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a selective-serotonin reuptake inhibitor commonly prescribed as an antidepressant (trade name Zoloft) (同)Zoloft

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/04/19 14:27:49」(JST)

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"Lustral" redirects here. For the electronic music band, see Lustral (band).

"Zoloft" redirects here. For the rock band, see Zolof the Rock & Roll Destroyer.

Sertraline (trade names Zoloft, Lustral) is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It was introduced to the market by Pfizer in 1991. Sertraline is primarily prescribed for major depressive disorder in adult outpatients as well as obsessive–compulsive, panic, and social anxiety disorders in both adults and children. In 2011, it was the second-most prescribed antidepressant on the U.S. retail market, with 37,208,000 prescriptions.^[4]

Differences with other newer antidepressants are subtle and mostly confined to side effects. Evidence suggests that sertraline may work better than fluoxetine (Prozac) for some subtypes of depression.^[5] Treatment of panic disorder with sertraline results in a decrease of the number of panic attacks and an improved quality of life.^[6] For obsessive-compulsive disorder, sertraline is not as effective as cognitive behavioral therapy; the best results have been achieved by combining these two treatments.^[7]^[8] Although approved for social phobia and posttraumatic stress disorder, sertraline leads to only modest improvement in these conditions.^[9]^[10] Sertraline also alleviates the symptoms of premenstrual dysphoric disorder and can be used in sub-therapeutic doses or intermittently for its treatment.

1 Medical uses
- 1.1 Depression
  - 1.1.1 Comparison with other antidepressants
  - 1.1.2 Elderly
- 1.2 Obsessive-compulsive disorder
- 1.3 Panic disorder
- 1.4 Social phobia
- 1.5 Premenstrual dysphoric disorder
- 1.6 Other indications
2 Adverse effects
- 2.1 Sexual side effects
- 2.2 Suicide
- 2.3 Overdosage
- 2.4 Pregnancy and lactation
- 2.5 Withdrawal syndrome
- 2.6 Interactions
- 2.7 Incidence
3 Mechanism of action
4 Pharmacokinetics
5 History
6 Pfizer advertisements
7 References
8 External links

Medical uses

Sertraline is used for a number of conditions including: major depression, obsessive-compulsive disorder (OCD), body dysmorphic disorder (BDD), posttraumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD), panic disorder and social phobia (social anxiety disorder).^[11] It has also been used for premature ejaculation and vascular headaches but evidence of the effectiveness in treating those conditions is not robust.^[11]

Depression

The original pre-marketing clinical trials demonstrated only weak-to-moderate efficacy of sertraline for depression. A 2008 review found that only 51% of studies of various ssri's yielded positive outcomes.^[12] Sertraline may be more effective for severe depression^[13]

Evidence does not show a benefit in children with depression.^[14]

With depression in dementia, there is no benefit compared to either placebo or mirtazapine.^[15]

Comparison with other antidepressants

TCAs as a group are considered to work better than selective serotonin reuptake inhibitors for melancholic depression^[16] and in inpatients,^[17] but not necessarily for simply more severe depression.^[18] In line with this generalization, sertraline was no better than placebo in inpatients (see History) and as effective as the TCA clomipramine for severe depression.^[13] The comparative efficacy of sertraline and TCAs for melancholic depression has not been studied. A 1998 review suggested that, due to its pharmacology, sertraline may be more efficacious than other SSRIs and equal to TCAs for the treatment of melancholic depression.^[19]

A meta-analysis of 12 new-generation antidepressants, sertraline and escitalopram are the best in terms of efficacy and acceptability in the acute-phase treatment of adults with unipolar major depression. Reboxetine was significantly worse.^[20]

Comparative clinical trials demonstrated that sertraline's efficacy in depression is similar to that of moclobemide,^[21] nefazodone,^[22] escitalopram,^[23] bupropion,^[24] citalopram, fluvoxamine, paroxetine and mirtazapine.^[25] Meta-analysis indicated that sertraline is more efficacious for the treatment of depression than fluoxetine (Prozac), with a 1.4 times higher probability of response, and is possibly better tolerated.^[26]^[27]

Elderly

Sertraline used for the treatment of depression in elderly (older than 60) patients was superior to placebo and comparable to another SSRI fluoxetine, and TCAs amitriptyline, nortriptyline (Pamelor) and imipramine. Sertraline had much lower rates of adverse effects than these TCAs, with the exception of nausea, which occurred more frequently with sertraline. In addition, sertraline appeared to be more effective than fluoxetine or nortriptyline in the older-than-70 subgroup.^[28] A 2003 trial of sertraline vs. placebo in elderly patients showed a statistically significant (that is, unlikely to occur by chance), but clinically very modest improvement in depression and no improvement in quality of life.^[29] The authors were sharply criticized by Bernard Carroll, a one-time chairman of the FDA Psychopharmacological Drugs Advisory Committee,^[30] for presenting these results as positive: "The study has all the hallmarks of an 'experimercial,' a cost-is-no-object exercise driven by a corporate sponsor to create positive publicity for its product in a market niche. ... Thus does the corporate mandate to put lipstick on the pig prevail over the academic duty to communicate independent analyses of the data."^[31]

Obsessive-compulsive disorder

Placebo-controlled studies have demonstrated sertraline to be effective for the treatment of OCD in adults and children.^[32] It was better tolerated and, based on intention to treat analysis, performed better than the gold standard of OCD treatment clomipramine.^[33] It is generally accepted that the sertraline dosages necessary for the effective treatment of OCD are higher than the usual dosage for depression.^[34] The onset of action is also slower for OCD than for depression. The treatment recommendation is to start treatment with a half of maximal recommended dose for at least two months. After that, the dose can be raised to the maximal recommended in the cases of unsatisfactory response.^[35]

Cognitive behavioral therapy alone was superior to sertraline in both adults and children; however, the best results were achieved using a combination of these treatments.^[7]^[8] A review mentions that sertraline can be used for the treatment of OCD co-morbid with Tourette syndrome;^[36] however, sertraline may cause exacerbation of tics in Tourette syndrome.^[37]

Panic disorder

In four double-blind studies sertraline was shown to be superior to placebo for the treatment of panic disorder. The response rate was independent of the dose. In addition to decreasing the frequency of panic attacks by about 80% (vs. 45% for placebo) and decreasing general anxiety, sertraline resulted in improvement of quality of life on most parameters. The patients rated as "improved" on sertraline reported better quality of life than the ones who "improved" on placebo. The authors of the study argued that the improvement achieved with sertraline is different and of a better quality than the improvement achieved with placebo.^[6]^[38] Sertraline was equally effective for men and women.^[38] While imprecise, comparison of the results of trials of sertraline with separate trials of other anti-panic agents (clomipramine, imipramine, clonazepam, alprazolam, fluvoxamine and paroxetine) indicates approximate equivalence of these medications.^[6]

Social phobia

Sertraline has been successfully used for the treatment of social phobia (social anxiety disorder).^[39] In a flexible dosing study, it appeared that a higher dose range was needed for adequate response. The response was higher among the patients with later onset, especially adult onset, of the disorder.^[9] In addition to psychological components of social phobia, such as fear and avoidance, sertraline also ameliorated some physiological components, such as blushing and palpitations but not sweating and trembling.^[40]

