Pharm Respiratory Drugs

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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:

β-2 adrenergic sympathomimetics (agonists): activate β-2 receptors→ ↑ mucus clearance, bronchodilation, suppress histamine. Anticholinergics: Block muscarinic receptors in the bronchi → bronchodilation. Methylxanthines: Inhibit phosphodiesterase to ↓cAMP degredation → bronchodilation

Discuss the advantages and disadvantages of each Bronchodilator class in the treatment of both acute asthma exacerbations and chronic asthma control.

β-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 or else ↑ risk of bronchospasm. Anticholinergics: long-acting for chronic control, disadvantages, dry mouth, tachycardia, constipation, urinary retention, blurred vision

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, Pseudoephedrine, Naphazoline, MOA= stim α-1 receptors on smooth muscle of nasal blood vessels (vasoconstriction). AE= rebound congestion if used > 3-5 days, irritability, anxiety, insomnia, contraindicated if HTN or CAD.

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 effects. Mucolytics: Acytylcysteine, MOA=break up mucous, makes watery. Or use or Expectorants: Guaifensin MOA= ↓ cough frequency, ↑ vol and ↓ viscosisty of mucous in trachea and bronchi

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?

β-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 β-2 Adrenergic Agonist?

Indication: Asthma or exercise induced asthma
MOA= Selective activation of β-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 β-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 β-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 α-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 α-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

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