Sertraline

Sertraline Uses, Dosage, Side Effects, Food Interaction and all others data.

Sertraline has potent and selective inhibitory action on CNS neuronal reuptake of 5-HT resulting in increased 5-HT concentrations at the synaptic clefts, leading to facilitation of its sustained activity at the postsynaptic receptor sites. It ultimately results in an improvement of depression. Reduction of Serotonin turnover in brain by Sertraline is also another contributing fact implicated in its action. Its prolonged elimination half-life offers a benefit of once daily administration.

Sertraline improves or relieves the symptoms of depression, OCD, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, and premenstrual dysphoric disorder via the inhibition of serotonin reuptake. Clinical studies have shown that it improves cognition in depressed patients. It has less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not exert significant anticholinergic, antihistamine, or adrenergic (alpha1, alpha2, beta) blocking activity. The onset of action and beneficial effects are usually noticed after 4-6 weeks, for reasons that are not fully understood and currently under investigation.

Trade Name Sertraline
Availability Prescription only
Generic Sertraline
Sertraline Other Names Sertralina, Sertraline, Sertralinum
Related Drugs Rexulti, trazodone, fluoxetine, alprazolam, clonazepam, Lexapro, amitriptyline, venlafaxine, Zoloft, citalopram
Type Oral solution
Formula C17H17Cl2N
Weight Average: 306.23
Monoisotopic: 305.073804963
Protein binding

Sertraline is highly bound to serum proteins, at about 98%-99%.

Groups Approved
Therapeutic Class SSRIs & related anti-depressant drugs
Manufacturer Ranbaxy (UK) Limited a Sun Pharmaceutical Company
Available Country United Kingdom, Canada, United States, Netherlands
Last Updated: September 19, 2023 at 7:00 am
Sertraline
Sertraline

Uses

Sertraline is used for Depressive illness, Obsessive-compulsive disorder, Post-traumatic stress disorder, Panic disorder

Sertraline is also used to associated treatment for these conditions: Binge Eating Disorder (BED), Bulimia Nervosa, Generalized Anxiety Disorder (GAD), Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD), Panic Disorder, Post Traumatic Stress Disorder (PTSD), Premenstrual Dysphoric Disorder, Social Anxiety Disorder (SAD)

How Sertraline works

Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, thereby increasing serotonergic activity. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. These changes are believed to be responsible for the antidepressant action and beneficial effects in obsessive-compulsive (and other anxiety related disorders). It has been hypothesized that obsessive-compulsive disorder, like depression, is also caused by the disregulation of serotonin.

In animal studies, chronic administration of sertraline results in down-regulation of brain norepinephrine receptors. Sertraline displays affinity for sigma-1 and 2 receptor binding sites, but binds with stronger affinity to sigma-1 binding sites. In vitro, sertraline shows little to no affinity for GABA, dopaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. It exerts weak inhibitory actions on the neuronal uptake of norepinephrine and dopamine and exhibits no inhibitory effects on the monoamine oxidase enzyme.

Dosage

Sertraline dosage

Depressive illness: 

  • Adult: Initially 50 mg daily, increased if necessary by increments of 50 mg over several weeks to maximum 200 mg daily. Usual maintenance dose is 50 mg daily.
  • Child and adolescent less than 18 years: Not recommended.

Obsessive-compulsive disorder: 

  • Adult and adolescent over 13 years: Initially 50 mg daily, increased if necessary in steps of 50 mg over several weeks. Usual dose range is 50-200 mg daily.
  • Child (6-12 years): Initially 25 mg daily, increased to 50 mg daily after 1 week, further increased if necessary in steps of 50 mg at intervals of at least 1 week (maximum 200 mg daily).

Post-traumatic stress disorder:

  • Adult: Initially 25 mg daily, increased after 1 week to 50 mg daily; if response is partial and if drug is tolerated, dose can be increased in steps of 50 mg over several weeks to maximum 200 mg daily.
  • Child and adolescent less than 18 years: Not recommended.

Side Effects

Sertraline may cause side effects like upset stomach, diarrhoea, constipation, vomiting, dry mouth, loss of appetite, weight changes, drowsiness, dizziness, headache, pain, burning or tingling in the hands or feet, excitement, sore throat etc.

Toxicity

The LD50 of sertraline is >2000 mg/kg in rats according to the FDA label. One other references indicates an oral LD50 of in mice and rats of 419 - 548 mg/kg and 1327 - 1591mg/kg, respectively.

