Drug Monograph
Sertraline (Zoloft)
sertraline hydrochloride
Pharmacokinetic Profile
Half-Life
~26 h (sertraline); 62–104 h (N-desmethylsertraline)
Metabolism
Hepatic (CYP2B6, 2C9, 2C19, 2D6, 3A4)
Protein Binding
98%
Tmax
4.5–8.4 h
CYP Inhibition
CYP2D6 (mild–moderate)
Clinical Information
Drug Class
SSRI
Available Doses
Tablets: 25, 50, 100 mg; Oral solution: 20 mg/mL
Route
Oral
Renal Adjustment
None required
Hepatic Adjustment
Mild: halve dose; Moderate–severe: not recommended
Pregnancy
Third trimester: neonatal withdrawal risk; PPHN risk
Lactation
Present in breast milk (~2% of maternal levels)
Schedule / Legal Status
Rx only; Not a controlled substance
Generic Available
Yes
Black Box Warning
Suicidal thoughts & behaviors in youth/young adults
Indications
| Indication | Approved Population | Therapy Type | Status |
|---|---|---|---|
| Major depressive disorder (MDD) | Adults | Monotherapy | FDA Approved |
| Obsessive-compulsive disorder (OCD) | Adults and paediatric patients aged 6–17 | Monotherapy | FDA Approved |
| Panic disorder (PD) | Adults | Monotherapy (with or without agoraphobia) | FDA Approved |
| Posttraumatic stress disorder (PTSD) | Adults | Monotherapy | FDA Approved |
| Social anxiety disorder (SAD) | Adults | Monotherapy | FDA Approved |
| Premenstrual dysphoric disorder (PMDD) | Adults (women) | Continuous or intermittent (luteal-phase) dosing | FDA Approved |
Sertraline is among the most widely prescribed SSRIs worldwide and has demonstrated efficacy across a broad range of anxiety and depressive disorders. It is the only SSRI with FDA approval for all six of the above indications. In MDD, sertraline has been considered a first-line agent in multiple guidelines including NICE and the APA. Paediatric approval is limited to OCD in patients aged 6–17 years; safety and efficacy in paediatric patients for other indications have not been established.
Off-Label Uses
Generalised anxiety disorder (GAD): Commonly prescribed off-label with moderate-quality evidence supporting efficacy. Premature ejaculation: SSRIs including sertraline delay ejaculation; used off-label at 25–50 mg daily or as needed. Evidence quality: Moderate. Body dysmorphic disorder, binge eating disorder: Evidence quality: Low–Moderate.
Dosing
| Clinical Scenario | Starting Dose | Maintenance Dose | Maximum Dose | Notes |
|---|---|---|---|---|
| MDD — adults | 50 mg/day | 50–200 mg/day | 200 mg/day | Once daily, morning or evening. Titrate in 25–50 mg increments q1wk based on response and tolerability. Given 24 h t½, wait at least 1 week between dose changes. |
| OCD — adults | 50 mg/day | 50–200 mg/day | 200 mg/day | OCD often requires higher doses (100–200 mg/day) for optimal response. Allow 4–6 weeks at therapeutic dose before assessing response. |
| OCD — paediatric (6–12 yr) | 25 mg/day | 50–200 mg/day | 200 mg/day | Lower starting dose to minimise GI side effects. Titrate in 25 mg increments q1wk. Monitor weight and growth in paediatric patients on SSRIs. |
| OCD — paediatric (13–17 yr) | 50 mg/day | 50–200 mg/day | 200 mg/day | Same titration as adults. |
| Panic disorder — adults | 25 mg/day | 50–200 mg/day | 200 mg/day | Start low (25 mg) to avoid initial worsening of panic symptoms. Increase to 50 mg after 1 week. May take 4–8 weeks for full anxiolytic effect. |
| PTSD — adults | 25 mg/day | 50–200 mg/day | 200 mg/day | Start at 25 mg; increase to 50 mg after 1 week. Titrate based on response. |
| Social anxiety disorder — adults | 25 mg/day | 50–200 mg/day | 200 mg/day | Start at 25 mg; increase to 50 mg after 1 week. |
| PMDD — continuous dosing | 50 mg/day | 50–150 mg/day | 150 mg/day | Take daily throughout menstrual cycle. Titrate in 50 mg increments per menstrual cycle. |
| PMDD — intermittent (luteal phase) | 50 mg/day | 50–100 mg/day | 100 mg/day | Start 14 days before anticipated menses, continue through onset. If increasing: 50 mg first 3 days, then 100 mg remaining days. Repeat cycle with each new menstrual cycle. |
| Mild hepatic impairment (Child-Pugh 5–6) | Halve all recommended starting and therapeutic doses | ~3-fold greater exposure with mild impairment. Use half dose across all indications. | ||
| Moderate–severe hepatic impairment | Not recommended | Insufficient safety data; significantly increased exposure expected. | ||
Clinical Pearl: Discontinuation
When stopping sertraline, reduce the dose gradually rather than abruptly to minimise discontinuation symptoms (dizziness, nausea, headache, irritability, paraesthesia, insomnia). Common strategies include reducing by 25–50 mg every 1–2 weeks. If intolerable symptoms occur, consider resuming the previous dose and tapering more slowly.
