Composition and release form
Capsules with powder for inhalation 1 cap.
tiotropium bromide 18 mcg
(equivalent to 22.5 mcg tiotropium bromide monohydrate)
excipients: lactose monohydrate
in a blister pack 10 pcs.; in a cardboard pack of 1, 3 or 6 packages complete with the HandiHaler inhaler or without an inhaler.
pharmachologic effect
Anticholinergic, bronchodilator.
The result of inhibition of M3 receptors in the airways is the relaxation of bronchial smooth muscles. High affinity for M3 receptors and slow dissociation from them determine a pronounced and long-lasting bronchodilator effect in inhalation use in patients with chronic obstructive pulmonary disease (COPD).
Indications
As maintenance therapy in patients with COPD, including Chronical bronchitis and emphysema (with persistent shortness of breath and to prevent exacerbations).
Contraindications
Hypersensitivity (including to atropine or its derivatives, for example, ipratropium or oxitropium), first trimester of pregnancy, age under 18 years.
Use during pregnancy and breastfeeding
Contraindicated in the first trimester of pregnancy. During other periods of pregnancy and breastfeeding- only if the expected benefit exceeds any possible risk for a fetus or infant.
Side effects
From the gastrointestinal tract: dry mouth (usually mild degree severity, often disappears with continued treatment), constipation.
From the respiratory system: cough, local irritation, possible development of bronchospasm, as well as when taking other inhalation agents.
Other: tachycardia, difficulty or retention of urination (in men with predisposing factors), angioedema, blurry vision, acute glaucoma (associated with anticholinergic effects).
It is possible to use tiotropium bromide in combination with other drugs commonly used for COPD treatment, - sympathomimetics, methylxanthines, oral and inhaled steroids.
Directions for use and doses
Inhalation using the HandiHaler device, 1 caps. per day at the same time. The capsules should not be swallowed.
Elderly people and patients with impaired renal or liver function can use the drug in recommended doses.
Instructions for use of the HandiHaler device
The HandiHaler device was specially designed for Spiriva and is used for 1 year. It should not be used to take other medications.
The HandiHaler device includes:
1) dust cap;
2) mouthpiece;
3) base;
4) piercing button;
5) central chamber.
Using the HandiHaler device
Open the dust cap by lifting it up.
Then open the mouthpiece.
Remove the Spiriva capsule from the blister (immediately before use) and place it in the central chamber. It does not matter which side the capsule is placed in the chamber.
Close the mouthpiece tightly until it clicks, leaving the dust cap open.
Holding the HandiHaler with the mouthpiece up, press the piercing button fully 1 time and then release. This creates an opening through which the drug is released from the capsule during inhalation.
You need to exhale completely without exhaling into the mouthpiece, then take the HandiHaler into your mouth and press your lips tightly around the mouthpiece. Keeping your head straight, inhale slowly and deeply, but at the same time with enough force to hear the vibration of the capsule. Take a deep breath; then hold your breath until you feel discomfort, while simultaneously removing the HandiHaler from your mouth. Continue breathing calmly.
Repeat the procedure to completely empty the capsule.
Open the mouthpiece again. Remove and discard the used capsule.
Close the mouthpiece and dust cap.
Clean the HandiHaler once a month.
Open the mouthpiece and dust cap. Then open the base of the device by lifting the piercing button. Rinse the inhaler thoroughly in warm water until complete removal powder. Wipe the HandiHaler with a paper towel and leave the mouthpiece, base and dust cap open to air dry for 24 hours. After cleaning the device according to the instructions, it is ready for the next use. If necessary outside surface The mouthpiece can be cleaned using a damp but not wet cloth.
Opening the blister
Separate the blister strip.
Open the blister strip immediately before use so that one capsule is completely visible.
Take out the capsule.
Neither in the device nor in the blister capsules should be exposed to high temperatures, i.e. action sun rays and etc.
Overdose
Symptoms: possible dry mouth, impaired accommodation, increased heart rate.
Treatment: symptomatic therapy.
Precautionary measures
Close monitoring of patients with moderate or severe renal failure receiving the drug in combination with other drugs excreted mainly by the kidneys.
Prescribed with caution to patients with narrow-angle glaucoma, hyperplasia prostate gland or bladder neck obstruction.
special instructions
The drug should not be used as an initial treatment for acute attacks bronchospasm (that is, in emergency cases).
As with other inhalation products, medicines, after inhalation, immediate hypersensitivity reactions may develop.
Do not allow the powder to get into your eyes.
The drug should only be used with the HandiHaler device.
Storage conditions
At a temperature not exceeding 25 °C (do not freeze). Do not freeze.
Keep out of the reach of children.
Best before date
Do not use after the expiration date stated on the package.
Compound
Active substance: tiotropium bromide;
1 capsule contains tiotropium bromide monohydrate 22.5 mcg, which corresponds to tiotropium 18 mcg
Excipients: micronized lactose, lactose 200 M.
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Dosage form
Powder for inhalation, hard capsules.
