Citalopram: Effects, Uses & Risks

Citalopram is used to treat depression, among other conditions. The active ingredient belongs to the group of selective serotonin reuptake inhibitors (SSRIs).

What is citalopram?

Citalopram is used to treat depression, among other conditions. The drug citalopram was developed by the Danish pharmaceutical company Lundbeck. It was patented in 1989, and the patent for the antidepressant expired in 2003, so there are now numerous generics on the market. Citalopram is the most frequently prescribed psychopharmacologically active preparation in Germany. The defined daily dose (DDD) is 338 million. Originally, the active ingredient was developed for the treatment of epilepsy. Quite quickly, however, it became apparent that citalopram could also be used to treat depression associated with emotional instability because of its mood-balancing effects.

Pharmacologic effects

Citalopram is a selective serotonin reuptake inhibitor. SSRIs act in the synaptic cleft. They inhibit the reuptake of the neurotransmitter serotonin (5-HT) into the presynapse. Serotonin is both a hormone and a neurotransmitter. The substance is found in the cardiovascular system and the central nervous system, among other places. Serotonin has a major influence on mood. Thus, the neurotransmitter conveys a feeling of contentment, serenity and inner peace. Serotonin dampens aggression, fears and sadness. It is suspected that a deficiency of serotonin or a deficiency of the serotonin precursor tryptophan is behind many depressions and anxiety disorders. Citalopram inhibits the reuptake of serotonin from the synaptic cleft into the presynapse. By allowing the available serotonin to remain in the synaptic cleft longer, the neurotransmitter’s effect is enhanced. However, the neurophysiological adaptation that initially occurs initially prevents the effect. The very high serotonin level in the synaptic cleft influences the autoreceptors of the presynapse. These serve as feedback sensors. They are activated by the high concentration of serotonin and convey the information to the cell that serotonin production must be throttled because there is too much serotonin. This initially causes another deficiency. However, as the receptor is permanently irritated by the SSRI, the body decreases the sensitivity of the autoreceptors. However, several weeks may pass before this process is completed. This is the reason why the antidepressant effect of citalopram often takes several weeks to appear.

Medical use and application

The main indication for citalopram is depression. In particular, citalopram is used for depression associated with emotional instability. These include, for example, bipolar disorder and borderline personality disorder. Bipolar disorder belongs to the affective disorders. Initially, the disorder was known as manic-depressive disorder. Borderline personality disorder is characterized primarily by impulsivity, unstable interpersonal relationships, moods, and a fragile self-image. However, when treating bipolar disorder, it is important to note that citalopram can trigger a manic phase. Furthermore, citalopram is used to treat obsessive-compulsive disorder. In this case, however, the drug must be dosed very high. The same applies to the treatment of panic disorders and post-traumatic stress disorder (PTSD) with citalopram. When treating depression, it should be noted that not all patients respond to citalopram. Symptoms improve in only about 50 to 75 percent of patients. In comparison, 25 to 33 percent respond to placebos. In mild depression, many comparative studies even found no difference in effect from placebos.

Risks and side effects

Adverse drug effects such as insomnia, nausea, a dry mouth, nervousness, headache, tremors, and profuse sweating often occur within the first few days after starting the drug. These side effects usually subside on their own after a few days. However, sexual dysfunction may occur. In particular, patients suffer from orgasm difficulties. However, these sexual dysfunctions are usually temporary and disappear after discontinuation of the drug. In rare cases, however, sexual dysfunction persists for months or years after citalopram is discontinued.This syndrome is also called Post SSRI Sexual Dysfunction. A very common side effect of citalopram is rhinitis (chronic rhinitis). In very rare cases, the so-called serotonin syndrome may develop. In particular, the risk of serotonin syndrome is greatly increased if other serotonergic drugs are taken at the same time. The syndrome is manifested by high fever, tremors, muscle twitching, confusion, and severe agitation. Therefore, citalopram should not be used with MAO inhibitors, tramadol, tryptophan, and the painkiller fentanyl. There are also interactions with St. John’s wort preparations. In addition, suicidal ideation is sometimes observed when citalopram is taken for the first time. In particular, citalopram appears to increase the risk of suicide in patients under 25 years of age. Although citalopram shows no dependence potential in the true sense, sudden discontinuation may lead to dizziness, nausea, sensory disturbances, anxiety, palpitations, increased sweating, and sleep disturbances. Citalopram should therefore always be discontinued gradually. During pregnancy, citalopram should be used only in exceptional cases. There are currently insufficient data to justify its use during pregnancy. However, sudden discontinuation of the drug during pregnancy should also be avoided. If citalopram was taken in the last trimester of pregnancy, the newborn should be monitored by a physician after birth. Withdrawal symptoms such as tremors, constant crying, constipation, muscle twitching, or diarrhea may be evident.