Sertraline

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Sertraline is one of a group of medicines called Selective Serotonin Reuptake Inhibitors (SSRIs); these medicines are used to treat depression and/or anxiety disorders.

Sertraline can be used to treat depression and to prevent recurrence of depression (in adults), panic disorder, Obsessive Compulsive Disorder (OCD), Social anxiety disorder and Post-Traumatic Stress Disorder (PTSD).

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Sertraline.jpg

[edit] MECHANISM OF ACTION

Low levels of serotonin in the central nervous system may be associated with depression.

Sertraline is a selective serotonin reuptake inhibitor (SSRI). It blocks the reuptake of serotonin into the presynaptic cell, increasing its level within the synaptic cleft. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs

[edit] INDICATIONS

  • Major depressive disorder: A major depressive episode implies a prominent and relatively persistent depressed or dysphoric mood that usually interferes with daily functioning (nearly every day for at least 2 weeks; it should include at least 4 of the following 8 symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest in usual activities or decrease in sexual drive, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and a suicide attempt or suicidal ideation
  • Social anxiety disorder: A marked and persistent fear of one or more social or performance situations in which the person is exposed to unfamiliar people or to possible scrutiny by others
  • Panic disorder: unexpected discrete period of intense fear or discomfort, symptoms can include palpitations, sweating, trembling, sensations of shortness of breath, chest pain or discomfort, nausea or abdominal distress, feeling dizzy and fear of dying
  • Obsessive compulsive disorder: Obsessive-compulsive disorder is characterized by recurrent and persistent ideas, thoughts, impulses, or images (obsessions) that are ego-dystonic and/or repetitive, purposeful, and intentional behaviors (compulsions) that are recognized by the person as excessive or unreasonable.
  • Premenstrual Dysphoric Disorder: depressed mood, anxiety or tension, affective lability, persistent anger or irritability, decreased interest in usual activities, difficulty concentrating, lack of energy and change in appetite or sleep
  • Posttraumatic stress disorder (PTSD)[1]

[edit] DOSAGE

Adult Dose:

  • Depression/OCD: 50mg/day and may increase up to max 200mg/day dose changes should not occur at intervals of less than 1 week
  • Panic disorder/PTSD= start with 25mg/day and increase to 50mg/day.

It may take up to 4-6 weeks to see full beneficial effects of sertraline

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Sertraline
  • It's use within 14 days of stopping an MAOI because of an increased risk of serotonin syndrome
  • Concomitant use with pimozide (Orap®) because this can cause serious heart problems (QT prolongation)
  • Do not start Sertraline in a patient who is being treated with linezolid or intravenous methylene blue

[edit] WARNINGS AND PRECAUTIONS

  • FDA Black Box Warning for Sertraline:

Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of Sertraline or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Sertraline is not approved for use in pediatric patients except for patients with obsessive compulsive disorder (OCD).

  • Bone Fractures: Epidemiological studies show an increased risk of bone fractures in patients receiving selective serotonin reuptake inhibitors (SSRIs) including sertraline.
  • Serotonin Syndrome: Serotonin syndrome has been reported with SSRIs and SNRIs, including Sertraline, both when taken alone, but especially when co-administered with other serotonergic agents (including Triptans, Tricyclic antidepressants, Fentanyl, Lithium, Tramadol, Tryptophan, Buspirone and St. John’s Wort) and with drugs that impair metabolism of serotonin (in particular, MAOI, both those intended to treat psychiatric disorders and also others, such as Linezolid and intravenous Methylene blue). Serotonin syndrome symptoms may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).If such symptoms occur, discontinue Sertraline and initiate supportive treatment. If concomitant use of Sertraline with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome, particularly during treatment initiation and dose increases
  • Weight Loss: Significant weight loss may be an undesirable result of treatment with sertraline for some patients
  • Abnormal Bleeding: May increase the risk of bleeding. Use with NSAIDs, Aspirin, Warfarin, or drugs that affect coagulation may potentiate the risk of gastrointestinal or other bleeding
  • Hyponatremia: Hyponatremia has been reported with Sertraline use, either alone or in combination with some diuretics (Hydrochlorothiazide, Furosemide). Hyponatremia appears to be the result of the syndrome of inappropriate antidiuretic hormone secretion (SIADH). Signs and symptoms include headache, new or increased seizure frequency, difficulty concentrating, memory impairment, confusion, weakness, and unsteadiness, which can lead to fall. Severe Hyponatremia may cause hallucination, syncope, seizure, coma, respiratory arrest, and death.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US) (There are no adequate and well-controlled studies in pregnant women, that's why, Sertaline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus)
  • It is not known if sertraline or its metabolites are excreted in human milk, caution should be exercised when Sertraline is administered to a nursing woman.

[edit] SIDE EFFECTS

Most frequently reported side effects are:

  • GI distress: Nausea, indigestion and diarrhea (major)
  • Nervousness
  • Insomnia
  • Decrease libido and ejaculatory disturbances
  • Headache, agitation, fatigue and sleep disturbances are associated with tapering or discontinuing Sertraline.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://www.ncbi.nlm.nih.gov/pubmed/17162624
  2. http://www.xagena.it/news/medicinenews_net_news/85ebad98d8a178be8baf16929526446e.html
  3. http://www.health-choices-for-life.com/medicinal_herbs.html
Antidepressants
Tricyclic antidepressants Amitriptyline (Elavil, Laroxyl)   Clomipramine (Anafranil)   Doxepin (Sinequan)   Imipramine (Tofranil)   Nortriptyline (Aventyl, Pamelor)   Trimipramine (Surmontil)
Selective serotonin reuptake inhibitors (SSRIs) Citalopram (Celexa, Seropram)   Escitalopram (Cipralex, Lexapro)   Fluoxetine (Prozac)   Fluvoxamine (Luvox, Maveral)   Paroxetine (Paxil, Seroxat)   Sertraline (Zoloft)
Serotonin–norepinephrine reuptake inhibitors (SNRIs) Desvenlafaxine (Pristiq)   Duloxetine (Cymbalta, Xeristar)   Venlafaxine (Efexor, Effexor)
Serotonin antagonists and reuptake inhibitors (SARIs) Trazodone (Desyrel, Oleptro)
Norepinephrine reuptake inhibitors (NRIs) Maprotiline (Ludiomil)   Reboxetine (Edronax)
Norepinephrine-dopamine reuptake inhibitors (NDRIs) Bupropion (Wellbutrin)
Noradrenergic and specific serotonergic antidepressants (NaSSAs) Mianserin (Lantanon)   Mirtazapine (Remeron)
Norepinephrine-dopamine disinhibitors (NDDIs) Agomelatine (Valdoxan, Thymanax)
Monoamine oxidase inhibitors Nonselective Tranylcypromine (Parnate)
Monoamine oxidase inhibitors B-Selective Selegiline (Transdermal) (Emsam)
Others 5-Hydroxytryptophan   S-Adenosyl methionine   Hypericum (St John's wort)