Apo-Fluoxetine
Apo-Fluoxetine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Apo-Fluoxetine
ATX code: N06AB03
Active ingredient: fluoxetine (Fluoxetine)
Manufacturer: Apotex Inc. (Apotex Inc.) (Canada)
Description and photo update: 2019-10-07
Apo-Fluoxetine is an antidepressant with thymoanaleptic and stimulating effects.
Release form and composition
The preparation is produced in the form of capsules: size No. 3, gelatinous solid, opaque, with a yellow-white body and a green cap and an inscription in black ink "APO 20"; the contents of the capsules are almost white or white powder (7 or 10 pieces in a blister made of aluminum foil and film, 1–5 or 10 blisters in a cardboard box; 14, 20, 28, 30, 35, 50, 100, 200 or 500 pieces in a bottle made of high-pressure polyethylene, 1 bottle in a cardboard box, for hospitals - 90 bottles of 100 or 500 pieces in a cardboard box. Each box also contains instructions for the use of Apo-Fluoxetine).
1 capsule contains:
- active substance: fluoxetine hydrochloride - 22.4 mg (which corresponds to 20 mg fluoxetine);
- additional components: stearic acid, wheat starch, lactose monohydrate;
- capsule shell: gelatin, titanium dioxide (E 171); body - iron oxide black (E 172), quinoline yellow dye (E 104); cap - dyes: yellow "Sunset" (E 110), quinoline yellow (E 104), brilliant blue FCF (E 133);
- composition of ink: iron oxide black (E 172), shellac, dyes - charming red AC (E 129), indigo carmine varnish (E 132), brilliant blue FCF (E 133), yellow "Sunset" (E 110).
Pharmacological properties
Pharmacodynamics
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) antidepressant with thymoanaleptic and stimulatory effects. The active substance selectively inhibits the reverse neuronal uptake of serotonin (5HT) in the synapses of the neurons of the central nervous system (CNS). The blocking of serotonin reuptake produced by Apo-Fluoxetine causes an increase in the level of this neurotransmitter in the synaptic cleft, contributes to the lengthening and enhancement of its action on the receptor sites of the postsynaptic membrane. Fluoxetine, obtained in therapeutic doses, inhibits the uptake of serotonin by human platelets. The active substance belongs to weak antagonists of muscarinic, adrenergic α- and α 2 -receptors, histamine H 1-receptors, has little effect on dopamine reuptake. In contrast to most antidepressants, fluoxetine, presumably, does not lead to a decrease in the functional activity of postsynaptic β-adrenergic receptors. Helps to improve mood, reduce feelings of tension and fear, eliminate dysphoria. Does not have a sedative effect, impairs appetite, which can cause weight loss. When used in moderate therapeutic doses, Apo-Fluoxetine has almost no effect on the functioning of the cardiovascular and other systems.
Pharmacokinetics
When taken orally, fluoxetine is quite well absorbed from the gastrointestinal tract (GIT) - up to 95% of the administered dose; simultaneous use with food slows down its absorption to a slight extent. Maximum plasma concentrations in the blood are observed after 6-8 hours. The bioavailability of fluoxetine after oral administration is more than 60%. The agent is well distributed in tissues, easily passes through the blood-brain barrier (BBB), and binds to blood plasma proteins by more than 90%. The metabolic transformation of fluoxetine occurs in the liver through demethylation to norfluoxetine (an active metabolite) and a group of unidentified metabolites.
Excreted by the kidneys, the clearance of fluoxetine can vary from 94 to 704 ml / min, norfluoxetine - from 60 to 336 ml / min. The presence of renal failure does not significantly affect the rate of elimination of the basic substance. Approximately 12% of the dose taken is excreted through the gastrointestinal tract, the half-life (T ½) of fluoxetine is approximately 2-3 days, norfluoxetine is 7-9 days.
Apo-Fluoxetine is excreted in breast milk - the level of content may correspond to 25% of that in serum.
In patients with liver failure, T ½ of both fluoxetine and its active metabolite is lengthened.
Indications for use
- obsessive compulsive disorder;
- depression of various origins;
- bulimic neurosis.
Contraindications
Absolute:
- pregnancy and lactation;
- severe functional disorders of the kidneys [creatinine clearance (CC) below 10 ml / min] and / or liver;
- combination therapy with monoamine oxidase (MAO) inhibitors (the period between the end of treatment with MAO inhibitors and the start of taking fluoxetine should be at least 14 days, and between the end of using fluoxetine and the start of treatment with MAO inhibitors - at least 35 days);
- hypersensitivity to any component of the drug.
Relative (use Apo-Fluoxetine capsules with extreme caution):
- Parkinson's disease;
- convulsive syndrome due to various conditions, epilepsy (including data in anamnesis);
- diabetes;
- compensated renal / hepatic impairment;
- excessive weight loss;
- suicidal tendencies.
Apo-Fluoxetine, instructions for use: method and dosage
Apo-Fluoxetine capsules are taken orally, regardless of meal time.
At the beginning of the course, it is recommended to use the drug in the morning at a dose of 20 mg 1 time per day. In the future, if necessary, it is allowed to increase the daily dose to 40-60 mg taken in 2-3 doses. The maximum allowable dose is 80 mg per day.
The clinical effect is observed approximately 1–4 weeks after the start of the course, but in some patients it can be observed even later.
With obsessive-compulsive disorder, the recommended daily dose of Apo-Fluoxetine is 20-60 mg, with bulimic neurosis - 60 mg in 2-3 doses.
The recommended dose of fluoxetine for elderly patients is 20 mg per day (at the beginning of the course, ½ of the recommended initial daily dose should be used - 10 mg).
