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Pharmacology > Anti-Asthmatics > Flashcards

Anti-Asthmatics Flashcards

1
Q

Asthma

A

a common disease characterized by airway inflammation and episodic, reversible bronchospasm with severe shortness of breath. Subsets of clinical asthma may reflect differently
pathogenic factors and different responsiveness to currently
available therapies

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2
Q

Drugs useful in classic allergic asthma include (Bronchodilators)

A

Beta agonist
Muscarinic agonist
Methylxanthines

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3
Q

Anti-inflammatory agents

A

inflammatory release inhibitorsSteroids

Slow-antiinflammatory drugs, Antibodies

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4
Q

leukotriene antagonists

A

Lipoxygenase inhibitors, Receptor inhibitors

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5
Q

COPD drugs

A

bronchodilators, Steroids, and antibiotics

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6
Q

Bronchial hyperreactivity

A

Pathologic increase in the bronchoconstrictor response to antigens and irritants; caused by
bronchial inflammation

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7
Q

IgE-mediated disease

A

Disease caused by excessive or misdirected immune response mediated by IgE antibodies.
Example: asthma

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8
Q

Mast cell degranulation

A

Exocytosis of granules (vesicles) from mast cells with a release of mediators of inflammation and bronchoconstriction

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9
Q

Phosphodiesterase (PDE)

A

Family of enzymes that degrade cyclic nucleotides to nucleotides, for example, second messenger
cAMP (active) converted to AMP (inactive) or cGMP to GMP

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10
Q

Tachyphylaxis

A

Rapid loss of responsiveness to a stimulus (eg, a bronchodilator drug)

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11
Q

PATHOPHYSIOLOGY OF ASTHMA (immunologic causes)

A

The immediate cause of asthmatic bronchoconstriction is the release
of several mediators from IgE-sensitized mast cells and other cells
involved in immunologic response

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12
Q

mediators involved in asthma

A

leukotrienes LTC4 and LTD4, tryptase, histamine, and
prostaglandin D2. These substances bring about the “early response”
consisting of bronchoconstriction and increased secretions

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13
Q

“late response” of asthma

A

chemotactic mediators such as LTB4 attract inflammatory cells
to the airways and several cytokines, and some enzymes are released,
resulting in the “late response” leading to inflammation

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14
Q

Chronic inflammation leads to

A

Hyperreactivity y to various inhaled substances, including antigens, histamine, muscarinic agonists, and irritants such as sulfur dioxide (SO2) and cold air. This
reactivity is partially mediated by vagal reflexes

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15
Q

STRATEGIES OF ASTHMA THERAPY

A

Acute bronchospasm must be treated promptly and effectively with bronchodilators (“reliever” drugs). Beta2 agonists, muscarinic antagonists, and theophylline and its derivatives are available for this indication.

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16
Q

How is asthma treated long term

A

The most important anti-inflammatory drugs in the treatment of chronic asthma are corticosteroids. Long-acting β2 agonists can improve the response to corticosteroids. Anti-IgE antibodies also appear promising for chronic therapy. The leukotriene
antagonists

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17
Q

mechanisms of Beta agonist

A

stimulate Adenylyl cyclase, cAMP activity increases- relaxation of bronchial smooth muscle

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18
Q

MOA of Methylxanthines (found in tea, coffee, and cocoa)

A

inhibits Phosphodiesterase activity (degrades cAMP to AMP)- to increase cAMP levels, in turn, cause vasodilation and relaxing bronchial smooth muscle.
Methylxanthines also inhibits adenosine receptors (which leads to constriction)

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19
Q

MOA of Leukotriene antagonist

A

`inhibit LTE4 receptor, prevents exercise-induced asthma and aspirin induced bronchospasm

20
Q

MOA of Musc. antagonists

A

block Ach receptors, preventing bronchoconstriction

21
Q

MOA of corticosteroids

A

reduce the synthesis of PA2 and inhibits COX-2, reduced levels of PGs and Leukotrienes

22
Q

CROMOLYN & NEDOCROMIL

A

Cromolyn (disodium cromoglycate) and nedocromil are unusually insoluble chemicals; so even massive doses given orally or by the aerosol result in minimal systemic blood levels.

