Asthma Medications

What Is Asthma?

Asthma is a lung disease that causes inflammation and narrowing of the breathing passages of the lungs (bronchi and bronchioles).

What Causes Asthma?

Asthma is caused by chronic (ongoing, long-term) inflammation of these airways. Individuals with asthma are highly sensitive to various "triggers" that lead to inflammation of the airways. When the inflammation is triggered by one or more of these factors, the air passages swell and fill with mucus. The muscles within the breathing passages contract and narrow (bronchospasm). The narrow airways make it hard to exhale (breathe out from the lungs).

What Are the Risks of Asthma?

Asthma causes symptoms like wheezing, breathing difficulties, chest pain or tightness, and spasmodic coughing that often worsens at night. Asthma may impair individuals' ability to exercise, to engage in outdoor activities, to have pets, or to tolerate environments with smoke, dust, or mold. Although asthma can be controlled with medications, asthma attacks vary in intensity from mild to life-threatening. Over the past several decades, the number of asthma attacks that result in death has increased dramatically.

Asthma:An Inflammatory Disorder of the Airways

What Are Asthma Medications and Medical Treatments?

The main goals in asthma treatment are to prevent asthma attacks and to control the disease. Avoiding triggers that induce or aggravate asthma attacks is an important aspect of prevention. Medications used to prevent asthma attacks (controller medications) focus on decreasing the airway inflammation that causes attacks. Rescue medications help open up your airway and are used for quick relief when asthma symptoms occur despite the use of controller medications.

Most of the inhaler therapies have been changed recently because of the government mandate to remove chlorofluorocarbons (CFCs) from the devices in an attempt to prevent further damage to the earth's ozone layer. These inhalers have changed to a new propellant, hydrofluoroalkane (HFA), or powder devices. This change in delivery system resulted inadvertently in removing all generic inhalers from the market and only proprietary (brand name) options were available until recently. The FDA approved levalbuterol as a generic for the rescue inhaler known as Xopenex. Additionally, this medication is also available as a generic in nebulized form along with the inhaled steroid budesonide (Entocort, Uceris, Pulmicort).

Corticosteroid Inhalers for Asthma: Use, Side Effects, and Interactions

Beclomethasone (Qvar), budesonide (Pulmicort), flunisolide (AeroBid), fluticasone (Flovent, Arnuity), mometasone (Asmanex), and triamcinolone (Azmacort, which was discontinued at the end of 2009) are used as first-line asthma medicines. A small amount of inhaled corticosteroids is swallowed with each dose, but it's much less than that contained in oral corticosteroids. Therefore, inhaled corticosteroids decrease the likelihood of adverse effects from long-term use of steroids.

How corticosteroid inhalers work

Inhaled corticosteroids are often the first type of medication prescribed to control asthma. By inhaling the medication, these drugs act locally to decrease inflammation within the breathing passages, thereby avoiding the side effects associated with long-term use of oral corticosteroids.

Who should not use these medications

  • Individuals allergic to corticosteroids or any of the inhaler contents should not use these drugs.
  • Individuals with status asthmaticus or acute asthma attacks should not use these drugs.

Use

Corticosteroids for asthma are typically available as handheld inhalers containing liquid or powder. Many inhaled products have specific devices, and you should be thoroughly informed on how to use the inhaler prescribed for you. Frequency of administration (how often you use the inhaler) depends on the specific product.

Drug or food interactions

Since the drug is localized to the airway, no drug interactions have been reported.

Side effects

Do not use for an acute asthma attack. Inhaled corticosteroids work to slowly decrease airway inflammation and usually are of limited benefit during an acute attack of asthma. That is why these medications are maintenance or controller medication. They are not intended for use to treat an acute attack. Inhaled corticosteroids may decrease growth in children, so use the lowest dose possible. Inhaled corticosteroids may also increase the risk of serious or fatal infection in individuals exposed to serious viral infections like chickenpox or measles. Long-term use may cause cataracts or glaucoma (increased pressure within the eyes). These medications may increase the risk of pneumonia.

Emergency Medical Treatment for Asthma

If you are in the emergency room, treatment will be started while the evaluation is still going on.

  • You may be given oxygen through a face mask or a tube that goes in your nose.
  • You may be given aerosolized beta-agonist medications through a face mask or a nebulizer, with or without an anticholinergic agent.
  • Another method of providing inhaled beta-agonists is by using a metered dose inhaler or MDI. An MDI delivers a standard dose of medication per puff. MDIs are often used along with a "spacer" or holding chamber. A dose of six to eight puffs is sprayed into the spacer, which is then inhaled. The advantage of an MDI with a spacer is that it requires little or no assistance from the respiratory therapist.

