Sertraline


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Panic disorder with or without agoraphobia, Posttraumatic stress disorder, Social anxiety disorder
Adult: Initially, 25 mg once daily, increased to 50 mg once daily after 1 week. Subsequent doses may be increased, if necessary, in increments of 50 mg at intervals of at least 1 week. Maintenance: Use lowest effective dose, once optimal response is achieved.  Max: 200 mg daily.

Oral
Obsessive compulsive disorder
Adult: Initially, 50 mg once daily, may be increased, if necessary, in increments of 50 mg at intervals of at least 1 week. Maintenance: Use lowest effective dose, once optimal response is achieved.  Max: 200 mg daily.
Child: 6-12 years Initially, 25 mg once daily, may be increased to 50 mg once daily after 1 week; 13-17 years Same as adult dose. Consider the body weight when increasing the dose. Max: 200 mg daily.

Oral
Depression
Adult: Initially, 50 mg once daily, may be increased, if necessary, in increments of 50 mg at intervals of at least 1 week. Maintenance: Use lowest effective dose, once optimal response is achieved. Max: 200 mg daily. Treatment duration: At least 6 months.

Oral
Premenstrual dysphoric disorder
Adult: Continuous dosing: Initially, 50 mg once daily,  may increase by 50 mg each menstrual cycle if necessary. Max: 150 mg daily. Luteal phase dosing: Initially, 50 mg once daily for the 1st 3 days, may increase by 100 mg daily. Maintenance: Use lowest effective dose, once optimal response is achieved.
Nhóm bệnh nhân đặc biệt
Pharmacogenomics:

Sertraline is metabolised primarily by CYP2C19 isoenzyme. Genetic polymorphism in CYP2C19 genotype can influence the metabolism, exposure, efficacy and safety of sertraline.

The prevalence of CYP2C19 allele varies among different ethnic backgrounds (e.g. CYP2C19*3 has low prevalence among most ethnic groups but has an allele frequency of approx 15% in some Asian populations). Thus, the alleles that should be tested for a given population may considerably vary.

CYP2C19 ultrarapid metabolisers (carriers of 2 increased function alleles, or 1 normal function allele and 1 increased function allele *17/*17, *1/*17)
Individuals may have increased sertraline metabolism. CPIC recommends initiation of treatment with the usual recommended dose. However, if the patient is unresponsive to the recommended maintenance dose, consider alternative drug not predominantly metabolised by CYP2C19.

CYP2C19 extensive metabolisers (carriers of 2 normal function alleles *1/*1)
No dosage adjustment needed.

CYP2C19 intermediate metabolisers (carriers of 1 normal function allele, or 1 increased function allele and 1 no function allele *1/*2, *1/*3, *2/*17)
Individuals may have reduced sertraline metabolism as compared to extensive metabolisers. However, no dosage adjustment is recommended.