Pharmacology
Mechanism of Action
Sertraline is a potent and selective inhibitor of neuronal serotonin (5-HT) reuptake, with only very weak effects on norepinephrine and dopamine reuptake. By blocking the serotonin transporter (SERT), sertraline increases serotonin availability in the synaptic cleft, enhancing serotonergic neurotransmission. Receptor binding studies confirm that sertraline has no significant affinity for adrenergic, cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5-HT1A, 5-HT1B, 5-HT2), or benzodiazepine receptors, which accounts for its favourable side effect profile compared with tricyclic antidepressants. The therapeutic onset typically requires 2–4 weeks of sustained treatment, reflecting downstream adaptive changes in receptor sensitivity and intracellular signalling.
ADME Profile
| Parameter | Value | Clinical Implication |
|---|---|---|
| Absorption | Tmax 4.5–8.4 h; food increases Cmax by ~25% and decreases Tmax to ~5.5 h for tablets; dose-proportional AUC over 50–200 mg range; extensive first-pass metabolism | Can be taken with or without food; food mildly enhances absorption. Absolute bioavailability not fully characterised due to first-pass effect |
| Distribution | 98% protein bound (albumin); extensive Vd; crosses blood-brain barrier | High protein binding means displacement interactions are theoretically possible but clinically uncommon. Large Vd makes dialysis ineffective in overdose |
| Metabolism | Extensive hepatic first-pass metabolism; primary pathway: N-demethylation to N-desmethylsertraline (t½ 62–104 h, substantially less active); further oxidative deamination, hydroxylation, glucuronidation. Multiple CYPs involved: CYP2B6, 2C9, 2C19, 2D6, 3A4. Sertraline is a mild–moderate CYP2D6 inhibitor | Low CYP2D6 inhibition compared with other SSRIs (fluoxetine, paroxetine) but still clinically relevant for narrow-TI CYP2D6 substrates. Elderly show ~40% lower clearance — may need lower doses |
| Elimination | t½ ~26 h; <5% excreted unchanged; urine ~40–45%, faeces ~40–45% (as metabolites); steady state within ~1 week | 24 h half-life supports once-daily dosing. The 1-week time to steady state informs the minimum interval between dose adjustments |
Side Effects
≥10%Very Common (Pooled Data: N=3,066 vs 2,293 Placebo)
| Adverse Effect | Incidence | Clinical Note |
|---|---|---|
| Nausea | 26% (vs 12% placebo) | Most common AE; usually dose-related and self-limiting within first 1–2 weeks. Taking with food may reduce severity |
| Diarrhoea / loose stools | 20% (vs 10% placebo) | More common with sertraline than other SSRIs; usually transient. Consider dose reduction if persistent |
| Insomnia | 20% (vs 13% placebo) | May be activating; consider morning dosing if sleep is affected. Distinguish from underlying anxiety/depression |
| Dry mouth | 14% (vs 9% placebo) | Mild anticholinergic-like effect despite minimal muscarinic receptor affinity |
| Fatigue | 12% (vs 8% placebo) | Often improves over time; differentiate from depression-related fatigue |
| Dizziness | 12% (vs 8% placebo) | Usually mild; counsel about fall risk, especially in elderly |
| Somnolence | 11% (vs 6% placebo) | Evening dosing may be preferred if daytime sedation is problematic |
2–10%Common
| Adverse Effect | Incidence | Clinical Note |
|---|---|---|
| Tremor | 9% (vs 2% placebo) | Fine postural tremor; dose-related. Evaluate for serotonin syndrome if severe |
| Agitation | 8% (vs 5% placebo) | May occur early in treatment; distinguish from akathisia |
| Dyspepsia | 8% (vs 4% placebo) | Take with food to mitigate |
| Ejaculation failure (males) | 8% (vs 1% placebo) | Most common sexual AE in men; dose-related. Discuss proactively |
