List the four major drug classes used for the prevention and treatment of asthma.
Anti-inflammatory classes: Glucocorticoids, Cromlyn, Leukotriene Modifiers, Anti-IgE. Bronchodilators: Beta-2 Adrenergic antagonists, methylxanthines, anticholinergics.
Describe the mechanism of action of each of the three classes of bronchodilator:
?-2 adrenergic sympathomimetics (agonists): activate ?-2 receptors? ? mucus clearance, bronchodilation, suppress histamine. Anticholinergics: Block muscarinic receptors in the bronchi ? bronchodilation. Methylxanthines: Inhibit phosphodiesterase to ?cAMP
Discuss the advantages and disadvantages of each Bronchodilator class in the treatment of both acute asthma exacerbations and chronic asthma control.
?-2 adrenergic sympathomimetics (agonists): short-acting for acute attacks =Albuterol [Ventolin], long-acting for longterm control= Salmoterol [Serevent]; disadvantage: albuterol can cause tremors angina and tachycardia, salmoterol must be used with ICS o
Which medication(s) are useful in the treatment of exercise induced asthma and why?
Cromolyn [Intal] cus inhibit mast cell degranulation, safest and first-line for mod asthma. Albuterol [Ventolin] cus bronchodilator w/ onset < 5 minutes
What is the mechanism of action of the non-steroidal anti-inflammatory medications?
Cromolyn [Intal] inhibits mast cell degranulation. Leukotriene modifiers prevent formation of leukotrienes (LT) or LT receptor interaction. Anti-IgE prevent mast cell degranulation by prevent IgE from binding mast cells.
Discuss why salmeterol should not be used without an inhaled glucocorticosteroid:
Black box warning for Salmeterol [Severvent] monotherapy, ? risk of bronchospasm.
Discuss the mechanism of action of the leukotriene inhibitor/receptor modifiers:
Inhibit formation of LT and prevent LT receptor interactions ? bronchodilation, ? mucus secretion, anti-inflammatory
Discuss the mechanism of action of Omalizumab:
Anti- IgE, prevents IgE from binding to mast cells= prevents mast cell degranulation
What are the benefits/drawbacks of inhaled glucocorticosteroids vs. oral glucocorticosteroids in the treatment of asthma?
Inhaled glucocorticosteoids if used properly have no systemic effects, but can cause oral candidiasis and dysphonia.
Oral glucocorticoids have systemic effects, only used for severe asthma. Both can cause growth suppression.
Discuss the adverse effects of Methylxanthines:
Narrow therapeutic index= quick toxicity. Signs of toxicity= N/V, insomnia, tachycardia, seizures. Other AEs= dysrhthymia & convulsion
Discuss the pharmacologic treatment of chronic obstructive pulmonary disease (COPD).
DOC= Anticholinergics: Ipatropium bromide [Atrovent], Tiotropium bromide [Spiriva]. If not effective add in a long acting beta-agonist (LABA) such as Salmeterol [serevent]
How does treatment for COPD differ from treatment for asthma?
Difference: Goal to slow disease progression, alleviate dyspnea thru bronchodilation and treat exacerbations. Similiarty: Asthma & COPD treatments are palliative not curative treatment. Monotherapy= Increased pneumonia risk.
Discuss the adverse effects of Anticholinergic medications:
Dry mouth, constipation, urinary retention, blurred vision, tachycardia
Discuss pharmacologic therapy for allergic rhinitis:
Antihistamines= Diphenhydramine, Loratadine [Claritin], Cetirizine [Zyrtec], Desloratadine, Corticosteroids= Fluticasone [Flonase], intranasal cromolyn sodium, decongestants= Phenylephrine, Pseudoephedine, Naphazoline
Compare/contrast the roles of antihistamines and decongestants with respect to their mechanisms of action and adverse effects?
Anti-histamines= Diphenhydramine, Loratadine, Cetirizine, Desloratadine, MOA= inhibit mast cell degranulation, antagonize histamine receptor-1, AE= sedation, anticholinergic effects.Indication: allergic rhinitis.
Decongestants= Phenylephrine, Pseudoephedr
How do the 2nd and 3rd generation antihistamines differ from the 1st generation antihistamines?
2nd and 3rd gen have less CNS effects, less sedation, and don't cross BBB. More selective and more potent
What is the role of Glucocorticosteroids in allergic rhinitis?
