Citalon (Tablets) Instructions for Use

ATC Code

N06AB04 (Citalopram)

Active Substance

Citalopram

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

Antidepressant. The mechanism of action is associated with the selective blockade of the neuronal reuptake of serotonin in the synapses of the CNS neurons with a minimal effect on the reuptake of norepinephrine and dopamine.

It has no or negligible ability to bind to a number of receptors, including serotonin HT_1A-, 5HT_2A-, dopamine D₁– and D₂-, α₁-, α₂– and β-adrenergic receptors, histamine H₁-receptors, GABA receptors, m-cholinergic receptors, and benzodiazepine receptors.

It helps improve mood, relieves anxiety, reduces feelings of fear and tension, eliminates dysphoria, reduces obsessive-compulsive states, and practically does not cause a sedative effect.

A stable clinical effect develops after 7-10 days of regular administration.

Pharmacokinetics

After oral administration, C_max of citalopram in plasma is reached in 2-4 hours. Oral bioavailability is about 80%.

Changes in plasma citalopram concentration are linear. C_ss in plasma is established after 1-2 weeks of therapy.

Plasma protein binding is less than 80%.

In blood plasma, Citalopram is present mainly in unchanged form. It is metabolized by demethylation, deamination, and oxidation.

T_1/2 is 1.5 days.

It is excreted by the kidneys and through the intestines.

Indications

Depressions of various origins (endogenous and exogenous); affective (depressive, bipolar, dysthymic) disorders; mixed anxiety-depressive disorders; anxiety-phobic disorders (phobic, panic, obsessive-compulsive, generalized anxiety, post-traumatic stress disorders); somatization disorder; psychosomatic diseases with autonomic dysfunction (including autonomic dysfunction of the cardiovascular system, respiratory system, gastrointestinal tract, genitourinary system); vascular dementias with depressive symptoms; depressive disorders in women (premenstrual dysphoria, depression in pregnancy, postpartum depression, premenopausal depression); eating disorders (anorexia, bulimia); depression in alcoholism; depression in the elderly.

ICD codes

Dosage Regimen

Take tablets orally, once daily, with or without food.

For adult patients, initiate therapy at a dose of 10 mg to 20 mg daily.

Based on individual therapeutic response and tolerability, increase the dose gradually.

The maximum recommended daily dose is 60 mg for most adult indications.

For elderly patients over 65 years of age, initiate treatment at 20 mg daily.

If necessary, the dose for elderly patients may be increased to a maximum of 40 mg daily.

Dose adjustments should be made at intervals of at least one week.

Administer the total daily dose as a single administration.

For long-term treatment, continue therapy for a minimum of 6 months after symptom remission is achieved to prevent relapse.

Discontinuation of therapy should be accomplished through a gradual dose reduction over several weeks to minimize potential withdrawal symptoms.

Adverse Reactions

From the nervous system: dizziness, headache, tremor, drowsiness, insomnia, agitation, nervousness, migraine, paresthesia; sleep disturbance, impaired concentration, amnesia, anxiety, decreased libido, increased appetite, anorexia, apathy, suicide attempts, confusion of thoughts, asthenia, mood changes, aggressive behavior, emotional lability, agitation, mania, hypomania, panic behavior, paranoid reaction, psychosis, excessive fatigue, restlessness, extrapyramidal disorders, convulsions, euphoria, serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, increased sweating, uncontrolled behavior), hallucinations, depersonalization; in exceptional cases when used in high doses – convulsive seizures.

From the cardiovascular system: atrial flutter, tachycardia, bradycardia, orthostatic hypotension, increase or decrease in blood pressure, supraventricular and ventricular arrhythmias.

From the digestive system: nausea, dry mouth, constipation, diarrhea, dyspepsia, vomiting, abdominal pain, flatulence, anorexia, increased salivation, increased activity of liver enzymes.

From the urinary system: frequent urination, polyuria.

Metabolic disorders: decrease or increase in body weight, hyponatremia, hyperthermia.

From the respiratory system: rhinitis, sinusitis, cough, shortness of breath.

From the reproductive system: ejaculation disorders, increased or decreased libido, female anorgasmia, dysmenorrhea, impotence, menstrual cycle disorders, galactorrhea.

From the skin: increased sweating, rash, itching, photosensitivity, epidermal necrolysis, angioedema.

From the sensory organs: accommodation disturbance, visual impairment, mydriasis, taste disturbance, tinnitus.

From the musculoskeletal system: myalgia, arthralgia.

From the blood coagulation system: rarely – development of bleeding (for example, bleeding due to gynecological causes, gastrointestinal bleeding, ecchymoses), thrombocytopenia.

Other: asthenia, fatigue, allergic reactions, fainting, malaise, mastodynia, yawning, teeth grinding, anaphylactoid reaction.

Contraindications

Hypersensitivity to citalopram.

Use in Pregnancy and Lactation

The safety of using citalopram during pregnancy and lactation has not been established. Use is justified only in cases where the potential benefit of therapy for the mother outweighs the possible risk to the fetus and child.

In experimental studies, no teratogenic effect or any effect of citalopram on reproductive function and perinatal development of the fetus was revealed.

Use in Hepatic Impairment

In patients with hepatic insufficiency, Citalopram should be used in minimal doses.

Use in Renal Impairment

In mild to moderate renal impairment, no adjustment of the citalopram dosage regimen is required; information on use in severe renal impairment is not available.

Pediatric Use

The efficacy and safety of using citalopram in children have not been established.

Special Precautions

In patients with hepatic insufficiency, Citalopram should be used in minimal doses.

In mild to moderate renal impairment, no adjustment of the citalopram dosage regimen is required; information on use in severe renal impairment is not available.

When using citalopram, a slight decrease in heart rate is possible, which has no clinical significance, however, in patients with initially reduced heart rate, Citalopram may cause more pronounced bradycardia.

Citalopram should not be used simultaneously with MAO inhibitors.

Citalopram should be used with caution in maximum doses while taking cimetidine in high doses.

Use in pediatrics

The efficacy and safety of using citalopram in children have not been established.

Effect on the ability to drive vehicles and operate machinery

It should be borne in mind that patients with depression often have a reduced ability to concentrate, which may be aggravated by the use of psychotropic drugs.

Drug Interactions

With simultaneous use with MAO inhibitors, the development of a hypertensive crisis (serotonin syndrome) is possible. Therefore, simultaneous use of citalopram with MAO inhibitors and within 14 days after their discontinuation is contraindicated.

It inhibits the CYP2D6 isoenzyme to a very small extent, therefore it does not interact with drugs metabolized by this isoenzyme.

However, a decrease in the plasma concentration of citalopram due to increased metabolism as a result of induction of liver microsomal enzymes by carbamazepine during their simultaneous use cannot be ruled out.

With simultaneous use of cimetidine, a moderate increase in C_ss of citalopram in blood plasma is possible.

The effects of sumatriptan and other serotonergic agents may be enhanced by citalopram when used simultaneously.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.