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Drugs for Asthma

TermDefinition
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