Active substanceCitalopramCitalopram
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substance: citalopram 20 mg or 40 mg (as citalopram hydrobromide 24.98 mg or 49.96 mg);

    Excipients: corn starch 38.1 / 76.2 mg, lactose monohydrate 23.05 (46.1 mg, povidone-K90 3 / 7.7 mg, microcrystalline cellulose (Avicel PH 200) 35 / 68.3 mg, magnesium stearate 0.87 / 1.74 mg;

    tablet shell: hypromellose 2/4 mg, macrogol-400 0.4 / 0.8 mg, titanium dioxide (E171) 0.7 / 1.4 mg.

    Description:Elliptical-shaped tablets, film-coated, white with a logo AI on one side and risk on the other.
    Pharmacotherapeutic group:antidepressant
    ATX: & nbsp

    N.06.A.B.04   Citalopram

    Pharmacodynamics:

    Antidepressant, a selective serotonin reuptake inhibitor (SSRI),has a pronounced ability to inhibit the reuptake of serotonin, has virtually no effect on neuronal uptake of noradrenaline, dopamine, and gamma-aminobutyric acid. Citalopram has no or very little affinity for cholinergic, histaminergic and most adrenergic, serotonergic and dopaminergic receptors. Virtually no effect on the conduction system of the heart and blood pressure, on hematologic indices, liver and kidney function. The antidepressant effect develops after 2-4 weeks of taking the drug.

    Pharmacokinetics:

    Citalopram is rapidly absorbed when taken orally, the time to reach the maximum concentration of citalopram in the blood plasma (TSmOh) is achieved on average after 4 hours. Absorption does not depend on food intake. Bioavailability for oral administration is approximately 80%. The apparent volume of distribution is from 12 to 17 l / kg. The binding of citalopram and its metabolites to plasma proteins is below 80%.

    Citalopram is metabolized to demethylcitalopram, didemethylcitalopram, citalopram-14-oxide and deaminated derivatives of propionic acid.The derivatives of propionic acid are pharmacologically inactive. Demethylcitalopram, didemethylcitalopram, citalopram-14-oxide are SSRIs, although in comparison with the active substance their effect is weaker.

    The half-life of plasma is approximately 1.5 days. The clearance of citalopram in plasma after oral administration is 0.4 l / min.

    Citalopram is mainly excreted through the intestine (85%), and also through the kidneys (15%). In unchanged form with urine is deduced 12-23% of the accepted dose of citalopram. The clearance of citalopram in the liver is approximately 0.3 l / min, in the kidneys - 0.05-0.08 l / min. In elderly patients, in patients with impaired hepatic function, the half-life and concentration in the blood plasma increase approximately 2-fold.

    Equilibrium concentrations of citalopram in blood plasma are achieved after 1-2 weeks. Between equilibrium concentrations of citalopram in blood plasma and the dose taken, there is a linear relationship. When taking citalopram at a dose of 40 mg per day, the average concentration of citalopram in blood plasma is about 300 nmol / l.

    Indications:

    - Depression of various genesis;

    - panic disorders (including agoraphobia).

    Contraindications:

    - Hypersensitivity to citalopram or any of the excipients included in the formulation;

    - hereditary intolerance of galactose, lactase deficiency or glucose-galactose malabsorption syndrome;

    - simultaneous administration with monoamine oxidase (MAO) inhibitors (including 14 days after discontinuation of MAO inhibitors);

    - severe renal failure (creatinine clearance less than 20 ml / min);

    - children and adolescents under 18 years of age (effectiveness and safety not established);

    - simultaneous application of citalopram with drugs that have a serotonergic effect (sumatriptan, tramadol, tryptophan, oxytryptane).

    Carefully:

    - Epilepsy;

    - Diabetes mellitus (the control of glucose concentration in the blood is necessary);

    - a history of mania, hypomania;

    - elderly age;

    - convulsive seizures;

    - hepatic and renal failure (mild to moderate);

    - pharmacologically uncontrolled epilepsy;

    - depression with suicidal attempts;

    - simultaneous reception with drugs that reduce the threshold of convulsive readiness, causing hyponatremia.

