CP-SERTRALINE 50

Indications

• Major depressive disorder
• Obsessive-compulsive disorder
• Panic disorder
• Social anxiety disorder
• Post-traumatic stress disorder
• Premenstrual dysphoric disorder

Dosage

Adults: Initially 50 mg daily, which may be

Mechanism of action

Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, leading to increased synaptic concentration of serotonin in the central nervous system. This enhancement in serotonergic neurotransmission is associated with its antidepressant effects. Chronic administration of sertraline has been shown to down-regulate norepinephrine receptors in the brain. It has a higher affinity for sigma-1 binding sites and exhibits weak inhibitory action on norepinephrine and dopamine uptake, without significant effects on monoamine oxidase activity.

Pharmacodynamics

Sertraline is effective in relieving symptoms of depression, obsessive-compulsive disorder, post-traumatic stress disorder, panic disorder, and premenstrual dysphoric disorder through serotonin reuptake inhibition. Clinical studies indicate that it can enhance cognitive function in patients with depression, and it has fewer sedative and cardiovascular effects compared to tricyclic antidepressants due to its lack of significant anticholinergic, antihistaminic, or adrenergic activity. The therapeutic effects typically become noticeable after 4-6 weeks of treatment.

Pharmacokinetics

Sertraline is well absorbed following oral administration, with peak plasma concentrations occurring approximately 4-6 hours after ingestion. It undergoes extensive hepatic metabolism, primarily via cytochrome P450 enzymes. The elimination half-life is about 24 hours, allowing for once-daily dosing. Sertraline is excreted mainly in the urine as metabolites, with only a small fraction excreted unchanged. Steady-state concentrations are generally achieved after about one week of consistent dosing.

Contra-indications

• Hypersensitivity to sertraline or any of its components
• Concomitant use with monoamine oxidase inhibitors (MAOIs)
• Use in patients with a history of seizures or epilepsy

Adverse effects

• Nausea
• Diarrhea
• Insomnia
• Dizziness
• Dry mouth
• Sexual dysfunction
• Increased sweating
• Fatigue
• Anxiety
• Tremors

Interactions

• Grapefruit juice may increase exposure to sertraline, leading to severe effects
• Caution with other serotonergic agents (risk of serotonin syndrome)
• May enhance effects of anticoagulants (e.g., warfarin)
• Possible interactions with other antidepressants

Precautions

• Monitor for worsening depression or emergence of suicidal thoughts
• Use with caution in patients with a history of bipolar disorder
• Careful in patients with liver impairment
• May cause withdrawal symptoms if discontinued abruptly

Pregnancy

Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult a healthcare provider.

Breast-feeding

Sertraline is excreted in breast milk. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Sertraline hydrochloride 25 mg tablets
• Sertraline hydrochloride 50 mg tablets
• Sertraline hydrochloride 100 mg tablets
• Sertraline hydrochloride 200 mg tablets

Mechanism of action

Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, thereby increasing serotonergic activity. This 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). It has been hypothesized that obsessive-compulsive disorder, like depression, is also caused by the disregulation of serotonin. In animal studies, chronic administration of sertraline results in down-regulation of brain norepinephrine receptors. Sertraline displays affinity for sigma-1 and 2 receptor binding sites, but binds with stronger affinity to sigma-1 binding sites. In vitro, sertraline shows little to no affinity for GABA, dopaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. It exerts weak inhibitory actions on the neuronal uptake of norepinephrine and dopamine and exhibits no inhibitory effects on the monoamine oxidase enzyme. Sertraline is a selective 5-HT reuptake inhibitor. It does not have cardiovascular, anticholinergic, antidopaminergic, convulsant, or monoamine oxidase-inhibiting effects. Most antidepressants are associated with either norepinephrine reuptake inhibition, 5-HT reuptake inhibition, & monoamine oxidase inhibition. Sertraline does not cause significant reuptake blockade of dopamine or norepinephrine. Sertraline through inhibition of 5-HT release, may cause beta-adrenoceptor downregulation.

Pharmacodynamics

Sertraline improves or relieves the symptoms of depression, OCD, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, and premenstrual dysphoric disorder via the inhibition of serotonin reuptake. Clinical studies have shown that it improves cognition in depressed patients. It has less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not exert significant anticholinergic, antihistamine, or adrenergic (alpha1, alpha2, beta) blocking activity. The onset of action and beneficial effects are usually noticed after 4-6 weeks, for reasons that are not fully understood and currently under investigation.