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Clinical Pharmacology

Citalopram is an antidepressant, belonging to the group of selective serotonin reuptake inhibitors (SSRIs). Has a pronounced ability to inhibit serotonin reuptake, does not have or has a very weak ability to bind to a number of receptors, including gamma-aminobutyric acid (GABA), H1-histamine, D1- and D2-dopamine receptors; α1-, α2-, beta-adrenergic; benzodiazepine and m-cholinergic receptors, which causes the almost complete absence of such undesirable effects as negative chrono-, dromo- and inotropic effects, orthostatic hypotension, sedation and dry mouth. Citalopram inhibits CYP2D6 isoenzyme only to a very small extent, and, therefore, practically does not interact with drugs metabolized by this enzyme. Thus, side effects and toxic effects are manifested to a much lesser extent.

Antidepressant effect usually develops after 2-4 weeks of treatment.

Citalopram has no effect on serum levels of prolactin and growth hormone.

Citalopram does not impair cognitive / intellectual functions and psychomotor function and has little or no sedative effect.

Citalopram in doses exceeding 40 mg per day can cause abnormal changes in the electrical activity of the heart (prolongation of the QT interval on an ECG).


- depressive episodes of moderate and severe;

- panic disorders.


1 tab. - Italopram (in the form of hydrobromide) 10 mg

Excipients: microcrystalline cellulose 46.90 mg, pregelatinized starch 20.20 mg, magnesium stearate 0.40 mg.

The composition of the film shell: Opadry II 3.20 mg, including polyvinyl alcohol 1.28 mg, macrogol 0.65 mg, talc 0.47 mg, titanium dioxide 0.80 mg.

Citalopram is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Citalopram Alsi Pharma Russia pills
Cipramil Lundbeck AS Denmark pills

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Dosage and Administration

Citalopram is taken orally once a day (without chewing, with a small amount of liquid). The drug can be used at any time of the day, regardless of the meal, it is advisable to take the drug at the same time of day.


Depression therapy begins with taking 20 mg of citalopram per day. Depending on the patient's individual response and the severity of depression, the dose may be increased to a maximum of 40 mg per day.

Panic disorder

For panic disorders for 1 week, the recommended dose is 10 mg per day, then the dose is increased to 20 mg per day. The daily dose, depending on the individual response of the patient, can be further increased to 40 mg per day.

Patients aged 65 and older

The recommended daily intake for the elderly is 10-20 mg. Depending on the individual response and the severity of depression, the dose may be increased to a maximum of 20 mg per day.

Impaired renal function

In chronic renal failure, weak and moderate severity of correction of the dosing regimen is not required. Patients with severe renal insufficiency (creatinine clearance below 30 ml / min) require caution in dose selection.

Impaired liver function

In patients with mild to moderate hepatic insufficiency, the initial dose is 10 mg per day for the first two weeks. Depending on the reaction, the dose may be increased to 20 mg per day. Patients with severe hepatic impairment require extreme caution in dose selection.

Patients with low isoenzyme CYP2C19 activity

In patients with low CYP2C19 isoenzyme activity, the initial dose is 10 mg per day for two weeks. Depending on the reaction, the dose may be increased to 20 mg per day.

Duration of treatment

The effect appears after 2-4 weeks, the duration of the course of treatment is determined by the patient's condition, the effectiveness and tolerability of the therapy being administered and averages 6 months.

Features of the drug when it is canceled

Symptomatology, which may occur with abrupt cancellation of citalopram, is not characteristic. These are most often dizziness, headache, paresthesias, sleep disturbances, asthenia, nervousness, tremor, nausea and / or vomiting.

If treatment is completed, citalopram should be withdrawn gradually over a period of several weeks in order to avoid the "withdrawal" syndrome. In most cases, this is approximately 2 weeks, but in each case, the doctor decides this question individually: for some patients it may take 2-3 months or more.

Adverse reactions

As in the case of the use of other drugs of the SSRI group, undesirable side reactions are noted against the use of citalopram, however, they have a transient nature and are weak.

Adverse reactions to the background of citalopram are observed during the first one or two weeks of treatment and usually weaken significantly as the condition of the patients improves.

The frequency of adverse reactions: very often - ≥10%; often - ≥1%, but

The following adverse reactions may occur.