Oral and Intravenous Corticosteroids for Asthma: Use, Side Effects, and Interactions

Methylprednisolone (Medrol, Solu-Medrol), prednisone (Deltasone, Orasone), and prednisolone (Pediapred) may need to be prescribed when inhaled medications fail to control asthma. Examples of such situations include after an acute asthma attack or when a respiratory infection or allergy aggravates asthma symptoms.

How corticosteroids work

Corticosteroids decrease the inflammation within the airway passages that contributes to asthma symptoms and acute attacks.

Who should not use these medications

  • Individuals who are allergic to corticosteroids should not use these drugs.
  • Individuals with systemic fungal infections or active tuberculosis should not use these drugs without medical supervision.

Use

  • Dosage varies depending on the situation for which corticosteroids are being used.
  • Corticosteroids may be given as an intravenous (IV) injection for an acute asthma attack in the emergency room.
  • The frequency of initial oral use may be as often as three to four times per day for one to two days following an acute asthma attack. This large dose can be administered for several days. When corticosteroids are taken regularly, they should be taken once daily upon awakening (usually in the morning) to coincide with your body's normal biological rhythm. The smallest possible dose should be given to avoid long-term side effects. Some individuals can control their asthma symptoms with every-other-day dosing. When taking steroids chronically, they should not be abruptly discontinued.
  • Your doctor may try other asthma control medications to avoid long-term use of oral corticosteroids.
  • Take these drugs with food or milk to avoid stomach upset.

Drug or food interactions

Use caution with other drugs that suppress the immune system, such as cyclosporine (Sandimmune, Neoral). Phenobarbital (Luminol), phenytoin (Dilantin), or rifampin (Rifadin) may decrease the effectiveness of corticosteroids. Some drugs, such as ketoconazole (Nizoral) or erythromycin (E-Mycin, E.E.S.), may increase blood levels and toxicity of corticosteroids. An increased risk of stomach bleeding (bleeding ulcer) may occur when taken with high-dose aspirin or with blood thinners such as warfarin (Coumadin). Corticosteroids tend to increase blood glucose levels in individuals with diabetes, so diabetic therapy, such as insulin or oral medicines, may need to be adjusted. Talk to your doctor or pharmacist before taking other medications with oral corticosteroids.

Side effects

These drugs may decrease growth in children, so the lowest dose possible must be used. Long-term use may cause mood changes, osteoporosis, sleep irregularities, increased hair growth, cataracts, increased eye pressures (risk for glaucoma), roundness of the face, or thinning skin, intestinal bleeding, and increase the risk of pneumonia. Suppression of internal corticosteroid production can occur with long-term use. Therefore, if taken for several weeks, dose adjustments should be under a physician's direction. Call your doctor if you experience any of the following:

  • Itching or hives, swollen face or hands, chest tightness, breathing troubles, tingling in mouth or throat
  • Headache, eye pain, or visual troubles
  • Increased urination or thirst
  • Seizures or dizziness
  • Stomach problems, stomach pain, bloody or black stools
  • Sudden pain, swelling, or loss of movement in the lower leg
  • Sudden fluid retention or weight gain
Asthma:An Inflammatory Disorder of the Airways

Leukotriene Inhibitors for Asthma: Use, Side Effects, and Interactions

Montelukast (Singulair), zafirlukast (Accolate), and zileuton (Zyflo) are used to control asthma symptoms. They are often used in addition to inhaled corticosteroids to avoid the use of oral corticosteroid.

How leukotrienes work

Leukotrienes are powerful chemical substances produced by the body. They promote the inflammatory response caused by exposure to allergens. Leukotriene inhibitors block the action or production of these chemicals, thereby reducing inflammation.

Who should not use these medications

  • Individuals who are allergic to leukotriene inhibitors should not take these drugs.
  • Individuals with phenylketonuria (PKU) should not take the chewable tablets that contain aspartame because this artificial sweetener contains phenylalanine

Use

  • Leukotrienes are available with a prescription as tablets, chewable tablets, and oral granules.
  • Granules may be taken directly in the mouth, or they may be mixed in soft foods like pudding or applesauce.
  • The drug is administered as a once-daily dose.

Drug or food interactions

No drug or food interactions have been reported.

Side effects

Leukotrienes are typically well tolerated, and side effects are similar to those of patients taking a placebo (sugar pill). Reports of headache, earache, sore throat, and respiratory infections have been noted.