The most common signs and symptoms associated with a non-fatal sertraline overdose are somnolence, vomiting, tachycardia, nausea, dizziness, agitation, and tremor. No cases of fatal overdose with only sertraline have been reported. Most fatal cases are associated with the ingestion of sertraline with other drugs. Consequences of a sertraline overdose may include serotonin syndrome, hypertension, hypotension, syncope, stupor, coma, bradycardia, bundle branch block, QT-prolongation, torsade de pointes, delirium, hallucinations, and pancreatitis.

Precaution

Precaution should be taken in case of liver problems, kidney diseases, seizures, heart problems and any allergies. This drug may cause dizziness or drowsiness. Caution should be taken in activities requiring alertness such as driving or using machinery. Caution is advised while using this product in the elderly because they may be more sensitive to the effects of the drug. Do not take this drug if you have taken monoamine oxidase inhibitor in the last five weeks.

Interaction

Potential effects of co-administration of drugs that are highly bound to plasma proteins- As Sertraline is tightly bound to plasma protein, the administration of Sertraline to a patient taking another drug which is tightly bound to protein, (e.g. warfarin, digitoxin) may cause a shift in plasma concentrations potentially resulting in an adverse effect. Conversely adverse effects may result from displacement of protein bound Sertraline by other tightly bound drugs. Sertraline may interact with other drugs such as Cimetidine, CNS active drugs like Diazepam, Hypoglycemic drugs, Atenolol etc.

Food Interaction

  • Avoid St. John's Wort.
  • Take with or without food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of sertraline.

Use in combination may result in additive central nervous system depression and

In addition, limited clinical data suggest that consumption of grapefruit juice during treatment with sertraline may result in increased plasma concentrations of sertraline.

The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism by certain compounds present in grapefruit.

An in-vitro study demonstrated that grapefruit juice dose-dependently inhibits the conversion of sertraline to its metabolite, desmethylsertraline.

In a study with eight Japanese subjects, mean plasma levels of sertraline increased by approximately 100% and maximum plasma concentrations increased by 66% after the ingestion of three 250 mL glasses of grapefruit juice per day for 5 days and administration of a single dose of sertraline 75 mg on the sixth day.

In another small study with 5 patients, mean sertraline trough levels increased by 47% after taking sertraline for at least 6 weeks, then taking sertraline with 240 mL grapefruit juice daily for 1 week.

The clinical significance is unknown; however, pharmacokinetic alterations associated with interactions involving grapefruit juice are often subject to a high degree of interpatient variability.

The possibility of significant interaction in some patients should be considered.

MANAGEMENT: Patients receiving sertraline should be advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how sertraline affects them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Some authorities recommend that consumption of grapefruit juice should be avoided during sertraline therapy.

Volume of Distribution

Sertraline is widely distributed, and its volume of distribution is estimated to be more than 20L/kg. Post-mortem studies in humans have measured liver tissue concentrations of 3.9–20 mg/kg for sertraline and between 1.4 to 11 mg/kg for its active metabolite, N-desmethyl-sertraline (DMS). Studies have also determined sertraline distributes into the brain, plasma, and serum.

Elimination Route

Following once-daily administration of 50 to 200 mg for two weeks, the mean peak plasma concentrations (Cmax) of sertraline occurred between 4.5 to 8.4 hours after administration, and measured at 20 to 55 μg/L. Steady-state concentrations are reached after 1 week following once-daily administration, and vary greatly depending on the patient. Bioavailability has been estimated to be above 44%. The area under the curve in healthy volunteers after a 100mg dose of sertraline was 456 μg × h/mL in one study.

Effects of food on absorption

The effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects given a single dose with and without food. For the tablet, AUC was slightly increased when sertraline was administered with food, the Cmax was 25% greater, and the time to peak plasma concentration was shortened by about 2.5 hours. For the oral concentrate preparation of sertraline, peak concentration was prolonged by approximately 1 hour with the ingestion of food.

Half Life

The elimination half-life of sertraline is approximately 26 hours. One reference mentions an elimination half-life ranging from 22-36 hours.

Clearance

In pharmacokinetic studies, the clearance of a 200mg dose of sertraline in studies of both young and elderly patients ranged between 1.09 ± 0.38 L/h/kg - 1.35 ± 0.67 L/h/kg.