Premenstrual dysphoric disorder

SSRIs, including sertraline, reduce the symptoms of premenstrual syndrome.^[41] Side effects such as nausea are common.^[41]

Sertraline is effective in alleviating the symptoms of PMDD, a severe form of premenstrual syndrome. Significant improvement was observed in 50–60% of cases treated with sertraline vs. 20–30% of cases on placebo. The improvement began during the first week of treatment, and in addition to mood, irritability, and anxiety, improvement was reflected in better family functioning, social activity and general quality of life. Work functioning and physical symptoms, such as swelling, bloating and breast tenderness, were less responsive to sertraline.^[42]^[43] Taking sertraline only during the luteal phase, that is, the 12–14 days before menses, was shown to work as well as continuous treatment.^[41]

Other indications

Sertraline when taken daily can be useful for the treatment of some aspects of premature ejaculation.^[44] A disadvantage of SSRIs is that they require continuous daily treatment to delay ejaculation significantly.^[45] And it is not clear how they affect psychological distress of those with the condition or the persons control over ejaculation timing.^[46]

Medications should not generally be used in posttraumatic stress disorder (PTSD).^[47] While sertraline may be useful in some, this benefit is not significant per the National Institute of Clinical Excellence.^[48] Others however do feel that there is a benefit from their use.^[49]

Adverse effects

Zoloft 50 mg & 25 mg tablets (US)

Zoloft 100 mg tablets (AU)

Compared to other SSRIs sertraline tends to be associated with a higher rate of psychiatric side effects and diarrhoea.^[50]^[51] It tends to be more activating (that is, associated with a higher rate of anxiety, agitation, insomnia, etc.) than other SSRIs, aside from fluoxetine.^[52]

Akathisia—that is, "inner tension, restlessness, and the inability to stay still"—caused by sertraline was observed in 16% of patients in a case series.^[53] This and other reports^[54]^[55]^[56] note that akathisia begins soon after the initiation of treatment or a dose increase; often, several hours after taking the medication. Akathisia usually disappears within several days after sertraline is stopped or its dose is decreased. In some cases, clinicians confused akathisia with anxiety and increased the dose of sertraline, causing further worsening of the patients' symptoms.^[56] Experts note that because of the possible link of akathisia with suicide and the distress it causes to the patient, "it is of vital importance to increase awareness amongst staff and patients of the symptoms of this relatively common condition."^[57]^[58]

Over more than six months of sertraline therapy for depression, patients showed an insignificant weight increase of 0.1%.^[59] Similarly, a 30-month-long treatment with sertraline for OCD resulted in a mean weight gain of 1.5% (1 kg).^[60] Although the difference did not reach statistical significance, the weight gain was lower for fluoxetine (Prozac) (1%) but higher for citalopram (Celexa), fluvoxamine (Luvox) and paroxetine (Paxil) (2.5%). Only 4.5% of the sertraline group gained a large amount of weight (defined as more than 7% gain). This result compares favorably with placebo, where, according to the literature, 3–6% of patients gained more than 7% of their initial weight. The large weight gain was observed only among female members of the sertraline group; the significance of this finding is unclear because of the small size of the group.^[60]

Over a two-week treatment of healthy volunteers, sertraline slightly improved verbal fluency but did not affect word learning, short-term memory, vigilance, flicker fusion time, choice reaction time, memory span, or psychomotor coordination.^[61]^[62] In spite of lower subjective rating, that is, feeling that they performed worse, no clinically relevant differences were observed in the objective cognitive performance in a group of people treated for depression with sertraline for 1.5 years as compared to healthy controls.^[63] In children and adolescents taking sertraline for six weeks for anxiety disorders, 18 out of 20 measures of memory, attention and alertness stayed unchanged. Divided attention was improved and verbal memory under interference conditions decreased marginally. Because of the large number of measures taken, it is possible that these changes were still due to chance.^[64] The unique effect of sertraline on dopaminergic neurotransmission may be related to these effects on cognition and vigilance.^[65]^[66]

Sexual side effects

Like other SSRIs, sertraline is associated with sexual side effects, including sexual arousal disorder and difficulty achieving orgasm. The observed frequency of sexual side effects depends greatly on whether they are reported by patients spontaneously, as in the manufacturer's trials, or actively solicited by the physicians. There have been several double-blind studies of sexual side effects comparing sertraline with placebo or other antidepressants.^[67] While nefazodone (Serzone) and bupropion (Wellbutrin) did not have negative effects on sexual functioning, 67% of men on sertraline experienced ejaculation difficulties vs. 18% before the treatment^[67] (or 61% vs. 0% according to another paper).^[24] Similarly, in a group of women who initially did not have difficulties achieving orgasm, 41% acquired this problem during treatment with sertraline.^[24] A 40% rate of orgasm dysfunction (vs. 9% for placebo) on sertraline was observed in a mixed group in another study.^[68] Sexual arousal disorder, defined as "inadequate lubrication and swelling for women and erectile difficulties for men", occurred in 12% of patients on sertraline as compared with 1% of patients on placebo. The mood improvement resulting from the treatment with sertraline sometimes counteracted these side effects, so that sexual desire and overall satisfaction with sex stayed the same as before the sertraline treatment. However, under the action of placebo the desire and satisfaction slightly improved.^[68]

Genital anesthesia,^[69] loss of or decreased response to sexual stimuli, and ejaculatory anhedonia are also possible. Although usually reversible, for some people these effects are long-term and may persist after drug treatment is discontinued.^[70] This is known as post-SSRI sexual dysfunction.

Suicide

The FDA requires all antidepressants, including sertraline, to carry a black box warning stating that antidepressants may increase the risk of suicide in persons younger than 25. This warning is based on statistical analyses conducted by two independent groups of FDA experts that found a 2-fold increase of suicidal ideation and behavior in children and adolescents, and a 1.5-fold increase of suicidal behavior in the 18–24 age group.^[71]^[72]^[73]

Suicidal ideation and behavior in clinical trials are rare. For the above analysis, the FDA combined the results of 295 trials of 11 antidepressants for psychiatric indications in order to obtain statistically significant results. Considered separately, sertraline use in adults decreased the odds of suicidal behavior with a marginal statistical significance by 37%^[73] or 50%^[72] depending on the statistical technique used. The authors of the FDA analysis note that "given the large number of comparisons made in this review, chance is a very plausible explanation for this difference".^[72] The more complete data submitted later by the sertraline manufacturer Pfizer indicated increased suicidal behavior.^[74] Similarly, the analysis conducted by the UK MHRA found a 50% increase of odds of suicide-related events, not reaching statistical significance, in the patients on sertraline as compared to the ones on placebo.^[75]^[76]

Overdosage

Acute overdosage is often manifested by emesis, lethargy, ataxia, tachycardia and seizures. Plasma, serum or blood concentrations of sertraline and norsertraline, its major active metabolite, may be measured to confirm a diagnosis of poisoning in hospitalized patients or to aid in the medicolegal investigation of fatalities.^[77] As with most other SSRIs its toxicity in overdose is considered relatively low.^[50]^[78]

