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Analogs of Fluoxetine.
Other names for this medication:
Actan, Adofen, Alental, Apo-fluoxetin, Astrin, Auscap, Bioxetin, Depreks, Deproxin, Diesan, Equilibrane, Erocap, Eufor, Flotina, Floxet, Flucti-nerton, Fluctin, Fluctine, Fludac, Flufran, Fluneurin, Flunil, Fluox, Fluox-puren, Fluoxac, Fluoxeren, Fluoxeron, Fluoxetina, Fluoxetinum, Fluoxil, Fluoxin, Fluseren, Flutine, Fluxet, Fluxil, Fluxonil, Fondur, Fontex, Fysionorm, Ladose, Lovan, Margrilan, Motivone, Oxetine, Pragmaten, Prodep, Pronil, Prozac, Reneuron, Rowexetina, Seronil, Zactin.
Fluoxetine tablets contain 20 mg fluoxetine, as well as lactose monohydrate, gelatin, corn starch, calcium stearate, povidone, silicon (Si) colloidal dioxide, talc, magnesium (Mg) light carbonate, tropeoline 0, additive E171 (titanium (Ti ) dioxide), mineral oil, sugar, yellow wax.
Form of issue
Tablets covered with a film coating of yellow color in blisters for 10 pcs, 1 or 2 blisters in a package.
The drug has an anorexigenic effect, eliminates depression and relieves feelings of depression.
Pharmacodynamics and pharmacokinetics Fluoxetine – what is it?
The active substance of the preparation fluoxetine hydrochloride is a water-soluble crystalline powder of white (or almost white) color.
What is Fluoxetine?
Fluoxetine is a selectively inhibitory reverse neuronal seizure of serotonin (ONS) agent. The drug belongs to the pharmacotherapeutic group “Antidepressants”.
The medicine is intended for oral administration. The mechanism of its action is related to the ability to selectively (selectively) and reverse the ONZS.
Antidepressant Fluoxetine slightly affects the capture of dopamine and norepinephrine and weakly affects acetylcholine receptors and H1-type histamine receptors.
Along with antidepressant also has a stimulating effect. After taking the tablets / capsules, the patient’s fear, anxiety and mental tension decrease, the mood improves, the symptoms of dysphoria are eliminated.
Wikipedia notes that the remedy does not cause orthostatic hypotension, does not have a sedative effect, is not cardiotoxic.
To achieve a stable clinical effect with regular use of the drug takes from 3 to 4 weeks.
➡absorption in the alimentary canal – good;
➡bioavailability – 60% (with oral administration);
➡ТСмах – from 6 to 8 hours;
➡binding to plasma proteins (including alpha (α) -1-glycoprotein and albumin) – 94.5%;
➡T½ – 48-72 hours.
The liver is involved in the metabolism of the substance. As a result of its biotransformation, a number of unidentified metabolites are formed, as well as norfluoxetine, the selectivity and activity of which is equivalent to that of fluoxetine.
Pharmacologically inactive metabolic products are eliminated by the kidneys.
Due to the fact that the substance is removed from the body slowly enough, the plasma concentration necessary for maintaining the therapeutic effect persists for several weeks.
Indications for use: what are the prescribed tablets and fluoxetine?
Indications for use of fluoxetine:
➡depression (in particular, accompanied by fears), including with the inefficiency of other antidepressants;
➡obsessive-compulsive disorder (OCD);
➡kinoreksiya (to reduce uncontrolled craving for food, the remedy is used as part of complex psychotherapy).
The drug is not prescribed when:
➢known hypersensitivity to its active substance or any of the auxiliary ➢components;
➢convulsive conditions in the anamnesis;
➢severe liver and / or kidney failure;
➢vatony of the bladder;
➢simultaneous application with MAO inhibitors .
After using MAO inhibitors, Fluoxetine can be used no earlier than 14 days; MAO inhibitors after the end of treatment with fluoxetine are prescribed no earlier than 5 weeks.
Side effects of fluoxetine
General disorders that occur during the use of the drug may manifest in the form of hyperhidrosis, chills, fever or cold sensation, photosensitivity, neuroleptic syndrome, alopecia, lymphadenopathy, anorexia, erythema multiforme, which can progress to malignant exudative or develop into Lyell’s syndrome.
