Lexapro

General information

Lexapro is an antidepressant from the group of selective serotonin reuptake inhibitors (SSRIs) intended for the treatment of depressive and anxiety disorders. The main active substance - escitalopram - helps to increase the level of serotonin in the brain, which helps to improve mood, reduce anxiety and restore emotional stability. The drug is characterized by high selectivity and fewer side effects than other antidepressants, which makes it a popular choice in psychiatric practice.

Trade name

Lexapro

International Nonproprietary Name (INN)

Escitalopram

Form of release

The drug is available in the following forms:

• Film-coated tablets: 5 mg, 10 mg, 20 mg;
• Internal solution: 10 mg/mL (in some countries).

Constitution

Acting substance: escitalopram oxalate.

Auxiliary components depend on the form of release:

• Tablets: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate; shell contains hypromellose, titanium dioxide, polyethylene glycol;
• Solution: sorbitol, citric acid, sodium citrate, flavorings (e.g., mint), purified water.

The tablets are oval-shaped with a groove for division, the color is white, with dosage engraved (e.g., “10” for 10 mg). The solution is a clear liquid with a slight aroma.

Pharmacologic properties

Pharmacodynamics

Escitalopram, the active ingredient in Lexapro, is a highly selective serotonin reuptake inhibitor. It blocks the serotonin transporter (SERT) in presynaptic neurons, increasing the concentration of serotonin in the synaptic cleft. This increases serotoninergic transmission in the brain, leading to improved mood, reduced anxiety, and normalized sleep. Escitalopram is the S-enantiomer of citalopram, which provides higher selectivity and less effect on other neurotransmitters such as norepinephrine or dopamine. The drug has virtually no affinity for muscarinic, histamine, or adrenergic receptors, which minimizes anticholinergic and sedative effects.

Therapeutic effects are apparent after 2-4 weeks of regular administration, although some patients show improvement after 7-10 days. Lexapro also demonstrates efficacy in preventing recurrences of depression with long-term use. Its mild action makes it suitable for patients with a high sensitivity to the side effects of other antidepressants.

Pharmacokinetics

Absorption

Escitalopram is well absorbed from the gastrointestinal tract, with a bioavailability of about 80%. The maximum plasma concentration (Cmax) is reached 4-5 hours after administration. Food intake has no clinically significant effect on the rate or extent of absorption, which allows taking the drug at any time of the day.

Distribution

The drug is distributed in tissues with a volume of distribution of about 12-26 l/kg, penetrating the blood-brain barrier. Binding to plasma proteins (predominantly albumin) is about 56%, which is lower than that of other SSRIs and provides less competition with other drugs for protein binding.

Metabolism

Metabolism of escitalopram occurs in the liver involving the isoenzymes CYP2C19, CYP3A4, and to a lesser extent CYP2D6. The major metabolites, S-demethylcitalopram and S-didemethylcitalopram, have negligible pharmacologic activity. The process of metabolism depends in part on the genetic characteristics of the enzymatic system, which may affect the rate of processing of the drug in different patients.

Metabolism of S-demethylcitalopram

Excretion

The elimination half-life of escitalopram is 27-32 hours, which allows it to be taken once a day. It is excreted mainly by the kidneys (about 70%) in the form of metabolites, a small part (8-10%) - in unchanged form. Complete excretion takes about 7-10 days. In case of hepatic or renal dysfunction, the elimination half-life increases, requiring dosage adjustment.

Indications for use

Lexapro is used for the treatment of the following conditions:

• Major depressive disorder (including mild, moderate, and severe forms);
• Generalized anxiety disorder (GAD);
• Social anxiety disorder (sociophobia);
• Panic disorder (with or without agoraphobia);
• Prevention of depression relapses in long-term therapy.

The drug is effective for both acute treatment and maintenance therapy of psychoemotional disorders.

Contraindications

The use of Lexapro is prohibited in the following conditions:

• Hypersensitivity to escitalopram, citalopram or excipients;
• Simultaneous administration of monoamine oxidase inhibitors (MAOIs) - an interval of 14 days after their withdrawal is required;
• Congenital or acquired QT interval prolongation (e.g., long QT syndrome);
• Simultaneous administration of QT-prolonging drugs (e.g., class IA and III antiarrhythmics);
• Severe hepatic impairment;
• Age less than 12 years of age (for any indication);
• Pregnancy and breastfeeding (unless absolutely necessary).

Method of administration and dosage

How to take

Lexapro is taken orally, drinking water (about 100 ml). Tablets are swallowed whole, without chewing, the solution is measured with a dosing pipette. The drug can be taken regardless of food, preferably in the morning or evening at the same time. Regularity of administration is important to maintain stable blood levels.

Dosages

Adults

• Depression: 10 mg/day, up to 20 mg/day if needed;
• HTR: 10 mg/day, up to a maximum of 20 mg/day;
• Panic disorder: 5 mg/day for 1 week, then 10-20 mg/day;
• Sociophobia: 10 mg/day, up to 20 mg/day if needed.

Children

• Depression (12-17 years of age): 10 mg/day, up to a maximum of 20 mg/day;
• Under 12 years of age: use is not recommended.

Dose adjustment

• Hiver failure: 5-10 mg/day in mild/moderate form, contraindicated in severe form;
• Rnal insufficiency: at creatinine clearance of 10-30 ml/min - 5-10 mg/day, less than 10 ml/min - with caution;
• Elderly patients: initial dose - 5 mg/day, maximum 10 mg/day;
• Drug withdrawal: gradual dose reduction by 5 mg every 1-2 weeks to avoid withdrawal syndrome.

Side effects

The following adverse reactions are possible when taking Lexapro:

• Nervous system: headache, insomnia, drowsiness, anxiety;
• Gastrointestinal tract: nausea, diarrhea, dry mouth, decreased appetite;
• Cardiovascular system: palpitations, rarely - QT prolongation;
• Skin: increased sweating, rash;
• Reproductive system: decreased libido, erectile dysfunction;
• General: fatigue, weight gain.

Side effects are more common in the first weeks and gradually diminish.

Overdose

Symptoms

Overdose is manifested by nausea, vomiting, tremor, seizures, tachycardia, in severe cases - serotonin syndrome (hyperthermia, confusion, muscle spasms) or coma. The critical dose is above 200 mg.

First aid measures

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

Hemodialysis is ineffective due to low protein binding.

Interaction with other drugs

Influence on the effect of other drugs

• Enhances the effect of triptans, tramadol (risk of serotonin syndrome);
• Elevates the concentration of metoprolol (inhibition of CYP2D6);
• increases the risk of bleeding when taking NSAIDs or anticoagulants;
• Decreases the efficacy of tamoxifen.

Compatibility with alcohol and food

Alcohol increases drowsiness and anxiety, its use is not recommended. Food does not affect absorption.

Special Instructions

Use in pregnancy and breastfeeding

Lexapro is used in pregnancy only when strictly necessary (risk of congenital anomalies). Penetrates into breast milk, breastfeeding is not recommended.

Effects on driving and mechanisms

The drug may cause drowsiness or decreased concentration, 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 12 years of age, the drug is not used, over 12 years of age - only for depression.