Citol (Tablets) Instructions for Use

Marketing Authorization Holder

NANOLEK LLC (Russia)

ATC Code

N06AB04 (Citalopram)

Active Substance

Citalopram (Rec.INN registered by WHO)

Dosage Forms

	Citol	Film-coated tablets, 20 mg: 28 pcs.
		Film-coated tablets, 40 mg: 28 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, elliptical, with the company logo on one side and a score line on the other.

Excipients: corn starch, lactose, polyvinylpyrrolidone, Avicel PH 200, magnesium stearate, hydroxypropyl methylcellulose, polyethylene glycol 400, titanium dioxide.

14 pcs. – blisters (2) – cardboard packs.

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

An antidepressant from the group of selective serotonin reuptake inhibitors.

Citol has a pronounced ability to inhibit serotonin reuptake. It practically does not bind to histamine and muscarinic receptors, as well as adrenoreceptors. Citol 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.

Citol practically does not affect the cardiac conduction system and blood pressure, hematological parameters, liver and kidney function, and does not cause weight gain.

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 less than 80%. It is present in plasma unchanged. When taken in doses of 10-60 mg/day, the pharmacokinetic parameters are characterized by 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 elderly patients, the AUC and T_1/2 of citalopram increase.

Indications

• Depressions of various etiologies.

ICD codes

Dosage Regimen

Citol is prescribed orally once a day at any time of the day, regardless of meals.

The initial daily dose is 20 mg. If necessary, the dose can be increased. The maximum daily dose is 60 mg.

For elderly patients 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 a maximum of 40 mg.

For mild to moderate chronic renal failure dose adjustment is not required.

For patients with hepatic impairment the drug is prescribed in minimal therapeutic doses.

Adverse Reactions

From the nervous system rarely – seizures, asthenia, increased fatigue, drowsiness or insomnia, anxiety, tremor, impaired concentration, agitation, amnesia, apathy, extrapyramidal effects, depressed mood, aggressive behavior, hallucinations, depersonalization, confusion, emotional lability, euphoria, mania, panic behavior, suicide attempts, paranoid reaction, psychosis, serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, tremor, increased sweating, agitation, uncontrolled behavior), catatonic reactions, drug dependence.

From the digestive system rarely – dry mouth, nausea, vomiting, hypersalivation, flatulence, diarrhea, abdominal pain, anorexia, gastritis, gastroenteritis, stomatitis, gingivitis, dysphagia, esophagitis, increased activity of liver transaminases, alkaline phosphatase; in isolated cases – colitis, gastric and duodenal ulcers, cholecystitis, gastroesophageal reflux, glossitis, jaundice, diverticulitis, hiccups.

From the cardiovascular system often – bradycardia, postural hypotension, decreased blood pressure; rarely – arterial hypertension, tachycardia, edema, angina pectoris, extrasystole, arrhythmia, heart failure, myocardial infarction; in isolated cases – transient ischemic attacks, phlebitis.

From the hematopoietic system thrombocytopenia, bleeding, purpura, blood clotting disorders.

From the respiratory system often – cough; rarely – rhinitis, sinusitis, dyspnea, bronchitis, shortness of breath, pneumonia; in isolated cases – asthma, bronchospasm, laryngitis.

From the musculoskeletal system: rarely – arthritis, muscle weakness; in isolated cases – bursitis, osteoarthritis.

From the senses rarely – mydriasis, accommodation paresis, taste disturbance.

From the reproductive system often – sexual dysfunction (impaired ejaculation, decreased libido, impotence), menstrual cycle disorders; rarely – vaginal bleeding.

From the endocrine system rarely – mastodynia, galactorrhea; in isolated cases – hypothyroidism, gynecomastia.

From the urinary system often – dysuria, polyuria; in isolated cases – hematuria, oliguria, pyelonephritis, kidney pain.

Allergic reactions often – skin rash; rarely – urticaria.

Dermatological reactions: often – itching, hair loss; rarely – increased photosensitivity, acne, eczema, dermatitis, psoriasis, epidermal necrolysis, alopecia; in isolated cases – hypertrichosis, decreased sweating, keratitis, cellulitis, anal itching.

Other rarely – hyponatremia, yawning, teeth grinding, increase or decrease in body weight, hemorrhoids.

Adverse reactions are usually noted in the first 2 weeks, are mild, transient in nature and usually weaken as the patient’s condition improves.

Contraindications

• Concomitant use with MAO inhibitors (including the period within 14 days after their discontinuation), sumatriptan and other serotonergic drugs;
• Childhood (safety and efficacy of use have not been established);
• Hypersensitivity to the components of the drug.

With caution the drug should be prescribed for hepatic and/or renal insufficiency, for seizures (including history), for elderly patients, during pregnancy and breastfeeding.

Use in Pregnancy and Lactation

Citalopram should not be prescribed during pregnancy and lactation (breastfeeding) except in cases where the potential benefit to the mother outweighs the possible risk to the fetus or child.

It should be borne in mind that when prescribing Citol during breastfeeding, infants may develop drowsiness, decreased sucking reflex, and weight loss.

Use in Hepatic Impairment

With caution the drug should be prescribed for hepatic insufficiency.

Use in Renal Impairment

Patients with mild to moderate chronic renal failure the drug is prescribed in usual doses.

Pediatric Use

Contraindication: childhood (safety and efficacy of use have not been established).

Geriatric Use

For elderly patients 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 a maximum of 40 mg.

Special Precautions

There is very little clinical experience with the use of Citol during electroconvulsive therapy.

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

Treatment with MAO inhibitors can be started no earlier than 7 days after discontinuation of citalopram.

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

Effect on ability to drive vehicles and mechanisms

During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms dizziness, drowsiness, dysarthria, sinus tachycardia, nodal rhythm, increased sweating, vomiting, cyanosis, tremor, amnesia, confusion, QT interval prolongation, torsades de pointes arrhythmia, ventricular arrhythmia, rhabdomyolysis, seizures, coma, EEG changes, pulmonary hyperventilation.

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

Drug Interactions

With simultaneous use, Citol 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 CYP2D6 isoenzyme, and therefore weakly interacts with drugs that are metabolized with the participation of citalopram.

With simultaneous use with MAO inhibitors, the development of a hypertensive crisis (serotonin syndrome) is possible.

With simultaneous use, cimetidine increases the concentration in the blood and enhances the effect of citalopram.

With simultaneous use with warfarin, prothrombin time increases by 5%.

Storage Conditions

The drug should be stored out of the reach of children, at room 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.