Some patients have symptoms of serotonin intoxication, including: ➳changes in mental status (delirium, euphoria, anxiety, agitation, hallucinations, mutism, confusion, manic syndrome, coma);
➳neuromuscular pathologies (akathisia, coordination disorders, bilateral Babinsky symptom, hyperreflexia, myoclonus, epileptiform seizures, nystagmus (horizontal and vertical), oculogic crises, paresthesia, opisthotonus, tremor, muscular rigidity);
➳vegetative dysfunction (hyperthermia, abdominal and headaches, diarrhea, dilated pupils, lacrimation, tachypnea, tachycardia, nausea, fluctuations in blood pressure, hyperhidrosis, chills).
From the digestive system of organs are possible: diarrhea, nausea, decreased appetite, vomiting, dysphagia, dyspepsia, taste change, pain in the esophagus, dry mouth, dyskinesia, liver dysfunction. In isolated cases, idiosyncratic hepatitis can develop.
CNS reactions to the taking of tablets are manifested in the form of: ➣bruxism, headache, weakness, sleep disorders (nighttime delirium, pathological dreams, insomnia), dizziness, fatigue (hypersomnia, drowsiness); ➣violations of attention, processes and concentration of thinking, memory; anxiety and associated psychovegetative syndrome, dysphemia, panic attacks, suicidal thoughts and / or attempts to deprive oneself of life.
Reactions from the urogenital tract: ➣dysuria, urine retention, polakii-and nocturia, protein and albuminuria, polyuria, oliguria, UTI, renal failure, cystitis, decreased libido (before its complete loss), erectile dysfunction, breast enlargement and soreness , disorders of ejaculation, anorgasmia, priapism, impotence, metro- and menorrhagia, painful menstruation.
The probability of development is not excluded:
➣immunopathological and allergic reactions;
➣myalgia, arthralgia, chondrodystrophy, bone pain, osteomyelitis, arthritis and a number of other side effects from the musculoskeletal system;
➣metabolic disorders (including hyponatremia, hypocalcemia, hyper- or hypokalemia, vasopressin secretion disorder, diabetes mellitus, hypercholesterolemia, hyperuricemia, edema, diabetic acidosis, dehydration, hypothyroidism);
➣skin reactions (including polymorphic rash, acne, ulcerative lesions of the skin, gyrustism, psoriasis, furunculosis, exfoliative dermatitis, etc.).
Discontinuation of treatment with the drug can trigger a withdrawal syndrome, the main signs of which are: sensitivity disorders, dizziness, sleep disorders, asthenia, nausea and / or vomiting, agitation, headache, tremor.
Reviews of side effects suggest that the drug with uncontrolled admission is addictive. In some cases, the dependence is so strong that a person needs the help of a specialist to treat it.
Other adverse reactions that patients mention in the reviews are severe drowsiness, tremors, convulsions, decreased appetite, nausea. Nevertheless, there are people who had no adverse effects on the background of treatment at all.
Instructions for use of fluoxetine
Tablets are taken orally. The intake of food for assimilation of the drug is not affected.
For relief of depressive symptoms, the drug should be drunk 1 time per day, in the morning, at a dose of 20 mg. With clinical need, 3-4 weeks after the start of therapy, the frequency of receptions is increased to 2 r. / Day. (tablets are taken in the morning and in the evening).
Patients with an insufficient response to treatment at a dosage of 20 mg / day, in some cases, the daily dose is gradually increased to 60-80 mg. In this case, divide it into 3-4 receptions. The highest dose for people of elderly and senile age is 60 mg / day.
Dosage for bulimic neurosis – 60 mg / day. (tablets take 3 r./day on one), in ROC – depending on the severity of clinical symptoms – from 20 to 60 mg / day.
It should be taken into account that increasing the dose may increase the severity of side effects.
The maintenance dose is 20 mg / day.
When does the drug start to act?
Significant improvement in the condition is usually observed after about 2 weeks of systematic drug intake.
How long should I take fluoxetine?
The elimination of depressive symptoms goes away from six months.
In obsessive manic disorders (HMP), the drug is given to the patient for 10 weeks. Further recommendations depend on the results of treatment. If there is no clinical effect, the fluoxetine treatment regimen is revised.
If there is a positive dynamics, therapy is continued with the use of an individually selected minimum maintenance dose. Periodically, the patient’s need for further treatment should be reviewed.
Long-term – more than 24 weeks in patients with HMR and more than 3 months in patients with bulimia nervosa – has not been studied.
After the treatment with Fluoxetine is completed, the active substance circulates in the body for another 2 weeks, which should be taken into account when discontinuing treatment or prescribing other medicines.
