Tsipraleks

Description overdue on 05/06/2014

• Latin name: Cipralex
• ATC code: N06AB10
• Active substance: Escitalopram (Escitalopram)
• Manufacturer: H. Laundbek A / S (Denmark)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use Tsipraleksa (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• With alcohol
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

Formulation is an equivalent to the three main forms of release (see. The following paragraph) of the mass per tablet active substance escitalopram oxalate   - 6.39 / 12.77 / 25.54 mg:

• fine crystalline cellulose (MCC) - 72.49 / 97.49 / 195 mg;
• talc ordinary 5.04 / 7/14 mg;
• sodium Valium - 3.24 / 4.5 / 9 mg;
• magnesium stearate - 0.9 / 1.25 / 2.5 mg.

Film-coated tablets is an important component of the drug Tsipraleks. It consists of:

• Valium 5sR - 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.

Product form

The drug comes in the form of round or oval biconvex white tablets, film-coated with different dosages:

• 5 mg of active substance (labeled " European Commission ') - In blisters (typically made of aluminum foil, or PVC) of 14 tablets, in a cardboard box 2 packaging.
• Cipralex 10 mg (symmetric mark " E "And" L "Relative risks on one surface) - 14 tablets in a blister, 1, 2 or 4 units per box.
• 20 mg of the active ingredient (labeled " E "And" N "On both sides of the lines on one side of the tablet) - 2 blisters in a box filled with 14 cells.

Pharmacological action

Tsipraleks refers to a group of potent pharmacological Antidepressants . Thanks to a biologically active substance that has an affinity to the allosteric site of the enzyme-carrier Serotonin , The drug inhibits the reuptake of the neurotransmitter in synaptic structures   (drug increasingly affects serotonin pathways, than any other messengers). Accordingly physiological impulse transmitter is in contact neuronal synaptic cleft longer period of time, which causes increased, a prolonged effect on postsynaptic membrane .

It should be noted that the preparation is strong and long-acting, as bound in two places to an enzyme-serotonin transporter. First of all, the main active component has High affinity to the primary amino acid sequence of the protein transporter. Also components Tsipraleksa bind to an allosteric center of the molecule that enhances the action of a second drug, i.e. results in a more complete inhibition of neurotransmitter reuptake.

Tsipraleks exhibits weak activity 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;
• m-cholinergic receptors.

Pharmacodynamics and pharmacokinetics

Absorption of the active ingredients is independent of food intake, since the drug is extremely strong pharmaceuticals. Absolute bioavailability   of about 80 percent, and the average   half life   - 4 hours (although the parameter can vary depending on the individual state of the organism and the environmental conditions).

Tsipraleks metabolized in the liver . Components of the drug even after oxidation remain biologically active and undergoing some changes in metabolic processes are allocated in the form glucuronide . Further metabolites are sent to the kidneys, which excrete   waste residue of the drug through the urine. The clearance of the drug when administered orally is 0.6 l / min.

Kinetics escitalopram oxalate   described linearly. The equilibrium concentration in the systemic circulation, at a daily dose of 10 mg (optimum amount of the active ingredient for an adult) is achieved after one week of treatment Tsipraleksom conservative.

In elderly patients   (over 65 years), pharmacological drug appears somewhat slower. Clinical trials have shown that during therapeutic bite after a single dose Tsipraleksa amount of active ingredient into the systemic circulation of elderly people by 50 percent more than in young volunteers.

Indications

Tsipraleks recommended for inclusion in the scheme of medical treatment, if there are neurological disorders such as:

• prolonged periods depression   any severity;
• panic disorders   (which may be due to agoraphobia - fear of open spaces);
• depressive stage manic-depressive psychosis ;
• Various types of social phobias   or just anxiety among the people;
• obsessive compulsive disorder   (medical explanation " obsession ");
• neurosis   obsessive-compulsive disorder;
• generalized anxiety syndrome.