Basic physical and chemical properties: hard gelatin capsules, size 3, containing white powder, for use with the HANDYHALER device;
Capsule shell: according to the relevant production procedure, light green, opaque, imprinted in black with the company symbol / TI 01.
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Pharmacological group
Drugs for the treatment of obstructive airway diseases, inhalation agents. Anticholinergics.
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Pharmacological properties
Pharmacological.
Mechanism of action. Tiotropium is a specific anticholinergic agent long acting. Tiotropium has a similar affinity for all muscarinic receptor subtypes (M 1 to M 5). In the airways, inhibition of M3 receptors causes smooth muscle relaxation. IN preclinical studies in vitro and in vivo, the bronchoprotective effect was dose-dependent and lasted more than 24 hours.
The duration of the effect is due to the very slow release from M 3 receptors; The half-life of tiotropium is significantly longer than that of ipratropium. As an N-quaternary anticholinergic, tiotropium is locally (bronchial) selective when administered by inhalation and exhibits an acceptable therapeutic range until systemic anticholinergic effects are detected. Dissociation from M2 receptors is faster than from M3 receptors functional studies in vitro. M 3 is a more acceptable (kinetically controlled) receptor subtype selectivity than M 2 . High activity and slow dissociation from the receptors have been clinically correlated with significant and prolonged bronchodilation in patients with chronic obstructive pulmonary disease (COPD).
Pharmacodynamic effects. Bronchodilation following inhalation of tiotropium is primarily a local effect on Airways, which is not systemic.
When Spiriva was used once daily, there was a significant improvement in lung function (increased forced expiratory volume in the first second (FEV 1) and forced vital capacity lungs) within 30 minutes after the first dose, the effect lasted 24 hours. Pharmacodynamic steady state is achieved within one week. In most patients, bronchodilation occurs on the 3rd day.
Based on daily measurements, Spiriva significantly improves morning and evening maximum expiratory flow.
Improvement in lung function persists without signs of tolerance.
Bronchodilation continued over the 24-hour dosing interval compared with placebo. It did not take into account whether Spiriva was prescribed in the morning or in the evening.
Spiriva significantly reduces shortness of breath; improvement in condition persisted throughout the entire treatment period.
Spiriva significantly reduces the number of exacerbations of COPD and increases the time until the onset of the first severe exacerbation.
Spiriva significantly improves the quality of life and health; improvements persisted throughout the treatment period.
Spiriva significantly reduces the number of hospitalized patients with exacerbations of COPD and delays the time to first hospitalization.
In two studies, Spiriva significantly improved tolerance to physical activity, limited by symptoms of the disease, by 19.7% and 28.3%.
In a study, the use of Spiriva 18 mcg and 54 mcg (three times 18 mcg) for 12 days did not cause prolongation of the QT interval as measured by ECG.
In a four-year study of 5,993 patients, Spiriva maintained improvements in FEV 1 over the entire period, but did not change the overall annual decline in FEV 1.
During treatment, the risk of mortality decreased by 16%. The overall incidence of death was 4.79 per 100 patient-years in the placebo group compared with 4.10 per 100 patient-years in the tiotropium group (hazard ratio (tiotropium/placebo) 0.84, 95% CI 0.73; 0.97). Treatment with tiotropium reduced the risk respiratory failure by 19% (2.09 versus 1.68 cases per 100 patient-years, relative risk (tiotropium/placebo) - 0.81, 95% CI - 0.65, 1.00).
Pharmacokinetics. Tiotropium is a quaternary ammonium compound and is moderately soluble in water. Tiotropium is used in the form of a dry powder for inhalation. As a rule, when administered by inhalation, most of the dose is released, deposited in gastrointestinal tract and in smaller quantities - in the lungs.
Absorption. After inhalation of the dry powder, the bioavailability is 19.5%, which is a sign of the high bioavailability of the fraction that reaches the lungs. The bioavailability of tiotropium solution for oral use is 2-3%. The maximum concentration of tiotropium in the blood plasma is achieved 5-7 minutes after inhalation.
At steady state, the maximum plasma level of tiotropium in patients with COPD was 12.9 pg/ml and decreased rapidly in a multicompartment model. Minimum concentration tiotropium in blood plasma at steady state is 1.71 pg/ml. Systemic exposure following inhalation of tiotropium through the HANDYHALER devices was similar to exposure following inhalation of tiotropium through the RESPIMAT inhaler.
Distribution. 72% of the drug binds to blood plasma proteins. The volume of distribution is 32 l/kg. Local concentration in the lungs is unknown, but based on the route of administration, high concentrations in the lungs are acceptable. Animal studies have shown that tiotropium does not penetrate the blood-brain barrier to a significant extent.
Metabolism. The degree of biotransformation is low, since 74% of the unchanged substance was excreted in the urine after administration to healthy volunteers. Tiotropium ester decomposes non-enzymatically to the alcohol N-methylscopine and dithienylglycolic acid, which do not bind to muscarinic receptors.