CYP2C19 poor metabolisers (carriers of 2 no function alleles *2/*2, *2/*3, *3/*3)
Individuals may have greatly reduced sertraline metabolism as compared to extensive metabolisers, thereby increasing sertraline plasma concentrations and the risk of adverse effects (e.g. insomnia, headache, gastrointestinal dysfunction, sexual dysfunction). CPIC recommends a 50% dose reduction of recommended starting dose, then titrate dose according to response. Alternatively, consider another drug not predominantly metabolised by CYP2C19.
Suy gan
Dose reduction may be necessary. Severe: Not recommended.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
Oral concentrate solution: Add to 120 mL of diluents (e.g. water, ginger ale, lemon or lime soda, lemonade or orange juice only) just before administration.
Chống chỉ định
Concomitant use or within 14 days of discontinuation of MAOIs. Concurrent use with pimozide. Concomitant use of sertraline oral concentrate solution with disulfiram.
Thận trọng
Patients with family history of bipolar disorder, mania or hypomania, schizophrenia; previous seizure disorder or condition predisposing to seizures (e.g. brain damage, alcoholism); volume depletion, diabetes mellitus, history of bleeding disorders, angle-closure glaucoma or history of glaucoma, risk factors for QTc prolongation. Avoid abrupt withdrawal. Hepatic impairment. Children and elderly. Pregnancy and lactation. CYP2C19 ultrarapid and poor metabolisers.
Tác dụng không mong muốn
Significant: Activation of hypomania or mania, seizures, CNS depression, QTc prolongation, Torsade de pointes, abnormal bleeding events including cutaneous bleeding (e.g. ecchymoses, purpura), bone fractures, mild pupillary dilation, sexual dysfunction, loss of glycaemic control, withdrawal symptoms.
Cardiac disorders: Palpitations, chest pain.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Visual disturbance.
Gastrointestinal disorders: Nausea, diarrhoea, dry mouth, dyspepsia, constipation, vomiting, abdominal pain, flatulence, dysgeusia.
General disorders and administration site conditions: Fatigue, malaise, asthenia, pyrexia.
Investigations: Weight increased.
Metabolism and nutrition disorders: Decreased or increased appetite.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia, myalgia.
Nervous system disorders: Headache, dizziness, somnolence, paraesthesia, tremor, extrapyramidal symptoms (e.g. hyperkinesia, hypertonia, dystonia, teeth grinding or gait abnormalities), disturbance in attention.
Psychiatric disorders: Insomnia, anxiety, agitation, depression, nervousness, nightmare, bruxism, decreased libido, depersonalisation.
Reproductive system and breast disorders: Ejaculation failure, erectile dysfunction, irregular menstruation.
Respiratory, thoracic and mediastinal disorders: Yawning, pharyngitis, rhinitis, upper respiratory tract infection.
Skin and subcutaneous tissue disorders: Rash, hyperhidrosis.
Vascular disorders: Hot flush.
Potentially Fatal: Suicidal thoughts and behavior, serotonin syndrome or neuroleptic malignant syndrome (NMS), haemorrhage (e.g. gastrointestinal or gynaecological bleeding), anaphylactoid reaction, angioedema, Stevens-Johnson syndrome, erythema multiforme, vasculitis, syndrome of inappropriate antidiuretic hormone secretion (SIADH), hyponatraemia.
PO: Z (Risk of postpartum haemorrhage, persistent pulmonary hypertension in infant, neonatal withdrawal/toxicity in late pregnancy use. Monitor closely.)
Thông tin tư vấn bệnh nhân
This drug may impair mental and physical abilities, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor BMI (longitudinal monitoring), height, weight; serum Na in at-risk patients. Closely monitor mental status for worsening of depression, suicidal ideation or other unusual behavioural changes at the start of treatment or when doses are adjusted; signs and symptoms of serotonin syndrome and glucose fluctuations.
Quá liều
Symptoms: Somnolence, dizziness, gastrointestinal disturbances (e.g. nausea, vomiting), tachycardia, tremor, agitation, QTc prolongation or Torsade de pointes, and coma. Management: Symptomatic and supportive treatment. Establish and maintain airway and ensure adequate oxygenation or ventilation if necessary. Administration of activated charcoal with a cathartic may be considered. Monitor cardiac and vital signs.
Tương tác
May increase risk of hyponatraemia with diuretics. Increased risk of QTc prolongation and/or ventricular arrhythmias with specific antipsychotics (e.g. ziprasidone, iloperidone, chlorpromazine, mesoridazine, droperidol), specific antibiotics (e.g. erythromycin, gatifloxacin, moxifloxacin, sparfloxacin), Class IA antiarrhythmics (e.g. quinidine, procainamide, Class III antiarrhythmics (e.g. amiodarone, sotalol) and other drugs that prolong QTc interval (e.g. pentamidine, methadone, halofantrine, mefloquine, probucol, tacrolimus). May increase serum concentration of phenytoin. May increase the exposure of CYP2D6 substrates (e.g. propafenone, flecainide). Increased exposure with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin. May prolong neuromuscular blocking effects of mivacurium or other neuromuscular blockers.
Potentially Fatal: Increased risk of serotonin syndrome with other serotonergic agents (e.g. triptans, TCAs, fentanyl, lithium, tramadol, buspirone, tryptophan, amphetamines, fenfluramine, serotonin agonists); agents which impair metabolism of serotonin (e.g. MAOIs, linezolid, IV methylene blue); antipsychotics or other dopamine antagonists, and opiate drugs. May enhance adverse/toxic effect of pimozide. Enhanced adverse/toxic effect of sertraline oral concentrate solution with disulfiram. Increased risk of bleeding with anticoagulants (e.g. aspirin, clopidogrel, heparin, warfarin) and NSAIDs (e.g. ibuprofen, naproxen).
Tương tác với thức ăn
Increased risk of serotonin syndrome with St. John’s wort. Increased risk of psychomotor impairment with alcohol. Increased plasma levels with grapefruit juice.
Ảnh hưởng đến kết quả xét nghiệm
May give false-positive result with urine detection of benzodiazepines.
Tác dụng
Description: Sertraline, a naphthalenamine-derivative antidepressant, selectively inhibits presynaptic serotonin (5-HT) reuptake. It has very weak effects on norepinephrine and dopamine neuronal uptake.
Onset: Depression: Within 1 week.
Pharmacokinetics:
Absorption: Slowly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 4.5-8.4 hours (sertraline).
Distribution: Widely distributed throughout body tissues. Crosses placenta and enters breast milk. Plasma protein binding: Approx 98%.
Metabolism: Metabolised in the liver mainly via N-demethylation by CYP2C19 and CYP2D6 to less active metabolite, N-desmethylsertraline; further metabolised via oxidative deamination and subsequent reduction, hydroxylation and glucuronide conjugation. Undergoes extensive first-pass metabolism.
Excretion: Via urine (40-45% as metabolites); faeces (40-45%; 12-14% as unchanged drug). Elimination half-life: Approx 26 hours (sertraline); 62-104 hours (N-desmethylsertraline).
Đặc tính

Chemical Structure Image
Sertraline

Source: National Center for Biotechnology Information. PubChem Database. Sertraline, CID=68617, https://pubchem.ncbi.nlm.nih.gov/compound/Sertraline (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Thuốc chống trầm cảm
Phân loại ATC
N06AB06 - sertraline ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.
Tài liệu tham khảo
Hicks JK, Bishop JR, Sangkuhl K et al. Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6 and CYP2C19 Genotypes and Dosing of Selective Serotonin Reuptake Inhibitors. CPIC Guidelines. 2015 Aug;98(2):127-134. doi: 10.1002/cpt.147. Accessed 11/09/2019

Hicks JK, Bishop JR, Sangkuhl K et al. Supplement to: Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6 and CYP2C19 Genotypes and Dosing of SSRIs. CPIC Guidelines. Accessed 11/09/2019

Annotation of CPIC Guideline for Sertraline and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 11/09/2019.

Annotation of DPWG Guideline for Sertraline and CYP2C19. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 11/09/2019.

Anon. Sertraline Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/09/2019.

Anon. Sertraline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/09/2019.

Buckingham R (ed). Sertraline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/09/2019.

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6 and CYP2C19 Genotypes and Dosing of Selective Serotonin Reuptake Inhibitors. Clinical Pharmacogenetics Implementation Consortium (CPIC). https://cpicpgx.org/. Accessed 11/09/2019.

Joint Formulary Committee. Sertraline Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/09/2019.

Zoloft Tablet, Film Coated; Solution, Concentrate (Roerig). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 11/09/2019.

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