Citalopram
Citalopram: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Citalopram
ATX code: N06AB04
Active ingredient: citalopram (citalopram)
Producer: ALSI Pharma (Russia), Aurobindo Pharma (India)
Description and photo update: 2018-21-11
Prices in pharmacies: from 175 rubles.
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Citalopram is a drug with an antidepressant effect.
Release form and composition
Dosage form of release of Citalopram - film-coated tablets: white, round biconvex; the inner layer on a cross section is white or white with a yellowish tinge (in a cardboard box 1–5 blisters of 10 tablets each or 1–2 blisters of 14 tablets).
Composition of 1 tablet:
- active substance: citalopram - 10, 20 or 40 mg (citalopram hydrobromide - 12.5; 25 or 50 mg);
- auxiliary components (10/20/40 mg): microcrystalline cellulose - 46.9 / 93.8 / 187.6 mg; magnesium stearate - 0.4 / 0.8 / 1.6 mg; pregelatinized starch - 20.2 / 40.4 / 80.8 mg;
- shell (10/20/40 mg): Opadry II (talc - 0.47 / 0.94 / 1.88 mg; polyvinyl alcohol - 1.28 / 2.56 / 5.12 mg; titanium dioxide - 0.8 / 1.6 / 3.2 mg; macrogol - 0.65 / 1.3 / 2.6 mg) - 3.2 / 6.4 / 12.8 mg.
Pharmacological properties
Pharmacodynamics
Citalopram is an antidepressant. It belongs to the group of SSRIs (selective serotonin reuptake inhibitors). It has a pronounced property to suppress the reuptake of serotonin, does not bind or very weakly binds to a number of receptors, including the GABA (gamma-aminobutyric acid) receptors, m-cholinergic receptors, H 1 -histamines, D 1 - and D 2 - dopamine, α 1 -, α 2 -, beta-adrenergic and benzodiazepine receptors. Due 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 almost does not interact with drugs metabolized by this enzyme. Due to this, side reactions and toxic effects are manifested to a much lesser extent.
Usually the antidepressant effect develops after 2-4 weeks of administration.
Citalopram has no effect on serum levels of growth hormone and prolactin. It practically does not have a sedative effect, does not impair intellectual, cognitive functions and psychomotor function.
When used in doses above 40 mg per day, citalopram can lead to abnormal changes in the electrical activity of the heart (prolongation of the QT interval on the ECG).
Pharmacokinetics
The biological availability of citalopram is 80%, the indicator practically does not depend on food intake. C max (maximum concentration of a substance) in plasma is reached on average in 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 citalopram is taken once a day, C ss (equilibrium concentration) in plasma is established after 1–2 weeks of therapy.
V d (volume of distribution) is in the range of 12-17 l / kg. Plasma protein binding - up to 80%. In plasma it is unchanged. Penetrates into breast milk.
Metabolized by demethylation, deamination and oxidation with the participation of cytochrome P 450 (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 for by other enzymes.
T 1/2 (half-life) of citalopram is 36 hours. It is excreted by the liver and kidneys (85% and 15%, respectively), 12–23% of the substance is excreted through the kidneys unchanged. Hepatic clearance is approximately 0.3 l / min, renal clearance is 0.05–0.08 l / min.
In patients over the age of 65, T 1/2 is longer. Also, due to a decrease in metabolism, lower clearance values are observed.
With reduced liver function, the elimination of citalopram is slower. T 1/2 and equilibrium concentrations of the substance are almost two times higher in comparison with patients with undisturbed liver function.
Excretion of citalopram with a mild to moderate degree of decreased renal function proceeds more slowly without a significant effect on pharmacokinetic parameters. When CC (creatinine clearance) is below 30 ml / min, the use of citalopram requires caution.
Indications for use
- panic disorder;
- depressive episodes of moderate to severe.