Further on in-vitro studies on liver microsomes and hepatocytes tiotropium (<20% дозы после внутривенного введения) метаболизируется путем зависимого от цитохрома Р450 окисления и последующей глутатионовой конъюгации в различных метаболитов фазы II в. Этот ферментный цепь может подавляться ингибиторами CYP450 2D6 (и ЗА4), хинидином, кетоконазолом и гестоденом. Указанные CYP450 2D6 и ЗА4 участвуют в метаболических превращениях, которые отвечают за вывод меньшей части дозы. Тиотропий даже в супратерапевтичних концентрация не ингибирует цитохром Р450 1А1, 1А2, 2В6, 2С9, 2С19, 2D6, 2Е1 и ПО на микросомах печени.
Excretion. The effective half-life of tiotropium is between 27 and 45 hours after administration in patients with COPD. The total clearance was 880 ml/min after administration to young healthy volunteers. After administration, tiotropium is primarily excreted unchanged in the urine. After inhalation of the dry powder, urinary excretion is 7% (1.3 mcg) of the unchanged amount within 24 hours, the remainder is not absorbed by the intestines and is excreted in the feces. The renal clearance of tiotropium exceeds the clearance of creatinine, indicating excretion in the urine. After continuous daily inhaled use in patients with COPD, a pharmacokinetic steady state was achieved after 7 days without further accumulation.
Linearity/nonlinearity. Tiotropium has demonstrated linear pharmacokinetic properties across the therapeutic range regardless of dosage form.
Pharmacokinetics in elderly patients. As with all drugs that are primarily excreted in the urine, renal clearance is reduced when tiotropium is used in elderly patients (365 ml/min in elderly patients with COPD<65 лет по сравнению с 271 мл / мин у пациентов с ХОБЛ в возрасте ≥ 65 лет). Это не приведет к соответствующему увеличению значений AUC 0-6, ss или C max , ss .
Pharmacokinetics in patients with impaired renal function. Inhaled use of tiotropium once daily in patients with COPD in a steady state with mild renal failure (creatinine clearance 50-80 ml/min) led to a slight increase in AUC values 0-6, ss (by 1.8-30%) and receiving similar Cmax values compared to patients with normal renal function (creatinine clearance >80 ml/min).
In COPD patients with moderate to severe renal impairment (creatinine clearance<50 мл / мин) введение тиотропия приводит к увеличению вдвое общей экспозиции (показатель AUC 0-4год выше на 82%, показатель C max выше на 52%) по сравнению с пациентами с нормальной функцией почек, что подтверждается данными о концентрации в плазме крови после ингаляции сухого порошка.
Pharmacokinetics in patients with impaired liver function. Hepatic impairment does not have a significant effect on the pharmacokinetics of tiotropium. Tiotropium is primarily excreted by renal elimination (up to 74% in young healthy volunteers) and by simple non-enzymatic ester degradation to products that do not bind to muscarinic receptors.
Patients with COPD of the Japanese nation. In a crossover comparison, the mean peak tiotropium plasma concentration 10 minutes after dosing at steady state was 20% to 70% higher in Japanese compared with Europeans after inhaled tiotropium, but there was no evidence of increased mortality or risk of cardiac complications in Japanese patients. there was no comparison with Europeans. For other races or ethnic groups, there is insufficient pharmacokinetic data.
Pharmacokinetics/pharmacodynamics relationship. There is no direct relationship between pharmacokinetics and pharmacodynamics.
Indications
Maintenance bronchodilator therapy to relieve symptoms in chronic obstructive pulmonary disease (COPD).
Contraindications
Spiriva inhalation powder is contraindicated in patients with known hypersensitivity to tiotropium bromide, atropine or its derivatives (pre-ipratropium or oxitropium) or to other components of the drug.
Interaction with other drugs and other types of interactions
Although formal drug interaction studies have not been conducted, tiotropium bromide has been used in combination with other drugs (sympathomimetics, bronchodilators, methylxanthines, oral and inhaled steroids used in the treatment of COPD) without clinical evidence of interaction with other drugs.
The use of long-acting beta-adrenergic agonists or inhaled corticosteroids has not been shown to alter tiotropium exposure.
However, Spiriva has not been studied in combination with anticholinergic drugs and is therefore not recommended for use.
Features of application
Spiriva is a bronchodilator that is prescribed once daily for maintenance therapy and is not intended for the initial treatment of acute bronchospasm attacks.
After using Spiriva, immediate hypersensitivity reactions are possible.
As with other anticholinergic drugs, Spiriva should be used with caution in patients with angle-closure glaucoma, prostatic hyperplasia, or bladder neck obstruction (see Adverse Reactions section).
Inhaled drugs may cause inhalation-induced bronchospasm.
The drug should be used with caution in the following patients: those who have recently suffered a myocardial infarction (<6 месяцев); лицам с любой неустойчивой или опасной для жизни аритмией или аритмией, которая требовала вмешательства или изменения терапии в прошлом году; госпитализированным с сердечной недостаточностью (NYHA класса III или IV) в течение последнего года. Эти пациенты были исключены из клинических испытаний. При таких состояниях антихолинергическим эффект может им навредить.
