Drug information of Aclidinium

Aclidinium

Drug group:

Aclidinium is an anticholinergic for the long-term management of chronic obstructive pulmonary disease (COPD). It has a much higher propensity to bind to muscarinic receptors than nicotinic receptors.

Mechanism of effect

Aclidinium is a long-acting, competitive, and reversible anticholinergic drug that is specific for the acetylcholine muscarinic receptors. It binds to all 5 muscarinic receptor subtypes to a similar affinity. Aclidinium's effects on the airways are mediated through the M3 receptor at the smooth muscle to cause bronchodilation. Prevention of acetylcholine-induced bronchoconstriction effects was dose-dependent and lasted longer than 24 hours.

Pharmacodynamic

Aclidinium does not prolong the QTc interval or have significant effects on cardiac rhythm.

Pharmacokinetics

~55% of administered dose is swallowed, but negligible oral absorption is observed; fraction of inhaled dose that reaches systemic circulation is low (<5%)

Peak Plasma Time: 10-15 minutes (in COPD)

Peak Plasma Concentration: 80 pg/mL (in COPD)

Whole lung deposition: 30% of the metered dose

Vd: 300 L (IV administration)

Metabolism:

Aclidinium bromide is rapidly hydrolyzed in plasma into its alcohol (LAS34823) and acid (LAS34850) metabolites by both enzymatic and non-enzymatic cleavage; neither of these metabolites are active

Half-life: 5-8 hr following repeat BID administration

Renal clearance: Low

Total clearance: 170 L/hr (IV administration)

Excretion: Urine 0.1% (as aclidinium bromide), 65% (as metabolites); feces 33% (as metabolites)

Dosage

Adult

Chronic Obstructive Pulmonary Disease

400 mcg (1 actuation) inhaled PO BID

Pediatric

Safety and efficacy not established

Alerts

Not for acute episodes of bronchospasm (ie, not for rescue therapy)

May cause paradoxical bronchospasm; if this occurs, discontinue and consider other treatments

Worsening of narrow-angle glaucoma may occur; use with caution in patients with narrow-angle glaucoma; instruct patients to consult a physician immediately if it occurs

Worsening of urinary retention may occur (eg, prostatic hyperplasia, bladder-neck obstruction); use with caution in patients with prostatic hyperplasia or bladder-neck obstruction; instruct patients to consult a physician immediately if it occurs

Immediate hypersensitivity reactions, including angioedema, bronchospasm, or anaphylaxis, may occur after administration; if hypersensitivity occurs, discontinue immediately and consider alternate treatment

Coadministration with other anticholinergics may increase risk for adverse effects

Points of recommendation

  • Tell all of your health care providers that you take aclidinium. This includes your doctors, nurses, pharmacists, and dentists.
  • Call your doctor right away if your breathing problems get worse, if your rescue inhaler does not work as well, or if you need to use your rescue inhaler more often.
  • Do not get aclidinium powder in your eyes. Side effects like eye pain or redness, blurred eyesight, or other eyesight problems may happen. Call your doctor right away if you have any of these signs.
  • Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.
  • For breathing into the lungs.
  • Keep using aclidinium as you have been told by your doctor or other health care provider, even if you feel well.
  • Clean mouthpiece by wiping with a dry tissue or cloth. Do not wash or put in water.
  • Skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

Pregnancy level

Group c - Not adequate studies in pregnant women


Ask a Pharmacist


User's questions
    No comments yet.