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58 Cards in this Set

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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.
Albuterol
(Proventil)
(Ventolin)
Bitolterol
(Tornalate)
Pirbuterol
(Maxair)
Terbutaline
(Brethine)

class
Short Acting B2 Agonist
Albuterol
(Proventil)
(Ventolin)
Bitolterol
(Tornalate)
Pirbuterol
(Maxair)
Terbutaline
(Brethine)

S.E.
Toxic SE:

Tachycardia
Hyperglycemia
Hypokalemia
Hypomagnesemia
Albuterol
(Proventil)
(Ventolin)
Bitolterol
(Tornalate)
Pirbuterol
(Maxair)
Terbutaline
(Brethine)

Uses
Mild Asthma

Symptomatic tx of bronchospasm

Rescue agents for acute brochospasm
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
Salmeterol
(Serevent)
Formoterol
(Foradil)

class
Long Acting B2 Agonist
Salmeterol
(Serevent)
Formoterol
(Foradil)

MOA
Like short-acting B2 but--
Lipophilic side chain increases affinity of drug for B receptor
Salmeterol
(Serevent)
Formoterol
(Foradil)

use
Prevention of Asthma Attacks
(including exercise-induced)
Salmeterol
(Serevent)
Formoterol
(Foradil)

S.E.
Similar to short-acting B2

ie:

Toxic SE:
Tachycardia
Hyperglycemia
Hypokalemia
Hypomagnesemia
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
Beclomethasone
(Qvar, Vanceril)

Class
Inhaled Corticosteroid
Beclomethasone
(Qvar, Vanceril)

MOA
Vasoconstriction and Anti-inflammatory

Precise MOA unknown—active against many inflammatory cells and mediators
Beclomethasone
(Qvar, Vanceril)

USE
Moderate to Severe Asthma

Asthma control in acute and late inflammatory phases
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
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
IHHALED STEROIDS
Benefits:
less sx/exacerbations/use of quick relief meds, better lung function and reduced airway inflammation
INHALED STEROIDS

DOC
-DOC in moderate to severe asthma, most effective long-term control therapy for persistant asthma
Inhaled Steroids

Effect on airway smooth muscle?
-no direct effect on airway smooth muscle
How must inhaled steroids be taken?
MUST be taken continuously to control inflammation
Pharmacokinetics of glucocorticoids?
inhaled glucocorticoids decrease # and activity of cells involved in airway inflammation
Inhaled steroids

Effect on need for systemic steroids?
-Inhaled steroids may reduce need for systemic steroids
Inhaled steroids

Effect on Bronchial activity?
-bronchial activity is reduced
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
Omalizumab
(Xolair)

Class
IgG1K Monoclonal Antibody
(recombinant DNA-derived, humanized)
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
Omalizumab
(Xolair)

USE
For patients 12 yoa or greater—moderate to severe persistent asthma with perennial aeroallergen and not contolled w/ inhaled steroids
Omalizumab
(Xolair)

SE
-Malignant neoplasms
(br, non-mel skin, prostate, melanoma, parotid)
-Anaphylaxis (rare)

Common: inj site rxn, viral inf, URTI, sinusitis, pharyngitis, HA
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
Cromolyn
(Intal)

Class
Mast Cell Stabilizer
Cromolyn
(Intal)

MOA
mast cell stabilizer
Cromolyn
(Intal)

Use
Prevention of exercise or allergen induced bronchospasm
Cromolyn
(Intal)
Bitter taste
Irriation of pharynx/larynx

SE
Cromolyn
(Intal)

Pharmacokinetics
-MDI (metered dose inhal), Neb soln
-progressively inhibits BHR
Nedocromil
(Tilade)

Class
Mast Cell Stabilizer
Nedocromil
(Tilade)

MOA
mast cell stabilizer
Nedocromil
(Tilade)

Use
Mild persistent or exercise-induced asthma
Nedocromil
(Tilade)

SE
Bitter taste
Irriation of pharynx/larynx
Nedocromil
(Tilade)

Pharmacokinetics
-MDI (metered dose inhal)
-inhibits early and late phase rxns
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
Theophylline

Class
Methyxanthine/
Bronchodilator
Theophylline

MOA
MOA unclear—phosphodiesterase inhibitor-adenosine receptor blocker*?
(adenosine causes bronchoconstriction and phosphodiesterase destroys cAMP—cAMP causes bronchodilation)
Theophylline

USE
Unable to tolerate/not responsive to B2 agonists/steroids???
Theophylline

SE
-Seizures, arrhythmias (narrow therapeutic window)
-Nausea/Vomiting
-HA
-Diuresis
-Increased gastric acid
-Tachycardia
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
Zileuton
(Zyflo)

class
Leukotriene Modifier
Zileuton
(Zyflo)

MOA
Inhibits 5-lipoxygenase which inhibits synthesis of leukotrienes
-antagonist at the CysLT1 receptors—blocks action of C4,D4,E4
Zileuton
(Zyflo)

Use
Long-term asthma control

Asthma prophylaxis
Zileuton
(Zyflo)

side effects
Increased serum hepatic enzymes (monitor—d/c if > 3x normal)
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)
Zifirlukast
(Accolate)
Montelukast
(Singulair)
Leukotriene Receptor antagonist
Zifirlukast
(Accolate)
Montelukast
(Singulair)

USE
Prevent exercise, antigen, and aspirin induced bronchospastic attacks
Zifirlukast
(Accolate)
Montelukast
(Singulair)

SE
-Increased serum hepatic enzymes (monitor—d/c if > 3x normal)
Zifirlukast
(Accolate)
Montelukast
(Singulair)

Pharmacokinetics
-food impairs absorption
-90% PPB
-inhibits CYP 450 (may inc warfarin)
-90% PPB
Phenylephrine

Class
Alpha-adrenergic agonist-Nasal Decongestant
(topical)
Phenylephrine

MOA
Constrict dilated arterioles in nasal mucosa
Phenylephrine

Use
Short term treatment of nasal congestion
Phenylephrine

SE
Few systemic effects
-rebound congestion
Phenylephrine

Pharmacokinetics
-rapid onset
-combo w/ antihistamines