Does Zoloft cause weight gain. How does it compare to other antidepressants. What are the long-term effects of sertraline on body weight. Can Zoloft lead to weight loss in some patients. How can patients manage weight changes while taking sertraline.

Understanding Zoloft’s Impact on Body Weight

Zoloft (sertraline) is a widely prescribed antidepressant belonging to the selective serotonin reuptake inhibitor (SSRI) class. While it’s highly effective in treating various mental health conditions, many patients express concerns about potential weight changes. Let’s delve into the relationship between Zoloft and body weight.

Does Zoloft Cause Weight Gain?

Research indicates that Zoloft may indeed lead to modest weight gain in some patients, particularly during long-term use. Studies have shown:

• Weight gain ranging from 1% to 1.6% of initial body weight over 6 months to 1 year
• For a 150 lb (68 kg) person, this translates to approximately 1.5 to 2.4 lbs (0.7 to 1.1 kg)
• Short-term treatment in adults typically doesn’t result in substantial weight gain

It’s important to note that weight changes can vary significantly between individuals. Some patients may experience more pronounced weight gain, while others may not notice any change at all.

Zoloft and Weight Loss in Children

Interestingly, the effects of Zoloft on weight can differ in pediatric populations. In children:

• Weight loss has been reported, possibly due to side effects like nausea or loss of appetite
• In a study of 281 children treated with Zoloft, at least 2% reported decreased weight
• The rate of weight loss was twice that of children taking a placebo

This highlights the importance of monitoring weight changes in children prescribed Zoloft, as nutritional status can impact growth and development.

Comparing Zoloft’s Weight Effects to Other SSRIs

When considering antidepressant options, it’s helpful to understand how Zoloft’s weight-related side effects compare to other SSRIs. Generally, the ranking of SSRIs in terms of weight gain potential is as follows:

1. Lowest: Fluoxetine (Prozac)
2. Slightly higher: Sertraline (Zoloft), Citalopram (Celexa), Escitalopram (Lexapro), Fluvoxamine (Luvox)
3. Highest: Paroxetine (Paxil)

Key Studies on SSRI-Related Weight Changes

Several studies have provided insights into the comparative weight effects of different SSRIs:

• A 26 to 32-week double-blind study with 284 patients found:
  • Paroxetine: Significant weight gain
  • Sertraline: Modest but nonsignificant weight gain
  • Fluoxetine: Nonsignificant weight loss
• A 2.5-year open-label study of 138 patients with OCD reported:
  • Significant weight gain in all groups except fluoxetine
  • Fluoxetine and sertraline had the lowest weight gain among SSRIs
  • Zoloft and Prozac had the lowest percentage of patients with a weight gain of 7% or more (4.5% for Zoloft and 8.7% for Prozac)

These findings suggest that while Zoloft may cause some weight gain, it’s generally less pronounced compared to other antidepressants, particularly paroxetine.

Weight Gain Patterns with Long-Term Antidepressant Use

Understanding the long-term effects of antidepressants on body weight is crucial for patients and healthcare providers. A large cohort study in the United Kingdom provided valuable insights into this topic.

UK Cohort Study Findings

The study, which included 136,762 men and 157,957 women, examined electronic health records to evaluate the association between antidepressant prescribing and weight gain over a 10-year period. Key findings include:

• Patients prescribed antidepressants had an increased risk of at least a 5% gain in body weight compared to those never prescribed antidepressants
• Weight gain substantially increased in the second and third years of treatment
• During the second year of treatment, the risk of gaining at least 5% of body weight was 46% higher in antidepressant users

These results highlight the importance of monitoring weight changes throughout the course of antidepressant treatment, particularly beyond the first year.

Factors Influencing Weight Changes with Antidepressants

The relationship between antidepressants and weight changes is complex and multifaceted. Several factors can contribute to weight fluctuations during treatment:

Medication-Specific Effects

• Different antidepressants can have varying effects on appetite and metabolism
• Some medications may increase cravings for carbohydrates or alter taste perceptions
• Certain antidepressants can affect hormones that regulate hunger and satiety

Individual Patient Factors

• Genetic predisposition to weight gain or loss
• Pre-existing metabolic conditions
• Age and gender
• Lifestyle habits, including diet and exercise

Depression-Related Factors

• Changes in appetite and eating habits associated with depression
• Reduced physical activity during depressive episodes
• Improvement in mood leading to increased appetite or social eating

Understanding these factors can help healthcare providers and patients develop strategies to manage weight changes effectively during antidepressant treatment.

Strategies for Managing Weight While Taking Zoloft

For patients concerned about potential weight gain while taking Zoloft, there are several strategies that can help maintain a healthy weight:

Dietary Approaches

• Focus on a balanced diet rich in fruits, vegetables, lean proteins, and whole grains
• Practice portion control and mindful eating
• Keep a food diary to track eating habits and identify potential triggers for overeating
• Consider working with a registered dietitian for personalized nutrition advice

Exercise and Physical Activity

• Aim for at least 150 minutes of moderate-intensity aerobic activity per week
• Incorporate strength training exercises to build muscle mass and boost metabolism
• Find enjoyable physical activities to increase adherence to an exercise routine
• Consult with a healthcare provider before starting any new exercise program

Regular Monitoring and Communication

• Keep track of weight changes and discuss them with your healthcare provider
• Report any significant weight fluctuations or changes in appetite
• Consider regular check-ins to assess the overall effectiveness of the medication and address any concerns

By implementing these strategies, patients can work to maintain a healthy weight while benefiting from the therapeutic effects of Zoloft.

