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Escitalopram Metabolization

Escitalopram is an antidepressant of the family of selective serotonin reuptake inhibitors or SSRIs, with high affinity for the serotonin binding site (5-HT) in neurons.

It has low or no affinity for other receptors such as 5-HT1a, 5-HT2, dopaminergic, adrenergic, histaminergic H1, muscarinic, benzodiazepine and opioid cholinergic receptors.

CONTRAINDICATIONS

Escitalopram is contraindicated in patients with hypersensitivity to the drug, with a history of prolonged QT cardiac interval or congenital long QT syndrome. Do not administer concomitantly with non-selective irreversible MAOIs, do not administer with reversible MAOIs (moclobemide) or with linezolid, do to the risk of serotonin syndrome or with drugs that prolong the QT cardiac interval.

CAUTIONS

Cautions should be taken in patients with severe renal failure, hepatic insufficiency or diabetes. Precaution should be taken also in patients with closed angle glaucoma or a history of glaucoma. Take precautions if patient is under electroconvulsive therapy (ECT). Cautions in patients with history of mania/hypomania.

Extreme caution in patients with stable epilepsy (monitor and discontinue treatment if seizure frequency increases) and do not administer escitalopram in patients with unstable epilepsy or if seizures develop for the first time.

Serious precautions should be taken in patients with other risk factors, such as development of Torsade de Pointes, decompensated heart failure, significant bradycardia, recent acute myocardial infarction or predisposition to hypokalemia or hypomagnesemia due to disease or concomitant medication.

Do not use in children and adolescents under 18 years old since they develop more frequent suicidal behaviors and hostility during treatment with escitalopram.

At the beginning of the treatment symptoms of anxiety (paradoxical anxiety) can be increased, start with lower doses. Monitor at the beginning of treatment for suicide risk in depression and other psychiatric illnesses. If signs of akathisia / psychomotor restlessness appear, take precautions when increasing the dose. In patients over 65 years old, there is a risk of cardiac QT prolongation (maximum dose 10 mg / day) and hyponatremia. There exists risk of hiponatremia patients with cirrhosis or treated with drugs that can cause cirrhosis.

When deciding to withdraw the treatment, gradually reduce the dose for a period of at least 1 to 2 weeks to reduce the risk of withdrawal symptoms.

SIDE EFFECTS

Nausea, diarrhea, constipation, vomiting, dry mouth; weight gain. Insomnia, drowsiness, dizziness, paresthesia, tremor; sinusitis, yawning; increased sweating; arthralgia, myalgia; decreased appetite, increased appetite; fatigue, pyrexia. Disorders of ejaculation, impotence; anxiety, restlessness, abnormal dreams, decreased libido, anorgasmia.

Post-marketing cases of prolongation of the QT cardiac interval and ventricular arrhythmia have been reported.

PHARMACOLOGIC INTERACTIONS

Risk of developing serotonin syndrome by selegiline.

Escitalopram enhances its effects if it is administered together with lithium and tryptophan.

Escitalopram enhances the toxicity of oral anticoagulants. There exists risk of hemorrhage associated with oral anticoagulants, drugs that affect platelet function (atypical antipsychotics and phenothiazines, tricyclic antidepressants, ASA and NSAIDs, ticlopidine and dipyridamole), or in patients with a tendency to hemorrhage.

Plasma concentrations of escitalopram are increased by cytochrome CYP2C19 inhibitors.

Escitalopram potentiates the action and toxicity of: flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine and haloperidol.

Caution is required when escitalopram is prescribed together with: tricyclic antidepressants, other SSRI antidepressants, phenothiazines, thioxanthenes, butyrophenones, mefloquine, bupropion and tramadol.

Caution if escitalopram is administered with drugs with serotonergic effects such as sumatriptan or other triptans, tramadol and tryptophan.

Concomitant use with herbal remedies containing St. John's Wort increases the incidence of adverse reactions.

BRAND NAMES

  • Cipralex ®
  • Escilan ®
  • Escimylan ®
  • Esertia ®
  • Heipram ®
  • Lexapro ®

Gene or region studied

  • CYP2C19
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