Fludac

General information

Fludac is an antidepressant that belongs to the class of selective serotonin reuptake inhibitors (SSRIs). The drug is used to treat depressive disorders, anxiety states and some other psychoemotional disorders. The main active ingredient, fluoxetine, helps to normalize serotonin levels in the brain, which helps to improve mood, reduce anxiety and restore emotional balance. Fludac is characterized by a relatively mild side effect profile compared to other antidepressants.

Trade name

Fludac

International Nonproprietary Name (INN)

Fluoxetine

Form of release

The drug is available in the following forms:

• Capsules: 10 mg, 20 mg;
• Water-soluble tablets: 20 mg;
• Cyrup for oral administration: 20 mg/5 ml.

Composition

Acting substance: fluoxetine hydrochloride.

Auxiliary components depend on the form of release:

• Capsules: lactose monohydrate, corn starch, magnesium stearate, colloidal silicon dioxide; capsule shell contains gelatin, titanium dioxide, dyes (eg, indigo carmine for 20 mg dosage);
• Tablets: mannitol, microcrystalline cellulose, flavorings (e.g., mint), sodium saccharinate;
• Syrup: sucrose, glycerin, sorbitol, flavorings (e.g., orange), purified water.

The capsules have an opaque shell that varies in color: white for 10 mg and a combination of white and green for 20 mg. The tablets are white, flat, with a groove for division.

Pharmacologic properties

Pharmacodynamics

Fluoxetine, the active ingredient in Fludaca, acts as a selective serotonin reuptake inhibitor. It blocks the serotonin transporter (SERT) in presynaptic neurons, which increases the concentration of this neurotransmitter in the synaptic cleft. Increased serotonin levels enhance signal transduction in serotoninergic pathways in the brain, resulting in improved mood, reduced anxiety, and normalization of the emotional background. Unlike tricyclic antidepressants, fluoxetine has minimal effects on norepinephrine and dopamine reuptake and virtually no anticholinergic activity, which reduces the risk of side effects such as dry mouth or sedation.

The therapeutic effect of Fludac develops gradually, usually after 1-4 weeks of regular use, although some patients notice improvement as early as the first week. The drug also has a weak stimulant effect, which makes it preferable for patients with apathy or lethargy as part of depression. In addition, fluoxetine can modulate appetite, which is used in the treatment of eating disorders.

Pharmacokinetics

Absorption

Fluoxetine is well absorbed from the gastrointestinal tract after oral administration, with a bioavailability of approximately 60-80%. The maximum concentration in plasma (Cmax) is reached after 6-8 hours. Food intake slows down absorption, but does not affect the overall degree of absorption, which allows taking the drug independently of meals.

Distribution

Fluoxetine is actively distributed in tissues, including the central nervous system, with a volume of distribution of 20-45 l/kg. Binding to plasma proteins (mainly albumin) reaches 94-95%. The drug penetrates the blood-brain barrier, providing therapeutic action in the brain. The active metabolite, norfluoxetine, is also involved in the pharmacological effect.

Metabolism

Metabolism of fluoxetine occurs in the liver with the participation of cytochrome P450 isoenzymes, mainly CYP2D6. The main pathway is demethylation to form norfluoxetine, which has similar pharmacological activity, but longer half-life. The process of metabolism is subject to genetic variability, which may affect the rate of transformation and accumulation of the drug in different patients.

Excretion

The half-life of fluoxetine is 1-3 days, norfluoxetine - 4-16 days, which provides a prolonged therapeutic effect after discontinuation. Excreted mainly by the kidneys (60-80%) in the form of metabolites, about 10% - through the intestine. Complete excretion from the body may take up to 4-6 weeks. In case of liver or kidney dysfunction, excretion is slowed down, which requires dosage adjustment.

Indications for use

Fludac is used for the treatment of the following diseases and conditions:

• Major depressive disorder;
• Obsessive-compulsive disorder (OCD);
• Panic disorder (with or without agoraphobia);
• Bulimia (to control bouts of overeating);
• Premenstrual Dysphoric Disorder (PMDD);
• Generalized anxiety disorder (in some cases).

