Tsipralex
Tsipralex: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Cipralex
ATX code: N06AB10
Active ingredient: escitalopram (escitalopram)
Manufacturer: H. Lundbeck A / S, Denmark
Description and photo update: 2019-13-08
Prices in pharmacies: from 700 rubles.
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Cipralex is an antidepressant drug, a selective serotonin reuptake inhibitor (SSRI).
Release form and composition
Cipralex is available in the form of film-coated tablets:
- 5 mg: white, round, biconvex, with EK marking (14 pcs. In blisters; 2 packages in a cardboard box);
- 10 mg: white, oval, biconvex, with a line and markings E and L symmetrically around the lines (14 pcs. In blisters; 1, 2 or 4 packages in a cardboard box);
- 20 mg: white, oval, biconvex, with a line and markings E and N symmetrically around the lines (14 pcs. In blisters; 2 packs in a cardboard box).
1 tablet contains:
- active substance: escitalopram (in the form of oxalate) - 5, 10 or 20 mg;
- auxiliary components: croscarmellose sodium, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, talc;
- film shell: macrogol 400, titanium dioxide (E 171), hypromellose 5cP.
Pharmacological properties
Pharmacodynamics
Escitalopram is an antidepressant and selective serotonin reuptake inhibitor (SSRI) with significant affinity for the primary binding site. The substance also binds to the allosteric binding site of the transporter protein, and the affinity is 1000 times less. Allosteric modulation of the transporter protein increases the binding of escitalopram at the primary binding site, which leads to a more complete inhibition of serotonin reuptake.
Escitalopram has little or no ability to bind to some receptors, including α 1-, α 2 - and β-adrenergic receptors, opiate and benzodiazepine receptors, serotonin 5-HT 1A and 5-HT 2 receptors, muscarinic cholinergic and histamine H 1 -receptors, dopamine D 1 and D 2 receptors.
Pharmacokinetics
Escitalopram is absorbed almost completely regardless of food intake. On average, its maximum concentration in blood plasma is reached in 4 hours with repeated administration. The absolute bioavailability of the substance is approximately 80%.
When administered orally, the apparent volume of distribution varies from 12 to 26 l / kg. Escitalopram and its main metabolites bind to blood plasma proteins by less than 80%. The active component of Cipralex is metabolized in the liver, forming demethylated and didemethylated metabolites with pharmacological activity. Nitrogen is capable of being oxidized to an N-oxide metabolite. Escitalopram and its metabolites are partially excreted in the form of glucuronides. With long-term treatment, the content of demethyl- and didemethylmetabolites on average is usually 28–31% and, accordingly, less than 5% of the level of escitalopram in the blood. The biotransformation of the active substance of Cipralex into a demethylated metabolite is carried out mainly through the isoenzyme CYP2C19. Sometimes the isoenzymes CYP2D6 and CYP3A4 are involved in the process. In patientsin which the isoenzyme CYP2C19 is characterized by weak activity, the concentration of escitalopram is 2 times higher than in cases with high activity of this isoenzyme. No significant changes in the content of the compound in blood plasma in cases with low activity of the CYP2D6 isoenzyme were detected.
After repeated administration, the half-life is approximately 30 hours. Oral clearance is approximately 0.6 L / min. The main metabolites of escitalopram are distinguished by a greater prolongation of the half-life. The active component of the drug and its main metabolites are excreted through the kidneys and liver (metabolic method). Most of the administered dose is excreted as metabolites in the urine.
The pharmacokinetics of escitalopram is linear. The equilibrium concentration of the substance is reached in about a week. The average equilibrium concentration is 50 nmol / L (varies from 20 to 125 nmol / L) with a daily dose of 10 mg.
In patients over 65 years of age, escitalopram is excreted at a slower rate than in younger patients. The amount of substance entering the systemic circulation, which is calculated using the pharmacokinetic parameter AUC ("area under the curve"), in elderly patients is 50% higher than in healthy young volunteers.
Indications for use
- social phobia (social anxiety disorder);
- obsessive compulsive disorder;
- depressive episodes of any severity;
- generalized anxiety disorder;
- panic disorder, including agoraphobia.
Contraindications
- age up to 18 years;
- concomitant use of pimozide or non-selective irreversible monoamine oxidase (MAO) inhibitors;
- hypersensitivity to any component of the drug.
