Anoro Ellipta 62.5/25MCG GSK Treatment maintains bronchiectasis (30 doses)

Dosage form Box
Specifications Umeclidinium, Vilanterol
Ingredient Glaxo

Ingredient

Composition informationContent
Umeclidinium55mcg
Vilanterol22mcg

Uses

indications

Anoro ellipta 62.5/25MCG drug indicated to maintain bronchodilator maintenance to reduce symptoms in adults with chronic obstructive pulmonary disease (COPD).

Pharmacology

Pharmacological therapy group: Drugs for respiratory obstruction, Adrenergic in combination with anti -cholinergic drugs

Code ATC: R03al03

Umeclidinium/Vilanterol is a combination of Muscarinic receptor antagonist for prolonged effect/Beta2-adrenergic-acting owner (LAMA/LABA). After inhalation, both components act on the spot on the gas path, relaxing bronchi by separate mechanisms.

umeclidinium

Umediclinium is a prolonged Muscarinic receptor antagonist (also considered as a cholinergic anti -cholinergic). It is a quinuclidine derivative, Muscarinic receptor antagonist is active on many types of Muscarinic receptors.

Umeclidinium has a bronchodilator effect by inhibiting the cohesion of acetylcholine with muscarinic receptors on the air of the air.

Umeclidinium is able to play slowly in the Muscarinic M3 receptor in humans on in vitro and have a prolonged effect on in vivo when it is taken directly to the lungs in preclinical models.

Vilanterol

Vilanterol is a beta2-adrenergic fortunist owner, which has a selective and prolonged effect (Beta2 transport owner).

Pharmacological effects of Beta2 agonors, including Vilanretol, are at least due to stimulation of intracellular adenylate enzymes, which are the enzyme catalyst the process of adenosine triphosphate (ATP) to cyclin-3 ′, 5′-adenosine monophosphate (AMP ring).

AMP concentration increases, causing bronchial smooth muscle relaxation and inhibiting the release of intermediate substances that cause instant hypersensitivity reactions from cells, especially masters.

Dynamic pharmacokinetics

When used in combination with Umeclidinium and Vilanterol through the inhalation, the pharmacokinetics of each component is recognized as similar to when using each active ingredient (see Metabolism-Drug-Interactive).

Therefore, the pharmacokinetics of the drug can be considered similar to each individual active ingredient.

absorption

umeclidinium:

After using Umeclidinium inhaled in healthy volunteers, CMAX is achieved from the 5th minute to the 15th minute. The absolute use of Umeclidinium inhaled in the average of about 13% of the drug, with negligible oral absorption.

After repeating the inhaled Umeclidinium dose, the stable state is about 7 to 10 days with the accumulation of 1.5 to 2 times higher.

vilanterol:

After using Vilanterol inhaled in a healthy volunteer, CMAX is achieved from the 5th minute to the 15th minute. The absolute bioavailability of Vilanterol inhaled form is 27%, with negligible oral absorption.

After repeating the dose of Vilanterol inhalation, the stable state is achieved within 6 days with a accumulation of 2.4 times higher.

distribution

umeclidinium:

After using intravenous lines for healthy subjects, the average distribution volume is 86 liters. The average cohesion of protein in human plasma is 89% on in vitro.

vilanterol:

After using intravenous lines for healthy subjects, the average distribution volume is 165 liters. The average cohesion of protein in human plasma is 94% on in vitro.

transformation

umeclidinium:

In vitro studies show that Umeclidinium is metabolized mainly through Cytochrome P450 2D6 (CYP2D6) and is the substrate for P-Glycoprotein transport channel (P-GP).

The main metabolic pathway of umeclidinium is oxidation (hydroxylation, o-deckylation) then conjugate (glucoronidation, etc.), forming metabolites that are reduced in pharmacological activity or metabolites that do not know the pharmacological activity. The body exposure to the metabolites is low.

vilanterol:

In vitro studies show that Vilanterol is metabolized mainly through Cytochrome P450 3A4 (CYP3A4) and is the substrate for P-GP transport channel. The main metabolic path is O-DEALYLation into metabolites with Beta 1 and beta 2 activity.

Metabolism in plasma after using vanterol mouth in the study marked radioactive in humans in accordance with the initial metabolism. The body exposure to the metabolites is low.

