29.11.2020

Fluoxetine is an antidepressant of the second generation

Fluoxetine belongs to the antidepressants, overwhelming the reuptake of serotonin (serotonergic antidepressants, inhibitors of serotonin reuptake). The drug is effective in the treatment of depression and anxiety – improves mood, reduces feeling of stress, anxiety, fear.

The main advantage of Fluoxetine over the traditional tricyclic antidepressants (so-called classical antidepressants) is to reduce side effects due to selective mechanism of action. When using Fluoxetine is better tolerated and, according to many studies, it has greater efficiency compared with classical antidepressants, although the results of the comparison is not entirely unambiguous.

The advantages and disadvantages of serotonergic antidepressants

The benefits of antidepressants selectively inhibit the reuptake of serotonin:

  • effective therapy and anxiety, and depressive symptoms;
  • security;
  • minimal cardiovascular risk;
  • the lack of habituation;
  • the possibility of long-term therapy;
  • preventive therapy – prevention of disorders;
  • voluntary adherence to the patient’s prescribed treatment regimen while taking the drug;
  • the effect lasts as long as treatment continues;
  • long-term treatment allows to avoid relapse.

Anxiety disorders are often accompanied by dependence on alcohol and psychoactive substances. In such cases, it is not recommended to prescribe benzodiazepines, and antidepressants selectively inhibit the reuptake of serotonin, become the main line drug in the treatment of depression, as it does not cause drug dependence.

Disadvantages of serotonergic antidepressants:

  • sexual side effects;
  • sometimes there is a need to gradually increase your dose up to a maximum amount to achieve a therapeutic effect;
  • difficulties may arise in determining the early reactions to therapy;
  • slow, gradual improvement over weeks or months;
  • a frequent occurrence during the first two to three weeks of taking the phenomena hyperstimulation – irritability, insomnia, nervousness, increased anxiety and panic symptoms.

The disadvantage of non-medical nature are less economic accessibility of medicines in this group (price) because they are taken for a long time, and the lack of injectable forms of most medications.

Pharmacological action

Selectively inhibits reverse neuronal uptake of serotonin (5-hydroxytryptamine) neurotransmission in the neurons of the Central nervous system. The suppression of serotonin reuptake increases the concentration of this neurotransmitter in the synaptic cleft, strengthens and prolongs its effects on the postsynaptic receptor sites.

Fluoxetine has a low affinity for α1, α2 and β-adrenergic, serotonin, dopaminergic, muskarinovymi, H1-histamine and the GABAergic receptors.
Improves mood, reduces fear, anxiety, stress, eliminates dysphoria, reduces appetite. Causes reduction obessive-compulsive disorders.

Not cardiotoksicnae. Not shown a sedative, hypnotic action, orthostatic hypotension.
The effect of treatment occurs within 7 to 14 days after ingestion.

Dosage forms

Fluoxetine is available in capsules.

Composition

The contents in a single capsule of fluoxetine hydrochloride – 22.36 mg, which corresponds to 20 mg fluoxetine It is the active ingredient of the medicine.
Additional ingredients: corn starch pregelatinization, Dimethicone.
The composition of the body of the capsule: gelatin, titanium dioxide, dye iron oxide yellow .
The lid of the capsule contains gelatin, colorant, patented blue V, titanium dioxide, dye iron oxide yellow.

Testimony

Obsessive-compulsive disorder.
Depression different Genesis.
Premenstrual dysphoria.
Bulemeezi neurosis.

Contraindications

Hypersensitivity to any component of the medication.
Severe disorders of renal function (KK less 10 ml/min) and liver.
Concomitant use of monoamine oxidase inhibitors and for 14 days after their withdrawal, thioridazine, pimozide.
Atony of the bladder.
Children up to age 18 years.
Pregnancy.
Lactation.
Caution: suicidal, epilepsy, diabetes mellitus, excessive weight loss, Parkinson’s disease.

