Sertraline

Last updated

Sertraline
Sertraline.svg
Sertraline-A-3D-balls.png
Clinical data
Pronunciation /ˈsɜːrtrəˌliːn/
Trade names Zoloft, Lustral, Setrona, others [1]
AHFS/Drugs.com Monograph
MedlinePlus a697048
License data
Pregnancy
category
Addiction
liability 		None [3]
Routes of
administration 		By mouth
Drug class Selective serotonin reuptake inhibitor (SSRI)
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances) [4]
  • CA: ℞-only
  • NZ:Prescription only
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 44%[ citation needed ]
Protein binding 98.5%[ citation needed ]
Metabolism Liver (primarily N-demethylation mainly by CYP2B6; also metabolism by CYP2C19, others) [5] [6]
Metabolites • Desmethylsertraline
• Others (e.g., hydroxylated metabolites, glucuronide conjugates) [5]
Elimination half-life • Sertraline: 26 hours (32 hours in females, 22 hours in males; range 13–45 hours) [5] [7] [8] [9]
• Desmethylsertraline: 62–104 hours [5]
Excretion Urine (40–45%) [5]
Feces (40–45%) [5]
Identifiers
  • (1S,4S)-4-(3,4-Dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C17H17Cl2N
Molar mass 306.23 g·mol−1
3D model (JSmol)
  • ClC1=CC=C([C@H]2C3=C([C@H](CC2)NC)C=CC=C3)C=C1Cl
  • 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 Yes check.svgY
  • Key:VGKDLMBJGBXTGI-SJCJKPOMSA-N Yes check.svgY
   (verify)

Sertraline, sold under the brand name Zoloft among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. [10] The effectiveness of sertraline for depression is similar to that of other antidepressants, and the differences are mostly confined to side effects. Sertraline is better tolerated than the older tricyclic antidepressants. Sertraline is effective for panic disorder, social anxiety disorder, generalized anxiety disorder (GAD), and obsessive–compulsive disorder (OCD). Although approved for post-traumatic stress disorder (PTSD), sertraline leads to only modest improvement in this condition. [11] [12] Sertraline also alleviates the symptoms of premenstrual dysphoric disorder (PMDD) and can be used in sub-therapeutic doses or intermittently (luteal phase dosing) for its treatment. [13]

Contents

Sertraline shares the common side effects and contraindications of other SSRIs, with high rates of diarrhea, nausea, insomnia, and sexual dysfunction, but it appears not to lead to much weight gain, and its effects on cognitive performance are mild. Similar to other antidepressants, the use of sertraline for depression may be associated with a mildly elevated rate of suicidal thoughts in people under the age of 25 years old. It should not be used together with monoamine oxidase inhibitors (MAOIs): this combination may cause serotonin syndrome, which can be life-threatening in some cases. Sertraline taken during pregnancy is associated with an increase in congenital heart defects in newborns. [14] [15]

Sertraline was invented and developed by scientists at Pfizer and approved for medical use in the United States in 1991. It is on the World Health Organization's List of Essential Medicines. [16] It is available as a generic medication. [10] In 2016, sertraline was the most commonly prescribed psychotropic medication in the United States. [17] In 2021, it was the eleventh most commonly prescribed medication in the United States, with over 39 million prescriptions. [18] [19]

Medical uses

Sertraline has been approved for major depressive disorder (MDD), obsessive–compulsive disorder (OCD), post-traumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD), panic disorder, and social anxiety disorder (SAD). Sertraline is approved for use in children with OCD. [20]

Depression

In meta-analyses, sertraline displays similar efficacy to other SSRI antidepressants, with an odds ratio for response in clinical depression of between 1.44 and 1.67. [21] [22] However, as with other antidepressants, the nature and clinical significance of this effect remain disputed. [23] [24] A major study of sertraline in a broad primary care population found improvements in general mental health, quality of life, and anxiety. [25] However, it failed to find significant effects on depression in either the mildly or severely depressed, and the clinical relevance and accuracy of the positive effects found have been questioned. [26] [27]

