Циталопрам: Антидепрессант из группы СИОЗС

SSRI antidepressant
the racemic form of the drug

Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. The antidepressant effects may take one to four weeks to occur. Common side effects include nausea, trouble sleeping, sexual problems, shakiness, feeling tired, and sweating. Citalopram was approved for medical use in the United States in 1998. It is available as a generic medication. In 2021, it was the 31st most commonly prescribed medication in the United States, with more than 18million prescriptions.

In the United States, citalopram is approved to treat major depressive disorder. Citalopram appears to have comparable efficacy and superior tolerability relative to other antidepressants. In the National Institute for Health and Clinical Excellence ranking of ten antidepressants for efficacy and cost effectiveness, citalopram is fifth in effectiveness (after mirtazapine, escitalopram, venlafaxine, and sertraline) and fourth in cost effectiveness. Evidence for effectiveness of citalopram for treating depression in children is uncertain.

Citalopram is licensed in the UK and other European countries for panic disorder, with or without agoraphobia.

Citalopram may be used off label to treat anxiety, and dysthymia, premenstrual dysphoric disorder, body dysmorphic disorder, and obsessive–compulsive disorder. It appears to be as effective as fluvoxamine and paroxetine in obsessive–compulsive disorder. Some data suggest the effectiveness of intravenous infusion of citalopram in resistant OCD. Citalopram is well tolerated and as effective as moclobemide in social anxiety disorder. There are studies suggesting that citalopram can be useful in reducing aggressive and impulsive behavior. It appears to be superior to placebo for behavioural disturbances associated with dementia. It has also been used successfully for hypersexuality in early Alzheimer's disease. A meta analysis, including studies with fluoxetine, paroxetine, sertraline, escitalopram, and citalopram versus placebo, showed SSRIs to be effective in reducing symptoms of premenstrual syndrome, whether taken continuously or just in the luteal phase. For alcoholism, citalopram has produced a modest reduction in alcoholic drink intake and increase in drink free days in studies of alcoholics, possibly by decreasing desire or reducing the reward. While on its own citalopram is less effective than amitriptyline in the prevention of migraines, in refractory cases, combination therapy may be more effective. Citalopram and other SSRIs can be used to treat hot flashes. A 2009 multisite randomized controlled study found no benefit and some adverse effects in autistic children from citalopram, raising doubts whether SSRIs are effective for treating repetitive behavior in children with autism. Some research suggests citalopram interacts with cannabinoid protein couplings in the rat brain, and this is put forward as a potential cause of some of the drug's antidepressant effect.

Citalopram is typically taken in one dose, either in the morning or evening. It can be taken with or without food. Its absorption does not increase when taken with food,

Citalopram theoretically causes side effects by increasing the concentration of serotonin in other parts of the body (e. g., the intestines). Other side effects, such as increased apathy and emotional flattening, may be caused by the decrease in dopamine release associated with increased serotonin. Citalopram is also a mild antihistamine, which may be responsible for some of its sedating properties. Citalopram is associated with a higher risk of arrhythmia than other SSRIs. Citalopram and other SSRIs can induce a mixed state, especially in those with undiagnosed bipolar disorder.

Sexual dysfunction is often a side effect with SSRIs. Some people experience persistent sexual side effects when taking SSRIs or after discontinuing them. Symptoms of medication induced sexual dysfunction from antidepressants include difficulty with orgasm, erection, or ejaculation.

In August 2011, the FDA announced, "Citalopram causes dose dependent QT interval prolongation. Citalopram should no longer be prescribed at doses greater than 40 mg per day". A further clarification, issued in March 2012, 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 2C19.7.

As with other SSRIs, citalopram can cause an increase in serum prolactin level. Citalopram has no significant effect on insulin sensitivity in women of reproductive age and no changes in glycaemic control were seen in another trial.

Antidepressant exposure (including citalopram) during pregnancy is associated with shorter duration of gestation (by three days), increased risk of preterm delivery (by 55%), lower birth weight (by 75 g), and lower Apgar scores (by <0.4 points). Antidepressant exposure is not associated with an increased risk of spontaneous abortion. It is uncertain whether there is an increased prevalence of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy.

Overdosage may result in vomiting, sedation, disturbances in heart rhythm, dizziness, sweating, nausea, tremor, and rarely amnesia, confusion, coma, or convulsions. It is the most dangerous of SSRIs in overdose.

In the United States, citalopram carries a boxed warning stating it may increase suicidal thinking and behavior in those under age 24. Electric shock like sensations are typical for SSRI discontinuation. Withdrawal symptoms can occur when this medicine is suddenly stopped, such as paraesthesiae, sleeping problems (difficulty sleeping and intense dreams), feeling dizzy, agitated or anxious, nausea, vomiting, tremors, confusion, sweating, headache, diarrhea, palpitations, changes in emotions, irritability, and eye or eyesight problems. Treatment with citalopram should be reduced gradually when treatment is finished.

Citalopram should not be taken with St John's wort, tryptophan or 5 HTP as the resulting drug interaction could lead to serotonin syndrome. With St John's wort, this may be caused by compounds in the plant extract reducing the efficacy of the hepatic cytochrome P450 enzymes that process citalopram. Tryptophan and 5 HTP are precursors to serotonin. When taken with an SSRI, such as citalopram, this can lead to levels of serotonin that can be lethal. This may also be the case when SSRIs are taken with SRAs (serotonin releasing agents) such as in the case of MDMA. It is possible that SSRIs could reduce the effects associated due to an SRA, since SSRIs stop the reuptake of Serotonin by blocking SERT. This would allow less serotonin in and out of the transporters, thus decreasing the likelihood of neurotoxic effects. However, these concerns are still disputed as the exact pharmacodynamic effects of citalopram and MDMA have yet to be fully identified. Citalopram is contraindicated in individuals taking MAOIs, owing to a potential for serotonin syndrome.

SSRIs, including citalopram, can increase the risk of bleeding, especially when coupled with aspirin, NSAIDs, warfarin, or other anticoagulants.

Citalopram was first synthesized in 1972 by chemist Klaus Bøgesø and his research group at the pharmaceutical company Lundbeck and was first marketed in 1989 in Denmark. It was first marketed in the US in 1998. The original patent expired in 2003, allowing other companies to legally produce and market generic versions.

On 19 June 2013, the European Commission imposed a fine of €93.8 million on the Danish pharmaceutical company Lundbeck, plus a total of €52.2 million on several generic pharmaceutical producing companies. This was in response to Lundbeck entering an agreement with the companies to delay their sales of generic citalopram after Lundbeck's patent on the drug had expired, thus reducing competition in breach of European antitrust law.

Citalopram is also a parasiticide. Schistosomula have high mortality when treated with citalopram.