Fluoxetine (Prozac) – medicine or poison?


Content:

  1. About the drug
  2. Pharmacological properties
  3. Impact on the body
  4. Side effects
  5. Prozac withdrawal syndrome
  6. How to ease Prozac withdrawal symptoms
  7. conclusions

Prozac is an antidepressant prescribed by doctors to treat bulimia, OCD, depression, neuroses and other nervous disorders. Available in capsule form, easy to use and affordable. If you stop taking it abruptly, Prozac withdrawal syndrome may occur, so it is very important to follow your doctor's instructions and take the medicine under his supervision.

Consequences of Fluoxetine - existing risks of taking

Taking the drug may cause side effects. They are polysystemic, i.e. can affect any system of the body. Clinically expressed by the following conditions:

  • Manic stalking
  • Suicidal tendencies
  • Dizziness
  • Shiver
  • Convulsions
  • Poor appetite
  • Diarrhea
  • Increased salivation
  • Heart rhythm disturbance
  • Urinary retention or incontinence
  • Sexual dysfunction
  • Allergic rashes.

Therefore, any discomfort and deviations in habitual behavior during treatment with Fluoxetine require consultation with a doctor. Such patients may need to adjust the dose of the antidepressant or replace it with another drug.

Allergic rashes are a common side effect of the drug fluoxetine.

About the drug


Prozac has a cumulative effect.
A positive result from taking it occurs approximately 1-2 weeks after the start of the course. Its effect is manifested in reducing anxiety, eliminating panic attacks and fear. If you adhere to the prescribed dosage regimen, in most cases Prozac withdrawal syndrome may not occur at all. Exit from the course of treatment should be gradual, just like the start of treatment. Over the course of several weeks, the dosage and frequency of administration are reduced. If you stop taking the medicine on one day, the effect will also last about a week, but withdrawal symptoms will occur. Interesting fact:
Prozac is often prescribed after treatment with other antidepressants. This drug is lighter, so such a transition allows you to gently reduce the load on the body and prevent withdrawal symptoms from other drugs.

Pharmacological properties

The main component of Prozac is fluoxetine. It ensures the reuptake of serotonin, trapping its molecules between nerve cells. An increase in the amount of this neurotransmitter in the central nervous system eliminates anxiety, improves emotional state, and increases appetite. In the case of treating Irritable Bowel Syndrome, SSRIs help improve gastrointestinal motility, eliminating constipation and diarrhea.

The advantage of Prozac is that it does not cause drowsiness and does not affect activity throughout the day, which allows patients to live a full life: work, perform daily duties.

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.

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Impact on the body

Absorption of the drug occurs through the gastrointestinal tract. 6-8 hours after administration, its maximum concentration in the blood is reached. In the liver it breaks down into metabolites. A few days after the start of use, withdrawal slows down, allowing it to accumulate in the body to a constant concentration within the prescribed dosage.

After treatment, fluoxetine remains in the brain for five weeks. In the first week, its concentration decreases by half. It should be noted that the drug can be detected in the blood 2 months after completion of the course.

Prozac withdrawal syndrome

Due to the long period of decay of the main substance, withdrawal syndrome does not have strong negative manifestations. It can appear if you abruptly stop taking it in the first days. This is due to the rapid elimination of fluoxetine, which has not yet had time to accumulate.

On average, the treatment course is about 6 weeks. And only 5% of patients experience Prozac withdrawal syndrome. This is expressed in the appearance or intensification of side effects if they were present during treatment. The most common symptoms are dizziness and drowsiness. This condition can last up to two weeks. These manifestations do not cause any particular discomfort and therefore do not require medical intervention.

In rare cases, Prozac withdrawal symptoms can last several months. Diagnosed symptoms include one or more of the following:


  • headaches;
  • dizziness;
  • drowsiness;
  • problems with coordination and orientation in space;
  • increased anxiety;
  • negative manifestations from the gastrointestinal tract (abdominal pain, diarrhea, nausea);
  • irritability, aggression;
  • decreased vision;
  • tremor in the limbs;
  • fast fatiguability.

Prozac®

Suicidal risk

Depression is associated with an increased risk of suicidal ideation, self-harm (self-harm), and suicidal events. This risk persists until stable remission occurs. Since improvement may not occur during the first few weeks of treatment, careful monitoring by the attending physician is necessary until the patient's condition improves. Clinical practice shows that the risk of suicide may increase in the early stages of recovery.

Other psychiatric diseases for which Prozach® is prescribed may also be associated with an increased risk of suicidal events. In addition, these diseases can accompany major depressive disorder. Therefore, the same caution should be exercised when treating patients with other psychiatric illnesses as when treating patients with major depressive disorder.

Patients with a history of suicidal behavior who clearly exhibit suicidal ideation before treatment are at increased risk for suicidal ideation or behavior. These patients should be closely monitored during therapy.

A meta-analysis of placebo-controlled clinical trials of antidepressants used to treat psychiatric conditions in adult patients found that among patients younger than 25 years, antidepressant use is associated with an increased risk of suicidal behavior compared with patients receiving placebo.