Beta-Agonists for Asthma: Use, Side Effects, and Interactions

Albuterol (Ventolin, Proventil), formoterol (Foradil), levalbuterol (Xopenex), metaproterenol (Alupent, Metaprel), pirbuterol (Maxair), and salmeterol (Serevent) are used to decrease bronchospasm. These medications work by stimulating the relaxation of tiny muscles in the airways.

Some long-acting (>12 hours) beta-agonists (for example, formoterol and salmeterol) are specifically designed to prevent asthma attacks and not to treat acute attacks. Other beta-agonists have a quicker onset and may be used for prevention (along with corticosteroid inhalers) and as rescue therapy. Beta-agonists are also useful to use before exercise for exercise-induced asthma.

How beta-agonists work

These drugs relax muscles within the airway that cause bronchospasm. Beta-agonists also cause the airway passages to open wider, thus making breathing easier.

Who should not use these medications

Individuals who are allergic to beta-agonists should not take these drugs.

Use

Both handheld inhalers and a solution for use with a nebulizer are available. Many inhaled products have specific devices and you should be thoroughly informed on how to use the inhaler or nebulizer prescribed for you. Frequency of administration depends on the specific product.

Drug or food interactions

Inhaled anticholinergic medications, such as ipratropium (Atrovent), enhance beta-agonists' effectiveness.

Side effects

Beta-agonists may cause rapid heartbeat and tremor (shakiness). Individuals with heart disease, hyperthyroidism, seizure disorders, or hypertension should be closely monitored by their doctor. There is a box warning from the FDA on all long-acting beta-agonists stating that there is an increased risk of death when taking these medications. This data is based on a study in asthmatic patients taking long-acting beta-agonists alone. This warning is seen on all FDA-approved medications that include long-acting beta-agonists, such as those used in combination therapy. There is no data demonstrating that taking a long-acting beta-agonist along with other medications such as steroids used in many combination products has any increased risk of death.

Combination therapy

Commonly, long-acting beta-agonist therapy and inhaled corticosteroids are used together. These drugs work so that the effectiveness of each component can by enhanced when the other agent is given simultaneously. Combining these agents into a single delivery system also enhances compliance and simplifies care. The two current available brands of combination therapy are Advair (fluticasone and salmeterol), Breo (fluticasone and vilanterol), which uses a powder form of the medications, and Symbicort (budesonide and formoterol) in an inhaler device that includes a propellant. These combination medications come in different strengths. The strength pertains only to the inhaled corticosteroid component. The long-acting beta-agonist dose does not change. Side effects are the same, as noted under the individual components discussed above. The point is that taking an increased number of doses of these combination medications would result in excessive intake of long-acting beta-agonists, and this could be potentially dangerous.

Asthma:An Inflammatory Disorder of the Airways

Anticholinergic Inhalers for Asthma: Use, Side Effects, and Interactions

Ipratropium bromide (Atrovent), tiotropium (Spiriva), and umeclidinium (Incruse) are used with beta-agonists for severe symptoms.

How anticholinergic inhalers work

These drugs decrease bronchospasm and secretion of mucus in airways and are often used with albuterol to enhance effectiveness. In general, they are not as effective as the beta-agonists in treating asthma. These medications work by blocking receptors that cause spasm.

Who should not use these medications

  • Individuals who are allergic to any components of the inhaled product should not take these drugs.
  • Individuals who are allergic to soya lecithin or similar food products, such as soybeans or peanuts, should not take these drugs.

Use

Both handheld inhalers and a solution for use with a nebulizer are available. Many inhaled products have specific devices and you should be thoroughly informed on how to use the inhaler or nebulizer prescribed for you. These drugs are typically used three to four times per day.

Drug or food interactions

Since anticholinergic inhalers have little or no effect beyond the area applied, they are unlikely to interact with other drugs.

Side effects

Anticholinergic inhalers are not indicated for acute asthma attacks. The most common adverse effect is dry mouth. Individuals with glaucoma should be closely monitored by their ophthalmologist.

Methylxanthines for Asthma: Use, Side Effects, and Interactions

Theophylline (Theo-24, Theolair, Theo-Dur, Slo-Bid, Slo-Phyllin) may be prescribed to take with other controller medications.

How methylxanthines work

Methylxanthines are related to caffeine. These drugs provide mild to moderate relaxation of muscles in the airway to decrease bronchospasm. Essentially, they work as long-acting bronchodilators. These medications may have a mild anti-inflammatory effect.

