Included in the formulation
АТХ:R.06.A.X.18 Acryvastin
R.06.A.X Other antihistamines for systemic use
Pharmacodynamics:Any allergic reaction occurs with the release of histamine into the systemic circulation. Histamine belongs to the group of biologically active substances, which determine the immune response of the body by type of allergy. He is responsible for such effects as swelling of the mucous membrane of the respiratory tract and related breathing disorders, arterial hypotension up to collapse, swelling of the skin with the appearance of papular rash and so on.The action of histamine develops through binding it to receptors located on target cells. Acryvastin - H1-blocker of the second generation, a representative of a group of ethanolamines.
Acryvastin competitively and reversibly blocks H1-receptors of effector cells. This leads to prevention of spasm of smooth muscles (including bronchospasm), inhibition of development of hyperemia, itching, restoration of normal secretion of exocrine (salivary, lacrimal and other) glands.
Antiallergic and antiexcudative effects begin to appear after 30 minutes, reach a maximum after 1-2 hours and last up to 6-8 hours.The drug shows little cholinolytic activity, as well as a mild sedative effect. In comparison with cetirizine, it has less antihistaminic activity.
Pharmacokinetics:The fastest action develops when ingested. Well absorbed regardless of food intake, relatively evenly distributed in the body. The apparent volume of distribution reaches 0.82 l / kg, but decreases in the elderly and in persons with chronic renal insufficiency. Poorly penetrates the blood-brain barrier. It binds well to plasma proteins - up to 48-52%. The maximum concentration in the serum after taking 8 mg (single dose) of acrivastine is reached after 1.5 hours and is 227 ± 47 ng / ml. The half-life is approximately 1.5 hours. Biotransformation in the liver is insignificant. It is excreted primarily by the kidneys - 84% (mainly in the form of metabolites), with faeces 13%. The hemodialysis session eliminates up to 20% of the drug. Kidney clearance to 2.9 ml / kg per minute.
Indications:Treatment of allergic rhinitis, pollinosis, allergic dermatosis, itchy atopic eczema, symptomatic dermographism, urticaria (chronic idiopathic, cholinergic, cold).
X.J30-J39.J30 Vasomotor and allergic rhinitis
XII.L20-L30.L20 Atopic dermatitis
XII.L20-L30.L30.9 Dermatitis, unspecified
Contraindications:Hypersensitivity to acrivastine or triprolidine. Severe chronic renal insufficiency (creatinine clearance less than 50 ml / min or serum creatinine content above 150 μmol / L). The age is under 12 years. Pregnancy, breast-feeding.
Carefully:In elderly people and people with renal insufficiency, the dose is reduced by 2 times.
Pregnancy and lactation:The action category for fetus by FDA is B. Application in pregnancy and lactation is indicated only if the possible benefit exceeds the potential risk to the fetus. When tested on animals, the teratogenicity of the drug is not proven. Adequate controlled studies in humans have not been conducted.
At the time of taking the drug should stop breastfeeding, as the drug increases excitability in infants. It can inhibit lactation due to weak anticholinergic activity.
Dosing and Administration:Inside, regardless of food intake. Adults and children over 12 years of age - 8 mg 3 times a day.The maximum single dose is 8 mg. The maximum daily dose is 24 mg.
Side effects:From the side of the central nervous system: dizziness, nervousness, insomnia, rarely - drowsiness; an overdose can cause a headache. Allergic reactions: skin rash, angioedema, bronchospasm, erythema polymorph, anaphylaxis.
From the digestive system: with an overdose of possible nausea, vomiting.
Other: dry mouth, pharyngitis, very rarely - dysmenorrhea.
Overdose:Anticholinergic effects: clumsiness or instability, dryness in the oral cavity, nose or throat, flush of blood to the face, shortness of breath. CNS depression (drowsiness) or CNS stimulation (hallucinations, convulsions, restless sleep, tremor). Cardiovascular disorders - rhythm disturbances, hypotension, collapsoid states. Treatment is symptomatic. Do not use respiratory analeptics (cordiamine, doxapram) due to the threat of seizures!
Interaction:Alcohol and drugs that depress the central nervous system (barbiturates, hypnotics, narcotic analgesics, sedatives, tranquilizers and neuroleptics) -increase CNS depression. Allergens used to conduct skin tests - should be canceled antihistamines before the conduct of skin tests due to the possibility of false-negative results.
Anticholinergics or other drugs with anticholinergic activity - increased anticholinergic effects, the development of paralytic intestinal obstruction.
MAO inhibitors, including furazolidone and procarbazine - prolongation and intensification of the inhibitory effect on the central nervous system and the anticholinergic effects of acrivastine.
Drugs that have ototoxic effect - masking symptoms of ototoxic action, such as tinnitus or dizziness.
Photosensitizing agents - enhanced photosensitization.
Special instructions:In the process of treatment, elderly patients need control of kidney function. During the period of use it is not recommended to drink alcohol. Data on the safety of the use of acrivastine in children under 12 years of age are currently not available, and therefore its use in this age group is contraindicated. Impact on the ability to drive vehicles and manage mechanisms
Persons engaged in potentially hazardous activities that require increased attention and rapid mental and motor reactions,caution should be exercised when taking acryvastatin because of its mild sedative effect and possible side effects from the CNS.