    Pregnancy and lactation:

    In pregnancy and lactation, the administration of the drug is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

    Dosing and Administration:

    Inside, once a day (morning or evening), regardless of food intake. The beginning of the therapeutic effect after 2 weeks of therapy. Taking the drug is recommended to continue for 4-6 months after the disappearance of symptoms.

    Depression: the usual dose of 20 mg once a day, the maximum daily dose - 60 mg.

    Panic disorders: the first week is recommended taking a dose of 10 mg once a day, after that the dose can be increased to 20 mg per day. Gradually, the dose can be increased to 60 mg per day.

    Elderly age: the recommended daily dose is -10 mg, the dose can be increased to a maximum daily dose of 30 mg.

    If there is a violation of the liver: the recommended daily dose is -10 mg, the dose can be increased to a maximum daily dose of 30 mg.

    With a mild to moderate degree of renal dysfunction, dose adjustment is not required.

    It is necessary to abolish the drug slowly, it is recommended that the dose be gradually reduced within 1-2 weeks.

    Side effects:

    The incidence of side effects is characterized as very common (> 10%), common (> 1% <10%), unresponsive (> 0.1% <1%), rare (> 0.01% <0.1%) and very rare (<0.01%).

    From the nervous system: > 10% - headache, tremor, dizziness, drowsiness insomnia, agitation, nervousness; > 1% <10% - migraine, paresthesia, sleep disturbance, impaired concentration, drowsiness, amnesia, anxiety, decreased libido, increased appetite, anorexia, apathy, suicidal attempts, confusion of thoughts; > 0.01% <0.1% - asthenia, mood changes, aggressive behavior, emotional lability, agitation, mania, hypomania, panic behavior, paranoid reaction, psychosis, excessive fatigue, anxiety, extrapyramidal disorders, convulsions, euphoria, increased libido , serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, tremor, increased sweating, agitation, uncontrolled behavior); <0.01% - hallucinations, depersonalization, panic attacks.

    From the side of the cardiovascular system:> 10% - atrial flutter (heart rhythm disturbance); > 1% <10% - tachycardia; > 0.01% <0.1% - a bradycardia; Orthostatic hypotension, increase or decrease in blood pressure; <0.01% - supraventricular and ventricular arrhythmias.

    From the gastrointestinal tract: > 10% - nausea, dry mouth, constipation, diarrhea; > 1% <10% - dyspepsia, vomiting, abdominal pain, flatulence, anorexia, increased salivation; > 0.01% <0.1% - an increase in the activity of liver enzymes.

    From the side of the urinary system: > 1% <10% - frequent urination, polyuria. Disturbances of metabolism: > 1% <10% - decrease or increase in body weight.

    From the respiratory system: > 1% <10% - rhinitis, sinusitis; > 0.01% <0.1% - cough.

    From the side of the reproductive system:> 1% <10% - violations of ejaculation, decreased libido, female anorgasmia, dysmenorrhea, impotence, menstrual irregularities; <0.01% is a galactorrhea.

    From the skin: > 10% - increased sweating; > 1% <10% - rash, itching; > 0.01% <0.1% - photosensitivity, epidermal necrolysis; <0.01% - angioedema.

    From the side of the organ of vision: > 10% - violation of accommodation; > 1% <10% - visual impairment, <0.01% - mydriasis.

    From the sense organs:> 1% <10% - a violation of taste.

    From the side of the auditory and vestibular apparatus: > 1% <10% - noise in the ears.

    From the side of the musculoskeletal system: > 10% - myalgia; <0.01% - arthralgia.

    On the part of the organs of hematopoiesis:> 0.01% <0.1% - bleeding is rarely possible (for example, bleeding due to gynecological causes, gastrointestinal bleeding, ecchymosis), thrombocytopenia.

