Fluoxetine (Prozac) - a drug or an antidepressant?

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Attention! The material contains information about substances, the use of which can cause serious harm to your health!

Article prepared by an expert

Egorova Yulia Viktorovna

Psychologist, diagnostician, author of rehabilitation programs for addicts. Member of the Association of Cognitive Behavioral Psychotherapy. More than 7 years of experience working with addicts and their families.

Read in the article:

1. Why is Fluoxetine considered a drug?
2. Why is the drug dangerous?
3. Consequences of non-medical use
4. Signs of overdose
5. Addiction treatment

Human life in today's society is filled with stress. He worries about his job, loans, bills. About the health of family and friends, your own health, about relationships in the family and with people you know. All these factors negatively affect the emotional state.

To support and normalize psychological health, people are prescribed antidepressants. Fluoxetine is the active ingredient in the widely known and frequently used drug Prozac in America. Read our article about whether it is safe to take such medications and why they cause addiction.

Indications

◊ Ministry of Health of Russia

F32 Depressive episode

F41.2 Mixed anxiety and depressive disorder

F42 Obsessive-compulsive disorder

F50.2 Bulimia nervosa

◊ FDA recommendations

• Major depressive disorder (adults and children over 8 years of age)
• OCD (in adults and children from 7 years old)
• Premenstrual dysphoric disorder
• Bulimia
• Panic disorder
• Bipolar depression (in combination with olanzapine)
• Resistant depression (in combination with olanzapine)

◊ Recommendations from UK Medicines and Healthcare Products Regulatory Agency

• Major depressive episode (adults and children over 8 years old only if 4-6 psychotherapeutic sessions have not produced results)
• OCD
• Bulimia (in combination with psychotherapy)

◊ Using Off-label

• Fibromyalgia
• Migraine
• Raynaud's disease
• Hot flashes caused by hormonal chemotherapy [4]
• Selective mutism
• Mild agitation in dementia
• PTSD
• Social anxiety disorder [6]

Consequences of taking fluoxetine

The use of this drug can provoke negative consequences, because the substances in the medicine have a bad effect on all organs and systems of the body. After using the medicine for a long time, a person begins to experience such consequences as:

• Paranoia.
• Severe dizziness.
• Cramps.
• Tremor of the limbs.
• Lack of appetite.
• Problems with stool.
• Muscular atrophy.
• Copious secretion of saliva.
• Urinary incontinence.
• Pimples on the face.
• Impotence and infertility.
• Anemia.
• Myocardial infarction.
• Heart failure.
• Formation of blood clots in blood vessels.
• Heart failure.

The most important consequence of using the drug is the high risk of suicide. There are 7 times more suicide attempts after using this substance than after using any other antidepressant. According to statistics, in America, almost 4 million people committed suicide from this drug over 9 years. This drug has ceased to be sold in Europe, but in our country the medicine is still sold in pharmacies.

You can take the medicine only if your doctor has prescribed it for you. In no case should you exceed the dose of the drug so as not to harm your health.

If it so happens that you or your loved ones are hooked on Prozac, urgently call our clinic hotline. Experienced, qualified doctors can help you cope with addiction.

Mechanism of action and pharmacokinetics

Fluoxetine is a propylamine derivative. Fluoxetine, metabolized to norfluoxetine, selectively blocks the neuronal reuptake of serotonin in the brain, enhancing the actions of serotonin at 5HT1A autoreceptors. Fluoxetine is a weak antagonist of cholinergic, adrenergic and histamine receptors.

• Maximum plasma concentration: 6-8 hours
• Half-life 2-3 days
• Metabolized by CYP2D6. Induces CYP2C9, inhibits CYP2C19, CYP2D6, CYP3A4.
• Active metabolites remain in the blood for two weeks

Comparison of the effectiveness of Prozac and Fluoxetine

The effectiveness of Prozac is quite similar to Fluoxetine - this means that the ability of the drug substance to provide the maximum possible effect is similar.
For example, if the therapeutic effect of Prozac is more pronounced, then using Fluoxetine even in large doses will not achieve this effect.

Also, the speed of therapy - an indicator of the speed of therapeutic action - is approximately the same for Prozac and Fluoxetine. And bioavailability, that is, the amount of a drug reaching its site of action in the body, is similar. The higher the bioavailability, the less it will be lost during absorption and use by the body.

