pulmonology pharmacology
Terms
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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 -
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
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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
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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
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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 -
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
- 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
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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 -
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
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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 -
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
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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 -
Cromolyn
(Intal)
Pharmacokinetics -
-MDI (metered dose inhal), Neb soln
-progressively inhibits BHR -
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 -
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???
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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
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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 -
Zileuton
(Zyflo)
Use -
Long-term asthma control
Asthma prophylaxis -
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) -
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 -
Phenylephrine
Class -
Alpha-adrenergic agonist-Nasal Decongestant
(topical) -
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 -
Phenylephrine
Pharmacokinetics -
-rapid onset
-combo w/ antihistamines