| Decreased appetite | 7% (vs 2% placebo) | Monitor weight, especially in paediatric patients and elderly |
| Hyperhidrosis | 7% (vs 3% placebo) | Excessive sweating; may persist throughout treatment |
| Decreased libido | 6% (vs 2% placebo) | Underreported; inquire proactively. May be compounded by psychiatric condition |
| Constipation | 6% (vs 4% placebo) | Less common than diarrhoea with sertraline |
| Palpitations | 4% (vs 2% placebo) | Benign; evaluate further if accompanied by syncope or chest pain |
| Erectile dysfunction (males) | 4% (vs 1% placebo) | Address alongside ejaculatory dysfunction; may improve with time or dose reduction |
| Vomiting | 4% (vs 1% placebo) | More common with initial dosing or rapid titration |
SeriousSerious (Regardless of Frequency)
| Adverse Effect | Estimated Frequency | Typical Onset | Required Action |
|---|---|---|---|
| Suicidal thoughts/behaviours | 14 per 1,000 (<18 yr); 5 per 1,000 (18–24 yr) vs placebo | First weeks of treatment or dose changes | Close monitoring; involve family/caregivers; consider changing or discontinuing therapy. FDA Boxed Warning |
| Serotonin syndrome | Rare | Hours to days after starting or increasing serotonergic drug | Discontinue all serotonergic agents immediately; supportive care; may require cyproheptadine and ICU if severe |
| QTc prolongation / Torsade de Pointes | Rare (post-marketing) | Variable; dose-related | Baseline and periodic ECG in at-risk patients; avoid concomitant QTc-prolonging drugs; discontinue if clinically significant prolongation |
| Hyponatraemia (SIADH) | Uncommon (higher risk in elderly) | First weeks of treatment | Check serum sodium if confusion, weakness, or falls develop. Discontinue sertraline and manage per standard of care if symptomatic. Cases with Na <110 mmol/L reported |
| Activation of mania / hypomania | 0.4% in controlled trials | First weeks of treatment | Screen for bipolar disorder before prescribing. Discontinue sertraline if mania develops |
| Severe bleeding events | Uncommon | Any time, increased with NSAIDs/anticoagulants | Counsel about bleeding risk; monitor INR with warfarin; GI bleeding may occur especially with NSAIDs |
| Seizures | Rare | Variable | Use with caution in patients with seizure disorders; discontinue if seizures occur |
| Angle-closure glaucoma | Rare | Variable | Avoid in patients with untreated anatomically narrow angles; refer for ophthalmological assessment if visual symptoms occur |
DiscontinuationDiscontinuation Rates
Overall Discontinuation Due to AEs
12% vs 4% placebo
Top reasons: Nausea (3%), diarrhoea (2%), agitation (2%), insomnia (2%)
MDD-Specific Additional Reasons
>2% (and twice placebo)
Decreased appetite, dizziness, fatigue, headache, somnolence, tremor, vomiting
Managing Sexual Dysfunction
Sexual side effects (decreased libido, ejaculatory delay, erectile dysfunction, anorgasmia) are class effects of SSRIs and are frequently underreported. Inquire about sexual function before starting sertraline and at follow-up visits. Management strategies include dose reduction, switching timing of dose, drug holidays (not recommended with daily dosing for depression), adding bupropion, or switching to an antidepressant with a lower sexual AE profile (e.g., bupropion, mirtazapine).
Drug Interactions
Sertraline is primarily metabolised by multiple CYP enzymes (CYP2B6, 2C9, 2C19, 2D6, 3A4) and is a mild-to-moderate inhibitor of CYP2D6. It is 98% protein-bound. The most clinically significant interactions involve MAOIs (contraindicated), pimozide (contraindicated), and other serotonergic agents (risk of serotonin syndrome). Sertraline has a lower CYP2D6 inhibition potential than fluoxetine or paroxetine but can still elevate levels of CYP2D6 substrates with narrow therapeutic indices.
