Richard H. Kaszynski, Ph.D., Saki Hamaguchi, Shizuka Yamamoto, Marin Takaso, Naoya Aburada

Pharmacology Presentation 2011

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1. Background: Understanding Asthma

2. Mild intermittent asthmaa. QVAR® 50μg

b. Singulair 10mg

c. Uniphyl 200mg

3. Severe persistent asthmaa. Flutide Discus 100μg

b. Meptin Air 10μg

c. Theo-Dur 100mg

d. Meptin tablets 50μg

e. Predonine 5mg

Presentation Outline

Normal bronchiole

Asthmaticbronchiole

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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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Treatment options

Mild Intermittent AsthmaMild Intermittent Asthma

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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

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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 AsthmaSevere Persistent AsthmaTreatment 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 xanthinesEffects/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

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Severe persistant asthma ：　 Meptin tablets 50 μg

Generic name: Procaterol hydrochlorideEffects/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

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Severe persistant asthma ：　 Predonine 5mg

Generic name: PrednisoloneEffects/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

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Bronchodilator

Selective　β２ agonist

Procaterol Sulfate

Meptin Air

Meptin　Tablets

Methylxanthines

TheophyllineTheo-Dur

Uniphyl

Anti-inflamatory　

drugsSteroids

Beclomethasone　Dipropionate

QVAR

Fluticasone　propionate

Flutide　Diskus

Prednisolone PredonineAnti-

allergicsLeukotriene　antogonist

Monelukast　Sodium Singulair

Summary

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Thank you