ACP, 10 mg 28 pcs.

Selectively inhibits serotonin reuptake; increases the concentration of the neurotransmitter in the synaptic cleft, enhances and prolongs the effect of serotonin on postsynaptic receptors. Estcitalopram binds almost completely to serotonin (5-HT), dopamine (D₁ and D₂) receptors, α-adreno-, m-cholinoreceptors, and benzodiazepine and opioid receptors.

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

Pharmacokinetics

Extraction is not dependent on food intake. Bioavailability is 80%. Time to reach C_max in plasma – 4 hours.

The kinetics of escitalopram are linear. C_ss is reached after 1 week. The mean C_ss is 50 nmol/L (20 to 125 nmol/L) and is reached at a dose of 10 mg/day. The apparent V_d is 12 to 26 l/kg. Binding to plasma proteins is 80%.

Metabolized in the liver to active demethylated and didemethylated metabolites. After repeated use, the average concentration of demethyl- and didemethylmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram.

The metabolism of escitalopram to form a demethylated metabolite occurs primarily with the participation of the CYP2C19, CYPZA4 and CYP2D6 isoenzymes. In patients with low activity of CYP2C19 isoenzyme the concentration of escitalopram may be 2 times higher than in patients with high activity of this isoenzyme.

There are no significant changes in drug concentrations when CYP2D6 isoenzyme activity is weak. T_1/2 After multiple administration – 30 h. The main metabolites of escitalopram have a longer T_1/2 duration.

Clearance is 0.6 l/min. Excitalopram and its major metabolites are excreted by the liver and most of them by the kidneys, partially excreted as glucuronides. T_1/2 and AUC increases in elderly patients.

Indications

Escitalopram is indicated for the treatment of major depressive disorder and generalized anxiety disorder.

Pharmacological effect

Selectively inhibits serotonin reuptake; increases the concentration of the neurotransmitter in the synaptic cleft, enhances and prolongs the effect of serotonin on postsynaptic receptors. Escitalopram practically does not bind to serotonin (5-HT), dopamine (D1 and D2) receptors, α-adrenergic, m-cholinergic receptors, as well as benzodiazepine and opioid receptors.

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

Pharmacokinetics

Absorption is independent of food intake. Bioavailability – 80%. The time to reach Cmax in plasma is 4 hours.

The kinetics of escitalopram is linear. Css is achieved after 1 week. The average Css is 50 nmol/l (range 20 to 125 nmol/l) and is achieved at a dose of 10 mg/day. Apparent Vd – from 12 to 26 l/kg. Plasma protein binding – 80%.

Metabolized in the liver to active demethylated and didemethylated metabolites. After repeated use, the average concentration of demethyl and didemethyl metabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram.

The metabolism of escitalopram with the formation of a demethylated metabolite occurs mainly with the participation of the isoenzymes CYP2C19, CYP3A4 and CYP2D6. In individuals with weak activity of the CYP2C19 isoenzyme, the concentration of escitalopram may be 2 times higher than in individuals with high activity of this isoenzyme.

There are no significant changes in the concentration of the drug with weak activity of the CYP2D6 isoenzyme. T1/2 after repeated use is 30 hours. For the main metabolites of escitalopram, T1/2 is longer.

Clearance – 0.6 l/min. Escitalopram and its main metabolites are excreted by the liver and most of them by the kidneys, partially excreted in the form of glucuronides. T1/2 and AUC increase in elderly patients.

Special instructions

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

Some patients with panic disorder may experience increased anxiety at the beginning of treatment with escitalopram, which usually disappears over the next 2 weeks. treatment. To reduce the likelihood of anxiety, low initial doses are recommended.

Escitalopram should be discontinued if epileptic seizures develop or become more frequent in pharmacologically uncontrolled epilepsy.

If a manic state develops, escitalopram should be discontinued.

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

Clinical experience with escitalopram indicates a possible increase in the risk of suicide attempts in the first weeks of therapy, and therefore it is very important to carefully monitor patients during this period.

Hyponatremia associated with decreased ADH secretion occurs rarely with escitalopram and usually disappears when it is discontinued.

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

Impact on the ability to drive vehicles and operate machinery

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

Active ingredient

Escitalopram

Composition

1 tablet contains

Active ingredient:

escitalopram – 10 mg.

Contraindications

Concomitant use of MAO inhibitors, children and adolescents under 15 years of age, pregnancy, lactation, hypersensitivity to escitalopram.

Caution should be used in patients with renal failure (creatinine clearance less than 30 ml/min), hypomania, mania, with pharmacologically uncontrolled epilepsy, with depression with suicidal attempts, diabetes mellitus, in elderly patients, with cirrhosis of the liver, with a tendency to bleeding, while taking medications that reduce the threshold of convulsive readiness, causing hyponatremia, with ethanol, with drugs metabolized with the participation of isoenzymes of the CYP2C19 system.

Side Effects

From the central nervous system and peripheral 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 laboratory parameters of liver function.

From the cardiovascular system: orthostatic hypotension.

From the endocrine system: decreased secretion of ADH, galactorrhea.

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

From the urinary system: urinary retention.

Dermatological reactions: skin rash, itching, ecchymosis, purpura, increased sweating.

Allergic reactions: angioedema, anaphylactic reactions.

Metabolism: hyponatremia, hyperthermia.

From the musculoskeletal system: arthralgia, myalgia.

Other: sinusitis, withdrawal syndrome (dizziness, headaches and nausea).

Interaction

When used simultaneously with MAO inhibitors, the risk of developing serotonin syndrome and serious adverse reactions increases.

Combined use with serotonergic drugs (including tramadol, triptans) can lead to the development of serotonin syndrome.

When used simultaneously with drugs that lower the seizure threshold, it increases the risk of developing seizures.

Escitalopram enhances the effects of tryptophan and lithium preparations, increases the toxicity of St. John’s wort preparations, and the effects of drugs that affect blood coagulation (monitoring of blood coagulation parameters is necessary).

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

Escitalopram increases plasma concentrations of desipramine and metoprolol by 2 times.

Storage conditions

Store out of the reach of children at a temperature not exceeding 25 °C.

Shelf life

2 years.

Manufacturer

Veropharm LLC, Russia