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Cipralex (Escitalopramum, Escitalopram) - antidepressant, selective serotonin reuptake inhibitor. Inhibition of reuptake of serotonin leads to increasing the concentration of the neurotransmitter in the synaptic cleft, amplifies and prolong its effect on post-synaptic receptor sites. Escitalopram has no or has a very weak ability to bind to a number of receptors including: serotonin 5-HT1A-, 5-HT2-receptors, dopamine D1- and D2- receptors, a1-, a2-, b-adrenergic receptors, histamine N1- receptors, m-cholinergic receptors, benzodiazepine and opioid receptors.
Pregnancy and breast-feeding:
Cipralex contraindicated during pregnancy and lactation (breastfeeding).
Escitalopram should not be administered concurrently with MAO inhibitors. Escitalopram can be assigned 14 days after cessation of treatment irreversible MAO inhibitors and at least 1 day after cessation of therapy reversible MAO-A inhibitors (including moclobemide). At least 7 days should elapse after stopping escitalopram before you can start treatment of non-selective MAO inhibitors.
Some patients with panic disorder at the beginning of treatment with selective serotonin reuptake inhibitors (including escitalopram) may experience increased anxiety. This paradoxical reaction usually disappears within 2 weeks of treatment. To reduce the likelihood of anxiogenic effects, it is recommended to use the drug in low initial doses.
Escitalopram should be repealed in the event of seizures. It is not recommended to use the drug in patients with unstable epilepsy; under controlled seizures should be closely monitored. An increase in the frequency of seizures, selective serotonin reuptake inhibitors, including escitalopram, you must cancel.
Caution should be used escitalopram in patients with a history of instructions to mania / hypomania. With the development of mania escitalopram should be abolished.
Escitalopram in the treatment of patients with diabetes may change in blood glucose levels. Therefore, correction may be required dose of insulin and / or oral hypoglycemic drugs.
Clinical experience with escitalopram and other selective serotonin reuptake inhibitors for evidence of a possible increase in suicide risk in the first weeks of therapy. It is important to closely monitor the patient during this period.
Hyponatremia, associated with the possible violation of ADH secretion in patients receiving escitalopram is rare and usually disappears when you cancel therapy. Precautions should be prescribed escitalopram and other selective serotonin reuptake inhibitor to patients within the risk group of hyponatremia: the elderly, patients with liver cirrhosis and receiving drugs that can cause hyponatremia.
When receiving escitalopram may develop skin bleeding (ecchymosis and purpura). It should be used with caution in patients with escitalopram with a tendency to bleeding, as well as taking oral anticoagulants and drugs that affect blood clotting.
Clinical experience with escitalopram in conjunction with electroconvulsive therapy is limited, so in this case you should be careful.
Not recommended simultaneous application of escitalopram and MAO inhibitors type A because of the risk of serotonin syndrome.
In patients taking escitalopram and other selective serotonin reuptake inhibitor simultaneously with serotonergic agents, serotonin syndrome may develop in rare cases. Caution should be used in conjunction with escitalopram drugs having serotonergic activity. A combination of symptoms such as agitation, tremor, myoclonus, hyperthermia may indicate the development of serotonin syndrome. If this happens, selective serotonin reuptake inhibitors and serotonergic drugs should be immediately withdrawn and symptomatic therapy.
Concomitant use of escitalopram and alcohol is not recommended.
Effects on ability to drive vehicles and management mechanisms
Although escitalopram has no effect on psychomotor activity, in the period of treatment is not recommended to drive or mechanisms.
Cipralex administered 1 time / day, regardless of the meal.
If depressive episodes, the drug is usually prescribed at a dose of 10 mg / day. Depending on the individual response of the patient the dose may be increased to a maximum of - 20 mg / day.
Antidepressant effect usually develops within 2-4 weeks after starting treatment. After the disappearance of the symptoms of depression for at least a further 6 months is necessary to continue treatment for fixing the resulting effect.
When panic disorder with / without agoraphobia during the first week of treatment recommended dose of 5 mg / day, followed by an increase to 10 mg / day. Depending on the individual response of the patient the dose may be increased to a maximum of - 20 mg / day.
The maximum therapeutic effect is reached after about 3 months after initiation of treatment. The therapy lasts several months.
Elderly patients (over 65 years) is usually recommended to use half the recommended dose (ie, a total of 5 mg / day) and a lower maximum dose (10 mg / day).
In renal insufficiency, mild to moderate dose adjustment is required. Patients with severe renal insufficiency (KKPatsientam with impaired hepatic function The recommended starting dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to the treatment dose can be increased up to 10 mg / day.
