Tsipramil
Tsipramil: 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: Cipramil
ATX code: N06AB04
Active ingredient: citalopram (citalopram)
Manufacturer: H. Lundbeck, A / S (Denmark)
Description and photo update: 2019-21-08
Prices in pharmacies: from 2034 rubles.
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Tsipramil is a psychotropic drug with antidepressant action; selective serotonin reuptake inhibitor.
Release form and composition
Dosage form Tsipramil - film-coated tablets: white, oval, with a line, on both sides of which the marking is symmetrically applied: for a dose of 20 mg - C | N, for a dose of 40 mg - C | R (14 pcs. In blisters, in cardboard boxes: 20 mg - 1, 2 or 4 blisters, 40 mg - 2 blisters).
Composition of 1 tablet:
- active substance: citalopram hydrobromide - 24.98 or 49.96 mg (equivalent to the content of citalopram - 20 or 40 mg);
- auxiliary components: lactose monohydrate, corn starch, copovidone, microcrystalline cellulose, glycerin 85%, magnesium stearate, croscarmellose sodium;
- film shell: macrogol 400, hypromellose 5, titanium dioxide (E 171).
Pharmacological properties
Pharmacodynamics
The active substance of Cipramil, citalopram, is an SSRI (superselective serotonin reuptake inhibitor), which has no or minimal effect on the uptake of dopamine, norepinephrine and gamma-aminobutyric acid.
Citalopram has no or very weak ability to bind to a number of receptors, including muscarinic cholinergic receptors, H 1 -histamine, 5-HT 1A - and 5-HT 2 -serotonin, D 1 - and D 2 -dopamine, α 1 -, α 2 and β-adrenergic, opioid and benzodiazepine receptors.
Suppression of the rapid sleep stage (REM) is considered a predictor of antidepressant action. Citalopram, like other SSRIs, tricyclic antidepressants and monoamine oxidase inhibitors, increases deep NREM sleep and suppresses REM sleep.
In studies conducted with a single dose in healthy volunteers, citalopram did not reduce salivation. There is also no evidence of a significant effect on cardiovascular indicators. Citalopram, like other SSRIs, can increase the plasma prolactin content, while not affecting the serum growth hormone content.
When conducting a double-blind, placebo-controlled ECG study on healthy volunteers, the change in QTc (correction according to the Fridericia formula) compared to baseline values was 7.5 and 16.7 (90% confidence intervals 5.9-9.1 and 15-18, 4) ms for a daily dose of 20 and 60 mg, respectively.
Pharmacokinetics
Absorption of citalopram is almost complete, does not depend on food intake. The average value of T max (time to reach the maximum concentration in the blood plasma) is approximately 3 hours. Bioavailability after oral administration is about 80%.
The apparent volume of distribution is in the range from 12 to 17 l / kg. The binding of a substance and its main metabolites with plasma proteins is up to 80%.
Citalopram is metabolized to form active metabolites - didemethylcitalopram, demethylcitalopram, citalopram-N-oxide. An inactive derivative of deaminated propionic acid is also formed. All active metabolites also have SSRI properties, although their properties are weaker than those of the parent compound.
The predominant component in blood plasma is unchanged citalopram. The concentration of didemethylcitalopram and demethylcitalopram averages 5–10 and 30–50% of the concentration of citalopram, respectively. The biotransformation of citalopram to demethylcitalopram is mediated by isoenzymes CYP2C19, CYP3A4 and CYP2D6 (about 38, 31 and 31%, respectively).
T 1/2 (half-life) - approximately 36 hours. Cl s (systemic plasma clearance) of citalopram is in the range from 0.3 to 0.4 l / min, Cl oral (oral clearance) is approximately 0.4 l / min.
Citalopram is excreted mainly through the kidneys and liver (15 and 85%, respectively). From 12 to 23% of the daily dose is excreted as unchanged substance in the urine. Residual (hepatic) clearance is about 0.3 l / min, the value of renal clearance is in the range from 0.05 to 0.08 l / min.
Citalopram has linear kinetics. Equilibrium plasma concentration is reached within 7-14 days. The average equilibrium concentration when using Tsipramil in a daily dose of 40 mg is 300 nmol / l (from 165 to 405 nmol / l).
