Опра®

General characteristics. Structure:

Active agent: a tsitaloprama hydrobromide (it is equivalent to a tsitalopram to the basis) 20 mg and 40 mg
Excipients: Mannitolum, cellulose microcrystallic, silicon oxide colloid anhydrous, magnesium stearate, gipromelloz, titanium dioxide, macrogoal 6000.

Description
Biconvex round tablets, coated white or almost white color with
risky on the one hand.

Pharmacological properties:

Pharmacodynamics. Tsitalopram - antidepressant, from group of the selective serotonin reuptake inhibitors (SSRI).
Tsitalopram having the expressed ability to suppress the return serotonin reuptake, has no or has very weak ability to contact a number of receptors, including histamine, muskarinovy and adrenoceptors. Tsitalopram only in very small degree inhibits P450IID6 cytochrome and, therefore, does not interact with the medicines which are metabolized this enzyme. Thus, side effects and toxic action it is shown in much smaller degree. The antidepressive effect usually develops after 2-4 weeks of treatment. Tsitalopram practically does not exert impact on the carrying-out system of heart and arterial pressure, on hematologic indicators, function of a liver and kidneys, does not cause increase in body weight.
Tsitalopram does not break cognitive functions of the person, does not cause sedation, in pilot studies at drug teratogenic action, influence on reproductive function and perinatal development of posterity is not revealed.
Pharmacokinetics. Bioavailability of a tsitalopram at intake makes about 80% and practically does not depend on meal. The maximum concentration (Tstakh) in plasma is reached in 2-4 hours after reception. Linkng with proteins of plasma - is lower than 80%. In plasma is present at not changed look. At doses of 10-60 mg/days pharmacokinetic parameters have linear dependence. Distribution volume - 12 l/kg. Equilibrium concentration (Css) at daily one-time reception is established in 7-14 days. Gets into breast milk.
It is metabolized by demethylation, deamination and oxidation with P450 cytochrome participation  (isoenzymes   of CYP3A4 and CYP2C19) with education less pharmacological active metabolites.
The elimination half-life (T1/2) of drug makes 1,5 days. Removal is carried out by kidneys and with a stake.
Patients are aged more senior than 65 years
More long biological elimination half-life is observed (1,5-3,75
days) and lower sizes of clearance (0,08-0,3 l/min). Concentration which were observed at an equilibrium state at aged patients exceeded the concentration observed at younger patients receiving the same dose almost twice.
Insufficiency of function of a liver
At patients with reduced function of a liver to tsitalopra it is removed more slowly. The biological elimination half-life of a tsitalopram is almost twice increased and equilibrium concentration of a tsitalopram in plasma are almost twice higher in comparison with patients with normal function of a liver after introduction of the same dose.
Insufficiency of function of kidneys
Removal of a tsitalopram proceeds more slowly at patients with small and average degree of depression of function of kidneys without significant influence on pharmacokinetics. In
the present experience of treatment of patients with heavy insufficiency of function of kidneys (the clearance of creatinine is lower than 20 ml/mol) is insufficient.

Indications to use:

Treatment of depressive diseases and prevention of a recurrence.
Treatment of panic frustration with / or without fear of open space.
Treatment of obsessivno-compulsive frustration (persistence neurosis).

Route of administration and doses:

Drug is accepted inside once a day at any time, or at meal, or on an empty stomach.
Depressions
The recommended daily dose makes 20 mg of a tsitalopram for reception once a day. Depending on the individual response of the patient to treatment and disease severity a dose it is possible to increase a maximum to 60 mg a day.
Panic frustration
It is recommended to apply 10 mg of a tsitalopram to reception once a day within the first week of treatment then the dose is increased to 20 mg a day. Depending on the individual response of the patient to treatment and disease severity a dose it is possible to increase a maximum to 60 mg a day. Obsessivno-kompulsivnye frustration
The recommended daily dose makes 20 mg of a tsitalopram for reception once a day. Depending on the individual response of the patient to treatment it is possible to increase a dose by 20 mg at most to 60 mg a day. Patients at the age of 65 years are also more senior
The recommended initial dose can be increased to 40 mg a day. Impaired renal function
Patients with slightly or moderately an impaired renal function can use drug in usual doses. Information on treatment tsitalopramy patients from heavy
renal failure (clearance of creatinine to 20 ml/min.) is not available. The broken function of a liver
Patients with the broken function of a liver should not appoint more than 30 mg a day.
Treatment duration
Usually antidepressive effect of drug is observed after 2-4 weeks of treatment. Treatment by antidepressants is symptomatic and has to is carried out for an appreciable length of time. Usually for the prevention of a recurrence treatment needs to be carried out within 6 months or even more long span. In case of patients with a periodic (recurrent) depression the supporting treatment needs to be carried out within several years for the prevention of the beginning of the subsequent phases of a disease. In case of completion of treatment drug needs to be cancelled gradually within several weeks.
At treatment of panic frustration the maximum effect of a tsitalopram is observed after  3  months of treatment.  This effect  remains   during  the entire  period of a maintenance therapy.
At treatment of obsessivno-compulsive frustration the effect of drug is shown after 2-4 weeks of treatment; at further continuation of treatment further improvement can be observed.

