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Drugs for Asthma
| Term | Definition |
|---|---|
| S/S of asthma | sense of breathlessness, tightness in chest, wheezing, dyspnea, and cough |
| Inflammatory process of asthma | allergen-> mast cells-> mediators (histamine, leukotrienes, interleukins, prostaglandins)-> infiltration of inflammatory cells (eosinophils, leukocytes, macrophages)-> mediator ( cytokines, leukotrienes-> inflammation |
| Metered-dose inhalers (MDIs) | small, hand-held, pressurized devices that deliver a measured dose drug with each actuation; 1-2 puffs; 1 minute between puffs; inhale prior to activating device; hand-lung coordination; only 10% of dose reaches the lungs |
| Dry-powdered inhalers (DPIs) | deliver drugs in the form of a dry, micronized powder directly to the lungs; breath activated; no hand-lung coordination required; 20% reaches the lungs, spacers are not used with DPIs |
| Nebulizer | drug converted into a mist; droplets in mist are much finer than produced by inhalers |
| Actions of Glucocorticoids | most effective antiasthma drug; reduces asthma symptoms by suppressing inflammation by decreased synthesis and release of inflammator mediators, decreased infiltration and activity of inflammatory cells, and decreased edema of the airway mucosa |
| Glucocorticoids are used on a fixed schedule NOT PRN why? | Because beneficial effects develop slowly, these drugs cannot be used to abort an ongoing attack |
| Inhaled glucocorticoids | first line therapy for asthma; very safe and effective; most common adverse effects oropharyngeal candidiasis and dysphonia (hoarseness, speaking difficulty) |
| How to minimize oropharyngeal candidiasis and dysphonia from glucocorticoids? | patient should gargle after each administration |
| In times of stress, what must be given to patients with adrenal supression from glucocorticoids? | Patients who have been switched from oral glucocorticoids to inhaled glucocorticoids must be given supplemental oral or IV doses at times of stress. |
| How to minimize bone loss that occurs from oral and inhaled glucocoticoids? | use lowest dose possible, ensure adequate intake of calcium and vitamin D, and participate in weight-bearing exercise |
| Oral glucocorticoids | potential adverse effects include adrenal supression, osteoporosis, hyperglycemia, peptic ucler disease, and ,in young patient , suprression of growth; only used for patients with severe asthma |
| Beclomethasone dipropionate (QVAR) inhaled glucocorticoids | MDI: 40 or 80 mcg/puff; Adults: 40-320 mcg BID; 40-80 mcg BID (5-11yr) |
| Budesonide (pulmicort flexhaler, pulmicort respules) inhaled glucocorticoids | Plumicort Flexhaler: DPI: 90 or 180 mcg/inhalation; Adults: 360-720 mcg BID; Kids: 180-360 mcg BID Pulmicort Respules: suspension for ned; adults: 250-500 mcg 1-2 x daily or 1000 mcg once daily; Kids: 500-1000 mcg.day (1-8 yrs) |
| Ciclesonide (Alvesco) inhaled glucocorticoids | MDI: 80-160 mcg/puff; Adults: 80-320 mcg BID; Kids: 80-320 mcg BID (12yrs and up) |
| Flumisolide (AeroSpan) inhaled glucocorticoids | MDI: 80 mcg/puff; Adults: 160-320 mcg BID; Kids: 80-320 mcg BID (6-11 yrs) |
| Fluticasone propionate (Flovent HFA, Flovent Diskus) inhaled glucocorticoids | Flovent HFS--> MDI: 44,110, or 220 mcg/puff; Adults: 88-440 mcg BID; Kids: 88 mcg BID (4-11 yrs) Flovent Diskus--> DPI: 50,100, or 250 mcg/puff; Adults: 100-1000 mcg BID; Kids: 50-100 mch BID (4-11 yrs) |
| Mometasone furoate (Asmanex twisthaler) inhaled glucocorticoids | DPI: 110 or 220 mcg/puff; Adults: 220-440 mcg 1-2 times daily; Kids: 110 mcg once daily (4-11 yrs) |
| Oral glucocorticoids (prednisone, prednisolone) | Short term therapy: 30-40 mg BID 5-7 days; long term therapy: alternate-day dosing recommended, initial dose 40-60 mg qam for adults, pediatrics 20/40 mg then dosage should be reduced by 5-10 mg every 2 weeks |
| What can all leukotrienes cause ? | Adverse neuropsychiatric effects, including depression, suicidal thinking, and suicidal behavior |
| Zileuton (zyflo, zyflo cr) | Inhibitor of leukotriene synthesis and is approved for asthma prophylaxis and maintenance therapy in adults and children age 12 yrs and older; can see effective after 1-2 hours; not for ongoing attacks; can injure liver so monitor ALT; |
| Which leukotrienes cannot be combined with theophylline, warfarin, or Coumadin ? | Zileuton and zafirlulast |
| Zafirlulast (Accolate) Leukotriene modifier | It is a leukotriene receptor notifier; for maintenance therapy of chronic asthma in adults and kids 5 yrs and up; give 1 hr before or 2 hrs after meals; common side effects headache and GIndisturbances; can cause liver damage and churg-Strauss syndrome |