Function during pregnancy and lactation

Is contraindicated during breastfeeding and pregnancy.

Method of application and dosing

Regardless of the meal, inside.
Depression
The initial dose of 20 mg once daily in the morning. The dose can be increased to 40 – 60 mg/day. Then it should be divided into two or three doses. Per day maximum dose of 80 mg of the drugs.
Obsessive-compulsive disorder
Fluoxetine 20 – 60 mg per day.
Bulemeezi neurosis
The dosage of 60 mg per day divided into two or three doses.
Premenstrual dysphoric disorder
Fluoxetine 20 mg per day.
In the elderly, liver disease, therapy is started with a 1/2 dose.
For patients with impaired renal function reduce the dose and increase the interval between administration of the drug.
The course of treatment is 3 to 4 weeks.

Side effects

Dizziness, headache, fatigue, asthenia, sleep disturbances, motor agitation, tremor, agitation, increased suicidal tendencies, anxiety, mania or hypomania.

Loss of appetite, dry mouth or hypersalivation, nausea, vomiting, taste disturbance, diarrhea.
Allergic reactions such as skin rashes, itching, urticaria, myalgia, arthralgia, fever.

Urinary incontinence, urinary retention, dysmenorrhea, vaginitis, decreased sexual desire, impaired sexual function in men (delay ejaculation).
Sweating, tachycardia, impaired visual acuity, weight loss, systemic disorders of lung, kidney or liver, vasculitis.

Overdose

Symptoms: nausea, vomiting, restlessness, agitated, convulsive disorder, a disorder of the cardiovascular system.
Treatment: specific antidote is not found. Symptomatic therapy, gastric lavage, the appointment activated carbon, in convulsions – the appointment of tranquilizers, maintaining heart activity, respiration.

Warnings, monitoring of therapy
Suicidal risk

Depression there is a likelihood of suicide attempts that can persist until the onset of stable remission. As in the case of other drugs similar pharmacological action (antidepressants), was described individual cases of suicidal behavior during treatment with Fluoxetine or after its completion.

Analysis of the combined studies assignment drugs in psychiatric disorders showed an increased risk of suicidal thoughts and/or suicidal behavior in young patients (under 25 years).

Drug therapy of high-risk patients should be under careful medical supervision.

Cardiovascular effects

Be wary appoint patients with the congenital syndrome of QT prolongation, acquired syndrome of QT prolongation(e.g., in concurrent use of Fluoxetine with drugs, extension QT interval), when there is a history of instructions to increase the duration of the interval QTу relatives of the patient with other clinical conditions predisposing to the development of arrhythmias (for example, hypokalemia or hypomagnesemia) or increased exposure of Fluoxetine (for example, reduced liver function).

Skin rash

Report the appearance of skin rash, anaphylactic reactions and systemic violations occurring in the progression, sometimes with involvement in the pathological process of the liver, kidneys, skin, lungs in patients taking Fluoxetine.

Electroconvulsive therapy (ECT)

There is evidence of increase in the duration of seizures in patients treated with Fluoxetine receiving ECT.

Epileptic seizures

Assign patients who have previously noted epileptic seizures, proceed with caution.

Mania

If the patient is in a manic state, drug not to take.

Akathisia/psychomotor restlessness

The use of drugs leads to the development of akathisia, which manifests itself subjectively unpleasant sensations or restlessness, a need for constant movement, often without the ability to sit or stand still. Most often such phenomena are observed during the first few weeks of treatment. Patients who have these symptoms, increasing the dose of Fluoxetine is undesirable.

Tamoxifen

The drug reduces the concentration of endoxifen, one of the most important active metabolites of tamoxifen. When treatment with tamoxifen Fluoxetine not be prescribed.

The loss of body weight

The patients had loss of body weight, however, usually it is proportional to the initial average body weight.

