PharmacologyPharmacologyPharmacology

DrugsDrugs usedused toto treat:treat: AsthmaAsthma RhinitisRhinitis && CoughCough TopicsTopicsTopics

•• Bronchodilators Bronchodilators •• Decongestants Decongestants •• Methylxanthines Methylxanthines •• Antihistamines Antihistamines •• Anticholinergics Anticholinergics •• Antitussives Antitussives •• Anti-inflammatory Anti-inflammatory •• Expectorants Expectorants && AgentsAgents mucolyticsmucolytics •• Leukotriene Leukotriene AntagonistsAntagonists •• Mast Mast cellcell stabilizersstabilizers AsthmaAsthmaAsthma

•• Inflammatory Inflammatory responseresponse toto allergenallergen •• Antibody Antibody bindsbinds withwith && rupturesruptures mastmast cellscells –– Releases Releases histamine,histamine, prostaglandins,prostaglandins, leukotrienesleukotrienes •• Two Two primaryprimary issuesissues –– Bronchoconstriction Bronchoconstriction –– Inflammation Inflammation (mucous(mucous production)production) ApproachesApproachesApproaches tototo TreatmentTreatmentTreatment

•• Relax Relax bronchialbronchial smoothsmooth musclemuscle –ß agonists –ß22 agonists –– methylxanthines methylxanthines –– anticholinergics anticholinergics •• Inhibit Inhibit releaserelease ofof mediatorsmediators –– Glucocorticoids Glucocorticoids –– Mast Mast cell cell stabilizers stabilizers •• Block Block affectsaffects ofof mediatorsmediators –– Leukotriene Leukotriene antagonists antagonists BronchodilatorsBronchodilatorsBronchodilators

albuterol (Proventil®), ß2 agonists metaproterenol (Alupent®) terbutaline (Breathair®) Nonselective epinephrine (Adrenalin®) Methylxanthines theophylline (TheoDur®) aminophyllin, (Aminophylline®) Anticholinergics ipratropium bromide (Atrovent®) AntiinflammatoryAntiinflammatoryAntiinflammatoryAgentsAgents Agents

Glucocorticoids

inhaled beclomethasone (Beclovent®) flucticasone (Flovent®) oral prednisolone (Deltasone®)

injected methylprednisolone (Solu-Medrol®) dexamethasone (Decadron®) Mast cell Stabilizer cromolyn (Nasalcrom®, Intal®)

Leukotriene Antagonists zafirlukast (Accolate®) zileuton (Zyflo®) ColdsColdsColds andandand AllergiesAllergiesAllergies

•• Nasal Nasal InflammationInflammation –– Vasodilation Vasodilation && engorgementengorgement •• Itching, Itching, redness,redness, rhinorrhearhinorrhea –– Mast/basophil Mast/basophil degranulation degranulation NasalNasalNasal DecongestantsDecongestantsDecongestants

•• ⇓⇓congestioncongestion viavia •• phenylephrine phenylephrine (Neo- (Neo- vasodilationvasodilation SynephrineSynephrine®®)) • Alpha stimulation • pseudoephedrine • Alpha11 stimulation • pseudoephedrine ® ® –– Topical Topical administration administration (Sudafed(Sudafed®,, ActifedActifed®)) •• A A momentmoment ofof silencesilence for:for: –– phenylpropanolamine phenylpropanolamine (AlkaSeltzer(AlkaSeltzer Cold Cold®®,, ContactContact®®, , AllerestAllerest®®)) AntihistaminesAntihistaminesAntihistamines

•Hreceptors • Other histamine •H11 receptors • Other histamine –– Vasodilation Vasodilation receptorsreceptors –– Increased Increased capillary capillary –– Sedation Sedation permeabilitypermeability –– Bronchoconstriction Bronchoconstriction •Hreceptors •H22 receptors –– Increase Increase gastric gastric acid acid secretionsecretion (Zantac(Zantac®®),), etc)etc) AntihistamineAntihistamineAntihistamine AgentsAgentsAgents

•• First First generationgeneration •• Second Second generationgeneration –– Sedation Sedation –– No No sedationsedation •• chlorpheniramine chlorpheniramine –– blood-brain blood-brain barrierbarrier (Chlor-Trimeton(Chlor-Trimeton®®)) •• Sniff, Sniff, sniff:sniff: •• diphenhydramine diphenhydramine –– terfenadine terfenadine (Seldane (Seldane®®)) ® (Benadry(Benadry®)) •• fexofenadine fexofenadine ® •• clemastine clemastine (Tavist (Tavist®®)) (Allegra(Allegra®)) ® •• promethazine promethazine •• cetirizine cetirizine (Zyrtec (Zyrtec®)) ® (Phergan(Phergan®)) •• loratadine loratadine (Claritin (Claritin®®)) CoughCoughCough SuppressantsSuppressantsSuppressants

•• Antitussives Antitussives •• Expectorants Expectorants –– Decrease Decrease coughcough reflexreflex –– guaifenesin guaifenesin may may work work –– Opioids Opioids –– others others areare doubtfuldoubtful •• codeine codeine & & hydrocodone hydrocodone •• Mucolytics Mucolytics – Non-opioids – Non-opioids –– Decreases Decreases viscocityviscocity •• dextromethorphan dextromethorphan –– acetlycysteine acetlycysteine •• benzonatate benzonatate (Mucomyst®®) (Tessalon®)(Tessalon®) (Mucomyst ) –– hypertonic hypertonic salinesaline ThankThankThank You!You!You!

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