Pharmacology Astepro Nasal Spray
Pharmacological action – anti-allergic, antihistamine, membrane.
Selectively blocks the histamine H1-receptors, reduces capillary permeability and exudation. Inhibits degranulation of mast cells, inhibits the synthesis or prevents liberatsii biologically active substances (histamine, serotonin, leukotrienes, platelet-activating factor, etc.) that cause bronchoconstriction and promote the development of early and late phase allergic reactions and inflammation. When intranasal administration reduces itching and nasal nose, sneezing, mucus production. Attenuation of allergic rhinitis symptoms develop within 3 h. The effect reaches a maximum after 4-5 h and lasts for 12 h. The local application in the form of eye drops is accompanied by a decrease in symptoms of allergic inflammation of the eye (redness, pain, itching, watery eyes, swelling of the eyelids). Ophthalmic effect appears after 10 minutes and lasts for 12 hours
In animal experiments revealed no carcinogenic and mutagenic effects. In mice at a dose of 68.6 mg / kg (up to 550 times the MRDCH for intranasal use) has embryotoxic, and teratogenic effects fetotoksicheskoe (external defects and abnormalities of the skeleton).
Readily absorbed from the mucous membranes of the respiratory tract, creating in the blood concentrations proportional to dose. After intranasal application of systemic bioavailability of 40%, volume of distribution – 14.5 L / kg. Binds to blood proteins by 80-90%. Passes gistogematicheskie barriers, including placental, fluid and penetrates into the tissue. Biotransformed in the liver by oxidation with cytochrome P450 to the active metabolite desmetilazelastina. In a single intranasal instillation desmetilazelastin in plasma is not defined, but against the background of a stable concentration of azelastine its level reaches 20-50% that of azelastine. Repeated application of eye drops is almost not detectable in the blood. When you use a dose of 0.56 mg / day in patients with allergic rhinitis, creates a higher blood concentration (0.65 ng / ml) than in healthy volunteers (0.27 ng / ml). T1 / 2 azelastine – 22 hours, desmetilazelastina – 54 hours is deduced by kidneys primarily as metabolites and excretory glands (including lactating dairy). Against the background of renal impairment (Cl creatinine less than 50 ml / min) AUC and Cmax (time to achieve it does not change) increased by 70-75%.
Application of Astepro Nasal Spray
Allergic rhinitis and conjunctivitis (seasonal and year-round).
Contraindications Astepro Nasal Spray
Hypersensitivity, pregnancy, lactation, infancy (eye drops – up to 4 years old, nasal spray – up to 6 years).
Pregnancy and breast feeding Astepro Nasal Spray
Contraindicated in pregnancy (especially in the I trimester).
Category of the fetus by FDA – C.
At the time of treatment should stop breastfeeding.
Side effects Astepro Nasal Spray
Allergic reactions: skin rash, hives, itching.
The respiratory system: seizures sneezing, sore throat, cough, shortness of breath, feeling of tightness in the chest, shortness of breath, bronchospasm.
The nervous system: headache, dizziness and fatigue.
From the digestive tract: a bitter taste in the mouth (19.7%), change in taste, dry mouth, nausea, gastralgia.
Other: tachycardia, hematuria, myalgia, weight gain, using a nasal spray: somnolence (11.5%), dryness, irritation, burning or itching of the nasal mucosa, rarely – nasal bleeding when applied eye drops: irritation of the conjunctiva, rarely – dry eyes, tearing, foreign body sensation or pain in the eye, swelling, chemosis, hemorrhage into the anterior chamber of the eye, keratopathy / keratitis, erosion, or excoriation of the cornea, blurred vision, blepharitis.
Interaction Astepro Nasal Spray
Increases (relatively) sedative effect of alcohol and other means of CNS depressants. Ketoconazole prevents the determination of the concentration of azelastine in the blood plasma, and cimetidine, by inhibiting cytochrome P450, its increases.
Overdose Astepro Nasal Spray
Symptoms: The possibility of an increased drowsiness.
Treatment: symptomatic.
Dosage and administration Astepro Nasal Spray
Astepro Nasal Spray: Intranasal (pre-clearing the nasal passages): 1 spray (0.14 mg / 0.14 ml) in each nostril 2 times a day until symptoms of the disease. The cure is not more than 6 months.
Eye drops: conjunctival 1 drop in each eye, morning and evening until symptoms of the disease. If necessary, increase the dose up to 4 times a day, one drop in each eye.
Precautions Astepro Nasal Spray
With care prescribe a nasal spray in patients with impaired renal function. When using the spray should not throw back your head back. During treatment, the need to avoid alcohol and use of CNS depressants. Keep in mind the possibility of dizziness and drowsiness.
Cautions
When using the eye drops do not recommend wearing contact lenses.
Azelastine (eye drops) can be used to treat infectious diseases of the eye only in the treatment of a doctor’s recommendation.