According to the instructions, Cipralex should be used with caution in the following cases:
- pronounced suicidal behavior;
- mania and hypomania;
- epilepsy that is not amenable to drug correction;
- bleeding tendency;
- diabetes;
- severe renal failure (creatinine clearance below 30 ml / minute);
- cirrhosis of the liver;
- the period of electroconvulsive therapy;
- pregnancy and lactation;
- elderly age;
- simultaneous use with ethanol; drugs metabolized with the participation of the isoenzyme CYP2C19; oral anticoagulants and drugs that affect blood clotting; tryptophan and lithium; Hypericum perforatum; serotonergic drugs; MAO A inhibitors (eg moclobemide) and MAO B inhibitors (eg selegiline); drugs that can cause hyponatremia or lower the seizure threshold.
Instructions for use of Tsipralex: method and dosage
Cipralex tablets should be taken orally 1 time per day, regardless of meals.
The recommended dosage regimen of Cipralex, depending on the disease / condition:
- social phobia, generalized anxiety disorder: 10 mg each, if necessary, it is possible to increase the daily dose to 20 mg. Improvement usually occurs after 2-4 weeks, but treatment should be continued for at least 3 months. To prevent relapse, the doctor may recommend long-term use of the drug - for 6 or more months;
- depressive episodes: 10 mg each, if necessary, an increase in the daily dose to 20 mg is possible. After the symptoms disappear (usually after 2–4 weeks), treatment is continued for at least 6 months to consolidate the effect obtained;
- obsessive-compulsive disorder: 10 mg, if necessary, it is possible to increase the daily dose to 20 mg. The course of treatment is long - at least 6 months. To prevent relapse, therapy is recommended for at least 1 year;
- panic disorder, including agoraphobia: the initial dose is 5 mg, then it is increased to 10 mg, if necessary, to 20 mg. The duration of treatment is determined individually, but is at least 3 months.
For the elderly, patients with reduced liver function or decreased activity of the CYP2C19 isoenzyme, the initial daily dose of Cipralex (during the first 2 weeks) is 5 mg, the maximum therapeutic dose is 10 mg.
To avoid the onset of withdrawal syndrome, treatment should be discontinued gradually, reducing the dose over 1–2 weeks.
Side effects
Most often, side effects occur in the first or second week of taking Cipralex, and then become less intense, with continued therapy they develop less often.
Possible adverse reactions from organs and systems (on the following scale: very often - ≥1 / 10; often - ≥1 / 100– <1/10; infrequently - ≥1 / 1000– <1/100; rarely - ≥1 / 10000– <1/1000):
- gastrointestinal tract (GIT): very often - nausea; often - diarrhea / constipation, dry mouth, vomiting; infrequently - gastrointestinal bleeding, including rectal;
- immune system: rarely - anaphylactic reactions;
- metabolic and nutritional disorders: often - decrease / increase in appetite, weight gain; infrequently - weight loss; unknown - anorexia, hyponatremia;
- endocrine system: frequency unknown - insufficient secretion of antidiuretic hormone;
- nervous system: often - dizziness, tremors, drowsiness, insomnia, paresthesia; infrequently - syncope, sleep disturbance, taste disturbances; rarely - serotonin syndrome; frequency unknown - akathisia, psychomotor agitation, movement disorders, dyskinesia, convulsive disorders;
- labyrinthine disorders, organ of hearing: infrequently - tinnitus (tinnitus);
- organ of vision: infrequently - visual impairment, mydriasis (dilated pupil);
- psyche: often - unusual dreams, anxiety, anxiety, anorgasmia (in women), decreased libido; infrequently - panic attacks, nervousness, confusion, agitation, bruxism; rarely - depersonalization, aggression, hallucinations; frequency unknown - mania, suicidal thoughts and behavior;
- hepatobiliary system: frequency unknown - functional disorders of liver parameters, hepatitis;
- cardiovascular system: infrequently - tachycardia; rarely - bradycardia; frequency unknown - orthostatic hypotension, prolongation of the QT interval on the electrocardiogram;
- kidneys and urinary tract: frequency unknown - urinary retention;
- connective and musculoskeletal tissue: often - arthralgia, myalgia;
- respiratory system, chest and mediastinal organs: often - yawning, sinusitis; infrequently - nosebleeds;
- blood and lymphatic system: frequency unknown - thrombocytopenia;
- skin and subcutaneous tissue: often - increased sweating; infrequently - rash, urticaria, alopecia, itching; frequency unknown - ecchymosis, angioedema;
- reproductive system and mammary gland: often - violation of ejaculation, impotence; infrequently - menorrhagia, metrorrhagia; frequency unknown - priapism, galactorrhea;
- other reactions: often - hyperthermia, weakness; infrequently - edema.
