Selrotine

A white oblong, biconvex film-coated tablet engraved with "S" on one side and "
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" logo on the other.
Each tablet contains Sertraline HCl 55.953 mg equivalent to Sertraline 50 mg.

Pharmacology: Pharmacodynamics: Sertraline, a selective serotonin-reuptake inhibitor (SSRI) antidepressant agent, is a naphthalenamine-derivative. It has been shown to selectively inhibit the reuptake of serotonin at the presynaptic neuronal membrane. Sertraline-induced inhibition of serotonin reuptake causes increased synaptic concentrations of serotonin in the CNS. In animal studies, long-term administration of Sertraline has been shown to downregulate noradrenergic receptors in the CNS. Sertraline appears to have only very weak effects on the reuptake of norepinephrine or dopamine and does not possess clinically important affinity for adrenergic (α₁, α₂, β), histaminergic, muscarinic, GABA, benzodiazepine, or dopamine receptors.
In animal studies, Sertraline has effects on sleep cycle by suppressing rapid eye movement (REM) sleep stage. It possesses anorexigenic activity. Sertraline does not appear to cause clinically important sedation and does not interfere with psychomotor performance.
Pharmacokinetics: Sertraline appears to be slowly but well absorbed from the GI tract following oral administration. Administration of a single dose of Sertraline tablet with food increases peak plasma concentrations approximately 25% and decreases the time to achieve peak plasma concentrations from 8 to 5.5 hours, but such changes do not appear to be clinically important. Peak plasma Sertraline concentrations are proportional and linearly related to dose which usually occur within 4.5-8.4 hours following oral administration of 50-200 mg once daily for 14 days.
Following multiple dosing, steady state plasma Sertraline concentrations should be achieved after approximately a week of once-daily dosing. Plasma clearance was approximately 40% lower in elderly patients. Therefore, steady state should be achieved after 2 to 3 weeks in elder patients.
When compared with single dose, there is an approximate two-fold accumulation of Sertraline after multiple daily dosing in dosage ranging from 50-200 mg daily.
Sertraline is approximately 98% bound to plasma proteins. Sertraline undergoes extensive first-pass metabolism in the liver to its mainly metabolite, N-desmethylsertraline via N-demethylation. Data from in vivo and in vitro studies have shown that N-desmethylsertraline is approximately 5-10 times less potent as an inhibitor of serotonin reuptake than Sertraline. Both Sertraline and N-desmethylsertraline are widely distributed in body tissues. Sertraline crosses the blood-brain barrier in human. Both Sertraline and N-desmethylsertraline are distributed into milk.
The elimination half-life of Sertraline and N-desmethylsertraline are 26 hours and 62-104 hours, respectively.
Sertraline and its metabolites are excreted in about equal amounts, approximately 40-45% in both urine and feces (12-14% of unchanged Sertraline was excreted in feces).

Sertraline is an antidepressant agent used in treatment of following disorders: Major Depressive Disorder (MDD); Obsessive Compulsive Disorder (OCD); Panic Disorder with or without agoraphobia; Social Anxiety Disorder (SAD); Post-traumatic Stress Disorder (PTSD); Premenstrual Dysphoric Disorder (PMDD).

