Spiolto Respimat Boehringer medicine for bronchodilator treatment (1 tube 4ml/60 times x 1 spray)
Dosage form Box
Specifications Tiotropium, olodaterol
Ingredient
| Composition information | Content |
| Tiotropium | 2.5mcg |
| Olodaterol | 2.5mcg |
Uses
Indications
Spiolto® Respimat® drugs are indicated for treatment of maintenance bronchodilator to reduce symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
Pharmacology
Pharmacological group treatment
Medicines for respiratory obstruction, Adrenergic agreed in combination with anti -cholinergic drugs.
Mechanism of action
Tiotropium, a long-lasting Muscarinic anti-antacarinic drug, and olodaterol, a beta2-adrenergic-acting owner, is coordinated in a fine-grain spray bottle. These two active ingredients are similar to bronchodilator effects because they have different mechanisms and the destination position on different lungs.
tiotropium
Tiotropium bromide is a prolonged Muscarinic receptor antagonist (Lama), clinically called cholinergic resistance. The drug has an equivalent affinity on Muscarinic receptors from M1 to M5. On the gas path, M3 receptor inhibitors on smooth muscles cause muscle relaxation. Competitive and reversible antagonism has been shown on receptors in humans, animals and isolated agencies.
In Vitro -in -Vivo Prelopician studies as well as in vivo, bronchial protection effect depends on the dose and lasts more than 24 hours. The prolonged time may be due to the slow decomposition rate of the drug from the M3 receptor, shown in the significant semi -decentralized time than ipratropium.Similar to anti -cholinergic drugs containing Group N of IV, Tiotropium has a selective effect on the spot (bronchial) when used inhaled. Therefore, the drug has an acceptable treatment interval before the body resistance is increased. The decentralization rate from receptor m2 is faster from the M3 receptor, which explains the selection of the drug on the M3 receptor compared to M2 in the in vitro (dynamic control).
High potential for attachment and slow -deliberation rate with clinical correlation, shown in significant and prolonged bronchodilator effects on COPD patients.
Bronchodilator effect after sniffing Tiotropium is mainly due to the local effect (on the gas path), not due to the systemic effect of this drug.
olodaterol
olodaterol has a strong affinity and high selection for his beta2-adrenergic receptor. In vitro studies show that Olodaterol has the host on the beta2-adrenergic receptor more than 241 times stronger than the beta1-adrenergic receptor and 2299 times stronger than the beta3-adrenergic receptor. The pharmacological effect of this substance is created by the ability to bind and activation of the beta2-adrenergic receptor after use on the spot in the inhalation line.
Activation of these receptors on the gas path that stimulates endogenous adenyl cyclase, an intermediate enzyme during the synthesis of 3 ', 5’-adenosine monophosphate ring (Camp). Increasing the concentration of Camp causes bronchiectasis through relaxation of plain muscle cells. Olodaterol has a predecessor properties of the Beta2-ADRENERGIC receptor receptor selection.
Beta-adrenergic receptors are divided into 3 subgroups, beta1-adrenergic receptors distributed mainly on the heart muscle, beta2-adrenergic receptor distributed mainly on smooth muscle and beta3-adrenergic receptors distributed mainly on adipose tissue. The substances on the beta2-adrenergic causing bronchiectasis.
Although the beta2-adrenergic receptor is the adrenergic receptor, mainly on the air of the gas pathway, this type of receptor is also present on the surface of many other cells, including epithelial and endothelial cells in the lungs and heart. The clear function of the Beta2-ADRENERGIC receptor receptor on the heart has not been determined, but the presence of this type of receptor increases the ability to act on the heart even the owner is highly selected on the beta2-adrenergic receptor.
pharmacokinetics
When using Tiotropium in combination with olodaterol in inhaled lines, the pharmacokinetic parameters of each component similar to when they are used separately.
pharmacokinetics of tiotropium and olodaterol linearly during the treatment dose. Use the dose repeated 1 time daily in the inhalation line, the stable state of Tiotropium is achieved after 7 days. Olodaterol's stable state is achieved after 8 days of dosage 1 time daily in inhalation and accumulating drugs up to 1.8 times compared to the single dose.
absorption
tiotropium
Data on drug excretion through urine on young healthy volunteers shows that about 33% of the inhaling dose from the fine -seeded Rescimat spray is absorbed into the circulation. The absolute bioavailability of the oral solution is about 2-3%. The maximum concentration of Tiotropium in plasma is achieved after 5-7 minutes of using respimat fine seed spray.
olodaterol
On the healthy, absolute bioavailability of olodaterol after using the inhaled form is estimated at 30%. On the contrary, absolute bioavailability when using oral solution is less than 1%. Olodaterol's maximum concentration in plasma is achieved after 10 to 20 minutes of using respimat fine particles.
distribution
tiotropium
Tiotropium combined with plasma proteins is about 72% and the distribution is 32 l/kg. Rat studies show that Tiotropium does not absorb through the brain barrier at any extent.
olodaterol
olodaterol binds to plasma proteins about 60% and an integral distribution 1110 l.