Pregnancy and lactation

The studies comparing the levels of sertraline and its principal metabolite, desmethylsertraline, in mother's blood to their concentration in umbilical cord blood at the time of delivery indicated that foetal exposure to sertraline and its metabolite is approximately a third of the maternal exposure.^[79]^[80] The use of sertraline during the first trimester of pregnancy was associated with increased odds of the following birth defects: omphalocele (six-fold), anal atresia and limb reduction defects (four-fold), and septal defects (two-fold); however these specific defects themselves are rare and therefore the absolute risks are small.^[81] Concentration of sertraline and desmethylsertraline in breast milk is highly variable and, on average, is of the same order of magnitude as their concentration in the blood plasma of the mother. As a result, more than half of breast-fed babies receive less than 2 mg/day of sertraline and desmethylsertraline combined, and in most cases these substances are undetectable in their blood.^[82] No changes in serotonin uptake by the platelets of breast-fed infants were found, as measured by their blood serotonin levels before and after their mothers began sertraline treatment.^[83]

Withdrawal syndrome

Main article: SSRI discontinuation syndrome

Abrupt interruption of sertraline treatment may result in withdrawal or discontinuation syndrome. This syndrome occurred in 60% of the remitted depressed patients taking sertraline in a blind discontinuation study, as compared to 14% of patients on fluoxetine and 66% of patients on paroxetine.^[84] During the 5–8-day period when sertraline was temporarily replaced by placebo, the most frequent symptoms (reported by more than a quarter of patients) were irritability, agitation, dizziness, headache, nervousness, crying, emotional lability, bad dreams and anger. Around a third experienced mood worsening to the level generally associated with a major depressive episode.^[84] In a double-blind study of remitted panic disorder patients, abrupt discontinuation of sertraline treatment resulted in insomnia and dizziness (both 16–17% vs. 4% for continuing treatment), although headache, depression and malaise did not increase significantly.^[85] In another double-blind study of recovered panic disorder patients, the withdrawal syndrome was completely avoided when sertraline was gradually discontinued over three weeks, while patients stopping paroxetine treatment still suffered from it.^[86] There is at least one report of orthostatic hypotension as a result of sertraline withdrawal.^[87]

Interactions

Sertraline is a moderate inhibitor of CYP2D6 and CYP2B6 in vitro.^[88] Accordingly, in human trials it caused increased blood levels of CYP2D6 substrates such as metoprolol, dextromethorphan, desipramine, imipramine and nortriptyline, as well as the CYP3A4/CYP2D6 substrate haloperidol.^[89]^[90]^[91] This effect is dose-dependent; for example, co-administration with 50 mg of sertraline resulted in 20% greater exposure to desipramine, while 150 mg of sertraline led to a 70% increase.^[92]^[93] In a placebo-controlled study, the concomitant administration of sertraline and methadone caused a 40% increase in blood levels of the latter, which is primarily metabolized by CYP2B6.^[94] Sertraline is often used in combination with stimulant medication for the treatment of co-morbid depression and/or anxiety in ADHD^[95] Sertraline reduces amphetamine metabolism as a result of CYP2D6 inhibition.^[96]

Sertraline had a slight inhibitory effect on the metabolism of diazepam, tolbutamide and warfarin, which are CYP2C9 or CYP2C19 substrates; this effect was not considered to be clinically relevant.^[92] As expected from in vitro data, sertraline did not alter the human metabolism of the CYP3A4 substrates erythromycin, alprazolam, carbamazepine, clonazepam, and terfenadine; neither did it affect metabolism of the CYP1A2 substrate clozapine.

Sertraline had no effect on the actions of digoxin and atenolol, which are not metabolized in the liver.^[88]^[92]^[97]^[98] Case reports suggest that taking sertraline with phenytoin or zolpidem may induce sertraline metabolism and decrease its efficacy,^[99]^[100] and that taking sertraline with lamotrigine may increase the blood level of lamotrigine, possibly by inhibition of glucuronidation.^[101]

Clinical reports indicate that interaction between sertraline and the MAOIs isocarboxazid and tranylcypromine may cause serotonin syndrome. In a placebo-controlled study in which sertraline was co-administered with lithium, 35% of the subjects experienced tremors, while none of those taking placebo did.^[92]

According to Pfizer, sertraline is contraindicated in individuals taking monoamine oxidase inhibitors or the antipsychotic pimozide (Orap). Sertraline concentrate contains alcohol, and is therefore contraindicated with disulfiram (Antabuse). The prescribing information recommends that treatment of the elderly and patients with liver impairment "must be approached with caution." Due to the slower elimination of sertraline in these groups, their exposure to sertraline may be as high as three times the average exposure for the same dose.^[97]

Incidence

Adverse effects by incidence.^[102]^[103]^[104]^[105]

Very common (>10%):

Fatigue
Insomnia
Somnolence (drowsiness)
Nausea
Dry mouth
Diarrhoea
Headache
Ejaculation disorder
Dizziness

Common (1-10%):

Agitation
Anorexia
Constipation
Dyspepsia (indigestion)
Decreased libido
Sweating
Tremor
Vomiting
Impaired concentration
Nervousness
Paroniria (i.e., depraved or morbid dreaming/nightmares)
Yawning
Palpitations
Increased sweating
Hot flushes
Weight decrease
Weight increase
Myoclonus
Hypertonia
Teeth grinding
Hypoaesthesia
Menstrual irregularities
Sexual dysfunction
Rash
Vision abnormal
Asthenia
Chest pain
Paraesthesia
Tinnitus (hearing ringing in the ears)

Uncommon (0.1-1%):

Hypertension (high blood pressure)
Hyperkinesia
Bronchospasm
Oesophagitis (swollen oesophagus)
Dysphagia
Haemorrhoids
Periorbital Oedema
Purpura
Cold Sweat
Dry skin
Nocturia
Urinary Retention
Polyuria (excessive urination)
Vaginal Haemorrhage
Malaise
Chills
Pyrexia (fever)
Thirst

Pollakiuria
Micturition disorder

Salivary Hypersecretion
Tongue Disorder
Osteoarthritis
Muscular Weakness
Back Pain
Muscle Twitching

Eructation (belching)
Dyspnoea (air hunger)
Epistaxis (nose bleed)
Oedema peripheral
Periorbital edema
Syncope
Postural dizziness
Tachycardia (high heart rate)
Urticaria (hives)
Migraine
Abnormal bleeding (esp. in the GI tract)
Muscle cramps
Arthralgia
Depressive symptoms
Euphoria
Hallucination
Alopecia (hair loss)
Urinary Retention (being unable to pass urine)
Pruritus
Amnesia memory loss.
Urinary incontinence
Eye pain
Asymptomatic elevations in serum transaminases
Abnormal semen
Melaena (black faeces due to a bleed in the stomach)
Haematochezia
Stomatitis (swollen mouth)
Tongue ulceration
Tooth Disorder
Glossitis (soreness/swelling of the tongue)
Mouth Ulceration
Laryngospasm
Hyperventilation (breathing more often than required to keep one's blood sufficiently oxygenated)
Hypoventilation (breathing less often than required to keep one's blood sufficiently oxygenated)
Stridor
Dysphonia (voice disorder)
Upper Respiratory Tract Infection
Rhinitis (irritation/inflammation inside the nose)
Hiccups
Apathy
Thinking Abnormal

Rare (<0.1%)