Contraindications
Absolute:
- congenital lengthening of the QT interval;
- combination therapy with drugs that prolong the QT interval on the ECG;
- combination therapy with MAO (monoamine oxidase) inhibitors, including selegiline, moclobemide, linezolid (antibiotic), as well as within 14 days after stopping them. MAO inhibitors can be used no earlier than 7 days after stopping the intake of Citalopram;
- age up to 18 years;
- individual intolerance to the components of the drug.
Relative (Citalopram is prescribed under medical supervision):
- pregnancy;
- lactation period.
Instructions for the use of Citalopram: method and dosage
Citalopram is taken orally with a small amount of liquid, without chewing.
It is preferable to use the drug at the same time of the day. At the same time, the time of day and food intake do not affect the effectiveness of therapy.
The daily dose is taken in one dose.
Recommended application scheme:
- depression: 20 mg with a possible increase to 40 mg (maximum);
- panic disorder: 10 mg for 7 days, then the dose is doubled; it is possible to use 40 mg of Citalopram (maximum).
Elderly patients are prescribed the drug in a dose of 10 to 20 (maximum) mg.
When choosing a dose in patients with CC below 30 ml / min, caution is required.
The initial dose (during the first two weeks of therapy) in patients with mild to moderate hepatic insufficiency and with low activity of the CYP2C19 isoenzyme should not exceed 10 mg. If necessary, it can be doubled. In severe hepatic impairment, extreme caution is required in dose selection.
The effect of therapy appears after 2-4 weeks. The duration of use depends on the patient's condition, the effectiveness and tolerability of treatment. On average, it is 6 months.
With a sharp cancellation of Citalopram, the development of headache, dizziness, paresthesias, sleep disturbances, asthenia, nervousness, tremor, nausea / vomiting may occur.
Citalopram should be canceled gradually, which will reduce the likelihood of withdrawal syndrome. Usually about 14 days are enough for this, but the doctor decides this issue individually in each case, since for some patients it may take 2-3 months or more.
Side effects
Usually, side effects with the use of Citalopram are observed at the beginning of therapy during the first one to two weeks, they are mild and transient in nature. As a rule, as the condition improves, their severity weakens significantly.
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):
- central nervous system: very often - headache, drowsiness, dizziness, tremor; often - paresthesia, migraine, sleep disorder; infrequently - convulsions, extrapyramidal disorders; rarely - serotonin syndrome (combination of tremor, excitement, hyperthermia and myoclonus); with an indefinite frequency - akathisia, psychomotor agitation;
- digestive system: very often - xerostomia, constipation, nausea; often - abdominal pain, vomiting, diarrhea, flatulence, hepatitis; with an indefinite frequency - gastrointestinal bleeding;
- cardiovascular system: very often - palpitations; often - arterial hypertension, tachycardia, orthostatic hypotension; rarely - arrhythmia, bradycardia, decreased blood pressure; with an indefinite frequency - lengthening of the QT interval on the ECG;
- reproductive system: often - sexual dysfunction (impotence, ejaculation / menstrual irregularities, decreased libido); rarely galactorrhea;
- respiratory system: often - sinusitis, rhinitis; infrequently - cough; rarely - dyspnea;
- urinary system: often - polyuria, painful urination;
- skin: very often - increased sweating; often - itching, skin rash; infrequently - urticaria, photosensitivity, purpura, alopecia; with an uncertain frequency - bruising, angioedema;
- musculoskeletal system: infrequently - arthralgia, myalgia, increased risk of fractures / injuries;
- mental sphere: very often - nervousness, agitation; often - violation of orgasm (in women), impaired concentration, decreased libido, confusion, anxiety, drowsiness, amnesia, strange dreams; infrequently - euphoria, aggression, depersonalization, mania, hallucinations, increased libido; with an indefinite frequency - suicidal thoughts, bruxism, panic attacks;
- sense organs: very often - violation of accommodation; often - impaired vision / taste; infrequently - ringing in the ears;
- hematopoietic organs: rarely - hemorrhages (in particular, bleeding of the gastrointestinal tract, gynecological bleeding, ecchymosis and other forms);
- allergic reactions: infrequently - hypersensitivity; very rarely - anaphylactic reactions;
- laboratory indicators: often - changes in laboratory indicators of liver function; infrequently - changes in the electrocardiogram (prolongation of the QT interval), increased activity of hepatic enzymes, hyponatremia;
- metabolism: often - weight loss, decreased / increased appetite; rarely - insufficient secretion of antidiuretic hormone, weight gain, hypokalemia, hyponatremia;
- others: rarely - yawning, hyperthermia.
