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DPPT Unit 3 > Asthma pharmacology > Flashcards

Asthma pharmacology Flashcards

1
Q

What are the pharmacological therapies for asthma?

Bronchodilators (4
Anti-inflammatory agents (4)
8 total)

A

Bronchodilators:

(1) β2-adrenergic agonists
(2) Epinephrine
(3) Anticholinergics
(4) Methylxanthines

Anti-inflammatory agents

(1) Corticosteroids
(2) Leukotriene inhibitors
(3) Cromolyn/Nedrocromil
(4) Anti-IgE

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2
Q

How does airway morphology change in asthma?

A

(1) Increased muscle mass
(2) Subepithelial fibrosis
(3) Edema
(4) Epithelial cell damage

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3
Q

How is asthma diagnosed?

A

hmm

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4
Q

What inflammatory mediators are released at different time intervals in asthma?

Immediate (4)
Minutes (2)
Hours (2)
(8 total)

A

Immediate (granule contents):

(1) Histamine
(2) TNF-α
(3) Proteases
(4) Heparin

Minutes (lipid mediators):

(5) Prostaglandins
(6) Leukotrienes

Hours (cytokine production):

(7) IL-4
(8) IL-13

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5
Q

What is the neurogenic cause of asthma?

A

hmm

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6
Q

What are the three main approaches to asthma therapy?

3

A

(1) Avoidance of causative factors
(2) Reverse bronchoconstriction
(3) Anti-inflammatory agents

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7
Q

What are characteristics of β-adrenergic agonists used to treat asthma?
(3)

A

(1) β2 most effective for bronchodilation without cardiovascular side effects
(2) Effective after oral or inhaled administration
(3) Stimulate adenylyl cyclase and increase cAMP, favoring bronchodilation

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8
Q

What are sites of drug action of β-adrenergic agonists?

A

hmm

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9
Q

What is a short-acting β2 adrenergic agonist and what are its features?

A

(1) Albuterol (Proventil)

(2) Maximal effect in 30 minutes but lasts several hours

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10
Q

What is a long-lasting β2 adrenergic agonist and what are its features?
(4)

A

(1) Salmeterol (Serevent)
(2) 12+ hour duration
(3) Not for acute attacks - 2 puffs daily for about 2 weeks for maximal effectiveness)
(4) Should not be used without corticosteroids

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11
Q

What are the adverse effects of β2 adrenergics?

2

A

Minimal due to low systemic absorption

(1) Tachycardia
(2) Muscle tremors

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12
Q

What are the non-selective β-adrenergic agonists used to treat asthma?

A

(1) Epinephrine - drug of choice for anaphylaxis, but with severe cardiovascular side effects
(2) Isoproterenol - very potent and fast acting, but can cause cardiac arrhythmias

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13
Q

What is the antimuscarinic/anticholinergic asthma drug and what are its features?

A

(1) Ipratropium bromide

(2) Not acute - peak effect in 1-2 hours

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14
Q

What are the adverse effects of ipratropium bromide?

A

Minimal side effects, alleviated by spacers

Drying of mouth and upper airways

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15
Q

What are the methylxanthines and their sources?

3

A

(1) Caffeine (coffee)
(2) Theobromine (cocoa)
(3) Theophylline (tea)

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16
Q

What is the mechanism of theophylline?

A

hmm

17
Q

What are the features of theophylline?

A

(1) Methylxanthine
(2) Oral administration
(3) Therapeutic dose: 5-15 ug/ml
(4) Not for acute bronchospasm

18
Q

What are the adverse effects of theophylline at therapeutic doses?
(5)

A

Therapeutic dose 5-15 ug/ml

(1) Headaches
(2) Nervousness
(3) Insomnia
(4) Nausea/vomiting
(5) Epigastric pain

19
Q

What are the adverse effects of theophylline at greater than therapeutic doses?
(3)

A

> 30 ug/ml:

(1) Hypokalemia
(2) Cardiac dysfunction

> 40 ug/ml:
(3) Seizures

20
Q

How is theophylline metabolized?

