preloder

Umeclidinium


Umeclidinium

is an

anticholinergic

. Vilanterol
is a
bronchodilator. These

medications

work by relaxing muscles
in the
airways to improve breathing.

Umeclidinium

and vilanterol
is a
combination

medicine

used to

prevent airflow obstruction or bronchospasm in people with COPD (

chronic obstructive pulmonary disease

).
Dosing
Adult dosing:

Chronic obstructive pulmonary disease

:

  • 62.5 mcg (1 inhalation) oral inhalation once daily

  • Pediatric dosing:
    General Dosage Information:
  • Safety and efficacy are not established in pediatric patients.
  • Indications
    FDA-Labeled Indications:
  • Chronic obstructive pulmonary disease

  • Mechanism of Action
  • Umeclidinium

    is a
    long-acting

    Antimuscarinic agent

    , which is often referred to as an

    anticholinergic

    . It has similar affinity to the subtypes of muscarinic receptors M1 to M5.
    In the
    airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than
    24 hours
    . The clinical relevance of these findings is unknown. The bronchodilation following inhalation of

    umeclidinium

    is predominantly a site-specific effect
  • Adverse Effect
    Common:
    Respiratory:
  • Nasopharyngitis

    (8%)
  • Upper respiratory infection

    (5%)

  • Serious:
    Immunologic:
  • Anaphylaxis

  • Ophthalmic:
  • Angle-closure glaucoma

  • Renal:
  • Urinary retention


  • Respiratory:
  • Paradoxical bronchospasm


  • Other:
  • Angioedema
  • Contraindication
  • Severe hypersensitivity to milk proteins
  • Hypersensitivity to

    umeclidinium

    or any product component
  • Interaction
  • Anticholinergics There are potential for an additive interaction with concomitantly used

    anticholinergic

    medicines

    . Therefore, avoid coadministration of

    Umeclidinium

    with other

    anticholinergic

    -containing drugs as this may lead to an increase in

    anticholinergic

    adverse effects

  • Phamacokinetics
    Absorption:
    Time for Maximum Plasma Concentration (Tmax):
  • Inhalation: 5 to 15 minutes

  • Distribution:
  • Protein binding: 89%
  • Volume of Distribution (Vd): 86 L

  • Metabolism:
  • Metabolism: oxidation followed by conjugation
  • Substrate of CYP2D6 and P-glycoprotein

  • Excretion:
  • Renal: less than 1% (oral) to 22% (IV)
  • Fecal: 58% (IV) to 92% (oral)

  • Elimination:
  • 11 hours
  • Precaution
    Concomitant Use:
  • Avoid co administration with other

    anticholinergics


  • Immunologic:
  • Hypersensitivity reactions (anaphylaxis, angioedema, pruritus, rash, and urticaria) have been reported; discontinue use with occurrence

  • Ophthalmic:
  • Worsening narrow-angle glaucoma may occur; monitoring recommended

  • Renal:
  • Worsening

    urinary retention

    may occur, especially in patients with prostatic hyperplasia or bladder-neck obstruction; monitoring recommended

  • Respiratory:
  • Acute bronchospasm; avoid use
  • Loss of bronchoconstriction control may indicate

    disease

    deterioration; immediate re-evaluation recommended
  • Life-threatening

    paradoxical bronchospasm

    may occur; symptomatic

    treatment

    and discontinuation required
  • Pregnancy Category
  • C (FDA)
  • Breast Feeding
  • Infant risk cannot be ruled out.
  • Monitoring
  • Improvement or maintenance of

    respiratory function

    in patients with COPD may indicate efficacy
  • Respiratory function

    , with symptoms suggestive of

    disease

    deterioration
  • How to Take or Administration
    General Information:
  • For oral inhalation only

  • Inhalation, oral:
  • Administer
    at the same time
    every day
  • Opening and closing the device without an inhalation will result in a lost dose
  • When ready for a dose, open the cover
    of the
    inhaler; a click will be heard and the counter will decrease to indicate the device is ready
  • Before inhaling the dose, breathe out fully;
    do not
    exhale into the device
  • Place device firmly between lips and inhale with a long, deep, steady breath through the mouth;
    do not
    breathe in through nose or cover air vent on the inhaler
  • Hold breath for 3 to 4 seconds or for as long as comfortable, and exhale slowly
  • Inhalation device
    is not
    reusable; discard 6 weeks after opening, or when dose counter reads zero (whichever comes first)
  • Dosage Form
    Inhalation Powder:
  • 62.5 MCG/1 Actuation
  • Treatment
    Management of

    Mild

    to Moderate Toxicity:

  • The vast majority of pharmaceutical overdoses that produce the

    anticholinergic

    toxidrome requires only supportive care; administer

    activated charcoal

    if the patient presents shortly after ingestion; sedate patients with benzodiazepines for agitation and delirium. Hypertension and tachycardia are generally

    mild

    and well tolerated, and
    do not
    require specific

    treatment

    . Physostigmine can
    be used to
    establish a diagnosis; it may help avoid an invasive, costly work-up, but should only be given in a setting where intensive monitoring and resuscitation is possible, and should NOT be given if the history or ECG (QRS widening) suggests tricyclic antidepressant poisoning.

  • Management of Severe Toxicity:
  • Orotracheal intubation for airway protection should be performed early. May benefit from gastric lavage if patient presents soon after a large ingestion; administer

    activated charcoal

    . GI decontamination should only be performed in patients who can protect their airway or who are intubated. Severe delirium may develop and require large

    doses

    of benzodiazepines for sedation. Seizures (may progress to status epilepticus) may require aggressive

    use of

    benzodiazepines, propofol and/or barbiturates. Monitor core temperature and

    treat

    hyperthermia with aggressive benzodiazepine sedation to control agitation, and external cooling. Clinical manifestations may be prolonged due to prolonged absorption
    in the
    setting of

    anticholinergic

    ileus.
  • Toxicology
    Adults:
  • Varies with the specific medication. In general, patients will have to ingest large

    doses

    of plant products (or make a tea) to develop symptoms.
  • Patient Counselling or Clinical Teaching
  • Instruct patient to seek immediate medical attention if their symptoms get worse or if they need more inhalations from their rescue inhaler than usual.
  • Advise patient that drug
    is not
    to
    be used to
    relieve

    acute symptoms

    and extra

    doses

    should not

    be used

    for that purpose. Instruct patient to treat

    acute symptoms

    with a short-acting beta-agonist rescue inhaler..
  • Side effects

    may include

    Nasopharyngitis

    ,

    upper respiratory tract infection

    , cough, joint pain, muscle pain, or upper abdominal pain.
  • Advise patient to report signs/symptoms of acute narrow-angle glaucoma (e.g., eye pain or discomfort, blurred vision, visual halos or colored images in association with red eyes from conjunctival congestion and corneal edema).
  • Instruct patient to report signs/symptoms of

    urinary retention

    (e.g., difficulty passing urine, painful urination).
  • Instruct patient
    to take
    drug
    at the same time
    every day
    and not use it more than once every
    24 hours
    .
  • Advise patient on proper preparation
    of the
    delivery device, and inhalation technique.
  • Advise patient that there are multiple significant drug-drug interactions for this drug. Consult a healthcare professional prior to new drug use (including over-the-counter and herbal drugs).












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