DOC for mod-severe and perennial allergic rhinitis. Relieve congestion, no systemic effects if used properly,
Discuss the pharmacologic treatment of cough:
Dry cough use Antitussives: Productive cough use Mucolytics: or Expectorants
Compare/contrast antitussives (opioids and non-opioids), mucolytics and expectorants with respect to their mechanisms of action and adverse effects?
Antitussives: Opiod or codeine. MOA= suppress central cough center in brain or peripheral cough center. Dextromethorphan [DXM] or Diphenhydramine, MOA suppress cough senter. DXM AE= respiratory suppression, Diphenhydramine AE= sedative, anticholinergic ef
What are the two main pharmacological classes use to treat asthma?
Anti-inflammatory drugs
Bronchodilators
What Anti-inflammatory agents are used to treat asthma?
Glucocorticosteroids
Cromolyn [Intal]
Leukotriene modifiers
Anti-IgE
What Bronchodilating agents are used to treat asthma?
?-2 adrenergic sympathomimetics (agonists)
Methylxanthines
Anticholinergics
List the glucocorticosteroids used to treat asthma:
Beclomethasone dipropionate [QVAR], IHC
Budenoside [Plumicort Flexhaler], IHC
Methylprednisolone [Medrol], oral
What is the indication MOA and AEs of Glucocorticosteroids?
Indication= Asthma
MOA= ? synthesis of inflammatory mediators
? infiltration of inflammatory cells
? airway edema, mucous production, & hypersecretion.
AE=Oropharyngeal candidiasis, dysphonia, self resolving growth suppression in children
What is the indication MOA and AEs of Leukotriene modifiers?
Indication= Asthma
MOA= inhibit LT formation or LT receptor interactions
AE= Headache, N/D, dyspepsia, liver injury
What are the two classes of Luekotriene modifiers and their respective drugs?
5-Lipooxygenase inhibitor: Zileuton
Leukotriene D4 receptor agonist: Zafirlukast, Montelukast
What is the indication MOA and AEs of Cromolyn [Intal]?
Indication: Asthma prophylaxis, exercise induced asthma
MOA= inhibit mast cell degranulation
AE= safest of all antiasthma meds, occasional cough or bronchospasm
What is the indication MOA and AEs of Anti-IgE, what drugs are in the class
Indication: Asthma
MOA= prevent IgE from binding mast cells= inhibit mast cell degranulation and histamine release
AE= none
Drugs= Omalizumab [Xolair]
What is the indication MOA and AEs of ?-2 Adrenergic Agonist?
Indication: Asthma or exercise induced asthma
MOA= Selective activation of ?-2 Adrenergic receptors, mucus clearance
AE= Black box warning if Salmeterol used without and IHC.
What is the indication MOA and AEs of Albuterol [Ventolin]?
Indication: Acute Asthma attack
MOA: short-acting, Selective activation of ?-2 Adrenergic receptors, mucus clearance
AE=Tachycardia, angina, tremor
What is the indication MOA and AEs of Salmeterol [Serevent]?
Indication: Asthma
MOA: long-term therapy, Selective activation of ?-2 Adrenergic receptors, mucus clearance
AE= Black box warning if used without and IHC, increased risk of bronchospasm
What is the indication MOA and AEs of Methylxanthine (theophylline)
Indication: Asthma
MOA: inhibit phosphodiesterase= suppress cAMP degradation=incr cAMP= bronchodilation
AE= toxicity, N/D, tachycardia, sleep disorders, seizures, convulsions
Which bronchodilator improves respiratory muscle function?
Methylxanthine (theophylline)
What is the indication, MOA, and AE of Anti-cholinergics?
Indication: Asthma, COPD
MOA: Block muscarinic receptors in the bronchii
AE: Dry mouth, constipation, blurred vision, tachycardia, urinary retention
What anti-cholinergic drugs are used to treat asthma?
Ipatropium Bromide [Atrovent], short-acting
Tiotropium Bromide [Spirivia], long-acting
What is the indication, MOA, and AE of Ipatropium Bromide and Tiotropium Bromide?
Indication: Asthma, COPD
MOA: Block muscarinic receptors in the bronchii ? bronchodilation
AE: Dry mouth, constipation, blurred vision, tachycardia, urinary retention
What classes of drugs are used to treat COPD?
Short-acting and long-acting Bronchodilators, Glucocorticosteroids
What classes of drugs are used to treat Allergic Rhinitis?