In several double-blind studies, sertraline was consistently more effective than placebo for dysthymia, a more chronic variety of depression, and comparable to imipramine in that respect. Sertraline also improves the functional impairments of dysthymia to a similar degree whether group Cognitive-Behavioural Therapy is undergone or not. [28]

Limited pediatric data also demonstrates reduction in depressive symptoms in the pediatric population though remains a second line therapy after fluoxetine. [29] [30]

Comparison with other antidepressants

In general, sertraline efficacy is similar to that of other antidepressants. [31] For example, a meta-analysis of 12 new-generation antidepressants showed that sertraline and escitalopram are the best in terms of efficacy and acceptability in the acute-phase treatment of adults with depression. [32] Comparative clinical trials demonstrated that sertraline is similar in efficacy against depression to moclobemide, [33] nefazodone, [34] escitalopram, bupropion, [35] citalopram, fluvoxamine, paroxetine, [32] venlafaxine, [36] and mirtazapine. [37] Sertraline may be more efficacious for the treatment of depression in the acute phase (first four weeks) than fluoxetine. [38]

There are differences between sertraline and some other antidepressants in their efficacy in the treatment of different subtypes of depression and in their adverse effects. For severe depression, sertraline is as good as clomipramine but is better tolerated. [36] Sertraline appears to work better in melancholic depression than fluoxetine, paroxetine, and mianserin and is similar to the tricyclic antidepressants such as amitriptyline and clomipramine. [31] In the treatment of depression accompanied by OCD, sertraline performs significantly better than desipramine on the measures of both OCD and depression. [28] [39] Sertraline is equivalent to imipramine for the treatment of depression with co-morbid panic disorder, but it is better tolerated. [40] Compared with amitriptyline, sertraline offered a greater overall improvement in quality of life of depressed patients. [31]

Depression in elderly

Sertraline used for the treatment of depression in elderly (older than 60) patients is superior to placebo and comparable to another SSRI fluoxetine, and tricyclic antidepressants (TCAs) amitriptyline, nortriptyline and imipramine. Sertraline has much lower rates of adverse effects than these TCAs, with the exception of nausea, which occurs more frequently with sertraline. In addition, sertraline appears to be more effective than fluoxetine or nortriptyline in the older-than-70 subgroup. [41] Accordingly, a meta-analysis of antidepressants in older adults found that sertraline, paroxetine and duloxetine were better than placebo. [42] On the other hand, in a 2003 trial the effect size was modest, and there was no improvement in quality of life as compared to placebo. [43] With depression in dementia, there is no benefit of sertraline treatment compared to either placebo or mirtazapine. [44]

Obsessive–compulsive disorder

Sertraline is effective for the treatment of OCD in adults, [20] adolescents and children. [45] [46] [47] It was better tolerated and, based on intention-to-treat analysis, performed better than the gold standard of OCD treatment clomipramine. [48] Continuing sertraline treatment helps prevent relapses of OCD with long-term data supporting its use for up to 24 months. [49] The sertraline dosages necessary for the effective treatment of OCD are higher than the usual dosage for depression. [50] 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. [51]

Cognitive behavioral therapy alone is not more effective than sertraline in adolescents and children; however, a combination of these treatments is effective. [47]

Panic disorder

Sertraline is superior to placebo for the treatment of panic disorder. [20] 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. [52] [53] Sertraline is equally effective for men and women, [53] and for patients with or without agoraphobia. [54] Previous unsuccessful treatment with benzodiazepines does not diminish its efficacy. [55] However, the response rate was lower for the patients with more severe panic. [54] Starting treatment simultaneously with sertraline and clonazepam, with subsequent gradual discontinuation of clonazepam, may accelerate the response. [56]

Double-blind comparative studies found sertraline to have the same effect on panic disorder as paroxetine or imipramine. [57] While imprecise, comparison of the results of trials of sertraline with separate trials of other anti-panic agents (clomipramine, imipramine, clonazepam, alprazolam, and fluvoxamine) indicates approximate equivalence of these medications. [52]

