Citalorin (Tablets) Instructions for Use

Marketing Authorization Holder

Shchelkovsky Vitamin Plant, JSC (Russia)

ATC Code

N06AB04 (Citalopram)

Active Substance

Citalopram

Dosage Forms

	Citalorin	Film-coated tablets, 10 mg: 10 or 20 pcs.
		Film-coated tablets, 20 mg: 10 or 20 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, biconvex.

Excipients: lactose, microcrystalline cellulose, potato starch, copovidone, magnesium stearate, Opadry II film coating.

10 pcs. – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

An antidepressant from the group of selective serotonin reuptake inhibitors.

Citalorin has a pronounced ability to inhibit serotonin reuptake. It practically does not bind to histamine and muscarinic receptors, as well as adrenoreceptors. Citalorin inhibits the CYP2D6 isoenzyme to a very small extent and, therefore, does not interact with drugs metabolized by this enzyme. Thus, side effects and toxic effects are manifested to a much lesser extent.

The antidepressant effect usually develops after 2-4 weeks of treatment.

Citalorin practically does not affect the cardiac conduction system and blood pressure, hematological parameters, liver and kidney function, and does not cause an increase in body weight.

Citalorin does not impair cognitive functions and does not cause a sedative effect.

Pharmacokinetics

Absorption

After oral administration, the bioavailability of citalopram is about 80% and is practically independent of food intake. C_max in plasma is reached 2-4 hours after administration.

Distribution

Plasma protein binding is 80%. It is present in plasma in an unchanged form. When taking doses of 10-60 mg/day, the pharmacokinetic parameters have a linear dependence. V_d – 12 l/kg. C_ss with daily single-dose administration is established after 7-14 days. Penetrates into breast milk.

Metabolism

It is metabolized by demethylation, deamination and oxidation with the participation of CYP3A4 and CYP2C19 isoenzymes to form less pharmacologically active metabolites.

Excretion

T_1/2 is 1.5 days. Excreted in urine and feces.

Pharmacokinetics in special clinical cases

In patients over 65 years of age, a longer T_1/2 (1.5-3.75 days) and lower clearance values (0.08-0.3 l/min) are observed. The concentrations observed at steady state in elderly patients were almost twice as high as those observed in younger patients receiving the same dose.

In patients with reduced liver function, Citalopram is eliminated more slowly. T_{1/2 and} C_ss of citalopram in plasma are almost 2 times higher compared to patients with normal liver function after administration of the same dose.

The elimination of citalopram is slowed in patients with mild to moderate renal impairment without a significant effect on pharmacokinetics. Currently, experience in treating patients with severe renal failure (creatinine clearance less than 20 ml/min) is insufficient.

Indications

• Treatment of depressive disorders and prevention of relapses;
• Treatment of panic disorders with or without agoraphobia;
• Treatment of obsessive-compulsive disorder.

ICD codes

Dosage Regimen

Citalorin is prescribed orally once a day at any time of the day, either with meals or on an empty stomach.

For depression, the recommended daily dose is 20 mg. Depending on the individual patient’s response to treatment and the severity of the disease, the daily dose can be increased to 60 mg.

For panic disorders, it is recommended to prescribe 10 mg/day during the first week of treatment, after which the dose is increased to 20 mg/day. Depending on the individual patient’s response to treatment and the severity of the disease, the dose can be increased to 60 mg.

For obsessive-compulsive disorders, the recommended daily dose is 20 mg. Depending on the individual patient’s response to treatment, the dose can be increased by 20 mg to a maximum of 60 mg/day.

For patients aged 65 years and older, the recommended initial dose may be increased to 40 mg/day.

For patients with mild to moderate renal impairment, the drug is prescribed in usual doses.

There is no information on the treatment of patients with severe renal impairment (creatinine clearance less than 20 ml/min) with Citalorin.

For patients with impaired liver function, no more than 30 mg/day should be prescribed.

The antidepressant effect of the drug is usually observed after 2-4 weeks of treatment. Treatment with antidepressants is symptomatic and should be carried out for a long time. Usually, to prevent relapse, treatment must be carried out for 6 months or even a longer period of time.

For periodic (recurrent) depression, maintenance treatment should be carried out for several years to prevent the onset of subsequent phases of the disease. In case of completion of treatment, the drug Citalorin must be discontinued gradually over several weeks.

In the treatment of panic disorder, the maximum effect of Citalorin is observed after 3 months of treatment. This effect persists throughout the entire period of maintenance therapy.

