Anoro Ellipta, 22 mcg + 55 mcg/dose 30 doses

The drug Anoro Ellipt® is a combination of a long-acting inhaled muscarinic cholinoreceptor antagonist and a long-acting inhaled beta2-adrenomimetic.

After oral inhalation, both compounds have a local effect on the airways, causing bronchodilation through different mechanisms of action.

Vilanterol belongs to the class of selective long-acting beta2-adrenergic receptor agonists (beta2-agonists).

The pharmacological effects of beta2-adrenergic receptor agonists, including vilanterol, are at least in part due to stimulation of intracellular adenylate cyclase, the enzyme that catalyzes the conversion of ATP to cAMP.

The increase in the level of cAMP leads to relaxation of the bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity reactions from cells (primarily from mast cells).

Umeclidinium is a long-acting muscarinic receptor antagonist (also called an anticholinergic). It is a quinuclidine derivative that is a muscarinic receptor antagonist that acts on muscarinic cholinergic receptors of various subtypes.

Umeclidinium has a bronchodilator effect by competitive inhibition of acetylcholine binding to muscarinic acetylcholine receptors of airway smooth muscle. In preclinical studies in in vitro models, the compound demonstrated slow reversibility of action on human M3 subtype muscarinic receptors, and in vivo models showed prolonged action of the drug after injection directly into the lungs.

Pharmacodynamic effects.

Two placebo-controlled clinical efficacy studies observed an increase in first-second forced expiratory volume (FEF1) after the first dose of vilanterol and umeclidinium combination on day 1.

This index increased by 0.11 and 0.13 L 15 min after using the drug at doses of 22+55 mcg/dose and 22+113 mcg/dose, respectively, compared with the same index when using placebo (in both cases pThe effect of vilanterol and umeclidinium combination on QT interval duration was evaluated in a placebo and moxifloxacin-controlled study. 103 healthy volunteers used the combination of vilanterol and umeclidinium for 10 days once daily at doses of 22+113 or 88+452 mcg/dose.

There was no clinically significant effect on QT interval duration (corrected by the Frederick method) after multiple uses of this drug.

. In addition, there was no clinically significant effect of vilanterol and umeclidinium combination on heart rate on 24-hour Holter ECG monitoring in 108 patients with COPD who received this drug for 6 months (of which 53 patients received 22+55 mcg/dose and 55 received 22+113 mcg/dose once daily) and in 226 patients who received 22+113 mcg/dose once daily for 12 months.

Indications

Supportive bronchodilator therapy to relieve symptoms of chronic obstructive pulmonary disease.

Active ingredient

Composition

1 dose/cell:

Vilanterol Strip:

– vilanterol triphenatate micronized 40 µg (equivalent to 25 µg vilanterol)

auxiliary substances:

Magnesium stearate 125 mcg;

Lactose monohydrate up to 12.5 mg

Strip with umeclidinium:

– umeclidinium bromide micronized 74.2 µg (equivalent to 62.5 µg umeclidinium)

auxiliary substances:

Magnesium stearate 75 µg;

Lactose monohydrate up to 12.5 mg

How to take, the dosage

Anoro Ellipt® should be used daily at the same time once a day. The recommended dose of Anoro Ellipt® is one inhalation of 22+55 mcg/dose once daily. In some patients, the use of Anoro Ellipt® at a dose of 22+113 mcg/dose once daily has been found to have an additional benefit with regard to the effect on lung function and the frequency of use of emergency drugs. Maximum dose is one inhalation of Anoro Ellipt® in dose 22+113 mcg/dose once daily.
Special patient groups.

Children. This drug is not used for the treatment of patients younger than 18 years of age taking into account the indications for its prescription.

Patients of advanced age.

Patients over 65 years of age do not require dose adjustment (see “Pharmacokinetics”).

Patients with impaired renal function.

Patients with impaired renal function do not require dose adjustment (see “Pharmacokinetics”).

Patients with impaired hepatic function.

Patients with mild to moderate hepatic impairment do not require dose adjustment.

There have been no studies on the use of the combination of vilanterol and umeclidinium in patients with severe hepatic impairment (see “Pharmacokinetics”).

Recommendations for use:

When using the Ellipt® Inhaler for the first time, there is no need to verify proper operation or special preparation of the inhaler for use. You must consistently follow the recommendations for use listed below.
The Ellipta® inhaler is packaged in a container containing a desiccant sachet of silica gel that is not intended for eating or inhaling. This bag should be disposed of. After removing the inhaler from the container, the lid of the inhaler is in the closed position. It should not be opened until you are ready to take the medication.

Instructions for Use of the Ellipt® Inhaler:

Opening and closing the Ellipt® Inhaler lid without taking the medication results in the loss of one dose. This dose remains closed inside the inhaler, but it will not be available for administration. You cannot accidentally receive a large dose or a double dose in one inhalation.
One dose of medication is ready for inhalation after each time the lid is opened.

The dose counter shows how many doses of medication are left in the inhaler. Before using the inhaler, the dose counter shows the number 30. Each time the lid is opened, the number of doses decreases by 1. When less than 10 doses are left, half of the counter turns red. After the last dose of medication is used up, half of the counter is highlighted in red, the counter shows the number 0. This means that the inhaler is empty. If you open the lid after that, the dose counter will turn completely red.

