Spiolto Respimat, 2.5mcg+2.5mcg/dose 4ml cartridge 1pc, with ing.

Composition

1 dose contains:

Olodaterol hydrochloride-2.736 mcg, which corresponds to the content of olodaterol-2.5 mcg

tiotropium bromide monohydrate-3.124 mg, which corresponds to the content of tiotropium-2.5 mgsupport substances:

benzalkonium chloride solution-0.0022 mg (respectively, benzalkonium chloride – 0.0011 mg),

disodium edetate-0.0011 mg,

citric acid anhydrous 1 M-up to pH 2.9,

purified water – up to 11.05 mg

Pharmacological action

Bronchodilator.

Olodaterol-a long-acting beta-2-adrenomimetic-and tiotropium bromide-m-a holinoblocker-provide complementary bronchodilation as a result of different mechanisms of action of active substances and different localization of target receptors in the lungs. Olodaterol has a high affinity and selectivity for beta-2-adrenergic receptors. Activation of beta-2-adrenergic receptors in the airways leads to stimulation of intracellular adenylate cyclase, which is involved in the synthesis of cAMP. An increase in cAMP levels causes bronchodilation, relaxing the smooth muscle cells of the airways.

Olodaterol is a long-acting selective beta-2-adrenergic agonist with a rapid onset of action and long-term (at least 24 hours) retention of the effect. Beta-2-adrenergic receptors are present not only in smooth muscle cells, but also in many other cells, including epithelial and endothelial cells of the lungs and heart. The exact function of beta-2 receptors in the heart is not fully understood, but their presence indicates that even highly selective beta-2-adrenergic agonists can affect the heart.

Tiotropium bromide is a long-acting muscarinic receptor antagonist, often referred to in clinical practice as an m-holinoblocker. It has the same affinity for m1-m5-subtypes of muscarinic receptors. Inhibition of M3 receptors in the airways results in smooth muscle relaxation.

The bronchodilating effect depends on the dose and persists for at least 24 hours. The significant duration of action is probably related to the very slow dissociation of tiotropium bromide from m3s: the half-dissociation period is significantly longer than that of ipratropium bromide.

When administered by inhalation, tiotropium bromide, as an N-quaternary ammonium derivative, has a local selective effect (on the bronchi), while at therapeutic doses it does not cause systemic m-holinoblocking side effects. Dissociation from m2 receptors occurs faster than from m3 receptors, which indicates a predominance of selectivity for the m3 receptor subtype over m2 receptors. High affinity for receptors and slow dissociation of tiotropium bromide from the receptor bond cause a pronounced and prolonged bronchodilating effect in patients with COPD.

Bronchodilation that develops after tiotropium bromide inhalation is primarily due to local action (on the respiratory tract), and not systemic.

Indications

The drug SPIOLTO RESPIMAT, taken once a day, is indicated for long-term maintenance therapy in patients with chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, to reduce airway obstruction and concomitant shortness of breath; reduce the frequency of exacerbations; improve exercise tolerance and quality of life.

Contraindications

SPIOLTO RESPIMAT is contraindicated in patients with hypersensitivity to olodaterol, tiotropium bromide or any component of the drug;

in patients who have previously been hypersensitive to atropine or its derivatives, such as ipratropia and oxytropia;

it is not recommended for use in children under 18 years of age (due to lack of data on efficacy and safety).

Side effects

Nervous system disorders:  dizziness, insomnia.

From the side of metabolism and nutrition: dehydration.

From the side of the visual organ:  increased intraocular pressure, glaucoma; blurred vision.

From the cardiovascular system:  atrial fibrillation, palpitation, tachycardia, supraventricular tachycardia, increased blood pressure.

Respiratory, thoracic and mediastinal disorders:  cough, nosebleeds, pharyngitis, dysphonia, bronchospasm, laryngitis, sinusitis.

From the gastrointestinal tract:  mild dry mouth, constipation, oral candidiasis, dysphagia, gastroesophageal reflux, gingivitis, glossitis, stomatitis; intestinal obstruction, including paralytic intestinal obstruction.

From the side of the skin:  skin infections and ulcers on the skin, dry skin.

Allergic reactions:  rash, pruritus, angioedema, urticaria, hypersensitivity, including immediate reactions.

Musculoskeletal system and related connective tissue diseases:  arthralgia, swelling in the joints, back pain*.

From the side of the kidneys and urinary system:  dysuria, urinary retention (more common in men with predisposing factors), urinary tract infection.

Infections and infestations:  nasopharyngitis.

Interaction

Although no specific drug interaction studies have been conducted, tiotropium bromide has been co-administered with other COPD medications, including methylxanthines, oral steroids, and inhaled steroids, with no clinical signs of drug interactions.

Long-term co-use of tiotropium bromide with other m-cholinoblockers has not been studied. Therefore, long-term co-use of Spiolto Respimat with other m-cholinoblockers is not recommended.

Concomitant use of other adrenergic medications may increase the undesirable effects of Spiolto Respimat.

Concomitant use of xanthine derivatives, steroids, or diuretics (not related to the potassium-sparing group) may increase the hypokalemic effect of adrenomimetics.

Beta-blockers may weaken or counteract the effect of olodaterol. In this case, the use of bega 1-adrenoblockers is preferable, although they should also be used with caution.