Medicine - Drugs

Existing pharmacokinetic data on healthy volunteers and COPD patients shows that the whole body exposure (CMAX and AUC) and exposure is predicted according to the population dynamic pharmacokinetics with Umeclidinium and Vilanterol not affected by the use of Umeclidinum/Vilanterol when compared with each individual ingredient.

Use in combination with strong CYP3A4 inhibitors Ketoconazole (400 mcg) increases the average AUC (0-T) and CMAX of Vilanterol, respectively 65% ​​and 22% respectively. The increase in exposure to Vilanterol is not associated with the increase in the body's body impact on the Beta movement on the heart rate, blood potassium or QT interval (adjusted by the Fridericia method).

Both Umeclidinium and Vilanterol are the substrate of P-Glycoprotein (P-GP). The impact of average P-GP transport channel inhibitors Verapamil (240 mg, 1 time/day) on pharmacokinetics in a stable state of Umeclidinium and Vilanterol has been assessed on healthy volunteers.

There is no effect of Verapamil on Cmax Umeclidinium or Vilanterol. There is an increase of about 1.4 times for the AUC of Umeclidinium which has been recorded but does not affect the AUC of Vilanterol.

Elimination

umeclidinium:

Plasma clearance after intravenously use is 151 liters/hour. After intravenous lines, about 58% of the dose is marked with radiation (or 73% of the radioactive activity found) is excreted in the stool at 192 hours after the dose.

Elimination through urine accounts for about 22% of the dosage marked radioactive after 168 hours (27% of radioactive activity is found).

The elimination of substances related to medication through feces after intravenous use shows the excretion of drugs into the bile.

After using the oral line on healthy men, the entire radioactive activity is excreted mainly in feces (92% of the dose is marked or 99% of the radioactive activity found) at 168 hours after the dose.

less than 1% of the oral dosage (1% of the radioactive activity is found) is excreted in the urine, suggesting that the absorption after the oral use is negligible.

Umeclidinium plasma sale time after taking the inhaled dose for 10 days is 19 hours, with 3% to 4% of the drug excreted in the form of unchanged urine in a stable state.

vilanterol:

Vilanterol's plasma clearance after intravenously 108 liters/hour. After using the vilanterol oral route, radioactive marks, the technique of balancing the volume recorded 70% of the dose marked radioactive in the urine and 30% in feces.

Vilanterol's main excretion path is metabolism, then excreting metabolites into urine and feces. The average selling time of Vilanterol is 11 hours after taking the dose for 10 days.

Before taking Anoro Ellipta 62.5/25MCG GSK Treatment maintains bronchiectasis (30 doses)

How to use

Anoro ellipta 62.5/25mcg inhaled in the mouth.

Dosage

adults

The recommended and maximum dose is an Anoro Ellipta 62.5/25 mcg, 1 time/day.

Children

Based on the instructions of the product, the use for patients under 18 years of age is inappropriate

Elderly

No dose adjustments in patients 65 years old.

kidney failure

No dose adjustments in patients with renal failure.

liver failure

No dose adjustment in patients with mild or medium liver failure. The use of Anoro Ellipta has not been studied in patients with severe liver failure, so it should be used cautiously.

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?

The overdose of Anoro Ellipta will be able to cause signs and symptoms due to the effects of separate ingredients, similar to the unwanted effects of the inhaled Muscarinic antagonist (such as dry mouth, visual disorders and tachycardia) and unwanted effects recorded when overdosed of other Beta2 -headed medications (such as tremor, fast cardiac pain).

Management

There is no specific treatment when an overdose of Anoro Ellipta. If an overdose occurs, patients should be supported with appropriate monitoring when necessary.

The next measures should follow the clinical indications or recommendations of the National Poison Control Center, if any.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Side Effects

Safety records of Anoro Ellipta 62.5/25MCG is based on about 3,000 COPD patients using Umeclidinium/Vilanterol 62.5/25 mcg doses or higher for a period of 1 year in clinical studies. Of these, about 1600 patients used a dose of 62.5/25 mcg and about 1300 patients using the dose of 125/25 mcg, used once a day.

The unwanted effects (ADRS) listed below are classified by the Agency of Meddra and the frequency.