Side effects
- CNS: hypomania / mania, increased irritability, insomnia / drowsiness, agitation, anxiety, headache, dizziness, asthenic disorders, tremors, increased suicidal tendencies; convulsive seizures (if they develop, therapy with Apo-Fluoxetine is canceled);
- digestive tract: hypersalivation or dry mouth, impaired taste, decreased appetite, nausea, diarrhea, vomiting; anorexia and a decrease in body weight are possible;
- genitourinary system: urinary incontinence / retention, vaginitis, dysmenorrhea, decreased libido, sexual dysfunction in men - delayed ejaculation;
- others: rarely - allergic reactions, manifested in the form of an increase in body temperature, chills, skin rash, itching, urticaria, pain in muscles and joints (with these violations, it is possible to prescribe steroid and antihistamines), increased sweating, impaired visual acuity, hyponatremia, tachycardia, vasculitis.
The above adverse events were more often recorded at the beginning of the course of treatment or with an increase in the dose of Apo-Fluoxetine.
Overdose
Symptoms of an overdose of fluoxetine include the following reactions: nausea, vomiting, psychomotor agitation, tachycardia, heart rhythm disturbances, seizures.
With these violations, symptomatic treatment is prescribed, gastric lavage with the intake of activated carbon. In the event of seizures, diazepam is administered and measures are taken to maintain respiration, cardiac activity and normal body temperature.
No specific antagonists to fluoxetine were found.
special instructions
During treatment with Apo-Fluoxetine, with concomitant electroconvulsive therapy, the risk of developing prolonged epileptic seizures increases.
Patients with diabetes mellitus may develop hypoglycemia during therapy, and hyperglycemia after discontinuation of fluoxetine.
When using the drug in patients with insufficient body weight, it is necessary to take into account the likelihood of anorexigenic effects, including progressive weight loss.
After completion of treatment with Apo-Fluoxetine, its therapeutic serum concentration in the blood can persist for several weeks.
During the period of fluoxetine therapy, ethanol-containing drinks are prohibited.
Influence on the ability to drive vehicles and complex mechanisms
During treatment, one should refrain from performing work that requires an increased speed of mental and physical reactions, including driving.
Application during pregnancy and lactation
Taking Apo-Fluoxetine during pregnancy and lactation is contraindicated.
Pediatric use
The safety of fluoxetine therapy in children and adolescents has not been established.
With impaired renal function
In the presence of a severe degree of impaired renal function (CC below 10 ml / min), drug treatment cannot be performed.
Patients with moderate / mild renal impairment should use Apo-Fluoxetine with extreme caution - it is recommended to use lower doses with longer intervals between doses.
For violations of liver function
The drug is contraindicated in patients with severe hepatic impairment.
In the presence of moderate / mild liver dysfunction, the use of Apo-Fluoxetine is required in lower doses with extended periods between doses. Patients in this group should start taking the drug with ½ the dose.
Use in the elderly
In elderly patients, at the beginning of the course, the dose of Apo-Fluoxetine should be ½ of the recommended initial dose, then the daily dose for patients of this age group is increased to 20 mg.
Drug interactions
- MAO inhibitors (including antidepressants from this pharmacotherapeutic group), procarbazine, furazolidone, selegiline, tryptophan (a precursor of serotonin): their simultaneous use with fluoxetine is contraindicated, since this combination aggravates the risk of developing serotonergic syndrome, the manifestations of which may be such effects as vomiting nausea, diarrhea, chills, dysarthria, confusion, tremors, psychomotor agitation, hypomania, convulsions, hypertensive crisis;
- hypoglycemic drugs: their effect increases;
- diazepam, carbamazepine, trazodone, terfenadine, metoprolol, phenytoin (diphenin), tricyclic and tetracyclic antidepressants: the metabolism of these drugs is suppressed, which leads to an increase in their level in the blood serum and causes an increase in their effect and an increase in the development of complications;
- alcohol, centrally acting drugs that suppress the function of the central nervous system: their effect increases;
- lithium salts: an increase in the level of lithium in the blood is possible, careful monitoring of its content is required;
- anticoagulants, digitoxin and other drugs that form a high degree of binding with proteins: the plasma concentration of unbound (free) drugs increases and, as a result, the threat of undesirable effects is aggravated.
Analogs
Analogs of Apo-Fluoxetine are: Flunisan, Prozac, Fluoxetine, Fluoxetine-OBL, Fluoxetine Lannacher, Fluoxetine-Canon.
Terms and conditions of storage
Store in a place protected from moisture and light, out of reach of children, at a temperature of 15-30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Apo-Fluoxetine
According to most of the reviews on medical websites about Apo-Fluoxetine, it is inexpensive, effective and convenient to use. Many patients note that the antidepressant is highly effective in treating depression of various origins, relieves obsessive and frightening thoughts, panic attacks, anxiety and other obsessive-compulsive disorders. Also, the remedy helps with bulimic neurosis, while patients do not recommend taking the drug on their own for weight loss, since it is not intended for these purposes and can lead to a significant deterioration in the condition. All reviews indicate the need to take Apo-Fluoxetine exclusively as directed by the attending physician and only in the doses recommended by him. During the period of therapy, patients are advised not to drink alcohol in any case,as this can cause irreparable consequences and even threaten life.
The disadvantages of the remedy include the frequent appearance of side effects, especially such as lack of appetite, nausea, headache, drowsiness, indifference to everything around. Some reviews indicate a short-term effect of Apo-Fluoxetine, which manifests itself only during the period of its administration. There are some complaints about the complete absence of positive changes after the course of treatment.
Price for Apo-Fluoxetine in pharmacies
The approximate price for Apo-Fluoxetine is 52–93 rubles. per pack of 28 capsules.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