    Other:> 10% - asthenia; > 1% <10% - fatigue; > 0.01% <0.1% - allergic reactions, fainting, malaise, hyperthermia, mastodonia, yawning, gnashing of teeth, dyspnea; hyponatremia; <0.01% anaphylactoid reaction.

    Overdose:

    Symptoms: dizziness, drowsiness, dysarthria, sinus tachycardia, nodal rhythm on the ECG, lengthening of the interval Q-T, Arrhythmia type "pirouette", ventricular arrhythmia, increased sweating, vomiting, cyanosis, hyperventilation, tremor, amnesia, confusion, changes in the electroencephalogram (nodal rhythm), rhabdomyolysis, seizures, coma.

    Treatment: gastric lavage, symptomatic and maintenance therapy; there is no specific antidote.

    Interaction:

    Combined use in combination with inhibitors of MAO (monoamine oxidase) and also in patients recently discontinued use of SSRIs and initiating MAO inhibitor therapy is not recommended because it can lead to the development of serotonin syndrome.

    It is not recommended simultaneous use of citalopram with drugs that have a serotonergic effect (sumatriptan, tramadol, tryptophan, oxytryptane).

    Caution is recommended when patients are simultaneously prescribed anticoagulants, drugs that affect the function of platelets, such as NSAIDs, acetylsalicylic acid, dipyridamole and ticlopidine, or other medications (eg, antipsychotic medications (neuroleptics), including phenothiazines, tricyclic antidepressants) that increase the risk of bleeding.

    It is possible to increase the incidence of unwanted reactions with simultaneous application of citalopram and herbal preparations containing St. John's Wort (perforated)Hypericum perforatum).

    Pharmacodynamic and pharmacokinetic interactions between citalopram and alcohol were not identified. However, when taking citalopram, drinking alcohol is not recommended.

    Citalopram is a weak inhibitor of isoenzyme CYP 2D6. In this connection, it is impossible to exclude interactions with citalopram with simultaneous use of other drugs metabolized by isoenzyme CYP 2D6. With the simultaneous use of citalopram and metoprolol (substrate isoenzyme CYP 2D6) the plasma content of the latter increases twofold.Clinically significant effects on blood pressure or heart rate were not detected.

    Cimetidine causes an increase in the mean plasma concentration of citalopram by 40%.

    Thus, with simultaneous use of high doses of citalopram and cimetidine, caution should be exercised.

    Citalopram does not interact with lithium preparations. However, there were descriptions of the increase in the serotonergic effect of other SSRIs in the appointment with lithium preparations. In such cases, the lithium content in the blood plasma is monitored.

    There was no interaction between citalopram and imipramine, while the plasma content of desipramine, the main metabolite of imipramine, increased. When combining desipramine with citalopram, an increase in the plasma concentration of desipramine was observed. Thus, a dose reduction of desipramine may be required.

    Citalopram does not interact with levomepromazine, digoxin or carbamazepine.

    With simultaneous use with warfarin, prothrombin time increases by 5%.

    Special instructions:

    If the drug is used during pregnancy, the dose should be reduced and taking the drug is discontinued the week before giving birth.

    When prescribing the drug during breastfeeding, it is possible to develop drowsiness in infants, reduce the sucking reflex, and lose weight.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and quick reaction.

    Form release / dosage:
    Tablets, film-coated, 20 mg and 40 mg.
    Packaging:
    For 14 tablets in a contour mesh package made of PVC / Al-foil.
    2 contour packs with instructions for use in a cardboard box.
    Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000428
    Date of registration:24.02.2011
    The owner of the registration certificate:NANOLEC, LTD. NANOLEC, LTD. Russia
    Manufacturer: & nbsp
    Representation: & nbspNANOLEC, LTD.NANOLEC, LTD.
    Information update date: & nbsp27.09.2015
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