Alternative Antidepressants and Their Weight Effects

For patients who are particularly concerned about weight gain or have experienced significant weight changes with Zoloft, it may be worth exploring alternative antidepressant options. Different classes of antidepressants can have varying effects on body weight:

Bupropion (Wellbutrin)

Bupropion is an atypical antidepressant that has been associated with weight loss in some patients:

• Studies show that 14% to 19% of patients taking bupropion lost at least 2.2 kg (5 lb)
• This is compared to only 6% of patients on a placebo
• Bupropion may be a suitable option for patients concerned about weight gain

Mirtazapine (Remeron)

In contrast to bupropion, mirtazapine, a tetracyclic antidepressant, is known to be associated with significant weight gain:

• Appetite increase was reported in 17% of patients treated with Remeron
• 7.5% of patients had a weight gain of at least 7% compared to the start of the study

Tricyclic Antidepressants (TCAs)

Older antidepressants like TCAs (e.g., amitriptyline, doxepin) are generally associated with more weight gain than SSRIs:

• TCAs are less frequently prescribed today for depression due to their side effect profile
• In studies, TCAs like clomipramine were associated with greater weight gain compared to SSRIs

It’s important to note that the choice of antidepressant should be based on overall efficacy, tolerability, and individual patient factors, not solely on potential weight effects. Always consult with a healthcare provider before making any changes to antidepressant medication.

The Importance of Balanced Treatment Decisions

While weight changes are a valid concern for many patients taking antidepressants, it’s crucial to consider the overall benefits of treatment when making decisions about medication:

Weighing Risks and Benefits

• The potential for modest weight gain should be balanced against the significant improvements in mood, functioning, and quality of life that effective antidepressant treatment can provide
• Untreated depression can also lead to weight changes and negatively impact overall health
• For many patients, the benefits of treatment outweigh the risk of modest weight gain

Individualized Treatment Approaches

Healthcare providers can work with patients to develop individualized treatment plans that address both mental health needs and concerns about weight:

• Exploring different medication options if weight gain is a significant concern
• Implementing lifestyle interventions alongside medication treatment
• Considering combination therapies or adjunct treatments to optimize outcomes
• Regular monitoring and adjustment of treatment plans as needed

By taking a comprehensive and personalized approach to treatment, patients and healthcare providers can work together to achieve optimal mental health outcomes while minimizing unwanted side effects like weight gain.

Future Directions in Antidepressant Research and Weight Management

As our understanding of the relationship between antidepressants and weight changes continues to evolve, several areas of research hold promise for improved treatment options and management strategies:

Pharmacogenomics and Personalized Medicine

Advances in genetic testing may help identify patients who are more likely to experience weight gain with specific antidepressants:

• Tailoring medication choices based on genetic profiles
• Predicting individual responses to different antidepressants
• Developing more targeted interventions to prevent or manage weight gain

Novel Antidepressant Formulations

Researchers are exploring new antidepressant formulations that may have more favorable weight profiles:

• Combination medications that incorporate weight-neutral or weight-loss promoting agents
• Novel drug delivery systems that may minimize systemic side effects
• Repurposing existing medications with known weight-neutral profiles for antidepressant use

Integrative Approaches to Depression Treatment

Holistic treatment strategies that address both mental health and weight management are gaining attention:

• Combining pharmacological treatments with evidence-based psychotherapies
• Incorporating lifestyle interventions, including nutrition and exercise programs, as core components of depression treatment
• Exploring the potential of alternative and complementary therapies in managing both depression and weight

As research in these areas progresses, patients and healthcare providers can look forward to more effective and personalized approaches to managing depression while minimizing the risk of unwanted weight changes.

Does Zoloft (sertraline) cause weight gain?

Medically reviewed by Leigh Ann Anderson, PharmD. Last updated on Jan 26, 2022.

Zoloft (sertraline) may lead to a small weight gain ranging from 1% to 1.6% of initial body weight when used over 6 months to 1 year. For example, in a 150 lb (68 kg) person, this would equal an added 1.5 to 2.4 lbs (0.7 to 1.1 kg) of weight. Shorter-term treatment in adults usually does not lead to substantial weight gain, but most patients need to take Zoloft for an extended period of time.

In children, weight loss has been reported with Zoloft possibly due to side effects like nausea or loss of appetite. In 281 children treated with Zoloft, at least 2% reported decreased weight, at a rate that was twice that of placebo (an inactive pill).

Zoloft is a selective serotonin reuptake inhibitor (SSRI) approved to treat

• Depression
• Obsessive-compulsive disorder
• Panic disorder
• Post-traumatic stress disorder
• Social anxiety disorder
• Premenstrual dysphoric disorder

How does weight gain with Zoloft compare to other SSRIs?

Of the SSRIs, Zoloft (sertraline) and Prozac (fluoxetine) appear to cause the least amount of weight gain.

Weight gain with SSRI treatment can vary. In general, weight gain is ranked:

• lowest with fluoxetine
• slightly higher with sertraline (Zoloft), citalopram (Celexa), escitalopram (Lexapro) and fluvoxamine (Luvox)
• highest with paroxetine (Paxil).

In a 26 to 32 week double-blind study, 284 patients with major depressive disorder were randomly assigned to long-term treatment with fluoxetine (Prozac), sertraline (Zoloft), or paroxetine (Paxil).

• Of the three SSRIs, paroxetine-treated patients had a significant weight gain, sertraline-treated patients had a modest but nonsignificant weight gain, and those receiving fluoxetine had a nonsignificant weight loss.
• The number of patients whose weight increased 7% or more from the start of the study was significantly greater for paroxetine-treated patients than for those receiving either fluoxetine or sertraline.