Contraindications

From pharmacological treatment is to give Tsipraleksom at:

• hypersensitivity   or intolerance   to the constituent components of the drug;
• childhood and adolescence (therapeutic course is not recommended to spend up to 18 years);
• simultaneous rehabilitation inhibitors monoamine oxidase   (antidepressant) or P imozidom   (antipsychotic medicinal products);
• acute or chronic renal failure   with lower creatine clearance of 30 mL / min;
• epilepsy Which is not controlled by pharmacological means.

Take Tsipraleks only under the supervision of qualified medical personnel should be one of the following situations:

• non-insulin diabetes   (at I necessarily show the type of consultation with an endocrinologist);
• old age;
• cirrhosis , Acute or chronic liver failure ;
• propensity to frequent hemorrhage   due to lack of blood coagulation;
• hereditary and acquired metabolic diseases .

Side effects

Tsipraleks - a strong drug, because its effect may be characterized by a large number of adverse reactions on the part of the body. Thus, for example, says:

• dyspepsia   ( nausea . vomiting . diarrhea , stomach ache);
• asthenic syndrome ( insomnia   or drowsiness , Headaches, constant fatigue, dizziness );
• metabolic disorders in the form of sweating . Hyperthermia   and hyponatremia ;
• thrombocytopenia and as a consequence of failure of blood coagulation;
• Orthostatic hypotension   or hypotension ;
• reduce reproductive function ( decreased libido   and potency In both men and women);
• allergic reactions (range of undesirable effects affect manifestations of angioneurotic angioedema , up to anaphylactic shock );
• arthralgia   and myalgia idiopathic origin That are not associated with the load on the joints or muscles;
• skin rash . purpura . ecchymosis .

It should be noted that the adverse effects of treatment usually appear on the first or second week of conservative therapy and significantly slow down the course in the forms, if we continue to reorganize for a given plan.

Since the drug is to list B of pharmaceutical products, the discontinuation of the sudden Tsipraleksa after a long drug treatment, it is possible withdrawal . That is, the body lacks the existing active substance. This is manifested in the form of a severe headache, irritability, nausea and frequent dizziness.

Instructions for use Tsipraleksa (method and dosage)

Using Tsipraleksa independent of meals during the day. The duration and intensity of the course of conservative treatment depends largely on the initial disease:

• So in order to achieve antidepressant effect   used shock doses for 2-4 weeks (Tsipraleksa 10 mg per day for an adult patient) and the next six months of maintenance therapy to consolidate the obtained results.
• Instructions on when Tsipraleks panic disorders   It differs - start pharmacological therapy with 5 mg of the drug to a further increase in the daily dose to 10 mg. Depending on the individual reactions, the amount of drug can be increased to 20 mg per day. The maximum effect is achieved after 3 months, but can take up rehabilitation of six months.
• Patients with kidney   or hepatic insufficiency   (both acute and chronic), but the absolute indications for primene6niyu Tsipraleksa maximum single dose of 5 mg. The increase is not recommended, but if the desired therapeutic effect is achieved, the amount administered is doubled.

Overdose

In clinical practice, there are cases of overdose Tsipraleksa which usually manifest as follows:

• pomrachёnnoe consciousness soporose ;
• tremor of the extremities , Breach of fine motor skills;
• seizures ;
• agitation   (strong emotional arousal, which is accompanied by a sense of anxiety and unreasonable demand on the move);
• significant changes in the electrocardiogram (expansion of the ventricular complex, depolarization depolarization segment);
• Arrhythmia   type tachycardias ;
• metabolic acidosis . hypokalemia ;
• inhibition of the respiratory function of the respiratory system.

Specific antidote or antagonist Tsipraleksa does not exist, therefore treatment of overdose is based on symptomatic and palliative care patient. The first thing to wash out the stomach, in order to evacuate the body not The absorbed the remnants of the pharmaceutical preparation. Next, you need to provide sufficient oxygenation and continuous monitoring of the vital systems of the human body.

Cooperation

Simultaneous use is strictly forbidden Tsipraleksa and drugs that irreversibly inhibits monoamine oxidase As the percentage of severe side effects increases several times (statistically increased percentage respiratory   or Heart Failure ).

On the basis of pharmacological studies is not recommended in the treatment and Tsipraleks reversible inhibitors of MAO   due to the risk of serotonin syndrome (a potentially deadly situation).

