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58 Cards in this Set
- Front
- Back
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Albuterol
(Proventil) (Ventolin) Bitolterol (Tornalate) Pirbuterol (Maxair) Terbutaline (Brethine) MOA |
Stimulates B2 receptors of SNS, activates adenyl cyclase increased cAMP (bronchial smooth muscle relaxation and inhibits release of inflammatory mediators by stabilizing mast cell membrane.
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Albuterol
(Proventil) (Ventolin) Bitolterol (Tornalate) Pirbuterol (Maxair) Terbutaline (Brethine) class |
Short Acting B2 Agonist
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Albuterol
(Proventil) (Ventolin) Bitolterol (Tornalate) Pirbuterol (Maxair) Terbutaline (Brethine) S.E. |
Toxic SE:
Tachycardia Hyperglycemia Hypokalemia Hypomagnesemia |
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Albuterol
(Proventil) (Ventolin) Bitolterol (Tornalate) Pirbuterol (Maxair) Terbutaline (Brethine) Uses |
Mild Asthma
Symptomatic tx of bronchospasm Rescue agents for acute brochospasm |
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Albuterol
(Proventil) (Ventolin) Bitolterol (Tornalate) Pirbuterol (Maxair) Terbutaline (Brethine) pharmacokinetics |
-Onset 15-30 min
-Relief 4-6 hrs -B2 agonists are not catecholamines -Slows inflammatory cascade, skeletal muscle stimulation -Most effective for relief of acute bronchospasm -Shouldn’t be scheduled (may decrease effectiveness or cause hyperresponsiveness |
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Salmeterol
(Serevent) Formoterol (Foradil) class |
Long Acting B2 Agonist
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Salmeterol
(Serevent) Formoterol (Foradil) MOA |
Like short-acting B2 but--
Lipophilic side chain increases affinity of drug for B receptor |
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Salmeterol
(Serevent) Formoterol (Foradil) use |
Prevention of Asthma Attacks
(including exercise-induced) |
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Salmeterol
(Serevent) Formoterol (Foradil) S.E. |
Similar to short-acting B2
ie: Toxic SE: Tachycardia Hyperglycemia Hypokalemia Hypomagnesemia |
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Salmeterol
(Serevent) Formoterol (Foradil) pharmacokinetics |
-Bronchodilation for at least 12 hours
-Slow onset -NOT for acute attacks -MDI(?), Diskus (dry powder) -Not for monotherapy -Not a substitute for anti-inflammatory therapy -Beneficial w/ inhaled steroids |
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Beclomethasone
(Qvar, Vanceril) Class |
Inhaled Corticosteroid
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Beclomethasone
(Qvar, Vanceril) MOA |
Vasoconstriction and Anti-inflammatory
Precise MOA unknown—active against many inflammatory cells and mediators |
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Beclomethasone
(Qvar, Vanceril) USE |
Moderate to Severe Asthma
Asthma control in acute and late inflammatory phases |
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Beclomethasone
(Qvar, Vanceril) SE |
Small risk at recommended dose—decrease risk by using spacer/rinsing mouth, lowest dose possible, in combo w/ long acting B2, monitor growth in children
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Beclomethasone
(Qvar, Vanceril) pharmacokinetics |
Qvar: aerosol MDI with no CFC and smaller particle size—goes to large, intermediate and small airways—contols at lower dose.
-max daily dose = 840 mcg/20 inh/day |
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IHHALED STEROIDS
Benefits: |
less sx/exacerbations/use of quick relief meds, better lung function and reduced airway inflammation
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INHALED STEROIDS
DOC |
-DOC in moderate to severe asthma, most effective long-term control therapy for persistant asthma
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Inhaled Steroids
Effect on airway smooth muscle? |
-no direct effect on airway smooth muscle
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How must inhaled steroids be taken?
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MUST be taken continuously to control inflammation
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Pharmacokinetics of glucocorticoids?
