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The antidepressant fluoxetine is one of the most popular drugs in its field. It is suitable for people with severe depression, feelings of fear, and motor problems. But if you use this drug constantly, it begins to act like fluoxetine as a drug. Because it develops a strong addiction that develops into a serious addiction. All these factors indicate that drug addicts love to use fluoxetine.
Fluoxetine is another name for Prozac. Its main effect occurs due to blocking the re-entry of serotonin into the synapse. Because of this, a person experiences the following effects:
- A feeling of mild euphoria.
- Stimulation of the nervous system.
- Decreased appetite.
- Increased muscle tone.
With an increased dose of fluoxetine, the effects become detrimental because the person becomes seriously intoxicated. And in terms of effects in case of overdose, this drug is practically not inferior to drugs with serious psychostimulant effects. Based on this fact, it can be argued that fluoxetine is a drug, but you can buy it at any pharmacy.
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]
Which fluoxetine is better
It is quite difficult to compare fluoxetines from different manufacturers. They all have similar properties and indications for use. The difference in the composition of additional ingredients and in the methods of purification of raw materials usually affects the frequency of adverse reactions and the speed of onset of the effect.
Most specialists in the treatment of depression and obsessive-compulsive disorder prefer the original drug, Prozac, due to the extensive evidence base of its effectiveness and safety. Other European-made fluoxetines also have the least amount of adverse reactions: Apo-Fluoxetine or Fluoxetine Lannacher. Since these drugs are more affordable, they are in great demand. At the same time, patients consider Apo-Fluoxetine to be the least effective drug among those listed, although it is well tolerated.
Among Russian antidepressants, Fluoxetine-Canon receives the most positive reviews, while drugs from Ozon and Biocom, which act more slowly, receive negative reviews. However, it must be borne in mind that the reaction to a particular medication is individual for each person. Many patients with depression do not see any difference at all in the action of Fluoxetine Lannacher or Ozone. Then they choose a cheaper product.
Weight loss is usually caused by medications from all manufacturers equally. If weight does not decrease while taking Fluoxetine, then this is usually not due to the low quality of the drug, but to deeper causes of excess weight: metabolic disorders or decreased function of the endocrine glands.
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
Mechanism of action of Fluoxetine
The drug prevents the reuptake of serotonin, helping to increase its concentration. As a result, after taking it, mood normalizes, apathy disappears, and performance increases. Fluoxetine has a slight effect on the uptake of dopamine and norepinephrine, having a selective antidepressant and pronounced stimulating effect.
The drug does not cause mental retardation, drowsiness, and does not reduce the speed of motor reactions and intellectual abilities. Fluoxetine helps get rid of dysphoria, fear, indecision, emotional instability, tension, absent-mindedness, and helps to better concentrate. The product has the property of reducing appetite until it is completely absent.
Fluoxetine is well absorbed through the mucous membranes, has high bioavailability, and binds to blood proteins. The presence or absence of food does not affect the speed of action of the medicine. The active substance is metabolized in liver tissue. The elimination period of the drug is long - up to 72 hours, during which their therapeutic effect persists. The antidepressant effect increases as the course continues. Lasting results are observed from 3-4 weeks of use and develop over several months.
Exceeding recommended doses or incorrect use of the drug can lead to withdrawal effects: increased depression, emotional swings.
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
Comparison of addiction between Prozac and Fluoxetine
Like safety, addiction also involves many factors that must be considered when evaluating a drug.
So, the totality of the values of such parameters as “o syndrome” in Prozac is quite similar to the similar values in Fluoxetine. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Prozac has a fairly low “syndrome” value, just like Fluoxetine.
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.
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.
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
- Wait
- If fluoxetine activates, take in the morning to avoid insomnia
- Reduce dose to 10 mg, when side effects go away, increase to 20 mg
- Side effects may appear briefly as the dose is increased
- 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
Comparison of side effects of Prozac and Fluoxetine
Side effects or adverse events are any adverse medical event that occurs in a subject after administration of a drug.
Prozac has almost the same level of adverse events as Fluoxetine. They both have few side effects. This implies that the frequency of their occurrence is low, that is, the indicator of how many cases of an undesirable effect of treatment are possible and registered is low. The undesirable effect on the body, the strength of influence and the toxic effect of Prozac is similar to Fluoxetine: how quickly the body recovers after taking it and whether it recovers at all.
