Sertraline: Basic Facts

 

   

Sertraline

BASIC-DESCRIPTION Brand Name
  • Zoloft
FDA Indications
    • MDD

 

    • OCD (> 6yr)

 

    • Panic disorder

 

    • Social Anxiety

 

    • PTSD

 

  • PMDD
PHARMACO-DYNAMICS Sertonin Reuptake Inhibition
  • Strong
Affinity for Serotonergic Receptors
  • None on 5HT1A, 5HT1B or 5HT2.
Norepinephrine Reuptake Inhibition
    • Weak.

 

  • Note:- Chronic treatment can down-regulate norepinephrine receptors in brain.
Dopamine Reuptake Inhibition
  • Weak
Affinity for  adrenergic (alpha1, alpha2, beta) receptors
  • None
Affinity for cholinergic or histaminergic receptors
  • None
PHARMACO-KINETICS Mean peak plasma concentrations (Cmax)
  • 4.5- 8.4 hours post dosing.
Terminal Elimination Half Life
  • 1d 2h (26 hours)
Time for Steady State Plasma Levels
  • ~1 week
Effect with Food
  • None
Metabolized to
  • N-desmethylsertraline (less active than sertraline)
DOSAGE Available Dose
  • 25, 50 & 100 mg tabs. Note: All are scored.
Liquid Form
    • Available in a multidose 60 mL bottle.

 

  • Each mL of solution ~ 20 mg of sertraline (20 mg/mL).
Dosage (Initiation)
    • Initiate at 50 mg daily X 1 week.

 

  • 25 mg daily for panic disorder, PTSD and Social Anxiety Disorder.
Dosage (Increase)
  • Increase on weekly basis by 25-50 mg/day basis.
Dosage (max)
  • 50-200 mg/day (higher doses may be needed for resistant OCD)
CO-MORBID MEDICAL CONDITIONS Renal Impairments
    • Recommendation (per package insert): No dosage adjustment necessary.

 

    • According to European Renal Best Practice: in Dialysis patient start at 25 mg daily and consider reducing max dose.

 

  • Minimal removal by hemodialysis.
Hepatic Impairments
    • Not studies in moderate and severe hepatic impairment.

 

  • Use lower or less frequent dose.
Cardiac Impairments
  • Considered safe in patients with recent history of myocardial infarction or unstable angina.
Abnormal Bleeding
    • Use with caution

 

    • At Risk Patient: with concomitant use of aspirin, nonsteroidal anti-inflammatory drugs, warfarin, and other anticoagulants

 

  • S/S: ranged from ecchymoses, hematomas, epistaxis, and petechiae to life-threatening hemorrhages.
Hyponatremia
    • Use with caution

 

    • Mostly result of SIADH

 

    • At risk patient: Elderly and patients taking diuretics or who are otherwise volume depleted

 

    • Discontinue sertraline with symptomatic hyponatremia.

 

  • S/S of hyponatremia include headache, difficulty concentrating, memory impairment, confusion, weakness, and unsteadiness, which may lead to falls.
Interference with Cognitive and Motor Performance
  • None noted
Seizures
  • No
PREGNANCY  
    • Comparatively safer

 

  • No evidence of teratogenicity at any dose
DRUG INTERACTIONS CYP450
    • Strong 2C9 Inhibitor

 

  • Strong 2D6 Inhibitor
  Interactions
  • Based on above CYP450 interactions
  False Positive UDS
  • Benzodiazepines

Please do post your questions or comments below. 


Dr. Harvinder Singh, M.D. (Admin)


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