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H 1 - histamine blocker is a derivative of ethanolamine.
Antipruritic, anti-allergic. Reduces vascular permeability. It has a sedative and M-anticholinergic effect. Does not possess hypnotic activity. Prevents the development of vasodilation and smooth muscle contractions induced by histamine. Reduces capillary permeability. Inhibits exudation and the formation of edema, reduces itching.
Antihistamine activity of the drug reaches a maximum after 5-7 hours, persists for 10-12 hours, and in some cases - up to 24 hours.
After ingestion, clemastine is almost completely absorbed from the gastrointestinal tract. The maximum concentration in plasma is reached in 2-4 hours. Communication with plasma proteins is 95%. Removal from plasma in two phases, the corresponding elimination half-life is 3.6 ± 0.9 hours and 37 ± 16 hours.
Clemastine undergoes significant metabolism in the liver. Metabolites are mainly (45-65%) excreted through the kidneys with urine; unchanged active substance is found in urine only in trace amounts.
During lactation, a small amount of clemastin can pass into breast milk.
- Hay fever (allergic rhinoconjunctivitis);
- urticaria of different origin;
- itching, itchy dermatosis;
- acute and chronic eczema, contact dermatitis;
- drug allergy;
- insect bites and stings.
1 tablet contains:
Active substances: clemastine 1 mg, equivalent to 1.34 mg of clemastine hydro-fumarate.
Excipients: lactose monohydrate, povidone (polyvinylpyrrolidone), corn starch, magnesium stearate, talc.
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Dosage and Administration
Adults and children over 12 years old: appoint 1 tablet (1 mg) in the morning and evening. In cases difficult to treat, the daily dose can be up to 6 pills (6 mg). pills should be taken before meals with water.
Children aged 6-12 years: appoint 1 / 2-1 tablet before breakfast and at night.
From the side of the central nervous system: possible fatigue, drowsiness, headache, dizziness, tremor, sedation, weakness, fatigue, lethargy, loss of coordination of movements; in rare cases, especially in children, a stimulating effect on the central nervous system is noted: anxiety, irritability, agitation, nervousness, insomnia, hysteria, euphoria, convulsions, paresthesia, and neuritis.
From the gastrointestinal tract: dyspepsia, nausea, epigastric pain, constipation, vomiting; rarely, dry mouth, occasional loss of appetite and diarrhea.
From the senses: violation of the clarity of visual perception, diplopia, acute labyrinthitis, tinnitus.
From the urinary system: very rarely - frequent or difficult urination.
On the part of the respiratory system: rarely - thickening of bronchial secretions and difficulty in expectoration of the sputum, a feeling of pressure in the chest and difficulty breathing, nasal congestion.
Since the cardiovascular system: rarely - lowering blood pressure (more often in elderly patients), heartbeat, extrasystole.
From the side of blood-forming organs: hemolytic anemia, thrombocytopenia, agranulocytosis.
Allergic reactions: very rarely - urticaria, skin rash, photosensitivity, anaphylactic shock.
Carefully: in patients with stenosing gastric ulcer; pyloroduodenal obstruction; with bladder neck obstruction; prostatic hypertrophy accompanied by urinary retention; with increased intraocular pressure; hyperthyroidism; diseases of the cardiovascular system, including arterial hypertension.
Tavegil enhances the action of drugs that depress the central nervous system (hypnotics, sedatives, anxiolytics), M-holinoblokatorov, as well as alcohol.
Not compatible with the simultaneous use of MAO inhibitors.
Pregnancy and Lactation
During pregnancy, Tavegil is used only if the expected benefit to the mother outweighs the potential risk to the fetus.
To prevent distortion of the results of skin scarification tests for allergens, the drug should be canceled 72 hours before the allergic testing.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
Patients taking Tavegil, it is recommended to refrain from driving vehicles, working with mechanisms, as well as from other activities that require high concentration of attention and psychomotor speed reactions.
Symptoms: An overdose of antihistamines can lead to both depressing and stimulating effects on the central nervous system. CNS stimulation is more common in children. Phenomena of anticholinergic action may also develop: dry mouth, fixed pupil dilation, blood rush to the upper half of the body, disorders of the gastrointestinal tract (nausea, epigastric pain, vomiting).
Treatment: if the patient does not vomit spontaneously, then it should be called up (only if the patient’s consciousness is preserved). If 3 hours or a little more has passed since the drug was taken, it is necessary to wash the stomach with 0.9% sodium chloride solution and activated charcoal. You can also assign a saline laxative. Symptomatic therapy is also indicated.
- Brand name: Tavegil
- Active ingredient: Clemastine
- Dosage form: Pills.
- Manufacturer: Novartis
- Country of Origin: Switzerland
Studies and clinical trials of Clemastine (Click to expand)
- Dual CD system-modified MEEKC method for the determination of clemastine and its impurities
- Development and full validation of a sensitive quantitative assay for the determination of clemastine in human plasma by liquid chromatography–tandem mass spectrometry
- Effect of clemastine on the ECG in healthy volunteers
- Determination of clemastine in human plasma by gas chromatography with nitrogen–phosphorus detection
- Pharmacokinetics and pharmacodynamics of clemastine in healthy horses
- Pharmacodynamics of clemastine in healthy horses
- Identification of some new clemastine metabolites in dog, horse, and human urine with liquid chromatography/tandem mass spectrometry
- Structural elucidation of N-oxidized clemastine metabolites by liquid chromatography/tandem mass spectrometry and the use of Cunninghamella elegans to facilitate drug metabolite identification
- Placebo controlled comparison of acute effects of ebastine and clemastine on performance and EEG
- A comparison of triprolidine and clemastine on histamine antagonism and performance tests in man: Implications for the mechanism of drug induced drowsiness
- Evaluation ofin vivoparameters of drug metabolizing enzyme activity in man after administration of clemastine, phenobarbital or placebo
- Histamine1-histamine2antagonism: Effect of combined clemastine and cimetidine pretreatment on allergen and histamine-induced reactions of the guinea pig lungin vivoandin vitro
- Effects of mizolastine and clemastine on actual driving and psychomotor performance in healthy volunteers
- Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the h1receptor antagonist clemastine
- Inhibition of mast cell degranulation-induced drop of blood pressure with clemastine, cromolyn and compound 48/80 pretreatment
- The effect of ranitidine and clemastine, alone and in combination, on histamine and allergen-induced cutaneous weal and flare reactions
- A comparison of ketotifen with clemastine, ipratropium bromide and sodium cromoglycate in exercise-induced asthma
- Toxic Pustuloderma associated with clemastine therapy
- Clinical pharmacology of clemastine in healthy dogs
- Acrivastine Versus Clemastine in the Treatment of Chronic Idiopathic Urticaria : A Double-Blind, Placebo-Controlled Study
- Effects of Ketotifen and Clemastine on Passive Transfer of Reaginic Reaction
- A multicentre study of loratadine, clemastine and placebo in patients with perennial allergic rhinitis
- Identification of Urinary Metabolites of Clemastine after Oral Administration to Man
- Risk of developing life-threatening ventricular arrhythmia associated with terfenadine in comparison with over-the-counter antihistamines, ibuprofen and clemastine