Momat Rhino Advance, 140 mcg+50 mcg/dose 150 doses spray

A combined anti-allergic agent (H1-histamine receptor blocker + GCS for topical use).

Indications

Symptomatic treatment of seasonal and year-round allergic rhinitis.

Pharmacological effect

Antiallergic agent – H1-histamine receptor blocker + glucocorticosteroid for local use

Pharmacodynamics:
Azelastine, a phthalazinone derivative, is a long-acting antiallergic agent. Azelastine is a selective H1-histamine blocker, has an antihistamine, antiallergic and membrane-stabilizing effect, reduces capillary permeability and exudation, stabilizes mast cell membranes and prevents the release of biologically active substances from them (histamine, serotonin, leukotrienes, platelet-activating factor, etc.) that cause bronchospasm and contributing to the development of early and late stages of allergic reactions and inflammation.

Mometasone is a synthetic glucocorticosteroid (GCS) for local use. It has anti-inflammatory and antiallergic effects when used in doses at which systemic effects do not occur. Inhibits the release of inflammatory mediators. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of arachidonic acid metabolic products – cyclic endoperoxides, prostaglandins. Prevents the marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, and leads to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of a chemotaxis substance (impact 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:
Azelastine hydrochloride. Bioavailability after intranasal administration is about 40%. The maximum concentration (Cmax) in blood plasma after intranasal administration is achieved after 2-3 hours. When administered intranasally at a daily dose of 0.56 mg of azelastine hydrochloride, the average equilibrium concentration of azelastine hydrochloride in plasma 2 hours after administration is 0.65 ng/ml. Doubling the total daily dose to 1.12 mg resulted in a steady-state mean plasma azelastine concentration of 1.09 ng/mL. However, despite the relatively high absorption in patients, systemic exposure after intranasal administration is approximately 8 times lower than after oral administration of a daily dose of 4.4 mg of azelastine hydrochloride, which is a therapeutic oral dose for the treatment of allergic rhinitis. Intranasal use in patients with allergic rhinitis causes an increase in the level of azelastine in the blood plasma compared to healthy subjects. Other pharmacokinetic data have been studied when administered orally. Communication with blood proteins is 80 – 90%. Metabolized in the liver by oxidation with the participation of the cytochrome P450 system to form the active metabolite 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. When administered intranasally, the systemic bioavailability of mometasone furoate is <1% (with a sensitivity of the detection method of 0.25 pg/ml). Mometasone suspension is very poorly absorbed from the gastrointestinal tract, and the small amount of mometasone suspension that can enter the gastrointestinal tract after nasal inhalation undergoes active primary metabolism even before excretion in urine or bile.

Special instructions

Below are special instructions for the active ingredients of the combination drug azelastine hydrochloride + mometasone furoate (nasal spray).

Momat Rino Advance is recommended for use only in adults over 18 years of age.

Azelastine hydrochloride

There are no special instructions for the use of azelastine hydrochloride in the form of a nasal spray.

Mometasone furoate

Immunosuppression

Mometasone furoate (nasal spray) should be used with caution or should not be used in patients with active or suspected active tuberculosis respiratory tract infection, or untreated fungal, bacterial or systemic viral infections.

Patients treated with glucocorticosteroids have a potentially reduced immune responsiveness and should be warned of their increased risk of infection if exposed to patients with certain infectious diseases (eg, chickenpox, measles), as well as the need for medical advice if such exposure occurs.

Local nasal action

After 12 months of treatment with mometasone furoate (nasal spray) in a study in patients with chronic rhinitis, there were no signs of atrophy of the nasal mucosa; In addition, when treated with mometasone furoate, there was a tendency for the nasal mucosa to return closer to the normal histological phenotype. However, patients using mometasone furoate nasal spray for several months or longer should be periodically monitored for possible changes in the nasal mucosa. If a localized fungal infection of the nasopharynx develops, it may be necessary to discontinue mometasone furoate (nasal spray) or prescribe appropriate treatment. An indication for discontinuation of mometasone furoate (nasal spray) may be a constantly present feeling of irritation of the nasopharynx.

Mometasone furoate (nasal spray) is not recommended for use in the presence of perforation of the nasal septum.

In clinical studies, nosebleeds occurred more frequently than with placebo. Nosebleeds were usually self-stopping and mild in severity.

Systemic effects of glucocorticosteroids

When using nasal glucocorticosteroids, systemic effects may occur, especially with long-term use of high doses of these drugs. These effects are much less likely to occur than with oral corticosteroids and may vary in individual patients and with different corticosteroids used. Potential systemic effects may include Cushing’s syndrome, development of Cushingoid features, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and much less commonly, a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disorders, anxiety, depression, or aggression (especially in children).

Cases of increased intraocular pressure have been described after the use of intranasal glucocorticosteroids.