MajorMAOIs (selegiline, tranylcypromine, phenelzine, linezolid, IV methylene blue)
MechanismDual inhibition of serotonin reuptake and metabolism leads to dangerous serotonin accumulation
EffectPotentially life-threatening serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability)
ManagementContraindicated. Minimum 14-day washout between sertraline and MAOIs in either direction
FDA PI — ContraindicationMajorPimozide
MechanismSertraline increases pimozide plasma concentrations (~40% AUC and Cmax increase at sertraline 200 mg/day)
EffectIncreased risk of QTc prolongation and ventricular arrhythmias
ManagementContraindicated. Use alternative antipsychotic
FDA PI — ContraindicationMajorOther serotonergic agents (triptans, TCAs, fentanyl, tramadol, lithium, St. John’s Wort, buspirone, amphetamines)
MechanismAdditive serotonergic activity through various mechanisms
EffectIncreased risk of serotonin syndrome, especially with multiple serotonergic agents
ManagementMonitor for serotonin syndrome signs; use lowest effective doses; consider alternatives. With lithium, monitor lithium levels
FDA PIModerateCYP2D6 substrates (e.g., metoprolol, propafenone, flecainide, atomoxetine, TCAs)
MechanismSertraline inhibits CYP2D6, increasing exposure of substrates
EffectElevated levels of co-administered CYP2D6 substrates, particularly those with narrow therapeutic indices
ManagementReduce dose of CYP2D6 substrate as needed; monitor for toxicity. If sertraline discontinued, may need to increase substrate dose
FDA PIModerateWarfarin & anticoagulants / NSAIDs
MechanismSSRIs impair platelet serotonin uptake, reducing aggregation; protein-binding displacement with warfarin
EffectIncreased bleeding risk (GI haemorrhage, ecchymosis, epistaxis); INR may fluctuate
ManagementMonitor INR carefully when starting/stopping sertraline in warfarin patients; counsel on bleeding signs
FDA PIModeratePhenytoin
MechanismSertraline may increase phenytoin concentrations (narrow therapeutic index drug)
EffectPotential phenytoin toxicity (nystagmus, ataxia, confusion)
ManagementMonitor phenytoin levels when initiating or titrating sertraline; adjust phenytoin dose as needed
FDA PI
Drugs with No Clinically Important Interaction
Based on pharmacokinetic studies, no sertraline dose adjustment is needed when co-administered with cimetidine, diazepam, lithium (monitor levels), atenolol, tolbutamide, digoxin, or CYP3A4 substrates (FDA PI). Sertraline also causes false-positive urine immunoassay screening for benzodiazepines; confirm with GC/MS if positive.
Monitoring
- Suicidality / Clinical WorseningWeekly for first 4 weeks, then biweekly, then monthly
RoutineFDA Boxed Warning: closely monitor all patients, especially under 25, for emergence of suicidal thoughts, clinical worsening, and unusual behavioural changes during initial treatment and dose adjustments. Counsel family/caregivers to be vigilant. - Symptom ResponseBaseline, then every 2–4 weeks initially
RoutineUse validated scales (PHQ-9 for depression, GAD-7 for anxiety, Y-BOCS for OCD, PCL-5 for PTSD) to track response. Allow 4–6 weeks at adequate dose before concluding inadequate response. - Sexual FunctionBaseline, then at follow-up visits
RoutineInquire proactively about changes in desire, arousal, and orgasm. Sexual AEs are underreported. Discuss management strategies early to support treatment adherence. - Weight / Growth (Paediatric)Baseline, then every 3 months
RoutineDecreased appetite and weight loss observed with SSRIs. Monitor height and weight in paediatric patients on long-term therapy. - Serum SodiumBaseline if at risk, then as indicated
Trigger-basedHyponatraemia (SIADH) risk higher in elderly, those on diuretics, and volume-depleted patients. Check sodium if confusion, weakness, or falls develop. - ECG (QTc)Baseline if risk factors present
Trigger-basedQTc prolongation reported post-marketing; positive concentration-QTc relationship in TQT study. Obtain baseline ECG in patients with cardiac risk factors, concomitant QTc-prolonging drugs, or electrolyte abnormalities. - Bipolar ScreeningBefore initiation
RoutineScreen for personal or family history of bipolar disorder, mania, or hypomania before starting sertraline. Mania/hypomania reported in 0.4% of patients in controlled trials.
Contraindications & Cautions
Absolute Contraindications
- Concomitant MAOI use or within 14 days of stopping MAOIs (including linezolid and IV methylene blue) — risk of serotonin syndrome.
- Concomitant pimozide — risk of QTc prolongation and ventricular arrhythmias.
- Known hypersensitivity to sertraline (anaphylaxis, angioedema reported).
- Oral solution with disulfiram — oral solution contains 12% alcohol; risk of disulfiram-alcohol reaction.
