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Exam #4 - Drugs for Treatment of Allergies & Asthma
n/a
31
Pharmacology
Graduate
11/11/2009

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Term
Type I (immediate hypersensitivity) Allergic Rxn
Definition
interaction of allergen with IgE-sensitized mast cells results in release of histamine & other mediators; may be localized to site of allergen exposure or it may be generalized anaphylactic response --> life-threatening, severe angioedema, bronchospasm, urticaria, hypotension, capillary leakage, & shock
Term
Type II (cytotoxic or autoimmune) Rxn
Definition
attachment of IgG or IgM Abs to target cells followed by complement activation & cell lysis; leads to: hemolytic anemia, agranulocytosis, or neutropenia
Term
Type III (immune complex) Rxn
Definition
circulating Ag & IgG complexes that localize near vascular wall & activate complement; leads to mast cell degranulation & an inflammatory response that manifests as "serum sickness" & a defuse vasculitis
Term
Type IV (cellular immune response) Rxn
Definition
Ag stimulation of sensitized T-cells; involved in delayed hypersensitivity conditions like allergic contact dermatitis & hypersensitivity pneumonitis
Term
Asthma
Definition
group of disorders characterized by intermittent reversible obstruction of airways; hallmark feature: hypersensitivity of airway to agents that are capable of causing bronchoconstriction (ACh, histamine); results from immunologically-mediated damage to bronchial epithelium
Term
Extrinsic Asthma
Definition
precipitation of symptoms related to exposure to specific environmental allergens
Term
Intrinsic Asthma
Definition
precipitation of symptoms provoked by a variety of stimuli: cold, exertion, infection, stress, etc.
Term
Acute Asthma Attack
Definition
bronchospasm, wheezing, cough, increased mucus production, & increased vascular permeability, congestion, pulmonary edema, airway inflammation, & WBC infiltration
Term
Inhibits release of histamine (degranulation)
Definition
cromolyn sodium [Intal]; agents that increase cAMP & stabilize mast cells (methylxanthines, beta-agonists); corticosteroids
Term
inhibit formation of generated autocoids (i.e. kinins, leukotrienes, superoxides, platelet activating factor, & arachidonic acid products)
Definition
zileuton [Zyflo] --> inhibits lipooxygenase enzyme, decreasing leukotriene formation; zafirlukast [Accolate] & monteleukast [Singulair] --> leukotriene receptor blockers
Term
block receptors for autocoids or bronchoconstrictors
Definition
H1-antihistamines; anticholinergic meds (ipratropium, tiotropium)
Term
bronchodilation by "physiologic antagonists"
Definition
beta-adrenergic agonists (epinephrine, isoproterenol, terbutaline, salmeterol); methylxanthines (theophylline, aminophylline)
Term
prevent inflammation & cell-mediated immunologic reactions
Definition
corticosteroids; immunosuppressives [methotrexate, cyclosporine]
Term
neutralize IgE
Definition
omalizumab [Xolair]
Term
cromolyn sodium [Intal]
Definition
inhibits release of histamine & other autocoids; used mainly for prophylactic treatment of bronchial asthma (inhalation) - NOT EFFECTIVE in acute attacks); ADRs are infrequent (bronchospasm, laryngeal edema, HA, rash, nausea); PRIMARY DRUGS for treatment of asthma in CONJUNCTION with other agents (bronchodilators and immunosuppressives); MOST USEFUL in treatment of EXTRINSIC asthma
Term
H1-Antihistamines
Definition
useful in treating allergic rhinitis & allergic dermatitis; NOT EFFECTIVE in treating bronchospastic conditions; SEs: dries secretions
Term
anticholinergic agents (ipratropium [Atrovent], tiotropium [Spiriva])
Definition
prevents bronchospasm indcued by ACh - limited effectiveness; ADRs: dries secretions; produces few systemic effects due to quaternary nature; used in combination with albuterol [Combivent]
Term
Beta-Adrenergic Agonists (epinephrine, metaproterenol, isoproterenol, albuterol, levalbuterol, salmeterol, terbutaline, pirbuterol)
Definition
act as bronchodilators & inhibit release of autocoids from mast cells; act quickly & are fairly effective in treating acute asthma attack; ADRs: CNS stimulation (anxiety, tremors, restlessness, irritability); development of tolerance & rebound bronchoconstriction are major problems
Term
epinephrine
Definition
drug of choice in treating life-threatening anaphylactic rxns
Term
methylxanthines [theophylline, aminophylline]
Definition
cause bronchodilation & may inhibit release of mediators from mast cells; inhibits phosphodiesterase leading to increased cAMP in smooth muscle & mast cells; interacts with adenosine receptors; have NARROW THERAPEUTIC WINDOWS --> monitor blood levels; Toxic Effects: mild - nausea, vomiting, HA, insomnia, & nervousness; severe - cardiac arrhythmias, seizures
Term
theophylline
Definition
methylxanthine taken orally in conjunction with other agents in more severe forms of asthma; available in time-release preparations
Term
aminophylline
Definition
more water soluble methylxanthine; given IV for treatment of severe asthma attacks
Term
corticosteroids (glucocorticoids: cortisone, prednisone)
Definition
have anti-inflammatory activity, inhibit recruitment of leukocytes into inflammatory response; inhibit synthesis or release of autocoids including prostaglandins, thromboxanes, leukotrienes, platelet activating factor, etc.; VERY BENEFICIAL in reducing severity of cell-mediated immunological damage to bronchial epithelium; very effective PROPHYLACTICALLY, not in acute attacks;
Term
ADRs of corticosteroids
Definition
development of cataracts (inhaled); Cushing syndrome; suppression of immune system; osteoporosis; peptic ulceration; suppression of growth in children; suppression of HPA axis; menstrual & reproductive problems
Term
zafirleukast [Accolate] & monteleukast [Singulair]
Definition
cysteinyl leukotriene receptor antagonists; oral - chronic use to reduce frequency & severity of asthma attacks; less effective than corticosteroids; approved for treatment of seasonal allergies
Term
zileuton (Zyflo)
Definition
5-lipoxygenase inhibitor; oral - reduces frequency & severity of asthma attacks; potential elevation of liver enzymes & hepatotoxicity; take 4x per day
Term
Goals of Asthma Therapy
Definition
prevention of bronchospams; stabilization of patients
Term
Mild Asthma treatment
Definition
use only a simple bronchodilator therapy (albuterol, levalbuterol, etc)
Term
More severe asthma therapy
Definition
requires long-term treatment with a combo of drugs: bronchodilator --> acute attacks; stabilizing agent (cromolyn) + antiinflammatory steroid or leukotriene modulator
Term
Drugs for treatment of Anaphylaxis
Definition
epinephrine, theophylline & isoproterenol, dopamine, corticosteroids, H1-antihistamines
Term
treatment of Mild Allergies
Definition
H1-antihistamines are ideal drugs of choice; mast cell stabilizers or corticosteroids used in more severe allergies; monteleukast (Singulair) for seasonal allergies; systemic corticosteroids for most severe allergies
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