Azelastine (Azelastinum)

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

H1-antihistamines

Included in the formulation
  • Allergodyl®
    drops d / eye 
    Meda Pharma GmbH & Co. KG     Germany
  • Allergodyl®
    spray nazal. 
    Meda Pharma GmbH & Co. KG     Germany
  • Allergodil® C
    spray nazal. 
    Meda Pharma GmbH & Co. KG     Germany
    • АТХ:

    R.01.A. C.03   Azelastine

    Pharmacodynamics:

    Competitive reversible blocker of histamine H1-receptors, antiallergic, antihistamine, membrane stabilizing agent.

    Reduces capillary permeability and exudation. It inhibits degranulation of mast cells, suppresses synthesis or prevents the liberation of biologically active substances (histamine, serotonin, leukotrienes, platelet-activating factor and others) that cause bronchospasm and promote the development of early and late stage of allergic reactions and inflammation.

    With intranasal administration reduces itching and stuffiness in the nose, sneezing, mucus secretion.

    Local application in the form of eye drops is accompanied by a decrease in signs of allergic inflammation of the eyes (hyperemia, soreness, itching, lacrimation, swelling of the eyelids).

    Pharmacokinetics:

    Easily absorbed from the mucous membranes of the respiratory tract, creates in the blood concentrations proportional to the dose. After intranasal application, the system bioavailability is 40%, the volume of distribution is 14.5 l / kg. It binds to blood proteins by 80-90%.Passes gistogematicalkie barriers, including placental, penetrates into liquids and tissues. Biotransformiruetsya in the liver by oxidation involving the cytochrome P450 system with the formation of an active metabolite desmethylazelastine. In the conditions of a single intranasal instillation, desmethylazelastine is not detected in the blood plasma, but against a background of stable concentration of azelastine, its level reaches 20-50% of that azelastine. With repeated use of eye drops is practically not determined in the blood. Half-life azelastine - 22 hours, desmethylazelastine - 54 hours. It is excreted by the kidneys mainly in the form of metabolites and excretory glands (including lactating dairy).

    With intranasal administration, the alleviation of symptoms of allergic rhinitis develops within 3 hours. The effect reaches a maximum in 4-5 hours and lasts 12 hours.

    The ophthalmic effect is manifested after 10 minutes and lasts for 12 hours.

    Indications:

    Conjunctivitis, rhinoconjunctivitis, all-the-year-round / seasonal rhinitis.

    ICD-10

    VII.H10-H13.H10.1   Acute atopic conjunctivitis

    X.J30-J39.J30   Vasomotor and allergic rhinitis

    X.J30-J39.J30.1   Allergic rhinitis caused by pollen of plants

    X.J30-J39.J30.3   Other allergic rhinitis

    Contraindications:

    Hypersensitivity, pregnancy (especially I trimester), breastfeeding, children's age (up to 6 years - nasal spray, up to 4 years - eye drops).

    Carefully:

    Kidney disease (nasal spray).

    Pregnancy and lactation:

    Category FDA - B. The drug can not be used in I trimester of pregnancy.

    There is no information on the penetration into breast milk. The use is not recommended, the drug increases excitability in infants. Can inhibit lactation due to anticholinergic activity. Do not apply!

    Dosing and Administration:

    Oral: 2 mg at night.

    Spray nasal: intranasally (after clearing the nasal passages): 1 spray (0.14 mg / 0.14 ml) in each nasal passage 2 times a day until the symptoms disappear. The course of treatment is not more than 6 months.

    Eye drops: Conjunctivally 1 drop in each eye in the morning and evening until the symptoms disappear. If necessary, increase the dose to 4 times a day, one drop in each eye.

    Side effects:

    Allergic reactions: skin rash, hives, itching.

    On the part of the respiratory system: bouts of sneezing, pharyngitis, cough, shortness of breath, a feeling of tightness in the chest, shortness of breath, bronchospasm.

    From the nervous system: headache, dizziness, fatigue.

    On the part of organs GIT: bitter taste in the mouth (dysgeusia), a change in taste, dry mouth, nausea, gastralgia.

    Other: tachycardia, hematuria, myalgia, weight gain; when using nasal spray: drowsiness, dryness, irritation, burning or itching of the nasal mucosa; rarely - epistaxis; with the application of eye drops: irritation of the conjunctiva; rarely - dry eyes, tearing, foreign body sensation or eye pain, swelling, chemosis, hemorrhage into the anterior chamber of the eye, keratopathy / keratitis, corneal erosion or excoriation eyes, blurred vision, blepharitis.

    Overdose:

    Anticholinergic effects: clumsiness or instability, dryness in the oral cavity, nose or throat, flush of blood to the face, shortness of breath. Anticholinergic effects are less likely compared with diphenhydramine or promethazine.CNS depression (drowsiness) or CNS stimulation (hallucinations, convulsions, restless sleep); hypotension.

    Treatment is symptomatic. Do not use respiratory analeptics - they can cause the development of seizures!

    Interaction:

    Ketoconazole and cimetidine helps increase the concentration of the drug in the blood plasma.

    Means that depress the central nervous system (barbiturates, hypnotics, narcotic analgesics, sedatives, tranquilizers and neuroleptics), alcohol - increased oppression of the central nervous system.

    Special instructions:

    When using eye drops, contact lenses are not recommended. When using the drug in complex therapy for the treatment of infectious eye diseases, a doctor's recommendation is needed.

    During treatment it is necessary to avoid drinking alcohol and using drugs that depress CNS. Consider the possibility of dizziness and drowsiness.

    When using a spray, do not throw your head back.

    Nasal spray as a preservative contains benzalkonium chloride, which has irritating effect, and can cause skin reactions.

    Impact on the ability to drive vehicles and manage mechanisms

    In rare cases, fatigue, fatigue, dizziness, or weakness, which may be a consequence of the disease itself, can develop with the use of the drug. In these cases, you should avoid driving the machine and working with complex mechanisms.

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