Tiotropium bromide (Thiotropii bromidum)

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

M-holinoblokatory

Included in the formulation
  • Spiriva®
    capsules d / inhal. 
    Boehringer Ingelheim International GmbH     Germany
  • Spiriva® Respimat®
    solution d / inhal. 
    Boehringer Ingelheim International GmbH     Germany
  • Tiotropium-native
    capsules d / inhal. 
    NATIVA, LLC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    R.03.B.B   Holinblockers

    R.03.B.B.04   Tiotropium bromide

    Pharmacodynamics:

    The blocker of m-holinoretseptorov prolonged action.

    Has the same affinity for different subtypes of muscarinic receptors from M1 to M5, however, with M3 receptors interacts for a longer time. As a result of inhibition of M3 receptors in the airways, the smooth muscle relaxes. The bronchodilator effect is dose dependent and persists for at least 24 hours.

    Pharmacokinetics:

    With inhalation, bioavailability is 19.5%. The connection with plasma proteins is 72%. Half-life with inhalation 5-6 days. Biotransformation in the liver is insignificant. Most of the inhaled dose is swallowed and excreted unchanged with feces. Elimination of the absorbed part mainly by the kidneys.

    Indications:

    As maintenance therapy in patients with COPD, including chronic bronchitis and emphysema (maintenance therapy with persistent dyspnea and to prevent exacerbations).

    ICD-10

    X.J40-J47.J43   Emphysema

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

    Contraindications:

    Hypersensitivity, pregnancy (I trimester), age to 18 years.

    Carefully:

    Closed-angle glaucoma, prostatic hyperplasia, obstruction of the neck of the bladder.

    Pregnancy and lactation:

    The drug is contraindicated in the first trimester of pregnancy.

    In the II and III trimesters of pregnancy and during lactation, the drug should be prescribed only in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus or infant.

    Recommendations for FDA - category C.

    Dosing and Administration:

    Assign 1 capsule / day at the same time.

    Side effects:

    From the side digestive system: slight dryness in the mouth, often disappearing as the treatment continues (≥1% and <10%); Candidiasis of the oral cavity (≥0.1% and <1%); constipation, gastroesophageal reflux (≥0.01% and <1%); in isolated cases - intestinal obstruction (including paralytic ileus), dysphagia.

    From the side respiratory system: dysphonia, bronchospasm, cough and local pharyngeal irritation (≥0.1% and <1%); nosebleeds (≥0.01% and <1%).

    From the side of cardio-vascular system: tachycardia, palpitation (≥0.01% and <1%); in single cases - supraventricular tachycardia, atrial fibrillation.

    From the side CNS: dizziness (≥0.1% and <1%).

    From the side urinary system: difficulty urination and urinary retention in men with predisposing factors, urinary tract infections (≥0.01% and <1%).

    Allergic reactions: rash, hives, itching, hypersensitivity reactions, including immediate-type reactions (≥ 0.01% and <1%); in isolated cases - angioedema.

    Other: in single cases - blurred vision, increased intraocular pressure (≥0.01% and <1%); glaucoma.

    Most of the above adverse reactions may be associated with the anticholinergic effect of the drug.

    Overdose:

    Strengthening of anticholinergic reactions (dry mouth, paresis of accommodation, tachycardia).

    Treatment symptomatic.

    Interaction:

    Anticholinergics or other drugs with anticholinergic activity - increased anticholinergic effects.

    Special instructions:

    It is not intended for relief of acute attacks of bronchospasm.

    After the inhalation of tiotropium bromide powder, the development of immediate-type hypersensitivity reactions is possible.

    The process of inhalation of tiotropium bromide (as well as other inhaled drugs) can cause bronchospasm.

    Patients with renal insufficiency (CK ≤ 50 mL / min) should be carefully monitored when tiotropium bromide is prescribed.

    Patients should be familiarized with the rules for using the inhaler. Do not let the powder get into the eyes. Pain in the eyes or discomfort, blurred vision, visual aureoles combined with red eyes, conjunctival stasis and corneal edema may indicate an acute attack of angle-closure glaucoma. If any combination of these symptoms develops, the patient should immediately consult a doctor. The use of only drugs that cause miosis, is not an effective method of treatment in this case.

    One capsule contains 5.5 mg of lactose monohydrate.

    Instructions
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