MAO inhibitors, tricyclic antidepressants, or other drugs that can prolong the QTc interval may increase the effect of Spiolto Respimat on the cardiovascular system.

Co-use of olodaterol with ketoconazole resulted in a 1.7-fold increase in systemic exposure to olodaterol. However, this did not affect security. No dose adjustment is required.

How to take, course of use and dosage

The recommended therapeutic dose is 2 inhalations of Respimat spray (5 mcg / therapeutic dose of tiotropium bromide and 5 mcg / therapeutic dose of olodaterol) 1 time/day, at the same time of day (see Instructions for use).

In elderly patients, you can use the drug Spiolto Respimat at the recommended dose.

In patients with mild to moderate hepatic insufficiency, Spiolto Respimat can be used at the recommended dose.

There are no data on the use of olodaterol in patients with severe hepatic insufficiency.

In patients with impaired renal function, you can use the drug Spiolto Respimat at the recommended dose.

Patients with moderate to severe renal insufficiency using Spiolto Respimat should be carefully monitored by a doctor.

Overdose

Overdose of olodaterol can lead to pronounced effects typical of beta-2-adrenomimetics, such as myocardial ischemia, increased or decreased blood pressure, tachycardia, arrhythmias, palpitations, dizziness, nervousness, insomnia, anxiety, headache, tremor, dry mouth, muscle spasms, nausea, fatigue, malaise, hypokalemia, hyperglycemia and metabolic acidosis.

When using high doses of tiotropium bromide, manifestations of m-holinoblocking action are possible. After 14 days of inhaled use of tiotropium bromide in doses up to 40 mcg, no significant adverse events were observed in healthy individuals, except for a feeling of dryness of the nasal and oropharyngeal mucous membranes, the frequency of which depended on the dose (10-40 mcg/day). The exception was a clear decrease in salivation, starting from the 7th day of drug use.

Treatment

Spiolto Respimat should be discontinued. Supportive and symptomatic treatment is indicated. In severe cases, hospitalization is necessary. The use of beta-1 blockers may be recommended, but only with extreme caution, as the use of these drugs can cause bronchospasm.

Special instructions

The drug Spiolto Respimat should not be used for bronchial asthma. The efficacy and safety of Spiolto Respimat in bronchial asthma have not been studied.

Hypersensitivity

Immediate hypersensitivity reactions may occur after the use of Spiolto Respimat.

Acute bronchospasm

The drug Spiolto Respimat is not indicated for the treatment of acute episodes of bronchospasm, i. e. as an ambulance.

Paradoxical bronchospasm

The use of Spiolto Respimat, like other inhaled medications, can lead to paradoxical bronchospasm, sometimes life-threatening. If paradoxical bronchospasm develops, the use of Spiolto Respimat should be stopped immediately and alternative therapy should be prescribed.

Patients with impaired renal function

Becausetiotropium bromide is mainly excreted by the kidneys in patients with moderate to severe renal insufficiency (CC

Visual disturbances

Patients should be informed about the correct use of Spiolto Respimat. Do not allow the solution or aerosol to get into the eyes. Pain or discomfort in the eyes, blurred vision, visual halos around light sources, combined with redness of the eyes caused by conjunctival and corneal edema can be symptoms of acute angle-closure glaucoma. If any combination of these symptoms develops, you should immediately consult a specialist. Eye drops that have a myotic effect are not considered an effective treatment.

Cardiovascular effects

Olodaterol, like other beta-adrenomimetics, may have a clinically significant effect on the cardiovascular system in some patients (increased pulse rate, increased blood pressure and/or the appearance of related symptoms). If these symptoms occur, discontinuation of treatment may be necessary. In addition, beta-2-adrenomimetics have been reported to cause ECG changes such as T wave flattening and ST segment depression, although the clinical significance of these changes is unknown.

Hypokalemia

Beta-2-adrenomimetics in some patients can lead to the development of hypokalemia, which creates prerequisites for the occurrence of undesirable effects on the cardiovascular system. The decrease in the concentration of potassium in the blood serum is usually short-lived and does not require its replenishment. In patients with severe COPD, hypokalemia may increase due to hypoxia and concomitant treatment and increase the risk of arrhythmias.

Hyperglycemia

Inhaled use of high doses of beta-2-adrenomimetics may lead to an increase in the concentration of glucose in the blood plasma.

Spiolto Respimat should not be used in combination with any other medicinal product containing long-acting beta-2-adrenomimetics.

Patients who frequently use short-acting inhaled beta-2-adrenomimetics (for example,4 times a day) should be instructed that these drugs are used only to relieve acute symptoms of bronchospasm.

Spiolto Respimat is intended for the maintenance treatment of patients with COPD. Due to the fact that the general population of COPD is significantly dominated by patients over the age of 40 years. when prescribing the drug to patients younger than 40 years of age, spirometric confirmation of the diagnosis of COPD is required.

Effect of the drug on the ability to drive vehicles and mechanisms

Studies on the effect on the ability to drive vehicles and mechanisms have not been conducted. Caution should be exercised when performing these activities, as dizziness or blurred vision may develop.

Form of production

Metered dose solution for inhalation

Active ingredient

Olodaterol, Tiotropium bromide

Conditions of release from pharmacies

By prescription

Dosage form

solution for inhalation

Purpose

Adults as prescribed by a doctor

Indications

Bronchial Asthma, Low Learning Rate, Bronchitis