Allergic reactions: infrequently - hypersensitivity; very rarely - anaphylactic reactions.

From the side of the central nervous system: very often - drowsiness, headache, tremor, dizziness; often - migraine, paresthesia, sleep disorder; infrequently - extrapyramidal disorders, convulsions; rarely, serotonin syndrome (a combination of arousal, tremor, myoclonus, and hyperthermia); frequency unknown - psychomotor agitation, akathisia.

From the psychic sphere: very often - agitation, nervousness; often - decreased libido, impaired orgasm (in women), anxiety, confusion, drowsiness, impaired concentration, strange dreams, amnesia; infrequently - aggression, depersonalization, hallucinations, mania, euphoria, increased libido; frequency unknown - panic attacks, bruxism, suicidal thoughts.

On the part of the digestive system: very often - dry mouth, nausea, constipation; often - vomiting, flatulence, diarrhea, abdominal pain, hepatitis; frequency unknown - gastrointestinal bleeding.

From the side of the cardiovascular system: very often - a sensation of heartbeat; often - tachycardia, arterial hypertension, orthostatic hypotension; rarely - bradycardia, decreased blood pressure, arrhythmia; frequency unknown - prolongation of the QT interval on the ECG.

From the side of blood-forming organs: rarely - hemorrhages (for example, gynecological bleeding, bleeding of the gastrointestinal tract, ecchymosis, and other forms).

From the senses: very often - accommodation disturbance; often - a violation of taste, visual disturbances, rarely - ringing in the ears.

On the part of the respiratory system: often - rhinitis, sinusitis; infrequently - cough; rarely - dyspnea.

On the part of the reproductive system: often - a violation of sexual function, namely, a violation of ejaculation, decreased libido, impotence, menstrual disorders; rarely - galactorrhea.

From the urinary system: often - painful urination, polyuria.

Metabolic disorders: often - loss of appetite, weight loss, increased appetite; rarely, insufficient secretion of antidiuretic hormone (ADH), weight gain, hyponatremia; hypokalemia.

On the part of the skin: very often - excessive sweating, often - skin rash, itching; infrequently - photosensitivity, urticaria, alopecia, purpura; frequency is unknown - angioedema, bruising.

On the part of the musculoskeletal system: infrequently - myalgia, arthralgia, increased risk of injuries and fractures.

Laboratory indicators: often - changes in laboratory parameters of liver function; infrequently, increased activity of liver enzymes, changes in the electrocardiogram (prolongation of the QT interval), hyponatremia.

Other: rarely - hyperthermia, yawning, increase or decrease in body weight.


- hypersensitivity to citalopram or to any of the excipients that make up this drug;

- Citalopram should not be used in combination with monoamine oxidase inhibitors (MAO), including selegiline, moclobemide, linezolid (antibiotic), and also for 14 days after discontinuation of their administration. Treatment with MAO inhibitors can be started no earlier than 7 days after discontinuation of citalopram;

- Citalopram is contraindicated in case of simultaneous use with drugs that prolong the QT interval on the ECG (in particular, with pimozide), as well as with congenital prolongation of the QT interval;

- Children under the age of 18 is a contraindication for the use of citalopram, since the efficacy and safety of its use at this age has not been established.

Drug interactions

Combined use is contraindicated

With MAO inhibitors

Concomitant treatment with MAO inhibitors is contraindicated (both non-selective and selective) due to the risk of serious side effects, including serotonin syndrome. Citalopram should not be used in combination, incl. with selegilin, moclobemide, linezolid (antibiotic), etc., as well as within 14 days after stopping their intake. Treatment with MAO inhibitors can be started no earlier than 7 days after discontinuation of citalopram.

With means extending the QT interval

Do not use with drugs that extend the QT interval, such as antiarrhythmics (procainamide, amiodarone, etc.), antipsychotics / neuroleptics (for example, phenothiazine derivatives, pimozide, haloperidol), tricyclic antidepressants, and SSRIs (fluoxetine); and their analogues, for example, erythromycin, clarithromycin, quinolone and fluoroquinolone derivatives: sparfloxacin, moxifloxacin, pentamidine, H1-histamine receptor blockers (astemizol, mizolastine), antigree Asocyanase agents (ketoconazole, fluconazole), domperidone, and ondansetron, since citalopram in doses exceeding 40 mg per day can cause abnormal changes in the electrical activity of the heart (prolongation of the QT interval on the ECG) and lead to a heart rhythm disorder (including the development of arrhythmias of the type "pirouette"), which can be fatal.


