CIPRALEKS
Active material: Escitalopram
When ATH: N06AB10
CCF: Antidepressant
ICD-10 codes (testimony): F31, F32, F33, F40, F41.0, F41.1, F41.2
When CSF: 02.02.04
Manufacturer: H.LUNDBECK A/S (Denmark)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Pills, coated white, convex, round, diameter 6 mm, labeled “EC”; of presentations – core and Shell white.
| 1 tab. | |
| escitalopram (in the form of oxalate) | 5 mg |
Excipients: talc, sodium croscarmellose, microcrystalline cellulose, silica colloidal anhydrous, magnesium stearate.
The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171).
14 PC. – blisters (2) – packs cardboard.
Pills, coated white, convex, Oval (8 mm x 5.5 mm), with Valium, labeled “E” and “L” symmetrically about the risks; of presentations – core and Shell white.
| 1 tab. | |
| escitalopram (in the form of oxalate) | 10 mg |
Excipients: talc, sodium croscarmellose, microcrystalline cellulose, silica colloidal anhydrous, magnesium stearate.
The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171).
14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.
14 PC. – blisters (4) – packs cardboard.
Pills, coated white, convex, Oval (11.5 mm x 7 mm), with Valium, labeled “E” and “N” symmetrically about the risks; of presentations – core and Shell white.
| 1 tab. | |
| escitalopram (in the form of oxalate) | 20 mg |
Excipients: talc, sodium croscarmellose, microcrystalline cellulose, silica colloidal anhydrous, magnesium stearate.
The composition of the shell: gipromelloza, macrogol 400, Titanium dioxide (E171).
14 PC. – blisters (2) – packs cardboard.
Pharmacological action
Antidepressant, selective serotonin reuptake inhibitor (SSRIs). Serotonin reuptake inhibition leads to increased concentrations of the neurotransmitter in the synaptic junctions, enhance and prolong the effect on postsynaptic receptor sites.
Escitalopram has no or very little has the ability to communicate with a number of receptors, including: serotoninove 5-HT1A-, 5-HT2-receptors, dopamine D1– and D2– receptors, a1-, a2-, β-adrenergic receptor, gistaminove n1-receptors, m-cholinergic receptors, benzodiazepine and opioid receptors.
Pharmacokinetics
Absorption
Absorption does not depend from taking screaming. Bioavailability is about jescitaloprama 80%. The average time to achieve Cmax in plasma is 4 hours after repeated use.
Distribution
Linking jescitaloprama and its major metabolites in blood plasma proteins below 80%.
In Кажущийсяd following oral administration ranged from 12 to 26 l / kg.
Эstsitaloprama linear kinetics.
Css It reached approximately 1 week. Average Css 50 nmoli / (from 20 to 125 nmoli /) achieved with a daily dose of 10 mg.
Metabolism
Escitalopram is metabolized in the liver to demetilirovannogo and didemetilirovannogo metabolites, which are pharmacologically active. Main substance and its metabolites are excreted in the form of glukuronidov partially.
After repeated use of the average concentration of demethyl- and didemetil-metabolites is typically 28-31% less 5% respectively from the concentration of escitalopram. Biotransformation of jescitaloprama in demetilirovannyj metabolite occurs mainly with the participation of izofermenta CYP2C19. Perhaps some part of isoenzymes CYP3A4 and CYP2D6. Persons CYP2C19 activity with low concentration of jescitaloprama in 2 times higher, than in cases with high activity this izofermenta. Significant changes in the concentration of the drug in cases with weak activity izofermenta CYP2D6 has been detected.
Deduction
T1/2 After repeated use is about 30 no. Clearance of oral application is about 0.6 l / min. The main metabolites of jescitaloprama T1/2 more long lasting. Escitalopram and its main metabolites are excreted by the liver (metabolic pathway) and kidneys. Most of the displays in the form of metabolites in urine.
Pharmacokinetics in special clinical situations
In the elderly (senior 65 years) escitalopram is excreted more slowly, than in younger patients. Amount of substance, located in the systemic blood, calculated using the AUC for elderly 50% better, than in young healthy volunteers.