| Churg-Strauss syndrome | A potentially fatal disorder characterized by weight loss, flu-like symptoms , and pulmonary vasculitis (blood vessel inflammation) |
| Montelukast (Singulair) Leukotriene modifier | A leukotriene receptor blocker; uses: prophylaxis and maintenance therapy if asthma in pts 1 yr old, EIB pts 15 yrs old, and allergic rhinitis; not for quick relief of asthma attacks; maximal effects in 24 hrs; does NOT cause liver damage |
| Cromolyn (Intal) | Inhalation also agent that suppresses bronchial inflammation; used for prophylaxis; produces adequate control in 60-70% of pts; give 15 min before anticipated exertion |
| Omalizumab (Xolair) | A monoclonal antibody with a unique mechanism of action: antoagonism of IgE; given sub Q; small risk of anaphylaxis and cancer; reduces amount of IgE available to bind with its receptors on mast cells; 12 yrs or older pts; observe pt after inj. |
| Beta2- adrenergic agonists | Promotes bronchialdilation, suppress histamine release and increases ciliary motility; SABA peak in 30-60 min and used for on going attack; LABA used on fixed schedule |
| Short acting inhaled beta2- agonists (SABA) | Taken PRN to relieve ongoing attack; taken before exercise to prevent attack; delivered by neb or MDI |
| Long acting inhaled beta2- agonists (LABA) | Dosing on fixed schedule NOT prn; not first line therapy and must always be combined with a glucocorticoid |
| Oral beta2- agonists | Only used for long term control |
| SABA adverse effects | Tachycardia, angina, tremor |
| Oral beta2- agonist adverse effects | Produce some activation of beta1 receptors in the heart which can cause angina pectoris and tachydysrhythmias and can cause tremors by activating beta 2 receptors in skeletal muscle |
| Theophylline (Theo-24, Theochron, Elixophyllin) Methylxanthines | Produces bronchodilation by blocking receptors for adenosine; dosage carefully controlled due to narrow therapeutic range; usually given PO; not effective when inhaled; most appropriate for pts with nocturnal attacks; IV theophylline given in emergencies |
| Pharmacokinetics for theophylline | Affected by food; smoking cigarettes accelerates metabolism and decreases the half-life by about 50%; levels between 5 and 15 mcg/ml are appropriate for patients; a level of 20 mcg/mL risk of adverse effects is high |
| Toxicity of theophylline | levels of 20-25 mcg/mL mild reactions are nausea, vomiting, vomiting, diarrhea, insomnia, restlessness; levels above 30 mcg/mL produce severe reactions such as severe dysrhythmias (V-Fib) and convulsions and death from cardiorespiratory collapse |
| Treatment for theophylline toxicity | stop the drug; administering activated charcoal can decrease absorption absorption of theophylline. Ventrical dysrhythmias respond to lidocaine; IV diazepam may help control seizures. |
| theophylline drug interactions | caffeine can intensify the adverse effects on the CNS and heart; phenobarbital, phenytoin, and rifampin lower theophylline levels by inducing hepatic metabolizing enzymes; cimetidine and fluoroquinolone antibiotics can elevate plasma levels |
| Aminophylline | preferred form of theophylline for IV use; infusion should be done slowly (no faster than 25mg/min) because rapid injection can produce severe hypotension and death |
| How do anticholinergic drugs improve lung function? | by blocking muscarinic receptors in the bronchi, thereby causing bronchial dilation |
| Ipratropium (Atrovent HFA) anticholingeric | promotes bronchodilation; effects within 30 sec; common adverse reactions are dry mouth and irritation of the pharynx; pts with peanut/ soy allergy should avoid this drug; it can be used alone or combination w/ albuterol as Combivent & Duoneb |
| Tiotropium (spiriva) anticholingeric | long acting; inhaled approved for bronchospasm associated with COPD; effective within 30 min; common adverse effects is dry mouth pt can suck in sugarless candy for relief |
| Glucocorticoid/LABA Combinations | provide anti-inflammtory benefits and the LABA provide bronchodilation; should be reserved for pts whose asthma has not been adequately controlled with an inhaled glucocorticoid alone |
| Fluticasone/ salmeterol (Advair Diskus) (Advair HFA) Glucocorticoid/LABA Combinations | Advair Diskus approved for pts 4yrs or older; Advair HFA approved for pts 12yrs or older |
| Budesonide/Formoterol (Symbicort) Glucocorticoid/LABA Combinations | MDI used for pts 12 yrs and older |
| Mometasone/Formoterol (Dulera) Glucocorticoid/LABA Combinations | MDI used by pts 12 yrs and older |
Created by:
anroles
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