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

Cover: the dye "Sunny Sunset", yellow (E 110) - 0.0217%; dye diamond brilliant blue FCF (E 133) - 0.0196%, quinoline dye, yellow (E 104) - 0.0119%, titanium dioxide (E 171) -1.8724%, gelatin to 100%.

Composition of ink: shellac, iron oxide black (E 172), indigo carmine dye (E132) lacquer, dye red enchanting AU (E 129), dye blue diamond FCF (E 133), dye "Sunset Sun", yellow (E 110).

Description:

Hard gelatin capsules with an opaque body of yellow-white color, an opaque green cap and an inscription in black ink "АРО 20". filled with white or almost white powder. The size of capsule number 3.

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.B.03 Fluoxetine

Pharmacodynamics:

Antidepressant group selective serotonin reuptake inhibitors. Has a timoanaleptic and stimulating effect.

Selectively blocks the reverse neuronal capture of serotonin (5HT) in the synapses of neurons of the central nervous system. Inhibition of reuptake of serotonin leads to an increase in the concentration of this neurotransmitter in the synaptic cleft, enhances and prolongs its effect on postsynaptic receptor sites. In therapeutic doses fluoxetine blocking the seizure of serotonin by human platelets. It is a weak antagonist of muscarinic, histamine H₁ adrenergic α and α₂receptors, has little effect on re-uptake of dopamine. It causes a reduction in obsessive-compulsive disorders, as well as a decrease in appetite, which can lead to a decrease in body weight. Does not cause sedation. When taken in moderate therapeutic doses, it practically does not affect the function of the cardiovascular and other systems.

Pharmacokinetics:

When ingested, the drug is well absorbed from the gastrointestinal tract (up to 95% of the dose taken), use with food slightly inhibits absorption of fluoxetine. The maximum concentration in the blood plasma is reached in 6-8 hours. Bioavailability of fluoxetine after ingestion is more than 60%. The drug is well accumulated in tissues, easily penetrates the blood-brain barrier, binding to plasma proteins is more than 90%. Metabolised in the liver by demethylation to the active metabolite of norfluoxetine and a number of unidentified metabolites. It is excreted by the kidneys, the amount of clearance of fluoxetine is 94-704 ml / min, norfluoxetine 60-336 ml / min. Kidney deficiency has no significant effect on the rate of fluoxetine removal.About 12% of the drug is released through the gastrointestinal tract. The half-life of fluoxetine is about 2-3 days, norfluoxetine is 7-9 days. In patients with liver failure, the half-life of fluoxetine and norfluoxetine is prolonged. The drug is excreted in breast milk (up to 25% of the concentration in the blood serum).

Indications:

Depression of various genesis.
Obsessive-compulsive disorder
Bulimic neurosis.

Contraindications:

Hypersensitivity to the drug.
Simultaneous reception with monoamine oxidase inhibitors (MAO).
Severe renal function impairment (creatinine clearance less than 10 ml / min) and liver.
Breastfeeding period.
Pregnancy.

Carefully:Diabetes mellitus, convulsive syndrome of various genesis and epilepsy (including in the anamnesis), Parkinson's disease, compensated renal and / or liver failure, excessive weight loss, suicidal mood.

Dosing and Administration:

The drug is taken orally.

The initial dose is 20 mg once a day in the morning, regardless of food intake. If necessary, the dose can be increased to 40-60 mg / day, divided into 2-3 receptions.The maximum daily dose is 80 mg.

The clinical effect develops 1-4 weeks after the start of treatment, in some patients it can be achieved later.

Obsessive-compulsive disorder: The recommended dose is 20-60 mg per day. With bulimic neurosis, the drug is used in a daily dose of 60 mg divided into 2-3 doses.

In elderly patients, the recommended daily dose is 20 mg.

In patients with impaired liver and kidney function, the use of lower doses and the lengthening of the interval between doses is recommended.

Side effects:

From the side of the central nervous system: hypomania or mania, increased suicidal tendencies, anxiety, increased irritability, agitation, dizziness, headache, tremor, insomnia or drowsiness, asthenic disorders.

From the gastrointestinal tract: decreased appetite, impaired taste, nausea, vomiting, dry mouth or hypersalivation, diarrhea.