Other anxiety disorders

Sertraline has been successfully used for the treatment of social anxiety disorder. [58] [59] All three major domains of the disorder (fear, avoidance, and physiological symptoms) respond to sertraline. [28] Maintenance treatment, after the response is achieved, prevents the return of the symptoms. [60] The improvement is greater among the patients with later, adult onset of the disorder. [61] In a comparison trial, sertraline was superior to exposure therapy, but patients treated with the psychological intervention continued to improve during a year-long follow-up, while those treated with sertraline deteriorated after treatment termination. [62] The combination of sertraline and cognitive behavioral therapy appears to be more effective in children and young people than either treatment alone. [63]

Sertraline has not been approved for the treatment of generalized anxiety disorder; however, several guidelines recommend it as a first-line medication referring to good quality controlled clinical trials. [64] [40] [49]

Premenstrual dysphoric disorder

Sertraline is effective in alleviating the symptoms of premenstrual dysphoric disorder (PMDD), a severe form of premenstrual syndrome. [65] 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. [66] [67] Taking sertraline only during the luteal phase, that is, the 12–14 days before menses, was shown to work as well as continuous treatment. [65] Continuous treatment with sub-therapeutic doses of sertraline (25 mg vs. usual 50–100 mg) is also effective. [68]

Other indications

Sertraline is approved for the treatment of post-traumatic stress disorder (PTSD). [20] The National Institute for Clinical Excellence recommends it for patients who prefer drug treatment to a psychological one. [69] Other guidelines also suggest sertraline as a first-line option for pharmacological therapy. [70] [40] When necessary, long-term pharmacotherapy can be beneficial. [70] There are both negative and positive clinical trial results for sertraline, which may be explained by the types of psychological traumas, symptoms, and comorbidities included in the various studies. [49] Positive results were obtained in trials that included predominantly women (75%) with a majority (60%) having physical or sexual assault as the traumatic event. [70] Somewhat contrary to the above suggestions, a meta-analysis of sertraline clinical trials for PTSD found it to be statistically superior to placebo in reduction of PTSD symptoms but the effect size was small. [11] Another meta-analysis relegated sertraline to the second line, proposing trauma focused psychotherapy as a first-line intervention. The authors noted that Pfizer had declined to submit the results of a negative trial for the inclusion into the meta-analysis making the results unreliable. [12]

Sertraline when taken daily can be useful for the treatment of premature ejaculation. [71] A disadvantage of sertraline is that it requires continuous daily treatment to delay ejaculation significantly. [72]

A 2019 systematic review suggested that sertraline may be a good way to control anger, irritability and hostility in depressed patients and patients with other comorbidities. [73]

Contraindications

Sertraline is contraindicated in individuals taking monoamine oxidase inhibitors or the antipsychotic pimozide. Sertraline concentrate contains alcohol and is therefore contraindicated with disulfiram. 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. [20]

Side effects

Nausea, ejaculation failure, insomnia, diarrhea, dry mouth, somnolence, dizziness, tremor, headache, excessive sweating, fatigue, restless legs syndrome and decreased libido are the common adverse effects associated with sertraline with the greatest difference from placebo. Those that most often resulted in interruption of the treatment are nausea, diarrhea and insomnia. [20] The incidence of diarrhea is higher with sertraline – especially when prescribed at higher doses – in comparison with other SSRIs. [74]

Over more than six months of sertraline therapy for depression, people showed no significant weight increase. [75] A 30-month-long treatment with sertraline for OCD also resulted in no significant weight gain. [76] Although the difference did not reach statistical significance, the average weight gain was lower for fluoxetine (1%) but higher for citalopram, fluvoxamine and paroxetine (2.5%). Of the sertraline group, 4.5% 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. [76]

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. [77] [78] 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. [79] 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. [80] The unique effect of sertraline on dopaminergic neurotransmission may be related to these effects on cognition and vigilance. [81] [82]

