An antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.
Brand name Celexa..
It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia.
Benefits may take one to four weeks to occur.
An oral agent.
US: C (Risk not ruled out)
Bioavailability 80%.
Metabolism by liver enzymes CYP3A4 and CYP2C19.
Elimination half-life 35 h.
Excretion mostly as unmetabolized citalopram.
Potent inhibitors of CYP2C19 and 3A4 might decrease clearance.
Approximately 80% is cleared by the liver and 20% by the kidneys.
Common side effects include nausea, trouble sleeping, sexual problems, shakiness, feeling tired, and sweating.
On those under the age of 25, serotonin syndrome, glaucoma, and QT prolongation and suicide are at increased risk.
Should not be used in someone on a MAO inhibitor.
Antidepressant discontinuation syndrome may occur.
Use during pregnancy may harm the baby.
In the National Institute for Health and Clinical Excellence ranking of 10 antidepressants for efficacy and cost-effectiveness it was fifth in effectiveness, after mirtazapine, escitalopram, venlafaxine, and sertraline.
Found to be more efficacious than paroxetine, and more acceptable than tricyclics, and venlafaxine, but less efficacious than escitalopram.
Evidence for effectiveness of citalopram for treating depression in children is uncertain.
Is fequently used off-label to treat anxiety, panic disorder, dysthymia, premenstrual dysphoric disorder, body dysmorphic disorder, and obsessive–compulsive disorder.
Effective in 85% of patients with generalized anxiety disorder, including some who had failed with other SSRIs.
Effective as fluvoxamine and paroxetine in obsessive–compulsive disorder.
Suggested effectiveness in resistant OCD, social anxiety disorder, aggressive and impulsive behavior, behavioral disturbances associated with dementia, hypersexuality in early Alzheimer’s disease, symptoms of premenstrual syndrome, reduction in alcoholic drink intake and increase in drink-free days in studies of alcoholics, possibly by decreasing desire or reducing the reward, reduce the symptoms of diabetic neuropathy, and treatment of hot flashes.
Typically taken in one dose, either in the morning or evening or without food.
Food can help prevent nausea.
Serotonin is absorbed by the 5HT3 receptors within the digestive tract, causing nausea.
The 5HT3 receptors stimulate vomiting.
It exhibits linear pharmacokinetics and minimal drug interaction potential, making it a better choice for the elderly or comorbid patients.
Common sexual side effects: difficulty becoming aroused, lack of interest in sex, and anorgasmia, however, when remission of major depressive disorder is achieved, quality of life and sexual satisfaction is reported to be higher in spite of sexual side effects.
Suspected that side effects are caused by increasing the concentration of serotonin in other parts of the body, such as in the intestines.
Increased apathy and emotional flattening, may be caused by the decrease in dopamine release associated with increased serotonin.
Has a mild antihistamine, which may be responsible for some of its sedating properties.
Common side effects include: drowsiness, insomnia, nausea, weight gain, increase in appetite, dreaming, frequent urination, decreased sex drive, anorgasmia, dry mouth, diaphoresis, trembling, diarrhea, excessive yawning, severe tinnitus, and fatigue.
Less common side effects include bruxism, vomiting, cardiac arrhythmia, blood pressure changes, dilated pupils, anxiety, mood swings, headache, and dizziness.
Rare side effects include convulsions, hallucinations, severe allergic reactions, nightmares, and photosensitivity.
If sedation occurs, the dose may be taken at bedtime rather than in the morning.
Associated with a higher risk of arrhythmia compared to other SSRIs.
Withdrawal symptoms include: paraesthesias, sleeping problems, dizziness , agitatation, anxiety, nausea, vomiting, tremors, confusion, sweating, headache, diarrhea, palpitations, changes in emotions, irritability, and eyesight problems.
The drug should be reduced gradually when treatment is finished.
Post-SSRI Sexual Dysfunction (PSSD) can occur: genital anesthesia, erectile dysfunction, anhedonia, decreased libido, premature ejaculation, vaginal lubrication issues, and nipple insensitivity in women.
Can cause dose-dependent QT interval prolongation, and should not be prescribed at doses greater than 40 mg per day, and restricted the maximum dose to 20 mg for subgroups of patients, including those older than 60 years and those taking an inhibitor of cytochrome P450.
As with other SSRIs, it can cause an increase in serum prolactin level.
Exposure in pregnancy is associated with shorter duration of gestation, increased risk of preterm delivery by 55%, lower birth weight, and lower Apgar scores, but is is not associated with an increased risk of spontaneous abortion.
Should not be taken with St John’s wort, tryptophan or 5-HTP as the resulting drug interaction could lead to serotonin syndrome.
Its use is contraindicated in individuals taking MAOIs, owing to a potential for serotonin syndrome.
It can increase the risk of bleeding, especially when coupled with aspirin, NSAIDs, warfarin, or other anticoagulants.
Taking it with omeprazole may cause higher blood levels of citalopram, and is a potentially dangerous interaction.
Associated with a SSRI discontinuation syndrome manifested by sensory, gastrointestinal symptoms, dizziness, lethargy, and sleep disturbances, as well as psychological symptoms such as anxiety/agitation, irritability, poor concentration, and shock-like sensations are typical for SSRI discontinuation.
Tapering off citalopram therapy, as opposed to abrupt discontinuation, is recommended.
Overdosage symptoms: vomiting, sedation, disturbances in heart rhythm, dizziness, sweating, nausea, tremor, and rarely amnesia, confusion, coma, or convulsions.
Overdose deaths have occurred.
It may be quantified in blood or plasma to confirm a diagnosis of poisoning or to assist in a medicolegal death investigation.
Blood or plasma citalopram concentrations are usually in a range of 50-400 μg/l in persons receiving the drug therapeutically, 1000–3000 μg/l in patients who survive acute overdosage and 3–30 mg/l in those who do not survive.
It is the most dangerous of SSRIs in overdose.
Carries a boxed warning stating it may increase suicidal thinking and behavior in those under age 24.
Its elimination is slower in the elderly and in patients with hepatic or renal failure.
With once-daily dosing, steady plasma concentrations are achieved in about a week.
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