Fluoxetine-canon - instructions for use, dose, side effects, contraindications

Description:capsule number 3 in blue. Contents of capsules - a mixture of granules and powder white or white with a yellowish hue.Presence of separate lumps is allowed.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.03 Fluoxetine

Pharmacodynamics:

Antidepressant. Selectively inhibits the reuptake of serotonin, which leads to an increase in its concentration in the synaptic cleft, enhance and prolong the action on postsynaptic receptors. Increasing serotonergic transmission, by the mechanism of negative feedback fluoxetine inhibits neuromediator metabolism. With prolonged use fluoxetine inhibits the activity of 5-HT1-receptors. Poorly affects the re-uptake of norepinephrine and dopamine. It has no direct effect on serotonin, m-cholinergic, H1-histamine and alpha-adrenergic receptors. Unlike most antidepressants, does not cause a decrease in the activity of postsynaptic beta-adrenoreceptors.

Effective with endogenous depression and obsessive-compulsive disorders. Improves mood, reduces tension, anxiety and fear, eliminates dysphoria. Has an anorexigenic effect, can cause weight loss.Does not cause orthostatic hypotension, sedation, non-cardiotoxic. A persistent clinical effect occurs after 1-2 weeks of treatment.

Pharmacokinetics:

Absorption is high. The time to reach the maximum concentration (15-55 ng / ml) in the blood plasma after taking the drug inside at a dose of 40 mg is 6-8 hours. Bioavailability when ingested - more than 60%. Eating does not affect bioavailability.

Binding to plasma proteins is 94.5% (including albumin and alpha1-acid glycoprotein). It is distributed throughout the body. Easily penetrates the blood-brain barrier. Equilibrium concentration in blood plasma is achieved after taking the drug for several weeks.

It is subjected to intensive biotransformation in the liver to the active metabolite of norfluxetine and a number of other unidentified metabolites. It is an inhibitor of isoenzymes CYP2C19, CYP3A2, CYP3A3, CYP3A5 and CYP3A7.

It is excreted by the kidneys in the form of metabolites (80%) and intestine (15%), mainly in the form of glucuronides. The half-life of fluoxetine after reaching the equilibrium concentration in blood plasma is 4-6 days. Half-life of activemetabolite of norfluoxetine for a single admission and after reaching the equilibrium concentration in blood plasma is 4-16 days. In patients with cirrhosis of the liver, the half-life period is 3-4 times longer.

Indications:

- depression of different etiology;

- bulimia nervosa;

- obsessive-compulsive disorder.

Contraindications:

- hypersensitivity;

- simultaneous administration of monoamine oxidase inhibitors (MAO) and within 14 days after their cancellation;

- simultaneous administration of thioridazine (and within 5 weeks after the abolition of fluoxetine), pimozide;

- liver failure;

- renal failure (creatinine clearance less than 10 ml / min);

- atony of the bladder;

- angle-closure glaucoma;

- hyperplasia of the prostate;

- pregnancy;

- lactation period;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- age to 18 years.

Carefully:

Suicide risk: with depression, there is a likelihood of suicide attempts, which can persist until the onset of persistent remission. Individual cases of suicidal thoughts and suicidal behavior have been described against the background of treatment with fluoxetine or shortly after its closure, similar to the effect of other drugs close pharmacological action (antidepressants).Careful monitoring of patients at risk is necessary. Physicians should convince patients to immediately report any thoughts and feelings of concern.

Epileptic seizures: as in the case of other antidepressants, fluoxetine should be administered with caution to patients who have previously had epileptic seizures.

Hyponatremia: cases of hyponatremia have been reported (in some cases, the level of sodium in the serum was less than 110 mmol / l). In most cases, such cases were observed in elderly patients and in patients who received diuretics due to a decrease in the volume of circulating blood.

Glycemic control: in patients with diabetes during treatment with fluoxetine, hypoglycemia was noted, and after the drug was discontinued, hyperglycemia developed. At the beginning or after the end of treatment with fluoxetine, you may need to adjust the doses of insulin and / or hypoglycemic drugs for ingestion.

Hepatic / Renal Failure: Fluoxetine undergoes intensive metabolism in the liver and is excreted by the kidneys. Patients with severe impairment of liver function are recommended to prescribe lower doses of fluoxetine, or prescribe the drug every other day.When fluoxetine was administered at a dose of 20 mg / day for two months, patients with severe renal impairment (creatinine clearance <10 ml / min) in need of hemodialysis did not show differences in fluoxetine and norfluoxetine plasma concentrations from healthy individuals with normal kidney function.

