Sertraline (Dosage)

Sertraline is a drug of the selective serotonin reuptake inhibitor group, used in the treatment of depression and anxiety, among others. Depending on the polymorphic variant present in the CYP2C19 gene, the main cytochrome involved in its metabolism, the patient may have a different metabolizing profile and may require a dose adjustment depending on the variant present.

Sertraline is a SSRI (Selective Serotonin Reuptake Inhibitor) antidepressant. Sertraline has antidepressant and anxiolytic effects. It is used clinically for the treatment of depression, obsessive compulsive disorder, panic disorder, social phobia and premenstrual dysphoric disorder. It has no affinity for muscarinic, serotonergic, dopaminergic, adrenergic, histaminergic, GABAergic or benzodiazepine receptors.

CONTRAINDICATIONS

Hypersensitivity to sertraline.

Concomitance with MAOIs (risk of NMS, neuroleptic malignant syndrome), do not start treatment with MAOI antidepressants until 7 days after discontinuing sertraline and 14 days between MAOI suspension and sertraline initiation.

CAUTIONS

Cautions should be taken when prescribing sertraline in patients with mania/hypomania, epilepsy, schizophrenia, history of bleeding disorders, liver failure, children and adolescents under 18 years except in treatment of obsessive-compulsive disorder, elderly, ECT (electroconvulsive therapy), diabetes (where the dose of antidiabetic treatment must be adjusted), patients with closed-angle glaucoma or with a history of glaucoma.

If treatment is withdrawn, this interruption should be gradual, for several weeks or months, as necessary, to avoid withdrawal symptoms. It has been associated with the appearance of akathisia/psychomotor restlessness. It is mandatory to be alert about the need to monitor the appearance of suicidal behavior and self-harm.

The prescription of sertraline may be associated with risk of hyponatremia, serotonin syndrome, or NMS (which increases when it is administered concomitantly with: other serotonergic agents such as triptans, which alter its metabolism, such as methylene blue, antipsychotics and other dopamine antagonists, and opioid medications. The patient should be monitored for signs / symptoms). Precautions should be taken with the co-administration with other serotonergic agents (tryptophan, fenfluramine, serotonin agonists, St. John's wort).

Strict control should be followed if it is changed from other antidepressant or anti-obsessive treatments to sertraline. The intake of sertraline with grapefruit juice is not recommended as it can inhibit the antidepressant effect

Caution in patients with risk factors for prolongation of the QT cardiac interval.

SIDE EFFECTS

Pharyngitis, anorexia, increased appetite, insomnia, depression, depersonalization, nightmares, anxiety, agitation, nervousness, decreased libido, bruxism, dizziness, drowsiness, headache, paresthesia, tremor, hypertonia, dysgeusia, impaired attention, visual disturbances, tinnitus , palpitations, flushing, yawning, diarrhea, nausea, dry mouth, abdominal pain, vomiting, constipation, dyspepsia, flatulence, rash, hyperhidrosis, arthralgia, myalgia, ejaculatory insufficiency, erectile dysfunction, fatigue, chest pain.

PHARMACOLOGIC INTERACTIONS

Sertraline increases the risk of bleeding with: AAS and derivatives, NSAIDs (non-steroidal anti-inflammatory drugs), anticoagulants and ticlodipine.

Sertraline increases the prothrombin time if taken concomitantly with warfarin.

Diminished clearance of sertraline with cimetidine.

Extreme caution with: lithium, fentanyl (in anesthesia or chronic pain treatment).

Risk of prolongation of the QT cardiac interval and / or ventricular arrhythmias with other medications that prolong the QT interval (some antipsychotics and antibiotics).

In concomitancy with sertraline, monitor plasma concentration of phenytoin.

It is recommended the surveillance of the patient is taking sertraline together with sumatriptan.

SSRIs (selective serotonin reuptake inhibitor antidepressants) can reduce the plasma activity of cholinesterase, leading to a prolongation of the neuromuscular blocking action of mivacurium or other neuromuscular blocking agents.

BRAND NAMES:

  • Altisben ®
  • Aremis ®
  • Aserin ®
  • Besitran ®
  • Sertrabrain ®

Genes analyzed

CYP2C19

Bibliography

Bråten LS, Ingelman-Sundberg M, Jukic MM, et al.Impact of the novel CYP2C:TG haplotype and CYP2B6 variants on sertraline exposure in a large patient population. Clin Transl Sci. 2022 Sep;15(9):2135-2145.

Bousman CA, Stevenson JM, Ramsey LB, et al.Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6, CYP2C19, CYP2B6, SLC6A4, and HTR2A Genotypes and Serotonin Reuptake Inhibitor Antidepressants. Clin Pharmacol Ther. 2023 Jul;114(1):51-68.

Brouwer JMJL, Nijenhuis M, Soree B, et al.Dutch Pharmacogenetics Working Group (DPWG) guideline for the gene-drug interaction between CYP2C19 and CYP2D6 and SSRIs. Eur J Hum Genet. 2022 Oct;30(10):1114-1120.

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