In elderly patients, T 1/2 is lengthened (1.5–3.75 days) and clearance values decrease (0.08–0.3 l / min), which is associated with a decrease in metabolic rate. The equilibrium concentration in this group of patients is about 2 times higher than in young patients.
Against the background of impaired hepatic function, citalopram is excreted more slowly. T 1/2 increases approximately 2 times, the equilibrium concentration indicators are approximately twice as high as in patients with no liver dysfunction.
In patients with mild / moderate renal impairment, citalopram is excreted more slowly. This change does not significantly affect the pharmacokinetics of citalopram. The safety profile in severely impaired renal function (with creatinine clearance <30 ml / min) has not been studied.
In patients with weak activity of the isoenzyme CYP2C19, the recommended initial daily dose of Cipramil is 10 mg.
Indications for use
- panic disorder with / without agoraphobia;
- depression of various structures and etiology;
- OCD (Obsessive Compulsive Disorder).
Contraindications
- complex use with linezolid (if it is not possible to carefully monitor the patient's condition and control blood pressure), pimozide and QT-prolonging substances / drugs;
- congenital / acquired QT prolongation syndrome;
- hereditary lactase deficiency, galactose intolerance, impaired glucose / galactose absorption;
- children and adolescents up to 18 years old;
- complex use with MAO (monoamine oxidase) inhibitors, including selegiline, and a period of 2 weeks after the end of their intake; you can start therapy with MAO inhibitors 1 week after the end of taking Tsipramil;
- increased individual sensitivity to citalopram or drug excipients.
According to the instructions, Tsipramil with caution, in view of the increased likelihood of complications, is taken with a history of prolongation of the QT interval, ventricular arrhythmias (including torsade de pointes), significant bradycardia, recent acute myocardial infarction, decompensated heart failure, hypokalemia and / or hypomagnesemia, severe renal failure (creatinine clearance ≤ 30 ml / min), severe hepatic failure, severe suicidal behavior, diabetes mellitus, a tendency to bleeding, electroconvulsive therapy, in old age (over 65 years).
The embryotoxic and teratogenic effects of the drug have not been studied. The use of Tsipramil during pregnancy and lactation is allowed only if the potential clinical benefit to the woman outweighs the estimated risk to the fetus / child.
Instructions for the use of Tsipramil: method and dosage
Tsipramil tablets are taken orally, regardless of food intake.
The recommended dosing regimen is once a day (at any suitable time) in the following doses:
- depression of various structures and etiology: initial dose - 20 mg / day; the dose can be increased, taking into account the severity of the condition and the individual response of the patient, to a maximum of 40 mg / day;
- panic disorder: first week - 10 mg / day, then the dose is increased to 20 mg / day with a possible further increase depending on the patient's response, maximum - 40 mg / day;
- OCD: starting dose 20 mg / day; if necessary, it can be increased, up to a maximum of 60 mg / day.
Dosage adjustment for special patient categories:
- elderly age (≥ 65 years): standard dose - 10–20 mg / day, maximum dose - 20 mg / day;
- liver failure: taking Tsipramil is limited to the minimum recommended doses; the maximum dose is 20 mg / day;
- renal failure of mild and moderate severity: dose adjustment is not required.
Side effects
Undesirable side effects of Tsipramil are transient and mild. They are usually observed during the first weeks of therapy and gradually weaken significantly as the patient's condition improves.
Dose-dependent reactions: dry mouth, increased sweating, nausea, diarrhea, insomnia / drowsiness, weakness.
