Zoloft

Generic Name: Sertraline hydrochloride

ZOLOFT contains sertraline hydrochloride, an SSRI. Sertraline hydrochloride has a molecular weight of 342.7 and has the following chemical name: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride. The empirical formula C17H17NCl2•HCl is represented by the following structural formula:

 

ZOLOFT (sertraline hydrochloride) tablets, for oral use ZOLOFT (sertraline hydrochloride) - Structural Formula Illustration

 

Sertraline hydrochloride is a white crystalline powder that is slightly soluble in water and isopropyl alcohol, and sparingly soluble in ethanol.

ZOLOFT tablets for oral administration contain 28.0 mg, 56.0 mg and 111.9 mg sertraline hydrochloride equivalent to 25, 50 and 100 mg of sertraline and the following inactive ingredients: dibasic calcium phosphate dihydrate, D & C Yellow #10 aluminum lake (in 25 mg tablet), FD & C Blue #1 aluminum lake (in 25 mg tablet), FD & C Red #40 aluminum lake (in 25 mg tablet), FD & C Blue #2 aluminum lake (in 50 mg tablet), hydroxypropyl cellulose, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate, synthetic yellow iron oxide (in 100 mg tablet), and titanium dioxide.

ZOLOFT oral solution are available in a multidose 60 mL bottle. Each mL of solution contains 22.4 mg sertraline hydrochloride equivalent to 20 mg of sertraline. The solution contains the following inactive ingredients: glycerin, alcohol (12%), menthol, butylated hydroxytoluene (BHT). The oral solution must be diluted prior to administration. The dispenser contains dry natural rubber.

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The mechanism of action of sertraline is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5HT). Studies at clinically relevant doses in man have demonstrated that sertraline blocks the uptake of serotonin into human platelets.

In vitro studies in animals also suggest that sertraline is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake.

In vitro studies have shown that sertraline has no significant affinity for adrenergic (alpha

1. alpha

2. (beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT 1A, 5HT 1B , 5HT 2), or benzodiazepinereceptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of sertraline was found in animals to down regulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Sertraline does not inhibit monoamine oxidase.


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

Depression

It is unclear if sertraline is any different than another SSRI paroxetine for depression.

Evidence does not show a benefit in children with depression.

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

Comparison with other antidepressants

Tricyclic antidepressants (TCAs) as a group are considered to work better than SSRIs for melancholic depression and in inpatients, but not necessarily for simply more severe depression. In line with this generalization, sertraline was no better than placebo in inpatients and as effective as the TCA clomipramine for severe depression. The comparative efficacy of sertraline and TCAs for melancholic depression has not been studied. A 1998 review suggested that, due to its pharmacology, sertraline may be more efficacious than other SSRIs and equal to TCAs for the treatment of melancholic depression.

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 unipolar MDD. Reboxetine was significantly worse.

Comparative clinical trials demonstrated that sertraline is similar in efficacy against depression to moclobemide, nefazodone, escitalopram, bupropion, citalopram, fluvoxamine, paroxetine, and mirtazapine. There is low quality evidence that sertraline is more efficacious for the treatment of depression than fluoxetine.

Elderly

Sertraline used for the treatment of depression in elderly (older than 60) patients was superior to placebo and comparable to another SSRI fluoxetine, and TCAs amitriptyline, nortriptyline (Pamelor) and imipramine. Sertraline had much lower rates of adverse effects than these TCAs, with the exception of nausea, which occurred more frequently with sertraline. In addition, sertraline appeared to be more effective than fluoxetine or nortriptyline in the older-than-70 subgroup. A 2003 trial of sertraline vs. placebo in elderly patients showed a statistically significant (that is, unlikely to occur by chance), but clinically very modest improvement in depression and no improvement in quality of life.

A meta-analysis on SSRIs and SNRIs that look at partial response (defined as at least a 50% reduction in depression score from baseline) found that sertraline, paroxetine and duloxetine were better than placebo. With respect to safety duloxetine and venlafaxine increased worsened dizziness, however not much safety data was reported.

Obsessive–compulsive disorder

Sertraline is effective for the treatment of OCD in adults and children. It was better tolerated and, based on intention to treat analysis, performed better than the gold standard of OCD treatment clomipramine. It is generally accepted that the sertraline dosages necessary for the effective treatment of OCD are higher than the usual dosage for depression. The onset of action is also slower for OCD than for depression.

Cognitive behavioral therapy alone was superior to sertraline in both adults and children; however, the best results were achieved using a combination of these treatments.