Because plasma concentrations of tiotropium bromide increase in patients with moderate to severe renal impairment (creatinine clearance £50 ml/min), Spiriva should only be used if the expected benefit outweighs the potential risk. There are no data on long-term use of Spiriva in patients with renal failure (see Section “Pharmacokinetics”).
Patients should avoid contact of the powder with the eyes. This may lead to worsening of angle-closure glaucoma, pain or discomfort in the eyes, temporary blurred vision, a sensation of halo or colored spots in front of the eyes, combined with redness of the eye in the form of conjunctival or corneal congestion.
If the listed symptoms appear in any combination, patients should stop using tiotropium bromide and, without wasting time, seek specialized medical help.
Dry mouth, which occurs with anticholinergic therapy, may potentially be associated with dental caries.
Spiriva should not be used more than once a day.
The drug contains 5.5 mg of lactose monohydrate per capsule.
Use during pregnancy or breastfeeding
Pregnancy. Data on the use of tiotropium in pregnant women are very limited. Preclinical studies have not revealed direct or indirect harmful effects associated with reproductive toxicity at clinically relevant doses. As a preventive measure, the use of Spiriva should be avoided during pregnancy.
Breastfeeding. It is not known whether tiotropium bromide passes into breast milk. Despite the results of studies conducted in rodents, which showed the excretion of tiotropium bromide into breast milk in only a small amount, the use of the drug during breastfeeding is not recommended.
Tiotropium bromide is a long-acting compound. The decision whether to continue/stop breastfeeding or continue/stop using Spiriva should be made taking into account the benefits of breastfeeding for the baby and the benefit of therapy for the woman.
Fertility. There are no clinical data available on the effects of tiotropium on fertility. Preclinical studies of tiotropium have not shown any adverse effects on fertility.
The ability to influence the reaction rate when driving vehicles or other mechanisms
The effect on the ability to drive a car or use other machinery has not been studied. Dizziness, headache, or blurred vision may affect your ability to drive a car or operate machinery.
Directions for use and doses
The medicinal product is intended for inhalation use only.
Capsules are for oral use; Spiriva capsules should not be swallowed.
The drug should only be used using the HENDYHALER inhalation device.
special groups
Elderly patients should use Spiriva only in the dosage recommended by the doctor.
Patients with renal failure should take Spiriva according to the dose recommended by the doctor. Information on the use of Spiriva in patients with moderate to severe renal failure (creatinine clearance ≤ 50 ml/min) is given in the sections “Peculiarities of use” and “Pharmacokinetics”.
Patients with liver failure can use Spiriva according to the dose recommended by the doctor (see Section “Pharmacokinetics”).
Instructions for use.
To ensure proper use of the drug, it is necessary to inform the patient how to use the inhaler.
When using Spiriva, you should follow your doctor's recommendations.
The HandyHaler inhalation device was developed specifically for Spiriva capsules. It should not be used with other medicines.
The HandiHaler inhalation device can be used for one year, provided it is used as intended.
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| 1. To open the dust cap, press the spray button all the way and release. |
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| 2. Open the dust cap by lifting it up. Then open the mouthpiece by lifting it up. |
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| 3. Remove the Spiriva capsule from the blister (immediately before use) and place it on the platform with the central chamber, as shown in the figure. It does not matter which side the capsule is placed into the chamber (5). |
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| 4. Close the mouthpiece tightly until it clicks, leaving the dust cap open. |
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| 5. Hold the HandyHaler with the mouthpiece up and press the spray button all the way once and release. This makes holes in the capsule shell and allows the drug to be released when inhaled. |
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6. Exhale completely. Important: do not exhale into the mouthpiece in any way. |
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| 7. Lift the HandyHeiler device into your mouth and wrap your lips tightly around the mouthpiece. Keep your head straight and inhale slowly and deeply, but in such a way that you hear or feel the vibration of the capsule. Inhale until the lungs are full; then hold your breath as long as possible and at the same time remove the mouthpiece from your mouth. Restore breathing. Repeat the steps indicated in Figures 6 and 7 again to completely empty the capsule. |
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| 8. Open the mouthpiece again. Remove the used capsule and discard. Close the mouthpiece and dust cap to store the HANDYHAILER device. |
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| Cleaning the HANDYHALER The HandiHaler device needs to be cleaned once a month. Open the dust cap and mouthpiece. Then open the base by lifting the spray button. Rinse the entire inhaler with warm water to remove the powder. Dry the HandyHaler thoroughly by blotting off any excess water with a paper towel and air drying, leaving the dust cap, mouthpiece and base uncovered. Air drying takes 24 hours, so cleaning should begin immediately after use to ensure the device is ready for the next use. If necessary, the outside of the mouthpiece can be cleaned using a damp, but not wet, cloth. |
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Spiriva capsules contain a small amount of powder, so the capsule is only partially filled.
Acute intoxication from oral administration of tiotropium capsules is unlikely due to low oral bioavailability.
Adverse reactions
Many of the side effects listed can be attributed to the anticholinergic properties of Spiriva.
Adverse reactions to the drug were determined from data obtained from clinical trials and spontaneous reports during the post-marketing period. The clinical trials database included 9647 patients treated with tiotropium in 28 placebo-controlled clinical trials with treatment periods ranging from 4 weeks to 4 years.
