Fluoxetine, 10 mg capsules 20 pcs

Pharmacotherapeutic group

Antidepressant

ATX code: N06AB03

Pharmacodynamics:

Blocks selectively the neuronal reuptake of serotonin (5NT) in the synapses of neurons of the central nervous system. Inhibition of serotonin reuptake leads to increased concentration of this neurotransmitter in the synaptic cleft enhances and prolongs its effect on postsynaptic receptor sites. In therapeutic doses, fluoxetine blocks serotonin uptake by human platelets. It is a weak antagonist of muscarinic histamine H1 adrenergic a1 and a2 receptors has little effect on dopamine reuptake. Causes reduction of obsessive-compulsive disorders as well as decreased appetite, which may lead to weight loss. It does not cause a sedative effect. It has practically no effect on cardio-vascular and other systems functions when administered in medium therapeutic doses.

Pharmacokinetics:

When taken orally the drug is well absorbed from the gastro-intestinal tract (up to 95% of the dose taken). Food use insignificantly inhibits absorption of fluoxetine. Maximum plasma concentrations are reached after 6-8 hours. Bioavailability of fluoxetine after oral administration is more than 60%. The drug accumulates well in tissues easily penetrates through the blood-brain barrier and binds to plasma proteins by more than 90%. The drug is metabolized in the liver by demethylation to the active metabolite norfluoxetine and a number of unidentified metabolites. Renal clearance of fluoxetine is 94-704 ml/min for norfluoxetine 60-336 ml/min. About 12% of the drug is excreted through the gastrointestinal tract. The half-life of fluoxetine is about 2-3 days for norfluoxetine – 7-9 days. In patients with hepatic impairment, the half-life of fluoxetine and norfluoxetine is prolonged. The drug is excreted with breast milk (up to 25% of the serum concentration).

Indications

Depressions of various etiologies.

– Obsessive-compulsive disorders.

– Bulimic neurosis.

– Premenstrual dysphoric disorder.

Active ingredient

Fluoxetine

Composition

Each capsule contains:

The active ingredient fluoxetine hydrochloride 11.2 mg in terms of fluoxetine 10 mg.

Excipients: microcrystalline cellulose – 153.0 mg, pregelatinized starch – 14.3 mg, magnesium stearate – 1.5 mg.

Capsule composition 10 mg: titanium dioxide, indigo carmine, iron oxide yellow dye, gelatin.

How to take, the dosage

The drug is taken orally.

Depression. The initial dose is 20 mg once a day in the morning, regardless of meals. If necessary and tolerated, the dose may be increased to 40-60 mg per day (20 mg per week) divided into 2-3 doses. The maximum daily dose is 80 mg. The therapeutic effect of the drug is established 1-4 weeks after the start of treatment in some patients it may be achieved later.

Obsessive-compulsive disorders – the recommended dose is 20-60 mg per day. In bulimia nervosa the recommended dose is 60 mg per day divided into 2-3 doses.

Premenstrual dysphoric disorder: the recommended dose is 20 mg per day.

In elderly patients the recommended initial daily dose is 20 mg. In patients with liver and renal function disorders it is recommended to use lower doses and prolongation of the interval between doses.

Interaction

Increases the effects of alprazolam diazepam ethyl alcohol and hypoglycemic drugs (drugs).

Increases the plasma concentration of phenytoin tricyclic antidepressants maprotiline trazodone by 2 times (the dose of tricyclic antidepressants should be reduced by 50% when used simultaneously).

Increased lithium concentration is possible – the risk of toxic effects of lithium. These drugs should be used simultaneously with caution recommended frequent determination of serum lithium concentration.

Against the background of electroconvulsive therapy may develop prolonged epileptic seizures.

Tryptophan increases serotonergic properties of fluoxetine (increased agitation motor disturbances of the gastrointestinal tract).

MAO inhibitors increase the risk of serotonin syndrome (hyperthermia chills increased sweating myoclonus hyperreflexia tremor diarrhea movement coordination disorders autonomic lability psychomotor agitation delirium disorders depression of consciousness up to coma).

Drugs with depressant effect on the central nervous system increase the risk of side effects and increased depressant effect on the central nervous system.

Concurrent use with drugs with high degree of binding to proteins, especially with anticoagulants and digitoxin may increase plasma concentration of free (unbound) drugs and increase the risk of adverse effects. Fluoxetine increases the effect of hypoglycemic drugs and anticoagulants.

Special Instructions

Anorexigenic effects (progressive weight loss is possible) should be considered when treating patients with weight deficiency.

In patients with diabetes mellitus, administration of fluoxetine increases the risk of hypoglycemia and hyperglycemia – when it is canceled. In this regard, the dose of insulin and/or any other hypoglycemic drugs used orally should be adjusted. Patients should be under medical supervision until a significant improvement in treatment.

During the treatment it is necessary to refrain from alcohol intake and potentially dangerous activities requiring increased attention and rapid mental and motor reactions.

After using MAO inhibitors fluoxetine may be administered not earlier than 14 days. MAO inhibitors and/or thioridazine should not be used earlier than 5 weeks after fluoxetine withdrawal.

If seizures occur while taking fluoxetine, the drug should be stopped. In case of liver diseases and in the elderly, treatment should be started with minimal doses.

Contraindications

Hypersensitivity concomitant use of MAO inhibitors (and for 14 days after their withdrawal) thioridazine (and for 5 weeks after fluoxetine withdrawal) pimozide severe renal impairment (creatinine clearance less than 10 ml/min) and liver pregnancy lactation age under 18 years.
With caution: Diabetes mellitus epilepsy seizure disorders (including anamnesis) suicidal tendencies.

Side effects

Central nervous system: increased suicidal tendencies anxiety headache tremor agitation increased irritability sleep disorders dizziness somnolence asthenic disorders decreased libido manic and seizure disorders.

Gastrointestinal tract: decreased appetite impaired taste nausea vomiting dry mouth or hypersalivation diarrhea.

Urinary system: incontinence or urinary retention dysmenorrhea vaginitis decreased libido sexual dysfunction in men (delayed ejaculation).

Rarely allergic reactions in the form of skin rash itching chills urticaria body temperature increase muscle and joint pain (possible use
antihistamines and steroids) hyponatremia orthostatic hypotension tachycardia visual acuity disorders.

Other: increased sweating tachycardia systemic pulmonary renal or hepatic disorders vasculitis.

Anorexia and weight loss are possible.

These side effects occur more frequently at the beginning of fluoxetine therapy or when increasing the drug dose.

Overdose

Symptoms: agitation manic and seizure disorders heart rhythm disorders tachycardia nausea vomiting.

Treatment: no specific antagonists to fluoxetine have been found. Symptomatic therapy gastric lavage with administration of activated charcoal in sudorags – diazepam maintenance of respiration cardiac activity body temperature.

Similarities

Prozac, Fluoxetine, Fluoxetine Lannacher