CITALOPRAM: PROPERTIES, SIDE EFFECTS AND INDICATIONS - ARTE - 2025

The citalopram is a known antidepressant drug that is part of the selective inhibitor drugs serotonin reuptake inhibitors (SSRIs). It is one of the substances most used to treat problems related to mood and depression.

Citalopram is marketed under brand names such as Celexa, Seropram, Talpram Prisdal Zanitus, or Cipramil. In this way, all these medicines refer to the same active substance, citalopram.

Citalopram is a medication indicated for the treatment of depression and the prevention of relapses, the treatment of panic disorder with or without agoraphobia, and the treatment of obsessive compulsive disorder.

Today this drug has enough evidence to be classified as a well-tolerated and effective antidepressant drug. For this reason, it is one of the most widely used medications to treat depression.

This article reviews the characteristics of citalopram. Its pharmacokinetic properties and its mode of action are explained, and possible adverse reactions, precautions and indications for this drug are postulated.

Characteristics and mechanism of action

Citalopram is an antidepressant medicine that belongs to the group of selective serotonin reuptake inhibitors (SSRIs).

Thus, it consists of a psychotropic drug that acts directly on the receptors for the neurotransmitter serotonin.

Serotonin is a highly important brain substance that performs a large number of functions. Among these, the regulation of the person's mood stands out.

Thus, the greater the amounts of serotonin in the brain, the higher the mood of the person. Instead, low levels of this substance in the brain are often associated with depressive episodes and depressed moods.

In this sense, citalopram is a drug that acts directly on the brain, inhibiting the reuptake of serotonin. By inhibiting its reuptake, the amounts of this substance are increased in the brain and the mood is increased.

The scientifically approved uses of citalopram are: symptoms of depression, social anxiety, panic disorder, obsessive-compulsive disorder, Huntington's disease, and premenstrual dysmorphic disorder.

However, in practice citalopram is frequently used to also intervene: anxiety problems, onychophagia, attention deficit hyperactivity disorder, eating disorders, alcoholism and different types of social phobia.

Indications and dosage

Treatment with citalopram must be specified by a medical professional, who must determine the appropriateness of the drug and the doses to be administered.

For this reason, before starting treatment with citalopram, the instructions for the administration of the drug indicated by the doctor who has received it must be followed exactly.

On the other hand, it should also be the medical professional who determines the duration of treatment with citalopram and the progressive period of drug reduction. It is important not to stop treatment abruptly or take doses other than those prescribed.

Although the doses and duration of treatment are procedures that the doctor must perform, citalopram presents a series of basic indications that can serve as a reference for users but not as a follow-up guideline. These are:

1- Depression

Depression is the main mental disorder for which the use of citalopram is indicated. The usual dose for the treatment of depression in adult subjects is 20 milligrams per day.

If deemed necessary, the doctor may decide to progressively increase said dose, up to a maximum of 40 milligrams per day.

2- Panic disorder

Panic disorder is another disorder for which the use of citalopram is indicated. In this case, the general doses of administration are lower, estimating an initial amount of 10 milligrams per day.

After one week of treatment, the medical professional may increase the dose to 20-30 milligrams per day. Only in specific cases, the administration of citalopram for the treatment of panic disorders reaches the maximum dose of 40 milligrams per day.

3-Obsessive compulsive disorder

The doses of citalopram indicated for the treatment of obsessive compulsive disorder are the same as for depression. The initial dose is usually 20 milligrams a day, which can be increased to a maximum of 40 milligrams a day.

Other uses of citalopram

The approved uses of citalopram are: treatment of symptoms of depression, social anxiety disorder, panic disorder, obsessive-compulsive disorder, Huntington's disease, and premenstrual dysmorphic disorder.

However, despite no scientific data on its efficacy, citalopram is also used to treat onychophagia, attention deficit hyperactivity disorder, body dysmorphic disorder, eating disorders, and alcoholism.

In this sense, certain pathologies seem to have a special relationship with citalopram, a fact that makes the effects of the drug in the treatment of these diseases a reason for study today. The most important ones are:

1- Alzheimer's

A study conducted in 2014 demonstrated that citalopram administered to mice largely (78%) stopped the growth of beta amyloid plaques, which cause the neuronal death typical of Alzheimer's disease.

The same study applied to a sample of 23 people showed that citalopram reduced the production of beta amyloid protein by 37%, which is why it is postulated that this drug could be beneficial in the treatment of Alzheimer's.

2- Diabetic neuropathy

Despite the lack of clinical data, citalopram has been used widely and with effective results to reduce the symptoms of diabetic neuropathy and premature ejaculation.

3- Prevention of migraine

Although citalopram is less effective than amitriptyline in preventing migraines, the combination of both drugs seems to show better results than the use of a single drug.

4- Autism

A multicenter randomized controlled study conducted in 2009 focused on examining the effects of citalopram in treating autism. The results found no benefit and showed some adverse effects, so the use of citalopram in the treatment of autism is in question.