From the genitourinary system: urinary incontinence or retention, dysmenorrhea, vaginitis, decreased libido, sexual dysfunction in men (delayed ejaculation).

When developing, against the background of taking fluoxetine, seizures, the drug should be discarded.

Seldom occur: allergic reactions in the form of skin rashes, hives, itching, chills, fever, pain in the muscles and joints (possible use of antihistamines and steroid drugs); increased sweating, hyponatremia, tachycardia, visual acuity, vasculitis.

Perhaps the development of anorexia and weight loss.

These side effects often occur at the beginning of fluoxetine therapy or with an increase in the dose of the drug.

Overdose:

Symptoms: psychomotor agitation, convulsive seizures, heart rhythm disturbances, tachycardia, nausea, vomiting.

Treatment: specific antagonists to fluoxetine have not been found. Symptomatic therapy, gastric lavage with the appointment of activated charcoal, with convulsions - diazepam, maintaining breathing, cardiac activity, body temperature.

Interaction:

It is impossible to apply the drug simultaneously with MAO inhibitors, including antidepressants - MAO inhibitors; furazolidone, procarbazine, selegiline, as well as tryptophan (a precursor of serotonin), since it is possible to develop a serotonergic syndrome, manifested in confusion, hypomania,psychomotor agitation, convulsions, dysarthria, hypertensive crises, chills, tremor, nausea, vomiting, diarrhea. After using MAO inhibitors, administration of fluoxetine is allowed no earlier than 14 days. Do not use MAO inhibitors earlier than 5 weeks after fluoxetine withdrawal.
Simultaneous reception of fluoxetine with alcohol or with drugs of central action, causing oppression of the central nervous system, enhances their effect.
Fluoxetine blocks the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin (diphenine), which leads to an increase in serum concentrations, increasing their effect and increasing the incidence of complications.
The combined use of fluoxetine and lithium salts requires careful monitoring of the concentration of lithium in the blood, as it may be increased.
Fluoxetine enhances the action of hypoglycemic drugs.
When used simultaneously with drugs that have a high degree of binding to proteins, especially with anticoagulants and digitoxin, it is possible to increase plasma concentrations of free (unbound) drugs and increase the risk of developing adverse effects.

Special instructions:

Patients with diabetes mellitus may develop hypoglycemia during fluoxetine and hyperglycaemia therapy after withdrawal.

Against the background of electroconvulsive therapy, it is possible to develop long-term epileptic seizures.

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

After the drug is withdrawn, its therapeutic concentration in the blood serum may persist for several weeks.

During the treatment with fluoxetine, alcoholic beverages are not allowed.

Taking fluoxetine can adversely affect the performance of work that requires a high rate of mental and physical reactions (management of mechanical vehicles, mechanisms, work at height, etc.).

The interval between the end of therapy with MAO inhibitors and the initiation of treatment with fluoxetine should be at least 14 days; between the end of treatment with fluoxetine and the onset of therapy with MAO inhibitors - at least 5 weeks.

With liver diseases and in old age, treatment should be started with 1/2 dose.

Form release / dosage:Capsules 20 mg.

Packaging:

For 14, 20, 28, 30, 35, 50 or 100 capsules in high-pressure polyethylene bottles.

1 bottle per cardboard pack together with instructions for use.

For 7, 10 capsules in a contour mesh box made of a polyvinylchloride film and aluminum foil.

For 1, 2, 3, 4, 5 or 10 contour packs in a cardboard box together with instructions for use.

For hospitals

For 100 or 500 capsules in a bottle of high-density polyethylene.

90 bottles in a cardboard box together with instructions for use (the number of instructions corresponds to the number of bottles).

Storage conditions:

List B. At a temperature of 15-30 °, in a dry, protected from light, out of reach of children.

Shelf life:

3 years. Do not use after the date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N015916 / 01

Date of registration:06.10.2009

The owner of the registration certificate:Apothec Inc.Apothec Inc. Canada

Manufacturer: & nbsp

APOTEX, Inc. Canada

Information update date: & nbsp10.09.2017

Illustrated instructions

Instructions

Apo-Fluoxetine (Fluoxetine-Apo)