Data on adverse reactions from organs and systems:
- lymphatic system and blood: frequency unknown - thrombocytopenia;
- immune system: frequency unknown - hypersensitivity reactions, anaphylactic reactions;
- endocrine system: frequency unknown - insufficient secretion of antidiuretic hormone;
- metabolic disorders and eating disorders: often - decreased appetite, weight loss; infrequently - increased appetite, weight gain; rarely, hyponatremia; frequency unknown - hypokalemia;
- psyche: often - decreased libido, anorgasmia (in women), agitation, anxiety, confusion, nervousness, unusual dreams; infrequently - aggression, mania, hallucinations, depersonalization; the frequency is unknown - panic attacks, anxiety, bruxism, suicidal thoughts, suicidal behavior (cases of the appearance of suicidal behavior and thoughts were recorded both during therapy with citalopram and immediately after the discontinuation of Cipramil);
- nervous system: very often - insomnia / drowsiness; often - paresthesias, tremors, dizziness, impaired attention; infrequently - fainting; rarely - dyskinesia, large seizures, taste disturbances; frequency unknown - akathisia, serotonin syndrome, convulsive, extrapyramidal and movement disorders;
- organ of vision: infrequently - dilated pupils (mydriasis); frequency unknown - visual impairment;
- organ of hearing and labyrinthine disorders: often - ringing or tinnitus;
- cardiovascular system: very often - palpitations; infrequently - tachycardia, bradycardia; rarely - bleeding; frequency unknown - orthostatic hypotension, prolongation of the QT interval, ventricular arrhythmia (including pirouette-type arrhythmias - torsades de pointes);
- respiratory system, chest and mediastinal organs: often - yawning; frequency unknown - nosebleeds;
- gastrointestinal tract: very often - nausea, dry mouth; often vomiting, diarrhea / constipation; frequency unknown - gastrointestinal bleeding (including rectal);
- hepatobiliary system: rarely - hepatitis; frequency unknown - changes in liver function tests;
- skin and subcutaneous tissues: very often - hyperhidrosis; often itching; infrequently - alopecia, photosensitivity, rash, urticaria, purpura; frequency unknown - angioedema, ecchymosis;
- musculoskeletal and connective tissue: often - arthralgia, myalgia;
- kidneys and urinary tract: frequency unknown - ischuria;
- reproductive system and mammary gland: often - problems with ejaculation, lack of ejaculation, impotence; infrequently - heavy menstruation in women; frequency unknown - uterine bleeding, galactorrhea, priapism (in men);
- other: often - weakness; infrequently - edema; rarely - hyperthermia.
Abrupt cessation of taking Tsipramil can cause withdrawal symptoms, the most typical and frequent of which are: sensitivity disorders (including paresthesias), dizziness, headache, sleep disorders (including insomnia / intense dreams), palpitations, anxiety, agitation, nausea / vomiting, hyperhidrosis, tremors, confusion, irritability, emotional instability, visual disturbances, diarrhea. As a rule, these phenomena are weakly or moderately expressed, and pass quickly, however, in some cases they are more acute / prolonged. Therefore, citalopram therapy should be discontinued gradually, by gradually reducing its dose.
Overdose
Clinical data on citalopram overdose are limited. In many cases, they are associated with a concomitant overdose of other drugs or alcohol.
Cases of fatal overdose of Tsipramil have been reported, but this was mainly due to concomitant overdose of other drugs.
The main symptoms: sweating, dizziness, nausea, vomiting, tachycardia, seizures, lengthening of the QT interval, drowsiness, coma, hypotension, tremor, cardiac arrest, serotonin syndrome, agitation, bradycardia, prolongation of the QRS complex, bundle blockade, hyperventilation, hypertension, pirouette-type arrhythmia, stupor, ventricular and atrial rhythm disturbances, cyanosis.
Therapy: symptomatic and supportive. Shows gastric lavage, the use of activated charcoal and osmotic laxatives (in particular, sodium sulfate). In case of impaired consciousness, the patient should be intubated. ECG and vital signs are monitored. There is no specific antidote.
ECG monitoring is recommended in cases of overdose in patients with congestive heart failure / bradyarrhythmias, metabolic disorders (in particular, in liver failure), as well as during concomitant therapy with drugs that prolong the QT interval.
special instructions
The antidepressant effect usually develops after 2-4 weeks from the start of treatment. Tsipramil does not contribute to an increase in body weight and does not affect the function of the liver / kidneys, the conducting system of the heart, hematological parameters, and blood pressure.
Careful monitoring of the condition of patients undergoing antidepressant therapy is required, especially at the initial stage, due to the risk of clinical deterioration and / or the appearance of suicidal thoughts and behavior. Such precautions should also be observed in the treatment of other mental disorders, since suicidal events can be a concomitant pathology in relation to a depressive episode. The risk of suicide inherent in depressive conditions may persist until a significant improvement in the condition occurs, either spontaneously or as a result of treatment.
