Stanil
Generic composition: Sertraline HCl
General description
Sertraline is a popular antidepressant medication commonly known as a selective serotonin reuptake inhibitor (SSRI). Sertraline displays enhanced safety or tolerability than other classes of antidepressants, which frequently cause high levels of drowsiness, dizziness, blurred vision, and other undesirable effects.
Therapeutic group
- SSRIs Anti-depressants
Dosage forms available
- STANIL 25mg Tablets
- STANIL 50mg Tablets
Uses
- Major Depressive Disorder
- Post-traumatic Stress Disorder
- Obsessive-compulsive Disorder
- Panic Disorder
- Premenstrual Dysphoric Disorder
- Social Anxiety Disorder
Dose
- Initial dose of 25mg to 50mg per day
- For adults and pediatric patients, subsequent dosages may be increased in case of an inadequate response in 25 to 50 mg per day increments once a week, depending on tolerability, up to a maximum of 200 mg per day.
Mechanism of action
Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, thereby increasing serotonergic activity. These results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. These changes are believed to be responsible for the antidepressant action and beneficial effects in obsessive-compulsive (and other anxiety related disorders).
Pharmacokinetics
- Absorption: mean peak plasma concentrations occurred between 4.5 to 8.4 hours after administration, and measured at 20 to 55 μg/L, highly protein bound;about 98%-99%.
- Distribution: widely distributed, and its volume of distribution is estimated to be more than 20L/kg.
- Metabolism: heavily metabolized in the liver and has one major active metabolite. It undergoes N-demethylation to form N-desmethylsertraline, which is much less potent in its pharmacological activity than sertraline
- Elimination: excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces
- Half-life: elimination half-life of sertraline is approximately 26 hours
Side effects
- Ejaculation failure, dry mouth, increased sweating, somnolence, dizziness, tremor, diarrhea, nausea, insomnia, fatigue, palpitations, weight loss.
- Rare: Menstrual irregularities, erythema multiforme and pancreatitis.
Contraindication
- Use with MAO Inhibitors
- With known hypersensitivity to sertraline and its excipients
- Taking pimozide
Drug Interaction
- The concomitant use of SSRIs with MAOIs increases the risk of serotonin syndrome; eg isocarboxazid, phenelzine, linezolid,
- Increased plasma concentrations of pimozide, a drug with a narrow therapeutic index, may increase the risk of QTc prolongation and ventricular
- The concomitant with another drug that is highly bound to plasma protein may increase free concentrations of sertraline or other tightly-bound drugs in plasma eg: Warfarin
- The concurrent use of an antiplatelet agent or anti-coagulant with ZOLOFT may potentiate the risk of bleeding. Eg aspirin, warfirin.
- Use with phenytoin increases concentration of phenytoin.
- Drugs metabolized by CYP2D6 like: flecainide, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, thoridazine, tolterodine, venlafaxine, propafenone as sertraline is CYP2D6 inhibitor
Precautions
- Not approved for bipolar depression. May precipitate mixed/manic episode in patients at risk for bipolar disorder.
- Less frequent dosing or reduced dose is recommended in hepatic impairment patients. While, no such caution is indicated for renal impairment. Gradual dose reduction recommended.
- Category C drug for Pregnancy. Caution during 3rd trimester of pregnancy due to risk of neonatal complications.