Treatment regimen

◊ Dosage and dose selection

• 20-80 mg/day for depression and anxiety disorders
• 60-80 mg/day for bulimia
• Depression and OCD: start with 20 mg in the morning and wait a few weeks if necessary increase to 80 mg
• Bulimia: start with 60 mg in the morning, but you can start with a smaller dose
• Due to the long half-life, changes in dosage will not be reflected quickly in blood concentrations; Accordingly, it is eliminated from the body longer than other drugs
• Usually taken in the morning, but can be taken at other times of the day
• The more anxious the patient, the lower the starting dose, the slower the dose is increased. In such cases, it is recommended to initially combine with trazadone or benzodiazepines [1].
• If anxiety, insomnia, agitation, or akathisia occur at the beginning of treatment or after interruption of treatment, the possibility of bipolar disorder should be considered and switched to a mood stabilizer or an atypical antipsychotic

◊ How quickly it works

• In some patients it begins to work immediately.
• Begins to act after 2-4 weeks
• If there is no effect after 6-8 weeks, you need to increase the dose or switch to another drug
• To prevent relapse, it can be taken for many years.

◊ Expected result

• Complete remission.
• After the symptoms of depression disappear, you should continue taking it for one year if this was the treatment of the first episode. If this is to treat a recurrent episode, treatment can be extended indefinitely.
• Use in the treatment of anxiety and bulimia can be indefinite [1].

◊ If it doesn't work

• Change the dose, switch to another medicine or add an auxiliary drug;
• Connect psychotherapy;
• Review the diagnosis by identifying comorbid conditions;
• In patients with undiagnosed bipolar affective disorder, the effectiveness of treatment may be low, in which case it is necessary to switch to a mood stabilizer [1].

◊ How to stop taking it

Gradual reduction is not necessary due to the long half-life of fluoxetine [1].

◊ Treatment combinations

• For insomnia: trazadone
• For fatigue, drowsiness, loss of concentration: modafinil [3].
• Combinations with other antidepressants may activate bipolar disorder and suicidal ideation
• The combination of fluoxetine + olanzapine has been very well studied, it gives excellent results in bipolar depression, resistant unipolar depression and psychotic depression.
• For bipolar depression, psychotic depression, treatment-resistant depression, treatment-resistant anxiety disorder: mood stabilizers, atypical antipsychotics
• For anxiety disorder: gabapentin, tiagabine

How to take Fluoxetine

The tablets are taken in the dose prescribed by the doctor, washed down with water. It is not necessary to associate the medicine with periods of eating. It is preferable to take Fluoxetine in the morning, as it has a pronounced stimulating effect.

The treatment regimen depends on the identified disorders. General recommendations:

• 1 tablet once a day: to eliminate symptoms of apathy and depression;
• 1 tablet 2-3 times a day: for the treatment of bulimia.

In some cases, the dosage may be increased to 5-6 or 8 tablets per day. Their intake is divided into 3-4 times.

The course of treatment for acute stress is 3–4 weeks. For prolonged depression, it is necessary to take Fluoxetine for at least 3-4 months, sometimes up to six months. It is necessary to discontinue therapy according to a specific regimen, gradually reducing the dose. Abrupt withdrawal of the drug can cause a relapse of negative conditions.

Special patient groups

◊ Patients with kidney problems

No special instructions

◊ Patients with liver disease

Reduce the dose - either take it less often, or reduce the dose by half [1].

◊ Patients with heart disease

Safe. Useful in recovery after a heart attack [1].

◊ Elderly patients

Lower doses are recommended for older patients

◊ Children and teenagers

• Recommended for the treatment of depression and OCD
• It is necessary to regularly and personally check the patient's condition, especially in the first weeks of treatment.
• Adult doses are suitable for adolescents.
• Inform adults about the risks.
• Growth may be slowed in children taking fluoxetine [1].

◊ Pregnant women

• There have been no adequate studies in pregnant women [1].
• Not recommended for pregnant women, especially in the first trimester
• All risks should be weighed and compared
• Bleeding can be expected during childbirth

◊ Breastfeeding

• The medicine passes into breast milk.
• If the infant shows signs of irritation or sedation, discontinue feeding or fluoxetine
• However, treatment after childbirth may be necessary, so the risks should be weighed.

Fluoxetine

Fluoxetine

(eng.
fluoxetine
) - an antidepressant, a selective serotonin reuptake inhibitor.

Fluoxetine is a chemical compound

Fluoxetine as a chemical is (RS)-N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine. Propylamine derivative. The empirical formula of fluoxetine is C17H18F3NO. Molecular weight 309.3 g/mol.

