Olodaterol (Olodaterolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Beta-adrenomimetics

Included in the formulation
  • Striverdi® Respimat®
    solution d / inhal. 
    Boehringer Ingelheim International GmbH     Germany
    • АТХ:

    R.03.A.C.19   Olodaterol

    Pharmacodynamics:

    The drug is a β2-adrenomimetic, bronchodilator. Relaxation of smooth muscles with stimulation β2-adrenoceptors (conjugated to Gs-proteins, stimulating adenylate cyclase) is associated with an increase in the level of cAMP and activation of cAMP-dependent protein kinase in smooth muscle cells. cAMP-dependent protein kinase A inhibits the kinase of light chains of myosin, as a result, phosphorylation of light chains of myosin is disrupted and its interaction with actin does not occur. In addition, cAMP-dependent protein kinase A inhibits phospholampane (an inhibitor of Ca2 + -ATPase), as a result, the activity of Ca2 + -ATPase transporting Ca2 + from the cytoplasm to the sarcoplasmic reticulum increases in smooth muscle cells and the concentration of cytoplasmic Ca2 + decreases. All this leads to a decrease in the tone and contractile activity of smooth muscles. The drug is characterized by a rapid onset of action and continued preservation of the effect (up to 24 hours).

    Pharmacokinetics:

    Quickly absorbed with inhalation. Cmax in plasma is usually achieved within 10-20 minutes after inhalation.Absolute bioavailability of olodaterol was about 30%, with oral administration - about 1%. Thus, the systemic effect of olodaterol after inhalation is mainly due to absorption in the lungs, and the contribution of the swallowed portion of the dose to the systemic effect is negligible. Vd is 1110 liters, indicating a large distribution of the drug in the tissues.

    The connection with plasma proteins is 60%, the half-life is 22 hours for intravenous and 45 hours for inhalation. Excreted in urine.

    Indications:

    For long-term maintenance therapy in patients with chronic obstructive pulmonary disease, including chronic bronchitis and pulmonary emphysema, to reduce airway obstruction, improve quality of life, and tolerate physical exertion.

    ICD-10

    X.J40-J47.J42   Chronic bronchitis, unspecified

    X.J40-J47.J43   Emphysema

    X.J40-J47.J44   Other chronic obstructive pulmonary disease

    Contraindications:

    Age under 18 years, hypersensitivity.

    Carefully:

    With caution should be used for cardiovascular diseases, including unstable coronary heart disease,heart rate abnormalities, QT interval prolongation, hypertrophic obstructive myocardiopathy, hypertension, thyrotoxicosis, seizures, and also in patients with a history of which there are indications of such diseases as myocardial infarction or hospitalization for heart failure (during the previous year), life-threatening arrhythmia, paroxysmal tachycardia with a heart rate of more than 100 beats per minute.

    Pregnancy and lactation:

    Category FDA - C. Apply only if the potential benefit to the mother exceeds the potential harm to the fetus. The drug inhibits the contractile activity of the uterus. There were no studies on the effect of the drug on breast-feeding.

    Dosing and Administration:

    Use inhalation. Therapeutic dose of 5 mcg once a day.

    Side effects:

    From the respiratory system: nasopharyngitis.

    From the nervous system: dizziness.

    From the cardiovascular system: arterial hypertension.

    From the skin: rash.

    From the musculoskeletal system: arthralgia.

    Consider the possibility of developing side effects,characteristic of the whole class of β-adrenomimetics: tachycardia, arrhythmia, palpitation, myocardial ischemia, angina pectoris, hypertension or hypotension, tremor, headache, nervousness, insomnia, dizziness, dry mouth, nausea, muscle spasms, fatigue, malaise, hypokalemia, Hyperglycemia and metabolic acidosis.

    Overdose:

    Not described.

    Interaction:

    Adrenomimetics, methylxanthines increase the side effects of the drug.

    With the simultaneous use of xanthine derivatives, steroids or diuretics (not belonging to the group of potassium-sparing), it is possible to increase the hypokalemic effect of β-adrenomimetics.

    MAO inhibitors, tricyclic antidepressants or other drugs that can prolong the QT interval can increase the effect of olodaterol on the cardiovascular system.

    Simultaneous use of olodaterol with ketoconazole led to increased bioavailability of olodaterol, but this did not affect safety; correction of the dose is not required.

    Beta-adrenoblockers can weaken the effect of olodaterol or counteract this effect. therefore olodaterol should be used together with beta-blockers (including eye drops) only in forced situations. In this case, it is preferable to use cardioselective beta-blockers (with caution).

    Special instructions:

    Olodaterol is intended for maintenance treatment of patients with chronic obstructive pulmonary disease. Due to the fact that in the general population of chronic obstructive pulmonary disease patients predominantly over the age of 40 years, the appointment of the drug to patients under the age of 40 years requires spirometric confirmation of the diagnosis of chronic obstructive pulmonary disease.

    Olodaterol should not be used for bronchial asthma. Long-term efficacy and safety of olodaterol in bronchial asthma have not been studied.

    Impact on the ability to drive vehicles and manage mechanisms

    Care should be taken, dizziness may develop.

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