In another 2.5 year open-label study of 138 patients treated for obsessive-compulsive disorder (OCD), weight changes were assessed for several SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, or sertraline), as well as the tricyclic antidepressant (TCA) clomipramine.

• In all groups except fluoxetine, a significant weight gain was reported. Clomipramine (a TCA) was associated with the greatest weight gain. TCAs are well known to cause more weight gain than SSRIs.
• Of the SSRIs, fluoxetine (Prozac) and sertraline (Zoloft) had the lowest weight gain.
• Zoloft and Prozac also had the lowest percentage of patients with a weight gain of 7% or more over their initial body weight (4.5% for Zoloft and 8.7% for Prozac).

Do all antidepressants cause weight gain?

Treatment with antidepressants and selective serotonin reuptake inhibitors (SSRIs) in general tend to cause weight gain with long-term treatment (more than one year). Overall weight changes depend upon which antidepressant you use. Most antidepressants lead to only modest weight gain which can be addressed with diet and exercise.

• Older antidepressants like the tricyclic antidepressants (TCAs), for example amitriptyline or doxepin, cause more weight gain than the SSRIs but are infrequently prescribed today for depression.
• Mirtazapine (Remeron), a tetracyclic antidepressant, is known to be associated with significant weight gain. In studies, appetite increase was reported in 17% of patients treated with Remeron, and 7.5% of patients had a weight gain of at least 7% compared to the start of the study.
• In contrast, bupropion (Wellbutrin SR, Wellbutrin XL), an atypical antidepressant, is often linked with weight loss. In studies, between 14% and 19% of patients taking bupropion loss at least 2.2 kg (5 lb) compared to 6% on an inactive placebo.

A large cohort study (136,762 men and 157,957 women) in the United Kingdom looked at electronic health records to evaluate the long-term association between antidepressant prescribing and weight gain. Over 90% of patients had a diagnosis of depression.

Researchers looked at data over a 10-year period to determine the incidence of at least a 5% increase in body weight, and the number who transitioned (based on body mass index) to a status of overweight or obese.

• In the year of study entry, 13% of men and 22.4% of women (mean age of 51.5 years) were prescribed antidepressants, but may have had other diagnoses besides depression.
• Over the follow-up period, those prescribed an antidepressant had an increased risk of at least a 5% gain in body weight compared to those who were never prescribed an antidepressant.
• Weight gain substantially increased in the second and third years of treatment. During the second year of treatment, the risk of at least a 5% weight gain was found to be 46.3% higher than in a general population comparison group. Those originally classified as normal weight were more likely to transition to an overweight or obese category.
• Researchers concluded that antidepressant treatment was associated with a sustained increase in risk of weight gain over at least 5 years.

Why does Zoloft cause weight gain?

• It is not fully clear if weight gain with antidepressants and Zoloft in particular is due to an increased appetite after recovery from a mental health disorder, due to the medicine itself, or some other factor.
• Antidepressants may cause weight gain by interfering with serotonin or histamine neurotransmitters in the brain that control appetite.
• Some antidepressants may cause drowsiness or fatigue that lower levels of activity, leading to weight gain.

References

• Zoloft (sertraline) prescribing information. 9/2021. Pfizer Inc. New York, NY. https://labeling.pfizer.com/ShowLabeling.aspx?id=517#page=1
• Gafoor R, Booth HP, Gulliford MC. Antidepressant utilisation and incidence of weight gain during 10 years’ follow-up: population based cohort study. BMJ. 2018;361:k1951. Published 2018 May 23. doi:10.1136/bmj.k1951
• Maina G, Albert U, Salvi V, et al. Weight gain during long-term treatment of obsessive-compulsive disorder: a prospective comparison between serotonin reuptake inhibitors. J Clin Psychiatry. 2004 Oct;65(10):1365-71. doi: 10.4088/jcp.v65n1011.
• Fava M, Judge R, Hoog SL, et al. Fluoxetine versus sertraline and paroxetine in major depressive disorder: changes in weight with long-term treatment. J Clin Psychiatry. 2000 Nov;61(11):863-7. doi: 10.4088/jcp.v61n1109.
• Hirsch M, Birnbaum R, et al. Selective serotonin reuptake inhibitors: Pharmacology, administration, and side effects. Up to Date. Accessed Jan. 26, 2022 at https://www.uptodate.com/contents/selective-serotonin-reuptake-inhibitors-pharmacology-administration-and-side-effects
• Bupropion prescribing information (FDA). Drugs.com. Accessed Jan. 26, 2022 at https://www.drugs.com/pro/bupropion.html

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Medical Disclaimer

Does Zoloft cause weight gain?

Learn how to minimize Zoloft weight gain and compare the symptoms to those of other popular SSRIs

Zoloft (sertraline) is a prescription medication that belongs to the selective serotonin reuptake inhibitor (SSRI) class of antidepressants. Zoloft is often prescribed as part of a treatment plan, which may include other methods such as cognitive behavioral therapy, to treat major depressive disorder (depression) or other mental health conditions, including:

• Obsessive-compulsive disorder (OCD)
• Panic disorder (PD)
• Post-traumatic stress disorder (PTSD)
• Social anxiety disorder (SAD)
• Premenstrual dysphoric disorder (PMDD)

Zoloft is a popular antidepressant medication. As of 2020, more than 38 million prescriptions have been written for this medication. Many patients want to know if Zoloft will cause weight gain. In fact, one of the most common reasons why people stop taking SSRIs is because of weight gain. Zoloft may cause weight gain with long-term use. It may also cause a slight weight loss in children. Continue reading to learn more about Zoloft and its effect on body weight.

Does Zoloft cause weight gain?

