framex.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Fluoxetine capsules have a shelf life of 3 years. The drug should be stored in the original intact original packaging, dark, dry, out of reach of children at air temperature not higher than + 25 ° C.

Watch the video: Loosing Weight from Fluoxetine Prozac. Mental Health (April 2020).

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