Celexa 20 mg Tablets

Brand name

The trade name of the drug is Celexa. Under this name the drug is registered and available in pharmacies for medical use.

International Nonproprietary Name (INN)

The international nonproprietary name is citalopram. This name denotes the active active ingredient and is used internationally in pharmacology.

Form of release

Celexa is available as film-coated tablets with dosages of 10 mg, 20 mg and 40 mg. Tablets are packed in blisters of 10, 14 or 28 pieces, which provides convenient storage and use. The drug may also be available as an oral solution (in some countries) with a concentration of 2 mg/mL in 15 mL or 30 mL vials with a measuring pipette. Emphasis is placed on the tablet form as the most commonly used form.

Composition

Active substance

The main active ingredient is citalopram hydrobromide. One tablet contains 10 mg, 20 mg or 40 mg of citalopram hydrobromide, and 1 ml of the solution contains 2 mg.

Auxiliary Components

The tablets include substances such as lactose monohydrate, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, and a film coating of hypromellose, titanium dioxide, and polyethylene glycol. The solution contains sorbitol, glycerin, sodium citrate, citric acid, methylparaben (preservative), and purified water.

Pharmacologic Properties

Pharmacodynamics

Citalopram, the active ingredient of Celexa, is a selective serotonin reuptake inhibitor (SSRI). Its primary mechanism of action is to block serotonin transporters in the presynaptic membrane of neurons, which increases the concentration of this neurotransmitter in the synaptic cleft. Increased serotonin level enhances signal transmission in serotoninergic pathways of the brain, which leads to mood improvement, reduction of depressive symptoms and normalization of emotional background. The drug is highly selective to serotonin receptors and minimally affects the reuptake of norepinephrine and dopamine, which distinguishes it from other classes of antidepressants.

The therapeutic effect of Celexa develops gradually: the first signs of improvement are observed after 1-2 weeks of regular intake, and maximum antidepressant activity is achieved after 4-6 weeks. The drug also demonstrates the ability to reduce anxiety associated with depression without significant sedative or stimulant effects. The absence of a pronounced effect on cholinoreceptors, histamine or adrenergic receptors reduces the risk of side effects typical of tricyclic antidepressants, such as dry mouth or orthostatic hypotension.

Pharmacokinetics

Absorption

Citalopram is well absorbed from the gastrointestinal tract after oral administration. The maximum concentration in blood plasma is reached in 2-4 hours, and bioavailability is about 80%, which does not depend on food intake. This allows to take the drug at any time of the day without the need to adjust the diet.

Distribution

The drug actively binds to blood plasma proteins (80%), mainly to albumin. The volume of distribution is about 12-16 l/kg, which indicates a wide penetration into the tissues of the body, including the central nervous system. Citalopram crosses the blood-brain barrier, ensuring its action at the level of the brain.

Metabolism

Citalopram is metabolized in the liver with the participation of cytochrome P450 enzymes, mainly CYP2C19 and CYP3A4, to form two major metabolites: desmethylcitalopram and didesmethylcitalopram. These metabolites have weak pharmacologic activity and contribute minimally to the overall effect. The process of metabolism is stepwise, including demethylation and oxidation.

Excretion

The half-life of citalopram is about 33-35 hours in adults, which allows to maintain a stable concentration at a single intake per day. The drug is excreted through the kidneys (about 20% unchanged, the rest in the form of metabolites) and intestine (about 65%). Complete excretion takes 7-10 days.

Indications for Use

Celexa is prescribed for the treatment of the following conditions:

• Major depressive disorder (MDD) of varying severity;
• Anxiety disorders, including generalized anxiety disorder (as part of complex therapy);
• Panic disorder with or without agoraphobia;
• Prevention of relapses of depression in patients with a chronic course of illness;
• Depressive states associated with somatic diseases.

The drug is effective for both acute treatment and long-term maintenance therapy.

Contraindications

The use of Celexa is prohibited in:

• Hypersensitivity to citalopram or auxiliary components;
• Simultaneous intake of MAO inhibitors (14 days break is required);
• Congenital long QT syndrome or taking QT-lengthening drugs;
• Severe hepatic impairment;
• Childhood under 18 years of age (due to insufficient data);
• Pregnancy and lactation.

Prescribe with caution in epilepsy, bipolar disorder, moderate renal impairment.

Method of Administration and Dosage

How to take

Tablets Celexa taken orally, drinking water (100-150 ml), regardless of meals. The solution is measured with a pipette and diluted in a small amount of water (10-20 ml) before taking. It is recommended to take the drug at the same time of day to maintain a stable concentration in the blood.

Dosages for adults and children

Adults

The initial dose - 20 mg once a day, if necessary after 2-4 weeks increase to 40 mg/day. The maximum daily dose is 40 mg.

Children

The drug is not used in children and adolescents under 18 years of age due to lack of sufficient safety data.

Dose adjustment in certain conditions

In moderate renal insufficiency (creatinine clearance 30-60 ml/min) dose correction is not required, but in severe renal insufficiency (less than 30 ml/min) reduction to 10-20 mg/day is recommended. In hepatic insufficiency the maximum dose is 20 mg/day.

Side Effects

Possible adverse reactions include:

• Nervous system: insomnia, somnolence, headache, anxiety;
• Gastrointestinal system: nausea, dry mouth, diarrhea, decreased appetite;
• Cardiovascular system: tachycardia, QT prolongation (rare);
• Allergic reactions: rash, itching, urticaria;
• Other: sweating, decreased libido, fatigue.

Effects usually diminish after 1-2 weeks of use.

Overdose

Symptoms of overdose

Doses above 600 mg may cause nausea, vomiting, convulsions, arrhythmias, drowsiness, and in severe cases, coma.

First aid measures

Stop taking, call an ambulance. Before the arrival of the doctor, wash the stomach and give activated charcoal.

Drug Interactions

Influence on the effects of other drugs

Celexa increases the effect of tryptophan and lithium preparations, increases the risk of serotonin syndrome when combined with SSRIs or tricyclic antidepressants. Inhibitors of CYP2C19 (omeprazole) increase the concentration of citalopram.

Compatibility with alcohol and food

Alcohol increases CNS side effects. Food does not affect absorption.

Special Precautions

Use in Pregnancy and Breastfeeding

Celexa is contraindicated in pregnancy and lactation due to the risk to the fetus and penetration into milk.

Effects on driving and driving mechanisms

The drug may cause drowsiness or decreased concentration, so caution is required.

Particularities of use in the elderly and children

In the elderly, the maximum dose is 20 mg/day. Do not use in children under 18 years of age.