Sertraline has a low level of exposure of an infant through the breast milk and is recommended as the preferred option for the antidepressant therapy of breast-feeding mothers. [83] [84] There is 29–42% increase in congenital heart defects among children whose mothers were prescribed sertraline during pregnancy, [14] [15] with sertraline use in the first trimester associated with 2.7-fold increase in septal heart defects. [14]

Abrupt interruption of sertraline treatment may result in withdrawal or discontinuation syndrome. Dizziness, insomnia, anxiety, agitation, and irritability are its common symptoms. [85] It typically occurs within a few days from drug discontinuation and lasts a few weeks. [86] The withdrawal symptoms for sertraline are less severe and frequent than for paroxetine, and more frequent than for fluoxetine. [85] [86] In most cases symptoms are mild, short-lived, and resolve without treatment. More severe cases are often successfully treated by temporary reintroduction of the drug with a slower tapering off rate. [87]

Sertraline and SSRI antidepressants in general may be associated with bruxism and other movement disorders. [88] [89] Sertraline appears to be associated with microscopic colitis, a rare condition of unknown etiology. [90]

Sexual

Like other SSRIs, sertraline is associated with sexual side effects, including sexual arousal disorder, erectile dysfunction and difficulty achieving orgasm. While nefazodone and bupropion do not have negative effects on sexual functioning, 67% of men on sertraline experienced ejaculation difficulties versus 18% before the treatment. [91] Sexual arousal disorder, defined as "inadequate lubrication and swelling for women and erectile difficulties for men", occurred in 12% of people 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. [92] Some people continue experiencing sexual side effects after they stop taking SSRIs. [93]

Suicide

The US Food and Drug Administration (FDA) requires all antidepressants, including sertraline, to carry a boxed warning stating that antidepressants increase the risk of suicide in persons younger than 25 years. [94] [95] [96] This warning is based on statistical analyses conducted by two independent groups of FDA experts that found a 100% increase of suicidal thoughts and behavior in children and adolescents, and a 50% increase in the 18–24 age group. [97] [98] [99]

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% [99] or 50% [98] 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". [98] The more complete data submitted later by the sertraline manufacturer Pfizer indicated increased suicidal behavior. [100] 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. [101] [102]

Overdose

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. [103] As with most other SSRIs its toxicity in overdose is considered relatively low. [104] [105]

Interactions

As with other SSRIs, sertraline may increase the risk of bleeding with NSAIDs (ibuprofen, naproxen, mefenamic acid), antiplatelet drugs, anticoagulants, omega-3 fatty acids, vitamin E, and garlic supplements due to sertraline's inhibitory effects on platelet aggregation via blocking serotonin transporters on platelets. [106] Sertraline, in particular, may potentially diminish the efficacy of levothyroxine. [107]

Sertraline is a moderate inhibitor of CYP2D6 and CYP2B6 in vitro . [8] 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. [108] [109] [110] 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. [9] [111] 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. [112]

Sertraline had a slight inhibitory effect on the metabolism of diazepam, tolbutamide and warfarin, which are CYP2C9 or CYP2C19 substrates; the clinical relevance of this effect was unclear. [9] 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. [9] [20] [113] [8]

Sertraline had no effect on the actions of digoxin and atenolol, which are not metabolized in the liver. [5] Case reports suggest that taking sertraline with phenytoin or zolpidem may induce sertraline metabolism and decrease its efficacy, [114] [115] and that taking sertraline with lamotrigine may increase the blood level of lamotrigine, possibly by inhibition of glucuronidation. [116]

CYP2C19 inhibitor esomeprazole increased sertraline concentrations in blood plasma by approximately 40%. [117]

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. [9]

Pharmacology

Pharmacodynamics

Molecular targets of sertraline [118]
SiteKi (nM)SpeciesReferences
SERT Tooltip Serotonin transporter0.15–3.3Human [119] [120] [121]
NET Tooltip Norepinephrine transporter420–925Human [119] [120] [121]
DAT Tooltip Dopamine transporter22–315Human [119] [120] [121]
5-HT1A >35,000Human [122]
5-HT2A 2,207Rat [121]
5-HT2C 2,298Pig [121]
α1A 1900Human [123]
α1B 3,500Human [123]
α1D 2,500Human [123]
α2 477–4,100Human [120] [122]
D2 10,700Human [122]
H1 24,000Human [122]
mACh Tooltip Muscarinic acetylcholine receptors427–2,100Human [121] [122] [124]
σ1 32–57Rat [125] [126]
σ2 5,297Rat [126]
Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to or inhibits the site.