Panic disorder

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

Other anxiety disorders

Sertraline is effective for the treatment of social phobia. Improvement in scores on the Liebowitz Social Anxiety Scale were found with sertraline but not with placebo. A combination of sertraline and cognitive behavioural therapy has a superior response rate when used in children.

There is tentative evidence that sertraline, as well as other antidepressants, can help with the symptoms of general anxiety disorder. The trials have generally been short in length and the medicals are associated with side effects.

Premenstrual dysphoric disorder

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

Other indications

Sertraline when taken daily can be useful for the treatment of some aspects of premature ejaculation. A disadvantage of SSRIs is that they require continuous daily treatment to delay ejaculation significantly, and it is not clear how they affect psychological distress of those with the condition or the person's control over ejaculation timing.

The benefit of sertraline in PTSD is not significant per the National Institute of Clinical Excellence. Others, however, do feel that there is a benefit from its use.


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

Over more than six months of sertraline therapy for depression, people showed a nonsignificant weight increase of 0.1%. Similarly, a 30-month-long treatment with sertraline for OCD resulted in a mean weight gain of 1.5% (1 kg). Although the difference did not reach statistical significance, the 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. The incidence of diarrhea is higher with sertraline—especially when prescribed at higher doses—in comparison to other SSRIs.

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.

Sexual

Like other SSRIs, sertraline is associated with sexual side effects, including sexual arousal disorder and difficulty achieving orgasm. The frequency of sexual side effects depends on whether they are reported by people spontaneously, as in the manufacturer's trials, or actively solicited by physicians. While nefazodone, bupropion, and reboxetine do not have negative effects on sexual functioning, 67% of men on sertraline experienced ejaculation difficulties versus 18% before the treatment. 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.

Some people experience persistent sexual side effects after they stop taking SSRIs. This is known as Post-SSRI Sexual Dysfunction (PSSD). Common symptoms in these cases include genital anesthesia, erectile dysfunction, anhedonia, decreased libido, premature ejaculation, vaginal lubrication issues, and nipple insensitivity in women. Rates of PSSD are unknown, and there is no established treatment.

Suicide

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

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% or 50% 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". The more complete data submitted later by the sertraline manufacturer Pfizer indicated increased suicidal behavior. 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.

Concerns have been raised that suicidal acts among participants in multiple studies were not reported in published articles reporting the studies.

Discontinuation syndrome

Main article: Antidepressant discontinuation syndrome

Antidepressant discontinuation syndrome is a condition that can occur following the interruption, dose reduction, or discontinuation of antidepressant drugs, including sertraline. The symptoms can include flu-like symptoms and disturbances in sleep, senses, movement, mood, and thinking. 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.


Adult

Dosing Forms Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

oral concentrate

  • 20mg/mL

Major Depressive Disorder

Initial: 50 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Obsessive-Compulsive Disorder

Initial: 50 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Panic Disorder, Posttraumatic Stress Disorder

Initial: 25 mg PO qDay

May increase by 25 mg at 1-week intervals; not to exceed 200 mg qDay

Social Anxiety Disorder

Initial: 25 mg PO qDay

May increase by 25 mg at 1-week intervals not to exceed 200 mg qDay

Premenstrual Dysphoric Disorder

Initial: 50 mg qDay PO given continuously throughout menstrual cycle or given during luteal phase only

May increase by 50 mg at the onset of each new menstrual cycle; no more than 150 mg qDay when administered continuously or 100 mg qDay when administered during luteal phase only

Pruritus (Off-label)

25-100 mg daily for up to 5 years; 75-100 mg doses found to be most effective

Dosage Modifications

Renal impairment: Dose adjustment not necessary

Hepatic impairment

  • Mild (Child-Pugh 5-6): Decrease recommended starting dose and therapeutic dose by 50%
  • Moderate-to-severe (Child-Pugh 7-15): Not recommended; sertraline is extensively metabolized, and the effects in patients with moderate and severe hepatic impairment have not been studied

Pediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

oral concentrate

  • 20mg/mL

Obsessive-Compulsive Disorder

<6 years: Safety and efficacy not established

6-12 years: 25 mg PO qDay initially

12-17 years: 50 mg PO qDay initially

May increase by 50 mg qDay at 1-week intervals to no more than 200 mg qDay; give qHS if somnolence experienced