Biological metabolism
tiotropium
less metabolized. This is evident when up to 74% of the dosage of intravenous tract is eliminated in urine in the form of unchanged. Tiotropium's ester linking reaction does not require catalytic enzymes, creating compounds containing alcohol groups and corresponding AC/ID parts (N-methylscopine and dithienylglycolic acid). Both of these components are not associated with the Muscarinic receptor.
In vitro experiments with microsomes and human liver cells show that a amount of drugs (
olodaterol
Mainly metabolized by direct glucuronic pathway and o-demethylation in the methoxy group with the following conjugated reaction. Of the 6 defined metabolites, only Demethylation products are in unmingered form (SOM 1522) that is capable of binding to the beta2 receptor. However, this metabolite is not detected in plasma after repeated doses of recommended or up to 4 recommended dose.
Cytochrome P450 isozyme including CYP2C9, CYP3C8, along with negligible contributions of CYP3A4, catalyzed Olodaterol Demethylation reactions, while the ISOform of Uridine Diphosphate Glycosyl Transferase includes UGT2B7, UGT1A1, 1A7 and 1A9 and 1A9 - Glucuronide.
Elimination
tiotropium
Tiotropium intravenous sugar is excreted mainly by intact excretion through urine (74%). The total clearance of healthy volunteers is 880 ml/minute. When inhaled in the COPD patient, in a stable state, 18.6% of the dose is excreted in the urine, the rest is mainly the amount of drugs that are not absorbed in the intestine and are eliminated in feces.
Tiotropium's clearance through the kidneys is greater than the filtration rate of the glomerular filtration, proving that there is an active excretion process into the urine. Half of the lifetime of Tiotropium after using a spray on COPD patient about 27 to 45 hours.
olodaterol
The total clearance of olodaterol on a healthy volunteer is 872 ml/min, and the renal clearance is 173 ml/min. Half life eliminated after using intravenously 22 hours. On the contrary, half -life excreted after inhalation is about 45 hours, proving this value is influenced by the greater absorption process than the elimination process.
After using olodaterol, a 14C isotope is mounted in a vein, 38% of the dosage of radioactive material is found in the urine and 53% is found in the feces. The intact amount of olodaterol is found in urine after using intravenous tract of 19%. After drinking, only 9% of radioactive substances are found in urine, while a large amount is found in feces (84%).
After using intravenous and oral lines, over 90% of the dose is excreted for 6 days and 5 days. After using the inhalation form, in a stable state, intact olodaterol is excreted through the urine during the period between two use on healthy volunteers estimated at 5 - 7% of the dose.
Before taking Spiolto Respimat Boehringer medicine for bronchodilator treatment (1 tube 4ml/60 times x 1 spray)
How to use
use inhaled line.
The amount of medicine in each spray is the amount of drug supplied to the patient inhaling the suck tube of the spray bottle (2 sprays equivalent to 1 dose).
Dosage
recommended dose for adults is 5 micrograms Tiotropium and 5 micrograms olodaterol, equivalent to 2 sprays from the respimat fine -spray bottle, used once a day at the same time of the same day.
Elderly
Elderly patients can use Spiolto® Respimat® with the recommended dose as above.
Hepatic failure and kidney failure
Spiolto® Respimat® contains Tiotropium - a drug excreted mainly by the excretion through the kidneys and olodaterol - a drug excreted mainly by metabolism in the liver.
Hepatic failure
Patients with mild and medium liver failure can use Spiolto® Respimat® with recommended dose.
There is no data on the use of olodaterol in patients with severe liver failure.
Patients with renal failure
Patients with renal failure can use Spiolto® Respimat® with recommended dose.
Spiolto® Respimat® contains Tiotropium as a drug excreted mainly by the excretion through the kidneys. Therefore, it is necessary to closely monitor the use of Spiolto® Respimat® on patients with average and severe renal failure.
Children
There is no data related to the use of Spiolto® Respimat® on COPD patients. Safety and effectiveness of Spiolto® Respimat® on children has not been set.
Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What to do when overdose?
Symptoms
High doses of Tiotropium can cause anti -cholinergic symptoms and symptoms.
There are no adverse reactions related to treatment after 14 days of dose of up to 40 μg of Tiotropium in the form of aerosol solution on healthy people, except for dry mouth/throat, dry nasal mucosa with the percentage of the dose depends on the dose ratio [10 - 40 mcg/day] and reducing salivation secretion starts from Saturday onwards. No significant adverse effects are recorded in 6 studies that last for COPD patients using Tiotropium gas solution 10 mcg/day for 4 - 48 weeks.
