Instruction for use: Fexofenadine

The Latin name of the substance Fexofenadine

Fexofenadinum (genus. Fexofenadini)

Chemical name

(±) -4- [1-Hydroxy-4- [4- (hydroxydiphenylmethyl) -1-piperidinyl) butyl] -alpha, alpha-dimethylbenzeneacetic acid (and as hydrochloride)

Gross formula

C₃₂H₃₉NO₄

Pharmacological group:

H1-Antihistamines

The nosological classification (ICD-10)

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

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

CAS Code

83799-24-0

Characteristics of the substance Fexofenadine

Fexofenadine hydrochloride is a white or colorless crystalline powder. Easily soluble in methanol and ethanol, slightly soluble in chloroform and water, insoluble in hexane.

Pharmacology

Pharmacological action - anti-allergic, antihistamine.

Selectively blocks peripheral histamine H1 receptors, stabilizes the membranes of mast cells, prevents the release of histamine. Eliminates allergy symptoms: sneezing, rhinorrhea, itching, redness of the eyes and lacrimation. The antihistamine effect is manifested after 1 hour after administration, reaches a maximum after 2-3 hours and persists for 12 hours or more. During 28 days of continuous use, there was no development of tolerance. It has no cholino- and adrenolytic, sedative effect. Does not cause changes in the function of calcium and potassium channels, the QT interval. Inhibits bronchospasm caused by histamine in animals.

In vitro reduces the basal expression of adhesion molecules on the epithelial cells of the human conjunctiva and inhibits the migration of leukocytes to the focus of inflammation. Suppresses the spontaneous release of interleukin-6 from fibroblasts induced by activated eosinophils by the release of interleukin-8, granulocyte-macrophage colony-stimulating factor and soluble adhesion molecules from nasal epithelial cells obtained from patients with seasonal allergic rhinitis.

In experimental studies, no carcinogenic, mutagenic and teratogenic effects were detected. When used at a dose of 150 mg / kg and above, a dose-related decrease in the number of implants, an increase in the frequency of postimplantation death of the fetus, a decrease in body weight and survival of the offspring in rats were noted.

Quickly and completely absorbed from the digestive tract. Cmax in plasma is observed after 2.6 hours after administration. Binding to plasma proteins (mainly with albumins and alpha1-glycoproteins) is 60-70%. The average concentration in plasma in healthy subjects after a single oral administration at a dose of 60 mg to 209 ng / ml, the equilibrium level after repeated administration is 286 ng / ml. After taking in doses of 120 mg / day and 180 mg / day single Cmax is 427 ng / ml and 494 ng / ml, respectively. Pharmacokinetics is practically linear with daily intake in the dose range of 40-240 mg. It does not penetrate the GEB, it is secreted into breast milk. AUC - 1521 mcg / l / h, T1 / 2 - 14.4 h. Clearance - 3.4 ml / min / kg. Weakly (5%) is metabolized, excreted with feces (80%) and urine (11%). In patients 65 years and older, T1 / 2 does not change, the concentration in the blood increases, but this does not affect the tolerability of the drug. Against the background of renal dysfunction and hemodialysis, Cmax rises, and T1 / 2 lengthens. The pharmacokinetic parameters of fexofenadine in patients with liver diseases vary slightly.

Application of substance Fexofenadine

Allergic rhinitis (vasomotor, seasonal), hay fever, hives.

Contraindications

Hypersensitivity, children under 6 years.

Restrictions

Chronic renal failure, hepatic insufficiency, pregnancy, breast-feeding.

Application in pregnancy and lactation

Perhaps, if the expected effect of therapy exceeds the potential risk to the fetus and newborn.

Action category for fetus by FDA - C.

Side effects of Fexofenadine

From the nervous system: headache, rarely - dizziness, drowsiness or insomnia, <1% - fatigue, weakness.

On the part of the digestive system: <2% - nausea, indigestion, constipation.

On the part of the respiratory system: rarely - rhinorrhea, viral infections of the upper respiratory tract, pain in the throat and chest.

From the cardiovascular system and blood: rarely - leukopenia, anemia.

Other: <1,5% - back pain, myalgia, hyperbilirubinemia, hyperlipidemia, increased AST, rarely - dysmenorrhea.

Interaction

Erythromycin and ketoconazole increase the plasma level (the incidence of side effects does not change). Antatsidy containing aluminum or magnesium hydroxide, reduce bioavailability (with the use of an interval of at least 2 hours). Compatible with omeprazole. Does not enhance the effect of alcohol on the central nervous system.

Overdose

Symptoms: dizziness, drowsiness, dry mouth.

Treatment: gastric lavage, the appointment of activated charcoal, laxatives, symptomatic and supportive therapy. Hemodialysis is ineffective.

Routes of administration

Inside.

Precautions for the substance Fexofenadine

During treatment, the individual reaction should be checked before allowing the patient to work, requiring increased concentration of attention and speed of psychomotor reactions (driving vehicles, working with mechanisms).