Selectra, 10 mg 28 pcs.
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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 Cmax in plasma is about 4 hours.
The kinetics of escitalopram are linear. Css is reached after approximately 1 week. An average Css of 50 nmol/L (20 to 125 nmol/L) is achieved at a daily dose of 10 mg.
After oral administration, the apparent Vd 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.
T1/2 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 T1/2. 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
depressive disorders of any severity,
panic disorder with/without agoraphobia,
social anxiety disorder (social phobia),
generalized anxiety disorder,
obsessive-compulsive disorder.
Pharmacological effect
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. Escitalopram practically does not bind to serotonin (5-HT), dopamine (D1 and D2), alpha-adrenergic, histamine, m-cholinergic receptors, 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 treatment for 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 reach Cmax in blood plasma is about 4 hours.
The kinetics of escitalopram is linear. Css is achieved in approximately 1 week. Average Css – 50 nmol/l (from 20 to 125 nmol/l) is achieved with a daily dose of 10 mg.
After oral administration, the apparent Vd ranges from 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 didemethyl metabolites is usually 28-31% and less than 5%, respectively, of the concentration of escitalopram. Biotransformation of escitalopram into a demethylated metabolite occurs mainly through the cytochrome CYP2C19. Some involvement of CYP3A4 and CYP2D6 isoenzymes is possible. In individuals 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 the concentration of the drug were found in cases with weak activity of the CYP2D6 isoenzyme.
Removal
T1/2 after repeated use is about 30 hours. Oral clearance is about 0.6 l/min. The main metabolites of escitalopram have a longer T1/2. Escitalopram and its main metabolites are excreted by the liver (metabolic pathway) and kidneys.
Pharmacokinetics in special clinical situations
In elderly patients (over 65 years of age), escitalopram is excreted more slowly than in younger patients. AUC in the elderly is 50% greater than in young healthy volunteers.
Special instructions
Some patients with panic disorder may experience increased anxiety when starting 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 if seizures develop. Use in patients with uncontrolled epilepsy is not recommended; Controlled seizures require careful monitoring. 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 change blood glucose levels (both hypoglycemia and hyperglycemia are possible). Therefore, dose adjustments of insulin and/or oral hypoglycemic agents may be necessary.
The risk of committing suicide is inherent in depression and may persist until the condition significantly improves, either spontaneously or as a result of therapy. Careful monitoring of patients being treated with antidepressants is necessary, especially at the beginning of treatment, due to the possibility of clinical deterioration and/or the emergence of suicidal manifestations (thoughts and behavior). This precaution should also be observed when treating other mental disorders due to the possibility of simultaneous development of depression.
In some cases, when treated with SSRI antidepressants, there was an increased risk of developing suicidal thoughts and behavior in children, adolescents and young adults under 24 years of age, compared to 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 persons at risk of developing hyponatremia: the elderly, those with liver cirrhosis, and those taking medications that can cause hyponatremia.
When taking escitalopram, subcutaneous hemorrhages (ecchymosis and purpura) may develop. Escitalopram should be used with caution in patients with a tendency to bleed, as well as those taking oral anticoagulants and other drugs that affect blood clotting.
Since clinical experience with the simultaneous 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 developing serotonin syndrome.
In rare cases, patients taking escitalopram and other SSRIs concomitantly with serotonergic drugs may develop serotonin syndrome. Escitalopram should be used with caution concomitantly with drugs that have serotonergic effects. A combination of symptoms such as agitation, tremor, myoclonus, and hyperthermia may indicate the development of serotonin syndrome. If this occurs, SSRIs and serotonergic drugs should be immediately discontinued and symptomatic treatment prescribed.
Impact on the ability to drive vehicles and operate machinery
During treatment with the drug, patients should avoid performing potentially hazardous activities that require high speed psychomotor reactions, such as driving a car or operating machinery.
Active ingredient
Escitalopram
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 white (Opadry 03F28446 White) – about 5.4 mg (hypromellose 6cP – 3.29 mg, titanium dioxide – 1.31 mg, macrogol 6000 – 0.8 mg).
Pregnancy
Escitalopram should only be taken during pregnancy when absolutely necessary and after a careful benefit/risk assessment.
Breastfeeding during treatment with the drug is not recommended.
The effects of escitalopram on fertility have 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;
simultaneous use of non-selective irreversible monoamine oxidase inhibitors (MAO);
simultaneous use of pimozide;
children and adolescents (up to 18 years) (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, movement 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, dry oral mucosa, taste disturbances, decreased appetite, diarrhea, constipation, changes in laboratory parameters of liver function.
From the cardiovascular system: orthostatic hypotension.
From the endocrine system: decreased secretion of ADH, galactorrhea.
From the reproductive system: decreased libido, impotence, impaired ejaculation, anorgasmia (in women).
From the urinary system: urinary retention.
Dermatological reactions: skin rash, itching, ecchymosis, purpura, increased sweating.
Allergic reactions: angioedema, anaphylactic reactions.
Metabolism: hyponatremia, hyperthermia.
From the musculoskeletal system: arthralgia, myalgia.
Other: sinusitis, withdrawal syndrome (dizziness, headaches and nausea).
Interaction
When used simultaneously with MAO inhibitors, the risk of developing serotonin syndrome and serious adverse reactions increases.
Combined use with serotonergic drugs (including tramadol, triptans) can lead to the development of serotonin syndrome.
When used simultaneously with drugs that lower the seizure threshold, it increases the risk of developing 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 coagulation (monitoring of blood coagulation parameters is necessary).
Drugs that are metabolized with the participation of the CYP2C19 isoenzyme (including omeprazole), and also are strong inhibitors of CYP3A4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase the concentration of escitalopram in blood plasma.
Escitalopram increases plasma concentrations of desipramine and metoprolol by 2 times.
Overdose
Symptoms: dizziness, tremor, agitation, drowsiness, confusion, seizures, tachycardia, ECG changes (changes in the ST segment, T wave, widening 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
Storage conditions
At a temperature not exceeding 25 °C
Shelf life
1 year
Manufacturer
Actavis Ltd, Malta
Shelf life | 1 year |
---|---|
Conditions of storage | At a temperature not exceeding 25 °C |
Manufacturer | Actavis Ltd, Malta |
Medication form | pills |
Brand | Actavis Ltd |
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