Pregnancy and lactation:

Fluoxetine may be taken during pregnancy, provided that the intended benefit to the mother exceeds the possible risk to the fetus.

Breast-feeding: fluoxetine excreted in breast milk, therefore, caution should be exercised when administering fluoxetine to nursing mothers.

Childbirth: the effect of fluoxetine on the process of childbirth in humans is not known.

Dosing and Administration:

Depression. The initial recommended dose is 20 mg / day 1 time. If necessary, increase the dose by 20 mg / day weekly. The maximum daily dose is 80 mg in 2-3 divided doses.

Bulimia. The recommended dose is 60 mg / day in 3 divided doses.

Obsessive-compulsive disorder. The recommended dose is 20-60 mg / day. All indications. The recommended dose can be reduced or increased.Doses over 80 mg / day were not systematically studied.

Age. There is no data on the need to change the dose depending on the age.

Food intake. Fluoxetine can be taken at any time, regardless of food intake.

Concomitant diseases and / or concomitant treatment. In patients with impaired hepatic function, concomitant diseases or taking other drugs, the dose should be reduced and the frequency of administration reduced.

Side effects:

The organism as a whole: autonomic symptoms (dry mouth, sweating, vasodilation, chills), hypersensitivity (itching, skin rashes, urticaria, anaphylactic reaction, vasculitis, a reaction like serum, angioedema), serotonin syndrome (characterized by a complex of clinical manifestations of mental state changes and neuromuscular activity in combination with disorders of the autonomic nervous system), photosensitivity, erythema multiforme exudative).

Cardiovascular system: palpitation, arrhythmia.

Digestive system: gastrointestinal disorders (diarrhea, nausea, vomiting, dysphagia, dyspepsia, taste distortion), very rarely idiosyncratic hepatitis.Endocrine system: abnormal secretion of antidiuretic hormone.

Hematopoietic and lymphatic system: ecchymosis.

Metabolic and nutritional disorders: weight loss.

The musculoskeletal system: arthritis, bone pain, bursitis, leg cramps, arthrosis, myasthenia gravis, myopathy, osteomyelitis, osteoporosis, rheumatoid arthritis.

Nervous system: abnormal movements / tremor (twitching, ataxia, bucco-glasal syndrome, myoclonus, tremor), anorexia, anxiety and its manifestations (palpitation, anxiety, nervousness, agitation), dizziness, fatigue (drowsiness, asthenia), violation of concentration and thinking including depersonalization), manic disorders, sleep disorders (unusual dreams, insomnia), seizures.

Respiratory system: yawning.

Skin: alopecia.

Organs of the senses: visual impairment (blurred vision, mydriasis).

Genitourinary system: urination disorders (including changes in frequency of urination), priapism / prolonged erection, sexual dysfunction (decreased libido, delay or lack of ejaculation, anorgasmia, impotence).

Overdose:

The main manifestations of an overdose included increased side effects, seizures, drowsiness, nausea, tachycardia and vomiting.

Other serious manifestations reported in an overdose of fluoxetine (both isolated and in combination with other drugs) included coma, delirium, QT interval prolongation and ventricular tachyarrhythmia, including ventricular fibrillation and heart failure, lowering of arterial pressure, syncope, mania, pyrexia, stupor and a condition similar to a malignant neuroleptic syndrome.

Interaction:

Fluoxetine and its main metabolite, norfluoxetine, have long half-lives, which must be considered when fluoxetine is combined with other drugs, and when it is replaced with another antidepressant.

Phenytoin. Changes in the concentration of phenytoin in the blood were detected when combined with fluoxetine. In some cases, there were manifestations of intoxication. An increase in the dose of phenytoin or fluoxetine when administered concomitantly should be carried out with caution and under the control of the clinical dynamics of the condition. Serotonergic drugs.Simultaneous reception of serotonergic drugs (eg, tramadol and triptans) contributes to an increased likelihood of developing serotonin syndrome. Simultaneous administration of triptans also contributes to an increase in the likelihood of development of constriction of coronary vessels and arterial hypertension.

Benzodiazepines. With the simultaneous use of fluoxetine and benzodiazepines, an increase in the half-life of the latter may be possible. With the simultaneous administration of alprazolam and fluoxetine, an increase in the concentration of alprazolam in the blood and an increase in its sedative effect were observed.

