Citalopram (Cipramil) - effect, application, side effect

Who is citalopram for?

Some indications for the use of citalopram: depression, panic disorder, chronic pain (idiopathic pain disorder, headache, neuropathic pain), etc.

A prescription for citalopram can be obtained from your doctor. Citalopram is contraindicated for the treatment of general anxiety disorder in people under 12 years of age.

In addition to depression, citalopram is also used to treat obsessive-compulsive disorder, panic disorder, and other types of disorders.

Citalopram is not sold in pharmacies without a prescription.

The antidepressant citalopram may also be used for purposes not listed here. The drug should be prescribed with caution to patients with chronic heart failure, myocardial infarction, coronary heart disease, conditions after a stroke, infectious diseases, diabetes mellitus, and children.

Drug interactions Citalopram

Taking citalopram simultaneously with MAO inhibitors can lead to the development of a hypertensive crisis (serotonin syndrome). Citalopram enhances the effect of sumatriptan and other serotonergic drugs. Cimetidine causes a moderate increase in the average steady-state concentration of citalopram in the blood plasma; this should be taken into account when prescribing these drugs in high doses simultaneously. There is no evidence of interaction of citalopram with lithium or alcohol, or clinically significant interaction of citalopram with phenothiazines or tricyclic antidepressants. Clinical studies have not established the interaction of citalopram with concomitantly prescribed benzodiazepines, neuroleptics, analgesics, lithium, antihistamines, antihypertensive drugs, beta-adrenergic receptor blockers and other drugs acting on the cardiovascular system.

How to use citalopram for depression: dose and frequency of use

It is advisable to take citalopram with food to reduce stomach upset. Instructions for using citalopram are in the box with the tablets, and instructions for citalopram are also available on the Internet in the public domain.

The doctor will usually start the adult on a low dosage initially for 1 week, then gradually increase the dosage over time if he or she feels it is needed.

The usual dose of citalopram is 20 mg per day in adults. But treatment can be started with a lower dose and increased to a maximum dose of 40 mg per day.

If you are over 65 years of age or have liver problems, the maximum recommended dose is 20 mg per day.

The usual dose of citalopram in children is 10 mg per day, but this can be increased to 40 mg per day.

Cancellation of citalopram should not occur abruptly; it is necessary to gradually reduce the dosage taken.

Reviews from those taking citalopram are usually positive; symptoms of depression are eliminated as much as possible with the correct dosage.

Pharmacological properties

Pharmacodynamics

Citalopram is an antidepressant. Belongs to the group of SSRIs (selective serotonin reuptake inhibitors). It has a pronounced property of suppressing the reuptake of serotonin, does not bind or binds very weakly to a number of receptors, including GABA (gamma-aminobutyric acid) receptors, m-cholinergic receptors, H1-histamine, D1- and D2-dopamine, α1 -, α2-, beta-adrenergic and benzodiazepine receptors. Thanks to this, such undesirable reactions as orthostatic hypotension, negative dromo-, chrono- and inotropic effects, sedation and xerostomia are almost completely absent.

It inhibits the CYP2D6 isoenzyme to a very small extent, and therefore citalopram has almost no interaction with drugs metabolized by this enzyme. Thanks to this, side reactions and toxic effects are manifested to a much lesser extent.

Typically, the antidepressant effect develops after 2–4 weeks of use.

Citalopram has no effect on serum levels of growth hormone and prolactin. It has virtually no sedative effect and does not impair intellectual, cognitive functions and psychomotor function.

When used in doses above 40 mg per day, citalopram may lead to abnormal changes in the electrical activity of the heart (prolongation of the QT interval on the ECG).

Pharmacokinetics

The bioavailability of citalopram is 80%, the indicator is practically independent of food intake. Cmax (maximum concentration of the substance) in plasma is achieved on average within 3 hours. Pharmacokinetic processes are linear, dose-dependent, both when taking single and multiple doses (in the range of daily doses from 10 to 60 mg). When taking citalopram once a day, Css (equilibrium concentration) in plasma is established after 1–2 weeks of therapy.

Vd (volume of distribution) is in the range of 12–17 l/kg. Plasma protein binding – up to 80%. It is found in plasma unchanged. Passes into breast milk.