Sertraline should be administered once daily in the morning or evening at the same time every day. Sertraline can be administered with or without food. If somnolence is noted, Sertraline should be given at bedtime.
Patients receiving Sertraline should be monitored for possible worsening of depression, suicidality, or unusual changes in behavior, especially at the beginning of therapy or during periods of dosage adjustment.
Recommended dosage: Major Depressive Disorder (MDD): Adult: Initial treatment: 50 mg orally once daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Note: For the management of depressive symptoms associated with dementia of the Alzheimer's type in geriatric patients, recommended an initial Sertraline dosage of 12.5-25 mg once daily. The dosage may then be gradually increased at intervals of 1-2 weeks up to a maximum dosage of 150-200 mg once daily.
Obsessive Compulsive Disorder (OCD): Adult: Initial treatment: 50 mg orally once daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Children: Initial treatment: 6 to 12 years: 25 mg orally once daily or following doctor's instruction.
13 to 17 years: 50 mg orally once daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Note: Increases in doses, the lower body weights of children should be considered in order to avoid excessive doses.
Panic Disorder: Adult: Initial treatment: 25 mg orally once daily, increased after one week to 50 mg daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Social Anxiety Disorder (SAD): Adult: Initial treatment: 25 mg orally once daily, increased after one week to 50 mg daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Post-traumatic Stress Disorder (PTSD): Adult: Initial treatment: 25 mg orally once daily, increased after one week to 50 mg daily or following doctor's instruction.
Maintenance treatment: Dose may be increased, if necessary, in increments of 50 mg daily at intervals of at least a week to a maximum of 200 mg daily or following doctor's instruction.
Premenstrual Dysphoric Disorder (PMDD): Adult: Initial treatment: 50 mg orally once daily, either daily throughout the menstrual cycle or limited to the luteal phase of the menstrual cycle, depending on physician assessment.
Maintenance treatment: Dose may be increased, if necessary, by 50 mg each menstrual cycle up to maximum of 150 mg daily when dosing daily throughout the menstrual cycle or 100 mg daily when dosing during the luteal phase of menstrual cycle or following doctor's instruction.
Note: If a 100 mg daily dose has been established with luteal phase dosing, utilize a 50 mg daily titration step for 3 days at beginning of each luteal phase dosing period.
Discontinuation of Sertraline: Symptoms associated with discontinuation of Sertraline and other selective serotonin-reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs) have been reported. Monitor patients for these symptoms e.g. dysphoric mood, irritability, agitation, dizziness, sensory disturbances, anxiety, confusion, headache, lethargy, emotional lability, insomnia, and hypomania when discontinuing treatment. A gradual reduction in the dose rather than abrupt cessation is recommended whenever possible. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the health care provider may continue decreasing the dose but at a more gradual rate.
Switching patients to or from MAOIs: At least 14 days should elapse between discontinuation of a MAOI and initiation of therapy with Sertraline. In addition, allow at least 14 days after stopping Sertraline before starting a MAOI.
Dosage in pediatric patients: Safety and efficacy of Sertraline in children with Obsessive Compulsive Disorder (OCD) younger than 6 years of age have not been established. Safety and efficacy of Sertraline in children younger than 17 years of age with Panic Disorder, Social Anxiety Disorder (SAD), Post-traumatic Stress Disorder (PTSD), and Premenstrual Dysphoric Disorder (PMDD) have not been established.
If the drug is considered to be used in child or adolescent for any clinical use must balance the potential risk of therapy with the clinical need.
Dosage in geriatric patients: The efficacy or adverse effects in the elderly was similar to that in younger patients. However, plasma clearance of Sertraline may be decreased in geriatric patients.
Dosage in hepatic impairment: Sertraline should be administered with caution and in a reduced dosage or less frequently in patients with hepatic impairment.
Dosage in renal impairment: No need for dosage adjustment in patients with renal impairment. Because Sertraline does not appear to be removed substantially by dialysis, supplemental doses of the drug are probably unnecessary after dialysis.
Dosage in pregnancy and lactation: There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed.
Neonates exposed to SSRIs or serotonin-norepinephrine reuptake inhibitors (SNRIs) late in the third trimester have developed complications requiring prolonged hospitalization, respiratory support, and tube feeding. Such complications can arise immediately upon delivery. Reported clinical findings have included apnea, constant crying, cyanosis, feeding difficulty, hyperreflexia, hypertonia, hypoglycemia, hypotonia, irritability, jitteriness, respiratory distress, seizure, temperature instability, tremor, and vomiting. These features are consistent with either a direct toxic effect of SSRIs and SNRIs or, possibly, a drug discontinuation syndrome. It should be noted that, in some cases, the clinical picture is constant with serotonin syndrome. When treating a pregnant woman with SSRIs during the third trimester, the physician should carefully consider the potential risks and benefits of treatment.