Popular (≥ 1/100 and

Infections and parasites:

  • Urinary tract infections.
  • Ho.
  • Constipation.
  • Dry mouth.
  • Headache.Heart disorders:
  • atrial fibrillation.
  • Hypersensitive reactions include: rash.

    • Mental disorders:

  • anxiety.

    • Nervous system disorders:

  • Run.
  • ventricular tachycardia.
  • Difficult to pronounce.
  • Muscle spasm.

    • Skin and subcutaneous tissue disorders:

  • rash.

    • rare (≥ 1/10,000 and

    immune system disorders:

  • Hypersensitivity reactions include: Anaphylaxis, angioedema, and urticaria.

    • Eye disorders:

  • blurred vision.
  • paradoxical bronchospasm.
  • urinary retention.
  • Difficult.

    • Warnings

    Before using the drug you need to read the instructions carefully and refer to the information below.

    contraindicated

    Anoro ellipta 62.5/25MCG drug contraindicated in the following cases:

  • Patients with severe protein-acid.

    Be cautious when used

    Beta2-adrenergic agreement (LABA), such as Vilanterol, increases the risk of death in asthma patients. A placebo control test with another laba (salmeterol) has also shown an increase in cases of asthma death. This effect of Salmeterol is considered the group effect of all laba.

    The use of Anoro Ellipta has not been studied in asthma patients, and is not recommended for this group of patients.

    Anoro ellipta is used in COPD maintenance treatment. Anoro ellipta should not be used to reduce acute symptoms, that is, use as a cutting drug in the treatment of acute bronchospasm.

    Should treat acute symptoms with bronchodilators short inhaled. The increase in the use of bronchodilators is short to reduce the symptoms showing that the disease controls deterioration and then the patient should go to the doctor again.

    Like other inhaled sugars, the use of Anoro Ellipta can cause paradoxical bronchospasm that threatens the life of patients. Anoro ellipta should be stopped if the paradoxical bronchial spasm occurs and the use of replacement therapy if needed.

    Heart effects, for example, arrhythmia such as atrial fibrillation and tachycardia, can be seen after using sympathetic nerve stimulants and Muscarinic receptor antagonists, including Anoro ellipta. Therefore, be careful when taking Anoro Ellipta for patients with severe cardiovascular disease.

    Due to the Muscarinic resistance of the drug, it should be cautious when taking Anoro ellipta for patients with glaucoma or urinary retention.

    Umeclidinium/Vilanterol's use of severe liver failure, so caution should be used with caution (see the dosage and usage).

    Beta2-adrenergic agreed owner can significantly reduce blood in some patients, which is likely to cause adverse cardiovascular effects.

    Serum decrease is usually transient, no additional therapy. There are no clinical related effects of hypokalemia, which is observed in clinical studies with Umeclidinium/Vilanterol at the recommended dose.

    Be careful when using Umeclidinium/Vilanterol with other drug products that also have the ability to cause hypokalemia (see interaction).

    Beta2-adrenergic movement masters can cause transient hyperglycemia in some patients. There are no clinical related effects on plasma glucose observed in clinical studies with Umeclidinium/Vilanterol at the recommended dose.

    As soon as it starts treatment with Umeclidinium/Vilanterol, plasma glucose concentration should be closely monitored in diabetics.

    This drug contains lactose. Patients with rare genetic problems such as galactose intolerance, Lapp Lactase deficiency or Glucose-Galactose should not take this drug.

    Be cautious when using Umeclidinium/Vilanterol in patients with convulsions or toxicity, and in patients who often do not respond to the Beta2-adrenergic owner.

    The effect of drugs on drivers and operating machinery

    umeclidinium/Vilanterol does not affect or negligible effects on the ability to drive and operate machinery.

    used for pregnant and lactating women

    pregnancy:

    No or limited data on the use of Anoro Ellipta in pregnant women. Animal studies show that toxicity on reproductive organs after using Vilanterol inhales. Anoro ellipta should only be used during pregnancy if the expected benefits for the mother surpasses the risk of pregnancy.

    Breastfeeding period:

    It is not known whether Umeclidinium or Vilanterol will be excreted through breast milk. However, other beta2 agonors have been discovered in breast milk. The risk for infants/breastfed babies cannot be excluded.