During the transition from treatment with systemic corticosteroids to treatment with mometasone furoate (nasal spray), some patients may experience initial symptoms of systemic corticosteroid withdrawal (for example, joint and/or muscle pain, fatigue and depression), despite a decrease in the severity of symptoms associated with damage to the nasal mucosa; such patients must be specifically convinced of the advisability of continuing treatment with mometasone furoate (nasal spray). Switching from systemic to topical glucocorticosteroids may also reveal pre-existing allergic diseases such as allergic conjunctivitis and eczema that were masked by systemic glucocorticosteroid therapy.

Therapy with doses higher than recommended may cause clinically significant suppression of adrenal function. Therefore, during periods of stress or planned surgical interventions, when the need to use doses exceeding the recommended ones is obvious, the possibility of additional use of systemic glucocorticosteroids should be considered.

Nasal polyps

The safety and effectiveness of mometasone furoate nasal spray have not been studied in the treatment of unilateral polyps, cystic fibrosis polyps, or polyps causing complete obstruction of the nasal passages. The use of the drug for unilateral polyps that are characterized by an unusual or heterogeneous appearance, especially if they are accompanied by ulceration or bleeding, needs further study.

Non-nasal symptoms

Although intranasal mometasone furoate (nasal spray) provides control of nasal symptoms in most patients, the combined use of appropriate additional medications may reduce other symptoms, especially ophthalmic ones.

The drug Momat Rino Advance contains benzalkonium chloride, which can cause irritation of the nasal mucosa and bronchospasm.

Impact on the ability to drive vehicles and machinery:

In rare cases, fatigue, fatigue, dizziness and weakness, which may be a consequence of the disease itself, may develop when using Momat Rhino Advance nasal spray. In such cases, you should avoid driving a vehicle and working with complex mechanisms.

Active ingredient

Azelastine, Mometasone

Composition

Nasal spray

Active ingredients:

azelastine hydrochloride – 140 mcg,

mometasone furoate – 50 mcg.

Excipients:

microcrystalline cellulose (Avicel RC-591) – 0.910 mg,

carmellose sodium -0.021 mg,

dextrose – 3,500 mg,

polysorbate-80 – 0.0175 mg,

benzalkonium chloride – 0.014 mg,

disodium edetate – 0.035 mg,

neotame – 0.0007 mg,

citric acid monohydrate – 0.0105 mg,

sodium citrate – 0.021 mg,

purified water – up to 70 mg.

Pregnancy

There have been no adequately designed and well-controlled studies of the drug in pregnant women.

Azelastine hydrochloride is capable of causing intrauterine toxicity in mice, rats and rabbits.

The use of the drug during pregnancy and breastfeeding is contraindicated.

Contraindications

Hypersensitivity to any of the components of the drug.

Recent surgery or trauma to the nose with damage to the mucous membrane of the nasal cavity – before the wound heals (due to the slowing effect of GCS on the healing process).

– Children under 18 years of age.

With 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 can be prescribed for the listed infections as directed by a doctor), the presence of an untreated infection involving the mucous membrane of the nasal cavity.

Side Effects

Common: headache, dysgeusia (unpleasant taste) as a result of improper use, namely, excessive tilting of the head back during administration.

Very rare: dizziness (may be caused by the disease itself).

Gastrointestinal disorders:
Rarely: feeling of irritation of the pharyngeal mucosa, nausea.

Disorders of the respiratory system, chest and mediastinal organs:

Common: nosebleeds, discomfort in the nasal cavity (burning sensation, itching), ulceration of the nasal mucosa, sneezing, pharyngitis, sinusitis, upper respiratory tract infections.

Immune system disorders:

Very rare: hypersensitivity, anaphylactoid reactions.

Skin and subcutaneous tissue disorders:

Very rare: rash, itchy skin, urticaria.

General disorders and disorders at the injection site:

Very rare: fatigue, drowsiness, weakness (may be caused by the disease itself).

With long-term use of glucocorticosteroids (GCS) in high doses, systemic side effects may develop, including glaucoma and cataracts.

Interaction

Azelastine. With intranasal use of azelastipe, no clinically significant interactions with other drugs were detected.

Mometasone furoate. Combination therapy with loratadine was well tolerated by patients.

However, no effect of the drug on the concentration of loratadine or its main metabolite in the blood plasma was noted. In these studies, mometasone furoate was not detected in blood plasma (with a sensitivity of the detection method of 50 pg/ml).

Overdose

At the moment, there are no known cases of drug overdose with intranasal use. In case of an overdose of azelastine as a result of accidental ingestion, disorders of the nervous system may occur (drowsiness, confusion, tachycardia, hypotension). Treatment of these disorders is symptomatic.

With long-term use of glucocorticosteroids in high doses, as well as with the simultaneous use of several GCS, suppression of the hypothalamic-pituitary-adrenal system is possible.

Due to the low systemic bioavailability of the drug, it is unlikely that in the event of an accidental or intentional overdose, any measures other than observation will be required, with possible subsequent resumption of the drug at the recommended dose.

Storage conditions

In a place protected from light at a temperature of 15 to 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life

2 years
Do not use the drug after the expiration date.

Manufacturer

Glenmark Pharmaceuticals Ltd, India