Citalopram - instructions for use, dose, side effects, contraindications

Antidepressant. The mechanism of action is associated with selective blockade of reverse neuronal seizure of serotonin in synapses of CNS neurons with a minimal effect on the reuptake of noradrenaline and dopamine. Has little or no ability to bind to a variety of receptors, including serotonin HT_1A-, 5HT_2A-, dopamine D₁- and D₂-, α₁-, α₂- and β-adrenergic receptors, histamine H₁receptors, GABA receptors, m-cholinergic receptors and benzodiazepine receptors.

Promotes mood improvement, relieves feelings of anxiety, reduces feelings of fear and tension, eliminates dysphoria, reduces obsessive conditions, almost does not cause sedation.

A persistent clinical effect develops after 7-10 days of regular admission.

Pharmacokinetics:

After oral administration, the maximum concentrationCitalopram in plasma is achieved after 2-4 hours Bioavailability with oral administration is about 80%.

Changes in the concentration of citalopram in plasma are linear. The equilibrium concentrationin plasma is established after 1-2 weeks of therapy.

Binding to plasma proteins is less than 80%.

In the blood plasma citalopram is present mainly unchanged. Metabolized by demethylation, deamination and oxidation.

Half-lifeis 1.5 days.

It is excreted by the kidneys and through the intestines.

Indications:

Depression of various genesis (endogenous and exogenous); affective (depressive, bipolar, dysthymic) disorders; mixed anxiety-depressive disorders; anxiety-phobic disorders (phobic, panic, obsessive-compulsive, generalized anxiety, post-traumatic stress disorders); somatization disorder; psychosomatic diseases with autonomic dysfunction (including autonomic dysfunction of the cardiovascular system,respiratory system, GIT, genitourinary system); vascular dementia with depressive symptoms; depressive disorders in women (premenstrual dysphoria, depression of pregnant women, postpartum depression, premenopausal depression); eating disorders (anorexia, bulimia); depression with alcoholism; depression in the elderly.

ICD-10

V.F40-F48.F42 Obsessive-compulsive disorder

V.F40-F48.F41.2 Mixed anxiety and depressive disorder

V.F40-F48.F41.0 Panic disorder [episodic paroxysmal anxiety]

V.F40-F48.F41 Other anxiety disorders

V.F30-F39.F33 Recurrent depressive disorder

V.F30-F39.F31 Bipolar affective disorder

V.F30-F39.F32 Depressive episode

Contraindications:

Hypersensitivity, including to escitalopram, simultaneous administration of MAO inhibitors.

Congenital syndrome of prolongation of the QT interval.

Carefully:

Pregnancy, breast-feeding, children's age (safety and effectiveness of use in children are not defined).

Bradycardia, hypokalemia, hypomagnesemia, recently transferred myocardial infarction, decompensated heart failure.

In patients with hepatic insufficiency citalopram should be used in minimal doses.

Pregnancy and lactation:

Action category for the fetus by FDA - C. In pregnancy, use is possible if the expected effect of therapy exceeds the potential risk for the fetus (adequate and strictly controlled studies of safety of use in pregnant women have not been conducted).

Lactation. There are 2 reports of cases of excessive drowsiness, reduced food intake and body weight in infants breastfed by women taking citalopram. In one case, the baby completely recovered after citalopram was stopped by the mother.

Breastfeeding women should stop breastfeeding or taking citalopram.

Dosing and Administration:

Take inside once a day.

For adults, depending on the indications, the initial dose is 10-20 mg per day, if necessary, an increase of up to 60 mg per day is possible. In patients older than 65 years - 20 mg per day, if necessary, it is possible to increase to 40 mg per day.

The duration of therapy (to prevent relapse) is 6 months or more.