Features of use:

At development of a maniacal state drug should be cancelled.
Patients with medicinal dependence (including in the anamnesis), need observation and control of drug use.
Treatment by MAO inhibitors can be begun not earlier than in 7 days after the termination of reception of a tsitalopram.
It is necessary to be careful at appointment during feeding as a breast owing to risk of emergence at babies of drowsiness, decrease in a sucking reflex, loss of body weight.
It is required from elderly patients dose declines of a tsitalopram.
Tsitalopram does not influence on intellectual both psychomotor functions and abilities.
Nevertheless, it is recommended to inform the patients accepting psychotropic medicines that their ability to concentrate and show attention can be broken somewhat as a result of their disease or action of the taken medicine, or as a result of a combination of these two factors.

Side effects:

From a nervous system: seldom - an adynamy, increased fatigue, drowsiness or sleeplessness, concern, a tremor, agitation, amnesia, apathy, extrapyramidal effects, change of mood, an agressive behavior, hallucinations, depersonalization, emotional lability, euphoria, a mania, a hypomania, panic behavior, paranoid reaction, psychosis, a serotoninovy syndrome (agitation, confusion of consciousness, diarrhea, a hyperthermia, a hyperreflexia, an ataxy, extraordinary fatigue, a tremor, the increased sweating, excitement, uncontrollable behavior). From a digestive tract: seldom - dryness in a mouth, nausea, vomiting, hypersalivation, a meteorism, diarrhea, an abdominal pain, anorexia.
From cardiovascular system: seldom - bradycardia, decrease in the ABP, orthostatic hypotension, arrhythmia.
From bodies of a hemopoiesis: seldom - thrombocytopenia, bleedings.
From sense bodys: seldom - a mydriasis, accommodation paresis, taste disturbance.
From reproductive system: disturbance of sexual function (disturbance of an ejaculation, decrease in a libido, impotence), disturbances of a menstrual cycle. Allergic reactions: skin rash, it is rare - an epidermal necrosis, rhinitis, sinusitis.

Interaction with other medicines:

Strengthens effect of a sumatriptan and other serotonergic medicines.
Does not influence effect of ethanol, the drugs Li+, benzodiazepines, antipsychotic drugs (neuroleptics), narcotic analgetics, beta adrenoblockers, fenotiazin, tricyclic antidepressants, antihistaminic and gipotenzivy drugs.
In insignificant degree inhibits CYP2D6 cytochrome in this connection poorly interacts with medicines which are metabolized with participation of a tsitalopram.
At a concomitant use with MAO inhibitors development of hypertensive crisis (a serotoninovy syndrome) is possible.
Cimetidinum increases concentration in blood and strengthens effect of a tsitalopram.
At co-administration with warfarin the prothrombin time increases for 5%.

Contraindications:

Hypersensitivity to a tsitalopram or to any component which is a part of drug. Children's age (up to 18 years).
Drug should not be used in combination with inhibitors of a monoaminooxidase (MAO), and also within 14 days after the termination of their reception. Treatment by MAO inhibitors can be begun not earlier than in 7 days after the termination of reception of a tsitalopram. It is not necessary to appoint to tsitalopra to pregnant women and the nursing women if the potential clinical advantage does not prevail over theoretical risk since safety of drug during pregnancy and a lactation at the person is not established. During feeding by a breast emergence at babies of drowsiness, decrease in a sucking reflex, loss of body weight is possible.

With care drug should be used at insufficient function of a liver and/or kidneys, in the presence of convulsive attacks in the anamnesis, at advanced age.

Overdose:

In cases of overdose there can be following signs and symptoms: nausea, dizziness, drowsiness, dysarthtia, sinkhkhevy tachycardia, nodal rhythm, strengthening of a potootdeeniye, cyanosis, tremor, amnesia, confusion of consciousness, disturbance of a heart rhythm and conductivity (lengthening of an interval of QT), рабдомиолиз, spasms, coma.
Treatment:  gastric lavage, symptomatic and maintenance therapy; the specific antidote is absent.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children! Period of validity 4 years. Not to apply on expiry date, specified on packaging.

Issue conditions:

According to the recipe

Packaging:

10 tablets in the blister  from PVC/PVDH / aluminum foil; on 1, 2 or 3 blisters together with the application instruction in a cardboard pack. On 10, 30, 60 blisters together with application instructions in a cardboard box (for hospitals).