Incidence of adverse reactions according to MedDRA:
very often (≥ 1/10);
often (≥ 1/100,<1/10);
uncommon (≥ 1/1000,<1/100)
single (≥ 1/10000,<1/1000);
rare (<1/10000);
unknown (cannot be determined from available data).
From the side of metabolism:
unknown - dehydration.
From the nervous system:
infrequently - dizziness, headache, disturbance of taste;
isolated - insomnia.
From the organs of vision:
infrequently - blurred vision;
single - glaucoma, increased intraocular pressure.
From the cardiovascular system:
uncommon - atrial fibrillation
single - supraventricular tachycardia, tachycardia, palpitations.
From the respiratory system, chest and mediastinal organs:
infrequently - cough, dysphonia, pharyngitis;
isolated - bronchospasm, nosebleeds, laryngitis, sinusitis.
From the gastrointestinal tract:
often - dry mouth;
uncommon - constipation, gastroesophageal reflux disease, candidiasis of the oral cavity and pharynx
single - intestinal obstruction, including paralytic intestinal obstruction; dysphagia, gingivitis, glossitis, stomatitis, nausea
unknown - dental caries.
From the immune system, skin and subcutaneous tissue:
uncommon - rash;
single - angioedema, hypersensitivity (including immediate allergic reactions), itching, urticaria;
unknown - dry skin, skin infections and ulcers, anaphylactic reactions.
From the musculoskeletal system and connective tissue:
unknown - joint swelling.
From the urinary system:
uncommon - urinary retention, dysuria
single cases - urinary tract infection.
Description of selected adverse reactions
In controlled clinical trials, a commonly observed anticholinergic adverse reaction was dry mouth, occurring in approximately 4% of patients.
Package
10 capsules with powder for inhalation in a blister, 3 blisters in a cardboard box.
10 capsules with powder for inhalation in a blister, 1 or 3 blisters complete with the HANDYHALER device in a cardboard box.
Name
Spiriva.
International name: Tiotropium bromide.
Release form Spiriva inhaler capsules
Capsules with Spiriva inhalation powder, 10 or 30 pieces per pack.
Spiriva - indications for use
Spiriva is prescribed for maintenance treatment (including long-term treatment) in patients with chronic obstructive pulmonary disease (COPD).
The medicine can be prescribed for other diseases that are accompanied by airway obstruction, including data on the effectiveness of the drug in bronchial asthma (Spiriva is not the drug of choice for bronchial asthma and can be prescribed only if it is not possible to use an alternative remedy).
Description of the properties of the drug Spiriva
Spiriva is a drug that has a long-lasting anticholinergic effect. Spiriva affects all types of muscarinic receptors. With a single use of Spiriva, its bronchodilator effect continues for 24 hours, which makes it possible to use the drug once a day. Spiriva improves lung function, promotes deeper breathing and increases maximum expiratory flow.
During the treatment period, patients experience significant reduction in shortness of breath, a reduction in the frequency of bronchospasm attacks, an improved quality of life and a reduction in the number of hospitalizations due to exacerbation of chronic obstructive pulmonary disease.
Spiriva increases exercise tolerance and does not cause ECG changes (including with long-term use).
The use of the drug significantly reduces the risk of developing respiratory failure in patients with COPD.
Instructions for use of the medicine Spiriva
Take 1 capsule of Spiriva per day. The drug is administered using a special inhaler, such as the Respimat inhaler. When prescribing the drug to a patient, the doctor must explain the rules for using capsules. Capsules must not be swallowed. To obtain the best effect, inhalation is carried out at the same time of day, convenient for the patient.
The course of treatment is determined by the doctor; usually Spiriva is used for a long time to maintain remission in patients with chronic obstructive pulmonary disease. During an exacerbation, the combined use of Spiriva with inhaled glucocorticosteroids or other bronchodilator drugs is allowed.
With a decrease in liver and kidney function, the dosage of Spiriva does not change.
Side effects
Rarely observed, adverse effects are predominantly associated with the anticholinergic effect of tiotropium bromide. Nausea, glaucoma, increased intraocular pressure, tachycardia and atrial fibrillation, inflammatory diseases of the upper respiratory tract, cough and nosebleeds are possible. Undesirable effects from the digestive tract, metabolism and urinary system developed less frequently.
It is possible to develop paradoxical bronchospasm when using the drug Spiriva.
Contraindications
A strict contraindication for the use of Spiriva is individual intolerance to the components of the drug.
Relative contraindications are angle-closure glaucoma, bladder neck obstruction, prostatic hyperplasia, and pregnancy.
Spiriva composition
1 capsule with powder for inhalation contains:
Active substance:
Tiotropium bromide - 18 mcg;
Other Ingredients.
Spiriva analogues
There are no synonyms for the drug Spiriva.
Storage
Shelf life is no more than 2 years at room temperature.
Spiriva - manufacturer of the drug
Boehringer Ingelheim, Germany.
