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 hydrochloride belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs)used to treatment of depression, obsessive-compulsive disorder, panic disorder, PTSD, social anxiety disorder, and PMDD. Common side effects are dizziness, insomnia, nervousness, and sleepiness. Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity.
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. Sertraline has one active metabolite and, like the other SSRIs, have less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not have clinically important anticholinergic, antihistamine, or adrenergic blocking activity.
Indications of Sertraline
- Anxiety and stress
- Depression
- Major depressive disorder
- Bipolar disorder
- Social anxiety disorder
- Panic disorder
- Body dysmorphic disorder
- Borderline personality disorder
- Dissociative identity disorder
- Dysautonomia
- Generalized anxiety disorder
- Obsessive compulsive disorder
- Persistent depressive disorder
- Post traumatic stress disorder
- Postpartum depression
- Premenstrual dysphoric disorder
- Transverse myelitis
- Major depressive disorder
- Social anxiety 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
- closed angle glaucoma
- liver problems
- Bleeding from Stomach
- seizures
- weight loss
- risk of angle-closure glaucoma due to narrow angle of anterior chamber of eye
Dosages of Sertraline
Strengths: 50 mg; 100 mg; 20 mg/mL; 25 mg
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
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
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
Pediatric Dose for 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
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
- a light-headed feeling, like you might pass out;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Serious
- agitation
- anxiety
- behavioural changes, including aggressiveness, angry outbursts, bizarre behaviour, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- sleepwalking
Drug Interactions of Sertraline
Sertraline may interact with following drugs, supplements & may change the efficacy of drugs
- amlodipine
- general anesthetics
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- aripiprazole
- baclofen
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- bupropion
- celecoxib
- cilostazol
- clopidogrel
- cyclosporine
- diabetes medications (e.g., chlorpropamide, metformin, nateglinide, rosiglitazone)
- diltiazem
- estrogens (e.g., conjugated estrogen, )
- glucosamine
- heparin
- low molecular weight heparins
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, )
- multivitamins
- muscle relaxants
- nifedipine
- non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
- omega-3 fatty acids
- pentoxifylline
- propranolol
- quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
- rasagiline
- seizure medications ( phenobarbital, phenytoin, valproic acid, )
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- tapentadol
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, )
- thyroid replacements (e.g., desiccated thyroid, levothyroxine)
- tizanidine
- tramadol
- tricyclic antidepressants (e.g., desipramine, nortriptyline)
- triptans (e.g., sumatriptan, rizatriptan)
Pregnancy and Lactation of Sertraline
Pregnancy
There are no well-controlled studies in pregnant women. However, a substantial amount of data did not reveal evidence of induction of congenital malformations by sertraline. Animal studies showed evidence for effects on reproduction probably due to maternal toxicity caused by the pharmacodynamic action of the compound and/or direct pharmacodynamic action of the compound on the fetus. Sertraline is not recommended in pregnancy unless the clinical condition of the woman is such that the benefit of the treatment is expected to outweigh the potential risk.
Lactation
Data concerning sertraline levels in breast milk show that small quantities of sertraline and its metabolite N-desmethylsertraline are excreted in milk. Generally negligible to undetectable levels were found in infant serum, with one exception of an infant with serum levels about 50% of the maternal level (but without a noticeable health effect in this infant). Use in nursing mothers is not recommended unless, in the judgment of the physician, the benefit outweighs the risk.
References
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