Umeclidinium (Incruse, Incruse ellipta) is a bronchodilator drug that acts on the M3 receptors in the bronchial wall. It is used in patients for the maintenance therapy of chronic obstructive pulmonary disease (COPD).
Umeclidinium (Incruse) Dose in Adults
Umeclidinium (Incruse) Dose in the treatment of COPD:
-
Dry powder for oral inhaler use:
- One inhalation (of incruse 62.5 mcg) once a day
- The maximum dose is 1 inhalation/day.
Umeclidinium (Incruse) Dose in Children
Safety and efficacy of the drug in children has not been established.
Pregnancy Risk Category: B
- Animals used in reproductive research have not been demonstrated to raise the likelihood of harmful consequences on foetuses, according to studies.
- It is not absorbed systemically so fetal exposure after maternal use is less probable.
Use during breastfeeding:
- It is unknown if the drug will be excreted into breastmilk.
- The possibility of drug exposure to the child who is being fed is lower, as systemic absorption is very low.
- Manufacturers recommend weighing the benefits and risks for the infant.
Dose in Renal disease:
Patients with kidney problems do not need to have their dosage changed.
Dose in liver disease:
-
Mild to moderate hepatic impairment:
- Adjustment in the dose in patients with mild hepatic impairment is not necessary.
-
Severe hepatic impairment:
- The manufacturer has not provided any dosage adjustment in patients with severe liver disease.
Side Effects of Umeclidinium (Incruse):
-
Cardiovascular:
- Tachycardia
-
Gastrointestinal:
- Toothache
- Upper Abdominal Pain
-
Hematologic & Oncologic:
- Bruise
-
Neuromuscular & Skeletal:
- Arthralgia
- Myalgia
-
Respiratory:
- Nasopharyngitis
- Upper Respiratory Tract Infection
- Cough
- Pharyngitis
- Viral Upper Respiratory Tract Infection
Contraindication to Umeclidinium (Incruse, Incruse Ellipta):
- Allergy reactions to any component of the drug or the drug itself
- Milk proteins severe allergy
Warnings and precautions
-
Bronchospasm
- Paradoxical bronchospasm can occur, which should be distinguished from an acute exacerbation.
- If a paradoxical response occurs, treatment must be stopped. These patients should receive alternate therapies.
-
Hypersensitivity
- Anaphylaxis may be severe, including pruritus and rash as well as angioedema and angioedema.
- If an allergic reaction occurs, the treatment must be stopped immediately.
-
Glaucoma:
- It can increase intraocular pressure. Patients with narrow-angle vision should not use it.
-
Urinary retention
- It shouldn't be used by patients who are at a high risk of experiencing urinary retention.
- Urinary retention symptoms should be constantly observed in older patients, prostatic hyperplasia patients, and patients with obstruction of the bladder neck.
Umeclidinium: Drug Interaction
Acetylcholinesterase Inhibitors |
May reduce an anticholinergic agent's therapeutic impact. Acetylcholinesterase Inhibitors' therapeutic impact may be reduced by anticholinergic drugs. |
Amantadine |
May strengthen an anticholinergic agent's anticholinergic action. |
Botulinum Toxin-Containing Products |
May strengthen an anticholinergic agent's anticholinergic action. |
Cannabinoid-Containing Products |
Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. |
Chloral Betaine |
May enhance the adverse/toxic effect of Anticholinergic Agents. |
Gastrointestinal Agents (Prokinetic) |
Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). |
Glucagon |
Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. |
Itopride |
Anticholinergic Agents may diminish the therapeutic effect of Itopride. |
Mianserin |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Mirabegron |
Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. |
Nitroglycerin |
Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. |
Opioid Agonists |
Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. |
Ramosetron |
Anticholinergic Agents may enhance the constipating effect of Ramosetron. |
Thiazide and Thiazide-Like Diuretics |
Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. |
Topiramate |
Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. |
Pramlintide |
May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. |
Secretin |
Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. |
Aclidinium |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Anticholinergic Agents |
Umeclidinium may enhance the anticholinergic effect of Anticholinergic Agents. |
Cimetropium |
Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. |
Eluxadoline |
Anticholinergic Agents may enhance the constipating effect of Eluxadoline. |
Glycopyrrolate (Oral Inhalation) |
Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). |
Glycopyrronium (Topical) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Ipratropium (Oral Inhalation) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Levosulpiride |
Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. |
Loxapine |
Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. |
Oxatomide |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Potassium Chloride |
Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. |
Potassium Citrate |
Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. |
Revefenacin |
Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. |
Tiotropium |
Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. |
Monitor:
- FEV1,
- peak flow, and other pulmonary function tests if indicated
- Monitor for the clinical featured of glaucoma
- Urinary retention especially in the elderly
- Allergic reactions
How to administer Umeclidinium (Incruse, Incruse ellipta)?
- It is available as a dry powder for oral inhalational use only.
- It should be administered at the same time of the day. The inhaler does not need to be shaken prior to its use.
- A click sound is heard each time the inhaler is opened and the counter will count by 1 number.
- After the click is heard, the inhaler is ready to be used. If a click is heard but the inhaler does not count down, the dose will not be delivered.
- The inhaler should only be opened when the dose is to be administered.
- Unnecessary opening and closing of the device will result in a missed dose. The inhaler device should not be closed until the dose is administered.
Mechanism of action of Umeclidinium (Incruse):
- It inhibits acetylcholine's competitive and irreversible action at type 3 muscarinic receptors (M3) in the bronchial smooth muscles, leading to bronchodilation.
Absorption
- It is mainly absorbed through the lungs. 89% of the drug's protein is bound.
- It is metabolized by the liver via CYP2D6. It has a half life of 11 hours.
- It takes between 5 and 15 minutes to reach peak serum concentration.
- After oral administration, 92% of drug is excreted in the stool.
International Brand Names of Umeclidinium:
- Encruse Ellipta
- Incruse
- Incruse Ellipta
- Rolufta
Umeclidinium Brand Names in Pakistan:
It is not available in Pakistan.