Sertraline is a selective serotonin reuptake inhibitor (SSRI). By binding serotonin transporter (SERT) it inhibits neuronal reuptake of serotonin and potentiates serotonergic activity in the central nervous system. [20] Over time, this leads to a downregulation of pre-synaptic 5-HT1A receptors, which is associated with an improvement in passive stress tolerance, and delayed downstream increase in expression of brain-derived neurotrophic factor (BDNF), which may contribute to a reduction in negative affective biases. [127] [128] It does not significantly affect norepinephrine transporter (NET), serotonin, dopamine, adrenergic, histamine, acetylcholine, GABA or benzodiazepine receptors. [20]

Sertraline also shows relatively high activity as an inhibitor of the dopamine transporter (DAT) [119] [129] [130] and antagonist of the sigma σ1 receptor (but not the σ2 receptor). [125] [126] [131] However, sertraline affinity for its main target (SERT) is much greater than its affinity for σ1 receptor and DAT. [118] [119] [126] [125] Although there could be a role for the σ1 receptor in the pharmacology of sertraline, the significance of this receptor in its actions is unclear. [31] Similarly, the clinical relevance of sertraline's blockade of the dopamine transporter is uncertain. [119]

Pharmacokinetics

Desmethylsertraline, the major metabolite of sertaline Desmethylsertraline skeletal.svg
Desmethylsertraline, the major metabolite of sertaline

Absorption

Following a single oral dose of sertraline, mean peak blood levels of sertraline occur between 4.5 and 8.4 hours. [5] Bioavailability is likely linear and dose-proportional over a dose range of 150 to 200 mg. [5] Concomitant intake of sertraline with food slightly increases sertraline peak levels and total exposure. [5] There is an approximate 2-fold accumulation of sertraline with continuous administration and steady-state levels are reached within one week. [5]

Distribution

Sertraline is highly plasma protein bound (98.5%) across a concentration range of 20 to 500 ng/mL. [5] Despite the high plasma protein binding, sertraline and its metabolite desmethylsertraline at respective tested concentrations of 300 ng/mL and 200 ng/mL were found not to interfere with the plasma protein binding of warfarin and propranolol, two other highly plasma protein-bound drugs. [5]

Metabolism

Sertraline is subject to extensive first-pass metabolism, as indicated by a small study of radiolabeled sertraline in which less than 5% of plasma radioactivity was unchanged sertraline in two males. [5] The principal metabolic pathway for sertraline is N-demethylation into desmethylsertraline (N-desmethylsertraline) mainly by CYP2B6. [5] [6] Reduction, hydroxylation, and glucuronide conjugation of both sertraline and desmethylsertraline also occur. [5] Desmethylsertraline, while pharmacologically active, is substantially (50-fold) weaker than sertraline as a serotonin reuptake inhibitor and its influence on the clinical effects of sertraline is thought to be negligible. [5] [120] [132] Based on in vitro studies, sertraline is metabolized by multiple cytochrome 450 isoforms; [6] [133] however, it appears that in the human body CYP2C19 plays the most important role, followed by CYP2B6. [134] In addition to the cytochrome P450 system, sertraline can be oxidatively deaminated in vitro by monoamine oxidases; [5] however, this metabolic pathway has never been studied in vivo . [6]

Elimination

The elimination half-life of sertraline is on average 26 hours, with a range of 13 to 45 hours. [5] [9] The half-life of sertraline is longer in women (32 hours) than in men (22 hours), which leads to 1.5-fold higher exposure to sertraline in women compared to men. [9] The elimination half-life of desmethylsertraline is 62 to 104 hours. [5]