The simultaneous use of pimozide and citalopram is contraindicated because their combined use lengthens the QT interval.This also applies to such agents as amitriptyline, maprotiline, venlafaxine, terfenadine, haloperidol, droperidol, chlorpromazine, thioridazine.

Combined use of Tsitalopram should be carried out with care:

Citalopram can reduce the threshold of convulsive readiness. It is necessary to exercise caution while taking other means of reducing the threshold of convulsive readiness (tricyclic antidepressants, SSRIs, neuroleptics - derivatives of phenothiazine, thioxanthene and butyrophenone; meflokhina and tramadol).

With the simultaneous use of citalopram and tryptophan, there have been reported cases of enhanced drug action. It is advisable not to combine serotonergic drugs such as sumatriptan or other triptans, as well as tramadol with citalopram.

The simultaneous use of citalopram and preparations containing Hypericum perforatum (Hypericum perforatum) can lead to an increase in side effects.

With simultaneous use of cimetidine causes a moderate increase in the equilibrium concentration of citalopram in the blood. Therefore, it is recommended to exercise caution when prescribing maximum doses of citalopram simultaneously with the use of high doses of cimetidine.

With simultaneous use of citalopram with indirect anticoagulants and other agents that affect blood clotting (atypical antipsychotics and phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and nonsteroidal anti-inflammatory drugs, ticlopidine and dipyridamol, can be exhausted by one another, a trifludolol antihydrogen stimulant can be exhausted, and a non-steroidal anti-inflammatory, ticlopidine and dipyridamole can be exhausted by one another. In such cases, at the beginning or end of treatment with citalopram, regular monitoring of blood clotting is necessary.

With simultaneous appointment with warfarin prothrombin time increases by 5%.

There was no interaction of citalopram with alcohol. However, as in the case of other psychotropic drugs, the simultaneous use of citalopram and alcohol is not recommended.

In vitro studies have revealed that citalopram is transformed into its demethylated derivatives with the participation of CYP2C19 and CYP3A4 isoenzymes, as well as with a small contribution of the CYP2D6 isoenzyme. It has been proven that inhibition of one of the enzymes can be compensated by other enzymes. The inhibitory effect of citalopram on these and other cytochrome P450 isoenzymes is weak or insignificant, therefore citalopram has a low ability for clinically significant drug interactions known for this situation. However, caution is needed if citalopram is prescribed in conjunction with drugs that are metabolized mainly by the CYP2D6 isoenzyme and have a low therapeutic index. Although clinical data on multiple-dose pharmacokinetic studies are not available, there is in vitro data (a model of human liver microsomes) that show a delay in the formation of demethylated citalopram derivatives by 45–60% and 75–85% compared to control after adding ketoconazole and omeprazole , respectively. It may prove necessary in these cases, care in assignment together with citalopram such strong inhibitors of CYP3A4, as ketoconazole, itraconazole, fluconazole, or such strong inhibitors of CYP2C19, as omeprazole, esomeprazole, fluvoxamine, ticlopidine, lansoprazole, as their co-administration with citalopram may significantly reduce clearance of citalopram. Therefore, the maximum recommended dose of citalopram for patients taking together drugs-inhibitors of the CYP2C19 isoenzyme should not exceed 20 mg / day, incl. and because the risk of lengthening the QT interval increases.

The combined use of citalopram with imipramine or desipramine does not affect the concentration of imipramine and citalopram, but increases the concentration of desipramine; dose adjustment of desipramine may be necessary.

Pregnancy and Lactation

Pregnant and lactating women should not be given to citalopram if the potential clinical benefit does not prevail over the theoretical risk, since safety of the drug during pregnancy and lactation in women has not been established.

The use of citalopram in the third trimester of pregnancy may adversely affect the psychophysical development of the newborn. The following disorders are possible in newborns whose mothers took selective serotonin reuptake inhibitors right up to delivery: respiratory failure, cyanosis, shortness of breath, convulsions, temperature instability, feeding difficulties, vomiting, hypoglycemia, muscle hypertension or hypotension, hyperreflexia, tremor, nervousness, irritability, lethargy, constant crying, drowsiness and insomnia.

