| Drug | MOA | Administration | Side Effects | Extra |
|---|---|---|---|---|
| SABAs Selective B-2 Agonist Proventil (Albuterol) Levalbuterol & Pirbuterol | Causes B-2 receptor activation- results in smooth muscle relaxation Sympathomimetics Short acting Beta agonist ↑bronchodilation (main effect) ↑mast cell stability, ↑mucociliary transport due to B-2 receptor activation | Give nasally or inhalation Albuterol (short acting drug) is only indicated and effective for acute symptom relief Rescue therapy can be used but not ideal for prophylaxis due to short duration of action Patients should have a short-acting inhaled B-2 agonist on hand regardless of whether primary therapy is with a long acting agent or another class of drugs Regularly scheduled, daily, chronic use of SABA is not recommended. Adult: Albuterol 90-180 mcg MDI q 4-6 hrs PRN 1.25-5 mg neb q 4-6 hr PRN | May involve both B-1 and B-2 stimulation: skeletal muscle tremors, CNS stimulation, HA, dizziness, insomnia Metabolic side effects: hypokalemia & decrease glucose levels Tolerance: desensitization with long term use caused by overprescribing & failure to use other adjunctive drugs such as steroids | XOPENEX (levalbuterol): has less side effects but cost more money If given over a long duration, the drug loses Beta 2 selectivity and stimulates Beta 1 (↑heart rate, ↑force of contraction of heart, ↑impulse transmission, arrhythmias, ↑BP) Beta stimulation can cause K+ to go into the cell (can give a hyperkalemia patient a breathing treatment to move potassium into the cell) Albuterol is the preferred SABA for use in pregnancy |
| LABAs Serevent (Salmeterol) Formoterol | Long acting Beta agonist Inhaled bronchodilators that have a duration of bronchodilation of 12 hours after a single dose. | Used for prophylaxis only Onset of action is too slow to be used for rescue therapy LABAs are not to be used as monotherapy for long-term control of asthma Daily use of LABA generally should not exceed 100 mcg salmeterol or 24 mpg formoterol Adults: Salmeterol: 1 blister q 12 hours Formoterol: 1 capsule q 12 hours | LABAs are used in combination with ICSs for long-term control and prevention of symptoms in moderate or severe persistent asthma | Asthma patient must have a short acting and long acting inhaler COPD can only have a long acting inhaler! |
| Inhaled Corticosteroids (ICS) Vanceril (Beclomethasone) | Used to treat the underlying disease state Prophylaxis only The cornerstone of asthma treatment- ↓ inflammation May boost actions of bronchodilators Restores sympathomimetic efficacy that’s lost Reduce airflow obstruction by reducing airway inflammation in bronchioles Modify the body’s immune responses to various stimuli Suppress cytokine production, airway eosinophil recruitment, and release of inflammatory mediators | Inhalant Inhaled corticosteroids (ICS) provide local therapeutic action with minimal systemic effects Educate patient to rinse mouth after each use Inhaled steroids are not associated with a “rush” of relief when used. It takes about 2 weeks of use for noticeable improvement to be felt. | Hoarseness, cough (rinse mouth after each use to help prevent) Thrush | Use the minimum amount of steroid as possible. Way the risk and benefits with DM patients -may have to increase insulin Used alone or with other drugs depending on asthma frequency & severity Inhaled Corticosteriods (ICSs) are the most consistently effective long-term control medication at all steps of care for persistent asthma, and ICSs improve asthma control more effectively in both children and adults than leukotriene receptor antagonists (LTRAs) or any other single, long-term control medication do. |
| Systemic Steroids Prednisone | anti-inflammatory medications that reduce airway hyperresponsiveness, inhibit inflammatory cell migration and activation, and block late phase reaction to allergen | Parenteral Used for severe, persistent or poorly controlled asthma Cause many side effects during therapy Adults: Methylprednisolone .5–60 mg daily in a single dose in a.m. or qod as needed for control Prednisolone: Short-course “burst”: to achieve control, 40–60 mg per day as single or 2 divided doses for 3–10 days | Fluid & electrolyte imbalances Renal: Na & H20 retention Metabolic: altered glucose, fat, & protein metabolism. Hyperglycemia (a problem for diabetics), ↓ lineal growth in children Immunosuppression Various CNS & mood changes | Easy to start treatment but harder to stop safely Even brief use of systemic steroids can cause long-term suppression of endogenous steroid production, put patient at risk of withdrawal |