Fluoxetine is a drug

Fluoxetine is the international nonproprietary name (INN) of the drug. According to the pharmacological index, fluoxetine belongs to the group “Antidepressants”. According to ATC, fluoxetine is included in the group “N06 Psychoanaleptics” and has the code N06AB03. Fluoxetine is also a trade name for a drug.

Indications for use of fluoxetine

Fluoxetine is indicated for use in:

• depression of various origins, especially those accompanied by fears
• obsessive-compulsive disorders
• bulimic neurosis

Experience with the use of fluoxetine in the treatment of functional heartburn

The American Gastroenterological Association's updated functional heartburn guidelines (2020) note that fluoxetine is the only selective serotonin reuptake inhibitor studied in the treatment of functional heartburn. Patients with refractory heartburn that persisted while taking omeprazole and negative endoscopy were randomized into three groups to receive different treatment options: a) double dose of omeprazole; b) omeprazole and fluoxetine 20 mg per day; c) omeprazole and placebo. Those who received fluoxetine showed a significantly greater increase in heartburn-free days (mean 35.7 days) compared to those who received double-dose PPI (mean 7.14 days) and placebo (mean 7.14 days) . This superior therapeutic effect of fluoxetine was observed only in a subgroup of patients with normal pH values ​​(Fass R, Zerbib F, Gyawali CP).

Indications for the use of fluoxetine in the treatment of obesity

The World Gastroenterological Organization includes fluoxetine in the list of drugs used in the treatment of obesity in patients with a body mass index of at least 27 kg/m2 (BMI. Obesity. Practical recommendations) and at least one of the following:

• sleep apnea
• night meals
• bulimia

Currently, fluoxetine is the drug of choice for the treatment of obesity in patients with depression who require both an antidepressant and a weight loss drug. The drug is not used for the treatment of obesity, since during long-term observation (12 months) doses 2-3 higher than usual doses of antidepressants were required to achieve weight loss. The effect was observed only for 6 months, and then a reverse increase in body weight occurred, despite ongoing treatment. A number of side effects were revealed - asthenia, increased sweating, nervous agitation, tremor, sexual dysfunction (Butrova S.A., Plokhaya A.A.).

How to take fluoxetine and dose

Fluoxetine is taken with food, orally, in 1-2 doses per day, preferably in the first half of the day.
The initial daily dose of fluoxetine is 20 mg. If necessary, the dose of fluoxetine is increased weekly by 20 mg per day. The maximum daily dose of fluoxetine is 80 mg, for the elderly - 60 mg. Duration of therapy is 3-4 weeks, for obsessive-compulsive conditions - 5 weeks or more, for bulimia nervosa - 1 week. The maintenance daily dose of fluoxetine is 20 mg. Fluoxetine is not recommended to be taken concomitantly with monoamine oxdase inhibitors (MAOIs), such as furazolidone, rasagiline (Azilect), selegiline (Yumex, etc.), isocarboxazid, phenelzine, procarbazine, tranylcypramine and others, or if MAO inhibitors were taken within the previous two weeks. With the simultaneous use of fluoxetine and MAO inhibitors, severe, sometimes fatal, reactions are possible, including hyperthermia, rigidity, myoclonus, autonomic disturbances, extreme agitation progressing to delirium and coma. Due to the prolonged elimination of fluoxetine, a gap of at least 5 weeks or more is necessary between stopping fluoxetine and starting an MAOI.

Side effects of fluoxetine

Side effects of fluoxetine therapy:

• very often: diarrhea, nausea, headache, insomnia,
• often: dry mouth, dyspepsia, vomiting, anorexia, atrial flutter, hot flashes, impaired attention, dizziness, lethargy, drowsiness, tremor, nightmares, nervousness, tension, decreased libido, euphoria, sleep disturbance, itching, skin rash , urticaria, blurred vision, frequent urination, ejaculation disorders, erectile dysfunction, gynecological bleeding.
• rarely: dysphagia, taste perversion, pain in the esophagus, hypotension, vasculitis, vasolidation, idiosyncratic hepatitis, muscle twitching, psychomotor agitation, hyperactivity, ataxia, incoordination, bruxism, dyskinesia, convulsions, depersonalization, hyperthymia, problems with orgasm, thinking disorders, manic disorders, tendency to bruise, cold sweat, priapism.