Because everyone is different in their symptoms of depression or anxiety, as well as side effects and response to medication, weight changes due to Zoloft will vary by individual. One person may gain weight while another may lose. Some people eat more when they are depressed, and when they start taking Zoloft and feeling better, they may return to a normal diet and lose weight. On the other hand, some people experience appetite loss when depressed and eat less. Then, when taking Zoloft and starting to feel better, they may start to eat more and gain weight. 

While it is difficult to know how each person will respond to Zoloft in terms of weight gain, we can look at the results of some clinical studies. 

• A 2016 study looked at weight gain in adults after two years of antidepressant use. In this study, people who took sertraline gained an average of 5.9 pounds after two years.
• A review of many studies published in 2017 noted that a small weight loss may occur with short-term use of SSRIs, including Zoloft—in an 8-week study, individuals who took Zoloft lost an average of 1.58 pounds. However, short-term use of SSRIs is very unusual, because most people take SSRIs for at least 6 months—or much longer. The review noted a 2000 study, which looked at people who took an SSRI for up to 32 weeks and found sertraline to cause a weight gain of 1% (this would equate to a 1.8-pound weight gain for someone who weighs 180 pounds). And 4.2% of individuals who took Zoloft gained more than 7% of body weight (which would equate to at least 12.6 extra pounds for someone who weighs 180 pounds). 

In terms of children, Zoloft may affect growth hormones, which may slow growth and cause weight loss. Children who take Zoloft will have their height and weight monitored regularly.

Why does Zoloft cause weight gain?

Weight gain due to Zoloft (or any SSRI antidepressant) is thought to possibly be due to several factors, including: 

• By affecting serotonin receptor activity, which may regulate appetite and weight
• By increasing appetite, especially carbohydrate cravings
• By improving symptoms of depression, and helping appetite return to normal in those who had appetite loss

Other SSRIs and weight gain

SSRI weight gain can occur with other SSRIs besides Zoloft. A 2018 study in the British Medical Journal (BMJ) looked at the long-term use of antidepressants and weight gain. The study found that those who took an antidepressant had an increased risk of at least a 5% increase in weight, as opposed to individuals who did not take an antidepressant. Weight gain increased in the second and third years of treatment. The study researchers concluded that antidepressant use increased the risk of weight gain over at least 5 years. 

A 4-year study published in 2017 concluded that SSRI use was associated with weight gain—in combination with certain lifestyle factors including a Western diet, lack of activity, and smoking.  

The 2017 review of studies (mentioned in the section above) noted that some individuals gain what is considered to be an “extreme” amount of weight, which is more than 7% of body weight. Paxil (paroxetine) caused the most weight gain. In the study, 25.5% of people who took Paxil, 6.8% of people who took Prozac (fluoxetine), and 4. 2% of people who took Zoloft (sertraline) gained more than 7% of body weight.  

Another study also concludes that Paxil (paroxetine) may be most likely to cause greater weight gain than other SSRIs during long-term treatment. Interestingly —bupropion, which is not an SSRI, also known by its brand name, Wellbutrin, is an antidepressant that may cause weight loss—and is one ingredient in the weight-loss drug Contrave. 

One study examined adults using antidepressants for 6 to 36 months and found that 55% of people gained weight. Of these, almost 41% gained 7% or more of their weight compared to baseline. The study found Celexa (citalopram), Lexapro (escitalopram), Paxil (paroxetine), and Zoloft (sertraline) to be associated with significant weight gain—but not Prozac (fluoxetine). The study also found some serotonin-norepinephrine reuptake inhibitors (SNRIs) to cause weight gain, including Cymbalta (duloxetine) and Effexor (venlafaxine).  

Although SSRIs and SNRIs may cause weight gain, other types of antidepressants may cause weight gain as well. For example, tricyclic antidepressants such as Elavil (amitriptyline) or Pamelor (nortriptyline) are well-known for causing weight gain. And Remeron (mirtazapine), which is classified as a tetracyclic antidepressant, is known for causing significant increases in body weight and body fat. 

How to avoid Zoloft weight gain 

Not everyone will gain weight when taking Zoloft or an SSRI, especially if you are aware and proactive. Here are some tips to help avoid weight gain while taking Zoloft—or any antidepressant: 

• First, do not stop taking Zoloft suddenly, even if you start to gain weight. Stopping an SSRI suddenly can cause withdrawal symptoms—as well as worsen depression or anxiety. If you have any concerns about your medication, consult your doctor first. You and your healthcare professional will need to consider all options regarding which medication is best and the possibility of weight gain. For example, a weight gain of 3 pounds over several years can be considered insignificant when compared to living with symptoms of depression. However, a larger weight gain caused by an antidepressant could lead to other health problems like high blood pressure, which could require either lifestyle changes or a change to a different drug.
• If you have gained weight, ask your healthcare professional if there could be another cause. The SSRI may not necessarily be the culprit of weight gain. Another medical condition could be the cause.
• Talk to your healthcare professional, or consult a registered dietician, about lifestyle changes, such as incorporating a healthy diet of nutritious foods and an exercise plan that will fit into your life. According to the Centers for Disease Control and Prevention (CDC), adults should get at least 150 minutes of moderate-intensity physical activity every week, plus two strength-training sessions. This can be done, for example, by walking for 30 minutes, 5 days per week, and adding in two strength-training workouts. You can walk outside, or even around a mall—or check YouTube for thousands of free exercise videos, including walking videos. In addition to helping avoid weight gain, this benefits overall health, too.
• Keep track of your weight while taking Zoloft. This way, you can see if there is a pattern of weight gain, and make changes if necessary.
• If weight gain becomes a problem, or you do not want to take a medication that may make you gain weight, ask your healthcare provider for medical advice about trying a different medication—such as bupropion—with a lower risk of weight gain. 