With reduced activity isoenzyme CYP2C19 the recommended starting dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to the medication dose can be increased to 10 mg / day.
Upon termination of treatment Cipralex dose should be reduced gradually over 1-2 weeks to avoid the development of the syndrome.
From the digestive system: the most common - nausea, decreased appetite, diarrhea, constipation; rarely - a violation of taste sensations; possible - vomiting, dry mouth, changes in laboratory parameters of liver function.
From the central and peripheral nervous system, most often - insomnia or drowsiness, dizziness, weakness; possible - vision disorder, seizures, tremor, movement disorders, serotonin syndrome, hallucinations, delusions, confusion, agitation, anxiety, depersonalisation, panic attacks, irritability.
From a metabolism: the most common - excessive sweating, hyperthermia; possible - hyponatremia.
From the reproductive system: most frequently - decreased libido, impotence, ejaculation disorder, anorgasmia (in women).
Since the cardiovascular system: possible orthostatic hypotension.
From endocrine system: possible - inadequate secretion of ADH, galactorrhea.
Allergic reactions: possible - anaphylactic reactions, angioedema.
Dermatological reactions: possible - skin rash, pruritus, ecchymosis, purpura.
Other: most often - sinusitis; possible - arthralgia, myalgia, urinary retention.
With a sharp lifting of the drug after prolonged use may cancel the reaction - dizziness, headaches and nausea. Intensity of these reactions is negligible, and the duration is limited.
Side effects most often develop for 1 or 2 weeks of treatment and then generally become less intense and less likely to occur with continued therapy.
Symptoms: dizziness, tremor, agitation, somnolence, dizziness, seizures, tachycardia, ECG changes (changes in the ST segment and the tooth T, the expansion of the complex the QRS, QT prolongation), arrhythmias, depression of respiratory activity, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.
Treatment: There is no specific antidote. Treatment is symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems.
In an application Cipralex with MAO inhibitors, and also at the beginning of the reception of MAO inhibitors sick shortly before stop taking Cipralex, may cause serious adverse reactions. In such cases, serotonin syndrome may develop.
The combined use of serotonergic drugs with Cipralex (eg tramadol, sumatriptan and other triptans) may lead to serotonin syndrome.
Cipralex may lower the seizure threshold. Care should be taken while appointing Cipralex and other drugs that reduce the seizure threshold.
Since cases enhance the action of an account with a joint appointment Cipralex and lithium or tryptophan, caution is advised with concomitant administration of these drugs.
Simultaneous with the appointment Cipralex and products containing St. John's wort (Hypericum perforatum), may lead to an increase in side effects.
When concomitant administration of escitalopram with oral anticoagulants and drugs that affect blood clotting (eg, phenothiazines and atypical antipsiholeptikami, the majority of tricyclic antidepressants, acetylsalicylic acid and NSAIDs, ticlopidine and dipyridamole), it may be a bleeding disorder. In such cases, at the beginning or at the end of therapy with escitalopram requires careful monitoring of blood clotting.
At simultaneous reception of alcohol does not take escitalopram pharmacodynamic or pharmacokinetic interaction. However, as with other psychotropic agents, simultaneous use of escitalopram and alcohol is not recommended.
The combined use of drugs that inhibit isozyme CYP2C19, escitalopram can increase the concentration in plasma. Caution should be used in conjunction with escitalopram similar preparations (including omeprazole); you may need to reduce the dose of escitalopram.
Precautions should be prescribed in high doses Cipralex simultaneously with cimetidine in high doses, which is a potent inhibitor of the isoenzyme CYP2D6, CYP3A4 and CYP1A2.
Escitalopram is an inhibitor of the isoenzyme CYP2D6. Caution must be exercised with concomitant administration of escitalopram and drugs metabolized by this isoenzyme, and having a small therapeutic index, eg flecainide, propafenone and metoprolol (in cases of heart failure), or drugs mainly metabolized by CYP2D6 isoenzyme and acting on the central nervous system eg antidepressants desipramine, clomipramine, nortriptyline or antipsychotics risperidone, thioridazine, haloperidol. In these cases, you may need a dose adjustment.
Co-administration of escitalopram and desipramine or metoprolol resulting in a doubling of the concentration of the latter two drugs.
Escitaloprame may slightly inhibit isoenzyme CYP2C19. Therefore, caution is advised during simultaneous use of escitalopram and drugs metabolized with the participation of isoenzyme.
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