23
Q

MOA of Cromolyn and Nedocromil

A

The mechanism of action of these drugs is poorly understood
but may involve a decrease in the release of mediators (such as
leukotrienes and histamine) from mast cells. The drugs have
no bronchodilator action but can prevent bronchoconstriction
caused by a challenge with antigen to which the patient is allergic.
Cromolyn and nedocromil are capable of preventing both early
and late responses to challenge

24
Q

ANTI-IgE ANTIBODIES

A

Omalizumab is a humanized murine monoclonal antibody to
human IgE. It binds to the IgE on sensitized mast cells and prevents activation by asthma trigger antigens and subsequent release
of inflammatory mediators. Although approved in 2003 for the
prophylactic management of severe asthma, experience with this
drug is limited because it is very expensive and must be administered parenterally

25
Q

benralizumab, mepolizumab, and reslizumab antibodies that target

A

IL-5

26
Q

dupilumab, which targets the

receptor for

A

IL4-alpha and IL-13

27
Q

Methylxanthines Clinical app

A

Asthma, especially prophylaxis against nocturnal attacks

28
Q

Pharmacokinetics of Methylxanthines

A

Oral slow-release
Duration: 12 h
Aminophylline,
salt for IV use

29
Q

Toxicities, Interactions of Methylxanthine

A

Insomnia, tremor,
anorexia, seizures,
arrhythmias

30
Q

Roflumilast

A

a nonpurine molecule with effects similar to theophylline but more selective for PDE4; approved for COPD

31
Q

Caffeine

A

similar to theophylline with increased CNS effect, not used in asthma or COPD

32
Q

Theobromine:

A

similar to theophylline not used in asthma or COP

33
Q

Antimuscarinic agents

A

Ipratropium, tiotropium, aclidinium

Competitive pharmacologic
muscarinic antagonists

Asthma and chronic
obstructive pulmonary disease
Inhalation (aerosol)
Duration: several hours

Dry mouth, cough

34
Q

prototype drugs (Cromolyn and nedocromil)

A

Reduce release of inflammatory and bronchoconstrictor mediators from sensitized mast cells

Rarely used prophylaxis of asthma; cromolyn also used for ophthalmic,
nasopharyngeal, and gastrointestinal allergy

Inhaled aerosol for asthma
• cromolyn local application for other applications

Duration: 3–6 h

Cough when used by
inhalation

35
Q

Leukotriene antagonists (Montelukast, zafirlukast)

A

Pharmacologic antagonists
at LTD4 receptors

Prophylaxis of asthma Oral

Duration: 12–24 h

Minimal side-effects

36
Q

Zileuton

A

Inhibitor of lipoxygenase
• reduces synthesis of leukotrienes

Prophylaxis of asthma Oral

Duration: 12 h

Elevation of liver enzymes

37
Q

Corticosteroids

Inhaled (Beclomethasone)

A

Inhibition of phospholipase A2 • reduces expression of cyclooxygenase
Prophylaxis of asthma: drugs of choice

Inhalation
Duration: 10–12 h

Pharyngeal candidiasis; minimal systemic steroid toxicity (eg, adrenal suppression)

38
Q

Systemic Corticosteroids (Prednisone)

A

Like inhaled corticosteroids Treatment of severe refractory chronic asthma

Oral; Duration: 12–24 h

Adrenal suppression, growth inhibition,
muscle wasting, osteoporosis, salt retention, glucose intolerance,
behavioral changes

39
Q

Antibody (Omalizumab)

A 
Binds IgE antibodies on mast cells; reduces the reaction to inhaled antigen
Prophylaxis of severe, refractory asthma not responsive to all other drugs
Parenteral • administered 
as several courses of 
injections
Extremely expensive 
• long-term toxicity not yet 
well documented
40
Q

Short-acting beta agonists

A 
Albuterol 
Beta2-selective agonist -bronchodilation
Asthma acute attack relief drug of choice (not for prophylaxis)
Inhalation (aerosol)
Duration: 2–4 h
Tremor, tachycardia
41
Q

Metaproterenol, terbutaline

A

similar to albuterol; terbutaline also available as oral and parenteral formulations

42
Q

Long-acting beta agonists

A

Salmeterol, formoterol, indacaterol, vilanterol

Beta2-selective agonists; bronchodilation; potentiation of corticosteroid action

Asthma prophylaxis (not for acute relief) 
• indacaterol and vilanterol for COPD

Inhalation (aerosol)
Duration: 12–24 h

Tremor, tachycardia, cardiovascular events

43
Q

Nonselective sympathomimetics

A

Epinephrine, isoproterenol
Nonselective β activation-epinephrine also an α agonist
Asthma (obsolete) Inhalation (aerosol, nebulizer)
Duration: 1–2 h

Nausea, Dizziness, Pale skin, Tachycardia

44
Q

Indirect-acting sympathomimetic

A 
Ephedrine 
Releases stored catecholamines- causes nonselective sympathetic effects
Asthma (obsolete) 
Oral
Duration: 6–8 h

Insomnia, tremor, anorexia, arrhythmias

45
Q

Roflumilast

A

a nonpurine molecule with effects similar to theophylline but more selective for PDE4; approved for COPD

46
Q

Caffeine

A

similar to theophylline with increased CNS effect, not used in asthma or COPD

47
Q

Theobromine

A

similar to theophylline not used in asthma or COPD

Pharmacology (19 decks)

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