Ask your healthcare professional for other ideas that are personalized to your individual needs. Working together with your healthcare team, you will be able to find the treatment that works best for your depression or anxiety—while also minimizing weight gain. 

Seralin (sertraline) in the treatment of depression | #10/05

The prevalence of depressive disorders, the variability of their structure, combination with other neurotic or psychotic disorders, connection with personal attitudes, somatic and social factors give rise to a large number of clinical forms of depression and, therefore, require the use of a variety of therapeutic agents.

Affective disorders occur during the life of every fifth person. The risk of developing depression reaches a level of 20%, 1% of cases are diagnosed initially each year, depression recurs in 55% of individuals, and becomes chronic in 12–15%. More than 60% of patients with depression do not fall into the field of view of psychiatrists, since atypical clinical forms predominate in the structure of morbidity.

Only 10-15% of patients with depression receive treatment, and only 0.1% of patients are admitted to psychiatric hospitals. According to WHO estimates, major depression is now the 4th leading cause of reduced life expectancy, taking into account reduced work capacity.

30-40% of patients with depression remain resistant to adequate thymoanaleptic therapy. In this case, resistance to the first drug reaches 40-60%.

Modern requirements for an antidepressant, along with a sufficiently effective thymoanaleptic effect, include good tolerability and a favorable side effect profile, as well as the absence of “behavioral toxicity”.

In this regard, there is a constant search for drugs that would optimally combine both high thymoanaleptic efficacy and a sufficient degree of safety.

Antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs) are the most widely used in the world psychiatric and general medical practice. Their therapeutic effect is associated with inhibition of serotonin reuptake both in the central nervous system and in the peripheral nervous system. At the next stage, the blocking function of serotonin IA receptors located in the somatodendritic part of neurons in the raphe region of the midbrain is disrupted. At the same time, the side effects of the drug that occur at the 1st stage are mitigated, and signs of a therapeutic antidepressant effect appear. Serotonin neurons are disinhibited (disinhibited), and serotonin begins to rapidly release from the axons leading to different brain structures. SSRI preparations do not have pronounced “behavioral toxicity”, anticholinergic side effects, adverse hepato-, cardiotropic effects and teratogenicity. They are convenient to use, as they have a prolonged action up to a day, can be used without dose titration, do not cause dependence and withdrawal syndrome.

This group of drugs includes sertraline (zoloft, seraline). However, it has its own specific features that predetermine its relevance in clinical practice.

Firstly, it is a balanced type of drug that does not cause an exacerbation of anxiety and emotional tension, which makes it possible to expand the scope of its application.

Secondly, it can be attributed to the SSRIs of the second generation, since the geometry of the antidepressant at the molecular level has been changed in its structure, as a result of which it was possible to achieve a more “precise” interaction with the receptor. So, when comparing the S- and R-enantiomers, it turned out that the S-enantiomer of the active substance is 30 times more potent serotonin reuptake inhibitor than its optical antipode.

Thirdly, sertraline is one of the few antidepressants approved for use in pediatric practice, which, apparently, may indicate the level of its safety.

Fourthly, this drug has proven itself in the treatment of depression with comorbid mental disorders, which expands the range of its use both in psychiatry and in general medical practice: chronic pain syndrome, bulimia, obesity, alcoholism, obsessive-compulsive disorders, attention deficit disorder with hyperactivity, panic disorders, etc.

Side effects of the drug are associated with hyperstimulation of the serotonin system: gastrointestinal disorders, loss of appetite, dizziness, nausea, diarrhea, hyperreflexia.

Sertraline hydrochloride is a bicyclic drug, a derivative of naphthylamine. It is a potent selective inhibitor of serotonin reuptake, does not cause blockade of muscarinic, serotonin, adrenergic and GABAergic receptors. The drug has practically no anticholinergic, cardiotoxic and sedative properties. The basis of its action profile is a distinct thymoleptic effect with a weak stimulating component. Relieving depressive symptoms, the drug also successfully affects the parameters of the immune, neurotransmitter and hormonal systems.

A number of works by modern authors are devoted to the clinical evaluation of the use of sertraline for the relief of depression in patients [1, 2, 3, 4, 5, 6, 7, 8, 9].

Our study pursued the following objectives: to confirm the antidepressant activity of the drug seralin ^* ; determine the effectiveness of the drug depending on the complexity, depth of the structure of depressive disorders; clarify the spectrum of psychotropic activity of the drug, identify the side effects.

The study involved 40 patients (14 men, 26 women), whose clinical picture revealed depressive conditions within a single or recurrent depressive episode (F-33.1; F-33.2), bipolar affective disorder (F-31, 3; F-31.4), cyclothymia with comorbid anxiety-phobic personality disorders (F-60.1; F-60.3).

The selection criteria were: the leading mental disorder — depressive syndrome; relative monomorphism of the disorder.

Exclusion criteria: children’s and senile age; severe somatoneurological pathology; the severity of the schizophrenic defect; substance abuse.

The patients’ age ranged from 20 to 61 years. The duration of the disease ranged from 1 week to 18 years. The mental state of patients at the start of therapy was determined by depressive symptoms of varying depth and structure.

The patients were diagnosed with the following syndromes: typical classical depression; anxious depression; apathetic depression; obsessive-phobic syndrome; depressive delusional syndrome.

