Last Updated on February 19, 2017 by Dr.Derek Fhisher

Astelin Azelastine 10 ml
Most popular brand: Astelin
Active ingredient: Azelastine
Available dosage forms: 10 ml
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Azelastine general information

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It’s proving particularly effectual in preventing underage alcohol usage. It’s going to vary dependent on the seriousness of the alcohol usage. It might be higher, obviously, in dishes where in fact the alcohol is simply splashed in at the end of cooking. For some reason, there seems to become a poetic link between the moon and alcohol.

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azelastine (Azelastine): instruction, and the use of a formula

Therapeutic substance azelastine

The nosological classification (ICD – 10)

Code CAS

substance azelastine features

phthalazinone derivative. Azelastine hydrochloride ; white crystalline powder bitter taste, and odorless. Limited soluble in water, methanol and propylene glycol, slightly soluble in ethyl, octyl alcohol and glycerin. Molecular weight 418,37.

Pharmacology

Mode of action – antiallergic, antihistamine, membrane.

Selectively blocking histamine H 1 – receptors, reduces capillary permeability and exudation. It stops the degranulation of mast cells, inhibits the synthesis or prevents liberatiou biologically active substances (histamine, serotonin, leukotrienes, platelet – activating factor, and others.) That cause bronchoconstriction and contributing to the development of early and late stage allergic reactions and inflammation.

When administered intranasally reduces itching and stuffy nose, sneezing, mucus. Easing the symptoms of allergic rhinitis develops within 3 hours maximum effect is achieved through 4 –. 5 hours and lasts 12 hours.

The local application in the form of eye drops is accompanied by a decrease in symptoms of allergic inflammation of the eyes (redness, pain, itching, watery eyes, swelling of the eyelids). Ophthalmic effect appears in 10 minutes and maintained for 12 hours.

In animal experiments revealed no carcinogenic and mutagenic effects. In mice at a dose of 68.6 mg / kg (550 times the MRDCH for intranasal use) has embryotoxic, foetotoxic and teratogenic (external defects and skeletal abnormalities).

It is easy absorbed by the mucous membranes of the respiratory tract, it produces blood concentrations proportional to dose. After intranasal application of systemic bioavailability is 40%, V d ; 14.5 L / kg. Associated with the blood supply to the 80 – 90%. Passes gistogematicalkie barriers, including the placenta, and the liquid penetrates the fabric. Biotransformed in the liver by oxidation with cytochrome P450 to the active metabolite desmetilazelastina. The terms single intranasal instillation plasma desmetilazelastin not determined, but the background concentration of azelastine its stable level reaches 20 – 50% azelastine thereof. Repeated application of eye drops hardly detected in the blood. Repeated application in 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). T 1/2 azelastine ; 22 hours, desmetilazelastina ; 54 h. Largely excreted by the kidneys as metabolites and excretory glands (including lactating dairy). In patients with renal insufficiency (Cl creatinine less than 50 mL / min), the AUC and C max (time to achieve it does not change) increased by 70 – 75%.

Application of the substance azelastine

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

Contraindications

Hypersensitivity, pregnancy, breast-feeding, child age (eye drops ; up to 4 years, nasal spray ; up to 6 years old).

Application of pregnancy and breastfeeding

is contraindicated during pregnancy (especially in I trimester).

Category effects on the fetus by FDA ; C.

breast-feeding should be discontinued at the time of treatment.

Side effects of substance azelastine

Allergic reactions: skin rash, hives, itching,.

From the respiratory system: sneezing fits, sore throat, cough, shortness of breath, feeling of tightness in the chest, shortness of breath, bronchospasm.

From the nervous system: headache, dizziness, 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 nasal spray: somnolence (11.5%), dryness, irritation, burning, or itching of the nasal mucosa; rare ; nose bleed; when applied eye drops: irritation of the conjunctiva; rare ; 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 cornea, blurred vision, blepharitis.

Interaction

(mutually) the sedative effect of alcohol and other CNS depressants. Ketoconazole inhibits the definition of azelastine plasma concentrations, and cimetidine, inhibiting cytochrome P450, it increases.

Overdose

Symptoms: is likely hypersomnia.

Dosing and Administration

nasal spray: intra-nasally (pre-clearing the nasal passages): 1 spray (0.14 mg / 0.14 ml) in each nostril 2 times a day until the disappearance of symptoms. The course of treatment is not more than 6 months.

Eye drops: conjunctival 1 drop in each eye in the morning and evening until disappearance of symptoms. If necessary, increase the dose to 4 – times a day by one drop in each eye.

Precautions substance azelastine

With care prescribe a nasal spray in patients with impaired renal function. When using the spray should not be to throw back his head back.

During treatment should avoid alcohol and the use of CNS depressants. Keep in mind the possibility of dizziness and drowsiness.

Cautions

If you are using eye drops is not recommended to wear contact lenses.

azelastine (eye drops) can be used for the treatment of infectious diseases of the eye only in the combined therapy on doctor’s advice.

In the case of concomitant therapy with other eye drops should be instilled in their eyes at intervals of not less than 15 minutes.

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