Spiriva - price in Moscow
The average price for Spiriva capsules 18 mcg n30 is 2,700 rubles (data from 09/13/2012)
Spiriva buy with delivery
You can take advantage of the free delivery service when purchasing Spiriva in our online pharmacy, and you can also buy Spiriva in one of
as maintenance therapy in patients with COPD, including chronic bronchitis and emphysema (maintenance therapy for persistent shortness of breath and to prevent exacerbations).
pharmachologic effect
A bronchodilator - a long-acting m-cholinergic receptor blocker.
It has equal affinity for various muscarinic receptor subtypes from M1 to M5. As a result of inhibition of M3 receptors in the airways, smooth muscles relax. The bronchodilator effect is dose dependent and lasts for at least 24 hours. The significant duration of action is probably due to a very slow release from M3 receptors compared to ipratropium bromide. When administered by inhalation, tiotropium bromide, as an anticholinergic agent of N-quaternary structure, has a local selective effect, while in therapeutic doses it does not cause systemic anticholinergic side effects. The release of tiotropium bromide from the connection with the M2 receptors occurs faster than from the connection with the M3 receptors. High affinity for receptors and slow release from binding to them determine an intense and long-lasting bronchodilator effect in patients with COPD.
Bronchodilation after inhalation of tiotropium bromide is a consequence of local rather than systemic action.
Clinical studies have shown that 30 minutes after a single dose of Spiriva® for 24 hours significantly improves lung function (increased FEV1 and FVC). Pharmacodynamic equilibrium was achieved within the 1st week, and a pronounced bronchodilator effect was observed on the 3rd day. Spiriva® significantly increases morning and evening peak expiratory flow rates measured by patients. The bronchodilator effect of Spiriva, assessed over a year, did not reveal any manifestations of tolerance.
Spiriva® significantly reduces the incidence of exacerbations of COPD and increases the period until the first exacerbation compared with placebo. Significantly improves the quality of life, which is observed throughout the entire treatment period. Spiriva® significantly reduces the number of hospitalizations associated with exacerbation of COPD and increases the time to first hospitalization.
Dosage regimen
Prescribed 1 capsule/day. at the same time in the form of inhalations using the HandiHaler inhaler.
The drug should not be swallowed. Spiriva should not be used more often than 1 time/day. Spiriva capsules should only be used with the HandiHaler inhaler.
Elderly patients should take the drug in recommended doses.
If kidney function is impaired, patients can use Spiriva in recommended doses. However, when prescribing Spiriva in combination with other drugs that are excreted primarily by the kidneys, monitoring the patient’s condition is necessary. Patients with moderate or severe renal failure (CR? 50 ml/min) require careful monitoring.
Patients with liver failure can take the drug in recommended doses.
How to use the HandiHaler® inhaler
The HandiHaler inhaler is designed specifically for the use of Spiriva and is not intended for taking other medications.
The inhaler includes: dust cap, mouthpiece, base, piercing button, central chamber.
Using the HandiHaler inhaler:
1. open the dust cap by pressing the piercing button fully and then releasing it;
2. completely open the dust cap by lifting it up; then open the mouthpiece by lifting it up;
3. immediately before use, remove the Spiriva capsule from the blister and place it in the central chamber (it does not matter which side the capsule is placed in the chamber);
4. Close the mouthpiece tightly until it clicks, leaving the dust cap open;
5. Holding the HandiHaler with the mouthpiece up, press the piercing button fully once and then release; thus, a hole is formed through which the drug is released from the capsule during inhalation;
6. exhale completely; never exhale into the mouthpiece.
7. take HandiHaler into your mouth and press your lips tightly around the mouthpiece; keeping your head straight, you should inhale slowly and deeply, but at the same time with enough force to hear the vibration of the capsule; inhale until your lungs are completely filled; then hold your breath as long as possible and remove the HandiHaler from your mouth; continue to breathe calmly; repeat procedures 6 and 7 to completely empty the capsule.
Cleaning the HandiHaler® inhaler
HandiHaler should be cleaned once a month. To do this, open the mouthpiece and dust cap, then open the base of the device by lifting the piercing button. Rinse the inhaler thoroughly in warm water until the powder is completely removed. HandiHaler should be wiped with a paper towel and with the mouthpiece, base and dust cap open, left to air dry for 24 hours. Once cleaned in this manner, the device is ready for subsequent use. If necessary, the outer surface of the mouthpiece can be cleaned using a damp, but not wet, cloth.
Opening the blister
Separate the blister strip along the perforated line. Open the blister strip immediately before use so that one capsule is completely visible. The capsule contains a small amount of powder, so it is not completely filled.
If the capsule is accidentally opened and exposed to air, it should not be used. Neither in the device nor in the blister, capsules should be exposed to high temperatures or exposure to sunlight.
Side effect
From the digestive system: slight dry mouth, often disappearing with continued treatment (? 1% and< 10%); кандидоз полости рта (? 0.1% и < 1%); запор, гастроэзофагеальный рефлюкс (? 0.01% и < 1%); в единичных случаях - кишечная непроходимость (включая паралитический илеус), дисфагия.