Comorbid anxiety-phobic disorders were represented by panic attacks in 21 patients, manifestations of the type of generalized anxiety – in 14, obsessive-compulsive disorders – in 5 patients. The duration of treatment was 6 weeks. The initial daily dose was determined individually (50 or 100 mg/day). The maximum dose is up to 150 mg / day. The drug was administered orally in the morning, along with food; combinations with other antidepressants were avoided whenever possible. However, the peculiarities of the mental state of patients dictated the need to prescribe sedative or hypnotic drugs. Therefore, we used clonazepam, phenazepam and small doses of neuroleptics: sonapax, chlorproxen. During the follow-up period, 5 patients dropped out of the study for various reasons: 2 of them were discharged from the hospital due to family reasons against the background of some improvement in their condition; in 2 clinical cases, there was a transition to another phase (affect inversion).

Feeling of nausea, mild diarrhea, increased heartburn, loss of appetite was noted by 1 patient.

The therapeutic effect of seralin was determined by the degree of reduction in the total score of the Hamilton scale (HDRS) to assess depressive symptoms at different periods of treatment. The total score was recorded during five visits: H0 — at inclusion in the study; H1 – 1 week after the start of the drug; H2 – after 2 weeks; H3 – after 4 weeks; H6 – after 6 weeks after the start of taking seralin.

The criterion for the effectiveness of therapy was a 50% reduction in symptoms according to HDRS. An additional assessment of the effectiveness of therapeutic measures was performed on the basis of the CGI scale of general clinical impression. All patients were examined daily by a doctor. The dynamics of the state was reflected in extended diaries according to rating scales and the results of paraclinical studies.

When analyzing the results of the study, attention is drawn to the dynamism and relative harmony of the reduction of depressive symptoms, the absence of a period of hyperstimulation, increased anxiety, agitation, and activation of suicidal tendencies. This is especially important for depressed patients with obsessive-phobic disorders in the form of panic attacks, since the initial level of anxiety in them at the beginning of therapy significantly exceeded the level of anxiety in other patients. At the 1st stage of treatment, the actualization of anxious fears decreases, a more relaxed attitude towards phobias is formed, hypochondriacal manifestations fade, by the end of the 2nd week, the manifestation of anxiety and somatization decreases in patients, the level of anxiety harmoniously decreases and mood improves.

Obsessive-phobic symptoms cease to dominate in consciousness, manifestations of avoidant behavior soften, obsessions and phobias cease to be painfully painful, their significance decreases. On the 4th week of therapy, patients have plans for the future, interest in cognitive and work activities awakens, they move more easily, communicate and gradually return to their usual way of life. Patients develop a positive attitude towards the drug and an understanding of the need for long-term maintenance therapy.

Dynamics in the form of a dissociated variant of the reduction of symptoms was observed in those clinical cases when melancholy or apathy was the predominant affect in the structure of the depressive syndrome, and comorbid symptoms were represented by a generalized anxiety state or “depressive alienation” of mental functions (apathy, anhedonia, abscess in the form of influxes of painful reasoning, without a pronounced somatovegetative component, adynamia, etc.). At the 1st stage of the study, anxiety and the relevance of painful experiences decreased, and at the 2nd stage, mood improved and vital activity appeared.

At the end of the study, the results of therapy showed that 22 patients had a “marked improvement” (according to the CGI scale), 11 patients had a “moderate improvement”, 4 patients had a “slight improvement”, 2 patients had an “undetermined antidepressant effect” ( short-term improvement, without stabilization of the condition) and 1 – no change.

The pronounced thymoleptic activity of the drug was confirmed by the dynamics of the HDRS depression scale indicators: a pronounced therapeutic effect (a decrease in indicators by more than 50%) was registered at the transition from the 3rd to the 4th week of the study. By the end of therapy, a decrease in the average score on the HDRS scale by 34% from the baseline was noted.

In all patients, the stimulating effect appeared on the 4th week of therapy.

In the course of the study, side effects were identified in 5 patients. On the 3rd day, 1 patient developed anxiety, an excited state, which, apparently, is associated with the still insufficiently formed anxiolytic effect of the drug. In three clinical cases, transient symptoms of nausea were observed. In 1 patient, there was a short-term urinary retention, which resolved without discontinuation of the drug and dose reduction. Side effects described in the literature (L. Ziplinski et al., 1989; H. Gommans, 1990) were not registered in our study.

Analyzing clinical observations, we can draw the following conclusions.

• Seralin (sertraline) has a pronounced thymoleptic effect.
• The profile of the therapeutic activity of the antidepressant seralin consists of a harmonious, sequentially formed anxiolytic, thymoleptic and stimulating effects.
• Seralin can serve as the drug of choice in the treatment of depression with a predominance of anxiety, especially with comorbid obsessive-phobic disorders.
• The peculiarity of the therapeutic profile of the drug makes it possible to avoid an increase in suicidal risk in the early stages of depression treatment.
• The drug seralin is well tolerated, side effects are minor, quickly stopped and do not interfere with therapy.
• The antidepressant seraline (sertraline) is characterized by a balanced therapeutic effect with sequentially occurring anxiolytic, thymoleptic and weak stimulant effects.

For literature, please contact the editor.

B. A. Tashmatov , Doctor of Medical Sciences, Professor
N. Bulycheva, Associate Professor
1st Tashkent State Medical Institute , Tashkent

^* The drug is registered in Ukraine, Kazakhstan, Uzbekistan and a number of other CIS countries; in Russia passes the stage of registration.

Sertralin (Sertralinum) – PsyAndNeuro.ru

Trade names in Russia

Zoloft, Stimuloton, Serenata, Aleval, Serlift, Torin 02 Presentation

Tablets: 50 mg, 100 mg

Content

Pharmacological group

Antidepressant

serotonin reuptake tor [2].