Epidemiological evidence suggests that using SSRIs during pregnancy, especially in late pregnancy, may increase the risk of persistent pulmonary hypertension in newborns. The observed risk was in 5 cases per 1000 pregnancies. In the general population, the risk is from 1 to 2 cases of persistent pulmonary hypertension in newborns per 1000 pregnancies.

Such violations may indicate serotonergic effects or the occurrence of the syndrome of "cancel". In the case of citalopram during pregnancy, its reception should not be abruptly interrupted.

Special instructions

Children under 18 years of age are a contraindication to the use of citalopram, since the efficacy and safety of its use at this age has not been established.

In connection with the possibility of suicidal attempts, in patients with depression, it is necessary to carefully monitor patients at the beginning of treatment and prescribe minimal effective doses to reduce the risk of overdose. This precaution must be observed when treating other mental disorders due to the possibility of simultaneous illness of a depressive episode.

Severe depression is characterized by the risk of suicidal acts, which can persist until a significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or neuroleptic drugs and constant medical supervision (to entrust the storage and distribution of drugs to trusted persons) can be shown. In the treatment of panic disorders with the prescription of antidepressants and / or benzodiazepines, in some patients, anxiety or anxiety is greatly increased in response to the treatment initiated. This condition (called by specialists “pathological disinhibition” or simply “paradoxical anxiety”, the term has not yet been approved) is considered as a rare phenomenon, although this pathological reaction has been repeatedly documented in the scientific literature. This "paradoxical anxiety" usually decreases during the first few weeks after the start of treatment. It is recommended to start with a low dose to reduce the risk of paradoxical anxiety. Discontinuation of the drug in this case is recommended if such a paradoxical reaction does not disappear for a long time, and if such complications of therapy exceed the benefits of the treatment.

In children, adolescents and young people (under 24 years) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, the appointment of citalopram or any other antidepressants in this category of patients should relate the risk of suicide and the benefits of their use. In short-term studies, the risk of suicide was not increased in people over 24 years of age, while in people over 65 years of age it somewhat decreased. During antidepressant treatment, all patients should be monitored for early detection of suicidal tendencies.

Citalopram should be used with caution in renal insufficiency (creatinine clearance below 30 ml / min), hypomania, mania, pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes mellitus, cirrhosis of the liver, bleeding tendency; simultaneous use with drugs that reduce the threshold of convulsive readiness and causing hyponatremia, with ethanol, as well as drugs that are metabolized by the CYP2C19 isoenzyme.

Citalopram can cause a dose-dependent lengthening of the QT interval, which can lead to a cardiac arrhythmia.

Hyponatremia develops due to impaired secretion of antidiuretic hormone, a particularly high level of risk in older women.

Treatment with Citalopram can alter the glycemic control in patients with diabetes. The dose of insulin and / or oral hypoglycemic agents should be adjusted.

It is rarely possible for akatizia to develop, characterized by a constant or recurring feeling of internal motor anxiety and manifested in the inability to sit still for a long time in one position or remain motionless for a long time. It takes place during the first weeks of treatment.

Patients with bipolar disorder may experience mania. Then treatment with citalopram must be stopped.

It is necessary to use caution citalopram in the presence of drug dependence (including history) and epileptic seizures in history.

Citalopram should not be used in combination with monoamine oxidase inhibitors (MAO), and for severely impaired renal function, caution is required. In case of abnormal liver function, taking the drug is limited to the minimum recommended doses. Elderly patients require a reduction in the dose of citalopram.

With the development of a manic state, the drug should be canceled.

Clinical experience with the simultaneous use of SSRIs and electroconvulsive therapy is insufficient, so caution is required.

At the beginning of treatment, insomnia and anxiety may occur, which can be resolved by adjusting the initial dose.

Abrupt cessation of citalopram therapy may lead to a "withdrawal" syndrome. Such adverse reactions may occur, such as dizziness, headaches, nausea. To avoid the emergence of the syndrome of "cancellation" requires the gradual removal of the drug within a few weeks.

Influence on ability to drive motor transport and control mechanisms

Citalopram should be used with caution in persons whose activities are related to the mechanisms or control of moving vehicles. Citalopram does not reduce the mental abilities and the speed of psychomotor reactions, however, in patients we can expect some reduction in attention and concentration due to the existing disease, adverse reactions from the treatment or from both.


