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Sertraline is a member of the serotonin reuptake inhibitor class of antidepressants, which is used to treat depression, obsessive-compulsive disorder, panic disorder, social anxiety disorder, and post-traumatic stress disorder. Depression is a mood condition characterized by feelings of melancholy, difficulty sleeping, and a diminished quality of life. OCD is a mental disorder with symptoms such as excessive thoughts or ideas, leading to repetitive behaviors. Anxiety and unexpected sensations of terror when there is no real threat are associated with panic disorder. PTSD is a mental illness with symptoms resembling those of anxiety and depression that develop after going through an extremely emotional or distressing incident. Severe anxiety or difficulty in social settings is linked to social anxiety disorder. It functions by preventing released serotonin from being reabsorbed into the nerve cells. It elevates serotonin levels in the brain, linked to mood, behavior, and emotion regulation. Sertraline relieves melancholy, elevates mood, and eases the symptoms of anxiety, including panic and terror. Sertraline was FDA-approved in 1999.
BRAND NAMES
Zoloft: It contains the active ingredients of sertraline. It is available in the form of tablets, capsules, and oral solutions used to treat depression, OCD, panic disorder, SAD, PTSD, and PMDD.
MECHANISM OF ACTION
Sertraline improves serotonergic activity by selectively blocking serotonin reuptake at the presynaptic neuronal membrane. As a result, the CNS experiences an increase in synaptic serotonin concentration, which leads to a number of functional changes linked to enhanced serotonergic neurotransmission. It is believed that these alterations are what give obsessive-compulsive disorder its antidepressant qualities and beneficial effects. Similar to depression, obsessive-compulsive disorder is thought to be brought on by serotonin imbalance.
PHARMACOKINETICS
ABSORPTION
Absorption of sertraline is increased by food. After administration of sertraline, it reaches the peak plasma concentration of 4.5–4 hr.
DISTRIBUTION
Sertraline is broadly dispersed; its volume of distribution is 20 L/kg.
METABOLISM
Sertraline is extensively metabolized in the liver, with one primary active metabolite. It undergoes N-methylation to produce N-desmethyl sertraline, which has substantially lower pharmacological activity than sertraline.
EXCRETION
Sertraline is excreted through urine and feces.
PHARMACODYNAMICS
Sertraline reduces or alleviates symptoms of depression, OCD, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, and premenstrual dysphoric disorder by inhibiting serotonin reuptake. It enhances cognitive function in depressed patients. It has fewer sedative, anticholinergic, and cardiovascular effects than tricyclic antidepressants because it lacks considerable anticholinergic, antihistamine, or adrenergic-blocking activity.
DOSAGE AND ADMINISTRATION
For oral usage, sertraline comes in tablet and concentrate form. Usually taken in the morning or evening, it is taken once a day. Sertraline is taken once daily, either daily or on particular days of the month, to treat premenstrual dysphoric disorder.
- It is available in tablet form in dosages of 25 mg, 50 mg, and 100 mg.
- There are 150mg and 200mg tablet forms available.
- It can also be purchased in a millilitre dose of 200 mg.
DRUG INTERACTIONS
Drug interactions with sertraline may include
- Anti-Parkinson’s drugs: selegiline
- Anti-microbial: linezolid
- Anti-psychotic drugs: olanzapine
- Opioid pain killers: tramadol, fentanyl
- Opioid antagonist—naloxone
- Blood thinner—Warfarin
- MOA inhibitors for depression—methylene blue
- Antifungals: fluconazole, posaconazole, and ketoconazole
- Antibiotics: erythromycin, clarithromycin
- Anti-depressants: fluoxetine
- Anti-manic drugs: lithium
- Anticonvulsants: phenytoin, carbamazepine
- Pain killers: aspirin, ibuprofen
- Anti-diabetic drugs: tolbutamide
- Antacids: omeprazole, pantoprazole
CONTRAINDICATIONS
Sertraline is not recommended for those who have a documented hypersensitivity to Druf or any of its components. Sertraline should not be taken in combination with thioridazine, pimozide, or monoamine oxidase inhibitors such as linezolid or methylene blue. Sertraline solution is contraindicated with disulfiram because it contains 12% alcohol, which might trigger alcohol-disulfiram interactions.
SIDE EFFECTS
Side effects of sertraline may include
- Diarrhea
- Vomiting
- Nausea
- Heartburn
- Constipation
- Loss of appetite
- Dizziness
- Weight changes
- Headache
- Excessive tiredness
- Nervousness
- Dry mouth
- Excessive sweating
Serious side effects may include
- Rash
- Swelling
- Seizures
- Headache
- Selling
- Hives
- Agitation
- Confusion
- Weakness
- Difficulty breathing
OVERDOSE
Symptoms of overdose may include
- Seizures
- Excessive tiredness
- Drowsiness
- Agitation
- Fever
- Nausea
- Vomiting
- Irregular heartbeat
- Dizziness
TOXICITY
Sertraline overdose is often well tolerated. Sertraline poisoning can cause serotonin syndrome, which includes myoclonus, muscle rigidity, diaphoresis, tremor, hyperreflexia, agitated delirium, and hyperthermia. Serotonin syndrome is treated by quitting the medication and providing supportive care. Consider anti-emetics, benzodiazepines, and basic cooling methods to alleviate symptoms.
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