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inhaled glucocorticoids decrease # and activity of cells involved in airway inflammation
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Inhaled steroids
Effect on need for systemic steroids? |
-Inhaled steroids may reduce need for systemic steroids
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Inhaled steroids
Effect on Bronchial activity? |
-bronchial activity is reduced
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Inhaled Steroids
Effect of prolonged effect of inhaled steroids on airway smooth muscle |
-prolonged inhalation of steroids reduces the hyperresponsiveness of the airway smooth muscle
-anti-inflammatory steroids reduce inflammation by reversing mucosal edema, decreasing permeability of capillaries and inhibiting release of leukotrienes |
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Omalizumab
(Xolair) Class |
IgG1K Monoclonal Antibody
(recombinant DNA-derived, humanized) |
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Omalizumab
(Xolair) MOA |
inhibits the binding of IgE to high-affinity IgE receptor (FceRI) on mast cells and basophils—limiting the release of allergic mediators
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Omalizumab
(Xolair) USE |
For patients 12 yoa or greater—moderate to severe persistent asthma with perennial aeroallergen and not contolled w/ inhaled steroids
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Omalizumab
(Xolair) SE |
-Malignant neoplasms
(br, non-mel skin, prostate, melanoma, parotid) -Anaphylaxis (rare) Common: inj site rxn, viral inf, URTI, sinusitis, pharyngitis, HA |
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Omalizumab
(Xolair) PHARMACOKINETICS |
-first to target IgE excess antibodies
-antibody to IgE antibodies -reduces the # of FceRI receptors on basophils in atopic patients -Stops body from overreacting to asthma triggers by incapacitating IgE—may interrupt excessive response before it starts -SQ q 2-4wks |
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Cromolyn
(Intal) Class |
Mast Cell Stabilizer
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Cromolyn
(Intal) MOA |
mast cell stabilizer
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Cromolyn
(Intal) Use |
Prevention of exercise or allergen induced bronchospasm
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Cromolyn
(Intal) |
Bitter taste
Irriation of pharynx/larynx SE |
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Cromolyn
(Intal) Pharmacokinetics |
-MDI (metered dose inhal), Neb soln
-progressively inhibits BHR |
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Nedocromil
(Tilade) Class |
Mast Cell Stabilizer
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Nedocromil
(Tilade) MOA |
mast cell stabilizer
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Nedocromil
(Tilade) Use |
Mild persistent or exercise-induced asthma
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Nedocromil
(Tilade) SE |
Bitter taste
Irriation of pharynx/larynx |
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Nedocromil
(Tilade) Pharmacokinetics |
-MDI (metered dose inhal)
-inhibits early and late phase rxns |
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Nedocromil (tilade)
Cromolyn (intal) Similar characteristics that both share |
Both mast cell stabilizers (Cromolyn/Nedocromil) -prophylactic, anti-inflammatory
-not direct dilators -not in acute attack -reduces allergic rhinitis sx |
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Theophylline
Class |
Methyxanthine/
Bronchodilator |
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Theophylline
MOA |
MOA unclear—phosphodiesterase inhibitor-adenosine receptor blocker*?
(adenosine causes bronchoconstriction and phosphodiesterase destroys cAMP—cAMP causes bronchodilation) |
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Theophylline
USE |
Unable to tolerate/not responsive to B2 agonists/steroids???
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Theophylline
SE |
-Seizures, arrhythmias (narrow therapeutic window)
-Nausea/Vomiting -HA -Diuresis -Increased gastric acid -Tachycardia |
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Theophylline
pharmacokinetics |
-monitor levels
-similar to caffeine -anti-inflammatory -enhances mucociliary clearance -strengthens diaphragmatic contractility -mostly replaced by B-agonist and corticosteroids -many DDIs -causes bronchodilation, lipolysis, glycenolysis, gluconeogenesis and epinephrine |
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Zileuton
(Zyflo) class |
Leukotriene Modifier
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Zileuton
(Zyflo) MOA |
Inhibits 5-lipoxygenase which inhibits synthesis of leukotrienes
-antagonist at the CysLT1 receptors—blocks action of C4,D4,E4 |
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Zileuton
(Zyflo) Use |
Long-term asthma control
Asthma prophylaxis |
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Zileuton
(Zyflo) side effects |
Increased serum hepatic enzymes (monitor—d/c if > 3x normal)
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Zileuton
(Zyflo) Pharmacokinetics |
-5-lipoxygenase inhibits arachidonic acid leukotrienes
-leukotrienes: inc vasc perm and mucus and activate airway inflammation -5-lipoxygenase in mast, baso, eosino, and neutrophils -90% PPB -inhibits CYP 450 (may inc warfarin) |
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Zifirlukast
(Accolate) Montelukast (Singulair) |
Leukotriene Receptor antagonist
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Zifirlukast
(Accolate) Montelukast (Singulair) USE |
Prevent exercise, antigen, and aspirin induced bronchospastic attacks
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Zifirlukast
(Accolate) Montelukast (Singulair) SE |
-Increased serum hepatic enzymes (monitor—d/c if > 3x normal)
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Zifirlukast
(Accolate) Montelukast (Singulair) Pharmacokinetics |
-food impairs absorption
-90% PPB -inhibits CYP 450 (may inc warfarin) -90% PPB |
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Phenylephrine
Class |
Alpha-adrenergic agonist-Nasal Decongestant
(topical) |
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Phenylephrine
MOA |
Constrict dilated arterioles in nasal mucosa
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Phenylephrine
Use |
Short term treatment of nasal congestion
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Phenylephrine
SE |
Few systemic effects
-rebound congestion |
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Phenylephrine
Pharmacokinetics |
-rapid onset
-combo w/ antihistamines |