Elimination Route

Since sertraline is extensively metabolized, excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Although animal studies did not provide any evidence of teratogenicity, the safety of Sertraline during human pregnancy has not been established. 

Lactation: Sertraline is known to be excreted in breast milk. Its effects on the nursing infant have not yet been established. If treatment with Sertraline is considered necessary, discontinuation of breast-feeding should be considered.

Contraindication

Sertraline is contraindicated in patients with a known hypersensitivity to Sertraline or any of the excipients of drug.

Storage Condition

Store at 25° C.

Innovators Monograph

You find simplified version here Sertraline

Sertraline contains Sertraline see full prescribing information from innovator Sertraline Monograph, Sertraline MSDS, Sertraline FDA label

FAQ

What are the side effects for Sertraline?

Sertraline may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • nausea
  • diarrhea
  • constipation
  • vomiting
  • difficulty falling asleep or staying asleep
  • dry mouth
  • heartburn
  • loss of appetite
  • weight changes
  • dizziness
  • excessive tiredness
  • headache
  • nervousness
  • uncontrollable shaking of a part of the body
  • changes in sex drive or ability
  • excessive sweating

What should I do if I forget to take Sertraline?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Is Sertraline a strong antidepressant?

Sertraline (sertraline) is a good and safe antidepressant that is also used to treat other psychiatric disorders such as panic disorder, post-traumatic stress disorder and obsessive compulsive disorder.

Is Sertraline good for anxiety?

A study in The Lancet Psychiatry found that taking Sertraline leads to an early reduction in anxiety symptoms, commonly found in depression, several weeks before any improvement in depressive symptoms.

Does Sertraline make you happy?

Sertraline will not change your personality or make you feel euphorically happy. It'll simply help you feel like yourself again. Do not expect to feel better overnight, though. Some people feel worse during the first few weeks of treatment before they begin to feel better.

Can I take Sertraline at night?

Sertraline is designed for use once per day. It's safe to take it at any time of day, with or without food. Many people who experience nausea and other side effects from Sertraline opt to take it at night in order to limit these side effects.

What can't I take with Sertraline?

Some products that may interact with this drug are: pimozide, other drugs that can cause bleeding/bruising (including antiplatelet drugs such as clopidogrel, NSAIDs such as ibuprofen/naproxen, "blood thinners" such as warfarin/dabigatran).

Why does Sertraline make gain weight?

One potential theory is that antidepressants like Sertraline can make you feel hungrier than normal. People who use Sertraline might also feel less satisfied after eating food, resulting in them eating bigger portions that contain a larger amount of calories.

Why is Sertraline making me so tired?

Fatigue and tiredness are two of the most common side effects of Sertraline, as well as several other SSRIs. If you're using Sertraline to treat depression, fatigue and tiredness from the medication can also be compounded by the effects of depression on your mood.

Will Sertraline calm me down?

Sertraline should help you feel calm and relaxed. It could take some time for Sertraline to have its full effect. This effect should reduce your behavior problem.

Can Sertraline work immediately?

Sertraline doesn't work immediately, so don't stop taking Sertraline if your symptoms don't improve right away. It takes two to six weeks to start reducing anxiety symptoms. Some people may feel a reduction in their anxiety symptoms within the first week of taking Sertraline, but this shouldn't be expected for everyone.

What happens if I drink alcohol with sertraline?

You should not mix alcohol with Sertraline. Combining the two can make you feel very drowsy, which can be dangerous. The combination can also raise your risk of other dangerous or unpleasant side effects from Sertraline. Even if you don't take Sertraline, you shouldn't drink alcohol if you have depression.

Is Sertraline a addictive?

Since Sertraline is a long-term antidepressant, it is not considered an addictive or narcotic substance. The potential for abuse is low according to psychiatrists, even though it is a mind-altering substance. Taken properly and as prescribed, Sertraline carries very little risk for abuse or addiction.

Does Sertraline give me energy?

It can improve sleep quality, appetite, energy levels, restore interest in daily life, and reduce unwanted thoughts and panic attacks. Sertraline is available in tablet form in dosage strengths of 25 mg, 50 mg, or 100 mg.

How long does Sertraline last in my body?

Sertraline last 5.4 days in our body and half life is about 26 hours. 

Does Sertraline make me sleepy?

