Description
Packaging
In the package of 150 doses.
Pharmacological action
Azelastine, a phthalazinone derivative, is a long-acting antiallergic. Azelastine is a selective H i-histamine-blocking agent, it has anti-histamine, anti-allergic and membrane stabilizing effects, reduces capillary permeability and exudation, stabilizes mast cell membranes and prevents the release of biologically active substances (histamine, serotonin, leukotrienocytes, factor, activating factor, etc.), causing bronchospasm and contributing to the development of early and late stages of allergic reactions and inflammation.
Mometasone is a synthetic glucocorticosteroid (GCS) for topical use. It has anti-inflammatory and anti-allergic effects when used in doses at which systemic effects do not occur. It inhibits the release of inflammatory mediators.
Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which leads to a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of metabolic products of arachidonic acid – cyclic endoperoxides, prostaglandins.
Prevents marginal accumulation of neutrophils, which reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, and reduces the rate of infiltration and granulation.
Reduces inflammation by reducing the formation of chemotaxis substance (effect on late allergy reactions), inhibits the development of an immediate allergic reaction (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).
Pharmacokinetics of
azelastine hydrochloride. Bioavailability after iptranasal administration is about 40%. The maximum concentration (Stax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally in a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium plasma concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng / ml.
Doubling the total daily dose to 1.12 inhibits the development of an allergic reaction of an immediate type (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).
Pharmacokinetics of
azelastine hydrochloride. Bioavailability after iptranasal administration is about 40%. The maximum concentration (Stax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally in a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium plasma concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng / ml.
Doubling the total daily dose to 1.12 inhibits the development of an allergic reaction of an immediate type (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).
Pharmacokinetics of
azelastine hydrochloride. Bioavailability after iptranasal administration is about 40%. The maximum concentration (Stax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally in a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium plasma concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng / ml.
Doubling the total daily dose to 1.12 Bioavailability after iptranasal administration is about 40%. The maximum concentration (Stax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally in a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium plasma concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng / ml.
Doubling the total daily dose to 1.12 Bioavailability after iptranasal administration is about 40%. The maximum concentration (Stax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally in a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium plasma concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng / ml.
Doubling the total daily dose to 1.12mg leads to a stable average plasma concentration of azelastine equal to 1.09 ng / ml. However, despite the relatively high absorption in patients, the systemic effect after intranasal administration is approximately 8 times lower than after oral administration of a daily dose of 4.4 mg azelastine hydrochloride, which is a therapeutic oral dose for the treatment of allergic rhinitis.
Intranasal administration in patients with allergic rhinitis causes an increase in plasma azelastine levels compared with healthy subjects. Other pharmacokinetic data have been studied when administered orally. Communication with blood proteins 80 – 90%. It is metabolized in the liver by oxidation with the participation of the cytochrome P450 system with the formation of the active metabolite of desmethylazelastine.
It is excreted mainly by the kidneys in the form of inactive metabolites. The half-life (T1 / 2) of azelastine is about 20 hours, its active metabolite desmethylazelastine is about 45 hours.
Mometasone furoate. With intranasal use, the systemic bioavailability of the mometa zone of the furoate is <1% (with a sensitivity of the determination method of 0.25 pg / ml). A suspension of mometasone is very poorly absorbed in the gastrointestinal tract, and then a small amount of a suspension of mometasone, which can enter the gastrointestinal tract after nasal inhalation, undergoes an active primary metabolism even before excretion with urine or bile. Indications Seasonal allergic rhinitis in adults from 18 years. Contraindications Hypersensitivity to any of the components of the drug. Recent surgical intervention or nasal injury with damage to the nasal mucosa – before wound healing (due to the inhibitory effect of corticosteroids on the healing process). Children under 18 years of age due to a lack of relevant data. Caution: Tuberculosis infection (active and latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection or infection, caused by Herpes simplex with eye damage (as an exception, the drug may be prescribed for the listed infections as directed by a doctor), the presence of untreated infection involving the nasal mucosa in the process. Use during pregnancy and lactation. Adequately planned and buried controlled studies of the drug in pregnant women have not been conducted. Azelastine hydrochloride is able to cause toxicity during fetal development in mice, rats and rabbits. The use of the drug during pregnancy and during breastfeeding is contraindicated. Use during pregnancy and lactation Contraindicated. Composition 1 dose of the spray contains: Active ingredients: azelastine hydrochloride – 140 mcg, mometasone furoate – 50 mcg. Excipients: microcrystalline microcrystalline cellulose (Avicel RC-591) – 0.910 mg, sodium carmellose -0.021 mg, dextrose – 3.500 mg, polysorbate-80 – 0.0175 mg, benzalkonium chloride – 0.014 mg, srdldp neotamum – 0.0007 mg, citric acid monohydrate – 0.0105 mg, sodium citrate – 0.021 mg, purified water – up to 70 mg. Dosage and administration of Iitranasal. Inhalation of the suspension contained in the vial is carried out using a special metering nozzle on the vial. 1 dose of spray (azelastine hydrochloride – 140 mcg / momstasone furoate – 50 mcg) in each nostril 2 times a day in the morning and evening. Duration of treatment – 2 weeks. Side effects The frequency of side effects is defined as follows: Very often:> 1/10
Frequently: <1/10> 1/100
Infrequently: 1/1000
Rarely: <1/1000> 1/10000
Very rare: <1/10000. Disorders of the nervous system: Often: headache, dysgeusia (unpleasant taste) as a result of improper use. namely, with an excessive deviation of the head back during administration. Very rare: dizziness (may be caused by the disease itself). Disorders of the gastrointestinal tract: Rarely: sensation of irritation of the mucous membrane of the pharynx, nausea. Disorders of the respiratory system, chest and mediastinal organs: Often: nosebleeds, discomfort in the nasal cavity (burning sensation, itching), ulceration of the nasal mucosa, sneezing, pharyngitis, sinusitis, upper respiratory tract infection. Immune system disorders: Very rare: hypersensitivity, anaphylactoid reactions. Disorders of the skin and subcutaneous tissue: Very rarely: rash, pruritus, urticaria. General disorder and disorders at the injection site: Very rare: fatigue, drowsiness, weakness (may be caused by the disease itself). With prolonged use of glucocorticosteroids (GCS) in high doses, systemic side effects, including glaucoma and cataracts, may develop. Drug Interaction Azelastine. No clinically relevant interactions with other drugs have been detected with the inganasal administration of azelastip. Mometasone furoate. Combination therapy with loratadine was well tolerated in patients. However, no effect of the drug on the concentration of lor-tadin or its major metabolite in the blood plasma was noted. In these studies, mometasone furoate was not detected in blood plasma (at a sensitivity of the 50 pg / ml determination method). Overdose It is unknown at this time about cases of overdose with inganasal administration. In case of overdose with azelastine as a result of accidental ingestion, disorders of the nervous system (drowsiness, confusion, tachycardia, hypotension) may occur. Therapy of these disorders is symptomatic. Long-term use of glucocorticosteroids in high doses, as well as the simultaneous use of several ACS may inhibit the hypothalamic-pituitary-adrenal system. Due to the low systemic bioavailability of the drug, it is unlikely that that in case of accidental or deliberate overdose, any measures will be required in addition to observation, with the possible subsequent resumption of the drug at the recommended dose. Storage conditions In a dark place at a temperature of 15 25 ° C (do not freeze). Keep out of the reach of children. Expiration 2 years. Do not use after the expiry date stated on the package. Mometasone dosage form dosage form nasal spray Glenmark Pharmaceuticals Ltd., India
