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, generalized anxiety disorder.

Active ingredient

Composition

1 tablet contains

The active ingredient:

escitalopram – 10 mg.

How to take, the dosage

It is taken orally, regardless of meals. Depending on indications, single dose is 10-20 mg/day.

The 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 onset of withdrawal syndrome.

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

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

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

Interaction

Concomitant use with MAO inhibitors increases the risk of serotonin syndrome and serious adverse reactions.

The concomitant use with serotonergic agents (including tramadol, triptans) may lead to serotonin syndrome.

Concomitant use with drugs that lower the seizure threshold increases the risk of seizures.

Escitalopram increases the effects of tryptophan and lithium preparations, increases the toxicity of Hypericum, the effects of drugs affecting blood clotting (control of blood clotting parameters is necessary).

The drugs metabolized with participation of CYP2C19 isoenzyme (including omeprazole), as well as being strong inhibitors of CYPZA4 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-fold.

Special Instructions

Escitalopram should not be administered until 2 weeks after withdrawal of irreversible MAO inhibitors and 24 hours after stopping therapy with a reversible MAO inhibitor. Non-selective MAO inhibitors can be administered not earlier than 7 days after withdrawal of escitalopram.

In some patients with panic disorder, an increase in anxiety may be observed at the beginning of treatment with escitalopram, which usually disappears within the next 2 weeks of treatment. Low starting doses are recommended to reduce the likelihood of anxiety.

Escitalopram should be discontinued if epileptic seizures develop or increase in frequency in pharmacologically uncontrolled epilepsy.

Escitalopram should be discontinued if manic states develop.

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

The clinical experience with escitalopram suggests that there may be an increased risk of suicide attempts during the first weeks of therapy, so close monitoring of patients during this period is very important.

Hyponatremia associated with decreased ADH secretion is rare with escitalopram and usually resolves with discontinuation.

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

Impact on driving and operating machinery

Patients should avoid driving and other activities requiring high concentration and speed of psychomotor reactions during treatment.

Contraindications

Concurrent 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 insufficiency (CKR less than 30 ml/min), hypomania, mania, pharmacologically uncontrolled epilepsy, depression with suicide attempts, diabetes, elderly patients, In patients with cirrhosis of the liver, in susceptibility to bleeding, concomitantly with the use of drugs that reduce the threshold of seizure readiness, causing hyponatremia, with ethanol, and with drugs metabolized with the participation of CYP2C19 isoenzymes.

Side effects

CNS and peripheral nervous system disorders: dizziness, weakness, insomnia or somnolence, seizures, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability, visual disturbances.

Digestive system disorders: nausea, vomiting, dry oral mucosa, taste disorders, decreased appetite, diarrhea, constipation, changes in laboratory values of liver function.

Cardiovascular system: orthostatic hypotension.

Endocrine system: decreased secretion of ADH, galactorrhea.

In the sexual system: decreased libido, impotence, impaired ejaculation, anorgasmia (in women).

Urinary system disorders: urinary retention.

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

Allergic reactions: angioedema, anaphylactic reactions.

Metabolic reactions: hyponatremia, hyperthermia.

Muscular system disorders: arthralgia, myalgia.

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

Similarities