Olodaterol overdose can lead to excessive effects, characteristic of the Beta2-ADRENERGIC's owner such as myocardial anemia, hypertension or lowering blood pressure, tachycardia, arrhythmia, nervousness, dizziness, stress, insomnia, anxiety, headache, tremor, dry mouth, muscle spasms, nausea, fatigue, hypoglycemic, hyperemia and metabolic acid.
Overdose
Should stop using Spiolto® Respimat®. Symptomatic treatment and supportive treatment. Severe cases should be hospitalized. The use of selected beta blockers on the heart, but must be especially cautious because the use of beta-adrenergic blockers can promote bronchospasm.
What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.
Side Effects
When using Spiolto® Respimat®, you may experience unwanted effects (ADR).
The safety of Spiolto Respimat is evaluated through cross -clinical trials, parallel and control groups with active ingredients over 7151 COPD patients. A total of 1988 patients with COPD use the target dose level of 5 micrograms Tiotropium and 5 micrograms olodaterol.The unwanted effects of Spiolto Respimat are determined mainly based on the data obtained from two clinical trials in parallel group, control with active ingredients, prolonged treatment (52 weeks) in COPD patients.
In this two long -lasting clinical trial analysis, the general ratio of adverse events in the group of patients using Spiolto Respimat is equivalent to a group of patients using Tiotropium -dose 5 micrograms or olodaterol 5 micrograms (74%, 73.3%and 76.6%).
Any unwanted effects previously recorded for one of the two ingredients of the drug are considered to be the adverse effects of Spiolto Respimat and are listed in the list below.
In addition, this list also includes adultery effects recorded for Spiolto Respimat but has not been recorded when used alone.
Nervous system disorders: dizziness, insomnia.
Respiratory disorders, chest and mediastinum: cough, nosebleeds, sore throat, difficulty pronouncing, bronchospasm, laryngitis, sinusitis.
musculoskeletal disorders and connective tissue: joint pain, joint swelling, back pain (adverse effects recorded with Spiolto Respimat but not recorded for each component).
Many unwanted effects have been listed above may be due to Tiotropium's cholinergic activity, or by Olodaterol's beta-adrenergic activity-two components of Spiolto Respimat.
In addition, it is also important to pay attention to other adverse effects related to the beta-adrenergic hosts that have not been listed above such as arrhythmia, myocardial ischemia, angina, hypotension, tremor, headache, stress, nausea, muscle spasms, fatigue, discomfort, hypotension, hyperglycemia and metabolic acidosis.
Instructions on how to handle ADR
When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Spiolto® Respimat® drug is contraindicated in the following cases:
Patients with a history of hypersensitivity to atropine or its conductors such as ipratropium or oxitropium.
Caution when using
General warning
Do not use Spiolto Respimat more than once a day.
Do not use Spiolto Respimat on asthma patients. Safety and effectiveness of Spiolto Respimat in Hen patient has not been studied.
Level bronchial spasm
Spiolto Respimat is not indicated to treat acute bronchospasm, which is not used as a cutting medicine.
hypersensitivity
Similar to all other drugs, hypersensitivity reactions may appear immediately after using Spiolto Respimat.
Naughty bronchospasm
Similar to other inhaled drugs, Spiolto Respimat can cause lifelong bronchospasm. If the bronchospasm is often inverse, should stop the drug immediately and use alternative therapy.
Narrow angle glaucoma, prostate proliferation or bladder obstruction.
Due to Tiotropium's anti -cholinergic properties, caution should be used with spiolto respimat in patients with glaucoma, prostate proliferation, or bladder obstruction.
Patients with renal failure
Due to the increased plasma concentration of Tiotropumpia when the renal function decreases in patients with average to severe renal failure (Creatinine clearance ≤ 50 ml/min), should only use Spiolto Respimat when the expected benefits are superior to the risk that may occur.
Inexperienced in long -term use of drugs in patients with severe renal impairment (see the pharmacokinetic characteristics).
Symptoms on the eye
Patients must be instructed to use Spiolto Respimat properly. Must be cautious, do not leave the solution or aerosols of fine granules fly into the eyes. Eye pain or discomfort, blurred vision, glow or image with many colors accompanied by red eyes due to conjunctival conjunctiva and corneal edema can be a sign of acute narrow angle glaucoma. Should be examined immediately if there is any combination of the above symptoms.
Eye drops that cause pupils are not considered in the treatment of the above symptoms.
