Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antidepressant. 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 practically does not bind to serotonin (5-HT), dopamine (D 1 and D 2 ) receptors, ОІ-adreno-, m-cholinergic receptors, as well as benzodiazepine and opioid receptors.
The antidepressant effect usually develops in 2-4 weeks. after the beginning of treatment. The maximum therapeutic effect of treatment of panic disorders is achieved approximately 3 months after the start of treatment.
PHARMACOKINETICS
Absorption is not dependent on food intake. Bioavailability - 80%. The time to reach C max in plasma is 4 hours. The kinetics of escitalopram is linear. C ss is achieved after 1 week. The average C ss is 50 nmol / L (20 to 125 nmol / L) and is achieved at a dose of 10 mg / day. Apparent V d is from 12 to 26 l / kg. Binding to plasma proteins - 80%. Metabolized in the liver to active demethylated and demodetylated metabolites. After repeated use, the average concentration of demethyl- and didemetilmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram. Metabolism of escitalopram with the formation of a demethylated metabolite occurs mainly with the participation of isoenzymes CYP2C19, CYPZA4 and CYP2D6. In persons with a weak activity of the isoenzyme CYP2C19, the concentration of escitalopram can be 2 times higher than in persons with a high activity of this isoenzyme. Significant changes in the concentration of the drug with a weak activity of the isoenzyme CYP2D6 is not observed. T 1/2 after repeated use - 30 hours. The main metabolites of escitalopram T 1/2 are longer. Clearance - 0.6 l / min. Escitalopram and its major metabolites are excreted by the liver and a large part - by the kidneys, partially excreted in the form of glucuronides. T 1/2 and AUC increases in elderly patients.
INDICATIONS
Depression, panic disorder (including with agoraphobia).
DOSING MODE
Is taken orally, regardless of food intake. Depending on the indications, a single dose of 10-20 mg / day. The maximum daily dose is 20 mg. Duration of treatment is several months. At the termination of treatment the dose should gradually decrease within 1-2 weeks. in order to avoid the occurrence of the "withdrawal" syndrome.
For elderly patients (over 65 years) the recommended dose is 5 mg / day, the maximum daily dose is 10 mg.
If the liver function is impaired, the recommended initial for the first 2 weeks. treatment is 5 mg / day. Depending on the individual reaction, the dose can be increased to 10 mg / day.
For patients with a weak activity of the isoenzyme CYP2S19, the recommended initial dose for the first 2 weeks. treatment - 5 mg / day. Depending on the individual reaction, the dose can be increased to 10 mg / day.
SIDE EFFECT
From the nervous system: dizziness, weakness, insomnia or drowsiness, convulsions, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability , a disorder of vision.
On the part of the digestive system: nausea, vomiting, dryness of the oral mucosa, impaired taste, decreased appetite, diarrhea, constipation, changes in liver function.
From the cardiovascular system: orthostatic hypotension.
On the part of the endocrine system: a decrease in the secretion of ADH, galactorrhea.
On the part of the reproductive system: decreased libido, impotence, ejaculation, anorgasmia (in women).
From the urinary system: urinary retention.
Dermatological reactions: skin rash, itching, ecchymosis, purpura, increased sweating.
Allergic reactions: angioedema, anaphylactic reactions.
From the side of metabolism: hyponatremia, hyperthermia.
From the musculoskeletal system: arthralgia, myalgia.
Other: sinusitis, withdrawal syndrome (dizziness, headaches and nausea).
CONTRAINDICATIONS
Simultaneous administration of MAO inhibitors, childhood and adolescence up to 15 years, pregnancy, lactation, increased sensitivity to escitalopram.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in patients with renal insufficiency (CC less than 30 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Use with caution in cirrhosis.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 15 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly patients.
SPECIAL INSTRUCTIONS
Caution should be used in patients with renal insufficiency (CC less than 30 ml / min), hypomania, mania, with pharmacologically uncontrolled epilepsy, with depression with suicide attempts, diabetes, in elderly patients, with cirrhosis, with a tendency to bleeding, simultaneously with 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.
Escitalopram should be administered only after 2 weeks. after the cancellation 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 the withdrawal of escitalopram.
In some patients with panic disorder at the beginning of treatment with escitalopram, anxiety can be increased, which usually disappears during the next 2 weeks.treatment. To reduce the likelihood of an alarm, it is recommended to use low initial doses.
Escitalopram should be withdrawn in the event of epileptic seizures or their increase in pharmacologically uncontrolled epilepsy.
With the development of the manic state, escitalopram should be discontinued.
Escitalopram is able to increase the concentration of glucose in the blood in diabetes mellitus, which may require correction of doses of hypoglycemic drugs.
The clinical experience of using escitalopram indicates a possible increase in the risk of suicide attempts in the first weeks of therapy, which is why it is very important to carefully monitor patients during this period.
Hyponatremia, associated with a decrease in ADH secretion, against the background of escitalopram is rare and usually disappears when it is withdrawn.
With the development of serotonin syndrome, escitalopram should be immediately withdrawn and symptomatic treatment should be prescribed.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment, patients should avoid driving motor vehicles and other activities that require a high concentration of attention and speed of psychomotor reactions.
DRUG INTERACTION
When used simultaneously with MAO inhibitors, the risk of developing serotonin syndrome and serious adverse reactions increases.
Joint application with serotonergic drugs (including tramadol, triptans) may lead to the development of serotonin syndrome.
With simultaneous use with drugs that reduce the threshold of convulsive readiness, increases the risk of seizures.
Escitalopram enhances the effects of tryptophan and lithium preparations, increases the toxicity of St. John's wort preparations, the effects of drugs that affect blood clotting (monitoring of blood coagulation indices is necessary).
Preparations metabolized with the participation of the isoenzyme CYP2S19 (including omeprazole), and also the strong inhibitors of CYPZA4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase concentration of escitalopram in blood plasma.
Escitalopram increases the plasma concentration of desipramine and metoprolol by a factor of 2.