Metabolized by demethylation, deamination and oxidation with the participation of cytochrome P450 (isoenzymes CYP2C19 and CYP3A4, and to a lesser extent CYP2D6). As a result, pharmacologically less active metabolites are formed. Inhibition of one of these enzymes can be compensated by other enzymes.

T1/2 (half-life) of citalopram is 36 hours. Excreted by the liver and kidneys (85% and 15%, respectively), 12–23% of the substance is excreted unchanged through the kidneys. Hepatic clearance is approximately 0.3 l/min, renal clearance is 0.05–0.08 l/min.

In patients over the age of 65 years, T1/2 is longer. Also, due to a decrease in metabolism, lower clearance values ​​are observed.

With reduced liver function, the elimination of citalopram is slower. T1/2 and equilibrium concentrations of the substance are almost two times higher compared to patients with unimpaired liver function.

The elimination of citalopram with mild to moderate degrees of decreased renal function proceeds more slowly without a significant effect on pharmacokinetic parameters. When creatinine clearance (creatinine clearance) is below 30 ml/min, the use of citalopram requires caution.

Can antidepressants cause addiction, and what are the side effects of citalopram?

Like all medicines, citalopram may cause side effects in some people, but many people have no or only minor side effects.

Some of the common side effects of citalopram will gradually improve as your body gets used to taking the antidepressant citalopram. Side effects like fatigue, dry mouth and sweat are common. They are usually standard and go away within a couple of weeks.

Some people who take citalopram for panic attacks find that their anxiety gets worse during the first few weeks of treatment.

This usually goes away after a few weeks, but talk to your doctor if it bothers you - a lower dose may help reduce your symptoms.

In adults and teenagers, some common side effects after taking citalopram include: dizziness, headache, insomnia, gastrointestinal upset, increased appetite, urinary retention.

Citalopram

Use in children and adolescents under 18 years of age

Antidepressants should not be prescribed to children and adolescents under 18 years of age. In clinical studies, children and adolescents taking antidepressants were more likely to experience suicidal behavior (suicide attempts and suicidal thoughts) and hostility (with a predominance of aggressive behavior, confrontational behavior, and irritation) than those in the placebo group.

When using drugs belonging to the SSRI therapeutic group, including citalopram, the following should be considered:

Paradoxical anxiety

Some patients with panic disorder may experience increased anxiety when starting antidepressant therapy. This paradoxical reaction usually resolves within the first two weeks after starting treatment. To reduce the likelihood of anxiogenic effects, low initial doses are recommended.

Hyponatremia

Rare cases of hyponatremia, apparently due to inadequate secretion of antidiuretic hormone (ADH), have been reported with the use of SSRIs. This reaction was generally reversible if treatment with the drug was discontinued. The risk was higher in older women.

Suicide/suicidal ideation or clinical worsening

Depression is associated with an increased risk of suicidal ideation, self-harm and suicide (suicidal events). This risk persists until stable remission develops.

Since improvement may not be observed during the first few weeks of treatment or even a longer period of time, patients should be closely monitored to ensure that such improvement is detected in a timely manner. Clinical experience shows that the risk of suicide increases in the early stages of recovery.

Other psychiatric disorders for which citalopram is prescribed may also be associated with an increased risk of suicidal events. In addition, these conditions may be a comorbidity in relation to a depressive episode. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with a depressive episode.

Patients with a history of suicidal tendencies or patients with a significant level of suicidal thoughts before treatment are at greater risk for suicidal ideation or suicide attempts and should be closely monitored during treatment.

A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders showed that there is an increased risk of suicidal behavior in patients under 25 years of age when taking antidepressants compared with placebo.

Drug treatment of these patients, and in particular those at high risk for suicide, should be accompanied by careful monitoring, especially early in treatment and during dose changes. Patients (and caregivers) should be warned to monitor for any signs of clinical worsening, suicidal behavior or ideation, or unusual changes in behavior, and to seek immediate medical advice if these symptoms occur.