In patients 50 years and older, additionally taking tricyclic antidepressants, according to the results of epidemiological studies, an increased risk of bone fractures was noted, the mechanism of which has not been established.
In the case of abrupt withdrawal of Cipralex, the development of a withdrawal syndrome is possible, the symptoms of which are: visual disturbances, sleep disorders (including insomnia and intense dreams), confusion, emotional instability, agitation or anxiety, irritability, headache, sensitivity disorders (including paresthesia and sensations of current flow), dizziness, diarrhea, nausea and / or vomiting, palpitations, increased sweating, tremors. These effects, as a rule, are mild to moderate and disappear quickly, but in some patients they can manifest themselves in a more acute form and / or over a long period.
Overdose
There are limited data on overdose of Cipralex. Her symptoms are mostly not manifested or manifested slightly. Cases of escitalopram overdose (against the background of the lack of taking other drugs) with a lethal outcome have been reported in isolated cases.
Signs of an overdose of Cipralex are reactions from the central nervous system (from agitation, tremor and dizziness to individual cases of serotonin syndrome, seizures and coma), the cardiovascular system (arrhythmia, hypotension, prolongation of the QT interval and tachycardia), gastrointestinal tract (nausea and vomiting)). In addition, electrolyte imbalance (hyponatremia, hypokalemia) was noted.
There is no specific antidote. It is necessary to ensure full airway patency, ventilation and oxygenation of the lungs. It is recommended to wash the stomach in the first hours after taking Cipralex and take activated charcoal. Symptomatic and supportive therapy is prescribed, as well as monitoring of the performance of the heart and other vital organ systems.
special instructions
At the beginning of treatment with Cipralex for panic disorders, an increase in anxiety is possible. This reaction usually resolves within 2 weeks. Low starting doses are recommended to reduce risks.
In case of an increase in the frequency of seizures (in patients with epilepsy) or the primary development of seizures, Cipralex should be canceled. In unstable epilepsy, the use of the drug is not recommended; in controlled seizures, careful monitoring of patients is required.
Cipralex is able to influence the concentration of glucose in the blood in patients with diabetes mellitus, which may entail the need to adjust the dose of insulin and / or oral hypoglycemic agents.
Depression is associated with an increased risk of suicidal ideation, self-harm, or suicide. The risk remains until the onset of severe remission, therefore, during the initial period of therapy, patients should be under constant supervision. The same applies to patients with other mental conditions in whom Cipralex is prescribed, and especially patients with a history of suicidal thoughts or attempting suicide.
Patients themselves and their caregivers should be warned about the need for immediate medical attention in case of clinical deterioration, the appearance of suicidal thoughts or behavior, as well as in case of unusual changes in behavior.
For the period of treatment with Cipralex, it is recommended to stop drinking alcohol, refrain from performing potentially dangerous work and driving a car.
Application during pregnancy and lactation
The available information on the use of the drug in pregnant women is currently insufficient. Experiments on the introduction of escitalopram to animals prove the presence of reproductive toxicity. Cipralex during pregnancy should be taken only under strict indications and after a careful assessment of the ratio of potential benefits and probable risks to the mother and the fetus.
If Cipralex was taken late in pregnancy, especially in the third trimester, the newborn should remain under observation for some time. If escitalopram is continued until the onset of labor or the drug is discontinued shortly before labor, the child may develop withdrawal symptoms.
When a mother takes Cipralex in late pregnancy, a newborn may experience the following side effects: poor sleep, drowsiness, irritability, continuous crying, lethargic sleep, high neuro-reflex excitability, tremor, hyperreflexia, muscle hypotension, convulsive disorders, apnea, cyanosis, depression respiratory center, hypertension, temperature surges, hypoglycemia, feeding problems, vomiting. The appearance of such symptoms is due to the serotonergic action of the drug and the development of a withdrawal syndrome. Most of these complications occur within 24 hours after birth.