Dose preparation:

Do not open the lid until you are ready to take the medicine. The inhaler should not be shaken.
1. Put the lid down until it clicks.
2. The dose of medication is ready for inhalation and the counter reduces the number of doses by one to confirm this.
3. If the counter has not reduced the number of doses after the click, then the inhaler is not ready to deliver the dose of medication. In this case, contact the telephone number or address listed under “For further information contact”.
4. The inhaler should not be shaken.
Inhalation of medication:
1. Holding the inhaler at some distance from your mouth, exhale as deeply as possible. Do not exhale into the inhaler.
2. Place the mouthpiece between your lips and wrap your lips tightly around it. Do not cover the vent with your fingers.
Lips should exactly follow the shape of the mouthpiece of the inhaler.
3. Take one deep, long, even breath. Hold your breath as long as possible (at least 3-4 seconds).
4. Take the inhaler out of your mouth.
5. Slowly and calmly exhale.

If the inhaler is used correctly, the patient may not taste or feel the medicine coming in.

Closing the inhaler:

If necessary to clean the mouthpiece, use a dry paper towel before closing the lid.
Raise the lid all the way until the mouthpiece is completely closed.

Interaction

Beta-adrenoblockers may attenuate the effects of beta2-agonists or act as antagonists of drugs of this group, including vilanterol.

The concomitant use of non-selective and selective beta-blockers should be avoided unless there is a good reason to use them together.

Vilanterol, a component of Anoro Ellipt®, is rapidly metabolized primarily in the GI tract and liver via the cytochrome P450 isoenzyme CYP3A4.

When concomitant administration of the drug with strong CYP3A4 isoenzyme inhibitors (e.g., ketoconazole) care should be taken because there is a possibility of increasing systemic exposure of vilanterol which in turn may increase the risk of adverse reactions (see “Pharmacokinetics”).

Special Instructions

Anoro Ellipt® is intended for use as maintenance therapy for COPD. This drug should not be used to relieve acute symptoms, i.e. as an emergency therapy for an acute episode of bronchospasm. A short-acting bronchodilator should be used to relieve acute symptoms. Increased frequency of use of short-acting bronchodilators to relieve symptoms indicates impaired disease control, in which case the patient should consult a physician.

There have been no studies of the use of Anoro Ellipt® in patients with bronchial asthma, therefore the use of this drug for therapy in this group of patients is not recommended.

As with other types of inhalation therapy, the use of Anoro Ellipt® may cause paradoxical bronchospasm, which may be life-threatening. If paradoxical bronchospasm develops, treatment with the drug should be discontinued and alternative therapy may be prescribed if necessary.

The drug Anoro Ellipt® is intended for maintenance treatment of COPD patients. Due to the fact that the general population of COPD is significantly dominated by patients over 40 years of age, spirometric confirmation of the diagnosis of COPD is required when prescribing the drug in patients under 40 years of age.

Influence on the ability to drive vehicles and operate machinery. Studies of the effect of Anoro Ellipt® preparation on the ability to drive vehicles and operate mechanisms have not been conducted.

Contraindications

– children under 18 years of age. and severe allergic reactions to milk protein or hypersensitivity to the active ingredients or any other component of the drug in the anamnesis;

With caution: after using sympathomimetics and muscarinic receptor antagonists, including Anoro Ellipt® .including Anoro Ellipt®, adverse reactions such as arrhythmias (e.g. atrial fibrillation and tachycardia) may occur in the cardiovascular system. 4

In this regard, Anoro Ellipt® should be used with caution in patients with severe forms of cardiovascular disease.

Given the antimuscarinic activity of this drug, it should be prescribed with caution in patients with closed-angle glaucoma or urinary retention.

Side effects

Heart: infrequent – atrial fibrillation, tachycardia.
Respiratory system, thoracic and mediastinal organs: frequent – cough.
Gastrointestinal disorders: frequent – constipation, dry mouth.

The safety profile of vilanterol and umeclidinium combination is based on data from clinical studies involving 2454 patients with COPD who received at least one dose of vilanterol and umeclidinium combination during the study.

All patients used the drug once daily; of these, 1,124 received the drug at a dose of 22 + 55 mcg/dose and 1,330 received 22 + 113 mcg/dose.

The adverse reactions presented below are listed according to organ and organ system involvement and frequency of occurrence. The frequency of occurrence is defined as follows: very common (≥1/10); common (≥1/100 and Infectious and parasitic diseases: common – pharyngitis.

Overdose

Treatment: In case of overdose, symptomatic therapy is required and if necessary, the patient shall be appropriately monitored. Further management of patients in case of overdose should be carried out in accordance with clinical indications.

There have been no data on overdose of vilanterol and umeclidinium combination in clinical studies.

Symptoms: Symptoms and signs due to the effects of individual drug components may develop, including known adverse reactions developing with muscarinic receptor antagonists (e.g., dry mouth, accommodation disorders, and tachycardia) and signs seen with overdose with other beta2-agonists (e.g., tremor, headache, and tachycardia).