Use of fluoxetine during pregnancy, breastfeeding and children

Fluoxetine is not recommended for pregnant women, nursing mothers and children under 18 years of age.
Fluoxetine passes into breast milk, so breastfeeding should be discontinued during fluoxetine therapy. Fluoxetine is FDA Category C for fetal risk use in pregnant women (animal studies have shown adverse effects on the fetus and there have been no adequate studies in pregnant women, but the potential benefits associated with use of this drug in pregnant women may justify it use despite the risk).

Trade names of drugs with the active substance fluoxetine

The following drugs with the only active ingredient fluoxetine are (were) registered in Russia: Apo-Fluoxetine, Deprex, Deprenon, Portal, Prodep, Prozac, Profluza, Floxet, Fluval, Fluxonil, Flunisan, Fluoxetine, Fluoxetine HEXAL, Fluoxetine Lannacher, Fluoxetine Nycomed, Fluoxetine-OBL, Fluoxetine-Canon, Fluoxetine hydrochloride, Framex.
In Ukraine, in particular, Fluxen is registered (see instructions for use below). Brands of fluoxetine in the USA: PROzac, PROzac Weekly, Rapiflux, Sarafem, Selfemra, PROzac Pulvules.

Instructions for use of fluoxetine

Some instructions from manufacturers for the medical use of drugs containing the only active ingredient fluoxetine (pdf):

• instructions for Ukraine (in Russian): “Instructions for the medical use of the drug Fluxen”, OJSC “Kievmedpreparat”
• US instructions (in English):
• “Prozac (fluoxetine hydrochloride) Pulvules for oral use. Prozac (fluoxetine hydrochloride) delayed-release capsules for oral use. Full Prescribing Information,” Eli Lilly and Company, January 2013.
• "Fluoxetine tablets, 60 mg. Medication Guide,” Edgemont Pharmaceuticals, LLC. June 2014.

Fluoxetine has contraindications, side effects and application features; consultation with a specialist is necessary. Back to section

Side effects and other risks

◊ Mechanism of side effects

Side effects are caused by an increase in serotonin. Most side effects occur immediately after starting treatment and go away over time, while the therapeutic effects increase over time. At the beginning of the course, agitation, activation and anxiety may appear

◊ Side effects

• Gastroenterological (reduced appetite, nausea, diarrhea, constipation)
• Insomnia, sedation, agitation, tremor
• Sweating
• Dangerous side effects: seizures, mania, suicidal ideation
• Weight gain: very rare
• Sedation: very rare
• Sexual dysfunction: yes

◊What to do about side effects

1. Wait
2. If fluoxetine activates, take in the morning to avoid insomnia
3. Reduce dose to 10 mg, when side effects go away, increase to 20 mg
4. Side effects may appear briefly as the dose is increased
5. Benzodazepines are recommended for anxious patients, especially at the beginning of treatment [1].

◊ Long-term use

Safely

◊Addiction

No.

◊ Overdose

• Very rare cases of fatal overdoses.
• In combination with alcohol – respiratory depression, ataxia, sedation

Signs of fluoxetine addiction

Frequent use of the drug or exceeding the dose causes a number of symptoms:

• Mental disorder. The person becomes excited, nervous, aggressive or very joyful.
• Excessive physical activity begins. It is similar to the effect of using psychostimulants.
• Problems with thinking.
• Cramps. Similar to a seizure in epilepsy.
• Rapid heartbeat and high blood pressure.
• Nausea and vomiting.

When mixed with other drugs, a person can become disabled or die even after the first use.

In case of an overdose of the drug, a person will experience the following sensations:

• Euphoria.
• Apathy.
• Hallucinations.
• Emotional swings.

If a person constantly uses an excessive amount of the drug, his central nervous system is destroyed and it will subsequently be impossible to cure it.

How does Fluoxetine work?

Fluoxetine (Prozac) blocks the flow of serotonin back into neuronal synapses (where nerve cells connect to each other). As a result, the content of this mediator (a substance involved in the transmission of nerve impulses) in the connecting elements increases significantly, so over a long period of time it manages to influence the postsynaptic areas, causing characteristic changes. This shows up:

• Stimulating effect on the nervous system
• Improved mood
• Activation of mental processes
• Suppressing anxiety and worry
• Decreased appetite, ultimately leading to weight loss.

In addition to inhibiting serotonin uptake in nervous tissue, Fluoxetine has a similar effect on platelets, reducing their aggregation (gluing) ability. This positive effect helps prevent thrombosis in patients at risk. But this property is not used as the main therapeutic effect; it is a “pleasant” addition to antipsychotic effects.