Relative Contraindications (Specialist Input Recommended)
- Moderate–severe hepatic impairment (Child-Pugh 7–15): Use is not recommended due to significantly increased drug exposure.
- Unscreened or known bipolar disorder: Antidepressant monotherapy may trigger mania. Screen before prescribing; if bipolar suspected, use mood stabiliser with specialist guidance.
- Untreated anatomically narrow angles: Mydriasis from SSRIs may precipitate angle-closure glaucoma.
Use with Caution
- Pregnancy, especially third trimester: Neonates exposed to SSRIs late in pregnancy have developed complications requiring extended hospitalisation (respiratory distress, cyanosis, feeding difficulty, withdrawal). Risk of persistent pulmonary hypertension of the newborn (PPHN) with late-pregnancy exposure. First-trimester epidemiological data suggest no significant increase in major birth defects overall.
- Seizure disorders: Not systematically evaluated; patients with seizure history were excluded from trials. Prescribe with caution.
- Elderly patients: ~40% lower clearance; higher risk of hyponatraemia, falls, and bleeding. Start at lower doses.
- Patients on anticoagulants / NSAIDs: Increased bleeding risk. Monitor INR; counsel on signs of bleeding.
- QTc prolongation risk factors: Use with caution; avoid combining with other QTc-prolonging agents.
FDA Boxed Warning
Suicidal Thoughts and Behaviours in Paediatric and Young Adult Patients
Antidepressants increased the risk of suicidal thoughts and behaviours in paediatric patients (14 additional per 1,000 treated) and young adults aged 18–24 (5 additional per 1,000 treated) in short-term studies. No completed suicides occurred in paediatric trials. In adults over 24, antidepressants were associated with a reduction in suicidality compared to placebo (1 fewer per 1,000 for ages 25–64; 6 fewer per 1,000 for ages 65+). All patients starting sertraline should be closely monitored for clinical worsening, suicidality, and unusual behaviour changes, especially during the first few months and at times of dose adjustment.
Patient Counselling
Purpose of Therapy
Sertraline works by increasing serotonin levels in the brain, which helps improve mood, reduce anxiety, and manage obsessive thoughts and other symptoms. It typically takes 2–4 weeks to notice meaningful improvement, and full benefits may take 6–8 weeks. Patients should continue taking sertraline even if they feel better, as stopping prematurely increases the risk of relapse. The dose may be adjusted over time to find the best balance of effectiveness and tolerability.
How to Take
Take sertraline once daily, with or without food. Food may reduce nausea. If using the oral solution, it must be diluted in 4 oz (half cup) of water, ginger ale, lemon/lime soda, lemonade, or orange juice only — take immediately after mixing. Do not use the oral solution if you are taking disulfiram (Antabuse) as it contains 12% alcohol.
Mood Changes & Suicidal Thoughts
Tell patientIn some people, especially those under 25, antidepressants may cause new or worsening thoughts of self-harm during the first weeks of treatment. Have a trusted person check in with you regularly during this time. This risk decreases as treatment continues.
Call prescriberImmediately if you experience new or worsening depression, anxiety, panic attacks, agitation, irritability, aggression, impulsive behaviour, or thoughts of harming yourself.
GI Side Effects (Nausea, Diarrhoea)
Tell patientNausea and loose stools are the most common side effects and usually improve within the first 1–2 weeks. Taking sertraline with food can help. If diarrhoea is persistent, stay well hydrated.
Call prescriberIf nausea or diarrhoea is severe, persistent beyond 2 weeks, or causing dehydration.
Sexual Side Effects
Tell patientSome patients experience changes in sexual desire or function. This is a known class effect and is not something you should feel embarrassed to discuss. In some cases, adjusting the dose or timing can help.
Call prescriberIf sexual side effects are significantly affecting your quality of life or relationship, discuss management options with your prescriber.
Stopping Treatment
Tell patientDo not stop sertraline suddenly. Abrupt discontinuation can cause dizziness, nausea, headache, irritability, electric-shock sensations, and sleep problems. Always taper gradually under medical supervision.
Call prescriberIf you experience distressing symptoms when reducing or stopping sertraline, contact your prescriber to slow the taper.
Serotonin Syndrome
Tell patientTell all your healthcare providers that you take sertraline. Combining it with certain other medications (especially migraine drugs, pain medications like tramadol, or supplements like St. John’s Wort) can cause a dangerous condition called serotonin syndrome.