Allergic reaction
Allergy
Anaphylactoid reaction
Face oedema
Priapism
Atrial arrhythmia
AV block
Coma
Peripheral Ischaemia
Injury
Vasodilation Procedure

Lymphadenopathy
Involuntary muscle contractions
Galactorrhoea (lactation that is unrelated to pregnancy or breastfeeding)
Gynaecomastia (swelling of breast tissue in men)
Hyperprolactinaemia (high blood prolactin levels)
Hypothyroidism (underactive thyroid gland)
Syndrome of inappropriate secretion of antidiuretic hormone (SIADH)
Pancreatitis (swollen pancreas)
Altered platelet function
Haematuria (blood in the urine)
Leukopenia (low white blood cell count)
Thrombocytopenia (low blood platelet count)
Increased coagulation times
Abnormal clinical laboratory results
Hyponatraemia (low blood sodium)
Conversion Disorder
Drug Dependence
Paranoia
Myocardial Infarction (heart attack)
Bradycardia
Cardiac Disorder
Suicidal Ideation/behaviour
Sleep Walking
Premature Ejaculation
Hyperglycemia (high blood sugar)
Hypoglycemia (low blood sugar)
Hypercholesterolaemia (high blood cholesterol)
Vasculitis
Aggressive reaction
Psychosis (hallucinations and delusions)
Mania (a dangerously elated mood)
Menorrhagia (an abnormally excessive amount of menstrual bleeding)
Atrophic Vulvovaginitis
Balanoposthitis
Genital Discharge
Angioedema
Photosensitivity skin reaction
Enuresis
Visual field defect
Abnormal liver function
Dermatitis
Dermatitis Bullous
Rash Follicular
Glaucoma
Lacrimal Disorder
Scotoma
Diplopia
Photophobia
Hyphaema
Mydriasis

Hair Texture Abnormal
Neoplasm
Diverticulitis
Choreoathetosis
Dyskinesia
Hyperaesthesia
Sensory Disturbance
Gastroenteritis
Otitis Media
Skin Odour Abnormal

Unknown frequency

QTc prolongation
Anaphylactoid Reaction
Allergic Reaction
Allergy

Neuroleptic malignant syndrome. A potentially fatal reaction that most often occurs as a result of the use of antipsychotic drugs. It is characterised by fever, muscle rigidity, rhabdomyolysis (muscle breakdown), profuse sweating, tachycardia, tachypnoea (rapid breathing), agitation.
Stevens-Johnson syndrome a potentially fatal skin reaction.
Toxic epidermal necrolysis another potentially fatal skin reaction.

Torsades de pointes a potentially fatal change in the heart's rhythm.
Cerebrovascular spasm
Serotonin syndrome similar to neuroleptic malignant syndrome but develops more rapidly (over a period of hours instead of days/weeks for neuroleptic malignant syndrome)
Bone fracture
Movement disorders
Diabetes mellitus
Dyspnoea
Jaundice yellowing of the skin, mucous membranes and eyes due to an impaired ability of the liver to clear the haem breakdown by product, bilirubin.
Hepatitis
Liver failure

Mechanism of action

Sertraline is primarily a serotonin reuptake inhibitor (SRI) with a binding affinity towards the serotonin transporter of K_i=0.3 nM.^[3] Therapeutic doses of sertraline (25–200 mg/day) taken by patients for four weeks resulted in 80–90% inhibition of serotonin transporter (SERT) in striatum as measured by positron emission tomography. A daily 9 mg dose was sufficient to inhibit 50% of SERT.^[106]

Sertraline molecule

Sertraline is also a dopamine reuptake inhibitor, (<50 nmol/L). However, this is not considered a tight binding, and this action is only 10% of its potency as a monoamine reuptake inhibitor.^[107] It is a σ₁ receptor agonist with 5% of its SRI potency,^[108] and an α₁-adrenoreceptor antagonist with 1–10% of its SRI potency.^[109] However, though confirming sertraline's high affinity for σ₁ receptors, different studies suggest that the drug actually behaves as an antagonist at those.^[110]

Sertraline demonstrated anti-fungal activity against Candida and Aspergillus species in vitro and in vivo.^[111]^[112]

Pharmacokinetics

Norsertraline, sertraline's chief active metabolite

Sertraline is absorbed slowly when taken orally, achieving its maximal concentration in the plasma 4–6 hours after ingestion. In the blood, it is 98.5% bound to plasma proteins. Its half-life in the body is 13–45 hours and, on average, is about 1.5 times longer in women (32 hours) than in men (22 hours), leading to a 1.5-times-higher exposure in women.^[92] According to in vitro studies, sertraline is metabolized by multiple cytochrome 450 isoforms: CYP2D6, CYP2C9, CYP2B6, CYP2C19 and CYP3A4. It appeared unlikely that inhibition of any single isoform could cause clinically significant changes in sertraline pharmacokinetics.^[1]^[113] No differences in sertraline pharmacokinetics were observed between people with high and low activity of CYP2D6;^[114] however, poor CYP2C19 metabolizers had a 1.5-times-higher level of sertraline than normal metabolizers.^[115] In vitro data also indicate that the inhibition of CYP2B6 should have even greater effect than the inhibition of CYP2C19, while the contribution of CYP2C9 and CYP3A4 to the metabolism of sertraline would be minor. These conclusions have not been verified in human studies.^[1] Sertraline can be deaminated in vitro by monoamine oxidases; however, this metabolic pathway has never been studied in vivo.^[1] The major metabolite of sertraline, desmethylsertraline, is about 50 times weaker as a serotonin transporter inhibitor than sertraline and its clinical effect is negligible.^[109]

Non-amine metabolites may also contribute to the antidepressant effects of this medication. Sertraline deaminated is O-2098, a compound that has been found to inhibit the dopamine reuptake transporter proteins in spite of its lack of a nitrogen atom.^[116]

Its chief active metabolite is norsertraline (N-desmethylsertraline) which is significantly less biologically active than its parent compound.^[117]

History

Skeletal formulae of chlorprothixene and tametraline, from which sertraline was derived

The history of sertraline dates back to the early 1970s, when Pfizer chemist Reinhard Sarges invented a novel series of psychoactive compounds based on the structures of neuroleptics chlorprothixene and thiothixene.^[118]^[119] Further work on these compounds led to tametraline, a norepinephrine and weaker dopamine reuptake inhibitor. Development of tametraline was soon stopped because of undesired stimulant effects observed in animals. A few years later, in 1977, pharmacologist Kenneth Koe, after comparing the structural features of a variety of reuptake inhibitors, became interested in the tametraline series. He asked another Pfizer chemist, Willard Welch, to synthesize some previously unexplored tametraline derivatives. Welch generated a number of potent norepinephrine and triple reuptake inhibitors, but to the surprise of the scientists, one representative of the generally inactive cis-analogs was a serotonin reuptake inhibitor. Welch then prepared stereoisomers of this compound, which were tested in vivo by animal behavioral scientist Albert Weissman. The most potent and selective (+)-isomer was taken into further development and eventually named sertraline. Weissman and Koe recalled that the group did not set up to produce an antidepressant of the SSRI type—in that sense their inquiry was not "very goal driven", and the discovery of the sertraline molecule was serendipitous. According to Welch, they worked outside the mainstream at Pfizer, and even "did not have a formal project team". The group had to overcome initial bureaucratic reluctance to pursue sertraline development, as Pfizer was considering licensing an antidepressant candidate from another company.^[118]^[120]^[121]

Sertraline was approved by the U.S. Food and Drug Administration (FDA) in 1991 based on the recommendation of the Psychopharmacological Drugs Advisory Committee; it had already become available in the United Kingdom the previous year.^[122] The FDA committee achieved a consensus that sertraline was safe and effective for the treatment of major depression.