Overdose symptoms: convulsions, drowsiness, tachycardia, bradycardia, hypotonia or hypertension, nausea, vomiting, tremor, serotonin syndrome, agitation, dizziness, mydriasis, stupor, sweating, cyanosis of the skin, heart failure, bundle branch block, hyperventilation , atrial arrhythmia, ventricular arrhythmia, coma.

Coma and lethal overdose with citalopram are extremely rare, most of them include a simultaneous overdose with other drugs.

Overdose treatment: there is no specific antidote. In case of overdose, gastric lavage should be carried out as soon as possible. Treatment is symptomatic and supportive. Medical observation is recommended, with loss of consciousness and respiratory failure - intubation, as well as careful monitoring of ECG and other vital functions, since there is a high risk of fatal arrhythmias accompanied by sinus tachycardia, nodal rhythm, lengthening of the QT interval, in particular, pirouette arrhythmias may develop , ventricular arrhythmias.

  • Brand name: Citalopram
  • Active ingredient: Citalopram
  • Dosage form: pills, film coated white, round, biconvex; in cross-section, the inner layer is white or white with a yellowish tinge.
  • Manufacturer: Evalar

Studies and clinical trials of Citalopram (Click to expand)

  1. The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation
  2. Citalopram Compared to Dothiepin and Placebo: Effects on Cognitive Function and Psychomotor Performance
  3. Short-term and long-term evaluation of selective serotonin reuptake inhibitors in the treatment of panic disorder: fluoxetine vs citalopram
  4. A randomised, double-blind comparison of the efficacy and safety of citalopram compared to mianserin in elderly, depressed patients with or without mild to moderate dementia
  5. Steady-state pharmacokinetics of the enantiomers of citalopram and its metabolites in humans
  6. Citalopram and panic disorder
  7. Use of the selective serotonin reuptake inhibitor citalopram in a possible animal analogue of obsessive-compulsive disorder
  8. Comparison of the tolerability and efficacy of citalopram and amitriptyline in elderly depressed patients treated in general practice
  9. Double-blind comparison of citalopram and placebo in depressed outpatients with melancholia
  10. Serotonin and information processing: a pharmacodynamic study on the effects of citalopram on cognitive and psychomotor function
  11. Citalopram
  12. Relationship between clinical effects, serum drug concentration, and concurrent drug interactions in depressed patients treated with citalopram, fluoxetine, clomipramine, paroxetine or venlafaxine
  13. SLC6A4 variation and citalopram response
  14. Neonatal Exposure to Citalopram Selectively Alters the Expression of the Serotonin Transporter in the Hippocampus: Dose-Dependent Effects
  15. Altered Expression of Tyrosine Hydroxylase in the Locus Coeruleus Noradrenergic System in Citalopram Neonatally Exposed Rats and Monoamine Oxidase A Knock Out Mice
  16. Fluoxetine and citalopram exhibit potent antiinflammatory activity in human and murine models of rheumatoid arthritis and inhibit toll-like receptors
  17. A highly sensitive LC-MS/MS method for the determination of S-citalopram in rat plasma: application to a pharmacokinetic study in rats
  18. Analytical procedures for the determination of the selective serotonin reuptake inhibitor antidepressant citalopram and its metabolites
  19. Stereoselective determination of demethyl- and didemethyl-citalopram in rat plasma and brain tissue by liquid chromatography with fluorescence detection using precolumn derivatization
  20. Increased deep sleep in a medication-free, detoxified female offender with schizophrenia, alcoholism and a history of attempted homicide: effect of concomitant administration of quetiapine and citalopram
  21. ChemInform Abstract: A New Alternative Synthesis of 5-Cyanophthalide, a Versatile Intermediate in the Preparation of the Antidepressant Drug Citalopram.
  22. Stereoselective single-dose kinetics of citalopram and its metabolites in rats
  23. Enantioselective analysis of citalopram and demethylcitalopram in human and rat plasma by chiral LC-MS/MS: Application to pharmacokinetics
  24. Cytochrome p450-dependent disposition of the enantiomers of citalopram and its metabolites: In vivo studies in Sprague-Dawley and Dark Agouti rats

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