Patients with liver / kidney failure, elderly people with concomitant diseases, as well as patients taking other medicines, are prescribed a half dose of the drug. In some cases, it is advisable to transfer the patient to an intermittent reception.
It is not recommended to abruptly stop therapy with fluoxetine. The drug is canceled, gradually reducing the dose for 1-2 weeks. This avoids the development of withdrawal syndrome.
If after the dose reduction / withdrawal the patient’s condition worsens, it is necessary to return to treatment with the previous effective therapeutic dose. Gradual reduction of the dose is resumed after the appearance of positive dynamics.
If we compare Fluoxetine and Fluoxetine Lannacher or Fluoxetine and Fluoxetine OZONE, we can conclude that the instructions for the use of Fluoxetine Lannacher and Fluoxetine OZON provide recommendations similar to those listed above.
Overdosage Fluoxetine is accompanied by: nausea / vomiting, convulsions, hypomania, anxiety, agitation, large epileptic seizures.
A high dose of the drug in combination with codeine, maprotiline, temazepam can lead to death.
The person suffering from an overdose should be washed with a stomach, give sorbitol, enterosorbent and – with convulsions – diazepam. Also, monitoring of respiratory activity and parameters characterizing the functional state of the heart is important. In the future, symptomatic and supportive therapy is performed.
Peritoneal dialysis, blood transfusion, hemodialysis, forced diuresis are ineffective.
Strengthens the effects of hypoglycemic drugs, ethanol, diazepam, alprazolam.
Twice increases the plasma concentration of tricyclic antidepressants, phenytoin, trazodone, maprotiline. When appointing fluoxetine in combination with tricyclic antidepressants, the dose of the latter should be reduced by 50%.
It can provoke an increase in the plasma concentration of Li +, which in turn increases the likelihood of developing its toxic effects. In case of simultaneous application, it is recommended to keep the concentration of Li + in the blood under control.
The use as an adjunct to electroconvulsive therapy can lead to the development of prolonged epileptic seizures.
Serotonergic effects of the drug are enhanced in combination with tryptophan. The likelihood of the development of serotonin intoxication is increased in the case of simultaneous administration with agents suppressing the enzyme MAO.
The likelihood of adverse reactions and increased oppressive effects on the central nervous system increases in combination with drugs that depress the central nervous system.
Admission with drugs that have a high degree of binding to proteins can trigger an increase in the plasma concentration of unbound (free) drugs, as well as an increase in the likelihood of unwanted effects.
Tablets should be stored at a temperature below 25 ° C.
In the treatment of patients with low body weight, anorexic effects should be considered when prescribing the drug.
In diabetics during treatment Fluoxetine may develop hypo-, and after discontinuation of the drug – hyperglycemia. In view of this, it is recommended to make changes in the dosage regimen of insulin and / or hypoglycemic agents for oral administration. Before the improvement of the clinical picture, patients with diabetes should be under constant medical supervision.
During treatment it is necessary to refrain from engaging in activities that require high speed of psychomotor reactions and increased attention.
The composition of the tablets includes lactose, so they should not be taken with galactosemia, lactase deficiency, the syndrome of impaired glucose / galactose absorption.
Like other antidepressants, fluoxetine can cause affective disorders (mania or hypomania).
The central organ of the metabolism of the drug is the liver, the excretion of metabolites is responsible for the kidneys. Patients with liver pathologies should be prescribed low or alternative daily doses.
With renal failure (with Clcr less than 10 ml / min.) After 2 months of treatment with a dose of 20 mg / day. the plasma concentration of fluoxetine / norflouxetine is the same as in patients with healthy kidneys.
Depression is associated with an increased risk of suicidal thoughts and attempts to kill oneself. The risk persists until complete remission. Clinical experience of the drug shows that the risk of suicide increases, usually in the early stages of recovery.
Patients with mental illness and depressive syndrome should be under constant supervision. In placebo-controlled studies, the group receiving antidepressant patients found that the risk of suicidal behavior is highest in people under 25 years of age.
Special attention is also required by patients who have been transferred to a lower / higher dose.
The use of fluoxetine is associated with the development of akathisia, the subjective features of which are the constant need to be in motion, as well as the inability to sit or stand. These phenomena are especially pronounced in the first weeks of treatment. Patients who developed similar symptoms, the drug is prescribed in the minimum effective dose.
With a sudden discontinuation, approximately 60% of patients develop withdrawal symptoms. The likelihood of their appearance depends on the dose used, the duration of the course, and the level of dose reduction. The dose is recommended to be reduced by titration within 7-14 days.