Sertraline entered the Australian market in 1994 and became the most often prescribed antidepressant in 1996 (2004 data).^[123] It was measured as among the top ten drugs ranked by cost to the Australian government in 1998 and 2000–01, having cost $45 million and $87 million in subsidies respectively.^[124]^[125] Sertraline is less popular in the UK (2003 data) and Canada (2006 data)—in both countries it was fifth (among drugs marketed for the treatment of MDD, or antidepressants), based on the number of prescriptions.^[126]^[127]

Until 2002, sertraline was only approved for use in adults ages 18 and over; that year, it was approved by the FDA for use in treating children aged 6 or older with severe obsessive-compulsive disorder (OCD). In 2003, the UK Medicines and Healthcare products Regulatory Agency issued a guidance that, apart from fluoxetine (Prozac), SSRIs are not suitable for the treatment of depression in patients under 18.^[128]^[129] However, sertraline can still be used in the UK for the treatment of OCD in children and adolescents.^[130] In 2005, the FDA added a black box warning concerning pediatric suicidal behavior to all antidepressants, including sertraline. In 2007, labeling was again changed to add a warning regarding suicidal behavior in young adults ages 18 to 24.^[131]

The U.S. patent for Zoloft expired in 2006,^[132] and sertraline is now available in generic form.

Pfizer advertisements

Further information: Chemical imbalance and Biology of depression#Monoamine hypothesis

The brand-name form of sertraline, Zoloft, was advertised to consumers by Pfizer using the following wording: "While the cause is unknown, depression may be related to an imbalance of natural chemicals between nerve cells in the brain. Prescription Zoloft works to correct this imbalance. You just shouldn't have to feel this way anymore." An essay published in the journal PLoS Medicine criticized these advertisements for their reliance on the "serotonin imbalance" theory of depression, although the monoamine hypothesis of antidepressant action was a leading theory at the time.^[133] When asked to comment, the FDA answered that such "reductionist statements" are acceptable to explain the neurochemistry of depression "to the fraction of the public that functions at no higher than a 6th-grade reading level."^[134]

An FDA Warning Letter was issued when a Zoloft advertisement omitted information about the risk of suicidal behavior.^[135]

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^ DeVane CL, Donovan JL, Liston HL, Markowitz JS, Cheng KT, Risch SC, Willard L (2004). "Comparative CYP3A4 inhibitory effects of venlafaxine, fluoxetine, sertraline, and nefazodone in healthy volunteers". Journal of Clinical Psychopharmacology 24 (1): 4–10. doi:10.1097/01.jcp.0000104908.75206.26. PMID 14709940.
^ Allard, S; Sainati, SM; Roth-Schechter, BF (1999). "Coadministration of short-term zolpidem with sertraline in healthy women". Journal of clinical pharmacology 39 (2): 184–91. doi:10.1177/00912709922007624. PMID 11563412. edit
^ Haselberger, MB; Freedman, LS; Tolbert, S (1997). "Elevated serum phenytoin concentrations associated with coadministration of sertraline". Journal of Clinical Psychopharmacology 17 (2): 107–9. doi:10.1097/00004714-199704000-00008. PMID 10950473. edit
^ Kaufman KR, Gerner R (1998). "Lamotrigine toxicity secondary to sertraline". Seizure 7 (2): 163–5. doi:10.1016/S1059-1311(98)80074-5. PMID 9627209.
^ "Zoloft (sertraline) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 30 September 2013.
^ "PRODUCT INFORMATION ZOLOFT® (sertraline hydrochloride)" (PDF). TGA eBusiness Services. Pfizer Australia Pty Ltd. 28 May 2013. Retrieved 30 September 2013.
^ "Sertraline 100mg Film coated Tablets - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Accord Healthcare Limited. 25 August 2013. Retrieved 27 November 2013.
^ "ZOLOFT (sertraline hydrochloride) tablet, film coated [PD-Rx Pharmaceuticals, Inc.]". DailyMed. PD-Rx Pharmaceuticals, Inc. September 2011. Retrieved 27 November 2013.
^ Meyer JH, Wilson AA, Sagrati S, Hussey D, Carella A, Potter WZ, Ginovart N, Spencer EP, Cheok A, Houle S (2004). "Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [¹¹C]DASB positron emission tomography study". The American Journal of Psychiatry 161 (5): 826–35. doi:10.1176/appi.ajp.161.5.826. PMID 15121647.
^ Owens JM, Knight DL, Nemeroff CB (2002). "Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine". Encephale 28 (4): 350–5. PMID 12232544.
^ Narita N, Hashimoto K, Tomitaka S, Minabe Y (1996). "Interactions of selective serotonin reuptake inhibitors with subtypes of sigma receptors in rat brain". Eur. J. Pharmacol. 307 (1): 117–9. doi:10.1016/0014-2999(96)00254-3. PMID 8831113.
^ ^a ^b Owens MJ, Morgan WN, Plott SJ, Nemeroff CB (1997). "Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites". J. Pharmacol. Exp. Ther. 283 (3): 1305–22. PMID 9400006.
^ Hashimoto, K (2009). "Sigma-1 Receptors and Selective Serotonin Reuptake Inhibitors: Clinical Implications of their Relationship". Central Nervous System Agents in Medicinal Chemistry 2009 (Sept): 197–204. [1] PDF
^ Lass-Flörl C, Ledochowski M, Fuchs D, et al. (2003). "Interaction of sertraline with Candida species selectively attenuates fungal virulence in vitro". FEMS Immunol. Med. Microbiol. 35 (1): 11–5. doi:10.1111/j.1574-695X.2003.tb00643.x. PMID 12589952.
^ Young, TJ; Oliver, GP; Pryde, D; Perros, M; Parkinson, T (April 2003). "Antifungal activity of selective serotonin reuptake inhibitors attributed to non-specific cytotoxicity". Journal of Antimicrobial Chemotherapy 51 (4): 1045–1047. doi:10.1093/jac/dkg184. PMID 12654745.
^ Kobayashi K, Ishizuka T, Shimada N, Yoshimura Y, Kamijima K, Chiba K (1999). "Sertraline N-demethylation is catalyzed by multiple isoforms of human cytochrome P-450 in vitro". Drug Metab. Dispos. 27 (7): 763–6. PMID 10383917.
^ Hamelin BA, Turgeon J, Vallée F, Bélanger PM, Paquet F, LeBel M (1996). "The disposition of fluoxetine but not sertraline is altered in poor metabolizers of debrisoquin". Clin. Pharmacol. Ther. 60 (5): 512–21. doi:10.1016/S0009-9236(96)90147-2. PMID 8941024.
^ Wang JH, Liu ZQ, Wang W, Chen XP, Shu Y, He N, Zhou HH (2001). "Pharmacokinetics of sertraline in relation to genetic polymorphism of CYP2C19". Clin. Pharmacol. Ther. 70 (1): 42–7. doi:10.1067/mcp.2001.116513. PMID 11452243.
^ Madras, Bertha K; Fahey, Michele A; Miller, Gregory M; De La Garza, Richard; Goulet, Martin; Spealman, Roger D; Meltzer, Peter C; George, Susan R; O'Dowd, Brian F et al. (2003). "Non-amine-based dopamine transporter (reuptake) inhibitors retain properties of amine-based progenitors". Eur. J. Pharmacol. 479 (1–3): 41–51. doi:10.1016/j.ejphar.2003.08.055. PMID 14612136.
^ Ciraulo, DA; Shader, RI, ed. (2011). "Pharmacotherapy of Depression". SpringerLink (2nd ed.) (New York, NY: Humana Press). doi:10.1007/978-1-60327-435-7. ISBN 978-1-60327-434-0. edit
^ ^a ^b The most complete account of sertraline discovery, targeted at chemists, see: Welch WM (1995). "Discovery and Development of Sertraline". Advances in Medicinal Chemistry. Advances in Medicinal Chemistry 3: 113–148. doi:10.1016/S1067-5698(06)80005-2. ISBN 978-1-55938-798-9.
^ Sarges R, Tretter JR, Tenen SS, Weissman A (1973). "5,8-Disubstituted 1-Aminotetralins. A Class of Compounds with a Novel Profile of Central Nervous System Activity". Journal of Medicinal Chemistry 16 (9): 1003–1011. doi:10.1021/jm00267a010. PMID 4795663.
^ See also: Mullin R (2006). "ACS Award for Team Innovation". Chemical & Engineering News 84 (5): 45–52. doi:10.1021/cen-v084n010.p045.
^ A short blurb on the history of sertraline, see: Couzin J (2005). "The brains behind blockbusters". Science 309 (5735): 728. doi:10.1126/science.309.5735.728. PMID 16051786.
^ Healy, David (1999). The Antidepressant Era. Cambridge, Massachusetts: Harvard University Press. p. 168. ISBN 0-674-03958-0.
^ Mant A; Rendle VA; Hall WD et al. (2004). "Making new choices about antidepressants in Australia: the long view 1975–2002". Med. J. Aust. 181 (7 Suppl): S21–4. PMID 15462638.
^ "Top 10 drugs – 1998". Australian Prescriber 22: 119. 1999. Retrieved 30 April 2008.
^ "Top 10 drugs – 2000–01". Australian Prescriber 24: 136. 2001. Retrieved 30 April 2008.
^ "Prescribing trends for SSRIs and related antidepressants" (PDF). UK MHRA. 2004. Retrieved 30 April 2008.
^ Skinner BJ, Rovere M (31 July 2007). "Canada's Drug Price Paradox 2007" (PDF). The Fraser Institute. pp. 21–29. Retrieved 11 July 2008.
^ "Safety review of antidepressants used by children completed". MHRA. 10 December 2003. Retrieved 11 July 2008.
^ Boseley, Sarah (10 December 2003). "Drugs for depressed children banned". The Guardian. Retrieved 19 April 2007.
^ "Overview of regulatory status and CSM advice relating to major depressive disorder (MDD) in children and adolescents". MHRA. Retrieved 17 April 2008.
^ Food and Drug Administration (2 May 2007). "FDA Proposes New Warnings About Suicidal Thinking, Behavior in Young Adults Who Take Antidepressant Medications". Retrieved 11 July 2008.
^ Smith, Aaron (17 July 2006). "Pfizer needs more drugs". CNNMoney.com. Retrieved 27 January 2007.
^ Owens MJ (2004). "Selectivity of antidepressants: from the monoamine hypothesis of depression to the SSRI revolution and beyond". J Clin Psychiatry. 65 Suppl 4: 5–10. PMID 15046536.
^ Lacasse J, Leo J (2005). "Serotonin and depression: a disconnect between the advertisements and the scientific literature". PLoS Med 2 (12): e392. doi:10.1371/journal.pmed.0020392. PMC 1277931. PMID 16268734. Free full text, open-access source
^ "Food and Drug Administration Division of Drug Marketing Advertising and Communications. (2005) Zoloft warning letter" (PDF). FDA. Archived from the original on 25 June 2008. Retrieved 11 July 2008.