In the treatment of obsessive-compulsive disorder, the effect of the drug appears after 2-4 weeks of treatment; with further continuation of treatment, further improvement may be observed.

Adverse Reactions

From the nervous system rarely – asthenia, increased fatigue, drowsiness or insomnia, anxiety, tremor, agitation, amnesia, apathy, extrapyramidal effects, mood changes, aggressive behavior, hallucinations, depersonalization, emotional lability, euphoria, mania, hypomania, panic behavior, paranoid reaction, psychosis, serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, unusual fatigue, tremor, increased sweating, agitation, uncontrolled behavior).

From the digestive system rarely – dry mouth, nausea, vomiting, hypersalivation, flatulence, diarrhea, abdominal pain, anorexia.

From the cardiovascular system rarely – bradycardia, decreased blood pressure, orthostatic hypotension, arrhythmia.

From the hematopoietic system rarely – thrombocytopenia, bleeding.

From the sensory organs rarely – mydriasis, accommodation paresis, taste disturbance.

From the reproductive system sexual dysfunction (impaired ejaculation, decreased libido, impotence), menstrual irregularities, mastodynia, galactorrhea.

From the urinary system urination disorder, polyuria.

Allergic reactions skin rash; rarely – epidermal necrolysis.

Other rarely – sinusitis, hyperthermia, hyponatremia, arthralgia, myalgia, yawning, teeth grinding, increase or decrease in body weight.

Contraindications

• Childhood;
• Hypersensitivity to citalopram or other components of the drug.

The drug should not be used in combination with MAO inhibitors, as well as within 14 days after their discontinuation. Treatment with MAO inhibitors can be started no earlier than 7 days after discontinuation of Citalorin.

With caution, the drug should be prescribed for insufficient liver and/or kidney function, with a history of seizures, and to elderly patients.

Use in Pregnancy and Lactation

Citalorin should not be prescribed during pregnancy and lactation (breastfeeding), unless the potential benefit to the mother outweighs the possible risk to the fetus or child, because the safety of the drug during these periods in humans has not been established.

It should be taken into account that when prescribing Citalorin during breastfeeding, infants may develop drowsiness, decreased sucking reflex, and weight loss.

In experimental studies, no teratogenic effects, effects on reproductive function and perinatal development of offspring were found.

Use in Hepatic Impairment

For patients with impaired liver function, no more than 30 mg/day should be prescribed.

Use in Renal Impairment

For patients with mild to moderate renal impairment, the drug is prescribed in usual doses.

There is no information on the treatment of patients with severe renal impairment (creatinine clearance less than 20 ml/min) with Citalorin.

Pediatric Use

The drug is contraindicated in childhood.

Geriatric Use

The drug should be prescribed with caution to elderly patients.

In elderly patients, a dose reduction of Citalorin is required.

Special Precautions

If a manic state develops, the drug should be discontinued.

Patients with drug dependence (including history) require observation and control over the use of the drug.

In elderly patients, a dose reduction of Citalorin is required.

Citalorin does not affect intellectual and psychomotor functions and abilities. Nevertheless, it is recommended to inform patients taking psychotropic drugs that their ability to concentrate and pay attention may be impaired to some extent as a result of their illness or the action of the drugs taken, or as a result of a combination of these two factors.

Overdose

Symptoms nausea, dizziness, drowsiness, dysarthria, sinus tachycardia, nodal rhythm, increased sweating, cyanosis, tremor, amnesia, confusion, heart rhythm and conduction disturbances (QT interval prolongation), rhabdomyolysis, convulsions, coma.

Treatment gastric lavage. Symptomatic and supportive therapy is carried out. There is no specific antidote.

Drug Interactions

With simultaneous use, Citalorin enhances the effect of sumatriptan and other serotonergic drugs.

It does not affect the action of ethanol, lithium preparations, benzodiazepines, antipsychotic drugs (neuroleptics), opioid analgesics, beta-blockers, phenothiazines, tricyclic antidepressants, antihistamines and antihypertensive drugs.

It slightly inhibits the CYPIID6 isoenzyme, and therefore weakly interacts with drugs that are metabolized with the participation of citalopram.

With simultaneous use with MAO inhibitors, a hypertensive crisis (serotonin syndrome) may develop. With simultaneous use, cimetidine increases the concentration in the blood and enhances the effect of Citalorin.

When prescribed simultaneously with warfarin, prothrombin time increases by 5%.

Storage Conditions

List B. The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

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.