Spiriva
Spiriva: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Spiriva
ATX code: R03BB04
Active ingredient: tiotropium bromide (tiotropium bromide)
Producer: Boehringer Ingelheim Pharma (Germany)
Description and photo update: 2019-26-08
Prices in pharmacies: from 2000 rubles.
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Spiriva is a medication with anticholinergic and bronchodilating action, blocker of m-cholinergic receptors.
Release form and composition
Spiriva is available in the form of hard gelatin capsules with powder for inhalation: size No. 3, light greenish blue, opaque; the capsule is printed in black ink with the TI 01 marking and the company symbol; the contents of the capsules are white powder (10 pieces in blisters, in a cardboard box of 1, 3 or 6 blisters; 10 pieces in blisters, in a cardboard box of 1, 3 or 6 blisters, complete with a special handiHaler inhaler).
Composition for 1 capsule:
- active substance: tiotropium bromide monohydrate - 22.5 μg (corresponds to a tiotropium content of 18 μg);
- auxiliary components: micronized lactose monohydrate and lactose monohydrate 200 M;
- capsule shell: gelatin, indigo carmine, iron oxide yellow, macrogol, titanium dioxide.
Pharmacological properties
Pharmacodynamics
Spiriva is one of the long-acting m-cholinergic receptor blockers.
Has the same affinity for different subtypes of muscarinic receptors from M 1 to M 5. Due to the inhibition of M 3 receptors in the airways, a process of relaxation of smooth muscles is observed. The bronchodilating effect of Spiriva is dose-dependent and lasts for at least 24 hours.
This duration of action in comparison with ipratropium bromide is probably due to the very slow release from the bond with the M 3 receptors. Tiotropium bromide, when administered by inhalation, has a local selective effect; when used in therapeutic doses, systemic anticholinergic side reactions does not cause.
The release of the substance from the bond with the M 2 receptors occurs faster than from the bond with the M 3 receptors. Slow release from binding to receptors, due to high affinity for them, leads to the development of an intense and long-lasting bronchodilatory effect in patients with COPD (chronic obstructive pulmonary disease).
After inhalation of tiotropium bromide, bronchodilation is a consequence of systemic rather than local action.
As a result of clinical studies, it was found that 30 minutes after a single dose of Spiriva for 24 hours, lung function significantly improves, which is manifested by an increase in FEV 1 (forced expiratory volume in the first second of a forced expiratory maneuver) and FVC (the difference between air volumes in the lungs at the start and end points of the forced expiratory maneuver).
A pronounced bronchodilatory effect was observed on the third day of therapy, the development of pharmacodynamic equilibrium was noted during the first 7 days. The use of Spiriva can significantly increase the morning and evening peak flow rate of expiration. Manifestations of tolerance after evaluating therapy for a year were not identified.
The use of Spiriva can significantly reduce shortness of breath throughout the treatment period. In two randomized, double-blind, placebo-controlled trials, the drug was shown to significantly improve exercise tolerance compared to placebo.
Other effects of Spiriva are also noted:
- persistent improvement in FEV 1 after application for 4 years without changing the rate of annual decrease in FEV 1;
- significant improvement in the quality of life, which is observed throughout the entire period of therapy. The drug significantly reduces the number of hospitalizations associated with exacerbation of COPD, while the time until the first hospitalization increases.
There is a statistically significant reduction in the risk of death during treatment by 16%.
Advantages of Spiriva in comparison with salmeterol therapy:
- an increase in the time to the first exacerbation;
- reducing the likelihood of exacerbations;
- an increase in the time of the onset of the first severe exacerbation, which requires hospitalization;
- a decrease in the annual number of moderate to severe exacerbations that require hospitalization.
Pharmacokinetics
Tiotropium bromide is a quaternary ammonium compound that is sparingly soluble in water.
After intravenous administration and inhalation of dry powder, it has linear pharmacokinetics within the therapeutic range.
The absolute bioavailability of the substance by inhalation is 19.5%. This indicates a high bioavailability of the drug fraction reaching the lungs.
C max (maximum concentration of the substance) in blood plasma after inhalation is reached in 5–7 minutes. Tiotropium bromide is poorly absorbed from the gastrointestinal tract; food intake does not affect the absorption of the substance. When the substance is taken orally in the form of a solution, the absolute bioavailability is 2-3%.
Binds to plasma proteins by 72%. V d (volume of distribution) is 32 l / kg.
In the equilibrium state, the C max value in the blood plasma in patients with COPD is 12.9 pg / ml and decreases rapidly, which indicates a multi-compartment type of substance distribution. In the equilibrium state, C min (the minimum concentration of the substance) in the blood plasma is 1.71 pg / ml.