In a small study of two males, sertraline was excreted to similar degrees in urine and feces (40 to 45% each within 9 days). [5] Unchanged sertraline was not detectable in urine, whereas 12 to 14% unchanged sertraline was present in feces. [5]

Pharmacogenomics

CYP2C19 and CYP2B6 are thought to be the key cytochrome P450 enzymes involved in the metabolism of sertraline. [134] Relative to CYP2C19 normal (extensive) metabolizers, poor metabolizers have 2.7-fold higher levels of sertraline [135] and intermediate metabolizers have 1.4-fold higher levels. [136] In contrast, CYP2B6 poor metabolizers have 1.6-fold higher levels of sertraline and intermediate metabolizers have 1.2-fold higher levels. [134]

History

Skeletal formulae of thiothixene, lometraline and tametraline, from which sertraline was derived. Commonalities to the structure of sertraline are highlighted in red. Sertraline precursors.svg
Skeletal formulae of thiothixene, lometraline and tametraline, from which sertraline was derived. Commonalities to the structure of sertraline are highlighted in red.

The history of sertraline dates back to the early 1970s, when Pfizer chemist Reinhard Sarges invented a novel series of psychoactive compounds, including lometraline, based on the structures of the neuroleptics thiothixene and pinoxepin. [137] [138] 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. [137] [139] [140]

Sertraline was approved by the US 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. [141] The FDA committee achieved a consensus that sertraline was safe and effective for the treatment of major depression. During the discussion, Paul Leber, the director of the FDA Division of Neuropharmacological Drug Products, noted that granting approval was a "tough decision", since the treatment effect on outpatients with depression had been "modest to minimal". Other experts emphasized that the drug's effect on inpatients had not differed from placebo and criticized poor design of the clinical trials by Pfizer. [142] For example, 40% of participants dropped out of the trials, significantly decreasing their validity. [143]

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 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. [144] [145] However, sertraline can still be used in the UK for the treatment of OCD in children and adolescents. [146] In 2005, the FDA added a boxed 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. [147]

Society and culture

Generic availability

The US patent for Zoloft expired in 2006, [148] and sertraline is available in generic form and is marketed under many brand names worldwide. [1]

In May 2020, the FDA placed Zoloft on the list of drugs currently facing a shortage. [149]

Interest during COVID-19 pandemic

Sertraline has been the most sought-after antidepressant worldwide before, during, and after the COVID-19 pandemic, according to Google Trends data. The pandemic has led to an increase in searches for antidepressants, with sertraline, fluoxetine, duloxetine, and venlafaxine showing the highest search volumes, whereas searches of citalopram decreased during the pandemic. [150]

Other uses

Sertraline may be useful to treat murine Zaire ebolavirus (murine EBOV). [151] The World Health Organization (WHO) considers this a promising area of research. [151]

Lass-Flörl et al., 2003 finds it significantly inhibits phospholipase B in the fungal genus Candida , reducing virulence. [152]

Sertraline is also a very effective leishmanicide. [153] Specifically, Palit & Ali 2008 find that sertraline kills almost all promastigotes of Leishmania donovani . [153]

Sertraline is strongly antibacterial against some species. [153] It is also known to act as a photosensitizer of bacterial surfaces. [154] In combination with antibacterials its photosensitization effect reverses antibacterial resistance. [154] As such sertraline shows promise for food preservation. [154]

Lass-Flörl et al., 2003 finds this compound acts as a fungicide against Candida parapsilosis . [155] Its anti-Cp effect is indeed due to its serotonergic activity and not its other effects. [155]

Sertraline is a promising trypanocide. [156] It acts at several different life stages and against several strains. [156] Sertraline's trypanocidal mechanism of action is by way of interference with bioenergetics. [156]

See also

Related Research Articles

<span class="mw-page-title-main">Antidepressant</span> Class of medication used to treat depression and other conditions

Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction.

An anxiolytic is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms.

