Citalopram: Properties, Side Effects and Indications

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

Citalopram is marketed under brands such as Celexa, Seropram, Talpram Prisdal Zanitus or Cipramil . In this way, all these medicines make reference to the same active principle, 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.

This drug has enough evidence today to be cataloged as a well tolerated and effective antidepressant medication. For this reason, it is one of the most used medications to treat depression.

Side Effects of Citalopram

In this article we review the characteristics of citalopram. Its pharmacokinetic properties and its mode of action are explained, and the possible adverse reactions, precautions and indications of this medicine are postulated.

side effects of citalopram

Characteristics and mechanism of action

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

Thus, it consists of a psychopharmaceutical that acts directly on the neurotransmitter receptors of serotonin.

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

Thus, the greater the amount of serotonin the brain possesses, the greater the mood of the person. In contrast, low levels of this substance in the brain, are often related to depressive episodes and mood decay.

In this sense, citalopram is a medication 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.

Scientifically approved uses of citalopram are symptoms of depression, social anxiety, the panic disorder, the obsessive-compulsive disorder, the disease of Huntington and premenstrual dysmorphic disorder.

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

Indications and doses

The treatment with citalopram must be specified by a medical professional, who must determine the adequacy of the medication and the doses that should be administered.

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

On the other hand, it must 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 different from those prescribed.

Although the doses and the duration of the treatment are procedures that the doctor must perform, citalopram presents a series of basic indications that can serve as a reference for the 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 a day.

If it deems it necessary, the doctor may decide to progressively increase this dose, until reaching a maximum of 40 milligrams per day.

2- Anguish disorder

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

After a week of treatment, the medical professional can increase the dose to 20 or 30 milligrams per day. Only in specific cases, the administration of citalopram for the treatment of distress 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 in the case of depression. The initial dose is usually 20 milligrams per day, and can be increased to a maximum of 40 milligrams per day.

Other uses of citalopram

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

However, despite not having scientific data about its effectiveness, citalopram is also used for the treatment of 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 subject of study today. The most important ones are:

1- Alzheimer’s

A study conducted in 2014 showed that citalopram administered in mice largely stopped (78%) the growth of beta-amyloid plaques, which cause 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 not having clinical data, citalopram has been used extensively and with effective results to reduce the symptoms of diabetic neuropathy and premature ejaculation.

3- Migraine prevention

Although citalopram is less effective than amitriptyline in the prevention of 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 the treatment of autism. The results found no benefits 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 examined medication. For this reason, firm data are now available about its pharmacokinetic properties.

The investigations on the drug have allowed to delimit the processes of absorption, metabolism and elimination of citalopram.

1- Selectivity

Citalopram is considered the most selective inhibitor of serotonin reuptake available today. Multiple in vitro studies have confirmed that the action of the drug in the brain focuses exclusively 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 rate of constant inhibition for serotonin uptake is more than 3,000 times lower than that of noradrenaline uptake .

Thus, citalopram shows a significantly higher efficacy than other drugs such as parxotin, sertraline and fluoxetine in the inhibition of this substance.

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

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

2- Absorption

Citalopram is a medicine 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 present between two and four hours after administration.

Citalopram is widely distributed by different peripheral tissues and has a plasma protein binding 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 a 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 medications with better absorption in the human body. The process of absorption and distribution is not altered by other variables, so its effects are usually quite direct.

3- Metabolism

When citalopram is ingested, the drug’s substances pass into the blood to reach the liver, where the drug is metabolized.

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

The oxidation is produced 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 in relation to the drug citalopram is between 30 and 50% for DCT and between 5 and 10% for DDCT.

4- Elimination

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

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

5- Pharmacokinetic effects related to age

Studies that have analyzed both single doses and multiple doses of citalopram in subjects over 65 indicate that the dose concentration of the drug increases between 23 and 30% compared to younger individuals.

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

6- Hepatic dysfunction and pharmacokinetic effects

In subjects with hepatic impairment, 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 in individuals with hepatic insufficiency is recommended.

7- Renal dysfunction and pharmacokinetic effects

In people with mild or moderate renal impairment, 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 medications, the use of citalopram can cause several adverse effects. These usually result from mild or moderate intensity, however, it is essential to notify the doctor whenever any of the effects is intense or does not disappear.

Also Read:The 4 Stages of Depression

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

  1. Nausea and vomiting.
  2. Diarrhea and constipation
  3. Stomach pain or heartburn.
  4. Decreased appetite and weight loss.
  5. Frequent urination.
  6. Excessive feelings of fatigue.
  7. Generalized weakness
  8. Uncontrollable trembling in some region of the body.
  9. Pains in muscles or joints.
  10. Dry mouth.
  11. Changes or decrease in sexual desire and ability.
  12. Abundant and excessive menstrual periods.
  13. Pains in the chest
  14. Lack of air
  15. Dizziness and fading.
  16. Increase in heart rate
  17. Auditory or visual hallucinations.
  18. High fever.
  19. Excessive sweating
  20. Confusion.
  21. Loss of knowledge or coordination.
  22. numbness of the muscles or spasmodic contractions.
  23. Urticaria, blisters or rash.
  24. Difficulty breathing or swallowing
  25. Inflammation 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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