Selectra pills 10 mg 28 pcs
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Active ingredients
Escitalopram
Release form
Pills
Composition
Active ingredient: EscitalopramActivating agents: talc, silica, microcrystalline cellulose, magnesium stearate, croscarmellose sodium. Active substance concentration (mg): 10 mg
Pharmacological effect
Antidepressant. selectively inhibits serotonin reuptake; increases the concentration of neurotransmitter in the synaptic cleft, strengthens and prolongs the action of serotonin on postsynaptic receptors. escitalopram practically does not bind to serotonin (5-ht), dopamine (d1 and d2) receptors, α-adreno-, m-cholinergic receptors, and also to benzodiazepine and opioid receptors. The antidepressant effect usually develops after 2-4 weeks. after starting treatment. The maximum therapeutic effect of treating panic disorders is reached approximately 3 months after the start of treatment.
Pharmacokinetics
Suction does not depend on food intake. Bioavailability - 80%. The time to reach Cmax in plasma is 4 h. The kinetics of escitalopram is linear. Css is reached after 1 week. The average Css is 50 nmol / l (from 20 to 125 nmol / l) and is achieved at a dose of 10 mg / day. Seeming Vd - from 12 to 26 l / kg. Plasma protein binding - 80%. Metabolized in the liver to active demethylated and dimethylated metabolites. After repeated use, the average concentration of demethyl and dimethylmetabolites is 28–31% and less than 5%, respectively, of the concentration of escitalopram. The metabolism of escitalopram with the formation of a demethylated metabolite occurs mainly with the participation of the isoenzymes CYP2C19, CYP3A4 and CYP2D6. In persons with a weak activity of the CYP2C19 isoenzyme, the concentration of escitalopram can be 2 times higher than in individuals 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. T1 / 2 after repeated use - 30 h. The major metabolites of escitalopram T1 / 2 are longer. Clearance - 0.6 l / min. Escitalopram and its major metabolites are excreted by the liver and most of it by the kidneys, partially excreted in the form of glucuronides. T1 / 2 and AUC increases in elderly patients.
Indications
panic states with or without agoraphobia; frustration depressive nature of any level of severity.
Contraindications
breast-feeding; hypersensitivity; age up to 15 years; concurrent use with MAO inhibitors; pregnancy.Relative: kidney failure, with CC less than 30 ml / min; age of 15-18; manic disorders; hypomania; uncontrolled epilepsy; diabetes; suicidal depression; elderly age; predisposition to bleeding; cirrhosis of the liver; combined use with ethanol; drugs that cause hyponatremia; reduce convulsive readiness; metabolized by cytochrome CYP2C19
Precautionary measures
Keep out of the reach of children.
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding).
Dosage and administration
Instructions for use Selectra recommends a single daily oral (internal) administration of pills to patients who have reached the age of 15 years. Panic conditions. During the first 7 days of therapy, a daily dose of 5 mg is recommended, with a further increase to 10 mg. Consistent with the individual sensitivity of the patient to escitalopram, you can increase the daily dose to a maximum of 20 mg. Therapy is long, the maximum effectiveness of treatment is observed, as a rule, after 3 months. Depressive states. As a rule, 10 mg of Selectra is prescribed once per 24 hours. Consistent with the individual sensitivity of the patient to escitalopram, you can increase the daily dose to a maximum of 20 mg. Antidepressant efficacy in most cases develops over the 2nd — 4th week. In order to consolidate the positive effect, after leveling the symptoms of depression, it is necessary to continue treatment for another 6 months. Age after 65 years. Recommended daily and maximum doses should be halved. Pathology of the kidneys. When QA is more than 30 ml / min, there is no need to adjust the dosages of Selectra. In the opposite case, use minimal doses of escitalopram, with their gradual increase according to the individual response of the patient. Liver pathology: The initial daily dosage of the Selectra is 5 mg. Consistent with the individual sensitivity of the patient to escitalopram, you can increase the daily dose to a maximum of 10 mg. Reduced CYP2C19 cytochrome activityPatients with insufficient CYP2C19 activity for 14 days require an initial daily dose of 5 mg.Consistent with the individual sensitivity of the patient to escitalopram, you can increase the daily dose to a maximum of 10 mg.
