Selectra, 10 mg 28 pcs.

Selectra is an antidepressant that 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 to serotonin (5-HT), dopamine (D1 and D2), alpha-adrenergic, histamine, m-cholinoreceptors, and benzodiazepine and opiate receptors. The antidepressant effect usually develops 2-4 weeks after the start of treatment. Maximum therapeutic effect of panic disorder treatment is reached approximately 3 months after the start of treatment.

Pharmacokinetics

Intake and distribution

Intake is not dependent on food intake. The bioavailability of escitalopram is about 80%. The average time to reach C_max in plasma is about 4 hours.

The kinetics of escitalopram are linear. C_ss is reached after approximately 1 week. An average C_ss of 50 nmol/L (20 to 125 nmol/L) is achieved at a daily dose of 10 mg.

After oral administration, the apparent V_d is 12 to 26 L/kg. The binding of escitalopram and its major 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 excreted 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. Biotransformation of escitalopram to a demethylated metabolite occurs primarily via the CYP2C19 cytochrome. Some involvement of CYP3A4 and CYP2D6 isoenzymes is possible. In persons with weak CYP2C19 activity, the concentration of escitalopram may be twice as high as in cases with high activity of this isoenzyme. No significant changes in drug concentrations were found in cases with weak CYP2D6 isoenzyme activity.

T_1/2 after multiple use is about 30 h. Clearance with oral administration is about 0.6 l/min. The main metabolites of escitalopram have a longer T_1/2. Excitalopram and its major metabolites are excreted by the liver (metabolic pathway) and the kidneys.

Pharmacokinetics in special clinical cases

Elderly (over 65 years) excrete escitalopram more slowly compared to younger patients. The AUC in the elderly is 50% higher than in young healthy volunteers.

Indications

Active ingredient

Composition

1 film-coated tablet contains:

the active ingredient:

escitalopram oxalate 12.78 mg, which corresponds to the content of escitalopram 10 mg,

auxiliary substances:

The 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,

coating composition:

Opadry White (Opadry 03F28446 White) – about 5.4 mg (hypromellose 6cP – 3.29 mg, titanium dioxide – 1.31 mg, macrogol 6000 – 0.8 mg).

How to take, the dosage

Selectra is taken orally, regardless of meals. Depending on the indication, the 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), 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.

For patients with weak CYP2C19 isoenzyme activity, 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.

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

Some patients with panic disorder may experience an increase in 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 that the drug be used in a low starting dose.

The drug should be discontinued if seizures develop. Use in patients with uncontrolled epilepsy is not recommended; in controlled seizures, close monitoring is necessary. If seizure frequency 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 withdrawn.

In patients with diabetes mellitus, treatment with escitalopram may alter blood glucose levels (both hypoglycemia and hyperglycemia are possible). Therefore, adjustment of insulin doses and/or oral hypoglycemic drugs may be required.

The risk of suicide is intrinsic to depression and may persist until a significant improvement has occurred spontaneously or as a result of ongoing therapy. Close monitoring of patients on antidepressant treatment is necessary, especially at the beginning of treatment, because of the potential for clinical deterioration and/or the appearance of suicidal ideation (thoughts and behavior). This precaution should also be observed when treating other psychiatric disorders because of the possibility of simultaneous development of depression.

In some cases, treatment with SSRI antidepressants has been shown to increase the risk of suicidal thoughts and behaviors in children, adolescents and young adults younger than 24 years compared to placebo.

Hyponatremia, possibly related to impaired ADH secretion, is rare with escitalopram and usually disappears with discontinuation of therapy. Caution should be exercised when prescribing escitalopram and other SSRIs in individuals at risk for hyponatremia: the elderly, patients with cirrhosis of the liver, and those taking medications that can cause hyponatremia.

The use of escitalopram may cause subcutaneous hemorrhages (ecchymoses and purpura). It is necessary to use escitalopram with caution in patients who are prone to bleeding, as well as those who take oral anticoagulants and other drugs affecting blood clotting.

Because 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 because of the risk of serotonin syndrome.

Patients taking escitalopram and other SSRIs concomitantly with serotonergic drugs may, in rare cases, develop serotonin syndrome. Caution should be exercised when using escitalopram concomitantly with drugs with serotonergic effects. The combination of symptoms such as agitation, tremor, myoclonus, hyperthermia, may indicate the development of serotonin syndrome. If this occurs, SSRIs and serotoninergic medications should be discontinued immediately and symptomatic treatment administered.

Impact on driving and operating machinery

Patients should avoid potentially hazardous activities requiring high-speed psychomotor reactions, such as driving or operating machinery, during treatment with the drug.

Synopsis

Contraindications

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).

Overdose

Symptoms: dizziness, tremor, agitation, somnolence, confusion, seizures, tachycardia, ECG changes (change of ST segment, T tooth, widening of QRS complex, QT interval prolongation), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia, very rarely – acute renal failure.

Treatment: symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring of cardiovascular and respiratory system function. There is no specific antidote

.

Pregnancy use

Escitalopram during pregnancy should be taken only if absolutely necessary and after careful assessment of the benefit/risk ratio.

Breast-feeding during treatment with the drug is not recommended.

The effects of escitalopram on fertility have not yet been observed, but reversible effects of other selective serotonin reuptake inhibitors (SSRIs) on sperm quality have been reported.

Similarities