A

Theophylline is metabolized by cytochrome p450 in the liver

21
Q

What are some theophylline drug interactions?

5

A

Increase serum theophylline:

(1) Erythromycin
(2) Oral contraceptives
(3) Anti-leukotrienes

Decrease serum theophylline:

(4) Barbiturates
(5) Chemicals in cigarette smoke, NOT nicotine

22
Q

What disease states may affect theophylline serum concentrations?

Increase (4)
Decrease (1)
(5 total)

A

Increase:

(1) Liver diseases
(2) Febrile illness: (a) pneumonia and (b) influenza

Decrease:
(3) Cystic fibrosis

23
Q

What corticosteroids are used to treat asthma?

Inhaled (2
Systemic (1)
3 total)

A

Inhaled:

(1) Flunisolide
(2) Fluticasone

Systemic:
(3) Prednisone

24
Q

What are the mechanisms by which corticosteroids treat asthma?
(4)

A

(1) Control eosinophils
(2) Reduce mucosal edema
(3) Potentiate β-adrenergic agonists
(4) Inhibit transcription of inflammatory agents

25
Q

What are the side effects of corticosteroids?

2

A

(1) Minimal if inhaled
(2) Oropharyngeal candidiasis
Systemic:
(3) Hypertension
(4) Diabetes
(5) Iatrogenic cushings
(6) Adrenal suppression
(7) Peptic ulcers

26
Q

What is Advair?

A

Combined therapy drug containing fluticasone and salmeterol

27
Q

What leukotrienes are involved in asthma?

A

(1) LTB4 - attracts neutrophils

(2) LTC4/D4 (SRS-A) - causes (a) bronchoconstriction, (b) hyperreactivity, (c) mucosal edema, and (d) mucus secretion

28
Q

What antileukotrienes are used to treat asthma?

A

(1) Zileutin - inhibits 5-lipoxygenase (converts arachidonic acid to leukotrienes)
(2) Zafirlukast - leukotriene receptor antagonist

29
Q

How are anti-leukotrienes metabolized?

A

In the liver by cytochrome p450

30
Q

What are anti-leukotriene drug interactions?

5

A

(1) Increases theophylline levels
(2) Decreases warfarin clearance (increased prothrombin time)
(3) Increases carbamazepine effect
(4) Erythromycin decreases zafirlukast
(5) Can be used to reduce dose of glucocorticoids

31
Q

What are the side effects of anti-leukotrienes?

A

(1) Abnormal liver function tests
(2) Tachycardia
(3) Alopecia
(4) Rash
(5) Fibromyalgia-like symptoms
(6) Churg-Strauss syndrome (eosinophilic)

32
Q

What is notable about the efficacy of anti-leukotrienes?

A

(1) Anti-leukotrienes don’t work on everyone and efficacy is unpredictable
(2) Not as potent of a bronchodilator as β-adrenergics or theophylline
(3) Less potent anti-inflammatory than glucocorticoids

33
Q

What is cromolyn/nedrocromil?

A

(1) Inhibitor of mediator release from mast cells, neutrophils, and eosinophils
(2) Causes interaction between secretory vesicles and cytoskeleton
(3) May suppress Ca2+ and Cl- channel activity

34
Q

How is cromolyn/nedrocromil used?

A

(1) Used prophylactically

(2) Administered by inhaler

35
Q

What are side effects of cromolyn/nedrocromil?

3

A

Minimal side effects and localized to site of action:

(1) Throat irritation
(2) Cough
(3) Mouth dryness

36
Q

What is the anti-IgE drug and how does it work?

A

(1) Omalizumab
(2) Binds circulating IgE regardless of specificity
(3) Forms biologically inert Omalizumab:IgE complexes
(4) Decreases IgE levels and downregulates IgE receptors within 90 days

37
Q

Overall, how are different severities of asthma treated?

A

(1) Mild (2 episodes per week) - long-acting β2 adrenergic agonist (salmeterol), inhaled glucocorticoids (fluticasone) or advair
(3) Severe (daily episodes) - oral glucocorticoids (not good chronically)

DPPT Unit 3 (15 decks)

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