Instruction for use: Astemizole

Latin name of the substance Astemizole

Astemizolum (genus. Astemizoli)

Chemical name

1 - [(4-Fluorophenyl) methyl] -N- [1- [2- (4-methoxyphenyl) ethyl] -4-piperidinyl] -1H-benzimidazole-2-amine

Gross formula

C₂₈H₃₁FN₄O

Pharmacological group of the substance Astemizole

H1-Antihistamines

The nosological classification (ICD-10)

H10.1 Acute atopic conjunctivitis: Allergic conjunctivitis; Allergic eye diseases; Allergic conjunctivitis; Allergic conjunctivitis caused by chemical and physical factors; Allergic rhinoconjunctivitis; Allergic inflammation of the eyes; Spring Qatar; Spring keratitis; Spring conjunctivitis; Conjunctivitis allergic; Year-round allergic conjunctivitis; Exacerbation of pollinosis in the form of rhinoconjunctival syndrome; Acute allergic keratoconjunctivitis; Acute allergic conjunctivitis; Superficial bacterial infection of the eyes; Rhinoconjunctivitis; Seasonal allergic conjunctivitis; Seasonal conjunctivitis; SENSORY; Chronic allergic keratoconjunctivitis; Chronic allergic conjunctivitis

J30 Vasomotor and allergic rhinitis: Allergic rhinopathy; Allergic rhinosinusopathy; Allergic diseases of the upper respiratory tract; Allergic rhinitis; Allergic rhinitis seasonal; Vasomotor runny nose; Prolonged allergic rhinitis; All-year-round allergic rhinitis; All-year allergic rhinitis; Year-round or seasonal allergic rhinitis; All-the-year-round rhinitis of an allergic nature; Rhinitis vasomotor allergic; Exacerbation of pollinosis in the form of rhinoconjunctival syndrome; Acute allergic rhinitis; Edema of the nasal mucosa; Edema of the nasal mucosa; Edema of the mucous membrane of the nasal cavity; Swelling of the nasal mucosa; Swelling of the nasal mucosa; Pollinosis; Permanent allergic rhinitis; Rhinoconjunctivitis; Rhinosinusitis; Rhinosinusopathy; Seasonal allergic rhinitis; Seasonal allergic rhinitis; Hay rhinitis; Chronic allergic rhinitis; Allergic diseases of the respiratory tract

J45 Asthma: Asthma of physical effort; Asthmatic conditions; Bronchial asthma; Bronchial asthma of light course; Bronchial asthma with difficulty in sputum discharge; Bronchial asthma of severe course; Bronchial asthma physical effort; Hypersecretory asthma; The hormone-dependent form of bronchial asthma; Curbing asthma attacks with bronchial asthma; Non-allergic bronchial asthma; Night Asthma; Exacerbation of bronchial asthma; Attack of bronchial asthma; Endogenous forms of asthma; Night attacks of asthma; Cough with bronchial asthma

L20 Atopic dermatitis: Allergic diseases of the skin; Allergic skin disease noninfectious etiology; Allergic skin disease etiology nemikrobnoy; Allergic skin diseases; Allergic skin lesions; Allergic reactions on the skin; atopic dermatitis; Allergic dermatosis; Allergic diathesis; Allergic itching dermatosis; Allergic skin disease; Allergic skin irritation; allergic Dermatitis; atopic Dermatitis; allergic dermatoses; exudative diathesis; Itchy atopic eczema Itchy allergic dermatosis; Allergic skin disease; Cutaneous allergic reaction to drugs and chemicals; Cutaneous reactions to medications; Skin and allergic disease; Acute eczema; common neurodermatitis; Chronic atopic dermatitis; Exudative diathesis

L29 Itching: Itching with partial obstruction of the biliary tract; Dermatitis itchy; Dermatosis with persistent itching; Other itching dermatoses; Itching dermatoses; Itching allergic dermatosis; Itching dermatitis; Itching dermatosis; Itching itch; Excruciating itching; Severe itching; Endogenous itching; Skin itching with dermatosis; Restricted itchy dermatitis; Itching of the skin; Itchy scalp; Itching eczema

L50 Urticaria: Idiopathic chronic urticarial; Injury Urticaria; Chronic urticarial; Hives of the newborn

T78.3 Angioedema: Edema Quincke; Laryngeal exacerbation with angioneurotic edema; Recurrent angioedema; Allergic edema; Recurrent swelling of Quincy

T78.4 Unspecified Allergy: Allergic reactions to insulin; Allergic reactions to insect stings; Allergic reactions similar to systemic lupus erythematosus; Allergic diseases; Allergic diseases of mucous membranes; Allergic diseases and conditions resulting from increased release of histamine; Allergic diseases of mucous membranes; Allergic symptoms; Allergic symptoms in the mucous membranes; Allergic reactions; Allergic reactions caused by insect bites; Allergic reactions; Allergic conditions; Allergic laryngeal edema; allergopathy; allergic conditions; Allergy; House dust allergy; Anaphylaxis; Cutaneous reactions to medications; Skin reaction to insect stings; Cosmetic allergy; Drug allergy; Acute allergic reaction; Laryngeal edema allergic genesis and background radiation; Food and drug allergy

Y40-Y59 Drugs, medicines and biological substances that cause adverse reactions during therapeutic use

CAS code

68844-77-9

Characteristics of the substance Astemizole

White or off-white powder. Insoluble in water, slightly soluble in ethanol, readily soluble in chloroform and methanol.