Lithium and tryptophan. There are known cases of the development of serotonin syndrome with the simultaneous administration of selective serotonin reuptake inhibitors (SSRIs) and lithium or tryptophan, and simultaneous administration of fluoxetine with these drugs should be carried out with caution. With the simultaneous administration of fluoxetine and lithium, more frequent and careful monitoring of the clinical state is necessary.

Drugs metabolized with the participation of the isoenzyme CYP2D6 (propafenone, carbamazepine, tricyclic antidepressants).It should be noted that the metabolism of fluoxetine (as well as tricyclic antidepressants, as well as selective serotonergic antidepressants) is carried out with the participation of the CYP2D6 isoenzyme of the liver cytochrome system. Simultaneous reception of drugs, the main pathway of biotransformation of which is metabolism with the participation of the CYP2D6 isoenzyme, and having a small interval of therapeutic doses (such as propafenone, carbamazepine, tricyclic antidepressants) should be given with the use of minimal therapeutic doses. The foregoing is also applicable if less than 5 weeks after fluoxetine has been discontinued.

Indirect anticoagulants and other drugs that affect the blood coagulation system (Nonsteroidal anti-inflammatory drugs, acetylsalicylic acid). It is known about the change in anticoagulant effect (according to laboratory indicators and / or clinical manifestations) without any general characteristic tendency, but with the probability of increased bleeding with simultaneous administration of fluoxetine and oral anticoagulants. Functional state of the blood coagulation system in patients receiving warfarin, should be carefully monitored when fluoxetine is prescribed and withdrawn.

Electroconvulsive therapy (ECT). There are rare reports of an increase in the duration of seizures in patients taking fluoxetine and receiving ECT, in this regard, it is recommended to be cautious.

Alcohol. In experimental studies fluoxetine did not contribute to increasing the concentration of alcohol in the blood, as well as enhancing the effects of alcohol. However, simultaneous intake of SSRIs and alcohol is not recommended.

Means based on the plant Hypericum perforatum. As with other SSRIs, it is possible to develop pharmacodynamic interactions between fluoxetine and Hypericum perforatum plants, which can lead to an increase in undesirable effects.

Special instructions:

In the treatment of patients with body weight deficiency, anorexic effects of fluoxetine should be considered (progressive weight loss is possible).

In patients with diabetes mellitus, administration of fluoxetine increases the risk of developing hypoglycemia; when it is canceled - hyperglycemia. In this regard, the dose of insulin and / or any other hypoglycemic medications used orally should be adjusted. Patients should be supervised by a physician.

The interval between the end of therapy with monoamine oxidase inhibitors MAO and the start of treatment with fluoxetine should be at least 14 days; between the end of fluoxetine treatment and the initiation of therapy with MAO inhibitors - at least 5 weeks. It requires careful monitoring of patients with suicidal tendencies, especially at the beginning of treatment. The highest risk is suicide in patients who have previously taken other antidepressants, and patients who have excessive fatigue, hypersomnia, or motor anxiety with fluoxetine.

When conducting electroconvulsive therapy with fluoxetine, prolonged epileptic seizures are possible.

During treatment, one should refrain from drinking alcohol and practicing potentially dangerous activities that require increased attention and speed of mental and motor reactions.

In children, adolescents and young people (under 24 years) with depression, other mental disorders, antidepressants compared with placebo increase the risk of suicidal thoughts and suicidal behavior. Therefore, in the appointment of fluoxetine or any other antidepressant drugs in children, adolescents and young people (younger than 24 years), the risk of suicide and the benefits of their use should be correlated.In short-term studies in people over 24 years of age, the risk of suicide did not increase, and people older than 65 years decreased slightly. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of abnormalities or behavioral changes, as well as suicidal tendencies.

It is reported the occurrence of skin rash, anaphylactic reactions and progressive systemic disorders, sometimes serious involving the pathological process of the skin, kidneys, liver and lungs in patients taking fluoxetine. If skin rashes or other possible allergic reactions occur, the etiology of which can not be determined, fluoxetine should be withdrawn.

Form release / dosage:Capsules 20 mg.

Packaging:

For 10 or 15 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3, 5 contour cell packs of 10 capsules or 1, 2, 3 contour cell packs of 15 capsules together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

List B.In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000352

Date of registration:27.04.2010

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Fluoxetine-canon (Fluoxetine-Kanon)