Sertraline; Uses, Dosage, Side Effects, Drug Interactions

Sertraline is a selective serotonin reuptake inhibitor (SSRI) used in the therapy of depression, anxiety disorders, and obsessive-compulsive disorder. Sertraline therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Sertraline is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is primarily used for the major depressive disorder, obsessive-compulsive disorder, panic disorder, and social anxiety disorder. Effectiveness is similar to other antidepressants. Sertraline is taken by mouth. Sertraline affects chemicals in the brain that may be unbalanced in people with depression, panic, anxiety, or obsessive-compulsive symptoms.

Mechanism of Action of Sertraline

The exact mechanism of action sertraline is not fully known, but the drug appears to selectively inhibit the reuptake of serotonin at the presynaptic membrane. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. It is suggested that these modifications are responsible for the antidepressant action observed during long term administration of antidepressants. It has also been hypothesized that obsessive-compulsive disorder is caused by the dysregulation of serotonin, as it is treated by sertraline, and the drug corrects this imbalance.As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D₂ or histamine H₁ receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT_1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT_1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission.

Indications of Sertraline

• Anxiety and stress
• Depression
• Social anxiety disorder
• Major depressive disorder
• Panic disorder
• Bipolar disorder
• Body dysmorphic disorder
• Borderline personality disorder
• Dissociative identity disorder
• Dysautonomia
• Persistent depressive disorder
• Post-traumaticc stress disorder
• Postpartum depression
• Premenstrual dysphoric disorder
• Somatoform pain disorder
• Transverse Myelitis
• Binge eating disorder
• Bulimia nervosa
• Generalized anxiety disorder
• Major depressive disorder
• Obsessive-compulsive disorder
• Post-traumatic stress disorder
• Premenstrual dysphoric disorder

Contra Indications of Sertraline

• Syndrome of inappropriate antidiuretic hormone secretion
• Low amount of sodium in the blood
• Increased risk of bleeding
• Behaving with excessive cheerfulness and activity
• Mild degree of mania
• Manic-depression
• Having thoughts of suicide
• Serotonin syndrome – adverse drug interaction
• Closed angle glaucoma
• Liver problems
• Bleeding from stomach
• Esophagus or duodenum
• Seizures
• Weight loss
• Risk of angle-closure glaucoma due to narrow angle of anterior chamber of eye

Dosage of Sertraline

Strengths: 25 mg;  50 mg; 100 mg; 20 mg/mL;

Depression

• Initial dose: 50 mg orally once a day
• Maintenance Dose: 50 to 200 mg orally once a day

Obsessive Compulsive Disorder

• Initial dose: 50 mg orally once a day
• Maintenance Dose: 50 to 200 mg orally once a day

Panic Disorder

• Initial dose: 25 mg orally once a day, increased after one week to 50 mg orally once a day
• Maintenance dose: 50 to 200 mg orally once a day

Post Traumatic Stress Disorder

• Initial dose: 25 mg orally once a day, increased after one week to 50 mg orally once a day
• Maintenance dose: 50 to 200 mg orally once a day

Social Anxiety Disorder

• Initial dose: 25 mg orally once a day, increased after one week to 50 mg orally once a day
• Maintenance dose: 50 to 200 mg orally once a day

Premenstrual Dysphoric Disorder

Continuous regimen

• Initial dose: 50 mg orally once a day during the menstrual cycle
• Maintenance dose: 50 to 150 mg orally once a day during the menstrual cycle

Cyclic regimen

• Initial dose: 50 mg orally once a day starting 14 days prior to the anticipated start of menstruation through to the first full day of menses, and repeated with each new cycle
• Maintenance dose: 50 to 100 mg orally once a day

Pediatric Obsessive Compulsive Disorder

6 to 12 years

• Initial dose: 25 mg orally once a day
• Maintenance dose: 25 to 200 mg orally once a day

13 to 17 years

• Initial dose: 50 mg orally once a day
• Maintenance dose: 50 to 200 mg orally once a day

Side Effects of Sertraline

The most common

• stomach or abdominal cramps, gas, or pain
• decreased sexual desire or ability
• Failure to discharge semen (in men)
• chest pain
• headache
• joint painPain
• dizziness
• nausea and vomiting
• Severe stomach ache
• epigastric pain,
• diarrhoea,
• anorexia,
• flatulence,
• headache,
• dizziness,
• fainting, fast or pounding heartbeats.

More common

• Fast or irregular heartbeat
• fever
• Back pain
• dizziness
• headache
• increased cough
• Acid or sour stomach
• decreased appetite
• Agitation
• chest congestion
• chest pain
• cold sweats
• confusion
• decreased sexual ability or desire
• diarrhea or loose stools
• heartburn
• sleepiness or unusual drowsiness
• trouble sleeping

Less common

• Abnormal dreams
• change in sense of taste
• congestion
• discouragement, feeling sad, or empty
• Suicide attempts
• Acting on dangerous impulses
• Aggressive or violent behavior
• Thoughts about suicide or dying
• New or worse depression
• New or worse anxiety or panic attacks
• Agitation, restlessness, anger, or irritability
• Trouble sleeping
• An increase in activity or talking more than normal

Drug Interactions of Sertraline

Sertraline may interact with following drugs, supplements & may decrease the efficacy of the drug

• antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine, quetiapine, risperidone)
• barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• beta-blockers (e.g., carvedilol, metoprolol, propranolol)
• bupropion
• captopril
• carvedilol
• celecoxib
• chloroquine
• cilostazol
• celecoxib
• clopidogrel
• dasatinib
• diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin, nateglinide, rosiglitazone)
• domperidone
• glucosamine
• heparin
• ketoconazole
• losartan
• low molecular weight heparins (e.g., dalteparin, enoxaparin, tinzaparin)
• macrolide antibiotics (e.g., clarithromycin, erythromycin)
• MAO inhibitors (e.g., linezolid, moclobemide, phenelzine, selegiline, )
• mirabegron
• multivitamins/minerals
• muscle relaxants (e.g., baclofen, cyclobenzaprine, methocarbamol, orphenadrine, tizanidine)
• metoprolol
• nonsteroidal anti-inflammatory medications (NSAIDs; diclofenac, ibuprofen, naproxen)
• omega-3 fatty acids
• pentoxifylline
• quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
• seizure medications (e.g., carbamazepine, clobazam,  felbamate, levetiracetam, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide)
• serotonin/norepinephrine reuptake inhibitors (SNRIs e.g., desvenlafaxine, duloxetine, venlafaxine)
• other selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, )
• 5-HT3 antagonists (e.g., granisetron, ondansetron)
• tamsulosin
• tapentadol
• thiazide diuretics (e.g., hydrochlorothiazide, indapamide)
• tramadol
• tricyclic antidepressants (e.g., nortriptyline, amitriptyline, imipramine, desipramine)
• tyrosine kinase inhbitors (e.g., imatinib, lapatinib, pazopanib, sunitinib)
• warfarin

Pregnancy & Lactation of Sertraline

FDA Pregnancy Category C 

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. There have been some reports that women taking SSRIs such as sertraline during the second half of pregnancy may be associated with lung disorders in newborns. Talk to your doctor if you have any concerns.

Breast-feeding

It is not known if sertraline passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

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