An important advantage of this antidepressant is the lack of sedation. Therefore, Fluoxetine (Prozac) can be used by persons engaged in precise work that requires care:

• Drivers
• Jewelers
• Aviation industry, etc.

Is there a problem with drug addiction in the family? Contact a private anonymous clinic

Manufacturers of Fluoxetine

Among foreign manufacturers, only 3 supply Fluoxetine to Russia:

1. Patheon France is a company that produces the original drug under the trade name Prozac. The original product was developed in Switzerland, but is currently produced in France. The advantage of Prozac is the greater number of clinical trials. This indicates its proven safety and effectiveness. For this reason, Patheon France is considered the best manufacturer of Fluoxetine. The negative point is the high cost of the medicine: about 500 rubles. for 14 capsules of 20 mg.
2. G.L. Pharma is an Austrian company that produces the antidepressant Fluoxetine Lannacher, which belongs to the average price category - 130 rubles. for 20 capsules of 20 mg.
3. Apotex is one of the largest pharmaceutical companies in Canada. It produces the drug Apo-Fluoxetine, which is delivered to Russia and packaged here. Probably for this reason, Apo-Fluoxetine is the cheapest European analogue of the original antidepressant.

Among domestic manufacturers, the companies Ozon, Biokom, ProMed, and Kanonpharma are involved in the production of Fluoxetine. All of them have a GMP quality certificate. This means that their products meet European manufacturing standards. However, in reality there cannot be 100% compliance, since quality control of raw materials in the Russian Federation is less strict.

Most domestic fluoxetines are characterized by an affordable price. The cheapest antidepressants are produced by ProMed and Ozone - 20 capsules of 20 mg each cost 40-50 rubles. The most expensive Russian version of the drug is Fluoxetine-Canon: the price of a similar release form is about 120 rubles.

Comparing the safety of Prozac and Fluoxetine

The safety of a drug includes many factors.

At the same time, in Prozac it is quite similar to Fluoxetine. It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others. When assessing the metabolism of Prozac, as well as Fluoxetine, we look at which organ is the metabolizing organ and how critical the effect on it is.

The risk-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use. At the same time, Prozac does not have any risks when used, just like Fluoxetine.

Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs. In other matters, as well as the reversibility of the consequences of using Prozac and Fluoxetine.

Efficacy of the drug

Considering the existing risks of treatment with Fluoxetine, a number of studies have been conducted to evaluate the therapeutic effectiveness of this drug and the validity of its prescription. They showed that it has a good ability to relieve anxiety and depression. Therefore, Fluoxetine is widely used in the complex treatment of many psychoneurological disorders. However, there is also conflicting data indicating the high danger of the drug and low effectiveness, comparable to a placebo (dummy). Therefore, the drug should be taken seriously and not taken without a doctor’s recommendation.

Scandal around Fluoxetine (Prozac)

Recently, the press discussed the possibility of prescribing fluoxetine in psychiatry. In Europe, a scandal erupted in connection with this, which resulted in a ban on treatment with this drug and withdrawal from the pharmacy chain. In the Russian Federation, similar actions were not followed - it remained in the Register of Medicines Approved for Medical Use.

To avoid the negative consequences of treatment with Fluoxetine, it is necessary to use it only on the recommendation of a doctor.

Therefore, in modern conditions, this antidepressant can only be purchased in the pharmacy chain with a prescription. But there is also the other side of the coin - online pharmacies prohibited by law. In them, the drug is sold illegally - over the counter. It should be remembered that if you purchase the drug without consulting a doctor, the risk of developing fluoxetine addiction is very high. It manifests itself with serious symptoms that a person cannot cope with on his own. An overdose can result in cardiac arrest and death.

Indications for use

Indications for taking Fluoxetine (Prozac) should only be determined by a doctor. Self-treatment with these antidepressants is prohibited, because they have a number of contraindications and side effects. The need to use Fluoxetine and its substitutes exists when a person suffers from certain mental disorders, namely:

• Depression (regardless of its cause)
• Neurosis, manifested by a strong increase in appetite, leading to obesity
• Obsessive states with constant checking of what has been done.

Comparing the ease of use of Prozac and Fluoxetine

This includes dose selection taking into account various conditions and frequency of doses. At the same time, it is important not to forget about the release form of the drug; it is also important to take it into account when making an assessment.

The ease of use of Prozac is approximately the same as Fluoxetine. However, they are not convenient enough to use.

The drug ratings were compiled by experienced pharmacists who studied international research. The report is generated automatically.

Last update date: 2020-12-04 13:48:41