According to epidemiological studies, the use of Cipralex during pregnancy, especially in late pregnancy, may increase the risk of persistent pulmonary hypertension in newborns (approximately 5 cases per 1000 pregnant women).
Researchers believe that escitalopram is excreted in breast milk, therefore, breastfeeding should be discontinued during treatment with Cipralex.
Drug interactions
- nonselective irreversible MAO inhibitors: a high risk of developing serious adverse reactions, including serotonin syndrome (the break should be 7 days before their appointment and 14 days after their cancellation);
- serotonergic drugs, irreversible MAO B inhibitors, reversible selective MAO A inhibitors: risk of developing serotonin syndrome (not recommended combination);
- lithium, tryptophan: it is possible to enhance the action of escitalopram;
- drugs that lower the seizure threshold (other SSRIs, tricyclic antidepressants, antipsychotics - phenothiazine derivatives, mefloquine, bupropion, butyrophenone, thioxanthene, tramadol): there is a pronounced decrease in the seizure threshold;
- St. John's wort: possible increase in the number of side effects;
- anticoagulants and drugs that affect blood clotting (most tricyclic antidepressants, atypical antipsychotics, phenothiazine derivatives, nonsteroidal anti-inflammatory drugs, acetylsalicylic acid, dipyridamole, ticlopidine): there is a possibility of blood clotting disorders (if necessary, the simultaneous use of blood clotting should be carefully monitored)
- inhibitors of isoenzymes CYP2D6, CYP3A4 and CYP1A2 (for example, cimetidine), inhibitors of isoenzyme CYP2C19 (for example, omeprazole, fluoxetine, lansoprazole, fluvoxamine, ticlopidine, fluoxetine): an increase in the concentration of escitalopram is observed in the blood plasma;
- drugs metabolized with the participation of the isoenzyme CYP2D6 (for example, clomipramine, desipramine, nortriptyline, thioridazine, haloperidol, risperidone), including those with a low therapeutic index (for example, metoprolol, propafenone, flecainide): an increase in the concentration of escitalopram in the blood may be noted correction of its dose);
- drugs metabolized with the participation of the isoenzyme CYP2C19: there is a change in their concentration (care should be taken).
Analogs
Analogues of Tsipralex are: Escitolopram-Teva, Elicea, Selektra, Miracitol.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
The drug is available by prescription.
Reviews about Tsipralex
In most cases, reviews of Cipralex from patients are favorable. The drug allows you to feel the joy of life, get rid of fears, anxiety, worries about trifles, and also cope with phobias of various nature. However, some patients note the presence of unpleasant side effects, among which constant painful agitation, insomnia, and a feeling of weakness are most common.
Many forum visitors claim that potency and / or libido often disappear during treatment, which is expressed in a change in the perception of intercourse, dystonia of the muscles responsible for reproductive functions, erectile dysfunction, etc. The frequency of complaints of such an adverse reaction among men and women turns out to be about the same. Some patients who took Cipralex, on the contrary, like it, because during the period of depression, the satisfaction of biological instincts did not bring joy or moral satisfaction.
Doctors confirm the effectiveness of Cipralex in the conservative treatment of neurological disorders. It is considered a powerful antidepressant and often helps with depression and psychosis that other drugs cannot deal with. Experts believe that side effects are harmless, since they quickly disappear after the drug is discontinued.
Price for Cipralex in pharmacies
The approximate price for Cipralex tablets with a dosage of 10 mg in pharmacy chains is about 921–1120 rubles (per pack of 14 pcs.) Or 1893–2059 rubles (per pack of 28 pcs.). The cost of the drug with a dosage of 20 mg is approximately 3925–4180 rubles (28 pcs per pack).
Tsipralex: prices in online pharmacies
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Drug name Price Pharmacy |
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Cipralex 10 mg film-coated tablets 14 pcs. RUB 700 Buy |
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Cipralex 10 mg film-coated tablets 28 pcs. 1950 RUB Buy |
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Cipralex tablets p.p. 10mg 28 pcs. 2049 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