Indications

disorder

F40.1 Social phobias

F41.0 Panic disorder (episodic paroxysmal anxiety)

F42.9 Obsessive-compulsive disorder, unspecified

F43.1 Post-traumatic stress disorder

◊ FDA recommendation

• Major depressive disorder
• Premenstrual dysphoric disorder
• Panic disorder
• Post-traumatic stress disorder
• Social phobia
• Obsessive Compulsive Disorder (OCD)
• Generalized Anxiety Disorder (GAD)

◊ Recommendations UK Medicines and Healthcare Products Regulatory Agency

• Major depressive disorder
• Panic disorder with/without agoraphobia
• OCD in adults and children from 6 years of age
• Social phobia
• Post-traumatic stress disorder

◊ Off-label use

• Prevention of arterial hypotension during hemodialysis [6]
• Itching [7]

Target symptoms

• Depressed mood
• Anxiety
• Sleep disturbance, especially insomnia
• Panic attacks, avoidance behavior

Mechanism of action and pharmacokinetics

Selectively blocks (mainly through serotonin 1A receptors) the reuptake of serotonin by the presynaptic membrane of brain neurons and platelets. With prolonged use, it reduces the amount of serotonin 5-HT1A and adrenoreceptors in the central nervous system. Sertraline also has some ability to block dopamine reuptake, which can increase dopamine neurotransmission. Sertraline also binds to sigma 1 receptors, which may explain its anti-anxiety effects.

• Sertalin is metabolized by several cytochrome P450 (CYP) enzymes: CYP2B6, CYP2C19, CYP2C9, CYP2D6 and CYP3A4, as well as monoamine oxidases and glucuronyltransferases [10]
• Maximum plasma concentration after 4.5-8.4 hours
• Half-life 22-36 hours;
• The half-life of metabolites is 62-104 hours [7].

Treatment regimen

◊

Dosage and dose selection

• Optimal dose: 50-200 mg/day
• Depression and OCD: start at 50 mg and wait a few weeks, but can be increased every week, maximum 200 mg/day
• Panic disorder, PTSD, social anxiety: start at 25 mg, increase to 50 mg after a week, wait a few weeks to assess whether to increase, maximum 200 mg/day
• Premenstrual dysphoric disorder: 50 mg/day entire menstrual cycle or luteal phase only
• Itching: 25-100 mg/day [7]
• Prevention of arterial hypotension during hemodialysis: 100 mg/day [6].
• 50 mg/day is insufficient for many patients [1]
• For severe anxiety and agitation, start at a lower dose, titrate more slowly, and add trazadone or benzodazepine
• If patient has a history of intolerance to antidepressants, start at 12.5 mg
• If anxiety, insomnia, agitation, akathisia occur at the start of treatment or after interruption of treatment, consider the possibility of bipolar disorder and switch to a mood stabilizer or an atypical antipsychotic

◊

How fast it works

• In some patients it works immediately.
• Begins to work after 2-4 weeks.
• If there is no effect after 6-8 weeks, increase the dose or switch to another drug.
• May be taken for many years to prevent relapse.

◊ Expected result

• Complete remission.
• After the disappearance of symptoms of depression, you should continue taking 1 year if it was the treatment of the first episode. If this is a re-episode treatment, treatment can be extended indefinitely.
• Use in the treatment of anxiety may be indefinite [1].

◊

If not working

• Change dose, switch to another drug, or add an ancillary drug;
• Connect psychotherapy;
• Reconsider the diagnosis, looking for comorbid conditions;
• Patients with undiagnosed bipolar affective disorder may be less effective, in which case switching to a Mood Stabilizer [1].
• Electroconvulsive therapy should be considered in the acute phase of a severe depressive disorder accompanied by psychotic or catatonic symptoms, as well as in patients with actual suicidal ideation [4].

◊

How to stop taking

• Gradually reduce the dose to avoid withdrawal symptoms;
• For many, the following scheme works: reduce by 50% in 3 days, then another 50% in 3 days, then stop;
• If withdrawal is very severe, increase dose and wait until withdrawal symptoms subside;
• It is important to distinguish the withdrawal syndrome from the return of symptoms of the disease [1].

◊

Treatment combinations

• For insomnia: trazadone
• In the US, sertraline is combined with bupropion. This combination is called “Well-loft”.
• For fatigue, drowsiness, loss of concentration: modafinil [3].
• Combinations with other antidepressants may activate bipolar disorder and suicidal ideation
• For bipolar depression, psychotic depression, resistant depression, resistant anxiety disorder: mood stabilizers, atypical antipsychotics
• For anxiety disorder: gabapentin, tiagabine
• Benzodiazepines

Warnings and contraindications

• Start another antidepressant 2 weeks after stopping sertraline;
• Use caution if patient has had convulsions;
• Use caution if patient has bipolar disorder;
• Do not use if patient is taking pimozide, thioridazine, MAOIs;
• Do not use if allergic to sertraline [1]

Special groups of patients

◊

Patients with diseased kidneys

Special dose selection is not required [1].

◊

Patients with diseased liver

Reduce doses or take twice as often [1].

◊

Heart patients

Useful in the recovery of depressed patients after a heart attack.

◊

Elderly patients

For some, low doses are better.

◊

Children and adolescents

• Patients should be checked regularly and personally, especially during the first weeks of treatment.
• Inform adults of the risks.
• Approved for OCD
• Ages 6-12: starting dose 25 mg/day
• Adult doses from 13 years of age [1].