You can feel drowsy in the first few days of taking Sertraline. This should get better after the first week or two. If it makes you feel drowsy, try taking it just before you go to bed. You could also, strangely, get insomnia (difficulty getting to sleep), and disturbing dreams or nightmares.

Can I take paracetamol with Sertraline?

It is OK to take Paracetamol with Sertraline, but if you are taking other kinds of medication every day you need to let your doctor know, as they may interact with Sertraline and change its effect on your body.

Can I stop Sertraline after 2 days?

After one day, the level is reduced to 50 percent of the original level, after two days to 25 percent, after three days to 12.5 percent, and so on. Because Sertraline leaves your body so quickly, stopping it too abruptly can cause discontinuation syndrome to develop.

Can I take 2 50mg Sertraline?

Talk to your doctor about any other medications you may be taking. You should never take two doses of Sertraline at the same time, as it can lead to an accidental overdose.

Can I drink coffee with Sertraline?

No interactions were found between caffeine and Sertraline. This does not necessarily mean no interactions exist. Always consult your healthcare provider.

Why is Sertraline making me sick?

When serotonin levels increase under the influence of SSRIs, they stimulate serotonin receptors in the GI tract as well as the brain. The combined stimulatory effect—on both the GI tract and CNS—can trigger such side effects as: Diarrhea. Loss of appetite (anorexia)

Can Sertraline become ineffective?

If you feel like your antidepressant has stopped working, you're not alone. It's common for a medication that once worked wonders to become ineffective, especially if you've been taking it for a long time. Symptoms return for up to 33% of people using antidepressants — it's called breakthrough depression.

Is Sertraline a powerful drug?

Sertraline are powerful prescription medications used to treat depression and other issues. They're both Sertraline-name drugs. The generic version of Sertraline is fluoxetine, while the generic version of Sertraline is sertraline hydrochloride. Both drugs are selective serotonin reuptake inhibitors (SSRIs).

Can Sertraline cause memory loss?

Most common side effects are agitation, hallucinations, fever, overactive reflexes, tremors; nausea, vomiting, loss of appetite, feeling unsteady, loss of coordination; trouble concentrating, memory problems, weakness, fainting, seizure, shallow breathing, or breathing that stops.

Does Sertraline really work?

Studies show that Sertraline is an effective treatment for social anxiety disorder. In a 2006 study, researchers found that Sertraline performed significantly better than a non-therapeutic placebo in reducing social anxiety symptoms.

What happens if I suddenly stop taking sertraline?

Stopping Sertraline abruptly may result in one or more of the following withdrawal symptoms: irritability, nausea, feeling dizzy, vomiting, nightmares, headache, and/or paresthesias (prickling, tingling sensation on the skin). Depression is also a part of bipolar illness.

How can I reduce the side effects of Sertraline?

Consider these strategies:

  • Take a brief nap during the day.
  • Get some physical activity, such as walking.
  • Avoid driving or operating dangerous machinery until the fatigue passes.
  • Take your antidepressant at bedtime if your doctor approves.
  • Talk to your doctor to see if adjusting your dose will help.

Can I take Sertraline during pregnancy?

Generally, these antidepressants are an option during pregnancy: Certain selective serotonin reuptake inhibitors (SSRIs). SSRIs are generally considered an option during pregnancy, including citalopram (Celexa) and sertraline (Sertraline). Potential complications include maternal weight changes and premature birth.

Can Sertraline give me night sweats?

Antidepressants are a common medication that can lead to night sweats with as many as 22% of people taking antidepressants reporting night sweats as a side effect (especially Sertraline and venlafaxine).

What does Sertraline treat?

Sertraline is a type of antidepressant known as a selective serotonin reuptake inhibitor (SSRI). It's often used to treat depression, and also sometimes panic attacks, obsessive compulsive disorder (OCD) and post-traumatic stress disorder (PTSD).

Why should not take Sertraline on a night?

Many people who experience nausea and other side effects from Sertraline opt to take it at night in order to limit these side effects. Since Sertraline can interfere with sleep in a small percentage of users, many people also opt to take Sertraline in the morning.

What are long term side effects of Sertraline?

Possible side effects include:

  • Dry mouth.
  • Constipation.
  • Weight gain or loss.
  • Bladder problems.
  • Sexual problems.
  • Blurred vision.
  • Drowsiness.
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