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Other names for this medication:Aramix, Celtium, Cipralex, Citoles, Citraz 5, Dexapron, E-zentius, Ectiban, Entact, Escitalopramum, Escitaloprim, Esertia, Esipram, Esita, Esital, Eslorex, Esram, Gaudium, Ipran, Lexamil, Lextor, Losiram, Losita, Meliva, Meridian, Neozentius, Nexcital, Oxapro, Seroplex, Sipralexa, Starcitin es, Tiopram.
The composition of the preparation is equivalent to three basic forms of release from the mass calculation for one tablet of the active substance of oxalate escitalopram – 6.39 / 12.77 / 25.54 mg:
Fine crystalline cellulose (MCC) – 72.49 / 97.49 / 195 mg;
Talcum ordinary 5.04 / 7/14 mg;
Sodium croscarmellose – 3.24 / 4.5 / 9 mg;
Magnesium stearate – 0.9 / 1.25 / 2.5 mg.
The film membrane of the tablets is an important component of the preparation of Cipralex. It consists of:
Hypromellose 5cP – 1.58 / 2.19 / 3.51 mg;
Titanium dioxide (E171) – 0.526 / 0.73 / 1.17 mg;
Macrogol 400 – 0.146 / 0.2 / 0.325 mg.
Form of issue
The preparation is issued in the form of round or oval biconvex tablets of white color, covered with a film membrane with various dosage:
5 mg of the active ingredient (“EC” label) – in a contoured cell package (usually aluminum foil or PVC) 14 tablets, in a carton 2 packs.
Cipralex 10 mg (symmetric marks “E” and “L” relative to the risks on one of the surfaces) – in the blister 14 tablets, 1, 2 or 4 contours in the box.
20 mg of the biologically active component (labeling “E” and “N” on either side of the dash on one side of the tablet) – in the box there are 2 blisters with 14 filled cells.
Cipralex refers to the pharmacological group of potent antidepressants. Due to the biologically active substance, which has an affinity for the allosteric center of the serotonin transfer enzyme, the drug inhibits the reuptake of the neurotransmitter in synaptic structures (the drug has a greater effect on the metabolic pathways of serotonin than on any other messengers). Accordingly, the physiological pulse transmitter is located in the synaptic gap of the neuronal contact for a longer period of time, which causes the enhanced, prolonged action of the postsynaptic membrane.
It should be noted that the drug is strong and long-acting, as it binds in two places with the serotonin transfer enzyme. First of all, the main active ingredient has a high affinity for the primary amino acid sequence of the transporter protein. Also, the components of the Cipralex bind to the allosteric center of the molecule, which again increases the effect of the drug, that is, leads to a more complete inhibition of the reuptake of the neurotransmitter.
Cipralex shows little activity towards such receptors as:
➠Serotonin 5-HT1A and 5-HT2;
➠Dopamine D1 and D2;
➠Alpha and beta adrenergic synapses;
➠Histamine H1 receptor cells;
➠Opioid and benzodiazepine;
Pharmacodynamics and pharmacokinetics
Absorption of the active ingredients does not depend on the intake of food, since the drug is an extremely strong pharmaceutical preparation. Absolute bioavailability is about 80 percent, and the average half-life is 4 hours (however, the parameter can vary depending on individual body parameters and environmental conditions).
LEXAPRO is metabolized in the liver. The constituent elements of the preparation even after oxidation remain biologically active and undergo certain changes in metabolic processes in the form of glucuronides. The metabolites are then sent to the kidneys, which excrete waste drug residues through urine. Clearance with oral administration of the drug is 0.6 l / min.
The kinetics of escitalopram oxalate is described linearly. Equilibrium concentrations in the systemic blood stream, with a daily dose of 10 mg (the optimal amount of active ingredient for an adult), is achieved after one week of a conservative course of treatment with LEXAPRO.
In elderly patients (over 65 years of age), the pharmacological drug is somewhat slower. Clinical trials have shown that during the therapeutic dose, after a single dose of Zipraplex, the amount of active component in the systemic bloodstream of the elderly is 50 percent greater than that of young volunteers.
Indications for use
LEXAPRO is recommended to be included in the conservative treatment regimen if neurological pathologies such as:
➣Long periods of depression of any severity;
➣Panic disorders (which can be explained by agoraphobia – fear of open spaces);
➣Depressive stage of manic-depressive psychosis;
➣Various kinds of social phobias or just anxiety among people;
➣Obsessive-compulsive disorder (medical explanation of “obsession with the idea”);
➣Syndrome of generalized anxiety.
From the pharmacological treatment of LEXAPRO should be abandoned when:
Hypersensitivity or intolerance to the constituent components of the drug;
Childhood and adolescence (the therapeutic course is not recommended to be performed until age 18);
Simultaneous sanation with monoamine oxidase inhibitors (antidepressants) or pimozide (antipsychotic medications);
Acute or chronic renal failure with creatinine clearance below 30 ml / min;
Epilepsy, which is not controlled by pharmacological agents.
Take Cipralex only under the supervision of qualified medical personnel in one of the following situations:
Insulin-independent diabetes mellitus (type I necessarily shows consultation with an endocrinologist);
Cirrhosis, acute or chronic liver failure;
Tendency to frequent hemorrhages due to insufficiency of the blood coagulation system;
Hereditary and acquired metabolic diseases.