Testimony
-depressive episodes of any degree of severity;
-panic disorder with or without agoraphobia;
-social anxiety disorder (social phobia);
- Disorder generalized anxiety.
Dosage regimen
Cipraleks assign 1 times / day, regardless of the meal.
At depressive episodes the drug is usually prescribed in a dose 10 mg / day. Depending on the individual reactions of the patient dose can be increased up to a maximum – 20 mg / day.
The antidepressant effect usually develops within 2-4 weeks after initiation of treatment. After the disappearance of the symptoms of depression at least within 6 months of therapy must continue to consolidate the obtained effect.
At panic disorder with or without agoraphobia during the first week of treatment recommended dose 5 mg/day, followed by an increase to 10 mg / day. Depending on the individual reactions of the patient dose can be increased up to a maximum – 20 mg / day.
Maximum therapeutic effect is achieved after approx. 3 months after initiation of treatment. Therapy lasts a few months.
At social alarming disorder (social phobia) appointed 10 mg 1 time / day. The easing of symptoms usually is a 2-4 weeks after initiation of treatment. Depending on the individual reactions of the patient dose can subsequently be reduced to 5 mg/day or increased to a maximum of – 20 mg / day.
Because social anxiety disorder is an illness with chronicity, the minimum recommended duration of therapeutic course is 12 weeks. To prevent recurrence of the disease, the drug may be prescribed for 6 months or longer depending on the individual patient's response.
At generalized anxiety disorder The recommended starting dose – 10 mg 1 time / day. Depending on the individual reactions of the patient dose can be increased up to a maximum – 20 mg / day. Allowed the prolonged use of the drug (6 months and longer) dose 20 mg / day.
In elderly patients (senior 65 years) We recommend that you use half usually recommended dose (ie. Total 5 mg / day) and a lower maximum dose (10 mg / day).
At renal insufficiency of mild to moderate severity dose adjustment is required. Patients with severe renal insufficiency (CC<30 ml / min) the drug should be used with caution.
At mild to moderate hepatic insufficiency the recommended initial dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to treatment dose can be increased to 10 mg / day. At expressed liver failure Use caution when titration.
With reduced activity of izofermenta CYP2C19 recommended initial dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to treatment dose can be increased to 10 mg / day.
Upon termination of the treatment Cipraleksom dose should be reduced gradually during the 1-2 weeks in order to avoid the development of syndrome.
Side effect
Side effects most often develop on 1 or 2 week of treatment and then usually become less intense and occur less frequently with continued therapy.
CNS: insomnia or drowsiness, dizziness; rarely – breach of taste sensations, and insomnia.
The respiratory system: sinusitis, zevota.
From the digestive system: nausea, diarrhea, constipation, decreased appetite.
For the skin: increased sweating.
On the part of the reproductive system: decreased libido, anorgazmija (female), impotence, abnormal ejaculation.
From the body as a whole: weakness, hyperthermia.
When taking medications, belonging to the class of SSRI, incl. and Cipraleksa, also possible:
Metabolism: giponatriemiya, inadequate secretion of antidiuretic hormone (ADG).
From the central and peripheral nervous system: hallucinations, craze, confusion, ažitaciâ, alarm, depersonalization, panic attacks, irritability, insomnia, dizziness, drowsiness, seizures, tremor, movement disorders, serotonin syndrome, visual disturbances.
Cardio-vascular system: orthostatic hypotension.
From the digestive system: vomiting, dry mouth, anorexia, changes in laboratory parameters of liver function.
For the skin: skin rash, itch, ecchymosis, angioedema, increased sweating.
On the part of the musculoskeletal system: arthralgia, myalgia.
On the part of the reproductive system: galactorrhea, impotence, abnormal ejaculation, anorgazmija.
From the urinary system: urinary retention.
From the body as a whole: anaphylactic reactions.