External links

Wikimedia Commons has media related to Sertraline.

List of international brand names for sertraline
U.S. National Library of Medicine: Drug Information Portal – Sertraline

UpToDate Contents

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1. 選択的セロトニン再取り込み阻害剤：薬理学、投与方法、および副作用 selective serotonin reuptake inhibitors pharmacology administration and side effects
2. 妊娠中の抗うつ薬のリスク：選択的セロトニン再取り込み阻害剤（SSRI） risks of antidepressants during pregnancy selective serotonin reuptake inhibitors ssris
3. 小児への授乳による抗うつ薬およびベンゾジアゼピン曝露の安全性 safety of infant exposure to antidepressants and benzodiazepines through breastfeeding
4. Psychotherapy for anxiety disorders in children and adolescents
5. 小児および思春期における不安障害の薬物療法 pharmacotherapy for anxiety disorders in children and adolescents

English Journal

Sertraline enhances the activity of antimicrobial agents against pathogens of clinical relevance.

Ayaz M1, Subhan F2, Ahmed J3, Khan AU4, Ullah F1, Ullah I5, Ali G2, Syed NI6, Hussain S7.
Journal of biological research (Thessalonikē, Greece).J Biol Res (Thessalon).2015 Apr 16;22(1):4. doi: 10.1186/s40709-015-0028-1. eCollection 2015.
BACKGROUND: Serotonin reuptake inhibitors were recently reported to possess antimicrobial potentials, potentiate activity of several antibiotics, reverse multidrug resistant phenotypes of bacteria and make them susceptible to previously resistant drugs. We investigated antimicrobial potentials of se
PMID 26029671

Polypyrrole/magnetic nanoparticles composite as an efficient sorbent for dispersive micro-solid-phase extraction of antidepressant drugs from biological fluids.

Asgharinezhad AA1, Karami S1, Ebrahimzadeh H2, Shekari N1, Jalilian N1.
International journal of pharmaceutics.Int J Pharm.2015 Oct 15;494(1):102-12. doi: 10.1016/j.ijpharm.2015.08.001. Epub 2015 Aug 4.
In this study, polypyrrole/magnetic nanoparticles composites in the presence of two different dopants were synthesized with the aid of chemical oxidative polymerization process for dispersive-μ-solid phase extraction (D-μ-SPE). The synthesized magnetic sorbents were characterized by various techni
PMID 26253373

Examining PTSD treatment choice among individuals with subthreshold PTSD.