The drug is effective both in monotherapy and in combination with psychotherapy or other medications.

Contraindications

The use of Fludaca is prohibited in the following conditions:

• Hypersensitivity to fluoxetine or other components of the drug;
• Simultaneous administration of monoamine oxidase inhibitors (MAOIs) - an interval of at least 14 days after their withdrawal is required;
• Severe renal insufficiency (creatinine clearance less than 10 ml/min);
• Severe hepatic impairment;
• Epilepsy or history of seizures (uncontrolled);
• Manic phase of bipolar disorder;
• Pregnancy and breastfeeding (unless absolutely necessary);
• Age less than 8 years (for any indication).

Method of administration and dosage

How to take

Fludak is taken orally, drinking water (about 100 ml). Capsules are swallowed whole, without chewing, dissolvable tablets dissolve in a small amount of water, syrup is measured with a dosing spoon. The drug can be taken independently of meals, preferably in the morning because of the possible stimulant effect. Regularity of administration is important to achieve a stable concentration in the blood.

Dosages

Adults

• Depression: 20 mg/day in the morning, if necessary up to 60 mg/day (in 1-2 doses);
• OCP: 20-60 mg/day, start with 20 mg;
• Bulimia: 60 mg/day (in 1-3 doses);
• Panic Disorder: 10 mg/day for 1 week, then 20-40 mg/day;
• PMDD: 20 mg/day during the period of symptoms.

Children

• Depression and OCD (8-18 years of age): 10 mg/day, up to 20 mg/day if needed;
• Maximum dose: 0.5 mg/kg/day, but not more than 60 mg.

Dose adjustment

• Hepatic insufficiency: dose reduction by 50% or administration every other day;
• Rnal insufficiency: at clearance of 10-30 ml/min - decrease by 25-50%, less than 10 ml/min - contraindicated;
• Elderly patients: initial dose - 10 mg/day, maximum 40 mg/day;
• Drug withdrawal: gradual dose reduction by 10 mg every 1-2 weeks to prevent withdrawal syndrome.

Side effects

The following adverse reactions may occur while taking Fludaca:

• Nervous system: insomnia, anxiety, headache, tremor;
• Gastrointestinal tract: nausea, diarrhea, decreased appetite, dry mouth;
• Cardiovascular system: palpitations, rarely - prolongation of the QT interval;
• Skin: sweating, rash, itching;
• Reproductive system: decreased libido, ejaculation disorders;
• General: weakness, weight loss.

Side effects are usually pronounced in the first weeks and decrease with time.

Overdose

Symptoms

Overdose is manifested by nausea, vomiting, convulsions, tachycardia, somnolence, in severe cases - serotonin syndrome (hyperthermia, confusion, muscle rigidity). The critical dose is above 500 mg.

First aid measures

• Gastric lavage (within 1 hour after ingestion);
• Take activated charcoal;
• ECG and respiratory control, symptomatic therapy;
• In serotonin syndrome - administration of benzodiazepines or cyproheptadine.

Hemodialysis is ineffective due to the large volume of distribution.

Interaction with other drugs

Influence on the effect of other drugs

• Increases the effect of triptans, tramadol (risk of serotonin syndrome);
• Enhances the concentration of tricyclic antidepressants and phenytoin;
• Decreases the effectiveness of codeine (inhibition of CYP2D6);
• increases the risk of bleeding when taking NSAIDs or warfarin.

Compatibility with alcohol and food

Alcohol increases side effects (drowsiness, anxiety), its use is not recommended. Food does not affect efficacy, but fatty foods may slow absorption.

Special Instructions

Use in pregnancy and breastfeeding

Fludac is used in pregnancy only if absolutely necessary (risk of fetal retardation). It penetrates into breast milk, therefore breastfeeding is not recommended.

Effect on driving and mechanisms

The drug may cause drowsiness or anxiety, driving is not recommended in the first weeks of treatment.

Particularities of use in elderly people and children

Elderly patients are prescribed reduced doses due to slow metabolism. In children under 8 years of age, the drug is not used, over 8 years of age - only on strict indications.

Comparison of Fludac and Prozac