Patients, particularly those at high risk of developing suicidal behavior, should be closely monitored, especially during the early stages of treatment and during subsequent dose changes. Patients (and their caregivers) should be warned to monitor for any clinical deterioration, monitor for the occurrence of suicidal behavior or thoughts, and unusual changes in behavior, and should contact their healthcare provider immediately if these symptoms occur.

Cardiovascular effects

QT prolongation may occur with fluoxetine, and ventricular arrhythmias or torsade de pointes (TdP) have been reported during post-marketing studies of fluoxetine. Fluoxetine should be used with caution in patients with congenital long QT syndrome, acquired long QT syndrome (for example, while taking fluoxetine with drugs that prolong the QT interval), if there is a history of indications of an increase in the duration of the QT interval in the patient's relatives, with other clinical conditions predisposing to the development of arrhythmia (for example, with hypokalemia, hypomagnesemia, bradycardia, acute myocardial infarction, decompensated heart failure) and with increased exposure to fluoxetine (for example, with reduced liver function). Patients with stable heart disease should undergo an ECG examination before starting fluoxetine therapy. If signs of arrhythmia develop during therapy, fluoxetine should be discontinued and an ECG study performed.

Skin rash

In patients taking fluoxetine, skin rash, anaphylactic reactions and progressive systemic disorders, sometimes serious involving the skin, kidneys, liver and lungs, have been reported. If a skin rash or other possible allergic reactions occur, the etiology of which cannot be determined, fluoxetine should be discontinued.

Epileptic seizures

As with other antidepressants, fluoxetine should be used with caution in patients with a history of seizures. Fluoxetine therapy should be discontinued if epileptic seizures develop in any patient. Also, fluoxetine therapy should not be prescribed to patients with unstable epilepsy; patients with controlled epilepsy require careful monitoring.

Electroconvulsive therapy

In patients receiving electroconvulsive therapy, prolonged seizures have been reported in rare cases while receiving fluoxetine. Caution is recommended when administering fluoxetine to these patients.

Mania

Antidepressants should be used with caution in patients with a history of mania/hypomania. Fluoxetine, like any antidepressant, must be discontinued if the patient is in a manic state.

Akathisia/ psychomotor restlessness

The use of fluoxetine leads to the development of akathisia, which is manifested by subjectively unpleasant sensations or restlessness, the 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. In patients with these symptoms, increasing the dose of fluoxetine may have negative consequences.

Withdrawal symptoms

Withdrawal symptoms were common when fluoxetine therapy was stopped, especially when discontinued abruptly. In clinical studies, approximately 60% of patients developed various adverse events when therapy was discontinued, both in the fluoxetine group and in the placebo group. In the fluoxetine group, 17% of these events were severe, and in the placebo group - 12%.

The risk of developing withdrawal symptoms depends on several factors, including duration of therapy, dose, and rate of dose reduction. The most commonly reported symptoms were dizziness, sensory disturbances (including paresthesia), sleep disturbances (including insomnia and vivid dreams), asthenia, anxiety or agitation, nausea and/or vomiting, tremor and headache. Typically these episodes were mild to moderate in severity, but in some patients they could be more severe. In most cases, these phenomena resolve on their own within two weeks, but sometimes they can last longer (2-3 months or more). Therefore, withdrawal of fluoxetine therapy should be done gradually over one or two weeks, depending on the patient's needs.

Tamoxifen

Fluoxetine, as a potent inhibitor of the CYP2D6 isoenzyme, can lead to a decrease in the concentration of endoxifen, one of the most important active metabolites of tamoxifen. Therefore, fluoxetine should be avoided during tamoxifen therapy.

Weight loss

When using fluoxetine, patients may experience a decrease in body weight, however, this is usually proportional to the initial average body weight.

Hyponatremia

There have been cases of hyponatremia (in some cases, serum sodium levels were less than 110 mmol/l). Mostly, such cases were observed in elderly patients, in patients receiving diuretics and in patients with a decrease in circulating blood volume.

Diabetes

In patients with diabetes mellitus, hypoglycemia was observed during treatment with fluoxetine, and hyperglycemia developed after discontinuation of the drug. At the beginning or after the end of treatment with fluoxetine, dose adjustment of insulin and/or oral hypoglycemic drugs may be required.

Liver/renal failure

Fluoxetine undergoes extensive metabolism in the liver and is excreted by the kidneys. For patients with severe liver dysfunction, it is recommended to prescribe lower doses of fluoxetine, or prescribe the drug every other day.

When taking fluoxetine at a dose of 20 mg/day for two months in patients with severe renal failure (creatinine clearance < 10 ml/min) requiring hemodialysis, there were no differences in the concentrations of fluoxetine and norfluoxetine in the blood plasma when compared with patients from control group with normal renal function.

Midriaz

Mydriasis has been reported in association with fluoxetine. Caution should be exercised when prescribing fluoxetine to patients with elevated intraocular pressure or patients at risk of developing acute angle-closure glaucoma.

