Ipratropium bromide + Salbutamol (Ipratropii bromidum + Salbutamolum)

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

M-holinoblokatory

Beta-adrenomimetics

Included in the formulation
  • Iprimol Steri-Neb
    solution d / inhal. 
    AIVEX Pharmaceuticals Yukey Limited     United Kingdom
    • АТХ:

    R.03.A.L.02   Salbutamol and ipratropium bromide

    Pharmacodynamics:
    Combined drug with a pronounced bronchodilator effect, caused by the action of ipratropium bromide and salbutamol.
    Ipratropium bromide is an anticholinergic agent. Blocks M3-cholinoreceptors of smooth muscles of the tracheobronchial tree (mainly large and medium bronchi), suppresses reflex bronchoconstriction, reduces the secretion of the glands of the mucous membrane of the respiratory tract. Having a structural similarity with the molecule of acetylcholine, it is its competitive antagonist. Effectively prevents bronchoconstriction, resulting from the inhalation of cigarette smoke, cold air, the effects of various bronchospasmodiruyuschih agents, and also eliminates spasm of the bronchi associated with the influence of the vagus nerve.
    Salbutamol is a beta2-adrenergic agent that exerts an effect on the smooth muscles of the respiratory tract, causing its relaxation and preventing bronchoconstriction.Reduces resistance in the airways, increases the vital capacity of the lungs. Prevents the release of histamine, leukotrienes, prostaglandin D2 and other biologically active substances from mast cells. In recommended therapeutic doses does not have a negative effect on the cardiovascular system, does not cause an increase in blood pressure. To a lesser degree, in comparison with the drugs of this group, it has a positive chrono- and inotropic effect. Causes the enlargement of the coronary arteries.
    Joint inhalation of ipratropium bromide and salbutamol has a simultaneous local effect on muscarinic and beta2-adrenergic receptors of the lungs, resulting in increased bronchodilator effect. Systemic absorption with simultaneous inhalation of ipratropium bromide and salbutamol does not increase.
    Pharmacokinetics:

    Ipratropium bromide is rapidly absorbed after inhalation, but systemic bioavailability is less than 10% of the dose taken. Binding to plasma proteins (mainly with albumin and glycoprotein) - 9%. 46% of the drug is excreted by the kidneys.The half-life is about 1.6 hours after intravenous administration. Ipratropium bromide does not penetrate the blood-brain barrier.

    Salbutamol is quickly and completely absorbed after inhalation. Cmax Salbutamol in blood plasma is observed after 3 hours. Binding to plasma proteins - 10%. It is subjected to presystemic metabolism in the liver and intestinal wall. The half-life is 3-7 hours. It is excreted by the kidneys, mostly unchanged (30% of the dose for 24 hours) and in the form of an inactive phenol sulfate metabolite for 72 hours, and with bile. Salbutamol penetrates the blood-brain barrier, creating concentrations equal to about 5% of the concentration in the blood plasma.

    Indications:Bronchospasticsyndrome in patients with chronic obstructive pulmonary disease and bronchial asthma.
    ICD-10

    I.A15-A19   Tuberculosis

    X.J40-J47.J43   Emphysema

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

    X.J40-J47.J44.9   Chronic obstructive pulmonary disease, unspecified

    X.J40-J47.J45   Asthma

    Contraindications:

    Hypersensitivity to salbutamol, ipratropium bromide, atropine or their derivatives.

    Hypertrophic obstructive cardiomyopathy; tachyarrhythmia; pregnancy (I trimester); children's age (up to 12 years).

    Carefully:Closed-angle glaucoma; obstruction of the urinary tract (including against the background of prostatic hyperplasia); severe organic diseases of the cardiovascular system; pheochromocytoma; hyperthyroidism; insufficiently controlled diabetes mellitus; cystic fibrosis; myocardial infarction (recently transferred); pregnancy (II-III trimesters); lactation period.
    Pregnancy and lactation:The category of FDA recommendations is C. It is not recommended to prescribe the drug in the II and III trimesters of pregnancy and during breastfeeding, except when the expected benefit for the mother exceeds any possible risk to the fetus and infant. Contraindicated in the first trimester of pregnancy.
    Dosing and Administration:

    Inhalation with nebulizer inhalers or a system for non-invasive ventilation in a positive airway pressure regime.

    Adults, including elderly patients and children over 12 years old - 1 nebula with a sterile solution 3-4 times a day, in the form of inhalation, with the help of a nebulizer.

    Data on the use of the drug in children under 12 years are absent.

    Side effects:

    From the nervous system: headache, dizziness, excessive fatigue, paresthesia, insomnia, nervousness, movement coordination disorders, mental disorders and psychotic reactions such as dysphoria, memory impairment, fear, depression.

    From the cardiovascular system: heart palpitations, tachycardia; increased systolic blood pressure, arrhythmia, lowering of systolic blood pressure.

    From the digestive system: dry mouth, nausea, vomiting, taste perversion, diarrhea.

    From the respiratory system: cough, dysphonia, nasal congestion, stridor, paradoxical bronchospasm, shortness of breath.

