Composition
1 film-coated tablet contains:
Active ingredient:
escitalopram oxalate 12.78 mg, which corresponds to the content of escitalopram 10 mg,
excipients:
prosolv SMCC®90 / HD90 – 147.42 mg (microcrystalline cellulose-144.47 mg, silicon dioxide-2.95 mg)
croscarmellose sodium-9 mg,
talc-9 mg,
magnesium stearate-1.8 mg,
film shell composition:
Opadry 03F28446 White – about 5.4 mg (hypromellose 6cP-3.29 mg, titanium dioxide-1.31 mg, macrogol 6000-0.8 mg).
Pharmacological action
Selectra is an antidepressant that 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 (D1 and D2), alpha-adrenergic, histamine, m-holinoreceptors, as well as benzodiazepine and opiate receptors. The antidepressant effect usually develops 2-4 weeks after the start of treatment. The maximum therapeutic effect of treating panic disorders is achieved approximately 3 months after the start of treatment.
Pharmacokinetics
Suction and distribution
Absorption is independent of food intake. The bioavailability of escitalopram is about 80%. The average time to reachcmax in blood plasma is about 4 hours.
The kinetics of escitalopram is linear. Css is reached in about 1 week. The average Css-50 nmol / l (from 20 to 125 nmol/L) is achieved at a daily dose of 10 mg.
After oraluse, the apparent Vd is 12 to 26 l / kg. The binding of escitalopram and its main metabolites to plasma proteins is about 80%.
Metabolism
Escitalopram is metabolized in the liver to demethylated and didemethylated metabolites. They are both pharmacologically active. The main substance and its metabolites are partially released in the form of glucuronides.
After repeated use, the average concentration of demethyl-and didemethylmetabolites is usually 28-31% and less than 5%, respectively, of the concentration of escitalopram. Escitalopram is biotransformed to a demethylated metabolite mainly by cytochrome CYP2C19. Some involvement of CYP3A4 and CYP2D6 isoenzymes is possible. In individuals with low CYP2C19 activity, the concentration of escitalopram may be twice as high as in cases with high activity of this isoenzyme. No significant changes in the drug concentration were found in cases with weak activity of the CYP2D6 isoenzyme.
The elimination
rate of T1/2 after repeated use is about 30 h. The oral clearance is about 0.6 l/min. In the main metabolites of escitalopram, T1/2 is longer. Escitalopram and its major metabolites are excreted by the liver (metabolic pathway) and kidneys.
Pharmacokinetics in special clinical cases
In the elderly (over 65 years of age), escitalopram is excreted more slowly compared to younger patients. AUC in elderly subjects is 50% higher than in young healthy volunteers.
Indications
- depressive disorders of any severity,
- panic disorder with / without agoraphobia,
- social anxiety disorder (social phobia),
- generalized anxiety disorder,
- obsessive-compulsive disorder.
Use during pregnancy and lactation
Escitalopram should be taken during pregnancy only when absolutely necessary and after careful assessment of the benefit / risk ratio.
Breast-feeding during drug treatment is not recommended.
The effect of escitalopram on fertility has not yet been observed, but there have been reports of reversible effects of other selective serotonin reuptake inhibitors (SSRIs) on sperm quality.
Contraindications
- hypersensitivity to escitalopram and other components of the drug;
- concomitant use of non-selective irreversible monoamine oxidase (MAO) inhibitors;
- concomitant use of pimozide;
- children and adolescents (under 18 years of age) (efficacy and safety have not been confirmed).
Side effects
From the central nervous system and peripheral 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, visual disturbances.
From the digestive system: nausea, vomiting, dryness of the oral mucosa, taste disorders, decreased appetite, diarrhea, constipation, changes in laboratory parameters of liver function.
From the cardiovascular system: orthostatic hypotension.
From the endocrine system: decreased ADH secretion, galactorrhea.
From the side of the reproductive system: decreased libido, impotence, ejaculation disorders, anorgasmia (in women).
Urinary system disorders: urinary retention.
Dermatological reactions: skin rash, pruritus, ecchymosis, purpura, increased sweating.
Allergic reactions: angioedema, anaphylactic reactions.
From the side of metabolism: hyponatremia, hyperthermia.
Musculoskeletal disorders: arthralgia, myalgia.
Others: sinusitis, withdrawal symptoms (dizziness, headaches, and nausea).
Interaction
Concomitant use with MAO inhibitors increases the risk of serotonin syndrome and serious adverse reactions.
