Alvesko - instructions for use, doses, side effects, contraindications

Active substanceCiclesonideCiclesonide

Similar drugsTo uncover

Alvesco®

aerosol d / inhal.

AstraZeneca AB Sweden

Dosage form: & nbspaerosol for inhalation dosed

Composition:

One spray contains:

Active substance:

Dosage 40 μg: ciclesonide 0.04 mg;
Dosage of 80 mcg: ciclesonide 0.08 mg;
Dosage 160 mcg: ciclesonide 0.16 mg;

Excipients:

Dosage 40 μg: norflurane (HFA-134a) 54.51 mg, ethanol 4.74 mg;
Dosage of 80 mcg: norflurane (HFA-134a) 54.46 mg, ethanol 4.74 mg;
Dosage 160 mcg: norflurane (HFA-134a) 54.37 mg, ethanol 4.73 mg.

Description:Colorless transparent solution in an aluminum can.

Pharmacotherapeutic group:Glucocorticosteroid for topical application

ATX: & nbsp

R.03.B.A Glucocorticoids

R.03.B.A.08 Ciclesonide

Pharmacodynamics:

Ciclesonide exhibits a low affinity for glucocorticosteroid receptors. After inhalation, it is converted by the enzymes into the lungs into the main metabolite (dezitslesonid, C21-desmethylpropionylcyclesonide), which has a pronounced anti-inflammatory activity and is therefore considered an active metabolite.

Ciclesonide suppresses inflammatory reactions in the respiratory tract and, thus, weakens the symptoms of bronchial asthma, improves lung function.

Pharmacokinetics:

Suction

Oral or intravenous administration of radiolabelled ciclesonide has shown that the degree of absorption is 24.5%.When taking the drug inside, the bioavailability of both the ciclesonide and the active metabolite is negligible (<0.5% for ciclesonide, and <1% for the metabolite) due to the significant effect of presystemic metabolism. The accumulation of ciclesonide in healthy patients in the lungs is over 50%. According to this figure, systemic bioavailability for the active metabolite after the inhalation dose is over 50%. Since the bioavailability of the active metabolite when taking ciclesonide inward is less than 1%, the accepted proportion of the inhalation agent does not have a systemic effect.

Distribution

After intravenous administration to healthy patients ciclesonide rapidly distributed due to its high lipophilicity. The volume of distribution averages 2.9 l / kg for ciclesonide and 12.1 l / kg for deztsiklesonida. The percentage of ciclesonide bound to plasma proteins is about 99%, and the percentage of active metabolite is 98 to 99% show almost complete binding of the circulating ciclesonide / active metabolite to plasma proteins.

Metabolism

Ciclesonide is hydrolyzed to the biologically active metabolite by the esterase enzyme in the lungs.The active metabolite of ciclesonide is mainly metabolized to hydroxylated inactive metabolites by catalysis with the participation of the CYP3A4 isoenzyme. The clearance of ciclesonide is about 152 l / h and dezitslesonida - about 228 l / h, which indicates a high degree of extraction of the substance by the liver.

Excretion

Ciclesonide is excreted mainly with feces, both after oral administration, and after intravenous administration, which indicates that it is primarily secreted with bile.

Pharmacokinetics in selected patient groups

Patients with renal or hepatic insufficiency, elderly patients

Dose adjustment for this group of patients is not required.

Since active metabolite is not excreted through the kidneys, studies in patients with impaired renal function have not been performed.

In patients with hepatic insufficiency, an elongated half-life and a slight increase in the retention time of dezitslesonida (active metabolite) in the blood were noted. As a result, the accumulation of this substance is not excluded when taking the drug in high doses.

Children

The pharmacokinetic parameters of dezitslesonida are identical for children and adults.

Indications:

Bronchial asthma.

Contraindications:

Hypersensitivity to the drug, age to 6 years.

Carefully:

In patients with pulmonary tuberculosis in active or chronic form;
In patients with bacterial, viral or fungal infections of the respiratory tract.

Pregnancy and lactation:

Controlled studies in pregnant women were not conducted. Nevertheless, after the inhalation administration of the drug, the serum ciclesonide concentration is very low, therefore, the effect on the embryo and the potential toxicity that affects the reproductive function are negligible. The isolation of ciclesonide or its metabolites through breast milk has not been investigated.

Like other inhaled glucocorticosteroids, ciclesonide can be used during pregnancy and lactation as prescribed by the doctor, if the expected curative effect exceeds the risk of possible side effects.

Newborns from mothers treated with glucocorticosteroids should be under the supervision of a physician to exclude hypofunction of the adrenal glands.

Dosing and Administration:

Alvesco^® apply only for oral inhalation.

Alvesco^® should be taken for a long period of time daily.
Alvesco^® dosed individually. The initial dose should be matched depending on the severity of the condition. When the desired clinical effect is achieved, the dose should be reduced to the minimum required to control the manifestations of the disease.