Overdose
The main symptoms: drowsiness, convulsions, tachycardia, bradycardia, cyanosis of the skin, muscle hyper- or hypotension, vomiting, nausea, dilated pupils, tremor, stupor, agitation, serotonin syndrome, dizziness, sweating, heart failure, pulmonary hyperventilation, blockade of the legs His, ventricular arrhythmia, atrial arrhythmia.
Coma and deaths with an overdose of Citalopram are extremely rare, in most cases this occurs with a simultaneous overdose of other drugs.
There is no specific antidote. In case of an overdose, gastric lavage is indicated as soon as possible. Therapy is symptomatic and supportive. Medical supervision is recommended, in case of impaired breathing and loss of consciousness - intubation, as well as careful monitoring of the ECG and other vital functions. This is associated with a high risk of fatal arrhythmias accompanied by a junctional rhythm, sinus tachycardia, prolongation of the QT interval, for example, the development of ventricular arrhythmias / arrhythmias of the "pirouette" type.
special instructions
Due to the existing likelihood of suicidal attempts, patients with depression need to be closely monitored at the beginning of therapy. To reduce the risk of overdose, Citalopram should be prescribed in the lowest effective doses. This recommendation should be followed when treating other psychiatric disorders, as there is the potential for a concurrent depressive episode.
The risk of suicidal action may persist until significant remission is achieved. Therefore, at the beginning of therapy, a combination with drugs from the benzodiazepine group or antipsychotics may be indicated.
When treating panic disorder with antidepressants / benzodiazepines, some patients experience significant increases in anxiety or anxiety in response to therapy. This condition (pathological disinhibition or paradoxical anxiety) is rare. Typically, the severity of this disorder decreases within the first few weeks after starting treatment. Cancellation of Citalopram is indicated in cases where such a paradoxical reaction does not disappear for a long time, or similar complications exceed the benefits of taking the drug.
Due to disturbances in the secretion of antidiuretic hormone, hyponatremia may develop. Older women are at increased risk.
In patients with diabetes mellitus, the use of Citalopram can alter glycemic control, as a result of which the dose of insulin and / or oral hypoglycemic agents must be adjusted.
In rare cases, the occurrence of akathisia is noted. This disorder is characterized by a constant or intermittent feeling of internal motor restlessness, which manifests itself as an inability to remain motionless for a long time / sit quietly in one position (usually disappears during the first weeks of treatment).
Manias can occur with bipolar disorder. In this case, Citalopram is canceled. Also, therapy is canceled with the development of a manic state.
In the presence of drug dependence and epileptic seizures (including a burdened history), therapy should be carried out with caution.
Clinical experience with the combined use of Citalopram and electroconvulsive therapy is insufficient (caution is required).
At the beginning of treatment, a feeling of anxiety and insomnia may develop, which may require a correction of the initial dose.
Influence on the ability to drive vehicles and complex mechanisms
Patients during the period of application of Citalopram should be careful, which is associated with the likelihood of a decrease in attention due to the existing disease and adverse reactions from the treatment, or a combination of these factors.
Application during pregnancy and lactation
According to the instructions, Citalopram during pregnancy / breastfeeding can be prescribed under medical supervision after assessing the ratio of the expected benefit with the possible risk.
When using the drug in the third trimester of pregnancy, it may have a negative effect on the psychophysical development of the fetus, in particular, convulsions, respiratory failure, shortness of breath, cyanosis, temperature instability, feeding difficulties, hypoglycemia, vomiting, muscle hypo- or hypertension, hyperreflexia, tremor may develop, irritability, nervousness, constant crying, lethargy, insomnia / drowsiness.