<span class="mw-page-title-main">Tricyclic antidepressant</span> Class of medications

Tricyclic antidepressants (TCAs) are a class of medications that are used primarily as antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade. They are named after their chemical structure, which contains three rings of atoms. Tetracyclic antidepressants (TeCAs), which contain four rings of atoms, are a closely related group of antidepressant compounds.

A psychiatric or psychotropic medication is a psychoactive drug taken to exert an effect on the chemical makeup of the brain and nervous system. Thus, these medications are used to treat mental illnesses. These medications are typically made of synthetic chemical compounds and are usually prescribed in psychiatric settings, potentially involuntarily during commitment. Since the mid-20th century, such medications have been leading treatments for a broad range of mental disorders and have decreased the need for long-term hospitalization, thereby lowering the cost of mental health care. The recidivism or rehospitalization of the mentally ill is at a high rate in many countries, and the reasons for the relapses are under research.

<span class="mw-page-title-main">Paroxetine</span> SSRI antidepressant medication

Paroxetine, sold under the brand names Paxil and Seroxat among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive-compulsive disorder, panic disorder, social anxiety disorder, post-traumatic stress disorder, generalized anxiety disorder, and premenstrual dysphoric disorder. It has also been used in the treatment of premature ejaculation and hot flashes due to menopause. It is taken orally.

<span class="mw-page-title-main">Citalopram</span> SSRI antidepressant

Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia. The antidepressant effects may take one to four weeks to occur. It is typically taken orally. In some European countries, it is sometimes given intravenously to initiate treatment, before switching to the oral route of administration for continuation of treatment. It has also been used intravenously in other parts of the world in some other circumstances.

<span class="mw-page-title-main">Fluvoxamine</span> SSRI antidepressant drug

Fluvoxamine, commonly sold under the brand names Luvox and Faverin, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is primarily used to treat major depressive disorder and obsessive–compulsive disorder (OCD), but is also used to treat anxiety disorders such as panic disorder, social anxiety disorder, and post-traumatic stress disorder.

<span class="mw-page-title-main">Venlafaxine</span> Antidepressant medication

Venlafaxine, sold under the brand name Effexor among others, is an antidepressant medication of the serotonin–norepinephrine reuptake inhibitor (SNRI) class. It is used to treat major depressive disorder, generalized anxiety disorder, panic disorder, and social anxiety disorder. Studies have shown that venlafaxine improves post-traumatic stress disorder (PTSD). It may also be used for chronic pain. It is taken by mouth. It is also available as the salt venlafaxine besylate in an extended-release formulation.

<span class="mw-page-title-main">Serotonin–norepinephrine reuptake inhibitor</span> Class of antidepressant medication

Serotonin–norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant medications used to treat major depressive disorder (MDD), anxiety disorders, social phobia, chronic neuropathic pain, fibromyalgia syndrome (FMS), and menopausal symptoms. Off-label uses include treatments for attention-deficit hyperactivity disorder (ADHD), obsessive–compulsive disorder (OCD), and migraine prevention. SNRIs are monoamine reuptake inhibitors; specifically, they inhibit the reuptake of serotonin and norepinephrine. These neurotransmitters are thought to play an important role in mood regulation. SNRIs can be contrasted with the selective serotonin reuptake inhibitors (SSRIs) and norepinephrine reuptake inhibitors (NRIs), which act upon single neurotransmitters.

<span class="mw-page-title-main">Azapirone</span> Drug class of psycotropic drugs

Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs).

<span class="mw-page-title-main">Reboxetine</span> NRI antidepressant drug

Reboxetine, sold under the brand name Edronax among others, is a drug of the norepinephrine reuptake inhibitor (NRI) class, marketed as an antidepressant by Pfizer for use in the treatment of major depression, although it has also been used off-label for panic disorder and attention deficit hyperactivity disorder (ADHD). It is approved for use in many countries worldwide, but has not been approved for use in the United States. Although its effectiveness as an antidepressant has been challenged in multiple published reports, its popularity has continued to increase.