Besides, After an abrupt end to the prolonged use of Cipraleksom therapy in some patients may cause reactions cancel. In a dramatic admission jescitaloprama might encounter such undesirable reactions, as dizzy, headaches and nausea, the severity of which is insignificant, and duration – limited. To avoid reactions cancel recommended phasing out of medication for 1-2 weeks.
Contraindications
- Simultaneous MAO inhibitors;
- Pregnancy;
- Lactation (breast-feeding);
- Childhood and adolescence up 15 years;
-hypersensitivity to jescitalopramu and other components of the drug.
Pregnancy and lactation
Cipralex is contraindicated for use during pregnancy and lactation. (breast-feeding).
The use of selective serotonin reuptake inhibitors in the third trimester of pregnancy may have a negative impact on the development of psychophysical newborn. The following violations are registered in newborns, whose mothers took selective serotonin reuptake inhibitors until delivery: irritability, tremor, hypertension, increased muscle tone, constant crying, difficulty sucking, bad dream. Abnormalities may indicate serotonergic effects or withdrawal symptoms. In the case of the use of selective serotonin reuptake inhibitors during pregnancy, their intake should not be abruptly interrupted.
Cautions
Escitalopram you cannot assign simultaneously with MAO inhibitors. Escitalopram can be assigned through 14 days after stopping treatment irreversible MAO inhibitors and at least 1 day after cessation of therapy with a reversible MAO inhibitor type A, incl. moclobemide. Least 7 days should pass after the end of taking escitalopram, before starting treatment with non-selective MAO inhibitors.
Some patients with panic disorder at the beginning of treatment, selective serotonin reuptake inhibitors (including escitalopram) You may experience increased anxiety. This paradoxical reaction usually disappears within 2 weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommended to use the drug in low initial doses.
Escitalopram should be discontinued if seizures develop. It is not recommended to use the drug in patients with unstable epilepsy.; controlled seizures require close monitoring. With an increase in seizure frequency, selective serotonin reuptake inhibitors, including escitalopram, should be abolished.
Escitalopram should be used with caution in patients with a history of mania / hypomania.. With the development of a manic state, escitalopram should be canceled.
When treating patients with diabetes mellitus escitalopram may change the level of glucose in the blood. Therefore, dose adjustment of insulin and / or oral hypoglycemic drugs may be required.
The risk of suicide is typical of depression and could persist until significant improvement of, coming spontaneously or as a result of therapy. Careful monitoring of patients, treated with antidepressants, especially at the beginning of treatment due to the possibility of clinical deterioration and / or the appearance of suicidal manifestations (thoughts and behavior). This precaution must be observed when treating other psychiatric disorders due to the possibility of a concurrent depressive episode..
Giponatriemiya, possibly associated with impaired secretion of ADH, while taking escitalopram occurs rarely and usually disappears when therapy is discontinued. Caution should be given to escitalopram and other selective serotonin reuptake inhibitors in patients, at risk of developing hyponatremia: seniors, patients cirrhosis of the liver and receiving drugs, can cause giponatriemia.
When receiving jescitaloprama may develop skin hemorrhages (ecchymosis and Purpura). It is necessary to use escitalopram with caution in patients with a tendency to bleeding., as well as those taking oral anticoagulants and medications, affecting blood coagulation.
Limited clinical experience with escitalopram in combination with electroconvulsive therapy, so be careful in this case.
The simultaneous use of escitalopram and MAO inhibitors type A is not recommended due to the risk of developing serotonin syndrome.
Patients, taking escitalopram and other selective serotonin reuptake inhibitors concurrently with serotonergic drugs, in rare cases can develop serotonin syndrome. You need to be wary of escitalopram concurrently with drugs, with serotonergic action. A combination of these symptoms, how agitation, tremor, myoclonus, hyperthermia, may indicate the development of serotonin syndrome. If this happens, selective serotonin reuptake inhibitors and serotonergic drugs should be discontinued immediately and symptomatic therapy should be prescribed.
