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Lecture 16

Drugs affecting the respiratory system

Expectorants-antitussives-bronchodilators
Phuong-Thuy Thi PHAN, M.S.
Recommended Reading

1) Thomas L.L., David A.W. (2013). Foye’s Principle of Medicinal


Chemistry 7th edition, Lippincott Williams & Wilkins: Baltimore.
Chapter 39. Asthma and chronic obstructive pulmonary disease, p.p.
1310-1344.

2) Trương Phương, Trần Thành Đạo (2017). Hóa dược 2 (Dùng cho đào
tạo dược sĩ đại học), NXB Giáo Dục Việt Nam. Chương 16. Thuốc tác
động lên hệ hô hấp, p.p. 426-446.

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Goals
1) Indentify the structural features of expectorants, antitussives and
bronchodilators

2) Describe mechanism of action of expectorants, antitussives and


bronchodilatos

3) Know the background information of expectorants, antitussives


and bronchodilators

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Respiratory system

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Regulating the secretion of mucus

• Bromhexine
• Ambroxol

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Mucolytics

• Acetylcysteine
• Amylase
• Alpha- chymotrypsin

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Expectorants
• Indirect stimulation: sodium iodide, sodium benzoate, ammonium
acetate, ammonium chloride….
• Direct stimulation: terpin hydrate, guaifenesin, guaiacol, eucalyptol

Guaifenesin Terpin hydrate Eucalyptol

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N-Acetylcysteine

Related substances

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Mucolytics

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Bromhexine hydrochloride

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Ambroxol

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Antitussives

▪ Coughing is a reflex to protect the body


▪ Coughing is a symptom of respiratory infections
▪ Antitissives can suppress coughing

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Antitussives

• Central antitussive
o Opioide: codeine, codethyline…
o Independent: dextromethorphan….
o Non-opiate: oxeladin, eprazinone…
o Anti-histamine H1: chlorpheniramine, chlorcyclizine…

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Antitussives
• Peripheral antitussive
o Local anesthesia action
Benzonatate
Tetracaine
Bromoform

o Alleviative action: extractum glycyrrhizae liquidum

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Dextromethorphan

▪ Related substances
• N,N-dimethylaniline
• 3-methoxymorphinan
• 17-methylmorphinan-3-ol
• 3-methoxy-17-methylmorphinan-10-on
• (4S) 3-methoxy-17-methylmorphinan

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Codethyline

apomorphine
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Eprazinone

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Eprazinone
• Suppress cough center

• Anti-histamin

• Peripheral anesthesia

• Mucolytic

• Reduce the viscosity of mucus

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Asthma

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Asthma

• Characteristics
o Increased response of bronchial mucosa
o Difficulty breathing
o Reversible bronchoconstriction

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Asthma

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Asthma

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Asthma

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Asthma

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ASTHMA

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β2 agonists

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β2 agonists - Contraindicated

• Patients being treated with IMAO

• Arrhythmia, coronary artery disease, high blood pressure,


diabetes

• Do not use with β-blocker agents

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Muscarinic antagonists

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Leukotrien antagonists

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