Side effects:

From the side nervous system: dizziness, headache, tremor, drowsiness, insomnia, agitation, nervousness, migraine, paresthesia; sleep disorder, impaired concentration, amnesia, anxiety, decreased libido, increased appetite, anorexia, apathy, suicidal attempts, confusion of thoughts, asthenia, mood changes, aggressive behavior, emotional lability, agitation, mania, hypomania, panic behavior, paranoid reaction, psychosis, excessive fatigue, anxiety, extrapyramidal disorders, convulsions, euphoria, serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, increased sweating s, uncontrolled behavior), hallucinations, depersonalization; in exceptional cases when used in high doses - convulsive seizures.

From the side of cardio-vascular system: atrial flutter, tachycardia, bradycardia, orthostatic hypotension, increase or decrease in blood pressure, supraventricular and ventricular arrhythmias.

From the side digestive system: nausea, dry mouth, constipation, diarrhea, indigestion, vomiting, abdominal pain, flatulence, anorexia, increased salivation, increased activity of liver enzymes.

From the side urinary system: frequent urination, polyuria.

Violations metabolism: decrease or increase in body weight, hyponatremia, hyperthermia.

From the side respiratory system: rhinitis, sinusitis, cough, shortness of breath.

From the side reproductive system: ejaculation disorders, increased or decreased libido, female anorgasmia, dysmenorrhea, impotence, menstrual irregularities, galactorrhea.

From the side leather: increased sweating, rash, itching, photosensitivity, epidermal necrolysis, angioedema.

From the side sense organs: violation of accommodation, visual impairment, mydriasis, taste disorder, tinnitus.

From the side musculoskeletal system: myalgia, arthralgia.

From the side blood coagulation system: rarely - development of bleeding (eg, bleeding due to gynecological causes, gastrointestinal bleeding, ecchymosis), thrombocytopenia.

Other: asthenia, fatigue, allergic reactions, fainting, malaise, mastodonia, yawning, gnashing of teeth, anaphylactoid reaction.

Overdose:

In clinical trials with an overdose of citalopram (up to 2000 mg), no lethal cases were noted. In post-marketing reports of drug overdose, including citalopram, 12 deaths were recorded, 10 of which - with combination with other drugs and / or alcohol and 2 - with citalopram alone (3920 mg and 2800 mg); 1 case of an overdose without a lethal outcome with 6000 mg was also reported.

Symptoms: dizziness, increased sweating, nausea, vomiting, tremor, drowsiness, sinus tachycardia. In more rare cases - amnesia, confusion, coma, convulsions, hyperventilation of the lungs, cyanosis, rhabdomyolysis, ECG change (including QT lengthening with nodal rhythm and ventricular arrhythmia and 1 possible case of torsades de pointes).

Treatment: gastric lavage and the use of activated charcoal. Maintenance of airway patency for adequate ventilation and oxygenation. It is recommended to closely monitor and monitor vital functions, including heart function, symptomatic and supportive therapy.Due to the high volume of citalopram distribution, the effectiveness of such activities as forced diuresis, dialysis, hemoperfusion and exchange blood transfusion is unlikely. There is no specific antidote.

Interaction:

With simultaneous application with MAO inhibitors, the development of hypertensive crisis (serotonin syndrome) is possible. Therefore, concurrent use of citalopram with MAO inhibitors is contraindicated and within 14 days after discontinuation of their administration.

It inhibits the isoenzyme CYP2D6 to a very small extent, so it does not interact with drugs metabolized by this isoenzyme. However, the decrease in citalopram concentration in the blood plasma can not be ruled out due to the enhancement of its metabolism due to the induction of microsomal liver enzymes by carbamazepine in their simultaneous application.

With the simultaneous use of cimetidine, a moderate increase in the equilibrium concentration of citalopram in the blood plasma is possible.

The effects of sumatriptan and other serotonergic drugs may be intensified by citalopram when applied simultaneously.)

Special instructions:

When citalopram is used, there may be a slight decrease in the heart rate, which is not clinically significant, but in patients with initially lower heart rate citalopram can cause a more pronounced bradycardia.

The efficacy and safety of citalopram in children is not established.

It should be borne in mind that in patients with depression, there is often a decrease in the ability to concentrate, which can be exacerbated by the use of psychotropic drugs.

Instructions

Citalopram (Citalopramum)