    Consider the benefits of breastfeeding for babies and the benefits of treatment for mothers to decide to stop breastfeeding or stop Anoro Ellipta.

    Reproduction:

    There is no data on the impact of Anoro Ellipta on human fertility. Animal studies show that Umeclidinium or Vilanterol does not affect fertility (see clinical safety section).

    Drug interaction

    drug interactions may affect the activity of the drug or cause side effects. Should notify the doctor or pharmacist a list of drugs and functional foods you are using. Do not use or increase or decrease the dose of the drug without the guidance of a doctor.

    Beta blockers

    Beta-adrenergic blockers can weaken or oppose the actor of beta2, for example Vilanterol. Anoro ellipta should be avoided simultaneously with selective or non-selective beta-adrenergic blockers, unless there are persuasive reasons for that combination use.

    interactions on transportation and transformation channels

    Vilanterol is a substrate of Cytochrome P450 3A4 (CYP3A4).

    Concomitance the strong use of CYP3A4 inhibitors (such as ketoconazole, clarithromycin, otraconazole, ritonavir, telithromycin) can inhibit metabolism and increase body exposure to Vilanterol.

    Concentrated with ketoconazole (400 mg) on ​​healthy volunteers increases AUC (0-T) and CMAX Vilanterol average of 65% and 22% respectively. The increase in exposure to Vilanterol is not associated with the increase in the Beta-adrenergic owner of the Beta-adrenergic related to the systemic effects on the heart rate, blood potassium, or QT interval (adjusted by Fridericia method).

    Be cautious when using a combination of Umeclidinium/Vilanterol with Ketoconazole and other powerful CYP3A4 inhibitors because there is the potential to increase the body exposure to Vilanterol, which can lead to increased ability to cause unwanted effects.

    Verapamil, an average CYP3A4 inhibitor, does not have a significant impact on Vilanterol's pharmacokinetics.

    Umeclidinium is a substrate of Cytochrome P450 2D6 (CYP2D6). Umeclidinium's sustainable pharmacokinetics has been evaluated on a healthy volunteer who lacks CYP2D6 (poor metabolism). There is no impact on AUC or CMAX of Umeclidinium is recorded at 8 times higher.

    The Umeclidinium's AUC increased by 1.3 times recorded at 16 times higher than the dose, while CMAX was not affected. Based on the importance of these changes, there is no clinical drug interaction that is predicted when using Umeclidinium/Vilanterol combination with CYP2D6 inhibitors or when used for patients with CYP2D6 inherited genetic factors (poor metabolism).

    Both Umeclidinium and Vilanterol are the substrates of P-Glycoprotein (P-GP).

    .

    The impact of average P-GP inhibitors Verapamil (240 mg once daily) on the stable pharmacokinetics of Umeclidinium and Vilanterol has been assessed in healthy volunteers. There is no effect of Verapamil on Umeclidinium or Vilanterol's CMAX recorded.

    has recorded the AUC of Umeclidinium increased by 1.4 times while Vilanterol's AUC did not change. Based on the importance of these changes, no clinical drug interactions are predicted when used in combination with Umeclidinium/Vilanterol with P-GP inhibitors.

    Muscarinic anti -nervous drugs and other sympathetic stimulation

    Concomitance Umeclidinium/Vilanterol's use with other prolonged Muscarinic anti-antacists, beta2-adrenergic-active drug owners or other drugs containing one of these substances, have not been researched and not recommended because this can increase the possibility of unwanted effects when using the inhaler antiviral or inhalers or substances beta2-adrenergic.

    Hypotoic potassium

    Use of blood-potassium-reducing drugs simultaneously with methylxanthine, steroids, or diuretic drugs that do not keep potassium that can increase the ability to reduce potassium potassium of the Beta2-adrenergic benefactor, so be used caution (see warning and caution).

    Other COPD treatments

    Although there is no official studies in Vivo interaction, it has been conducted, but when used simultaneously Umeclidinium/Vinalterol inhaled with other COPD drugs, including bronchodilators stimulating nervous sympathetic effects and inhaled corticosteroids, there is no clinical evidence of drug interaction.

    • Storage

    Leave a cool place, avoid light, temperature below 30⁰C.

    Other drugs

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