Azelastine

Chemical name

4-[(4-Хлорфенил)метил]-2-( гексагидро-1-метил-1H-а��епин-4-ил)-1(2H)-фталазин он (and as hydrochloride)

Gross

C22-H24-Cl-N3-O

Characteristics

Derived phtalazinon. Limited soluble in water, alcohol metilovom and propilenglikole, poorly soluble in ethanol, oktilovom alcohol and glycerine.

Of drugs

The drugs-antigistaminnoe, protiwallergicescoe, мембраностабилизирую щее. Selectively blocking gistaminove H_1-retseptora, reduces the permeability of capillaries and exudation. Degranulatia stops fat cells, suppresses the synthesis or prevents liberation of biologically active substances (histamine, serotonin, lakotriena, тромбоцит-активирующ��й factor, etc.) of bronhospazm and to the development of the early and late stages of allergic reactions and inflammation. In intra reduces itching and zalojennosti the nose, sneeze, the mucus. Reducing allergic symptoms rinita develops over 3h The effect reaches through 4-5 hours and lasts 12 hours Local application in the form of eye drops by lower signs allergic inflammation of the eyes (hyperemia, pain, itching, slezotechenie, swelling century). Dear effect manifests itself after 10 minutes and lasts for 12 C.v experiments on animals have been detected cancer and mutagennogo action. The mice at the dose of 68.6 mg / kg (550 times MRDC for intranasal application) has embriotoksicescoe, fetotoksicescoe and teratogenic effects (external defects and skeletal anomalies). Easily absorbed by mucous membranes lining the airways of a blood concentrations proportional dose. Following intranasal application system bioavailability of 40%, the volume of 14.5 l / mm Associated with the supply of blood to 80-90%. Passes gistogematicalkie barriers, including placental infiltrates the fluids and tissues. Biotransformiroetsa in the liver by oxidation with the system zitohroma R450 with the formation of the active metabolita desmetilazelastina. In a single intranasal instillation desmetilazelastin in plasma is not defined, but in a stable azelastina its level reaches 20-50% azelastina itself. The application of repeated eye drops little in the blood. In reconsidering the application of the dose of 0.56 mg / day in patients with allergic rhinitis, a blood concentrations higher (0.65 ng / ml) than in healthy volunteers (0.27 ng / ml). T_1/2 azelastina-22 hour desmetilazelastina-54 p.m. Report the news, largely in the form of metabolites and exkrethornami disorders (including lactoirute dairy). While renal failure (Cl creatinine less than 50 ml / min) and the AUC C_max (time to achieve it does not change) increased by 70-75%.

Indications

Allergic rhinitis and conjunctivitis (seasonal, year-round).

Pregnancy and lactation

Contraindicated in pregnancy (especially in the first trimester). At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, pregnancy, breast-feeding, child age (eye drops to 4 years nazalny fine-up to 6 years).

Side-Effects

Allergic reactions : skin rash, urticaria, Zud.so the respiratory system : deep chihanya, pharyngitis, cough, shortness of breath, a sense of cynicism in the chest, difficulty breathing, Bronhospazm.so the nervous system : headache, dizziness, Ustalosti.so part of the intestine : a bitter taste in his mouth (19.7%), changing the taste sensations, dry mouth, nausea, Gastralgia.prochie : tachycardia, gematuria, mialgia, increased body mass index; using spray nazalnogo : drowsiness (11.5%), dryness, irritation, burning or itchy nasal mucous membrane; rarely active bleeding; in the fashion eye drops : kongyunctiv irritation; rarely dry eye slezotechenie, feeling foreign body or pain in the eye, swelling, hemos, bleeding in the front chamber eye keratopatia / keratit, erosion or exkoriation cornea eyes, impaired vision, blefarit.

Specific guidance

Using eye drops is not recommended wearing contact lenses.

Patient interaction

Do (mutually) sedative effects of alcohol and other means, oppressive central nervous system. Ketokonazol prevents the azelastina concentration in plasma and zimetidin, oppressing zitohrom R450, it adds.

Overdosing

Symptoms : likely increased Sonlivosti.lechenie : symptomatic.

Precautions

Be wary appoint nazalny similar patients with compromised renal function. Using spray should not be zaprokidawati head ago. During treatment, it is necessary to avoid the use of alcohol and the use of oppressive central nervous system. It should take into account the possibility of dizziness and sleepiness.

Dosing and Administration

Fresh nazalny : route (tentatively clearing bow moves) : 1 dilution (0.14 mgu/0 .14 ml), in each of the bow twice a day to the disappearance of symptoms. The course of treatment is not more than 6 Mes.glaznae drops : kongungualno 1 drop in the eye every morning and evening to the disappearance of symptoms.

Literature

J. Slater, D. Zechnich, Haxby D. Second-antihistamines. A comparative review / / Drugs - 1999 .- V. 57-N-1 P. 31-47.

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