Spiriva Inhaler (Tiotropium bromide) is a long-acting antimuscarinic drug m-cholinoblocker, often called an anticholinergic agent in clinical practice. It has the same affinity for different subtypes of muscarinic receptors – from M1 to M5. The result of M3 receptors’ inhibition in the respiratory tract is the relaxation of smooth muscles. The bronchodilating effect is dose-dependent which lasts for at least 24 hours. A significant action duration is probably associated with very slow dissociation from the M3 receptors compared to ipratropium bromide. In the case of inhalation administration of tiotropium, this substance, as an N-quaternary anticholinergic, has a local selective effect, while at therapeutic doses it does not cause systemic m-anticholinergic side effects. Dissociation from M2 receptors occurs faster in comparison with M3. High affinity for receptors and slow dissociation cause an expressed and long-lasting bronchodilatory effect in patients with COPD.
Composition
- Active ingredient: 22.5 μg tiotropium bromide monohydrate, equivalent to 18 μg tiotropium.
- Additional components: lactose monohydrate 200 M; lactose monohydrate micronized.
- The composition of the capsule: gelatin, macrogol 3350, indigo carmine (E 132), titanium dioxide (E 171), iron oxide yellow (E 172).
Indications
It is prescribed as maintenance therapy for patients with COPD, including chronic bronchitis and emphysema (with persistent dyspnea and to prevent exacerbations).
Contraindications
- Hypersensitivity to atropine or its derivatives (for example, ipratropium or oxitropium) or components of this drug (in particular, to lactose monohydrate, which contains milk protein, due to lactase deficiency, lactose intolerance, glucose-galactose malabsorption);
- Pregnancy (I term);
- Children under 18 years old.
Take care in the case of the presence: angle-closure glaucoma, prostatic hyperplasia, the neck of the urinary bladder obstruction.
Side effects
- Metabolism and nutrition: dehydration.
- Digestive tract: often – a mild form of dry mouth; infrequently – stomatitis; constipation, GERD; rarely – oropharyngeal candidiasis, gingivitis, glossitis; intestinal obstruction, including paralytic ileus, dysphagia.
- Respiratory system, organs of the chest and mediastinum: infrequently – dysphonia, cough, pharyngitis; rarely – paradoxical bronchospasm, laryngitis, sinusitis, nosebleeds.
- Central nervous system: infrequently – atrial fibrillation; rarely, tachycardia (including supraventricular tachycardia), palpitations.
- Kidneys and urinary tract: infrequently – difficulty urinating and urinary retention (in men with predisposing factors), dysuria; rarely – urinary tract infections.
- Allergic reactions: infrequently – rash; rarely – urticaria, pruritus, hypersensitivity reactions, including immediate type reactions, angioedema.
- Skin: skin infections and ulcers on the skin, dry skin.
- Musculoskeletal system and related connective tissue diseases: swelling of joints.
- Nervous system: infrequently – dizziness; rarely – insomnia.
- Organ of vision: infrequently – blurry vision; rarely – increased IOP, glaucoma.
Dosage and administration
It is prescribed for inhalation.
- When using Spiriva in the form of inhalation with the device HandiHaler, it is recommended to use 1 caps/day, at the same time. The drug is not intended for swallowing.
- Elderly patients should take Spiriva inhaler in recommended by doctor doses.
- Patients with impaired renal function can use this inhaler in the recommended doses.
- However, careful monitoring of patients with moderate or severe renal failure who are buying Spiriva inhaler is necessary (as is the case with other drugs that are mainly kidney-treated).
- Patients with liver failure can take this drug in recommended doses.
Overdose
When using high doses, manifestations of anticholinergic action are possible. However, systemic anticholinergic side effects were not detected after a single inhalation dose of up to 282 μg of tiotropium when taken by healthy volunteers.
Bilateral conjunctivitis in combination with the dry mouth was observed in healthy volunteers after repeated administration of a single daily dose of 141 μg. These effects were disappeared with long-lasting treatment. In a study that examined the effect of multiple doses of tiotropium in patients with COPD who received a maximum of 36 micrograms of the drug for more than 4 weeks, the only side effect was dry mouth. Acute intoxication associated with accidental ingestion of capsules is unlikely due to the low drug bioavailability.
Interactions
It is possible to use tiotropium in combination with other drugs commonly used for COPD treatment: sympathomimetics, methylxanthines, oral and inhaled corticosteroids. Combined use with long-acting beta2-agonists, inhaled GCS and their combinations do not affect tiotropium.
Limited information on co-administration with anticholinergic drugs was obtained from 2 clinical trials: a single dose of 1 dose of ipratropium bromide on the background of continuous Spiriva use in patients with COPD (64 patients) and healthy volunteers (20 people) did not result in a decrease in adverse reactions, changes in parameters and ECG. However, the constant combined use of anticholinergic drugs and Spiriva inhaler has not been studied and, therefore, is not recommended.
Pregnancy and lactation
There are no clinical data on this inhaler use during pregnancy. Preclinical trials did not reveal a direct or indirect adverse effect on pregnancy, embryo/fetus development, childbirth, or postnatal development.
Clinical data on the use of tiotropium by lactating mothers are not available. The results of animal studies suggest that a small amount of tiotropium is penetrated in breast milk.
Pregnant and lactating women should use this medication only if the expected benefit exceeds any possible risk to the fetus or newborn. Clinical data on tiotropium effects on human fertility are not available. Preclinical studies have not demonstrated any adverse effect on fertility.