Astelin Nasal Spray

Brand name

The trade name of the drug is Astelin It is registered and used in medical practice to identify this drug on the market.

International Nonproprietary Name (INN)

The international nonproprietary name of the drug is azelastine. This name is used in pharmacology to designate the active active ingredient, regardless of brand names.

Form of release

Astelin is available in the form of a nasal spray, which provides convenience of application and spot action on the nasal mucosa. Each vial contains a metered solution, designed for a certain number of injections. The volume of the vial may vary depending on the manufacturer, but most often there are versions of 10 ml or 20 ml, containing 140 or 280 doses, respectively.

Composition

Active substance

The main active component of the drug is azelastine hydrochloride. 1 ml of the solution contains 1 mg of azelastine hydrochloride, which corresponds to the standard therapeutic concentration for topical application.

Auxiliary components

The composition includes additional substances that ensure the stability and effectiveness of the drug: purified water, sodium chloride, benzalkonium chloride (as a preservative), citric acid, sodium hydrophosphate dihydrate. These components maintain an optimal pH level and ensure the safety of the solution during storage.

Pharmacologic Properties

Pharmacodynamics

Azelastin, which is the main active substance of the drug, belongs to the group of H1-histamine receptor blockers of the second generation. Its mechanism of action is inhibition of histamine activity - the key mediator of allergic reactions. By blocking H1 receptors, the drug prevents the development of such symptoms as itching, sneezing, nasal congestion and profuse secretion from the nasal passages. In addition to antihistamine effect, azelastin has anti-inflammatory and membrane-stabilizing properties, which reduces vascular permeability and reduces tissue edema. The effect of use comes within 15-30 minutes after injection and lasts up to 12 hours, which makes the drug convenient for use once or twice a day.

Pharmacokinetics

Absorption

When administered intranasally, azelastine is minimally absorbed through the nasal mucosa. Systemic bioavailability is about 40%, which is due to partial swallowing of the drug and subsequent absorption in the gastrointestinal tract. However, the main therapeutic effect is achieved through local action.

Distribution

Azelastine binds to blood plasma proteins by approximately 80-90%. The volume of distribution is relatively small, as the drug mainly acts locally, minimizing systemic effects.

Metabolism

The metabolism of azelastine occurs in the liver with the participation of the cytochrome P450 enzyme, resulting in the formation of the active metabolite, desmethylazelastine. This metabolite also has antihistamine activity, enhancing the therapeutic effect of the drug.

Excretion

Half-life of azelastine is about 20 hours, and its metabolite - up to 45 hours. The drug is excreted predominantly through the kidneys in the form of inactive metabolites, and also in an insignificant amount through the intestine. When applied topically, systemic accumulation is practically absent.

Indications for Use

Astelin is prescribed for the symptomatic treatment of various allergic conditions affecting the upper respiratory tract. The main indications include:

• Seasonal allergic rhinitis (pollinosis) caused by plant pollen;
• Year-round allergic rhinitis associated with exposure to household allergens (dust, animal hair, mold);
• Symptomatic relief in allergic conjunctivitis in combination with rhinitis (when used as part of a complex therapy).

The drug is effective in eliminating such manifestations as nasal congestion, sneezing, itching in the nose and throat, as well as copious mucus secretion.

Contraindications

The use of Astelin is prohibited in the following cases:

• Individual hypersensitivity to azelastine or any of the excipients;
• Children under 6 years of age (due to insufficient data on safety and efficacy in this age group);
• Acute infectious diseases of the nasal cavity requiring other treatment;
• Severe damage to the nasal mucosa (e.g. ulcers or atrophy), as this may increase irritation.

The drug should be used with caution in the presence of chronic liver or kidney disease, as well as during pregnancy and lactation (see section “Special Instructions”).

Method of Administration and Dosage

How to take

Astelin is intended for intranasal administration. Before use, the vial should be shaken, remove the protective cap and perform a trial air injection (for new vials or after a long break). The patient should keep the head straight, insert the nozzle into the nostril and press the atomizer, while taking a slight inhalation through the nose. After injection, it is recommended to tilt the head back slightly for even distribution of the drug. It is not necessary to drink water or take with food, as it is a topical agent.

Dosages for adults and children

Adults and children over 12 years of age

The standard dose is 1 injection (0.14 mg) into each nostril twice daily - morning and evening. The maximum daily dose is 4 injections (0.56 mg).

Children 6 to 12 years of age

It is recommended 1 injection into each nostril once a day (in the morning). If necessary, the doctor can increase the frequency up to twice a day.

Dose adjustment for certain conditions

Dose adjustment is usually not required in renal or hepatic insufficiency, as the systemic effect of the drug is minimal. However, in case of severe dysfunction of these organs, a physician should be consulted before starting therapy.

Side Effects

Astelin is well tolerated in most cases, but the following adverse reactions are possible:

• Local reactions: burning, dryness or irritation of the nasal mucosa, bitter taste in the mouth (due to flow of the drug down the throat);
• Systemic effects: headache, drowsiness, dizziness (rare);
• Allergic manifestations: skin rash, itching, in exceptional cases - angioedema;
• Repiratory system: sneezing, cough (usually temporary).

In case of occurrence of pronounced side effects, discontinue use and consult a physician.

Overdose

Symptoms of overdose

The cases of overdose in topical application are extremely rare due to low systemic absorption. However, in case of accidental ingestion of large amounts of the drug may be observed: drowsiness, confusion, tachycardia, decreased blood pressure.

First aid measures

If you suspect an overdose, you should immediately stop using the drug, provide the patient with rest and seek medical attention. Before the arrival of a doctor, the stomach can be washed (if the drug was swallowed) and activated charcoal can be given to reduce absorption.

Drug Interactions

Influence on the effects of other drugs

Astelin has minimal systemic action, so significant interactions with other drugs are rare. However, concomitant use with sedatives or other antihistamines may increase drowsiness.

Compatibility with alcohol and food

Alcohol may increase the sedative effect of azelastine, although it is already weakly expressed. Food does not affect the efficacy of the drug, as it is applied topically.

Special Precautions

Use in pregnancy and breastfeeding

Data on the safety of Astelin use in pregnant women are limited. The drug may be prescribed only if the expected benefit to the mother exceeds the potential risk to the fetus. During lactation azelastine penetrates into breast milk in minimal amounts, but it is recommended to temporarily discontinue breastfeeding for the period of treatment.

Effects on driving and mechanisms

In rare cases, the drug may cause drowsiness or dizziness, which requires caution when driving a car or working with dangerous mechanisms. Patients should evaluate individual reaction to the drug before performing such tasks.

Particularities of use in the elderly and children

Dose adjustment is not required in elderly patients, but possible increase of side effects, such as drowsiness, should be taken into account. For children under 6 years of age the drug is not used due to lack of sufficient clinical data.