medicalmeds.eu Medicines Antidepressant. Ципралекс

Ципралекс

Producer: CJSC ZIO-Zdorovye Russia

Code of automatic telephone exchange: N06AB10

Release form: Firm dosage forms. Tablets.

Indications to use: Depression. Agoraphobia.

General characteristics. Structure:

Active agent: to estsitalopra 5/10/20 of mg

Pharmacological properties:

Pharmacodynamics. Antidepressant, selectively inhibits the return serotonin reuptake; increases concentration of a neurotransmitter in a synaptic gap, strengthens and prolongs effect of serotonin on postsynaptic receptors. Estsitalopram practically does not communicate with serotoninovy (5-HT), dopamine (D1 and D2), alpha and adrenergic, histamine, m-holinoretseptorami, and also benzodiazepine and opiate receptors. The antidepressive effect usually develops in 2-4 weeks after an initiation of treatment. The maximum therapeutic effect of treatment of panic frustration is reached approximately in 3 months after an initiation of treatment.

Pharmacokinetics. Absorption does not depend on meal. Bioavailability - 80%. TCmax is 4 h. The kinetics of an estsitalopram is linear. Css is reached in 1 week. Average Css the 50th nmol/l (from 20 to 125 nmol/l) is reached at a daily dose of 10 mg. The seeming distribution volume - from 12 to 26 l/kg. Communication with proteins - 80%. It is metabolized in a liver to active demetilirovanny and didemetilirovanny metabolites. After repeated use average concentration demetil-and didemetilmetabolit makes 28-31% and less than 5% respectively of concentration of an estsitalopram. Metabolism of an estsitalopram in a demetilirovanny metabolite happens mainly to the help of isoenzymes of P450 cytochrome: CYP2C19, CYPZA4 and CYP2D6. At persons with weak activity of an isoenzyme of CYP2C19 concentration of an estsitalopram can be twice higher, than at persons with high activity of this isoenzyme. Considerable changes of concentration of drug at weak activity of an isoenzyme of CYP2D6 are not noted. T1/2 after repeated use is 30 h. At the main metabolites of an estsitalopram of T1/2 is more long. Clearance - 0.6 l/min. Estsitalopram and his main metabolites are removed by a liver and the most part - kidneys, is partially removed in the form of glucuronides. T1/2 and AUC increases at elderly patients.

Indications to use:

Depression, panic frustration (including with an agoraphobia).

Route of administration and doses:

Inside, regardless of meal. Depressive episodes: on 10-20 mg of 1 times a day. After disappearance of symptoms of a depression, it is necessary to continue therapy for fixing of the gained effect within 6 months. Panic frustration (including with an agoraphobia): on 5 mg/days within the first week, then on 10-20 mg/days. The maximum daily dose - 20 mg. Treatment duration - several months. At the termination of treatment of a doy has to decrease gradually during 1-2 weeks to avoid emergence of a syndrome of "cancellation". At elderly patients (65 years are more senior) the recommended dose - 5 mg/days, the maximum daily dose - 10 mg. At a slight and moderate renal failure of dose adjustment it is not required. The recommended initial dose at reduced function of a liver within the first two weeks of treatment makes 5 mg/days. Depending on individual reaction of the patient the dose can be increased to 10 mg/days. For patients with weak activity of an isoenzyme of CYP2C19 the recommended initial dose within the first two weeks of treatment - 5 mg/days. Depending on individual reaction of the patient the dose can be increased to 10 mg/days.

Features of use:

Estsitalopram it is necessary to appoint only in 2 weeks after cancellation of the MAO irreversible inhibitors and in 24 h after the therapy termination the MAO reversible inhibitor. It is possible to appoint the MAO non-selective inhibitors not earlier than in 7 days after cancellation of an estsitalopram. At some patients with panic frustration in an initiation of treatment estsitalopramy strengthening of alarm which disappears usually during the subsequent 2 weeks of treatment can be observed. To reduce probability of emergence of alarm, it is recommended to use low initial doses. It is necessary to cancel drug in case of development of epileptic seizures or their increase at pharmacological uncontrollable epilepsy. At development of a maniacal state to estsitalopra it has to be cancelled. Estsitalopram can increase concentration of glucose in blood at a diabetes mellitus that can demand correction of doses of hypoglycemic HP. Clinical experience of use of an estsitalopram demonstrates possible increase in risk of implementation of suicide attempts in the first weeks of therapy in this connection it is very important to carry out careful observation of patients during this period. The hyponatremia connected with decrease in secretion of ADG against the background of reception of an estsitalopram arises seldom and usually disappears at drug withdrawal. At development of a serotoninovy syndrome drug has to be the symptomatic treatment is immediately cancelled and is appointed. During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From TsNS: dizziness, weakness, sleeplessness or drowsiness, spasms, tremor, motive disturbances, serotoninovy syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, mania, confusion of consciousness, agitation, alarm, depersonalization, panic attacks, acrimony, visual disturbances.

From the alimentary system: nausea, vomiting, dryness in a mouth, disturbances of flavoring feelings, a loss of appetite, diarrhea, a lock.

From CCC: orthostatic hypotension.

From endocrine system: decrease in secretion of ADG, galactorrhoea.

From urinogenital system: decrease in a libido, impotence, disturbance of an ejaculation, an anorgazmiya (at women), an ischuria.

From integuments: skin rash, itch, ecchymoma, purpura, Quincke's disease.

Allergic reactions: anaphylactic reactions. Laboratory indicators: hyponatremia, change of laboratory indicators of function of a liver.

Others: the increased perspiration, a hyperthermia, sinusitis, an arthralgia, a mialgiya, a syndrome of "cancellation" (dizziness, headaches and nausea).

Interaction with other medicines:

At a concomitant use with MAO inhibitors the risk of development of a serotoninovy syndrome and serious undesirable reactions increases. Combined use with serotonergic HP (including with tramadoly, sumatriptany, etc. triptanes) can lead to development of a serotoninovy syndrome. The concomitant use with the HP reducing a threshold of convulsive readiness increases risk of development of spasms. Strengthens effect of tryptophane and the drugs Li+. Increases toxicity of drugs of a St. John's Wort. Strengthens effect of the HP influencing a blood coagulation (control of indicators of a blood coagulation is necessary). The drugs which are metabolized with participation of the CYP2C19 system (including омепразол), and also being strong CYPZA4 and CYP2D6 inhibitors (including флекаинид, пропафенон, метопролол, desipramine, кломипрамин, нортриптилин, рисперидон, thioridazine, a haloperidol), increase concentration of an estsitalopram. Increases concentration in plasma of desipramine and a metoprolol twice.

Contraindications:

Hypersensitivity, concomitant use of MAO inhibitors, age up to 15 years, pregnancy, the lactation period.

Overdose:

Symptoms: dizziness, tremor, agitation, drowsiness, stupefaction, spasms, tachycardia, changes of an ECG (change of a segment of S-T, T tooth, expansion of the QRS complex, lengthening of Q-T of an interval), arrhythmias, respiratory depression, vomiting, рабдомиолиз, metabolic acidosis, hypopotassemia. Treatment: the symptomatic and supporting, including gastric lavage, adequate oxygenation, control of function cordial сосљдистой and respiratory systems. There is no specific antidote.