Hyponatremia

There have been cases of hyponatremia in elderly patients and in patients taking diuretics because of the reduction of circulating blood volume.

Glycemic control

During the treatment of Fluoxetine may need to adjust doses of insulin and/or hypoglycemic drugs.

Hepatic/renal failure

Patients with apparent violations of the liver, or prescribe a lower dose, or every other day. The appointment of Fluoxetine at a dose of 20 mg/day for two months to patients with impaired renal function (creatinine clearance < 10 ml/min), undergoing hemodialysis, have not revealed differences in the concentration of fluoxetine and norfluoksetina in plasma between patients and healthy people.

Mydriasis

Be wary appoint patients with high intraocular pressure or risk of acute angle-closure glaucoma.

St. John’s wort

Perhaps the development of a pharmacodynamic interaction between Fluoxetine and products containing St. John’s wort.

Withdrawal symptoms

Often when cessation of drug therapy, especially with the sharp reversal, observed syndrome. In 60% of patients experienced adverse events when canceling a treatment. The most commonly reported dizziness, sensory disturbances (including paraesthesia), sleep disturbances (deep sleep, insomnia), fatigue, anxiety, agitation, nausea and/or vomiting, tremor and headache.

In most cases, these phenomena cease on their own within 14 days, but sometimes they were prolonged for 2 – 3 months or more. Therefore, the abolition of treatment with Fluoxetine is carried out gradually over one to two weeks depending on the condition of the patient.

In rare cases were reported in Association with Fluoxetine the development of serotonin syndrome or neuroleptic malignant syndrome (hyperthermia, extrapyramidal neurological disorders and catatonic symptoms, muscle tension), especially when combined with other serotonergic drugs.

As these syndromes can lead to life threatening condition, treatment with fluoxetine is discontinued in the case of a combination of symptoms – hyperthermia, rigidity, myoclonus, disorders of the autonomic nervous system with the development of fluctuations in vital functions, altered mental status, including confusion, irritability, extreme agitation with the possible development of delirium and coma, and assign appropriate therapy.

Increased bleeding

Fluoxetine may increase the tendency to bleeding, including the gastrointestinal tract. In this regard, we recommend caution when prescribing the drug to patients, while receiving anticoagulants and/or medicinal products that can change the properties of the platelets (for example, nonsteroidal anti-inflammatory drugs, acetylsalicylic acid), or patients who already have increased bleeding.

Interaction with other drugs

Do not use the medicine simultaneously with MAO inhibitors as possible development of serotonin syndrome (hyperthermia, chills, sweating, myoclonus, hyperreflexia, tremor, diarrhea, incoordination, autonomic lability, agitation, delirium and coma).

Tryptophan enhances the serotonergic properties of the drug (increased agitation, motor restlessness, disorders of the gastro-intestinal tract).
When using with products containing St. John’s wort (Hypericum perforatum) may occur, increasing the serotonergic effect, increasing unwanted effects.

Increases plasma concentration of tricyclic antidepressants, phenytoin, maprotiline, trazodone twice. 50% to reduce the dose of these drugs at simultaneous application with Fluoxetine. Enhances the effects of alprazolama, diazepam, ethanol, hypoglycemic drugs.

Concomitant use of Fluoxetine with alcohol or centrally acting drugs, causing inhibition of the function of the Central nervous system, increases the effect and increases the risk of side effects.

Medicinal products containing lithium should be used with caution due to the possible increase of lithium concentration and risk of development of toxic effects.
Against the background of electroconvulsive therapy may develop prolonged seizures.

With simultaneous use with drugs having a high degree of protein binding, especially with anticoagulants and digitoxin, may increase the plasma concentration of free (unbound) drugs and an increased risk of developing adverse effects.

Fluoxetine dispensed by prescription. During treatment should refrain from drinking alcoholic beverages and activities potentially hazardous activities, require increased attention and rapid mental and motor reactions.

