Cytisine (Cytisinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

N-holinomimetiki

Means for correcting disorders in alcoholism, toxic and drug addiction

Included in the formulation
  • Tabex®®
    pills inwards 
    Sopharma, AO     Bulgaria
    • АТХ:

    N.07.B.A   Drugs used in nicotine addiction

    Pharmacodynamics:

    Alkaloid cytisine, which is an active substance of the drug, has an n-cholinomimetic effect; excites the ganglion of the autonomic nervous system, reflexively stimulates the respiratory center, causes adrenaline release from the adrenal medulla, raises blood pressure.

    With a close resemblance to the mechanism of action of nicotine cytisine has a much lower toxicity and a greater therapeutic index.

    Cytisine competitively suppresses the interaction of nicotine with the corresponding receptors, which leads to a gradual decrease and disappearance of nicotine (tobacco) dependence.

    Pharmacokinetics:

    Data on pharmacokinetics are not available.

    Indications:

    Nicotine addiction (to facilitate quitting).

    ICD-10

    V.F10-F19.F17   Mental and behavioral disorders caused by tobacco use

    XXI.Z70-Z76.Z72.0   Tobacco use

    XIX.T51-T65.T65.2   Toxic effect of tobacco and nicotine

    Contraindications:

    Hypersensitivity, acute myocardial infarction, unstable angina, arrhythmia, recently suffered impaired cerebral circulation, severe atherosclerosis,bleeding from large vessels, arterial hypertension, pulmonary edema, bronchial asthma, peptic ulcer of the stomach and duodenum in the acute stage, pregnancy, breastfeeding.

    The medicinal preparation in the form of tablets contains an auxiliary substance - lactose. Patients with rare hereditary problems of galactose intolerance, lactase deficiency (Lapp type) or glucose-galactose malabsorption should not use this form.

    Carefully:

    Schizophrenia, chromaffin adrenocortical tumors, gastroesophageal reflux, ischemic heart disease, chronic heart failure, cerebral vascular disease, hyperthyroidism, peptic ulcer of the stomach, diabetes mellitus, renal and / or hepatic insufficiency, age 18 and over 65.

    Pregnancy and lactation:It is not recommended in pregnancy because of the potential risk of embryotoxic action with uncontrolled admission. It is not recommended to take during breastfeeding.
    Dosing and Administration:

    Tablets are taken orally according to the following scheme: the first 3 days - 1.5 mg (1 tablet) with an interval of 2 hours (6 tablets per day) with a simultaneous decrease in the number of cigarettes smoked.In the absence of efficacy, discontinue treatment, and repeat after 2-3 months. With a good effect, the treatment is continued according to the following scheme: from the 4th to the 12th day, 1.5 mg (1 tablet) at intervals of 2.5 hours (5 tablets per day), from the 13th to the 16th day - 1.5 mg every 3 hours (4 tablets per day), from the 17th to the 20th day - 1.5 mg every 5 hours (3 tablets a day), from the 21st to the 25th day - 1,5-3,0 mg per day (1-2 tablets a day). Smoking should be discontinued no later than the 5th day after the start of treatment.

    Adhesive-TDTS (125 mg / 30 cm2) are glued onto a skin area without hair (usually on the inner surface of the forearm) that is not subjected to mechanical attack, pre-treated with alcohol or water. The dose is selected individually, cutting the TDTC into appropriate parts, the duration of a one-time application is 2-3 days. Course treatment (1-3 weeks) consists of successive applications of TDTS (each successive TDTT is glued to a symmetrical area of ​​the skin of the other hand) with a 1-2 h interval for hygienic procedures (after removing the TDTS the place of application is washed with soap and water).

    Films are glued on the gum or buccal mucosa 4-8 times a day in the first 3-5 days, then (in the presence of a positive effect) according to the following scheme: from the 5th to the 8th day - 1 film 3 times a day ,from the 9th to the 12th day - 1 film 2 times a day, from 13th to 15th day, 1 film once a day.

    Side effects:

    From the side organs of the digestive tract: change in taste and appetite, dry mouth, abdominal pain, nausea, constipation, diarrhea.

    From the side nervous system and sense organs: headache, dizziness, insomnia, drowsiness, increased irritability.

    From the side cardiovascular system and blood (hematopoiesis, hemostasis): heart palpitations, tachycardia, increased blood pressure, pain in the chest.

    Other: allergic reactions (itching, rash, eosinophilia), myalgia, dyspnea, weight loss, increased sweating.

    Overdose:

    Symptoms: nausea, vomiting, dilated pupils, general weakness, tachycardia, convulsions, respiratory paralysis.

    Treatment: gastric lavage (with oral intake), heart rate control, blood pressure, respiratory function, if necessary - the introduction of infusion solutions, anticonvulsants, cardiotonic, analeptic and other symptomatic agents.

    Interaction:

    Do not share TSTD with other drugs that have a similar mechanism of action or side effects.

    After smoking cessation, the side effects of theophylline, ropinirole, clozapine and olanzapine may increase.

    When used simultaneously with acetylcholine, carbachol, galantamine, pyridostigmine, revastigmine, distigmine, cholinomimetic side effects may increase (salivation, lacrimation, bronchial secretion with a cough and the risk of an asthma attack, pupil narrowing, colic, nausea, vomiting, frequent urination, increased muscle tone or sudden muscle contractions).

    The area of ​​skin with TDTS should not be exposed to water.

    Do not use cytisine simultaneously with anti-tuberculosis drugs.

    Application simultaneously with inhibitors of HMG-CoA reductase (including lovastatin, simvastatin, fluvastatin, pravastatin) increases the risk of pain in the muscles.

    Simultaneous use with antihypertensive drugs (including propranolol) can weaken their effect.

    Special instructions:

    When used for smoking cessation, a positive result is possible only with a firm decision of the smoker to quit smoking.

    The patient should be warned that the use of the drug against the background of continued smoking can lead to nicotine intoxication.

    Although there was no adverse effect on the ability to drive vehicles and work with the mechanisms, despite the use of the drug, however, due to the possible occurrence of drowsiness and other adverse reactions, care should be taken in the listed situations.

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