Also, when using Citalopram during pregnancy, especially in the later stages, the likelihood of persistent pulmonary hypertension in newborns increases. The drug should be withdrawn gradually.
Pediatric use
Citalopram therapy is not prescribed to patients under 18 years of age, which is due to the lack of experience with its use in this age group of patients.
With impaired renal function
When QC is below 30 ml / min, when selecting a dose, caution is required.
For violations of liver function
- mild / moderate hepatic impairment: Citalopram is used in reduced doses;
- severe hepatic impairment: dose selection requires caution.
Use in the elderly
Citalopram is prescribed in reduced doses.
Drug interactions
The combined use is contraindicated:
- MAO inhibitors (non-selective and selective), including selegiline, moclobemide, linezolid: development of serious adverse reactions, including serotonin syndrome. You can start taking citalopram 14 days after you stop using these drugs; therapy with MAO inhibitors can be carried out no earlier than 7 days after the end of taking citalopram;
- drugs that lengthen the QT interval, including blockers of H 1 -histamine receptors (mizolastine, astemizole), antiarrhythmics (amiodarone, procainamide, etc.), tricyclic antidepressants and SSRIs (fluoxetine), antipsychotics / neuroleptics (pimosidiazidines), haloperidol), ondansetron, domperidone, antifungal agents of the azole series (fluconazole, ketoconazole), antimicrobial drugs (macrolide antibiotics and their analogs, fluoroquinolone and quinolone derivatives, pentamidine): development of abnormal changes in the electrical activity of the heart (lengthening of the H interval) QT on EC heart rate (including the occurrence of arrhythmias of the "pirouette" type), which can lead to death (when taking citalopram in a dose of more than 40 mg per day);
- pimozide, as well as chlorpromazine, maprotiline, amitriptyline, venlafaxine, haloperidol, terfenadine, droperidol, thioridazine: prolongation of the QT interval.
Careful combinations:
- drugs that lower the seizure threshold, including tricyclic antidepressants, SSRIs, antipsychotics - derivatives of phenothiazine, butyrophenone and thioxanthene, as well as mefloquine, tramadol: the seizure threshold may decrease;
- preparations containing St. John's wort (Hypericum perforatum): side effects may increase;
- tryptophan, as well as serotonergic drugs, including sumatriptan or other triptans, tramadol: their effect may be enhanced;
- cimetidine (in high doses): the equilibrium concentration of citalopram in the blood increases moderately;
- indirect anticoagulants and other drugs that affect blood clotting (atypical antipsychotics, phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid, non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole): a blood clotting disorder may develop (at the beginning of therapy with Cyitalopram) monitor blood clotting indicators);
- warfarin: prothrombin time increases slightly;
- alcohol: no interaction has been identified, but combined use is not recommended;
- strong inhibitors of CYP3A4 and CYP2C19, including itraconazole, ketoconazole, fluconazole, ticlopidine, omeprazole, fluvoxamine, esomeprazole, lansoprazole: the clearance of citalopram can significantly decrease, while the likelihood of prolongation of the QT interval increases; Citalopram when combined with these drugs should be taken in a daily dose of up to 20 mg;
- imipramine, desipramine: their concentration increases, which may require dose adjustment.
Analogs
Analogs of Tsitalopram are: Tsitol, Tsitalon, Umorap, Siozam, Tsipramil, Tsitalift, PRAM, Oprah.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Citalopram
According to reviews, Citalopram is an effective drug. It is noted that with the development of side effects, in some cases, therapy has to be discontinued.
The price of Citalopram in pharmacies
The approximate price for Citalopram (30 tablets of 10, 20 or 40 mg) is 153-175, 330-394 or 389-432 rubles, respectively.
Citalopram: prices in online pharmacies
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Drug name Price Pharmacy |
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Citalopram 10 mg film-coated tablets 30 pcs. 175 RUB Buy |
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Citalopram 20 mg film-coated tablets 30 pcs. 329 r Buy |
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Citalopram 40 mg film-coated tablets 30 pcs. 349 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