Fluoxetine is a Russian pharmaceutical companies FP Obolenskoe, ALSI Pharma,medicine Manufacturing, Ozone,Medisorb, Biokom, kanonfarma prodakshn, as well as foreign companies Apotex Inc. (Canada), new farm, Inc. (Canada), Hexane AG (Germany), Lannacher (Austria).

Analogues of the drug

Commercial names of drugs, containing as active substance fluoxetine: Fluoxetine, Prodep (India), Prozac (US), Prilosec (Russia).
To the group of selective inhibitors of capture of serotonin include:

  • citalopram (trade name Cipramil);
  • ESCITALOPRAM (ESCITALOPRAM);
  • fluvoxamine (Awoken, Fevarin);
  • paroxetine (paxil);
  • sertraline (zoloft, Stimuloton);
  • venlafaxine.

The mechanism of action of these drugs is the same and is associated with effects on the serotonin Transporter, and clinically significant differences between them relate primarily to the elimination half-life (the time during which the concentration of the drug in the body decreases by 50 %, T½) and features lekarstvennyh interactions.

The half-life of fluoxetine is about 330 h, while the other drugs in this group it is 15 – 30 h. This figure is extremely important if the patient is transferred from the reception of a selective inhibitor of the capture of serotonin in the drug of the other group, and also for assessing the prognosis in the case of serious adverse reactions requiring immediate cancellation of the serotonergic antidepressant.

Another difference among the analogues of Fluoxetine is the different degree of selectivity of the suppression of serotonin reuptake. Most selective in this respect, ESCITALOPRAM, next – citalopram, sertraline, fluvoxamine, paroxetine and fluoxetine.

Sertraline and venlafaxine are the only modern antidepressants with the evidence base in relation to the lengthening of remission in depressive disorders.

Inhibitors of serotonin reuptake in treatment of premature ejaculation

The literature shows the possibility of application of various psychotropic drugs for the treatment of men are premature ejaculation. Medicines that can increase the duration of sexual intercourse used including antidepressants belonging to the group of inhibitors of reverse capture of serotonin. This is because in the pathogenesis of premature ejaculation is confirmed by the role of the Central serotoninergicheskih mechanisms of regulation. For the treatment of premature ejaculation are used sertraline, paroxetine, clomipramine (trade name Anafranil, Clofranil), fluoxetine, citalopram, fluvoxamine, ESCITALOPRAM, buspirone, dapoxetine.

These antidepressants are taken daily on a regular basis. The exception is dapoxetine, which applies “on demand” a few hours before intercourse. The research noted that paroxetine exerts the strongest effect on ejaculation. The purpose clomipramine, paroxetine, sertraline, fluoxetine 4 to 6 hours before intercourse, effective and well tolerated, but is less ejaculation delay than daily treatment.

The use of serotonergic antidepressants are advised for young people with existing from the beginning of sexual life premature ejaculation and acquired the disease when the causative factors are eliminated, but the problem still exists.

Some authors argue that the effectiveness of these drugs to increase the duration of sexual intercourse, combined with their low side effect profile, makes them first line therapy tools premature ejaculation as when taken daily, and in the use of “on demand”. However, the importance of the drugs in this group, apparently, should not be exaggerated, since the termination of their use in men with lifelong premature ejaculation leads to restoration of the pre-treatment ejaculatory threshold for 5 – 7 days.

Attention! Description of the preparation is simplified and augmented version of the official instructions for use. Information about the drug provided solely for informational purposes and should not be used as a guide to self-healing.

International nonproprietary name The trade name of the drug Price Release form Manufacturer
fluoxetine Fluoxetine 34 RUB. Capsules 10 mg, 20 pieces Russia
Fluoxetine 37 RUB Capsules of 20 mg, 20 pieces Russia
Fluoxetine 118 RUB Capsules of 20 mg, 20 pieces Austria
Prozac 336 RUB Capsules 20 mg, 14 pieces USA

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