It does not penetrate the blood-brain barrier.
Tiotropium bromide has an insignificant degree of biotransformation. It is cleaved non-enzymatically to dithienyl glycolic acid and alcohol-N-methylscopine, which do not bind to muscarinic receptors.
As a result of the studies, it was shown that the drug (less than 20% of the dose after intravenous administration) is metabolized using cytochrome P 450 isoenzymes by oxidation and subsequent conjugation with glutathione to form various metabolites. When using inhibitors of CYP2D6 and CYP3A4 (gestodene, quinidine and ketoconazole), metabolic disorders may occur. Thus, these isozymes are included in the metabolism of the drug.
After inhalation, T 1/2 (half-life) of tiotropium is in the range of 27–45 hours. The total clearance observed in young healthy volunteers after intravenous administration is 880 ml / min. The substance after intravenous administration is excreted mainly unchanged by the kidneys (74%). Renal excretion after inhalation of dry powder at steady state is 7% per day of the dose. The rest of the non-absorbed substance is excreted through the intestines.
The renal clearance of tiotropium is higher than the clearance of creatinine, which indicates tubular secretion. After long-term administration of Spiriva once a day by patients with COPD, the development of pharmacokinetic equilibrium is observed on the seventh day, while cumulation is not observed in the future.
In elderly patients, there is a decrease in renal clearance of tiotropium. However, this does not lead to a corresponding increase in AUC values of 0-6 (area under the concentration-time curve) or C max.
In mild renal impairment (with creatinine clearance in the range of 50–80 ml / min), inhalation of tiotropium once a day in an equilibrium state led to an increase in the AUC value of 0-6. In this case, the C max value did not change. Against the background of moderate / severe renal dysfunction (with creatinine clearance up to 50 ml / min), intravenous administration of the substance led to a 2-fold increase in the drug concentration in plasma. Similar changes are noted after inhalation of dry powder.
It is expected that liver failure will not have a significant effect on the pharmacokinetic parameters of tiotropium bromide, since the substance is excreted mainly in the urine, and the formation of pharmacologically active metabolites with the participation of enzymes is not associated.
Indications for use
According to the instructions, Spiriva is prescribed to patients with COPD (chronic obstructive pulmonary disease), including emphysema and chronic bronchitis, as a supportive treatment (to prevent exacerbations and with persistent shortness of breath).
Contraindications
- pregnancy period (first trimester);
- age up to 18 years;
- increased individual sensitivity to atropine, as well as its derivatives;
- increased individual sensitivity to any component of the drug.
Spiriva is used with caution in patients with prostatic hyperplasia, angle-closure glaucoma and bladder neck obstruction.
Instructions for the use of Spiriva: method and dosage
Spiriva capsules are intended for inhalation use (they must not be swallowed).
The recommended dose is 1 capsule once a day, at the same time. Do not exceed the indicated dosage. Capsules are used only with the HandiHaler inhaler.
With hepatic failure, mild renal failure and elderly patients, dose adjustment is not required.
In case of moderate or severe renal failure, as well as in the case of simultaneous use with drugs that are mainly excreted by the kidneys, it is necessary to monitor the patient's condition.
Recommendations for the use of the inhaler HandiHaler
Components of the HandiHaler inhaler: mouthpiece, center chamber, piercing button, base, dust cap.
Procedure during inhalation:
- Open the special dustproof cap (to do this, press the piercing button and release it).
- Open the cap completely, then open the mouthpiece.
- Take out the Spiriva capsule and place it in the central chamber.
- Close the mouthpiece tightly (a characteristic click is heard), the dust cap should be open.
- While holding the inhaler in an upright position with the mouthpiece up, press the piercing button once and release it (this creates a hole for the drug to be released from the capsule).
- Exhale (you cannot exhale into the mouthpiece).
- Grasp the mouthpiece tightly with your lips and inhale slowly and deeply so that the lungs are completely filled; hold your breath for the maximum possible time and remove the inhaler from your mouth; breathe calmly and repeat steps 6 and 7 to completely empty the capsule.
- Open the mouthpiece, take out and dispose of the used capsule, then close the inhaler.
The HandiHaler inhaler should be cleaned monthly. It should be rinsed in warm water, then wiped off with a paper towel and allowed to air dry for one day.
Before the inhalation procedure, the Spiriva capsules must be checked, they must be intact and undamaged.