Do not use the drug with escitalopram   parallel   anticoagulants   or drugs lowering blood coagulation As this may lead to serious hemorrhagic syndrome   and anemia As the outcome of a pathological situation that complicates the treatment of the patient.

There are a number of pharmaceutical drugs that interact with allosteric centers of carrier proteins   increase the activity of Tsipraleksa. For example, Omeprazole   (anti-ulcer drug) leads to an increase in the concentration of active substance in the systemic circulation twice, and Cimetidine   (blocker H2-histamine receptors, which is assigned in the pathology of the gastrointestinal tract) - 70%.

Means of inhibiting the reuptake Serotonin And Tsipraleks as a typical representative of this pharmacological group, lowers the threshold for seizure activity, that is, tremor   and / or convulsions   It may appear less intense excitement. This action will be potentiated when taking simultaneous Tsipraleks other strong antipsychotic agents ( neuroleptics ), eg Tramadol, phenothiazines, butyrophenones   and so on.

Terms of sale

Sold only signed by a doctor receptor forms because the drug is a potent and is included in the B list of medications.

Storage conditions

The drug should be stored in a warm, dry place, away from children of all ages, and direct light at a temperature no higher than 25 degrees Celsius.

Shelf life

3 years.

Cautions

Tsipraleks has no inhibitory effect on psychomotor or intellectual sphere of the patient, but is continuing a course of conservative treatment is recommended to give up driving or control of technical devices, which require long-term concentration and fine motor skills.

The drug can help to change glucose   (significant increase her) and insulin   (relative reduction hormone) in the systemic circulation, and therefore the treatment requires a certain correction hypoglycemic agents in patients with diabetes .

Treatment with antidepressants can lead to suicidal thoughts in the early stages of the course sanation. Autographic increased risk of injury, suicidal saved until remission of the underlying disease, because Tsipraleksom conservative treatment should be carried out in special departments under the supervision of qualified medical personnel.

Analogs Tsipraleksa

Match code ATC 4th level:

• Paxil
• Reksetin
• Luvox
• Fluoxetine

Currently, the pharmacy shelves can be found the following analogues Tsipraleksa:   Estsitolopram-Teva, selectors, Elitseya, Miratsitol .

Synonyms

Escitalopram (Escitalopram) .

Tsipraleks and alcohol

According to pharmaceutical research, alcohol does not come with the active ingredients of the drug in the chemical reaction and does not modulate its effects, however, as is the case with other substance, it is not recommended their simultaneous use.

During pregnancy and lactation

Tsipraleks strictly contraindicated for use during pregnancy and lactation.

Reviews Tsipralekse

Those who drank Tsipraleks, the vast majority are satisfied with the effects of conservative treatment. The drug does help to cope with phobias of various origins, it allows to live a fuller life, not limited by fear, anxiety, or feelings of trifling occasions. However, reviews are often overshadowed by taking personal experiences of adverse reactions. Very often celebrated broken state . insomnia . constant painful excitement .

Also reviews of Tsipralekse forums say that in most cases completely disappeared libido   and / or potency   ( erectile dysfunction . dystonia,   responsible for reproductive functions, changing perception intercourse and so on). At the side effect of an equal amount of complaining and men and women. What's interesting is that the reviews taking antidepressants are filled with gratitude and preparations for the reduction of desire, as the satisfaction of animal instincts did not bring joy or welcome relief during the Depression.

Doctors about Tsipralekse primarily clinically and statistically confirm the efficacy of the drug in the conservative treatment Neurological Disorders . Antidepressant such strength to cope with depression and psychoses, where more sparing techniques do not bring absolutely no result. Side effects are perceived by experts as necessary loss, because undesirable effects come to naught after the full course of rehabilitation.

Price Tsipraleksa

Price Tsipraleksa, of course, depends on the dosage of the active ingredient. Buy in Moscow can be over 900/1400/1800 rubles, respectively 5/10/20 mg of active substance. In Ukraine, the cost of antidepressant varies from 270 to 500 hryvnia, but the vast majority of pharmacies sell the drug for $ 400 hryvnia.

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