Symptoms: Alopecia, decreased libido, diarrhea, ejaculation disorder, fatigue, insomnia, serotonin syndrome, and somnolence. The most common signs and symptoms associated with nonfatal Sertraline overdosage were agitation, dizziness, nausea, somnolence, tachycardia, tremor and vomiting.
Other important adverse events reported with Sertraline overdose (single or multiple drugs) include bradycardia, bundle branch block, coma, convulsion, delirium, hallucinations, hypertension, hypotension, manic reactions, pancreatitis, QT interval prolongation, serotonin syndrome, stupor and syncope.
Treatment: There are no specific antidote. Establish and maintain an airway; ensure adequate oxygenation and ventilation. Activated charcoal, which may be used with sorbitol, may be as or more effective than emesis or lavage.
Monitor cardiac and vital signs along with general symptomatic and supportive measures. SSRIs-induced seizures that fail to respond spontaneously may respond to diazepam.
Because of the large volume of distribution of SSRIs, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit.

Hypersensitivity to Sertraline or any component of the formulation.
Because of the potential risk of serotonin syndrome or NMS-like reactions, concomitant use of Sertraline and MAOIs is contraindicated. At least 2 weeks should elapse between discontinuance of MAOIs therapy and initiation of Sertraline therapy and vice versa.
Sertraline may increase serum concentration of pimozide; concurrent use is contraindicated.

Use of selective serotonin-reuptake inhibitors (SSRIs) such as Sertraline concurrently or in close succession with other drugs that affect serotonergic neurotransmission may result in serotonin syndrome or neuroleptic malignant syndrome (NMS)-like reaction. Symptoms of serotonin 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 GI symptoms (e.g. nausea, vomiting, diarrhea). Although the syndrome appears to be relatively uncommon and usually mild in severity, serious and potentially life-threatening complications, including seizures, disseminated intravascular coagulation, respiratory failure, and severe hyperthermia as well as death occasionally have been reported. In its most severe form, serotonin syndrome resembles NMS, which is characterized by hyperthermia, muscle rigidity, autonomic instability with possible rapid fluctuation in vital signs, and mental status changes.
If signs and symptoms of serotonin syndrome or NMS develop during therapy, treatment with Sertraline and any concurrently administered serotonergic or antidopaminergic agents, including antipsychotic agents, should be discontinued immediately. Supportive and symptomatic treatment should be initiated.
The effectiveness of long-term use of SSRIs for OCD, panic disorder, social anxiety disorder, PMDD, and PTSD has not been systematically evaluated. However, the long-term use of SSRIs for depression has been evaluated and demonstrated to maintain antidepressant response for up to 1 year. Periodically reevaluate the SSRIs used for extended periods to determine long-term usefulness of the drug for the individual patient.
In patients receiving a SSRI in combination with a MAOI, serious, sometimes fatal reactions have occurred, including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include confusion, irritability, extreme agitation progressing to delirium, and coma. These reactions also have occurred in patients who have recently discontinued a SSRI and have been started on a MAOI. Therefore, it is recommended that SSRIs not be used in combination with a MAOI or within 14 days of discontinuing treatment with a MAOI. Allow at least 2 weeks after stopping the SSRIs before starting a MAOI.
Patients with major depressive disorder, both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and suicidality. Nevertheless, closely observe patients being treated with antidepressant for clinical worsening and suicidality, especially at the beginning of the course of drug therapy or at the time of dose changes, either increases or decreases.
Alter platelet function and/or abnormal results from laboratory studies in patients taking Sertraline have occurred. There have been reports of abnormal bleeding or purpura in several patients. Caution patients regarding the risk of bleeding associated with the concomitant use of SSRIs with NSAIDs, aspirin, or other drugs that affect coagulation.
Significant weight loss, especially in underweight depressed patients, has occurred. Approximately 3% to 7% of patients treated with a SSRI initially experienced anorexia. However, after prolonged treatments, patients tend to gain weight. Monitor weight change during therapy.
Activation of mania/hypomania occurred infrequently in approximately 0.1% to 2.6% of patients taking SSRIs. Use cautiously in patients with a history of mania.
Sertraline has not been evaluated in patients with a seizure disorder. Use with care in patients with history of seizure; discontinue therapy if seizures occur.
Several cases of Sertraline-induced hyponatremia (some with serum sodium less than 110 mmol/L) have occurred. The hyponatremia appeared to be reversible when the drug was discontinued. Although these cases were complex with varying possible etiologies, some were possibly because of the syndrome of inappropriate antidiuretic hormone secretion (SIADH). The majority have been in elderly patients and in patients taking diuretics or who were otherwise volume-depleted.
Asymptomatic elevations in serum transaminase (AST or ALT) have occurred infrequently in association with Sertraline administration. These hepatic enzyme elevations usually occurred within the first 1 to 9 weeks of drug treatment and promptly diminished upon drug discontinuation. Sertraline therapy was associated with small mean increases in total cholesterol (approximately 3%) and triglycerides (approximately 5%) and a small mean decrease in serum uric acid (approximately 7%) of no apparent clinical importance.
Although SSRIs have not been shown to increase the impairment of mental and motor skills caused by alcohol, advise patients to avoid alcohol during therapy.

