1. Richard H. Kaszynski, Ph.D., Saki Hamaguchi, Shizuka Yamamoto, Marin Takaso, Naoya Aburada Pharmacology Presentation 2011

2. Here comes your footer 1.Background: Understanding Asthma 2.Mild intermittent asthma a.QVAR® 50μg b.Singulair 10mg c.Uniphyl 200mg 3.Severe persistent asthma a.Flutide Discus 100μg b.Meptin Air 10μg c.Theo-Dur 100mg d.Meptin tablets 50μg e.Predonine 5mg Presentation Outline Normal bronchiole Asthmatic bronchiole

3. Here comes your footer 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

4. Here comes your footer Treatment options

5. Here comes your footer 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 Mild intermittent asthma ： QVAR® 50μg 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

6. Here comes your footer 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

7. Here comes your footer 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

8. Here comes your footer Treatment options

9. Here comes your footer 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

10. Here comes your footer Severe persistant asthma ： Meptin Air 10μg Generic name: Procaterol hydrochloride Effects/Mechanism of action selectivity on the b 2 -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

11. Here comes your footer 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 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 Side effects nausea and vomiting, headache, stomachache, loss of appetite, palpitations, diarrhea, heartburn, etc. Rhabdomyolysis, disturbance of consciousness, hyperglycemia, limpairment of liver function

12. Here comes your footer 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 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 β- adrenergic stimulation. Side effects Palpitations and tachycardia Tremor and headache Nausea and vomiting Skin rash

13. Here comes your footer 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 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 Side effects impaired wound healing peptic ulcer fluid retention hypertension プレドニン ® Menstrual irregularity Development of Cushingoid state

14. Here comes your footer Bronchodilator Selective β ２ agonist Procaterol Sulfate Meptin Air Meptin Tablets Methylxanthine s Theophylline Theo-Dur Uniphyl Anti- inflamatory drugs Steroids Beclomethasone Dipropionate QVAR Fluticasone propionate Flutide Diskus PrednisolonePredonine Anti-allergics Leukotriene antogonist Monelukast SodiumSingulair Summary

15. Here comes your footer Thank you