Pharmacology

Pharmacological action - anti-allergic, antihistamine.

It blocks histamine H1 receptors. Weaken bronchospasm, caused by physical exertion and hyperventilation of the lungs. The action develops within 24 hours (sometimes 2-3 days) and reaches a maximum after 9-12 days. The duration of the effect depends on the duration of the previous therapy (suppression of skin tests may persist for several weeks after discontinuation). Has a weak antiserotonin activity. Practically does not have a sedative effect (does not pass the BBB), does not enhance the depriming effect of ethyl alcohol or other drugs that depress the central nervous system.

In experimental studies, no mutagenic and carcinogenic effects were identified. When administered to rats, a dose 100 times higher than that recommended for humans has a toxic effect on the maternal organism and embryo. In rats and rabbits, at doses 50 times that recommended for humans, it does not have a teratogenic effect and does not change fertility in males and females.

After oral administration, it is rapidly absorbed. Cmax is recorded for 1 hour. Food intake by 60% reduces absorption and extends the time to reach Cmax for 1 hour. Protein binding is 96%. Almost completely metabolized in the liver (including the "first pass") with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system with the formation of an active metabolite - desmethylastamizole, Cmax of which in the blood is reached after 1 hour. The equilibrium total concentration (astemizole and its active metabolite) In the blood is 3-5 ng / ml and is created within 4-6 weeks. Excreted mainly with bile in the form of metabolites (54-73%) and partially with urine (5-6%). T1 / 2 astemizole - 1 day, the volume of distribution - 250 l / kg, Cl - 11 ml / min / kg. The excretion (astemizole + hydroxylated metabolites) is biphasic: T1 / 2 for the distribution phase is 20 hours, for the elimination phase is 7-11 days (with repeated application 7-9 days and 19 days, respectively). According to calculated data, metabolites can remain in the body for up to 4 months. Penetrates the milk of lactating dogs.

Allergic rhinitis (seasonal and year-round), allergic conjunctivitis, allergic skin reactions (chronic idiopathic urticaria, etc.), skin itching, angioedema (treatment and prevention), bronchial asthma (ancillary therapy).

Contraindications

Hypersensitivity, pregnancy, breast-feeding, early childhood (up to 2 years).

Restrictions

Elongation of QT interval on ECG, hypokalemia, expressed violations of liver function.

Application in pregnancy and breastfeeding

Contraindicated in pregnancy.

Action category for fetus by FDA - C.

For the duration of treatment, breastfeeding should be stopped.

Side effects of Astemizole

From the nervous system and sensory organs: weakness, headache, drowsiness, in some cases - dizziness, nervousness, mood disorders, insomnia, nightmares, paresthesia, seizures, rarely - depression, conjunctivitis.

From the cardiovascular system: hypotension, palpitation, at high doses - ventricular arrhythmias, hematopoiesis (fatigue or weakness, sore throat, fever, bleeding or hemorrhage).

On the part of the intestine: dry mouth, increased appetite, nausea, abdominal pain, diarrhea, rarely - increased activity of hepatic transaminases, hepatitis.

Allergic reactions: rarely - rashes, itching, angioedema, bronchospasm, anaphylactoid reactions.

Other: photosensitization, weight gain (in case of prolonged use), myalgia, arthralgia, rarely - pharyngitis.

Interaction

Imidazole antifungal agents (ketoconazole, intraconazole, miconazole, etc.), macrolides (erythromycin, clarithromycin), metronidazole, quinine, mibefradil lower the rate of biotransformation. It is not recommended to combine with HIV protease inhibitors and serotonin reuptake inhibitors. Drugs that extend the QT interval (antiarrhythmics, terfenadine, tricyclic antidepressants, phenothiazines, calcium channel blockers, etc.), potentiate cardiotoxicity. May mask the ototoxic effect of other drugs. Enhances the side effects of photosensitizing agents.

Overdose

Symptoms: ventricular arrhythmias, syncope, convulsions, cardiac or respiratory arrest.

Treatment: induction of vomiting, gastric lavage, intake of activated charcoal, saline laxatives; ECG monitoring, symptomatic and supportive therapy, if necessary - intravenous fluid administration, the appointment of antiarrhythmic drugs that do not extend the QT interval, hypertensive drugs (adrenaline and analeptic administration is not recommended), oxygen therapy. Hemodialysis is ineffective.

Precautions for the substance Astemizole

It is not recommended to take grapefruit juice at the same time (inhibits metabolism and increases concentration in the blood). With caution appoint patients with kidney disease, impaired electrolyte metabolism (hypokalemia, hypomagnesemia), receiving non-potassium-sparing diuretics. Patients with diseases of the lower respiratory tract should be warned of potential cholinolytic effects (dry mucous membranes). Use with caution to treat patients whose work requires increased attention and speed of physical and mental reactions.

Special instructions

It is recommended to stop using at least 4 weeks before the skin test for allergens.