Cardiovascular: Edema, hypotension, peripheral ischemia, postural dizziness, aggravated hypertension, cerebrovascular disorder, MI, precordial/substernal chest pain, atrial arrhythmia, AV block, bradycardia, pulmonary hypertension, QT prolongation, ventricular tachycardia (including torsade de pointes).
Central nervous system: Abnormal coordination, abnormal gait, aggravated depression, aggressive reaction, ataxia, delusion, euphoria, headache, hallucination, hyperesthesia, leg cramps, migraine, nystagmus, paranoid reaction, paroniria, choreoathetosis, coma, dyskinesia, dysphonia, hyporeflexia, hypotonia, illusion, libido decreased, ptosis, somnambulism, suicidal ideation, withdrawal syndrome, extrapyramidal symptoms, neuroleptic malignant syndrome-like events, psychosis, serotonin syndrome.
Dermatologic: Alopecia, cold clammy skin, dry skin, erythematous rash, maculopapular rash, photosensitivity, urticaria, bullous eruption, contact dermatitis, dermatitis, eczema, hypertrichosis, follicular rash, pustular rash, skin discoloration, vasculitis, Stevens-Johnson syndrome.
Gastrointestinal: Eructation, esophagitis, increased saliva, teeth grinding, aphthous stomatitis, colitis, diverticulitis, fecal incontinence, gastritis, glossitis, gum hyperplasia, hemorrhagic peptic ulcer, hiccough, melena, proctitis, rectal hemorrhage, stomatitis, tenesmus, tongue edema/ulceration, ulcerative stomatitis.
Urogenital: Amenorrhea, dysmenorrheal, menorrhagia, intermenstrual bleeding, leucorrhea, vaginal hemorrhage, acute female mastitis, atrophic vaginitis, female breast pain, breast enlargement, dysuria, nocturia, polyuria, urinary incontinence, cystitis, oliguria, hematuria, pyelonephritis, renal pain, strangury, acute renal failure, gynecomastia, balanoposthitis, priapism.
Musculoskeletal: Arthrosis, dystonia, muscle cramps, muscle weakness.
Respiratory: Bronchospasm, epistaxis, apnea, bradypnea, hemoptysis, hyperventilation, hypoventilation, laryngismus, laryngitis, stridor.
Special senses: Conjunctivitis, xerophthalmia, eye pain, mydriasis, diplopia, photophobia, scotoma, visual field defect, blindness, optic neuritis, exophthalmos, glaucoma, cataract, abnormal accommodation, abnormal lacrimation, earache, hyperacusis, labyrinthine disorder.
Miscellaneous: Thirst, abnormal hepatic function, anemia, anterior chamber eye hemorrhage, facial edema, hypoglycemia, pallor, rigors, anaphylactoid reaction, angioedema, agranulocytosis, aplastic anemia, galactorrhea, hyperprolactinemia, hypothyroidism, increased coagulation time, leucopenia, lupus-like syndrome, oculogyric crisis, pancreatitis, pancytopenia, serum sickness, thrombocytopenia, liver events including elevated enzymes, increased bilirubin, hepatomegaly, hepatitis, jaundice, abdominal pain, vomiting, liver failure, and death.