Call prescriberSeek emergency care if you develop agitation, confusion, rapid heart rate, high fever, muscle stiffness or twitching, or loss of coordination.
Sources
Regulatory (PI / SmPC)
- Viatris Inc. ZOLOFT (sertraline hydrochloride) tablets and oral solution: US Prescribing Information. NDA 019839/020990. Revised 08/2023. FDA LabelPrimary source for all dosing, pharmacokinetic, safety, and indication data in this monograph.
Key Clinical Trials
- Cipriani A, Furukawa TA, Salanti G, et al. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder: a systematic review and network meta-analysis. Lancet. 2018;391(10128):1357–1366. doi:10.1016/S0140-6736(17)32802-7Landmark network meta-analysis of 21 antidepressants; identified sertraline as one of the best first-line options based on combined efficacy and tolerability.
- Brady K, Pearlstein T, Asnis GM, et al. Efficacy and safety of sertraline treatment of posttraumatic stress disorder: a randomized controlled trial. JAMA. 2000;283(14):1837–1844. doi:10.1001/jama.283.14.1837Pivotal RCT demonstrating sertraline efficacy for PTSD, contributing to FDA approval for this indication.
- March JS, Biederman J, Wolkow R, et al. Sertraline in children and adolescents with obsessive-compulsive disorder: a multicenter randomized controlled trial. JAMA. 1998;280(20):1752–1756. doi:10.1001/jama.280.20.1752Key paediatric OCD trial supporting FDA approval of sertraline for OCD in children aged 6–17.
- Halbreich U, Bergeron R, Yonkers KA, Freeman E, Stout AL, Cohen L. Efficacy of intermittent, luteal phase sertraline treatment of premenstrual dysphoric disorder. Obstet Gynecol. 2002;100(6):1219–1229. doi:10.1016/s0029-7844(02)02326-8RCT supporting the luteal-phase intermittent dosing strategy for PMDD approved in the FDA label.
Guidelines
- American Psychiatric Association. Practice guideline for the treatment of patients with major depressive disorder, third edition. Am J Psychiatry. 2010;167(10 Suppl):1–152. APA GuidelinesAPA guideline recommending SSRIs including sertraline as first-line pharmacotherapy for MDD.
- National Institute for Health and Care Excellence (NICE). Depression in adults: treatment and management. NICE guideline [NG222]. June 2022. NICE NG222UK guideline recommending SSRIs as first-line pharmacotherapy for moderate-to-severe depression; sertraline listed as a preferred option.
Mechanistic / Basic Science
- Stahl SM. Mechanism of action of serotonin selective reuptake inhibitors: serotonin receptors and pathways mediate therapeutic effects and side effects. J Affect Disord. 1998;51(3):215–235. doi:10.1016/S0165-0327(98)00221-3Foundational review of SSRI pharmacology explaining receptor-mediated therapeutic effects and side effects relevant to clinical use of sertraline.
- Preskorn SH. Clinically relevant pharmacology of selective serotonin reuptake inhibitors: an overview with emphasis on pharmacokinetics and effects on oxidative drug metabolism. Clin Pharmacokinet. 1997;32(Suppl 1):1–21. doi:10.2165/00003088-199700321-00003Comprehensive review of SSRI pharmacokinetics comparing CYP inhibition profiles; positions sertraline as having lower CYP2D6 inhibition than fluoxetine or paroxetine.
Pharmacokinetics / Special Populations
- DeVane CL, Liston HL, Markowitz JS. Clinical pharmacokinetics of sertraline. Clin Pharmacokinet. 2002;41(15):1247–1266. doi:10.2165/00003088-200241150-00002Comprehensive PK review covering absorption, distribution, metabolism, elimination, and special populations for sertraline.
- Obach RS, Cox LM, Tremaine LM. Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyltransferases in human: an in vitro study. Drug Metab Dispos. 2005;33(2):262–270. doi:10.1124/dmd.104.002428Definitive in vitro study identifying the multiple enzymes (CYP2B6, 2C9, 2C19, 2D6, 3A4, MAO-A/B, UGTs) involved in sertraline metabolism.
- Wisner KL, Sit DK, Hanusa BH, et al. Major depression and antidepressant treatment: impact on pregnancy and neonatal outcomes. Am J Psychiatry. 2009;166(5):557–566. doi:10.1176/appi.ajp.2008.08081170Study evaluating neonatal outcomes with antidepressant exposure in pregnancy; informs clinical decision-making about sertraline use in pregnant women.