Use in Pediatrics
Antidepressants should not be prescribed children and adolescents under the age of 18 years due to an increased risk of suicidal behavior (suicidal attempts and thoughts), hostility (with a predominance of aggressive behavior, propensity for confrontation and irritation). In the case of a decision concerning the beginning of antidepressant therapy, the patient should be under close supervision.
Effects on ability to drive vehicles and management mechanisms
Although escitalopram does not affect psychomotor activity, during the period of treatment, it is not recommended to drive a car or machinery.
Overdose
Symptoms: dizziness, tremor, ažitaciâ, drowsiness, darkening of consciousness, seizures, tachycardia, ECG changes (change in ST segment and T wave, extension of the QRS complex, QT prolongation), Arrhythmia, respiratory depression, vomiting, raʙdomioliz, metabolic acidosis, kaliopenia.
Treatment: There is no specific antidote. Treatment is symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems.
Drug Interactions
Pharmacodynamic interactions
If you are applying with Cipraleksa MAO inhibitors, and also at the beginning of the admission of MAO inhibitors sick, shortly before that have separated reception Cipraleksa, possible serious adverse reactions. In such cases, serotonin syndrome may develop..
Combined use of Cipralex with serotonergic drugs (eg, tramadol, sumatriptan and other triptans) It can lead to serotonin syndrome.
Cipralex may lower the seizure threshold. Caution is required with the simultaneous appointment of Cipralex and other drugs, lowering the seizure threshold (tricyclic antidepressants, SSRIs, antipsychotics-phenothiazines, thioxanthenes and butyrophenones, mefloquine and tramadol).
Since there have been cases of increased action with the joint appointment of Cipralex and lithium or tryptophan, are advised to be cautious while appointing these drugs.
The simultaneous appointment Cipraleksa and drugs, containing St. John's wort (Hypericum perforatum), can lead to an increase in side effects.
Together with the appointment of jescitaloprama with antikoagulyantami and drugs, affect blood coagulation (eg, atypical antipsihotikami and fenotiazinami, the majority of the tricyclic antidepressants, acetylsalicylic acid and NSAIDS, Ticlopidine, and dipyridamole), blood clotting can occur. In such cases, at the beginning or at the end of the therapy jescitalopramom required careful monitoring of blood coagulability.
While admission alcohol escitalopram no pharmacodynamic or pharmacokinetic interaction. But, as with other psychotropic substances, the simultaneous use of jescitaloprama and alcohol is not recommended.
Pharmacokinetic interactions
The simultaneous use of jescitaloprama and omeprazole dose 30 mg 1 time / day (izofermenta inhibitors 2s19 cytochrome p 450) leads to moderate (about 50%) increased concentrations of jescitaloprama in plasma.
Simultaneous reception jescitaloprama and cimetidine in the dose 400 mg 2 times / day (inhibitor, izofermentov 2 d 6, 3A4, 1A2 cytochrome P450) leads to increased (about 70%) jescitaloprama concentration in the blood plasma.
Thus, escitalopram, caution should be appointed simultaneously with inhibitors izofermenta 2s19 cytochrome p 450 (eg, omeprazole, jezomeprozolom, fluvoksaminom, lansoprazolom, ticlopidine) and cimetidine. Together admission jescitaloprama and the above drugs based on the monitoring of side effects may require dose reduction jescitaloprama.
Escitalopram is an inhibitor of izofermenta CYP2D6. Caution must be exercised while appointing jescitaloprama and drugs, metaboliziruthan by using this izofermenta and having a small Therapeutic index, eg, flekainida, propafenon and metoprolol (in cases of heart failure) or preparations, mostly metaboliziruthan by izofermenta CYP2D6 and acting on the central nervous system, for example antidepressants dezipramina, clomipramine, nortriptilina or antipsychotics risperidone, tioridazina, haloperidol. In these cases, you might need to dose adjustment.
Co-administration of escitalopram and desipramine or metoprolol resulting in a twofold increase in the concentration of the latter two drugs.
Escitalopram can significantly inhibit isoenzyme CYP2C19. Therefore, caution is advised while using escitalopram and drugs, metabolized with the participation of isoenzyme.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.