There have been reports of subcutaneous hemorrhages, such as purpura or ecchymosis, occurring during the treatment period. Therefore, patients taking oral anticoagulants, affecting the function of platelets and increasing the likelihood of hemorrhages, as well as patients with bleeding history, Fluoxetine is prescribed taking into account possible risks.
Which is better: Prozac or Fluoxetine?
The active substance of the drug Prozac is fluoxetine. Therefore, when choosing in favor of this or that tool, the decisive factors are price and subjective sensations. The cost of fluoxetine is much lower than the cost of its analogue.
Not applicable for treatment of patients younger than 18 years.
A nineteen-week clinical trial showed that in children suffering from depression, 8-18 years of age, Fluoxetine causes a decrease in body height and weight. The effect of the drug on achieving normal growth in adulthood has not been studied.
At the same time, the probability of growth retardation in the pubertal period can not be ruled out.
Fluoxetine and alcohol
Drinking alcohol during treatment with fluoxetine is contraindicated.
Fluoxetine for weight loss
Fluoxetine is often prescribed for a bulimic syndrome – a mental syndrome, which is accompanied by a lack of satiety and uncontrolled overeating.
The use of the drug can reduce appetite and relieve a constant feeling of hunger.
Thus, it can be concluded that fluoxetine can get rid of excess weight only if the reason for its collection is the appetite.
However, the drug is not intended for weight loss, its main purpose is the treatment of depression. Reducing appetite and losing weight are side effects.
The drug is quite powerful, and the body often responds to its reception with anaphylactic reactions and systemic disorders involving the pathological process of the lungs, skin, kidneys and liver.
How to take fluoxetine for weight loss?
At the initial stage, diet pills are taken in the minimum dosage – one once a day. With good tolerability, you can go to the reception of two tablets – one drink in the morning, the second – in the evening.
The maximum allowable dose is 4 tab. / Day.
The drug begins to act after 4-8 hours, removing fluoxetine from the body takes about a week.
Reviews on the forums confirm the effectiveness of the means – for 1-3 months people without much effort got rid of 5-13 kg. In this case, all patients taking Fluoxetine note that it is not worth while to drink it just for the sake of losing weight, like Fenibut or Fentropil, in the absence of evidence.
The safety of the drug in pregnant women is poorly understood, the results of individual published epidemiological studies are contradictory. In some random and cohort studies, there was no increase in the likelihood of congenital developmental abnormalities.
ENTIS prospective study suggests an increase in the likelihood of developing congenital anomalies in the structure of large vessels or heart in children whose mothers took fluoxetine in the 1st trimester of pregnancy, compared with children whose mothers did not receive this medication.
It was not possible to establish a reliable relationship between the use of the drug in the early stages of pregnancy and the formation of malformations in the fetus. The specific group of CCC abnormalities was also not determined.
The use of SSRIs in the last weeks of pregnancy contributes to the development of complications in newborns, in particular, the prolongation of the duration of ventilation and probe nutrition and the duration of hospitalization.
There are mentions of 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.
The listed pathological conditions can be a consequence of the syndrome of withdrawal of SSRIs or the manifestation of their toxic effects.
Reviews of fluoxetine
Feedback from the host fluoxetine (APO, Lannacher, Kanon) patients leave the impression of the efficacy of this remedy for depression, bulimic neuroses and OCD.
At forums also the possibility of application of a preparation for the control of appetite and correction of weight is quite often discussed.
Reviews of doctors about fluoxetine for weight loss are unequivocal: you can use a medicine to fight excess pounds only if the cause of weight gain is a mental disorder.
When excess weight is the result of depression caused by stress or overeating, the drug for 2-3 weeks can completely get rid of binge eating attacks and for the first month to remove up to 5 kg.
Reviews losing weight about Fluoxetine (Lannacher, OZONE, etc.) allow you to conclude that to reduce weight on this drug is not possible to all: someone has completely lost appetite (right up to aversion in food), someone has left it the former.
However, in most cases, the remedy has serious side effects: many people who took it noted a decrease in sexual desire and a deterioration in sexual life, a sense of inhibition, severe pain, drowsiness, increased aggression, the appearance of suicidal thoughts.
In addition, for many of the debilitated drugs, the need to stop driving and drinking alcohol, and the fact that fluoxetine is highly addictive.
Summarizing reviews, the following conclusions can be drawn: Fluoxetine is primarily a cure for depression and can only be taken if there is evidence and only under the supervision of a doctor.