Chronic Bronchial Asthma
Richard H. Kaszynski, Ph.D., Saki Hamaguchi,
Shizuka Yamamoto, Marin Takaso, Naoya Aburada
Pharmacology Presentation 2011
Presentation Outline
1. Background: Understanding Asthma
2. Mild intermittent asthma
a. QVAR® 50μg
b. Singulair 10mg
c. Uniphyl 200mg
Normal
bronchiole
3. Severe persistent asthma
a.
b.
c.
d.
e.
Flutide Discus 100μg
Meptin Air 10μg
Theo-Dur 100mg
Meptin tablets 50μg
Predonine 5mg
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Asthmatic
bronchiole
Understanding Asthma
Characteristics
• Inflammation (swelling) of the
lining of the airways
• Fluid/mucus filling the
airways
• Bronchoconstriction tightening of muscles around
the airways
Methods of drug delivery
• Tablet
• Syrup
• Aerosol
• Inhaler
• Discus
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Mild Intermittent Asthma
Treatment options
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Mild intermittent asthma： QVAR® 50μg
QVAR® - “Quality and Value in Asthma Relief (Beclomethasone)
Effects/Mechanism of action
• small-particle inhaled corticosteroid (ICS）
• most effective anti-inflammatory agent used in asthma
• used to prevent attacks of asthma and not to treat acute attacks
• requires continuous and prolonged use to be effective
Side effects
• oral candidiasis occurs more frequently with higher doses
• pharyngitis, nausea and cough
Contraindications
•primary treatment of status asthmaticus or other acute episodes of
asthma where intensive measures are required
•hypersensitivity to any of the ingredients of QVAR contraindicates
use
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Mild intermittent asthma： Singulair 10mg
Generic name: Montelukast
Effects/Mechanism of action
•oral leukotriene receptor antagonist
•delivered orally (tablet form)
•takes 3 to 14 days of therapy before becoming
effective
•should not be used for the treatment of an
acute asthmatic attack
Side effects
• Headache and dizziness
• abdominal pain, sore throat, and rhinitis
Contraindications
•hypersensitivity to any component of this drug
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Mild intermittent asthma： Uniphyl 200mg
Generic name: Theophylline
Effects/Mechanism of action
•smooth muscle relaxation (i.e., bronchodilation)
•non-bronchodilator prophylactic effects—inhibits release of
bronchoconstrictor factors→suppression of the response of the
airways to stimuli
•sustained release preparation
Side effects
• Headache and dizziness
• abdominal pain, sore throat, and rhinitis
Contraindications
•hypertension, cardiac disease, liver disease, renal disease
•concurrent treatment with other xanthines may prohibit its use
•drinks or foods that contain caffeine (e.g. coffee, tea, cola, and
chocolate) should be avioded
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Severe Persistent Asthma
Treatment options
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Severe persistant asthma： Flutide Diskus 100μg
Generic name: Fluticasone
Effects/Mechanism of action
•synthesized adrenocorticosteroids
•provides potent, local anti-inflammatory effects
•minimally adverse systemic effects (e.g.
pituitary→adrenocortex function)
Side effects
•laryngopharyngeal symptoms (unpleasantness, irritation
and pain)
•oral candidiasis
•hoarseness and drymouth
Contraindications
•hypersensitivity to any component of this drug
•patients infected with tuberculosis
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Severe persistant asthma： Meptin Air 10μg
Generic name: Procaterol hydrochloride
Effects/Mechanism of action
•selectivity on the b2-adrenergic receptors of the bronchial smooth
muscle is high
•markedly bronchodilatory in small doses
•onset of action is prompt and duration of action is long
•potent anti-allergic action
Side effects
•Palpitation, fever, flush, tremor, headache, dizziness, fatigue,
sleeplessness, nausea
Contraindications
•Concomitant use with catecholamines (e.g. epinephrine or
isoproterenol) may induce arrhythmia & cardiac arrest
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Severe persistant asthma： Theodur 100mg
Generic name: Theophylline→ belongs to xanthines
Effects/Mechanism of action
•smooth muscle relaxation (i.e., bronchodilation) and stimulates
respiratory center
•non-bronchodilator prophylactic effects—inhibits release of
bronchoconstrictor factors
•should not be used for the treatment of an acute asthmatic attack
Side effects
•nausea and vomiting, headache, stomachache, loss of appetite,
palpitations, diarrhea, heartburn, etc.
•Rhabdomyolysis, disturbance of consciousness, hyperglycemia,
limpairment of liver function
Contraindications
•hypertension, cardiac disease, liver disease, renal disease
•concurrent treatment with other xanthines may prohibit its use
•drinks or foods that contain caffeine (e.g. coffee, tea, cola, and
chocolate) should be avoided
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Severe persistant asthma： Meptin tablets 50 μg
Generic name: Procaterol hydrochloride
Effects/Mechanism of action
•procaterol hydrochloride
•β-adrenergic receptors in the respiratory system was greater than
that for such receptors in the cardiovascular system
•long duration of bronchodilative action
•inhibits antigen-induced increases in airway resistance, the PCA
reaction, and histamine release from sensitized lung tissues
Side effects
•Palpitations and tachycardia
•Tremor and headache
•Nausea and vomiting
•Skin rash
Contraindications
•Catecholamines(e.g.,epinephrine)→may cause arrhythmias, or
cardiac arrest
• Xanthine derivatives drinks or foods that contain caffeine (e.g.
coffee, tea, cola, and chocolate)→tachycardia, arrhythmias) due to βadrenergic stimulation.
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Severe persistant asthma： Predonine 5mg
Generic name: Prednisolone
Effects/Mechanism of action
•smooth muscle relaxation (i.e., bronchodilation)
•synthetic adrenal corticosteroid
•oral prednisolone is a systemic steroid→goes directly into the
bloodstream
•wide applications in excessive inflammation (i.e. asthma, RA)
•should not be used for the treatment of an acute asthmatic attack
Side effects
•impaired wound healing
•peptic ulcer fluid retention
•hypertension
• Menstrual irregularity
• Development of Cushingoid
state
Contraindications
•hypertension, cardiac disease, liver disease, renal disease
•concurrent treatment with other xanthines may prohibit its use
•drinks or foods that contain caffeine (e.g. coffee, tea, cola, and
chocolate) should be avioded
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プレドニン®
Summary
Selective β２
agonist
Meptin Air
Procaterol Sulfate
Bronchodilator
Methylxanthines
Anti-inflamatory
drugs
Anti-allergics
Steroids
Leukotriene
antogonist
Theophylline
Meptin Tablets
Theo-Dur
Uniphyl
Beclomethasone
Dipropionate
QVAR
Fluticasone propionate
Flutide Diskus
Prednisolone
Predonine
Monelukast Sodium
Singulair
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Thank you
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