Combined use with serotonergic agents (including tramadol, triptans) can lead to the development of serotonin syndrome.
When used concomitantly with drugs that lower the threshold of convulsive readiness, it increases the risk of 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 clotting (monitoring of blood clotting parameters is necessary).
Drugs that are metabolized with the participation of the CYP2C19 isoenzyme (including omeprazole), as well as strong inhibitors of SURZA 4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase the concentration of escitalopram in blood plasma.
Escitalopram increases the plasma concentrations of desipramine and metoprolol by 2 times.
How to take, course of use and dosage
Selectra is taken orally, regardless of food intake. Depending on the indications, a single dose is 10-20 mg / day. The maximum daily dose is 20 mg. The duration of treatment is several months. When stopping treatment, the dose should be gradually reduced over 1-2 weeks. in order to avoid the occurrence of “withdrawal” syndrome.
For elderly patients (over 65 years of age), the recommended dose is 5 mg / day, the maximum daily dose is 10 mg.
If liver function is impaired, the recommended initial dose is within the first 2 weeks. the treatment dose is 5 mg / day. Depending on the individual response, the dose may be increased to 10 mg / day.
For patients with low activity of the CYP2C19 isoenzyme, the recommended initial dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response, the dose may be increased to 10 mg / day.
Overdose
Symptoms: dizziness, tremor, agitation, drowsiness, confusion, convulsive seizures, tachycardia, ECG changes (changes in the ST segment, T wave, expansion of the QRS complex, prolongation of the QT interval), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia, very rarely – acute renal failure.
Treatment: symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems. There is no specific antidote
Description
White film-coated tablets, oval, biconvex, with the inscription “E” on one side, a risk on the other side and side risks.
Special instructions
Some patients with panic disorder may experience increased anxiety at the start of SSRI treatment. This paradoxical reaction usually disappears within two weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommended to use the drug in a low initial dose.
The drug should be discontinued in case of convulsive seizures. It is not recommended for use in patients with uncontrolled epilepsy; for controlled seizures, careful monitoring is necessary. If the frequency of seizures increases, SSRIs, including escitalopram, should be discontinued.
Escitalopram should be used with caution in patients with a history of mania / hypomania. If a manic state develops, escitalopram should be discontinued.
In patients with diabetes mellitus, treatment with escitalopram may alter blood glucose levels (both hypoglycemia and hyperglycemia are possible). Therefore, it may be necessary to adjust the dose of insulin and / or oral hypoglycemic drugs.
The risk of suicide is associated with depression and may persist until significant improvement occurs spontaneously or as a result of ongoing therapy.Patients treated with antidepressants should be carefully monitored, especially at the beginning of treatment, because of the possibility of clinical deterioration and / or the appearance of suicidal thoughts and behaviors. This precaution should also be taken in the treatment of other psychiatric disorders because of the possibility of simultaneous development of depression.
In some cases, treatment with SSRI antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults under 24 years of age, compared with placebo.
Hyponatremia, possibly associated with impaired ADH secretion, occurs rarely with escitalopram and usually disappears when therapy is discontinued. Caution should be exercised when prescribing escitalopram and other SSRIs to people at risk of developing hyponatremia: the elderly, patients with cirrhosis of the liver, and taking drugs that can cause hyponatremia.
When taking escitalopram, subcutaneous hemorrhage (ecchymosis and purpura) may develop. Escitalopram should be used with caution in patients with a tendency to bleed, as well as taking oral anticoagulants and other medications that affect blood clotting.
Since clinical experience with concomitant use of escitalopram and electroconvulsive therapy is limited, caution should be exercised in such cases.
The combination of escitalopram and MAO type A inhibitors is not recommended due to the risk of serotonin syndrome.
Patients taking escitalopram and other SSRIs concomitantly with serotonergic medications may develop serotonin syndrome in rare cases. Escitalopram should be used with caution simultaneously with medications that have a serotonergic effect. A combination of symptoms such as agitation, tremor, myoclonus, and hyperthermia may indicate the development of serotonin syndrome. If this occurs, SSRIs and serotonergic medications should be discontinued immediately and symptomatic treatment should be prescribed.
Influence on the ability to drive motor vehicles and manage mechanisms
During treatment with the drug, patients should avoid performing potentially dangerous activities that require a high rate of psychomotor reactions, such as driving a car or operating mechanisms.
Form of production
Film-coated tablets
Storage conditions
At a temperature not exceeding 25 °C
Shelf life
1 year
Active ingredient
Escitalopram
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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