Akathisia/psychomotor restlessness

The use of drugs from the SSRI/SNRI group is associated with the development of akathisia, characterized by a feeling of subjectively unpleasant or unbearable motor restlessness, restlessness and the need to move. Often patients in this condition cannot sit or stand quietly. Most often this condition occurs during the first weeks of treatment. In patients with such symptoms, increasing the dose may cause a sharp deterioration of the condition.

Mania

Patients with bipolar affective disorder may develop a manic phase. If a manic state develops, citalopram should be discontinued.

Seizures

There is a risk of seizures when taking antidepressants. In any patient who experiences a seizure, citalopram should be discontinued. Citalopram should not be used in patients with unstable epilepsy; Controlled seizures require careful monitoring. If the frequency of seizures increases, citalopram should be discontinued.

Diabetes

In patients with diabetes mellitus, the use of SSRIs may change blood glucose concentrations. In this case, dose adjustment of insulin and/or oral hypoglycemic drugs may be required.

Serotonin syndrome

In rare cases, the development of serotonin syndrome has been reported when taking SSRIs. The development of this condition may be indicated by a combination of symptoms such as agitation, myoclonus and hyperthermia. If such phenomena occur, citalopram should be immediately discontinued and symptomatic treatment should be started.

Serotonergic drugs

Citalopram should not be used in combination with drugs that have serotonergic effects, such as sumatriptan or other triptans, tramadol, oxytriptan and tryptophan.

Bleeding

There are reports of the development of skin hemorrhages, such as ecchymosis, gynecological, gastrointestinal bleeding and other hemorrhagic complications of the skin or mucous membranes while taking SSRIs. Caution should be exercised when using SSRIs concomitantly with drugs that affect platelet function or drugs that may increase the risk of bleeding, as well as when treating patients with a history of bleeding disorders.

Electroconvulsive therapy (ECT)

Because clinical experience with the concomitant use of SSRIs and electroconvulsive therapy (ECT) is limited, caution should be used when citalopram and ECT are used concomitantly.

Reversible selective MAO A inhibitors

Concomitant use of citalopram and MAO A inhibitors is not recommended due to the risk of developing serotonin syndrome.

St. John's wort

Citalopram and preparations containing St. John's wort (Hypericum perforatum) should not be used simultaneously, because this may increase the risk of adverse reactions.

Psychosis

Treatment of psychotic patients with a depressive episode may increase the manifestation of psychotic symptoms.

Withdrawal symptoms when stopping SSRI therapy

Withdrawal symptoms occur quite often, especially when therapy is abruptly stopped.

The likelihood of withdrawal symptoms may depend on a number of factors, including the duration of treatment, the dose of the drug, and the rate at which it is tapered.

The most commonly reported symptoms were: dizziness, sensory disturbances (including paresthesia), sleep disturbances (including insomnia and vivid dreams), agitation or anxiety, nausea and/or vomiting, tremor, confusion, sweating, headache, diarrhea, rapidity palpitations, emotional lability, irritability and visual disturbances. These symptoms are usually mild or moderate in severity, but in some patients they can be severe. Typically, such manifestations develop during the first days after discontinuation of the drug, however, there are isolated reports of the development of such conditions in patients who accidentally missed taking the next dose.

In most cases, these complications resolve within 2 weeks, although in some patients symptoms may persist for 2-3 months or longer. Therefore, before ending the course of taking citalopram, it is recommended to gradually reduce the dose of the drug over a period of several weeks to several months, depending on the patient’s condition.

QT prolongation

Citalopram has been found to cause dose-dependent prolongation of the QT interval. Cases of QT prolongation and ventricular arrhythmias, including torsade de pointes

, predominantly in female patients, with hypokalemia or pre-existing QT prolongation or other cardiac disease.

The drug is recommended to be used with caution in patients with significant bradycardia, in patients who have recently suffered a myocardial infarction, or with decompensated heart failure. Electrolyte disturbances, such as hypokalemia and hypomagnesemia, increase the risk of malignant arrhythmias and should therefore be corrected before initiating citalopram therapy.

In patients with compensated heart disease, an ECG study should be performed before starting treatment.

If any signs of cardiac arrhythmias occur during treatment with citalopram, the latter should be discontinued and an ECG study performed.

Citalopram

Active substance:

Citalopram*

Pharmgroup:

Antidepressants

Average price in pharmacies