Side effects
- cardiovascular system: palpitations, tachycardia; isolated cases - supraventricular tachycardia and atrial fibrillation;
- digestive system: oral candidiasis, slight dry mouth (disappears with continued therapy), gastroesophageal reflux, constipation; isolated cases - difficulty swallowing, intestinal obstruction;
- respiratory system: bronchospasm, epistaxis, local irritation of the pharynx, cough, dysphonia;
- urinary system: urinary tract infections, retention and difficulty urinating in men with risk factors;
- central nervous system: dizziness;
- allergic reactions: itchy skin, urticaria, rash, hypersensitivity reactions; isolated cases - Quincke's edema;
- other reactions: isolated cases - increased intraocular pressure, glaucoma, blurred vision.
Overdose
The main symptoms: disturbances of accommodation, dry mouth, increased heart rate (manifestations of anticholinergic action).
After inhalation of doses up to 282 μg once in healthy volunteers, systemic anticholinergic effects were not revealed. After repeated use of a single daily dose of 141 μg, the development of bilateral conjunctivitis in combination with xerostomia was noted, which, with continued treatment, passed independently. In a study that examined the effects of tiotropium with repeated use of Spiriva in patients with COPD who received a maximum of 36 mcg per day for more than 4 weeks, it was found that the only side effect was dry mouth.
The occurrence of acute intoxication associated with accidental ingestion of capsules is unlikely, which is associated with the low bioavailability of Spiriva.
special instructions
The drug is not intended for the relief of acute bronchospastic attacks.
After inhalation of Spiriva, an immediate hypersensitivity reaction may develop.
The process of inhalation of the drug (like other inhalation agents) can lead to the development of bronchospasm.
With renal failure (creatinine clearance ≤ 50 ml / min), careful monitoring of the patient's condition is required.
Powder from capsules should not come into contact with eyes. If symptoms of angle-closure glaucoma appear (blurred vision, corneal edema, conjunctival congestion, discomfort or pain in the eyes, visual halos with redness of the eyes), consult a doctor immediately.
One capsule of Spiriva contains 5.5 mg of lactose monohydrate.
Influence on the ability to drive vehicles and complex mechanisms
Studies on the effect of Spiriva on a patient's ability to drive and operate mechanisms have not been conducted, however, the possibility of developing such side effects as blurred vision and dizziness should be taken into account. If these reactions occur, it is recommended to be careful or to refuse to perform work associated with increased concentration of attention and a quick reaction.
Application during pregnancy and lactation
In the first trimester of pregnancy, Spiriva is contraindicated.
Information on the use of tiotropium bromide during pregnancy in humans is limited. In animal studies, direct / indirect adverse effects on pregnancy, embryo / fetal development, labor, or postnatal development have not been proven. In preclinical studies, it was found that tiotropium bromide in small amounts is excreted in breast milk.
As a precautionary measure in the II-III trimesters of pregnancy and during lactation, Spiriva should be used only in cases where the expected benefit outweighs the possible risk.
Pediatric use
Spiriva therapy is contraindicated in patients under 18 years of age.
With impaired renal function
When Spiriva is prescribed to patients with renal insufficiency (with creatinine clearance ≤ 50 ml / min), their condition should be monitored.
Drug interactions
Allowed to use Spiriva simultaneously with other drugs that are usually used for the treatment of COPD: methylxanthine derivatives, sympathomimetics, inhaled glucocorticosteroids and oral glucocorticosteroids.
The constant combined use of Spiriva and anticholinergics has not been studied, so this combination is not recommended. With a single simultaneous intake of the above drugs, changes in the ECG and vital parameters were not observed, the severity of adverse reactions did not decrease.
Analogs
Spiriva's analogues are Spiriva Respimat, Tiotropium-native.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C out of reach of children. Capsules must not be frozen, exposed to high temperatures or sunlight.
The HandiHaler inhaler is used for no more than a year. Opened blister with capsules must be used within 9 days.
The shelf life of the drug is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Spiriva
According to reviews, Spiriva is most often rated as an effective drug with good tolerance. A convenient dosing regimen is noted. In bronchial asthma, the agent can be used as part of a combination therapy. The main disadvantage is the high cost of the drug. Also, some consider it advisable to release capsules without an inhaler included.
The price of Spiriva in pharmacies
The approximate price for Spiriva (30 capsules) is 2416-2742 rubles.
Spiriva: prices in online pharmacies
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Drug name Price Pharmacy |
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Spiriva 18 mcg capsules with powder for inhalation complete with HandiHaler inhaler 30 pcs. 2000 RUB Buy |
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Spiriva Respimat 2.5 μg / dose 60 doses solution for inhalation complete with inhaler Respimat 4 ml 1 pc. 2423 RUB Buy |
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Spiriva Respimat solution for inhalation. 2.5mcg / dose 4ml 2697 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
