Umeclidinium-Vilanterol (umeclidinium bromide/vilanterol trifenatate)

Beta-Adrenergic Agents Long-Acting (Inhaled) Inhalation Blister, With Inhalation Device

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Umeclidinium bromide and vilanterol trifenatate (umeclidinium/vilanterol) is a fixed-combination preparation containing a long-acting muscarinic antagonist (umeclidinium) and a long-acting beta2-adrenergic agonist (vilanterol trifenatate).

Umeclidinium bromide, a synthetic quaternary ammonium antimuscarinic agent, is a long-acting, orally inhaled bronchodilator. The drug is a nonselective competitive antagonist at muscarinic (M1-M5) receptors. Umeclidinium competitively and reversibly inhibits the actions of acetylcholine and other cholinergic stimuli at M3 receptors in the smooth muscle of the respiratory tract leading to bronchodilation.

Vilanterol trifenatate, a synthetic sympathomimetic amine, is a relatively selective, long-acting beta2-adrenergic agonist. In vitro, the functional selectivity of vilanterol is similar to that of salmeterol; however, the clinical importance of this in vitro finding is unknown. The drug's beta2-adrenergic effects appear to result at least in part from stimulation of the production of cyclic adenosine-3',5'-monophosphate (cAMP) by activation of adenyl cyclase.

Increased concentrations of cAMP are associated with relaxation of bronchial smooth muscle. Vilanterol appears to inhibit release of mediators of immediate hypersensitivity from cells, especially mast cells.

Umeclidinium exhibits linear pharmacokinetics over a dosage range of 62.5-500 mcg. Steady-state plasma umeclidinium concentrations are achieved within 14 days, with 1.8-fold accumulation, following repeated once-daily inhalation of umeclidinium. Peak plasma umeclidinium concentrations are reached within 5-15 minutes following oral inhalation; however, umeclidinium plasma concentrations may not predict therapeutic effect.

Umeclidinium is mostly absorbed from the lungs after an orally inhaled dose, with minimal contribution from oral absorption. Umeclidinium is approximately 89% bound to human plasma proteins. Umeclidinium is metabolized, primarily by cytochrome P-450 (CYP) isoenzyme 2D6, and also is a substrate for the P-glycoprotein (P-gp) transporter.

Following repeated administration of umeclidinium 500 mcg (8 times the usual recommended dosage), no clinically important effect was observed on umeclidinium exposure in individuals who were poor-metabolizers of CYP2D6 substrates compared with healthy ultrarapid, extensive, and intermediate metabolizers. The principal routes of metabolism are oxidation via hydroxylation and O-dealkylation followed by conjugation (e.g., glucuronidation); systemic exposure to metabolites with reduced or undetermined pharmacologic activity compared with the parent drug is low. Umeclidinium undergoes biliary elimination with excretion of 58% and 22% of a radiolabeled IV dose in feces and urine, respectively.

Following oral administration, 92% and less than 1% of a radiolabeled dose of umeclidinium is excreted in feces and urine, respectively. The effective half-life following once daily oraldosing of umeclidinium is 11 hours. Age, gender, weight, race, and use of inhaled corticosteroids have not been found to affect umeclidinium pharmacokinetics.

Vilanterol exhibits linear pharmacokinetics over a dosage range of 25-100 mcg. Steady-state plasma vilanterol concentrations are achieved after 14 days of repeated once-daily inhalation, with up to 1.7-fold accumulation observed. Peak plasma vilanterol concentrations are reached within 5-15 minutes following oral inhalation; however, vilanterol plasma concentrations may not predict therapeutic effect.

Vilanterol is highly bound (approximately 94%) to human plasma proteins. Vilanterol is extensively metabolized, principally by CYP3A4, to metabolites with substantially reduced beta1- and beta2-agonist activity compared with the parent drug; it is also a substrate for P-glycoprotein. The effective half-life from inhalation administration of multiple doses of vilanterol is 11 hours.

Following oral administration, approximately 70 and 30% of a radiolabeled dose of vilanterol is excreted in urine and feces, respectively. Age, gender, weight, race, and use of inhaled corticosteroids have not been found to affect vilanterol pharmacokinetics.

USES: This product is used to control and prevent symptoms (such as wheezing and shortness of breath) caused by ongoing lung disease (chronic obstructive pulmonary disease-COPD, which includes chronic bronchitis and emphysema). Controlling symptoms of breathing problems helps you stay active. This inhaler contains 2 medications: umeclidinium and vilanterol.

Both drugs work by relaxing the muscles around the airways so that they open up and you can breathe more easily. Umeclidinium belongs to a class of drugs known as anticholinergics. Vilanterol belongs to the class of drugs known as long-acting beta agonists (LABAs).

Both drugs are also known as bronchodilators. This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden shortness of breath.

If sudden breathing problems occur, use your quick-relief inhaler as prescribed. Umeclidinium/vilanterol is not approved to treat asthma. People with asthma using long-acting inhaled beta agonists (such as vilanterol) without also using an inhaled corticosteroid may have an increased risk of serious (sometimes fatal) breathing problems.

Generic name: umeclidinium bromide/vilanterol trifenatate
Pronunciation: (ue-ME-kli-DIN-ee-um/vye-LAN-ter-ol)
Drug class: Beta-Adrenergic Agents Long-Acting (Inhaled)
Therapeutic class: Respiratory Therapy Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Umeclidinium-Vilanterol:

  • Bronchospasm Prevention With Copd

Also known as: Copd With Bronchospasms Prophylaxis.

Dosing

Dosage of umeclidinium bromide is expressed in terms of umeclidinium. Dosage of vilanterol trifenatate is expressed in terms of vilanterol.

Umeclidinium/vilanterol is supplied with a disposable plastic inhaler containing 2 foil strips, each with 30 blisters (or 7 blisters in the institutional package). One strip contains umeclidinium (62.5 mcg per blister), and the other strip contains vilanterol (25 mcg per blister). A blister from each strip is used to create 1 dose. After the inhaler is activated, the powder within a pair of blisters is exposed and dispersed into the air stream created by the patient's inhalation. The precise amount of drug delivered to the lungs with each activation of the inhaler device depends on patient factorssuch as inspiratory flow.

Drug interactions

Umeclidinium is metabolized primarily by cytochrome P-450 (CYP) 2D6. Vilanterol is a substrate of cytochrome CYP3A4. Vilanterol and umeclidinium are both substrates of P-glycoprotein (P-gp).

Contraindications

*Severe hypersensitivity to milk proteins or known hypersensitivity to umeclidinium, vilanterol, or any ingredients in the formulation.

*Use of long-acting beta2-adrenergic agonists (LABA), including vilanterol, without an inhaled corticosteroid is contraindicated in patients with asthma. Umeclidinium/vilanterol is not indicated for the treatment of asthma.

Adverse reactions

The most common adverse reactions (>=1%) reported with umeclidinium/vilanterol in clinical studies were pharyngitis, sinusitis, lower respiratory tract infection, constipation, diarrhea, pain in extremity, muscle spasms, neck pain, and chest pain.

Precautions

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ICD codes

CodeTypeDescription
Bronchospasm prevention with COPD
J44ICD10CMOther chronic obstructive pulmonary disease
J44.8ICD10CMOther specified chronic obstructive pulmonary disease
J44.89ICD10CMOther specified chronic obstructive pulmonary disease
J44.9ICD10CMChronic obstructive pulmonary disease, unspecified

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data