Cipralex is a strong drug, because its effect can be characterized by a large number of unwanted reactions from the body. So, for example, are noted:
☞ Dyspeptic disorders (nausea, vomiting, diarrhea, abdominal pain);
☞ Asthenic syndrome (insomnia ordeal, headache, constant fatigue, dizziness);
☞ Metabolic disorders in the form of sweating, hyperthermia and hyponatremia;
☞ Thrombocytopenia and, as a consequence, insufficiency of the blood coagulation system;
☞ Orthostatic collapse or hypotension;
☞ Decrease in reproductive function (decreased libido and potency, both in men and women);
☞ Allergic reactions (a range of undesirable effects affect the manifestations of angioneurotic edema of Quincke, down to anaphylactic shock);
☞ Arthralgia and myalgia of idiopathic genesis, which are not related to the load on the joints or muscles;
☞ Skin rash, purpura, ecchymosis.
It should be noted that the adverse effects of treatment usually occur during the first or second week of the conservative therapeutic course and significantly decrease in manifestations if the sanation is continued according to the plan.
Since the drug belongs to the list of B pharmacological products, then with a sharp discontinuation of Zipraplex after long-term treatment with the drug, withdrawal syndrome is possible. That is, the body lacks an active active substance. This manifests itself in the form of severe headache, irritability, nausea and frequent dizziness.
Instructions for the use of Zipraplex (Method and dosage)
The use of LEXAPRO does not depend on meals a day. The duration and intensity of the course of conservative treatment largely depends on the initial disease:
So to achieve an antidepressant effect, shock doses are used for 2-4 weeks (10 mg of Zipraplex per day for an adult patient) and the next 6 months of maintenance therapy to consolidate the results.
The instructions for Cipralex in panic disorders are very different – they begin pharmacological therapy with 5 mg of the drug with a further increase in the daily dose to 10 mg. Depending on the individual reaction of the body, the amount of the drug can be increased to 20 mg per day. The maximum effect is achieved after 3 months, however, sanation can last up to six months.
In patients with renal or hepatic insufficiency (both acute and chronic), but with absolute indications for the use of LEXAPRO, the maximum single dose is 5 mg. The increase is not recommended, but if the desired therapeutic effect is not achieved, the amount of the drug administered is doubled.
In clinical practice cases of overdose of Zipraplex are known, which usually manifest themselves as follows:
☞ Darkened consciousness, confusion;
☞ Tremor of extremities, violation of fine motor skills;
☞ Convulsive seizures;
☞ Agitation (a strong emotional excitement, which is accompanied by a sense of anxiety and an unreasonable need for movement);
☞ Significant changes in the electrocardiogram (expansion of the ventricular complex, depolarization of the depolarization segment);
☞ Arrhythmias by type of tachycardia;
☞ Metabolic acidosis, hypokalemia;
☞ Oppression respiratory function of the respiratory system.
There is no specific antidote or antagonist of Zipraplex, so the overdose treatment is based on symptomatic and palliative care to the patient. First of all, you should wash the stomach, in order to evacuate from the body are not absorbed the remains of the pharmaceutical product. Further, it is necessary to ensure sufficient oxygenation and constant monitoring of the vital systems of the human body.
It is strictly prohibited simultaneous application of LEXAPRO and drugs that irreversibly inhibit monoamine oxidase, as the percentage of development of severe side effects increases several times (the percentage of respiratory or heart failure is statistically increased).
Based on pharmacological studies, it is not recommended to include in the course of treatment of cipralex and reversible MAO inhibitors because of the risk of serotonin syndrome (potentially deadly situation).
Do not use the drug with escitalopram in parallel with anticoagulants or drugs that reduce blood clotting, as this can lead to severe hemorrhagic syndrome and anemia, as an outcome of the pathological situation, which will complicate the patient’s treatment.
There are a number of pharmaceuticals that interact with the allosteric centers of carrier proteins to increase the activity of Cipralex. For example, omeprazole (against ulcer drug) leads to an increase in the concentration of active substance in the systemic circulation twice, and cimetidine (the blocker of H2-histamine receptors, which is prescribed in the pathology of the gastrointestinal tract) – by 70%.
Serotonin reuptake inhibiting agents, and Cipralex, as a typical representative of this pharmacological group, reduce the threshold of convulsive activity, that is, tremor and / or convulsive syndrome may manifest itself to less intense stimulation. This action will be potentiated if Cipralex and other strong antipsychotics (neuroleptics) are taken concomitantly, for example, Tramadol, Phenothiazine, Butirofenone, and so on.
The drug should be stored in a warm, dry place, inaccessible to children of all ages and direct rays of light at a temperature of no higher than 25 degrees Celsius.
Cipralex does not exert a depressing effect on the intellectual or psychomotor sphere of the patient, however, while continuing the course of conservative treatment, it is recommended to refuse driving the car or controlling technical devices that require a long concentration of attention and fine motor skills.
The drug can contribute to a change in the concentration of glucose (a significant increase in it) and insulin (a relative decrease in the hormone) in the systemic blood stream, and accordingly this treatment requires a certain correction of hypoglycemic agents in patients with diabetes mellitus.
Therapy with antidepressants can lead to suicidal thoughts in the early stages of the sanation course. Increased risk of self-injury, suicidal tendencies remain until the remission of the underlying disease, therefore, conservative treatment with LEXAPRO should be carried out in special departments under the supervision of qualified medical personnel.
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