<span class="mw-page-title-main">Clomipramine</span> Antidepressant

Clomipramine, sold under the brand name Anafranil among others, is a tricyclic antidepressant (TCA). It is used in the treatment of various conditions, most-notably obsessive–compulsive disorder but also many other disorders, including panic disorder, major depressive disorder, trichotilomania, body dysmorphic disorder and chronic pain. It has also been notably used to treat premature ejaculation and the cataplexy associated with narcolepsy.

<span class="mw-page-title-main">Olanzapine/fluoxetine</span> Antidepressant medication

Olanzapine/fluoxetine is a fixed-dose combination medication containing olanzapine (Zyprexa), an atypical antipsychotic, and fluoxetine (Prozac), a selective serotonin reuptake inhibitor (SSRI). Olanzapine/fluoxetine is primarily used to treat the depressive episodes of bipolar I disorder as well as treatment-resistant depression.

<span class="mw-page-title-main">Fluoxetine</span> SSRI antidepressant

Fluoxetine, sold under the brand name Prozac, among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder (OCD), anxiety, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. It is also approved for treatment of major depressive disorder in adolescents and children 8 years of age and over. It has also been used to treat premature ejaculation. Fluoxetine is taken by mouth.

<span class="mw-page-title-main">Serotonin reuptake inhibitor</span> Class of drug

A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin by blocking the action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in serotonergic neurotransmission. It is a type of monoamine reuptake inhibitor (MRI); other types of MRIs include dopamine reuptake inhibitors and norepinephrine reuptake inhibitors.

The number of new psychiatric drugs, and especially antidepressants on the market in Japan, is significantly less than Western countries.

<span class="mw-page-title-main">Vortioxetine</span> Serotonin modulator antidepressant

Vortioxetine, sold under the brand names Trintellix and Brintellix among others, is a medication used to treat major depressive disorder. Its effectiveness is viewed as similar to that of other antidepressants. It is taken by mouth.

<span class="mw-page-title-main">Selective serotonin reuptake inhibitor</span> Class of antidepressant medication

Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions.

The pharmacology of antidepressants is not entirely clear. The earliest and probably most widely accepted scientific theory of antidepressant action is the monoamine hypothesis, which states that depression is due to an imbalance of the monoamine neurotransmitters. It was originally proposed based on the observation that certain hydrazine anti-tuberculosis agents produce antidepressant effects, which was later linked to their inhibitory effects on monoamine oxidase, the enzyme that catalyses the breakdown of the monoamine neurotransmitters. All currently marketed antidepressants have the monoamine hypothesis as their theoretical basis, with the possible exception of agomelatine which acts on a dual melatonergic-serotonergic pathway. Despite the success of the monoamine hypothesis it has a number of limitations: for one, all monoaminergic antidepressants have a delayed onset of action of at least a week; and secondly, there are a sizeable portion (>40%) of depressed patients that do not adequately respond to monoaminergic antidepressants. Further evidence to the contrary of the monoamine hypothesis are the recent findings that a single intravenous infusion with ketamine, an antagonist of the NMDA receptor — a type of glutamate receptor — produces rapid, robust and sustained antidepressant effects. Monoamine precursor depletion also fails to alter mood. To overcome these flaws with the monoamine hypothesis a number of alternative hypotheses have been proposed, including the glutamate, neurogenic, epigenetic, cortisol hypersecretion and inflammatory hypotheses. Another hypothesis that has been proposed which would explain the delay is the hypothesis that monoamines don't directly influence mood, but influence emotional perception biases.

Selective serotonin reuptake inhibitors, or serotonin-specific re-uptake inhibitor (SSRIs), are a class of chemical compounds that have application as antidepressants and in the treatment of depression and other psychiatric disorders. SSRIs are therapeutically useful in the treatment of panic disorder (PD), posttraumatic stress disorder (PTSD), social anxiety disorder, obsessive-compulsive disorder (OCD), premenstrual dysphoric disorder (PMDD), and anorexia. There is also clinical evidence of the value of SSRIs in the treatment of the symptoms of schizophrenia and their ability to prevent cardiovascular diseases.

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