Antihistamines
Inhaled Corticosteroids (ICS)
Intranasal Cromylyn Sodium
Decongestants (sympathomimetics)
What is the indication, MOA, and AE of Antihistamines?
Indication: Allergic Rhinitis
MOA: prevent mast cell degranulation/ anatagonize histamine receptor to prevent histamine release
AE: Sedation, anticholinergic effects
List the 1st, 2nd, and 3rd gen Antihistamines
1st: Diphenhydramine,
2nd: Loratadine [Claritin], Cetirizine [Zyrtec]
3rd: Desloratadine [Clarinex]
When are antihistamines most effective?
When taken prophyllactically
What is the indication, MOA, and AE of Corticosteroids?
Indication: Allergic Rhinitis
MOA:? synthesis of inflammatory mediators
? infiltration of inflammatory cells
? airway edema, mucous production, & hypersecretion.
AE: Oral candidiasis, dysphonia, growth suppresion
What corticosteroids are used to treat Allergic Rhinitis?
Fluticasone [Flonase]
What is the indication, MOA, and AE of Fluticasone [Flonase]?
Indication: Allergic Rhinitis
MOA:? synthesis of inflammatory mediators
? infiltration of inflammatory cells
? airway edema, mucous production, & hypersecretion.
AE: anticholinergic effects
What is the indication, MOA, and AE of Intranasal Cromolyn Sodium?
Indication: Allergic Rhinitis prophylaxis
What is the indication, MOA, and AE of decongestants?
Indication: Allergic Rhinitis
MOA: Stimulate ?-1 receptors on smooth muscle of nasal blood vessels= vasoconstriction
AE= Rebound congestion if used > 3 -5 days
Contraindicated w/ HTN & CAD, cause irritability, anxiety, insomnia, abuse potential
Name decongestants used to treat Allergic Rhinitis:
Pseudoephedrine
Phenylephrine
Naphazoline
What is the indication, MOA, and AE of Pseudoephedrine, Phenylephrine, Naphazoline?
Indication: Allergic Rhinitis
MOA: Stimulate ?-1 receptors on smooth muscle of nasal blood vessels= vasoconstriction
AE= Rebound congestion if used > 3 -5 days
Contraindicated w/ HTN & CAD, cause irritability, anxiety, insomnia, abuse potential
What class of drugs are used to treat dry cough?
Opiod Antitussives
Non-Opiod Antitussives
What is the indication, MOA, and AE of Opiod Antitussives?
Indication: Dry cough
MOA: Suppress CNS cough center by inhibit excitatory neuropeptides and mu receptor
AE: respiratory depression
List the Non-Opiod Antitussives:
Dextromethorphan (DXM)
Diphenhydramine
What is the indication, MOA, and AE of Dextromethorphan (DXM)?
Suppress CNS cough center
What classes of drugs are used to treat productive cough?
Mucolytics and Expectorants
What is the class, indication, MOA, and AE of Acetylcysteine [Mucomyst]?
Class: Mucolytic
Indication: Productive Cough
MOA: breaks up mucous to be more watery,
What is the class, indication, MOA, and AE of Gauifenesen [Robitussin, Mucinex]
Class: Expectorant
Indication: Productive Cough
MOA: Facilitates coughing and mucus removal from respiratory tract by ? cough frequency, ? viscosisty of mucous in trachea and bronchi
Name the Glucocorticosteroids used for asthma:
Beclomethasone Dipropionate [QVar]
Budenoside [Plumicort Flexhaler]
Methylprednisolone
What is the class, indication, MOA, and AE of Beclomethasone Dipropionate [QVar]
Class: Glucocorticosteroids
Indication: DOC for Asthma
MOA: ? synthesis of inflammatory mediators= ?airway inflammation, mucus & edema
AE: Oral candidiasis, dysphonia, growth suppression
What is the class, indication, MOA, and AE of Budenoside [Plumicort Flexhaler]
Class: Glucocorticosteroids
Indication: DOC for Asthma
MOA: ? synthesis of inflammatory mediators= ?airway inflammation, mucus & edema
AE: Oral candidiasis, dysphonia, growth suppression
What is the class, indication, MOA and AE of: Methylprednisolone
Class: Glucocorticosteroids
Indication: DOC for Asthma
MOA: ? synthesis of inflammatory mediators= ?airway inflammation, mucus & edema
AE: Oral candidiasis, dysphonia, growth suppression + systemic affects