    From the sense organs: violation of accommodation (if the product gets into the eyes); Eye contact may increase intraocular pressure, acute pain in the eye, visual acuity, mydriasis, scleral injection, conjunctival hyperemia, and closed angle glaucoma.

    From the musculoskeletal system: tremor, myalgia, muscle cramps, muscle weakness, arthralgia.

    From the urinary system: retention of urine, dysuria.

    From the side of metabolism: hypokalemia, hyperglycemia.

    Allergic reactions: angioedema, tongue, lips, face, skin rash (including hives, up to the giant), laryngospasm, bronchospasm, pruritus, anaphylactic shock.

    Other: alopecia, sweating.

    Overdose:

    Manifestations of an overdose of ipratropium bromide are unlikely due to low systemic absorption after inhalation or ingestion. As a consequence, all manifestations of an overdose are associated with the systemic action of salbutamol.

    Symptoms: headache, nausea, vomiting, angina, hypertension, hypotension, hypokalemia, hyperkalemia, tachycardia, arrhythmia, chest pain, tremor, hyperemia, anxiety, hallucinations and dizziness.

    Treatment: symptomatic, including the introduction of cardioselective beta-blockers. However, it should be borne in mind that these drugs can enhance bronchospasm.

    Interaction:

    Joint application of additional beta2adrenomimetics, glucocorticosteroids, anticholinergics and xanthine derivatives can enhance the bronchodilatory action of the combination on the respiratory tract and cause severe side effects.

    With concomitant treatment with beta-blockers, there may be a significant decrease in the effectiveness of the drug.

    MAO inhibitors and tricyclic antidepressants can enhance the beta-adrenergic effect of salbutamol and lead to a sharp drop in blood pressure.

    Inhalational anesthesia using anesthetics containing halogenated hydrocarbons, for example halothane, trichlorethylene and enflurane, may exacerbate side effects beta2-adrenomimetics on the cardiovascular system, which requires careful monitoring of the patients' condition. Alternatively, the drug can be discontinued before surgery.

    Theophylline and other xanthines increase the likelihood of developing tachyarrhythmias.

    The drug due to the hypokalemic effect of salbutamol can enhance the effect of stimulants of the central nervous system, increase the likelihood of glycosidic intoxication, enhance the cardiotropic action of thyroid hormones.

    Possible increase in the number of heartbeats and blood pressure on the background of taking the drug may cause the need to correct the dose of antihypertensive and antianginal drugs.

    Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol.

    Anticholinergic drugs increase the risk of increased intraocular pressure.

    Special instructions:

    To avoid overdose, do not exceed the maximum daily allowable dose. Patients should be instructed about the correct use of the drug with a nebulizer and warn about the inadmissibility of getting a solution or aerosol into the eyes.

    In patients with bronchial asthma or moderate-to-severe forms of chronic obstructive pulmonary disease, symptomatic treatment may be preferable to regular use.

    It is necessary to further analyze the attachment or enhancement of anti-inflammatory therapy to control inflammation of the airways in patients with bronchial asthma and steroid-dependent forms chronic obstructive pulmonary disease.

    Regular use of high dosages beta2-adrenomimetics, including in the composition of the drug, to control the symptoms of bronchial obstruction can worsen the course of the disease.With the increase of bronchial obstruction, a simple increase in the dose over a long period of time is inappropriate and even dangerous.

    To prevent a life-threatening deterioration in the course of the disease, the treatment plan of the patient should be reviewed, and especially the degree of adequacy of anti-inflammatory therapy with glucocorticosteroid drugs. When using an inhalation solution based on ipratropium bromide together with beta2-adrenomimetics rarely occurred cases of acute angle-closure glaucoma. Pain or discomfort in the eyes, fuzzy vision, the appearance of a characteristic halo in combination with reddening of the eyes, edema (from the conjunctival to the corneal) can be regarded as signs of the development of acute closed-angle glaucoma. If these symptoms do not disappear, it is necessary to begin treatment with myotics in the form of eye drops and immediately undergo an examination with a specialist.

    It should be explained to the patient that in the case of acute, rapidly worsening shortness of breath or an obvious decrease in the response to the drug, you should consult a doctor.

    Treatment beta2-adrenomimetics can lead to severe hypokalemia.Particular caution should be exercised in cases of severe airway obstruction, since the occurrence of hypokalemia can be facilitated by concomitant treatment with xanthine derivatives, diuretics and glucocorticosteroids. Hypokalemia can lead to an increased risk of arrhythmia in patients taking digoxin. In addition, hypoxia can aggravate the effect of hypokalemia on the heart rhythm. In such situations it is recommended to check the concentration of potassium in the blood serum.

    Patients with cystic fibrosis should be administered with caution because of the possible appearance of symptoms of gastrointestinal motility disorder. Such patients should be warned about the need to inform the doctor about any changes in the function of the digestive tract.

    If more doses are required to relieve the symptoms of bronchial obstruction (or bronchospasm) than recommended, a treatment plan should be reviewed.

    Influence on the ability to drive a car and work with machinery

    Data on the impact on the ability to manage motor vehicles and / or other mechanisms are not available. However, taking into account the possibility of developing side effects from the CNS, care should be taken during the treatment period.

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