From the respiratory system: dysphonia, bronchospasm, cough and local irritation of the pharynx (? 0.1% and< 1%); носовое кровотечение (? 0.01% и < 1%).
From the cardiovascular system: tachycardia, palpitations (? 0.01% and< 1%); в единичных случаях - суправентрикулярная тахикардия, мерцательная аритмия.
From the side of the central nervous system: dizziness (? 0.1% and< 1%).
From the urinary system: difficulty urinating and urinary retention in men with predisposing factors, urinary tract infections (? 0.01% and< 1%).
Allergic reactions: rash, urticaria, itching, hypersensitivity reactions, including immediate reactions (? 0.01% and< 1%); в единичных случаях - ангионевротический отек.
Other: in isolated cases - blurred vision, increased intraocular pressure (? 0.01% and< 1%); глаукома.
Most of the above adverse reactions may be associated with the anticholinergic effect of Spiriva.
Contraindications to the use of SPIRIVA®
- I trimester of pregnancy;
- children and adolescents up to 18 years of age;
- hypersensitivity to atropine or its derivatives (including ipratropium and oxitropium);
- hypersensitivity to the components of the drug.
The drug should be used with caution in case of angle-closure glaucoma, prostatic hyperplasia, and bladder neck obstruction.
Use of SPIRIVA® during pregnancy and breastfeeding
The drug is contraindicated for use in the first trimester of pregnancy.
In the second and third trimesters of pregnancy and lactation, the drug should be prescribed only in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus or infant.
special instructions
The drug Spiriva® is not intended for the relief of acute attacks of bronchospasm.
After inhalation of Spiriva powder, immediate hypersensitivity reactions may develop.
The process of inhalation of Spiriva (as well as other inhaled drugs) can cause bronchospasm.
Patients with renal insufficiency (CrCl 50 ml/min) should be carefully monitored when prescribing Spiriva.
Patients should be familiarized with the rules for using the inhaler. Do not allow the powder to get into your eyes. Eye pain or discomfort, blurred vision, visual halos in combination with eye redness, conjunctival congestion and corneal edema may indicate an acute attack of angle-closure glaucoma. If any combination of these symptoms develops, the patient should consult a doctor immediately. The use of only drugs that cause miosis is not an effective treatment in this case.
One capsule contains 5.5 mg of lactose monohydrate.
Use in pediatrics
The use of the drug in children and adolescents under 18 years of age is contraindicated.
Impact on the ability to drive vehicles and operate machinery
No studies have been conducted to study the effect of the drug on the ability to drive vehicles and operate machinery. Cases of dizziness and blurred vision while using the drug may have a negative impact on the above-mentioned ability.
Overdose
Symptoms: when using high doses, manifestations of anticholinergic effects are possible - dry mouth, accommodation disturbances, increased heart rate.
After inhalation of a single dose of up to 282 mcg in healthy volunteers, no systemic anticholinergic effects were detected. After repeated administration of a single daily dose of 141 mcg, bilateral conjunctivitis in combination with dry mouth was observed in healthy volunteers, which disappeared with continued treatment. In a study examining the effects of multiple-dose tiotropium in COPD patients receiving a maximum of 36 mcg of the drug for more than 4 weeks, dry mouth was the only adverse effect.
Acute intoxication associated with accidental ingestion of capsules is unlikely due to the low bioavailability of the drug.
Drug interactions
It is possible to prescribe Spiriva in combination with other drugs commonly used to treat COPD: sympathomimetics, methylxanthine derivatives, oral and inhaled corticosteroids.
Limited information on combined use with anticholinergic drugs was obtained from two clinical studies: a single dose of 1 dose of ipratropium bromide against the background of continuous use of Spiriva in patients with COPD (64 people) and in healthy volunteers (20 people) did not lead to a decrease in adverse reactions or changes in life parameters and ECG. However, chronic concomitant use of anticholinergic drugs and Spiriva has not been studied and is therefore not recommended.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
The drug should be stored out of the reach of children at a temperature not exceeding 25°C; do not freeze. Shelf life - 2 years.
Once opened, use the blister within 9 days.
The HandiHaler device can be used for 1 year.
Spiriva is a drug with a bronchodilator, anticholinergic effect, increasing lung function and reducing shortness of breath.
Release form and composition
The dosage form of Spiriva is capsules with powder for inhalation: gelatin, hard, opaque, size No. 3, light greenish-blue color, the manufacturer’s logo and “TI 01” are written in black ink, the capsules contain white powder (10 pcs. in blisters, in a cardboard pack of 1, 3 or 6 blisters complete with or without the HandiHaler inhaler).
Composition of 1 capsule:
- active substance: tiotropium – 0.018 mg (in the form of tiotropium bromide monohydrate – 0.022 5 mg);
- auxiliary components: micronized lactose monohydrate – 0.275 mg, lactose monohydrate 200 M – 5.202 5 mg;
- capsule: gelatin – 44.516 mg, macrogol – 2.4 mg, titanium dioxide (E171) – 1.024 mg, indigo carmine (E132) – 0.012 mg, yellow iron oxide (E172) – 0.012 mg.
