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| SERTRALINE-HAKIM |
| :: Antidepressant :: |
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 Tab. 50, 100 mg |
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Pharmacologic category
Antidepressant(selective serotonin reuptake inhibitor); Antiobsessional agent; Antipanic agent.
Mechanism of action
Sertraline is a potent and selective inhibitor of neuronal uptake of serotonin (5 – HT) . It has only weak effects on neuronal uptake of norepinephrine and dopamine . Sertraline’s inhibition of serotonin reuptake enhances serotonergic transmission , which results in subsequent inhibition of adrenergic activity in the locus seruleus. Specifically, sertraline depresses the firing of the raphe serotonin neurons ; this , in turn , increases the activity of the locus ceruleus.
Indications
Treatment of major depression; obsessive- compulsive disorder (OCD); panic disorder with or without agoraphobia; post- traumatic stress disorder (PTSD); premenstrual dysphoric disorder (PMDD); social anxiety disorder
Side/Adverse effects
a-Those indicating need for medical attention: Sexual dysfunction (decreased libido, impotence, delayed ejaculation, or anorgasmia); Abnormal bleeding; Akathisia; Breast tenderness or enlargement; Galactorrhea; Extrapyramidal effects,dystonic; Fever;Hyponatremia; Mania or hypomania; Palpitation; Serotonin syndrome(diarrhea , fever ,increased sweating , mood or behavior changes ,overactive reflexes,racing heartbeat , restlessness , shivering or shaking); Skin rash, hives, or itching.
b-Those indicating need for medical attention only if they continue or are bothersome: Dizziness; Drowsiness; Gastrointestinal effects including anorexia, diarrhea, dryness of mouth, nausea, abdominal cramps; Weight loss; Headache; Increased sweating; Insomnia; Tiredness or weakness; Tremor; Agitation; Blurred vision; Constipation; Flushing; Increased appetite; Vomiting; Yawning .
c–Those indicating the need for medical attention if they occur after medication is discontinued: Agitation; Anxiety; Dizziness; Gait instability; Headache; Increased sweating; Insomnia; Nausea; Tremor; Unusual tiredness; Vertigo .
Contraindications
Hypersensitivity to sertraline or any component of the formulation; Use of MAO inhibitors within 14 days; Concurrent use of pimozide .
Warnings / Precautions
Potential for severe reaction when used with MAO inhibitors . May worsen psychosis in some patients.May precipitate a shift to mania or hypomania in patients with bipolar disorder. Monotherapy in patients with bipolar disorder should be avoided. Monitor for worsening of depression or suicidality, especially during initiation of therapy or with dose increases or decreases. Use caution in patients with a previous seizure disorder or condition predisposing to seizures such as brain damage, alcoholism, or concurrent therapy with other drugs which lower the seizure threshold. Use with caution in patients with hepatic or renal dysfunction and in elderly patients. Sertraline acts as a mild uricosuric; use with caution in patients at risk of uric acid nephropathy. Use with caution in patients at risk of bleeding or receiving anticoagulant therapy ; may cause impairment in platelet aggregation.
Pregnancy
FDA pregnancy category D. Oxazepam crosses the placenta and has been reported to increase the risk of congenital malformations when used during the first trimester of pregnancy . Therefore, oxazepam should be avoided during pregnancy , especially during the first trimester.
Breast–Feeding
FDA pregnancy category C. Use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus. If treatment during pregnancy is required, consider tapering therapy during the third trimester.
Drug Interactions
Sertraline inhibits cytochrome P450 and a potential exists for clinically significant interactions with medications that are metabolized by this enzyme, particularly medications having a narrow therapeutic index , such as tricyclic antidepressants and the type 1C antiarrhythmics propafenone and flecainide . A lower dosage of these medications may be needed when they are used concomitantly with sertraline. Concomitant use with alcohol is not recommended. Sertraline may inhibit the metabolism of tricyclic antidepressants (TCAs); TCA plasma concentration monitoring and dosage adjustments of the TCA and / or sertraline may be necessary. Because of increasing the risk of cardiac arrhythmias, concurrent use with astemizole and terfenadine is not recommended. Concurrent use with cimetidine results in an increase in mean half-life of sertraline; monitoring of serum cimetidine concentration is recommended. Sertraline may inhibit the metabolism of alprazolam and diazepam; monitor for increased sedation and psychomotor impairment. Sertraline may increase the hypoprothrombinemic response to warfarin; prothrombin time should be carefully monitored when sertraline therapy is initiated or stopped in patients taking warfarin. Sertraline may increase the risk of adverse effects of digitoxin. If combination of lithium with sertraline is used, close monitoring of lithium concentrations is recommended. Concomitant use of MAO inhibitors, including furazolidone , procarbazine and selegiline is contraindicated; a wash- out period of at least 14 days should elapse between discontinuation of either medication and initiation of the other. Serotonergics increase the risk of developing the serotonin syndrome. Sertraline may decrease the metabolism of tolbutamide; monitor for changes in glucose control. Concurrent use with pimozide is contraindicated.
Monitoring Parameters
Monitor nutritional intake and weight ; mental status for depression , suicidal ideation , anxiety , social functioning , mania , panic attacks , or unusual changes in behavior ; akathisia ; growth in pediatric patients.
Dietary Considerations
Sertraline may be taken with or without food. Some clinicians advise their patients to take this medication with food to lessen gastrointestinal side effects.
Administration and dosage
- Usual adult dose: Depression or obsessive – compulsive disorder - Oral, initially 50 mg a day as a single morning or evening dose . The dosage may be increased after several weeks in increments of 50 mg , with increases made at intervals of at least one week , as needed and tolerated.
Note: Some clinicians recommend an initial dosage of 25mg a day for one to two days.
Panic disorder or posttraumatic stress disorder – Oral , initially 25 mg a day , as a single morning or evening dose . After one week , the dosage should be increased to 50 mg a day , as a single dose . Further dosage increases may be made in increments of 50 mg , at intervals of at least one week , as needed and tolerated .
Premenstrual dysphoric disorder – Oral , 50 mg a day either throughout menstrual cycle or limited to the luteal phase . Patients not responding to 50 mg a day may benefit from dose increases (50 mg increments per menstrual cycle) up to 150 mg a day when dosing throughout menstrual cycle or up to 100 mg a day when dosing during luteal phase only.
- Usual adult prescribing limits: 200 mg a day.
- Usual pediatric dose: Depression or panic disorder or posttraumatic stress disorder – Safety and efficacy have not been established.
Obsessive – compulsive disorder –
Children 6 to 12 years of age : Oral , initially 25 mg a day as a single morning or evening dose . Dosage may be increased at intervals of at least one week , as needed and tolerated .
Children 13 to 17 years of age : Oral , initially 50 mg a day as a single morning or evening dose . Dosage may be increased at intervals of at least one week , as needed and tolerated.
- Usual geriatric dose: Oral , initially 12.5 to 25 mg a day , as a single morning or evening dose ; dosage may be increased gradually as needed and tolerated .
How Supplied
Tablet 50 mg and 100 mg.
Storage
Store below 40°C, preferably between 15 and 30°C .
References
- USP DI, 2004
- Up To Date, Vol. 13.3 (2005)
- Martindale, The Complete Drug Reference, 34 rd edition 2005
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