Cytochrome P450 Effect: Substrate of CYP2B6 (minor), 2C9 (minor), 2C19 (major), 2D6 (major), 3A4 (minor); Inhibits CYP1A2 (weak), 2B6 (moderate), 2C8 (weak), 2C9 (weak), 2C19 (moderate), 2D6 (moderate), 3A4 (moderate).
Concomitant administration of Sertraline with other SSRIs or SNRIs potentially may result in Serotonin syndrome or NMS-like reactions and is therefore not recommended.
Sertraline should not be used with nonselective MAOIs (phenelzine, isocarboxazid) or other drugs with MAO inhibition (linezolid); fatal reactions have been reported. Wait 2 weeks after stopping a MAOI before starting Sertraline. Concurrent selegiline (a selective MAO-B inhibitor) has been associated with mania, hypertension, or serotonin syndrome (risk may be reduced relative to nonselective MAOIs).
Sertraline may increase serum concentrations of pimozide. Concomitant use of Sertraline and pimozide is contraindicated because of the low therapeutic index of pimozide and because the reported interaction between the 2 drugs occurred at a low dose of pimozide.
Sertraline may inhibit the metabolism of thioridazine or mesoridazine, resulting in increased plasma levels and increasing the risk of QT interval prolongation. This may lead to serious ventricular arrhythmias, such as torsade de pointes and sudden death. Do not use together. Wait at least 5 weeks after discontinuing Sertraline prior to starting thioridazine.
Sertraline may increase the levels/effects of amphetamines, selective beta-blockers, bupropion, selected benzodiazepines, calcium channel blockers, cisapride, cyclosporine, dextromethorphan, ergot alkaloids, fluoxetine, selected HMG-CoA reductase inhibitors, lidocaine, mesoridazine, mirtazapine, nateglinide, nefazodone, paroxetine, phenytoin, promethazine, propofol, risperidone, ritonavir, selegiline, sildenafil (and other PDE-5 inhibitors), tacrolimus, thioridazine, tricyclic antidepressants, venlafaxine, and other substrates of CYP2B6, 2D6 or 3A4.
Combined use of Sertraline and warfarin may increase the prothrombin time. In addition, prothrombin time should be monitored carefully whenever Sertraline therapy is initiated or discontinued in patients receiving anticoagulants.
The levels/effects of Sertraline may be increased by chlorpromazine, delavirdine, fluconazole, fluoxetine, fluvoxamine, gemfibrozil, isoniazid, miconazole, omeprazole, paroxetine, pergolide, quinidine, quinine, ritonavir, ropinirole, ticlopidine, and other CYP2C19 or 2D6 inhibitors.
Combined use of SSRIs and amphetamines, buspirone, meperidine, nefazodone, serotonin agonists (such as sumatriptan), sibutramine, other SSRIs/SNRIs, sympathomimetics, ritonavir, tramadol, and venlafaxine, may increase the risk of serotonin syndrome. Combined use of sumatriptan (and other serotonin agonists) may result in toxicity; weakness, hyperreflexia, and incoordination have been observed with sumatriptan and SSRIs. In addition, concurrent use may theoretically increase the risk of serotonin syndrome; includes sumatriptan, naratriptan, rizatriptan, and zolmitriptan.
In patients receiving lithium, plasma lithium concentrations should be monitored following initiation of Sertraline and lithium dosage should be adjusted accordingly. In addition, because of the potential risk of serotonin syndrome or NMS-like reactions, caution is advised during concurrent Sertraline and lithium use.
Risk of hyponatremia may increase with concurrent use of loop diuretics (bumetanide, furosemide, torsemide).
Concomitant use of Sertraline and NSAIDs, aspirin, or other drugs affecting coagulation has been associated with an increased risk of bleeding. Patients receiving Sertraline should be cautioned about the concomitant use of drugs that interfere with hemostasis.
The levels/effects of Sertraline may be decreased by aminoglutethimide, carbamazepine, phenytoin, rifampin, and other CYP2C19 inducers.
Sertraline may decrease the metabolism of tolbutamide; monitor for changes in glucose control.
Sertraline may decrease the levels/effects of CYP2D6 prodrug substrates (e.g. codeine, hydrocodone, oxycodone, tramadol).
Because SSRIs are highly bound to plasma protein, administration to a patient taking another drug that is highly protein-bound (e.g. warfarin, digoxin) may cause increased free concentrations of the other drug, potentially resulting in adverse events. Conversely, adverse effects could result from displacement of SSRIs by other highly bound drugs.
Combined use of Sertraline and St. John's wort (Hypericum perforatum) may cause increased sedative-hypnotic effects. Avoid concurrent use.

Store below 30°C.

Antipsychotics

N06AB06 - sertraline ; Belongs to the class of selective serotonin reuptake inhibitors. Used in the management of depression.

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