Indications for use
Spiriva is prescribed as maintenance therapy for chronic obstructive pulmonary disease (COPD), including emphysema and chronic bronchitis against the background of persistent shortness of breath, in order to prevent exacerbations.
Contraindications
- age under 18 years;
- I trimester of pregnancy;
- individual intolerance to the components of the drug, as well as atropine or its derivatives (including ipratropium and oxitropium).
Spiriva is prescribed with caution in the presence of the following diseases/conditions (relative contraindications):
- angle-closure glaucoma;
- bladder neck obstruction;
- prostatic hyperplasia;
- II-III trimester of pregnancy and breastfeeding period (prescription of Spiriva is possible only in cases where the expected benefit outweighs the possible risk).
Directions for use and dosage
Spiriva is taken 1 capsule per day as an inhalation using the HandiHaler inhaler, preferably at the same time of day.
- The capsule is removed from the blister immediately before use. If it is accidentally damaged or exposed to air, it should not be used. After removal, the capsule is placed in the central chamber (which side it is placed in the inhaler chamber does not matter).
- Before using the drug, you should exhale completely (do not exhale into the inhaler).
- The mouthpiece is placed in the mouth, tightly pressed between the lips, after which a slow deep breath is taken until the lungs are completely filled (head position is vertical). When used correctly, vibration of the capsule will be heard. Then you need to hold your breath as long as possible. After removing the inhaler, breathing is restored. The procedure is repeated 6-7 times (until the capsule is completely empty).
- After use, the empty capsule is removed and discarded.
The HandiHaler inhaler is intended only for the use of Spiriva.
The inhaler should be cleaned once a month: rinse it with warm water and then air dry it for 24 hours.
When used in combination with other drugs that are primarily excreted by the kidneys, renal function should be monitored. Patients with moderate/severe renal impairment (creatinine clearance ≤ 50 ml/min) require careful monitoring.
Side effects
The incidence of adverse reactions (> 10% - very common; > 1% and< 10% – часто; >0.1% and< 1% – нечасто; >0.01% and< 0,1% – редко; < 0,01%, включая отдельные сообщения – очень редко; с неизвестной частотой – при невозможности по имеющимся данным определить частоту развития нарушения):
- digestive system: often – dry mouth (usually mild); uncommon – constipation, stomatitis, gastroesophageal reflux; rarely - oropharyngeal candidiasis, glossitis, gingivitis, dysphagia, intestinal obstruction (including paralytic ileus);
- respiratory system, chest organs and mediastinum: infrequently - cough, dysphonia, pharyngitis; rarely – nosebleeds, paradoxical bronchospasm, sinusitis, laryngitis;
- nervous system: infrequently – dizziness; rarely – insomnia;
- musculoskeletal system: with unknown frequency - swelling of the joints (cause-and-effect relationship has not been confirmed);
- cardiovascular system: infrequently – atrial fibrillation; rarely - a feeling of increased heartbeat, tachycardia (including supraventricular tachycardia);
- kidneys and urinary tract: infrequently - difficulty urinating and retention (in men with predisposing factors), dysuria; rarely - urinary tract infections;
- metabolism: with unknown frequency - dehydration (cause-and-effect relationship has not been confirmed);
- skin: with unknown frequency - skin ulcers and skin infections, dry skin (cause-and-effect relationship has not been confirmed);
- organ of vision: infrequently – blurred vision; rarely – glaucoma, increased intraocular pressure;
- allergic reactions: infrequently - rash; rarely - itching, urticaria, hypersensitivity reactions, including immediate reactions; with unknown frequency - angioedema (cause-and-effect relationship has not been confirmed).
special instructions
Spiriva should not be used to relieve acute bronchospasm attacks.
It must be taken into account that inhalation can cause bronchospasm, and after the end of inhalation, immediate hypersensitivity reactions may develop.
During therapy, acute attacks of angle-closure glaucoma may occur. Main symptoms: discomfort/pain in the eyes, visual halos with corneal edema, red eyes and conjunctival congestion, as well as blurred vision. If these symptoms appear in any combination, consultation with a doctor is required (the use of exclusively medications that cause miosis is not an effective treatment).
Please note that 1 capsule contains 5.5 mg of lactose monohydrate.
Some adverse reactions, such as dizziness and blurred vision, may affect the ability to drive vehicles and operate machinery.
Drug interactions
The use of Spiriva is possible in combination with other drugs that are usually used in the treatment of COPD, including sympathomimetics, methylxanthine derivatives, inhaled/oral glucocorticosteroids.
Chronic combination use with anticholinergic drugs has not been studied and such combinations are not recommended.
Analogs
Analogues of Spiriva are: Sibri Breezhaler, Ipravent, Ipratropium, Truvent, Troventol, Atrovent.
Terms and conditions of storage
Store without freezing at temperatures up to 25 °C. Keep away from children.
Shelf life – 2 years.
Once opened, the blister can be used for 9 days.
The HandiHaler inhaler is suitable for use for 1 year.
Conditions for dispensing from pharmacies
Dispensed by prescription.
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