Hemorrhages

Ecchymosis, purpura and other similar disorders associated with increased bleeding have been reported with the use of SSRIs. Ecchymosis has been rarely reported. Other hemorrhagic phenomena (gynecological bleeding, gastrointestinal bleeding, etc.) were observed rarely. Caution should be exercised when treating fluoxetine, in particular in patients with concomitant therapy with oral anticoagulants and other drugs that affect platelet function (for example, with atypical antipsychotics such as clozapine, with phenothiazines, with most tricyclic antidepressants, acetylsalicylic acid, non-steroidal anti-inflammatory drugs) , as well as with concomitant therapy with drugs that may increase the tendency to bleeding, and in patients with a history of bleeding.

Phenomena similar in symptoms to serotonin syndrome or neuroleptic malignant syndrome

In rare cases, the development of serotonin syndrome or neuroleptic malignant syndrome associated with fluoxetine has been reported, especially when used together with other serotonergic drugs (including those containing L-tryptophan) and/or antipsychotics. Because these syndromes can lead to life-threatening conditions, fluoxetine therapy should be discontinued if a combination of symptoms such as pyrexia, rigidity, myoclonus, autonomic nervous system disorders, mental status changes including confusion, irritability, extreme agitation with possible development of delirium and coma occur. , and prescribe the necessary symptomatic therapy.

All patients taking antidepressants for any indication should be closely monitored for signs of clinical worsening, suicidal ideation, and unusual behavioral changes, especially during the first months of therapy or during dose changes (increases or decreases).

How to ease Prozac withdrawal symptoms

To improve the condition when negative reactions of the body manifest themselves, you should adhere to the following rules:


  1. Follow the doctor's instructions when leaving the course of treatment: reduce the dosage and frequency of administration gradually.
  2. Avoid stressful situations and excessive mental stress. During this period, patients are advised to rest and rest. Ideally, you should combine a vacation or vacation with stopping the medication, since studying or fulfilling work responsibilities will be difficult.
  3. Reduce physical activity to a minimum. Avoid sports and any activity. To stay in shape, you can do simple exercises, relax in your favorite asanas, if you practice yoga, and do breathing exercises. But you should give up training in the gym, running, and long walks.
  4. Follow your diet, switch to light, dietary foods. It will be helpful to add more liquid foods to your diet, as well as fruits and vegetables.
  5. Support the body with vitamins. This will help him recover faster.

conclusions


Compared to its analogues, Prozac is a mild antidepressant. It does not cause significant harm to the body and can be prescribed as a means of transitioning from potent drugs to completing a course of treatment.

Prozac withdrawal syndrome is uncommon, occurring in only 5% of patients. At the same time, the manifestations of withdrawal are not the most severe and do not require medication.

In order to avoid unpleasant symptoms after stopping its use, you should strictly follow your doctor’s recommendations. The cumulative effect ensures long-lasting action and high efficiency of the drug. The exit from it should be as smooth as the beginning.

Symptoms of fluoxetine overdose

Exceeding the dose of the drug recommended by the doctor and the frequency of its administration leads to the appearance of a number of symptoms indicating an overdose. In this case, immediate contact with a specialist is required, because the likelihood of death due to complications is high. The main signs indicating fluoxetine poisoning are:

  • Mental excitement
  • Increased motor activity that does not have any purpose
  • Convulsions resembling epileptic seizures
  • Arrhythmias of various types
  • Cardiopalmus
  • Nausea, the climax of which is repeated vomiting.

Nausea and vomiting are signs of fluoxetine overdose

Patients should know that they cannot exceed the recommended dose, much less prescribe the drug themselves, because There is no effective specific antidote. In case of overdose, it is possible to carry out only symptomatic therapy - this is the fight against the clinical signs of poisoning, and not the elimination of its cause (binding of Fluoxetine molecules). Required components are:

  • gastric lavage
  • prescribing enterosorbents (activated carbon, Enterosgel and others), anticonvulsants and antiarrhythmic drugs.

Literature:

  1. Kokin, Ivan Vitalievich. Pharmacokinetics and clinical effectiveness of domestic drugs Amitriptyline and Fluoxetine: dissertation of a candidate of medical sciences: 14.00.25 / Kokin Ivan Vitalevich; - Moscow, 2008. - 154 p.
  2. Arushanyan, Eduard Beniaminovich. Antidepressants: (In questions and answers) / E. B. Arushanyan. - Stavropol, 2002. - 331 p.
  3. Antidepressants and treatment of depressive conditions: (Psychopharmacol. and clinical research): Ed. I. P. Lapin, T. Ya. Khvilivitsky. — Leningrad: Medicine. Leningr. department, 1966. - 291 p.
  4. Pharmacology of antidepressants: a textbook for students in the areas of specialty training “General Medicine”, “Pediatrics”, “Pharmacy” / [I. A. Vinogradova, V. D. Yunash, S. V. Goranskaya, etc.] - Petrozavodsk: PetrSU Publishing House, 2021. - 36 p.
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