Siozam

General characteristics. Structure:

Active agent: a tsitaloprama hydrobromide ( in terms of tsitalopra) — 20 mg or 40 mg; excipients: starch corn, lactoses monohydrate (sugar milk), povidone (polyvinylpirrolidone 25000), глицерол (glycerin), magnesium stearate; structure of a cover: Опадрай II (gipromelloz (gidroksipropilmetiltsellyuloz), lactose monohydrate, macrogoal (polyethyleneglycol 4000), titanium dioxide).

Pharmacological properties:

Pharmacodynamics. Tsitalopram — the antidepressant relating to group of the selective serotonin reuptake inhibitors (SSRI). 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 in very small degree inhibits P450IID6 cytochrome and, therefore, does not interact with the medicines which are metabolized this enzyme (the risk of development of side effects and toxic action is lower). 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 makes about 80% and practically does not depend on meal. The maximum concentration (Tcmax) in plasma is reached in 2–4 hours after reception. Linkng with proteins of plasma — less 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 (1,5–3,75 days) and lower sizes of clearance (0,08–0,3 l/min) is observed. 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.

Indications to use:

Depression of various etiology, treatment and prevention. Panic frustration (in t.   h with an agoraphobia). Obsessivno-kompulsivnye frustration (persistence neurosis).

Route of administration and doses:

Inside, once a day , at any time, irrespective of meal. Depressions the Recommended daily dose of Siozam makes 20 mg. Depending on the individual response of the patient to treatment and disease severity the dose can be increased. The maximum daily dose makes 60 mg. Panic frustration the Recommended daily dose of Siozam — 10 mg  within the first week of treatment then the dose is increased to 20 mg a day. The maximum daily dose makes 60 mg. Obsessivno-kompulsivnye frustration the Recommended daily dose of Siozam — 20 mg. Depending on the individual response of the patient to treatment and disease severity the dose can be increased. The maximum daily dose makes 60 mg. Patients at the age of 65 years are also more senior the Maximum daily dose makes no more than 40 mg. An impaired renal function Patients with slightly or moderately an impaired renal function can use drug in usual doses. Now experience of treatment of patients with heavy insufficiency of function of kidneys (the clearance of creatinine is lower than 20 ml/mol) is insufficient. 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 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 Siozam it is necessary to cancel 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. To patients with medicinal dependence (in t.   h in the anamnesis), observation and control of drug use is required. 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. The dose decline of a tsitalopram is required from elderly patients. Tsitalopram usually 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, drowsiness or sleeplessness, concern, a tremor, agitation, amnesia, apathy, extrapyramidal effects, change of mood, an agressive behavior, depersonalization, emotional lability, euphoria, maniacal and/or psychotic (in t.   h hallucination) frustration, panic reactions, serotoninovy syndrome (agitation, confusion of consciousness, diarrhea, hyperthermia, hyperreflexia, ataxy).
From a digestive tract: seldom — dryness in a mouth, nausea, vomiting, hypersalivation, a meteorism, diarrhea, an abdominal pain, anorexia.
From cardiovascular system: seldom — bradycardia, a lowering of arterial pressure (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.
Others: seldom — a hyperthermia, a polyuria, a mastodynia, галакротея, a hyponatremia, disturbance of an urination, an arthralgia, a mialgiya, yawning, a gnash teeth, increase or decrease in body weight, диспноэ.

Interaction with other medicines:

Strengthens effect of a sumatriptan and other serotonergic medicines. Does not influence effect of ethanol, drugs of lithium, 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 its participation. 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; simultaneous use with inhibitors of a monoaminooxidase (MAO), and also within 14 days after the termination of their reception; children's age (efficiency and safety of use are not established). Treatment by MAO inhibitors can be begun not earlier than in 7 days after the termination of reception of a tsitalopram.

With care drug should be used at insufficient function of a liver and/or kidneys, in the presence of convulsive attacks in the anamnesis, to patients 65 years are more senior.  Tsitalopra should not appoint pregnancy and the period of a lactation to pregnant women and the nursing women if the potential clinical advantage does not prevail over theoretical risk, t.   to. safety of drug during pregnancy and a lactation at the person is not established.

Overdose:

Symptoms: nausea, dizziness, drowsiness, dysarthtia, disturbance of a heart rhythm and conductivity (lengthening of an interval of QT, sinus tachycardia, nodal rhythm), sweating strengthening, cyanosis, tremor, amnesia, confusion of consciousness, рабдомиолиз, spasms, coma. Treatment: gastric lavage, symptomatic and maintenance therapy; the specific antidote is absent.

Storage conditions:

 List B. In dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity 2 years. Not to apply after expiry date.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 20 mg and 40 mg. On 10 or 14 tablets in a blister strip packaging. 14, 28 or 56 tablets in bank of light-protective glass or bank polymeric, or a bottle polymeric. Each can or a bottle, 1, 2 or 4 blister strip packagings together with  the application instruction are placed in a pack.