Suncipam (Tablets) Instructions for Use

ATC Code

N06AB10 (Escitalopram)

Active Substance

Escitalopram (Rec.INN WHO registered)

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

Antidepressant. It selectively inhibits the reuptake of serotonin; increases the concentration of the neurotransmitter in the synaptic cleft, enhances and prolongs the action of serotonin on postsynaptic receptors.

Escitalopram has virtually no binding affinity with serotonin (5-HT), dopamine (D₁ and D₂) receptors, α-adrenergic, m-cholinergic receptors, as well as with benzodiazepine and opioid receptors.

The antidepressant effect usually develops 2-4 weeks after the start of treatment. The maximum therapeutic effect in the treatment of panic disorders is achieved approximately 3 months after the start of treatment.

Pharmacokinetics

Absorption is not dependent on food intake. Bioavailability is 80%. Time to reach C_max in plasma is 4 hours. The kinetics of escitalopram are linear. C_ss is achieved after 1 week. The mean C_ss is 50 nmol/L (range 20 to 125 nmol/L) and is achieved at a dose of 10 mg/day.

Apparent V_d ranges from 12 to 26 L/kg. Plasma protein binding is 80%. It is metabolized in the liver to active demethylated and didemethylated metabolites. After multiple administration, the mean concentration of demethyl and didemethyl metabolites is 28-31% and less than 5%, respectively, of the escitalopram concentration.

The metabolism of escitalopram to form the demethylated metabolite occurs mainly with the participation of the CYP2C19, CYP3A4 and CYP2D6 isoenzymes. In individuals with weak CYP2C19 isoenzyme activity, the concentration of escitalopram may be 2 times higher than in individuals with high activity of this isoenzyme. No significant changes in drug concentration are observed with weak CYP2D6 isoenzyme activity.

T_1/2 after multiple administration is 30 hours. The main metabolites of escitalopram have a longer T_1/2. Clearance is 0.6 L/min. Escitalopram and its main metabolites are excreted by the liver and mostly by the kidneys, partially excreted in the form of glucuronides. T_1/2 and AUC are increased in elderly patients.

Indications

Depression, panic disorders (including those with agoraphobia).

ICD codes

Dosage Regimen

Tablets

Take orally, regardless of meals. Depending on the indication, a single dose is 10-20 mg/day. Maximum daily dose is 20 mg. The duration of treatment is several months. When discontinuing treatment, the dose should be gradually reduced over 1-2 weeks to avoid the occurrence of withdrawal syndrome.

For elderly patients (over 65 years), the recommended dose is 5 mg/day, maximum daily dose is 10 mg.

In case of impaired liver function, the recommended initial dose during the first 2 weeks of treatment is 5 mg/day. Depending on individual response, the dose may be increased to 10 mg/day.

For patients with weak CYP2C19 isoenzyme activity, the recommended initial dose during the first 2 weeks of treatment is 5 mg/day. Depending on individual response, the dose may be increased to 10 mg/day.

Adverse Reactions

From the nervous system dizziness, weakness, insomnia or drowsiness, convulsions, tremor, movement disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability, visual disturbances.

From the digestive system nausea, vomiting, dry oral mucosa, taste disturbances, decreased appetite, diarrhea, constipation, changes in liver function parameters.

From the cardiovascular system orthostatic hypotension.

From the endocrine system decreased secretion of ADH, galactorrhea.

From the reproductive system decreased libido, impotence, ejaculation disorder, anorgasmia (in women).

From the urinary system urinary retention.

Dermatological reactions skin rash, itching, ecchymoses, purpura, increased sweating.

Allergic reactions angioedema, anaphylactic reactions.

From metabolism hyponatremia, hyperthermia.

From the musculoskeletal system arthralgia, myalgia.

Other sinusitis, withdrawal syndrome (dizziness, headache and nausea).

Contraindications

Concomitant use of MAO inhibitors, childhood and adolescence under 15 years, pregnancy, lactation period, hypersensitivity to escitalopram.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and during the lactation (breastfeeding) period.

Use in Hepatic Impairment

Should be used with caution in liver cirrhosis.

Use in Renal Impairment

Should be used with caution in patients with renal failure (creatinine clearance less than 30 ml/min).

Pediatric Use

Contraindicated in children and adolescents under 15 years of age.

Geriatric Use

Should be used with caution in elderly patients.

Special Precautions

Should be used with caution in patients with renal failure (creatinine clearance less than 30 ml/min), hyponatremia, mania, in pharmacologically uncontrolled epilepsy, in depression with suicidal attempts, diabetes mellitus, in elderly patients, in liver cirrhosis, in patients with a tendency to bleeding, concomitantly with drugs that lower the seizure threshold, cause hyponatremia, with ethanol, with drugs metabolized with the participation of CYP2C19 isoenzymes.

Escitalopram should be prescribed only 2 weeks after discontinuation of irreversible MAO inhibitors and 24 hours after cessation of therapy with a reversible MAO inhibitor. Non-selective MAO inhibitors can be prescribed no earlier than 7 days after discontinuation of escitalopram.

In some patients with panic disorder, increased anxiety may be observed at the beginning of treatment with escitalopram, which usually disappears during the subsequent 2 weeks of treatment. To reduce the likelihood of anxiety, it is recommended to use low initial doses.

Escitalopram should be discontinued in case of development of epileptic seizures or their increased frequency in pharmacologically uncontrolled epilepsy.

If a manic state develops, Escitalopram should be discontinued.

Escitalopram can increase blood glucose concentration in diabetes mellitus, which may require adjustment of the doses of hypoglycemic drugs.

Clinical experience with escitalopram indicates a possible increased risk of suicidal attempts during the first weeks of therapy, therefore it is very important to carry out careful monitoring of patients during this period.

Hyponatremia associated with decreased ADH secretion during escitalopram administration occurs rarely and usually disappears upon its discontinuation.

If serotonin syndrome develops, Escitalopram should be immediately discontinued and symptomatic treatment should be prescribed.

Effect on ability to drive vehicles and operate machinery

During the treatment period, patients should avoid driving vehicles and other activities requiring high concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use with MAO inhibitors, the risk of developing serotonin syndrome and serious adverse reactions increases.

Concomitant use with serotonergic agents (including tramadol, triptans) may lead to the development of serotonin syndrome.

With simultaneous use with drugs that lower the seizure threshold, increases the risk of developing convulsions.

Escitalopram enhances the effects of tryptophan and lithium preparations, increases the toxicity of St. John’s wort preparations, the effects of drugs affecting blood clotting (control of blood clotting parameters is necessary).

Drugs metabolized with the participation of the CYP2C19 isoenzyme (including omeprazole), as well as those that are strong inhibitors of CYP3A4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase the plasma concentration of escitalopram.

Escitalopram increases the plasma concentration of desipramine and metoprolol by 2 times.

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.