How Do Respiratory Anticholinergics Work?

Respiratory anticholinergics are medications prescribed to treat chronic obstructive pulmonary disease (COPD) and asthma. Respiratory anticholinergics make breathing easier by relaxing the smooth muscles of bronchial tubes, improving lung function, and reducing mucus secretion in the respiratory system.

Some of the respiratory anticholinergics are combined with other medications that reduce hypersensitivity reaction in the respiratory system and reduce inflammation. Anticholinergics work by blocking the activity of acetylcholine, a neurotransmitter that nerve endings secrete to make muscles contract.

Acetylcholine binds to protein molecules known as muscarinic receptors on the surface of muscle cells to make them contract. Acetylcholine also stimulates muscarinic receptors on exocrine gland cells to secrete fluids such as mucus, saliva, tears, and sweat.

Respiratory anticholinergics are long-acting muscarinic antagonists (LAMA), which relax airway smooth muscles and reduce mucus secretion by blocking muscarinic receptors on the bronchial smooth muscles and the exocrine gland cells in the bronchial passage.

Other medications combined with anticholinergics include:

• Long-acting beta-2 agonists (LABAs): LABAs enhance the activity of beta-2 adrenergic receptors which are stimulated by epinephrine, a natural hormone in the body. Stimulation of beta-2 receptors results in intracellular action that relaxes bronchial muscles and inhibits hypersensitivity reaction from mast cells, a type of immune cells that initiate allergic reactions.
• Corticosteroids: Corticosteroids are powerful anti-inflammatory agents used to control inflammation.

Respiratory anticholinergics are orally inhaled in the form of powders, aerosolized tiny particles or droplets, or solutions nebulized into a fine mist. Many types of inhalation devices such as metered dose inhalers and nebulizers are available.

Respiratory anticholinergics are used to treat the following conditions:

FDA-approved:

• Long term maintenance treatment of chronic obstructive pulmonary diseases including:
  • Chronic bronchitis
  • Emphysema
  • Bronchospasm
• Long term maintenance treatment of asthma, an inflammatory bronchial condition

Off-Label:

• Acute asthma exacerbation

Orphan designation:

• Cystic fibrosis, an inherited disorder that damages the lungs and the digestive system

Side effects of respiratory anticholinergics may include the following:

• Headache
• Nasopharyngitis (inflammation of nose and throat)
• Upper respiratory tract infection
• COPD exacerbation
• Bronchitis (inflammation of bronchial passage)
• Sinusitis (inflammation of the sinuses)
• Rhinitis (inflammation of the nasal passage)
• Pharyngitis (throat inflammation)
• Laryngitis (inflammation of the larynx)
• Oropharyngeal pain (mouth and throat pain)
• Dyspnea (shortness of breath)
• Pneumonia
• Cough
• Dryness and irritation in the throat
• Paradoxical bronchospasm
• Urinary tract infection
• Urinary retention
• Dysuria (painful urination)
• Diarrhea
• Dyspepsia (indigestion)
• Abdominal pain
• Constipation
• Nausea
• Vomiting
• Gastroesophageal reflux disease (GERD)
• Gastroenteritis (inflammation of the gastrointestinal tract)
• Tooth abscess and toothache
• Angina pectoris (chest pain due to coronary heart disease)
• Hypotension (low blood pressure)
• Cardiac arrhythmias (irregular heart rhythm and heart rate)
• Tachycardia (rapid heartbeat)
• Palpitations
• Atrial fibrillation (irregular and rapid heart rate with the atria out of synchronization with the ventricles)
• Supraventricular tachycardia (rapid heart rate beginning above the ventricles)
• Ventricular and supraventricular extrasystoles (extra heartbeats)
• Myocardial infarction (heart attack)
• Nonspecific chest pain
• Musculoskeletal chest pain
• Chest discomfort
• Back pain
• Neck pain
• Arthralgia (joint pain)
• Leg pain
• Skeletal pain
• Myalgia (muscle pain)
• Muscle spasms
• Pain in extremities
• Paresthesia (prickling sensation)
• Tremor
• Influenza or flu-like symptoms
• Fatigue
• Asthenia (weakness)
• Dizziness
• Fall
• Contusion
• Anxiety
• Agitation
• Restlessness
• Depression
• Sleep disturbance
• Insomnia
• Dehydration
• Dry mouth
• Mouth edema
• Stomatitis (inflammation and soreness inside the mouth)
• Glossitis (tongue inflammation)
• Oral candidiasis (Candida infection)
• Dysgeusia (taste disorder)
• Dysphonia (hoarseness)
• Eye pain
• Cataract
• Conjunctivitis (inflammation of conjunctiva, the membrane on the whites of the eyes and the inner surface of eyelids)
• Conjunctival hyperemia (dilation and redness of blood vessels in the conjunctiva)
• Blurred vision
• Halo vision
• Corneal edema
• Mydriasis (dilation of pupils)
• Increased intraocular pressure
• Glaucoma (a progressive disease that damages the optic nerve)
• Narrow-angle glaucoma (a type of glaucoma in which the fluid drainage angle in the eye becomes narrow and impairs drainage)
• Epistaxis (nasal bleeding)
• Hypersensitivity reactions such as:
  • Rash
  • Urticaria (hives)
  • Pruritus (itching)
  • Angioedema (swelling in the tissue under the skin or mucous membranes)
  • Anaphylaxis (severe allergic reaction)
• Edema
• Herpes zoster
• Infections
• Candidiasis (Candida albicans fungal infection)
• Hypercholesterolemia (high cholesterol in the blood)
• Hyperglycemia (high glucose levels in the blood)

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of respiratory anticholinergic drugs include:

• aclidinium
• Anoro Ellipta
• Atrovent HFA
• Bevespi Aerosphere
• glycopyrrolate inhaled
• glycopyrrolate inhaled/formoterol
• Incruse Ellipta
• ipratropium
• Lonhala Magnair
• Spiriva HandiHaler
• Spiriva Respimat
• tiotropium
• Trelegy Ellipta
• Tudorza Pressair
• umeclidinium bromide
• umeclidinium bromide/vilanterol inhaled
• umeclidinium bromide/vilanterol inhaled/fluticasone furoate inhaled