Pharmacokinetic properties

Citalopram is a highly studied and vetted drug. For this reason, today there are firm data on its pharmacokinetic properties.

Research on the drug has made it possible to define the absorption, metabolism and elimination processes of citalopram.

1- Selectivity

Citalopram is considered the most selective serotonin reuptake inhibitor available today. Multiple in vitro studies have confirmed that the action of the drug in the brain is exclusively focused on the inhibition of serotonin reuptake.

In this sense, unlike other SSRI medications, citalopram minimally inhibits the reuptake of other substances such as adrenaline or dopamine.

Specifically, the data show that its constant inhibition rate for serotonin uptake is more than 3,000 times lower than that for norepinephrine uptake.

Thus, citalopram shows significantly greater efficacy than other drugs such as parxotine, sertraline, or fluoxetine in inhibiting this substance.

However, despite being the most selective drug, that is, it acts more specifically in the brain mechanisms that it must act, citalopram is not the most powerful antidepressant.

Paroxetine, for example, despite acting in a less selective way and, therefore, affecting other brain mechanisms not involved with depression, has been shown to be more potent in inhibiting serotonin reuptake, since its effects are more intense.

2- Absorption

Citalopram is a drug that is easily absorbed. Its absorption is not affected by food intake and shows an oral bioavailability of approximately 80%, The highest plasma levels of the substance are seen between two and four hours after its administration.

Citalopram is widely distributed in the different peripheral tissues and has a binding to plasma proteins of 80%. This means that it has a minimal probability of being involved in drug interactions that occur secondary to the displacement of a protein-binding drug.

At clinically relevant doses, citalopram has linear pharmacokinetics. That is, it presents a linear correlation between the dose and the stable concentration of the drug and its metabolites.

For all this, citalopram is considered today as one of the antidepressant drugs with the best absorption in the human body. The absorption and distribution process is not altered by other variables, so its effects are usually quite direct.

3- Metabolism

When citalopram is ingested, the drug substances pass into the blood until they reach the liver, where the drug is metabolized.

The liver metabolizes citalopram via two N-demethylation steps to dimethylcitalopram (DCT) via CYP2C19 and to didemethylcitalopram (DDCT) via CYP2D6.

The oxidation occurs by monoamine oxidase A and B, and aldehyde oxidase, to form a derivative of propionic acid and oxide-N-citalopram.

Through stable concentrations, the amount of metabolites relative to the drug citalopram is between 30 and 50% for DCT and between 5 and 10% for DDCT.

4- Elimination

Citalopram exhibits a biphasic elimination. The distribution phase in the body lasts about 10 hours and the half-life of the drug is between 30 and 35 hours.

Thus, citalopram is a drug that has a long life in the body, which is why it can be administered only once a day. Up to 23% of the drug is excreted in the urine.

5- Age-related pharmacokinetic effects

Studies that have looked at both single and multiple doses of citalopram in subjects over 65 years of age indicate that the drug's dose concentration increases 23-30% compared to younger individuals.

For this reason, it is recommended that elderly patients receive lower initial doses of citalopram, since the effect it has on their body is higher.

6- Hepatic dysfunction and pharmacokinetic effects

In subjects with hepatic impairment, the oral clearance of citalopram is reduced by 37%. Thus, the drug may pose a greater number of risks for this population, which is why the administration of low and controlled doses is recommended in individuals with liver failure.

7- Renal dysfunction and pharmacokinetic effects

In people with mild or moderate renal impairment, the clearance of citalopram is reduced by 17%. In these subjects, no dose adjustment is required, but it may be necessary to decrease the amount of medication in people with chronic or severe renal dysfunction.

Side effects

As with all medicines, the use of citalopram can cause various side effects. These tend to be of mild or moderate intensity, however, it is essential to notify the doctor whenever any of the effects are intense or do not disappear.

The main side effects that the use of citalopram can cause are:

1. Nausea and vomiting
2. Diarrhea and constipation
3. Stomach pain or heartburn
4. Decreased appetite and weight loss.
5. Frequent urge to urinate.
6. Excessive tired feelings.
7. General weakness
8. Uncontrollable shaking in some region of the body.
9. Pain in the muscles or joints.
10. Dry mouth
11. Changes or decrease in sexual desire and ability.
12. Heavy and excessive menstrual periods.
13. Chest pains
14. Shortness of breath.
15. Dizziness and lightheadedness
16. Increased heart rate.
17. Auditory or visual hallucinations.
18. High fever.
19. Excessive sweating
20. Confusion.
21. Loss of consciousness or coordination.
22. numbness of the muscles or jerky contractions.
23. Hives, blisters, or rash
24. Difficulty breathing or swallowing.
25. Swelling of the face, throat, tongue, lips, eyes, hands, or feet.
26. Unusual bleeding or bruising.
27. Headache and problems with concentration or memory.

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