| LT Receptor Antagonists Leukotriene Receptor Antagonists (LTRAs) Singular (Montelukast) | Blocks cysteinyl LT receptors, “ interrupt” various inflammatory processes including bronchoconstriction, eosinophil migration & local edema For control treatment only- not rescue Modestly effective | Inhalation: once a day dosing For use in patients .≥ 5 years old Monitor Liver function Black letter warning box for suicidal ideation Adults: Montelukast 10 mg ohs Zafirlukast 40 mg daily (20 mg tablet bid) | Black letter warning box for suicidal ideation | Is quite $$$ For use in mild-persistent symptoms Can be an alternative to inhaled steroid, but using a steroid is preferred |
| Bronchodilators Methylxanthines Anhydrous theophylline | Methylxanthines consists of caffeine & tea Theophylline/ aminophylline are bronchodilators Inhibition of phosphodiesterase causes vasodilation Blockade of bronchoconstriction by adenosine receptors | Oral agents used for 24 hr control & nocturnal symptoms Not used for acute symptom control Parenteral (aminophylline, IV) for acute symptoms- only used In hospitals No inhaled formulations 3rd or 4th line drugs because of potential complications Used with neonates to stimulate the breathing center in preemies Used for sleep apnea Monitoring of serum theophylline concentration is essential. Adult: Starting dose 10 mg/kg/day up to 300 mg maximum; usual maximum: 800 mg/day | Extensive hepatic metabolism: important in context of interactions with drugs that↑ or↓ hepatic metabolism Low therapeutic index Think about toxicity because these drugs are metabolized by the liver CNS stimulation: (intensity parallels blood level of drug)-this is the earliest sign of toxicity Seizures are a major consequence of toxicity- apnea during seizure is the major cause of death Cardiac stimulation (rate, contractility) GI irritation: ulcerogenicity | Dosing adjustments: ↑((mg/kg) for children (age,weight-dependent), smokers, & use of drugs that stimulate metabolism Reduced (mg/kg) doses for: ↓ liver function, history of CV disease, seizures, & use of drug that ↓ hepatic metabolism Use of other cardiac stimulants (caffeine & tea) belong to the same family of methy-xanthines Does not play a major role in the treatment of asthma |
| Anticholinergic Atrovent (Ipratropium) Spiriva | Methylxanthines= consists of caffeine & tea, Theophylline/ aminophylline are bronchodilators Inhibition of phosphodiesterase causes vasodilation Blockade of bronchoconstriction by adenosine receptors Inhibits muscarinic cholinergic receptors and reduces intrinsic vagal tone of the air- way | Ipratropium bromide may be used as an alternative bronchodilator for patients who do not tolerate SABA Adult: Ipratropium HFA MDI 17 mcg/puff, 200 puffs/canister 2–3 puffs q 6 hours Nebulizer solution 0.25 mg/mL (0.025%) 0.25 mg q 6 hours | Drying of mouth and respiratory secretions, increased wheezing in some individuals, blurred vision if sprayed in eyes. If used in the ED, produces less cardiac stimulation than SABAs. | Treatment of choice for bronchospasm due to beta-blocker medication. |
| Mast Cell “Stabilizers” Intal and Tilade | Used for treatment of COPD & exercise induced asthma ↓↓ mediator release from mast cells & prevents inflammatory response Acts locally to inhibit release of mediators of type 1 allergic reactions, including histamine and leukotrienes, from sensitized mast cells after exposure to an antigen Antiasthmatic and antiallergenic | Orally inhaled powder | Negligible toxicity Few serious side effects (coughing) | |
| Xolair (Omalizumab) | Used for severe asthma Monoclonal antibody against IgE | Given SC injection every 2-4 weeks | Control medication-not for rescue (no bronchodilator activity) ↓frequency and severity of symptoms ↓ steroid dosage requirements Very $$$$! |