Adults, elderly patients and adolescents over 12 years of age

Asthma from mild to moderate severity: The recommended daily dose is 160 μg to 640 μg; The dose of 640 mcg should be divided into two doses per day.

Severe asthma: The dose can be increased to a maximum of 2 x 640 mcg daily.

Improvement of the manifestations of the disease occurs within 24 hours after taking Alvesco^®. It is assumed that the maximum effect of treatment - as with other inhaled glucocorticosteroids - is achieved after 2-3 months of use of the drug.

Patients should not stop treatment, even in the absence of symptoms of asthma.

Children over 6 years old

The recommended daily dose is 80-160 mcg once or 80 mcg twice daily.

Alvesco^® can be used with or without a spacer. If using a spacer is necessary, it is recommended to use the AeroChamberPlus spacer.

Instructions for individual cases

There is no need to adjust the dose for elderly patients or patients with hepatic or renal insufficiency.

Adults and adolescents who regularly take oral glucocorticosteroids

In patients with severe bronchial asthma who are dependent on oral glucocorticosteroid therapy (eg, prednisolone), the dose of Alvesco^® is 640 mcg twice daily. To transfer patients from an oral glucocorticosteroid to Alvesco^®, patients should be in remission. Dose of Alvesco^® (640 μg twice daily) should be used within 10 days in combination with an oral glucocorticosteroid. The dose of oral glucocorticosteroid should then gradually decrease every week to as low a level as possible, with a daily dose not decreasing by more than 2.5 mg each time.

Instructions for use of the inhaler

Patients should be instructed about the proper handling of the inhaler. If the inhaler is new or has not been used for more than one week, the first three valve strokes must be performed in the air. There is no need to shake the balloon, since it is a dissolved aerosol.Carefully follow these instructions and use the pictures as a guide.

1. Remove the protective cap from the spray gun and check the mouthpiece inside and out. Make sure it is clean and dry.

2. Turn the inhaler upside down (the bottom of the cylinder up), place your index finger on the bottom of the cylinder, and your thumb under the mouthpiece.

3. Make the maximum exhalation as much as possible. Do not exhale into the inhaler.

4. Place the mouthpiece in the mouth and close the lips around it.

5. Only after you have started inhaling, press your index finger on the top of the inhaler to release the medicine during your slow and deep breath. Take care that the medicine can not pass through the space between the lips and the mouthpiece.

6. Hold your breath, remove the mouthpiece from your mouth and remove your finger from the top of the inhaler. Continue to hold your breath for about 10 seconds or as long as you can. Slowly exhale through the mouth. Avoid breathing out through the mouthpiece. It is important not to rush during steps 3-6.

7. If you need to take an additional breath, wait half a minute and repeat steps 3-6.

8. After use, always wear a protective cap to protect it from dust.Firmly close and secure in place.

9. For hygiene purposes:

please clean the mouthpiece regularly on the outside and inside with a dry cloth;
Using a dry folded napkin, wipe the surface with a small hole, where the medicine comes from;
Do not use water or any other liquid.

Side effects:

System of organs	Infrequently (> 1:1000 <1:100)	Rarely (> 1: 10000 <1: 1000)
From the side of the cardiovascular system		Enhanced palpitations **, Increased blood pressure
From the gastrointestinal tract	Nausea, vomiting* Unpleasant taste	Abdominal pain * Dyspepsia *
General disorders and disorders at the site of administration	Reactions at the injection site: sensation of irritation and perspiration in the throat Dryness mucousth shell of the oral cavity and pharynx
From the immune system		Angioedema hypersensitivity
InfectioInfectious and parasitic diseases	Fungal infections of the oral cavity *
From the nervous system	Headache*
From the respiratory system	Dysphonia. Cough after inhalation * Paradoxical bronchospasm *
From the skin	Eczema and skin rash

* identical or lower percentage compared with placebo

** Palpitations were observed during clinical trials in cases of concomitant use with drugs that may have a side effect on the heart rhythm (for example, theophylline or salbutamol).

Paradoxical bronchospasm may occur immediately after inhalation and be a nonspecific acute reaction to any inhalation medication that may be associated with the active substance, excipients or cooling due to evaporation of the propellant in the case of metered-dose inhalers. In most cases, this is a mildly adverse reaction that does not require discontinuation of Alvesco's treatment^®, and which can pass by itself.

Inhaled glucocorticosteroids can produce systemic effects, especially at high doses prescribed for a long period. Possible systemic effects include Cushing's syndrome and cushing-like symptoms, such as adrenal suppression (suppression of the adrenal glands), growth retardation in children and adolescents, decreased bone density, cataracts and glaucoma. That is why it is important,so that the dose of the inhaled glucocorticosteroid is reduced to the lowest, at which satisfactory control of manifestations of the disease is conducted.

Overdose:

Sharp

Inhaled use of a single dose of 2880 μg of ciclesonide in healthy volunteers was tolerated well. The possibility of acute toxic effects following an overdose of inhaled ciclesonide is low.