Side effects
Most often, side effects were observed during the first 14 days of therapy, after which their activity and frequency of manifestation decreased or completely stopped. CNS: depersonalization; dizziness; panic attacks; weakness; anxiety; insomnia; irritability; drowsiness; agitation; convulsions; visual impairment; tremor; confusion; movement disorders; hallucinations; serotonin syndrome (myoclonus, hyperthermia, tremor, agitation); manic disorders. GI: dryness in the mouth; diarrhea; nausea; taste disorders; vomiting; decreased appetite; constipation. Endocrine system: galactorrhea; decrease in secretion of ADH. Cardiovascular system: orthostatic hypotension. Genitourinary system: anorgasmia (in women); decreased libido; impaired ejaculation; urine retention; impotence. Skin: ecchymosis; rash; purpura; itching; angioedema. Laboratory indicators: changes in hepatic function; hyponatremia. Allergic reactions: anaphylactic manifestations. Others: hyperthermia; excessive sweating; sinusitis; myalgia; arthralgia; withdrawal syndrome (with sudden discontinuation of treatment).
Interaction with other drugs
With simultaneous use with MAO inhibitors increases the risk of serotonin syndrome and serious adverse reactions. Combined use with serotonergic drugs (including tramadol, triptanami) can lead to the development of serotonin syndrome. When used simultaneously with drugs that reduce the threshold of convulsive readiness, increases the risk of seizures. Estsitalopram enhances the effects of tryptophan and lithium preparations, increases the toxicity of Hypericum drugs, the effects of drugs that affect clotting blood count (control of blood coagulation indices is necessary). Preparations metabolized with the participation of CYP2C19 isoenzyme (including omeprazole), as well as being strong inhibitors of CYPZA4 and CYP2D6 (including flekainid, propafenone, metoprolol, desipramine, clomipramine, nortriptilin, risperidone, thioridazine, haloperidol), increase the concentration of escitalopram in the blood plasma. Escitalopram increases the plasma concentration of desipramine and metoprolol by 2 times.
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 suicidal attempts, diabetes mellitus, in elderly patients, with cirrhosis of the liver, with a tendency to bleed, simultaneously with taking medications that reduce the threshold of convulsive readiness, causing hyponatremia, with ethanol, with drugs that are metabolized with the participation of isoenzymes of the CYP2C19 system. Escitalopram should be prescribed only es 2 weeks. after discontinuation of irreversible MAO inhibitors and 24 hours after cessation of therapy with a reversible MAO inhibitor. Non-selective MAO inhibitors can be prescribed no earlier than 7 days after withdrawal of escitalopram. In some patients with panic disorder, at the beginning of treatment with escitalopram, an increased anxiety may occur, which usually disappears within the next 2 weeks. treatment. To reduce the likelihood of anxiety, it is recommended to use low initial doses. Escitalopram should be canceled if epileptic seizures develop or their frequency increases with pharmacologically uncontrolled epilepsy. Escitalopram should be discontinued when a manic state develops. correction of doses of hypoglycemic drugs. Clinical experience of using escitalopram indicates a possible increased and the risk of suicidal attempts in the first weeks of therapy, and therefore it is very important to carefully monitor patients during this period. Hyponatremia associated with a decrease in the secretion of ADH, while receiving escitalopram, occurs rarely and usually disappears when it is canceled. With the development of serotonin syndrome escitalopram should be immediately canceled and symptomatic treatment prescribed. Impact on the ability to drive vehicles and control mechanisms. During the period of treatment, patients should avoid driving vehicles. ort and other activities that require high concentration and speed of psychomotor reactions.