Cardiovascular effects
Spiolto Respimat contains a prolonged Beta2-ADRENERGIC agonor. Beta2-commenergic agreements are long-lasting should be used cautiously in patients with cardiovascular disease, especially coronary heart failure, arrhythmia, obstructive hypertrophy and hypertension; In patients with convulsions or toxicity, patients have a history or suspected a long QT range, patients have abnormal response to sympathetic amines.
Similar to other beta2-adrenergic agreements, olodaterol can affect clinical implications in some patients, manifested by increased heart rate, hypertension and/or clinical symptoms. May need to stop using the drug when this effect appears. Moreover, the Beta2-adrenergic transport owners have been recorded as the cause of changes on the ECG (ECG), such as making T wave and the st difference, although the clinical meaning of these records is unclear.
Hypotension
Beta2-adrenergic-controlled host drugs can cause significant hypoglycemia in some patients, and are likely to lead to adverse effects on the cardiovascular disease. Reducing serum concentration is usually transient and does not require additional potassium. Patients with severe COPD have the ability to lower potassium caused by oxygen deficiency and accompanying treatment leading to increased sensitivity to arrhythmia.
Hyperglycemia
Beta2-adrenergic-doses of high-dose inhaled formats can cause increased plasma concentration.
When used with anesthesia
Be cautious in case of surgical plans using hydrocarbon Halogenization due to an increase in sensitivity to the cardiovascular effects of the beta bronchodilators.
Do not use Spiolto Respimat simultaneously with other drugs containing the Beta2-ADRENERGIC-acting owner. Patients who are regularly using the beta2-adrenergic shipping owners are short of inhalation (e.g. 4 times/day) should be recommended to use these agents only to reduce acute respiratory symptoms.
The ability to drive and operate machinery
No research on the effects of drugs on driving and operating machinery.
Despite this, patients should be recommended that it may appear dizzy and blurred when using Spiolto Respimat. Therefore, it is necessary to be cautious when driving or operating machinery. If the patient has the above symptoms, avoid dangerous jobs such as driving or operating machinery.
Pregnancy
data on the use of tiotropium in pregnant women is quite limited. There is no clinical data related to olodaterol exposure during pregnancy. Pre -clinical studies of Tiotropium do not show any direct or indirect effects related to reproductive toxicity at clinical dose.
Olodaterol's preclinical studies show that the drug has a typical effect of Beta2-adrenergic agreeders at many times higher doses of treatment.
To ensure safety, avoid using Spiolto Respimat for pregnant women.
Should pay attention to the inhibitory effect of the uterine smooth muscle contraction of beta -adrenergic -like owners like olodaterol - a component of Spiolto Respimat.
The period of breastfeeding
There is no clinical data related to Tiotropium and/or Olodaterol exposure in nursing women. In animal studies of tiotropium and olodaterol, their derivatives and/or metabolites are found in the milk of nursing mice. However, it is not sure whether tiotropium and/or olodaterol will be secreted into the milk of nursing people.
Therefore, Spiolto Respimat should not be used in breastfeeding women unless the benefits of the drug are superior to the risk that may occur for children.
fertility
There is no clinical data on the influence of Tiotropium, Olodaterol or preparations combining these two components on fertility. Pre -clinical studies have been conducted with Tiotropium or Olodaterol alone does not show any adverse effects on fertility.
Drug interaction
Although the official drug interactive studies have not been conducted, Tiotropium Bromide has been used simultaneously with common drugs used in COPD treatment such as methylxanthine, oral steroids and inhaled steroids without clinical evidence about drug interactions.
Simultaneous use of Tiotropium Bromide with other anti -cholinergic drugs has not been studied. Therefore, it is not recommended to use Spiolto Respimat for a long time with other anti -cholinergic drugs.
Medications acting on the Adrenergic system
Concentrated with drugs on the Adrenergic system can increase the unwanted effects of Spiolto Respimat.
Xanthine, steroid or diuretics
Concentrated with Xanthine, Steroid, or Diuretless Potassium Potters that are likely to be affected by the hypokalemia of adrenergic agonists.
Beta blockers
Beta-adrenergic blockers may reduce or antagonistic effects of olodaterol. Can consider using selective beta blockers on the heart but need to be cautious.
Mao inhibitors, three -round antidepressants, the drugs that extend QTC.
Monoamin oxidase inhibitors, three -round antidepressants or other QTCs that can increase the effects of Spiolto Respimat on the cardiovascular system.
Pharmacokinetic interaction
In an Olodaterol's interactive study, Ketoconazole, a strong inhibitor, and CYP and P-GP, the level of body exposure increased by 1.7 times. There is no risk related to safety recorded in clinical studies that last up to a year with an olodaterol dose of up to 2 recommended dose. No need to adjust the dose of Spiolto Respimat.
Storage
Store less than 300C. Not frozen.
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