It is possible to increase the dryness of the mucous membrane of the oral cavity and pharynx, sensation of irritation or perspiration in the throat, dysphonia.

Treatment:

After acute overdose, there is no need for specific treatment.

Chronic

After prolonged administration of 1280 μg of ciclesonide, no clinical signs of adrenal suppression were observed. However, if the excess of the recommended dose continues for an extremely long period of time, some degree of suppression of the adrenal glands can not be ruled out.

Treatment:

It is recommended to monitor the function of the adrenal glands. In cases of an overdose of Alvesco^® Therapy can be continued with a dose sufficient to maintain a therapeutic effect.

Interaction:

The in vitro data show that the CYP3A4 isoenzyme is the main enzyme involved in the metabolism of the active metabolite of ciclesonide-M1 (dezitslesonida) in humans.

In studies of drug interactions between ciclesonide and ketoconazole, as a potent inhibitor of the CYP3A4 isoenzyme, the effect on the active metabolite of dezicylesonide increased approximately 3.5-fold, while the effects on ciclesonide was not noted. Therefore, the simultaneous use of potential inhibitors of the isoenzyme CYP3A4 and ciclesonide should be avoided.

Investigation of the interaction between ciclesonide and the substrate of erythromycin CYP3A4 isoenzyme showed no interactions between the two substances.

Special instructions:

Alvesco^® is not indicated for the treatment of asthmatic status or other acute episodes of asthma requiring intensive therapeutic measures.

The effect of inhaled glucocorticosteroids in prolonged use in children is not fully understood. The physician should constantly monitor the development of the growth of children taking glucocorticosteroids for a long period. If growth slows, therapy should be revised to reduce the dose of an inhaled glucocorticosteroid.If possible, then to the smallest dose, which helps maintain a constant control over the manifestations of asthma. Dose of Alvesco^® can be reduced in patients who need oral glucocorticosteroids.

For patients transferred from oral glucocorticoid therapy to inhaled treatment, Alvesco^®, a decrease in the function of the adrenal cortex may persist for a significant period of time after the transfer. The possibility of developing undesirable effects from the use of oral glucocorticosteroids may persist for some time after their withdrawal. In such cases, it is recommended to monitor the reserve function of the adrenal cortex. The possibility of residual deterioration of the adrenocortical response in a critical situation (therapeutic or surgical) and in other individual cases that can be caused by a stress reaction should always be taken into account, as a result of which appropriate glucocorticosteroid treatment should be started.
In case of insufficient adrenocortical response or serious exacerbations, the dose of Alvesco^® should be increased; if necessary, oral glucocorticosteroids should be used. In case of infection, antibiotics should be used. Paradoxical bronchospasm with increased wheezing and other symptoms of bronchoconstriction that appear immediately after inhalation should be treated with a fast-acting bronchodilator, which usually leads to rapid relief. The patient should be examined, and therapy with Alvesco^® should continue only if, after a balanced consideration, the expected effect is higher than the possible risk. The relationship between the severity of asthma and the general predisposition to acute bronchial reactions should be taken into account.

Transfer of patients taking oral glucocorticosteroids to Alvesco^®

Transfer of patients treated with oral glucocorticosteroids to Alvesco^® and their subsequent management needs attention, since the restoration of a reduced function of the adrenal gland caused by prolonged systematic glucocorticosteroid therapy may take some time.

In patients who took systemic glucocorticosteroids for a long period of time, or at a high dose, suppression of adrenal function may be observed. The adrenal function of these patients should be monitored regularly, and the dose of systemic glucocorticosteroids should decrease gradually. After about one week, gradual elimination of systemic glucocorticosteroids with a decrease in their daily dose of 1 mg of prednisolone, or its equivalent, may be initiated. For a maintenance dose of prednisolone exceeding 10 mg daily, it may be advisable to carefully apply large dose reductions during weekly intervals.

Some patients may feel bad during the withdrawal, despite the preservation or even improvement in respiratory function. They need to be screened for adrenocortical insufficiency.

When transferring patients from taking systemic glucocorticosteroids to inhalation therapy, allergic reactions (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs, may appear.These allergies should be treated with symptomatic antihistamines and / or topical agents, including topical glucocorticosteroids.

Effect on the ability to drive transp. cf. and fur:

There is no evidence of the effect of the drug on the ability to drive vehicles and mechanisms.

Form release / dosage:Aerosol for inhalation dosage 40 μg / spray, 80 μg / spray, 160 μg / spray.

Packaging:5 ml (60 sprays) or 8 ml (120 sprays) into an aluminum can with a metering valve and a mouthpiece with a protective cap. A balloon along with the instructions for use are placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

The contents of the cylinder are under pressure. The cylinder should not be opened and subjected to heating above 50 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000823

Date of registration:07.10.2011 / 10.04.2017

Expiration Date:Unlimited

The owner of the registration certificate:AstraZeneca ABAstraZeneca AB Sweden