Dosage Modifications

Renal impairment: Dose adjustment not necessary

Hepatic impairment

  • Mild (Child-Pugh 5-6): Decrease recommended starting dose and therapeutic dose by 50%
  • Moderate-to-severe (Child-Pugh 7-15): Not recommended; sertraline is extensively metabolized, and the effects in patients with moderate and severe hepatic impairment have not been studied

Geriatric

The elderly are prone to SSRI/SNRI-induced hyponatremia; monitor closely

Major Depressive Disorder

25 mg PO qDay initially; may increase by 25 mg every 2-3 days; not to exceed 200 mg qDay

Alzheimer dementia related depression: Start at 12.5 mg/day and titrate every 1-2 weeks to response; not to exceed 150-200 mg

Dosage Modifications

Renal impairment: Dose adjustment not necessary

Mild hepatic impairment (Child 5-6years): Decrease recommended starting dose and therapeutic dose by 50%

Moderate-to-severe hepatic impairment (Child- 7-15years): Not recommended; sertraline is extensively metabolized, and the effects in patients with moderate and severe hepatic impairment have not been studied.

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. As with most other SSRIs its toxicity in overdose is considered relatively low.


Sertraline is a moderate inhibitor of CYP2D6 and CYP2B6 in vitro. 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. This effect is dose-dependent. 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. Sertraline is often used in combination with stimulant medication for the treatment of co-morbid depression and/or anxiety in ADHD. Amphetamine metabolism inhibits enzyme CYP2D6, but has not been known to interfere with Sertraline metabolism.

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

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

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.

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


If you take more Sertraline KR Tablets than you should

If you have taken too much medicine, always contact a physician, hospital or poison information centre.

If you forget to take Sertraline KR Tablets

Do not take a double dose to make up for a forgotten dose, but continue using the medicine by taking the next dose at its usual administration time.

If you stop taking Sertraline KR Tablets

Do not stop taking Sertraline KR Tablets without your doctor’s order. This medicine is discontinued slowly by gradually decreasing the dose according to the doctor’s instructions. If this medicine is stopped too quickly, the following symptoms may occur: dizziness, headache, nausea, restlessness and anxiety. The symptoms are usually mild and disappear automatically.


Before taking this medicine

You should not use Zoloft if you are allergic to sertraline, or if you also take pimozide. Do not use the liquid form of Zoloft if you are taking disulfiram (Antabuse) or you could have a severe reaction to the disulfiram.

Do not take Zoloft within 14 days before or 14 days after you take an MAO inhibitor. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine.

To make sure Zoloft is safe for you, tell your doctor if you have ever had:

  • heart disease, high blood pressure, or a stroke;

  • liver or kidney disease;

  • a seizure;

  • bleeding problems, or if you take warfarin (Coumadin, Jantoven);

  • bipolar disorder (manic depression); or

  • low levels of sodium in your blood.

Some medicines can interact with sertraline and cause a serious condition called serotonin syndrome. Be sure your doctor knows if you also take stimulant medicine, opioid medicine, herbal products, other antidepressants, or medicine for mental illness, Parkinson's disease, migraine headaches, serious infections, or prevention of nausea and vomiting. Ask your doctor before making any changes in how or when you take your medications.

Some young people have thoughts about suicide when first taking an antidepressant. Your doctor should check your progress at regular visits. Your family or other caregivers should also be alert to changes in your mood or symptoms.

Taking an SSRI antidepressant during pregnancy may cause serious lung problems or other complications in the baby. However, you may have a relapse of depression if you stop taking your antidepressant. Tell your doctor right away if you become pregnant. Do not start or stop taking Zoloft during pregnancy without your doctor's advice.

It is not known whether sertraline passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Do not give Zoloft to anyone younger than 18 years old without the advice of a doctor. Zoloft is FDA-approved for children with obsessive-compulsive disorder (OCD). It is not approved for treating depression in children.

How should I take Zoloft?

Take Zoloft exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Zoloft may be taken with or without food. Try to take the medicine at the same time each day.

The liquid (oral concentrate) form of Zoloft must be diluted before you take it. To be sure you get the correct dose, measure the liquid with the medicine dropper provided. Mix the dose with 4 ounces (one-half cup) of water, ginger ale, lemon/lime soda, lemonade, or orange juice. Do not use any other liquids to dilute the medicine. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.

Zoloft can cause you to have a false positive drug screening test. If you provide a urine sample for drug screening, tell the laboratory staff that you are taking Zoloft.

It may take up to 4 weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Do not stop using Zoloft suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using this medicine.

Store at room temperature away from moisture and heat.

 

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