◊

Pregnant

• Not recommended for pregnant women, especially in the first trimester [9]
• All risks should be weighed and compared
• Bleeding can be expected at delivery

◊

Breastfeeding

• The drug passes into breast milk.
• If infant shows signs of irritation or sedation, discontinue feeding or sertraline
• However, postpartum treatment may be necessary and the risks should be weighed.
• Sertraline has proven effective in the treatment of postpartum depression
• Sertraline is the most studied antidepressant used in breastfeeding women. It is the preferred antidepressant during lactation [8].

Interactions with other substances

• Tramadol increases the risk of seizures
• Cannot be used with MAO inhibitors. After the end of the intake of MAO inhibitors, 14 days should pass. Start treatment with MAO inhibitors 7 days after the end of citalopram.
• Together with anticoagulants, probably increases the risk of bleeding.
• Urine tests for benzodiazepines may give a false positive result in those taking sertraline.
• Due to inhibition of CYP450 2D6, sertraline may increase thioridazine levels and cause arrhythmias
• Due to inhibition of CYP450 3A4, sertraline may increase the levels of alprozalam, buspirone and triazolam
• By inhibiting CYP450 3A4, sertraline could theoretically increase concentrations of certain cholesterol-lowering HMG-CoA reductase inhibitors, especially simvastatin, atorvastatin and lovastatin, but not pravastatin or fluvastatin, which would increase the risk of rhabdomyolysis. Therefore, co-administration of sertraline with certain HMG CoA reductase inhibitors should be undertaken with caution

Tests during treatment

Not required.

Side effects and other risks

◊

Mechanism of occurrence of side effects ina. Most side effects occur immediately after the start of treatment and go away over time, while therapeutic effects increase over time.

◊

Side effects

• Gastroenterological (decreased appetite, nausea, diarrhea, constipation)
• Insomnia, sedation, agitation, tremor, headache
• Sweating
  • Rare hyponatremia in the elderly (resolves after discontinuation of sertraline) [1]
  • Dangerous side effects: convulsions, mania, suicidal ideation
  • Weight gain: rare
  • Sedation: rarely
  • Sexual dysfunction: yes (dose-dependent effect)

◊

Dealing with side effects

1. Wait;
2. If sertraline activates, take in the morning;
3. Reduce dose to 25 mg or 12. 5 mg, increase dose when side effects subside;
4. If side effects persist, change drug [1]

◊

Long term use

Safe

◊

Addictive

90 002

No.

◊

Overdose

• Very rare cases of fatal overdose. Fatal outcomes are associated with the combination of sertraline with alcohol and drugs.
• Vomiting, sedation, cardiac arrhythmias.

Benefits

• Good for patients with atypical depression
• Good for patients with fatigue and low energy
• Sertraline is the only SSRI that does not increase prolactin [1]
• Sertraline is the most studied antidepressant used in breastfeeding women. It is the preferred antidepressant during lactation [8]

Weaknesses

• Difficulty starting treatment for anxious patients with insomnia;
• Not suitable for irritable bowel syndrome;
• May require dose titration.

Expert Advice

• Antidepressant with the best proven cardiac safety.
• More likely to cause gastrointestinal side effects (diarrhea) than some other antidepressants [1].
• Sertraline shows efficacy in the treatment of depression in patients with vascular cognitive impairment [5].
• May be more effective treatment for women with PTSD or depression than for men with PTSD or depression, but clinical relevance is unknown
• SSRIs may be less effective in women over 50, especially if they are not taking estrogen
• Some evidence suggests that treatment with sertraline during the luteal phase alone may be more effective than continuous treatment in patients with PMDD.
• In combination with olanzapine, sertraline has been shown to be effective in the treatment of psychotic depression [10]. It is important to bear in mind that sertraline increases the clearance of olanzapine by 30%. Moreover, such an effect is difficult to explain by the interaction of drugs at the level of cytochromes. Perhaps this is related to P-glycoprotein.
• The fact that sertraline can be metabolized by multiple pathways is clinically beneficial: it is less susceptible to drug interactions than antidepressants that rely on only one enzyme or pathway as their main metabolic pathway.
• An additional advantage of sertraline over some other SSRIs (especially fluoxetine, paroxetine and fluvoxamine) is that it is not a strong inhibitor of any particular CYP enzyme [10].

Footnotes

1. Stephen Stahl “Prescriber’s Guide”, 6th edition, 2017

2. Neuroscience-Based Nomenclature (https://www.nbn2.com/ taskforce)

3. In Russia, modafinil listed on the Restricted and Controlled Narcotic Drugs and Psychotropic Substances List (Schedule II)

4. American Psychiatric Association. Guideline Watch: Practice Guideline for the Treatment of Patients with Major Depressive Disorder, Second Edition. American Psychiatric Association Practice Guidelines .

5. Weissberger GH et al. Sertraline for the treatment of depression in vascular cognitive impairment [published online April 25, 2018]. American J Geriatr Psychiatry.

6. Hamid Noshad et al. (2018) Sertraline Prevents Hypotension During Hemodialysis: A Randomized Clinical Trial. Nephro Urology Monthly. In Press. 10.5812/numonthly.66060.

7. Sertraline medscape.com

8. American Psychiatric Association (APA) Annual Meeting on Psychopharmacology 2018 Highlights

9. Shen ZQ, Gao SY, Li SX, et al. Sertraline use in the first trimester and risk of congenital anomalies: a systemic review and meta-analysis of cohort studies. Br J Clin Pharmacol . 2016;83(4):909-922.

10. Davies S. J. C., Mulsant B. H., Flint A. J., Meyers B. S., Rothschild A. J. Whyte E. M. (2016). SSRI-antipsychotic combination in psychotic depression: sertraline pharmacokinetics in the presence of olanzapine, a brief report from the STOP-PD study. Human Psychopharmacology: Clinical and Experimental, 31(3), 252–255.