Bergman HE1, Kline AC2, Feeny NC2, Zoellner LA3.
Behaviour research and therapy.Behav Res Ther.2015 Oct;73:33-41. doi: 10.1016/j.brat.2015.07.010. Epub 2015 Jul 22.
Subthreshold posttraumatic stress disorder (PTSD) is associated with impairment and has a prevalence rate comparable to full PTSD. Yet, little is known regarding treatment preferences among individuals with subthreshold PTSD, even though they seek trauma-related treatment at a similar rate to those
PMID 26246029

Japanese Journal

Comparison of the Anti-tumor Effects of Selective Serotonin Reuptake Inhibitors as Well as Serotonin and Norepinephrine Reuptake Inhibitors in Human Hepatocellular Carcinoma Cells

Kuwahara Jun,Yamada Takaaki,Egashira Nobuaki [他],Ueda Mitsuyo,Zukeyama Nina,Ushio Soichiro,Masuda Satohiro
Biological and Pharmaceutical Bulletin 38(9), 1410-1414, 2015
… The half-maximal inhibitory concentration was lower in the order of: sertraline, paroxetine, duloxetine, fluvoxamine, escitalopram, and milnacipran. … Exposure to sertraline (2 µM) significantly increased caspase-3/7 activity. … These results suggest that, of the agents tested here, sertraline had the highest sensitivity to HepG2 cells, and activation of the caspase pathway is involved in the anti-tumor effects of sertraline in HepG2 cells. …
NAID 130005096993

セルトラリン (特集新規抗うつ薬の特徴と使用法)

伊賀淳一,大森哲郎
精神科 25(5), 474-478, 2014-11
NAID 40020262183

気分障害を伴う概日リズム睡眠障害に対してramelteonが著効した1例

吉原慎佑,吉澤門土,白田朱香,松田美夏,玉城元之,斉藤一朗,坂本一剛,藤村洋太,田村義之,千葉茂
精神神経学雑誌 116(9), 746-751, 2014-03
… 告する.症例は25歳,男性.5年前から情動の不安定さが出現した.また日中の過度の眠気や朝の起床困難が随伴したため,某精神科で気分障害およびナルコレプシーの疑いと診断された.十分量と思われる薬物治療(sertraline,milnacipran,valproate,methylphenidateなど)が数年間行われたが著効せず,当科を受診した.睡眠習慣についての問診票や睡眠日誌から睡眠相の後退が認められ,また,actigraphyやvideo-polysomnographyなどの諸検査の結果,ICSD-2に …
NAID 120005521572

Related Pictures

★リンクテーブル★

リンク元	「セルトラリン」「選択的セロトニン再取り込み阻害薬」「SER」「ZOLOFT」
拡張検索	「sertraline hydrochloride」

「セルトラリン」

Sertraline
Systematic (IUPAC) name
	(1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine
Clinical data
Trade names	Zoloft, Lustral, Daxid, Deprax, Altruline, Besitran, Eleval, Emergen, Gladem, Implicane, Sedoran, Sealdin, Serivo, Lowfin, Stimuloton, Serimel, Seretral, Tresleen, Sertralin Bluefish
AHFS/Drugs.com	monograph
MedlinePlus	a697048
Pregnancy cat.	C (AU) C (US)
Legal status	Prescription Only (S4) (AU) POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	44%
Protein binding	98.5%
Metabolism	Hepatic (N-demethylation mainly by CYP2B6)
Half-life	~23-26 h (66 h [less-active metabolite, norsertraline])
Excretion	Renal
Identifiers
CAS number	79617-96-2
ATC code	N06AB06
PubChem	CID 68617
DrugBank	DB01104
ChemSpider	61881
UNII	QUC7NX6WMB
KEGG	D02360
ChEBI	CHEBI:9123
ChEMBL	CHEMBL809
Chemical data
Formula	C17H17Cl2N
Mol. mass	306.229 g/mol
	SMILES ClC1=CC=C([C@H]2C3=C([C@H](CC2)NC)C=CC=C3)C=C1Cl;
	InChI InChI=1S/C17H17Cl2N/c1-20-17-9-7-12(13-4-2-3-5-14(13)17)11-6-8-15(18)16(19)10-11/h2-6,8,10,12,17,20H,7,9H2,1H3/t12-,17-/m0/s1 ; Key:VGKDLMBJGBXTGI-SJCJKPOMSA-N ;
(what is this?) (verify)

　　[★]

英: sertraline
化: 塩酸セルトラリン sertraline hydrochloride
商: ジェイゾロフト
関: [[]]

抗うつ薬

選択的セロトニン再取り込み阻害剤

適応

うつ病・うつ状態、パニック障害

注意

禁忌

1. 本剤の成分に対し過敏症の既往歴のある患者
2. MAO阻害剤を投与中あるいは投与中止後14日間以内の患者
3. ピモジドを投与中の患者

副作用

承認時までのうつ病・うつ状態患者及びパニック障害患者を対象とした国内臨床試験において、本剤が投与された総症例1478例中881例（59.6％）に2075件の副作用が発現した。主な副作用は、悪心（18.9％）、傾眠（15.2％）、口内乾燥（9.3％）、頭痛（7.8％）、下痢（6.4％）、浮動性めまい（5.0％）等であった。

添付文書

http://www.info.pmda.go.jp/go/pack/1179046F1028_2_02/

「選択的セロトニン再取り込み阻害薬」

　　[★]

英: selective serotonin reuptake inhibitor, SSRI
関: 薬理学、向精神薬

特徴

TCAと違いcaridiotoxicityがない。また、ムスカリン受容体、ヒスタミン受容体、アドレナリン受容体、ドパミン受容体に結合しない。

適応

うつ病・うつ状態、強迫性障害、社会不安障害 (フルボキサミン添付文書より)

副作用

some degree of sexual dysfunction
GI distress

sertraline：diarrhea

paroxetine：comstipation

serotonin syndrome: rare but dangeraous elevation of 5HT： can occur when both an SSRI and a monoamine oxidase inhibitor are administered simultaneously.

hyperthermia, muscle rigidity, myoclonus, and rapid fluctuations in mental status and vital signs.

「SER」

　　[★]

「ZOLOFT」

　　[★] セルトラリン sertraline

「sertraline hydrochloride」

　　[★]

塩酸セルトラリン

関: sertraline

[pmid15547048-1] Obach RS, Cox LM, Tremaine LM (2005). "Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study". Drug Metab. Dispos. 33 (2): 262–70. doi:10.1124/dmd.104.002428. PMID 15547048.

[FDALabel-2] Sertraline FDA Label. http://www.fda.gov/ohrms/dockets/ac/04/briefing/4006b1_06_zoloft-label.pdf

[GG-3] Brunton L, Chabner B, Knollman B. Goodman and Gilman’s The Pharmacological Basis of Therapeutics, Twelfth Edition. McGraw Hill Professional; 2010.

[4] John M. Grohol (2012). "Top 25 Psychiatric Medication Prescriptions for 2011". Psych Central. Retrieved 9 January 2013.

[pmid10529069-5] Flament MF, Lane RM, Zhu R, Ying Z (1999). "Predictors of an acute antidepressant response to fluoxetine and sertraline". Int Clin Psychopharmacol 14 (5): 259–75. doi:10.1097/00004850-199914050-00001. PMID 10529069.

[pmid10945134-6] Hirschfeld RM (2000). "Sertraline in the treatment of anxiety disorders". Depress Anxiety 11 (4): 139–57. doi:10.1002/1520-6394(2000)11:4<139::AID-DA1>3.0.CO;2-C. PMID 10945134.

[pmid15507582-7] Pediatric OCD Treatment Study (POTS) Team (2004). "Cognitive-behavior therapy, sertraline, and their combination for children and adolescents with obsessive-compulsive disorder: the Pediatric OCD Treatment Study (POTS) randomized controlled trial". JAMA 292 (16): 1969–76. doi:10.1001/jama.292.16.1969. PMID 15507582.