Who should not use these medications

  • Individuals who are allergic to methylxanthines
  • Individuals with abnormal heart rhythms that are poorly controlled
  • Individuals with seizures (epilepsy) that are poorly controlled
  • Individuals diagnosed with hyperactive thyroid
  • Individuals with active peptic ulcer disease

Use

Methylxanthines are administered orally as tablets, capsules, liquid preparations, or sprinkles (tiny beads that may be sprinkled on the tongue or on soft food). Some oral preparations are available in long-acting doses, allowing the dose to be taken once or twice each day. Your doctor will adjust the dose to maintain specific blood levels known to be effective to decrease bronchospasm.

Drug or food interactions

Ingesting large amounts of caffeine contained in coffee, tea, or soft drinks may increase theophylline side effects. Some drugs that may increase theophylline blood levels include cimetidine (Tagamet), erythromycin (E-Mycin, E.E.S.), and ciprofloxacin (Cipro). Some drugs that may decrease theophylline blood levels include phenytoin (Dilantin) and carbamazepine (Tegretol). Check with your doctor or pharmacist before taking or stopping other medications to know how your theophylline blood levels will be affected by the change.

Side effects

Side effects include severe nausea or vomiting, tremors, muscle twitching, seizures, severe weakness or confusion, and irregular heartbeat. Less severe side effects include heartburn, loss of appetite, upset stomach, nervousness, restlessness, insomnia, headache, and loose bowel movements.

Mast Cell Inhibitors for Asthma: Use, Side Effects, and Interactions

Cromolyn sodium (Intal) and nedocromil (Tilade) are used to prevent allergic symptoms like runny nose, itchy eyes, and asthma. The response is not as potent as that of corticosteroid inhalers.

How mast cell inhibitors work

These drugs prevent the release of histamine and other chemicals from mast cells that cause asthma symptoms when you come into contact with an allergen (for example, pollen). The drug is not effective until four to seven days after you begin taking it.

Who should not use these medications

Individuals who are allergic to any components of the inhaled product should not take these drugs.

Use

Frequent dosing is necessary, since the effects last only six to eight hours. Mast cell inhibitors are available as a liquid to be used with a nebulizer, a capsule that is placed in a device that releases the capsule powder to inhale, and handheld inhalers.

Drug or food interactions

Since these drugs have little or no effect beyond the area applied, they are unlikely to interact with other drugs. Mast cell inhibitors may cause a cough, irritation or unpleasant taste.

Side effects

These drugs are only effective for prevention and are not to be used to treat an acute asthma attack.

Monoclonal Antibodies for Asthma: Use, Side Effects, and Interactions

Omalizumab (Xolair) is one of the newer asthma medications. It may be considered for individuals with persistent, moderate to severe asthma due to seasonal allergies that is not controlled by inhaled corticosteroids. The cost of omalizumab is estimated at $12,000-$15,000 per year.

Mepolizumab (Nucala) is another monoclonal antibody that is also used for moderate to severe asthma not controlled with standard care, including inhaled steroids.

How monoclonal antibodies work

Omalizumab binds to human immunoglobulin E (IgE) on the surface of mast cells and basophils (cells that release chemicals that cause allergic symptoms). By binding to IgE, omalizumab reduces the release of the allergy-inciting chemicals.

Mepolizumab binds to interleukin 5, which results in a decrease certain inflammatory cells (eosinophils). These eosinophils contribute to the development of asthma attacks.

Who should not use these medications

Individuals who are allergic to omalizumab or mepolizumab or its contents should not use it.

Use

For omalizumab, the dose depends on the IgE levels in the blood.

Adults and children older than 12 years of age are given an injection every two to four weeks.

For mepolizumab, adults and children older than 12 years of age who have elevated eosinophils (a specific inflammatory white blood cell) receive 100 mg by injection every four weeks.

Drug or food interactions

Drug interactions have not been reported.

Side effects

Omalizumab and mepolizumab are not effective in treating acute asthma attacks. Inhaled corticosteroids should not be suddenly stopped when initiating these medications. Swelling or pain at the area of injection may be experienced.

Reviewed on 9/11/2017

REFERENCES:

Fanta, Christopher H. "An overview of asthma management." May 31, 2016. UpToDate.com. <https://www.uptodate.com/contents/an-overview-of-asthma-management>.

Lee, S.L., et al. "Regulatory considerations for approval of generic inhalation drug products in the US, EU, Brazil, China, and India." AAPS J 17.5 Sept. 2015: 1285-1304.

United States. Food & Drug Administration (FDA). "FDA Approves Nucala to Treat Severe Asthma." Nov. 4, 2015. <https://www.fda.gov/newsevents/newsroom/pressannouncements/ucm471031.htm>.

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