Escitalopram

When ATH:
N06AB10

Pharmacological action

Antidepressant. Selectively inhibits the reuptake of serotonin; increases the concentration of neurotransmitter in the synaptic cleft, increases and prolongs action on postsynaptic serotonin receptors. Escitalopram hardly binds with serotonin (5-HT), dopamine (D1 и D2) receptors, a-адрено-, m-cholinergic receptors, as well as benzodiazepine and opioid receptors.

The antidepressant effect usually develops within 2-4 Sun. after treatment. The maximum therapeutic effect of the treatment of panic disorder is reached after about 3 months after initiation of treatment.

Pharmacokinetics

The absorption is not dependent on the ingestion. Bioavailability – 80%. Time to achieve Cmax in plasma – 4 no. Эstsitaloprama linear kinetics. Css achieved through 1 Sun. The average is Css 50 nmoli / (from 20 to 125 nmoli /) and is achieved at a dose 10 мг/ Кажущийся Vd – from 12 to 26 l / kg. Plasma protein binding – 80%. It is metabolized in the liver to the demethylated active metabolites and didemetilirovannogo. After repeated use of the average concentration of demethyl- and is didemetilmetabolitov 28-31% less 5% respectively from the concentration of escitalopram. The metabolism of escitalopram to the demethylated metabolite formation occurs mainly with the participation of isoenzymes CYP2C19, CYPЗA4 и CYP2D6. In persons with a weak CYP2C19 isozyme activity concentration of escitalopram may be 2 times higher, than those with a high activity of this isoenzyme. No significant changes in the concentration of the drug in a weak CYP2D6 isoenzyme activity is not marked. T1 / 2, after repeated use – 30 no. In 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 the – kidney, partially displayed in the form of glucuronides. T1 / 2 and AUC increased in elderly patients.

Testimony

Depression, panic disorder (incl. with agoraphobia).

Dosage regimen

Is the inside, regardless of the meal. Depending on the indication unit dose – 10-20 mg / maximum daily dose – 20 mg. Length of treatment – several months. Upon termination of the treatment the dose should be gradually reduced over the 1-2 Sun. for, to avoid syndrome “cancel”.

For elderly patients (senior 65 years) the recommended dose – 5 mg /, the maximum daily dose – 10 mg.

If abnormal liver function recommended starting for the first 2 Sun. treatment is 5 mg / Depending on the individual response the dose can be increased to 10 mg /

For patients with weak activity isoenzyme CYP2C19 recommended starting dose for the first 2 Sun. treatment – 5 mg / Depending on the individual response the dose can be increased to 10 mg /

Side effect

From the central and peripheral nervous system: dizziness, weakness, insomnia or drowsiness, convulsions, tremor, movement disorders, serotonin syndrome (ažitaciâ, tremor, myoclonus, hyperthermia), hallucinations, craze, confusion, ažitaciâ, alarm, depersonalization, panic attacks, irritability, visual disturbances.

From the digestive system: nausea, vomiting, dryness of the oral mucosa, dysgeusia, decreased appetite, diarrhea, constipation, changes in laboratory parameters of liver function.

Cardio-vascular system: orthostatic hypotension.

On the part of the endocrine system: decreased secretion of ADH, galactorrhea.

On the part of the reproductive system: decreased libido, impotence, abnormal ejaculation, anorgazmija (female).

From the urinary system: urinary retention.

Dermatological reactions: skin rash, itch, ecchymosis, purpura, increased perspiration.

Allergic reactions: angioedema, anaphylactic reactions.

Metabolism: giponatriemiya, hyperthermia.

On the part of the musculoskeletal system: arthralgia, myalgia.

Other: sinusitis, syndrome “cancel” (dizziness, headaches and nausea).

Contraindications

Simultaneous reception of MAO inhibitors, childhood and adolescence up 15 years, pregnancy, lactation, hypersensitivity to escitalopram.

Pregnancy and lactation

Contraindicated for use in pregnancy and lactation (breast-feeding).

Cautions

C Caution should be used in patients with renal insufficiency (CC less than 30 ml / min), hypomania, mania, at pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes, in elderly patients, liver cirrhosis, with a propensity to bleed, simultaneously with administration of the drug, lowering the seizure threshold, causing hyponatremia, ethanol, with drugs, metabolized with the participation of isoenzymes CYP2C19.

Escitalopram should be administered only through 2 Sun. after the abolition of irreversible MAO inhibitors and after 24 h reversible after discontinuation of MAO inhibitor. Non-selective MAO inhibitors may be administered no earlier than 7 days after discontinuation of escitalopram.

Some patients with panic disorder, early treatment can be observed escitalopram increased anxiety, which normally disappears during the subsequent 2 Sun. treatment. To reduce the chance of an alarm, it is recommended to use low initial doses.

Escitalopram should be repealed in the event of seizures or increased rates of pharmacologically uncontrolled epilepsy.

With the development of mania escitalopram should be abolished.

Escitalopram can increase blood glucose in diabetes, which may require dose adjustments hypoglycemic agents.

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

Giponatriemiya, associated with a decrease in the secretion of ADH, while taking escitalopram is rare and usually disappear with its abolition.

With the development of serotonin syndrome escitalopram should be lifted immediately and appoint a symptomatic treatment.

Effects on ability to drive vehicles and management mechanisms

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

Drug Interactions

At simultaneous application with MAO inhibitors increases the risk of serotonin syndrome and severe adverse reactions.

The combined use of serotonergic agents (incl. with tramadol, triptans) It can lead to serotonin syndrome.

In an application with drugs, lowering the seizure threshold, It increases the risk of seizures.

Escitalopram enhances the effects of tryptophan and lithium preparations, St. John's Wort increases the toxicity of drugs, effects of drugs, affecting blood coagulation (requires monitoring of blood coagulation parameters).

Preparations, metabolized involving isoenzyme CYP2C19 (incl. omeprazole), as well as a potent inhibitor of CYP2D6 and CYPZA4 (incl. flekainid, propafenone, metoprolol, desipramine, clomipramine, nortryptylyn, risperidone, tioridazin, haloperidol), increase the concentration in plasma escitalopram.

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