Cancellation of Tsipramil is required with phase inversion and the development of a manic state.
Influence on the ability to drive vehicles and complex mechanisms
Caution should be exercised in patients in whose work an increased concentration of attention and speed of psychomotor reactions (control of complex machines and mechanisms, driving a vehicle) are important - due to an existing disease, therapy carried out by Tsipramil, or both at the same time.
Application during pregnancy and lactation
Tsipramil during pregnancy can be prescribed under strict medical supervision after the doctor assesses the ratio of the expected benefit to the possible risk.
When using Tsipramil in late pregnancy, especially during the third trimester, the condition of the newborn should be monitored. In pregnant women, the drug should be withdrawn gradually.
Possible symptoms in newborns during the use of Tsipramil by the mother in late pregnancy: vomiting, instability of body temperature, respiratory distress, constant crying, apnea, cyanosis, seizures, difficulty feeding, hypoglycemia, muscle hyper- and hypotension, hyperreflexia, tremor, irritability, increased neuro-reflex excitability, lethargy, restless sleep and drowsiness. These symptoms may appear as a consequence of a withdrawal syndrome or serotonergic action. Usually, complications develop immediately after or shortly (<24 hours) after delivery.
According to epidemiological data, it can be assumed that the use of Tsipramil during pregnancy, especially in the later stages, increases the likelihood of persistent pulmonary hypertension in newborns. The observed risk was about 5 cases per 1000 pregnancies (the risk of this disorder in the general population is 1–2 cases per 1000 pregnancies).
Citalopram passes into breast milk. It is believed that infants receive approximately 5% of the maternal daily dose of citalopram (based on weight in mg / kg). For children, practically no consequences were observed. However, to assess the risks, the available information is insufficient, and therefore, taking Tsipramil during breastfeeding is not recommended.
Pediatric use
Cipramil therapy is contraindicated for patients under 18 years of age.
With impaired renal function
With severe renal failure (in patients with creatinine clearance below 30 ml / min), Tsipramil should be used under medical supervision.
For violations of liver function
Tsipramil with severe hepatic insufficiency is used with caution (careful dose selection is recommended).
Use in the elderly
Cipramil therapy in elderly patients should be carried out under medical supervision (dose reduction is recommended).
Drug interactions
There are currently no data on the chemical incompatibility of citalopram with other substances / drugs.
Pharmacological interaction of Tsipramil with other drugs:
- MAO inhibitors: possible serotonin intoxication with the subsequent development of a hypertensive crisis;
- sumatriptan and other serotonergic drugs: citalopram may enhance their effects;
- cimetidine: moderately increases the equilibrium concentration of citalopram in the blood (it is recommended to use the maximum doses of Cipramil in combination with high doses of cimetidine with caution);
- alcohol: no interaction with the drug has been identified, however, it is not recommended to use Tsipramil simultaneously with alcohol;
- phenothiazines and tricyclic antidepressants: no clinically significant pharmacokinetic interaction with citalopram has been established;
- benzodiazepines, antipsychotics, analgesics, lithium preparations, antihistamines and antihypertensive agents, β-blockers and other cardiotropic drugs: no pharmacodynamic interaction was found in clinical studies.
Analogs
Analogs of Tsipramil are: Oprah, Pram, Sedopram, Siozam, Umoral, Tsitalift, Tsitalon, Tsitalopram, Tsitalorin, Tsitol, etc.
Terms and conditions of storage
Store out of the reach of children at a temperature not exceeding 30 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tsipramil
According to reviews, Tsipramil is an effective drug. It is noted that its action develops gradually. Side effects most often occur at the beginning of use, when changing the dosage, and also at the end of the course. The cost of the drug is estimated to be high.
Price for Tsipramil in pharmacies
The approximate price for Tsipramil (14 or 28 tablets of 20 mg) is 869–1126 or 1522–1995 rubles.
Tsipramil: prices in online pharmacies
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Drug name Price Pharmacy |
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Tsipramil 20 mg film-coated tablets 28 pcs. 2034 RUB 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!