[pmid16889458-8] Sousa MB, Isolan LR, Oliveira RR, Manfro GG, Cordioli AV (2006). "A randomized clinical trial of cognitive-behavioral group therapy and sertraline in the treatment of obsessive-compulsive disorder". The Journal of Clinical Psychiatry 67 (7): 1133–9. doi:10.4088/JCP.v67n0717. PMID 16889458.

[pmid14709946-9] The BSPS15 criterion identified 28 (21%) of sertraline-treated patients and 4 (6%) of placebo-treated patients as responders. The 50% reduction in BSPS criterion identified 47 (35%) of sertraline-treated patients and 9 (13%) of placebo-treated patients as responders. Finally, the 50% reduction in MFQ-SP criterion identified 53 (39%) of sertraline-treated patients and 9 (13%) of placebo-treated patients as responders. Van Ameringen M, Oakman J, Mancini C, Pipe B, Chung H (2004). "Predictors of response in generalized social phobia: effect of age of onset". J Clin Psychopharmacol 24 (1): 42–8. doi:10.1097/01.jcp.0000104909.75206.6f. PMID 14709946.

[pmid11343529-10] CGI-Improvement, mean ± SD: Sertraline = 2.3 ± 0.1 Placebo = 2.8 ± 0.1. CGI-Severity, mean ± SD: Change Sertraline = −1.3 ± 0.1; placebo = −1.0 ± 0.1 Davidson JR, Rothbaum BO, van der Kolk BA, Sikes CR, Farfel GM (2001). "Multicenter, double-blind comparison of sertraline and placebo in the treatment of posttraumatic stress disorder". Arch. Gen. Psychiatry 58 (5): 485–92. doi:10.1001/archpsyc.58.5.485. PMID 11343529.

[AHFS-11] "Sertraline hydrochloride". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.

[pmid18199864-12] Turner EH, Matthews AM, Linardatos E, Tell RA, Rosenthal R (2008). "Selective publication of antidepressant trials and its influence on apparent efficacy". N. Engl. J. Med. 358 (3): 252–60. doi:10.1056/NEJMsa065779. PMID 18199864.

[pmid10993128-13] Lépine JP, Goger J, Blashko C, Probst C, Moles MF, Kosolowski J, Scharfetter B, Lane RM (2000). "A double-blind study of the efficacy and safety of sertraline and clomipramine in outpatients with severe major depression". International Clinical Psychopharmacology 15 (5): 263–71. doi:10.1097/00004850-200015050-00003. PMID 10993128.

[Cohen2007-14] Cohen, D (2007). "Should the use of selective serotonin reuptake inhibitors in child and adolescent depression be banned?". Psychotherapy and psychosomatics 76 (1): 5–14. PMID 17170559.

[Banerjee2013-15] Banerjee S, Hellier J, Romeo R, Dewey M, Knapp M, Ballard C, Baldwin R, Bentham P, Fox C, Holmes C, Katona C, Lawton C, Lindesay J, Livingston G, McCrae N, Moniz-Cook E, Murray J, Nurock S, Orrell M, O'Brien J, Poppe M, Thomas A, Walwyn R, Wilson K, Burns A (2007). "Study of the use of antidepressants for depression in dementia: the HTA-SADD trial – a multicentre, randomised, double-blind, placebo-controlled trial of the clinical effectiveness and cost-effectiveness of sertraline and mirtazapine". Health Technol Assess 17 (7): 1–116. PMID 23438937.

[pmid11247097-16] Parker G, Roy K, Wilhelm K, Mitchell P (2001). "Assessing the comparative effectiveness of antidepressant therapies: a prospective clinical practice study". J Clin Psychiatry 62 (2): 117–25. doi:10.4088/JCP.v62n0209. PMID 11247097.

[pmid9597346-17] Anderson IM (1998). "SSRIS versus tricyclic antidepressants in depressed inpatients: a meta-analysis of efficacy and tolerability". Depress Anxiety 7 (S1): 11–7. doi:10.1002/(SICI)1520-6394(1998)7:1+<11::AID-DA4>3.0.CO;2-I. PMID 9597346.

[pmid10362442-18] Hirschfeld RM (1999). "Efficacy of SSRIs and newer antidepressants in severe depression: comparison with TCAs". J Clin Psychiatry 60 (5): 326–35. doi:10.4088/JCP.v60n0511. PMID 10362442.

[pmid9808081-19] Amsterdam JD (1998). "Selective serotonin reuptake inhibitor efficacy in severe and melancholic depression". J. Psychopharmacol. (Oxford) 12 (3 Suppl B): S99–111. doi:10.1177/0269881198012003061. PMID 9808081.

[20] Cipriani, Andrea; Furukawa, Toshiaki A; Salanti, Georgia; Geddes, John R; Higgins, Julian PT; Churchill, Rachel; Watanabe, Norio; Nakagawa, Atsuo et al. (2009). "Comparative efficacy and acceptability of 12 new-generation antidepressants: a multiple-treatments meta-analysis". The Lancet 373 (9665): 746–758. doi:10.1016/S0140-6736(09)60046-5. PMID 19185342. Lay summary – The Washington Post (29 January 2009). |displayauthors= suggested (help)

[pmid17168253-21] Papakostas GI, Fava M (2006). "A metaanalysis of clinical trials comparing moclobemide with selective serotonin reuptake inhibitors for the treatment of major depressive disorder". Canadian Journal of Psychiatry 51 (12): 783–90. PMID 17168253.

[pmid8626364-22] Feiger A, Kiev A, Shrivastava RK, Wisselink PG, Wilcox CS (1996). "Nefazodone versus sertraline in outpatients with major depression: focus on efficacy, tolerability, and effects on sexual function and satisfaction". The Journal of Clinical Psychiatry. 57. Suppl 2: 53–62. PMID 8626364.

[pmid17288677-23] Ventura D, Armstrong EP, Skrepnek GH, Haim Erder M (2007). "Escitalopram versus sertraline in the treatment of major depressive disorder: a randomized clinical trial". Current Medical Research and Opinion 23 (2): 245–50. doi:10.1185/030079906X167273. PMID 17288677.

[pmid9448656-24] Kavoussi RJ, Segraves RT, Hughes AR, Ascher JA, Johnston JA (1997). "Double-blind comparison of bupropion sustained release and sertraline in depressed outpatients". The Journal of Clinical Psychiatry 58 (12): 532–7. doi:10.4088/JCP.v58n1204. PMID 9448656.

[pmid16172440-25] For the review, see:Hansen RA, Gartlehner G, Lohr KN, Gaynes BN, Carey TS (2005). "Efficacy and safety of second-generation antidepressants in the treatment of major depressive disorder". Ann. Intern. Med. 143 (6): 415–26. PMID 16172440.

[pmid16235353-26] Cipriani A, Brambilla P, Furukawa T, Geddes J, Gregis M, Hotopf M, Malvini L, Barbui C (2005). "Fluoxetine versus other types of pharmacotherapy for depression". In Cipriani, Andrea. Cochrane Database of Systematic Reviews (Online) (4): CD004185. doi:10.1002/14651858.CD004185.pub2. PMID 16235353.

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