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Pharmacotherapy of asthma and copd 1.pptx

  1. Amity Institute of Pharmacy Pharmacotherapy of Asthma And COPD Advanced Pharmacology II M.PHARM (Pharmacology) SEM 2 BY: ABHINAV SINGH 1
  2. Amity Institute of Pharmacy Disorders of Respiratory Function • Mainly disorder of the respiratory system are : 1. Brochial asthma 2. cough 3.allergic rhinitis 4.Chronic obstructive pulmonary disease (COPD) also k/a emphysema 2
  3. Amity Institute of Pharmacy What is Bronchial Asthma? Bronchial asthma is a chronic respiratory disease characterized by inflammation and narrowing of the airways in the lungs, which causes difficulty in breathing. The inflammation causes the airways to become hyperreactive to certain triggers, such as allergens, irritants, and exercise, leading to symptoms such as wheezing, coughing, chest tightness, and shortness of breath. 3
  4. Amity Institute of Pharmacy Clinical Feature • Wheezing: a high-pitched whistling sound when breathing out • Shortness of breath: a feeling of breathlessness or difficulty in breathing • Chest tightness: a sensation of tightness or pressure in the chest • Coughing: a persistent cough, especially at night or early in the morning • Difficulty in breathing: breathing is rapid and shallow with a feeling of suffocation 4
  5. Amity Institute of Pharmacy • These symptoms may occur intermittently or persistently, and they may be triggered by certain factors such as: 1. Allergens: such as pollen, dust mites, animal dander, and molds 2. Irritants: such as tobacco smoke, air pollution, and strong odors 3. Exercise: physical activity or exertion can cause symptoms in some people 4. Respiratory infections: such as the common cold or flu, which can aggravate asthma symptoms 5. Emotional stress: stress or anxiety can also trigger asthma symptoms in some people. 5
  6. Amity Institute of Pharmacy Risk Factor • Genetics: asthma tends to run in families, and certain genetic variations may make a person more susceptible to the condition. • Allergies: people with allergies are more likely to develop asthma, as the inflammation caused by allergies can trigger asthma symptoms. • Environmental factors: exposure to pollution, dust, and other environmental irritants can increase the risk of developing asthma, especially in children. • Respiratory infections: certain respiratory infections, such as the common cold or flu, can increase the risk of developing asthma or exacerbate existing symptoms. • Obesity: being overweight or obese can increase the risk of developing asthma, especially in women. 6
  7. Amity Institute of Pharmacy • Occupational exposure: exposure to certain chemicals, dust, or fumes at work can increase the risk of developing occupational asthma. • Smoking: smoking or exposure to secondhand smoke can increase the risk of developing asthma or exacerbate existing symptoms. • Physical activity: in some people, physical activity or exercise can trigger asthma symptoms. • Stress: emotional stress or anxiety can trigger asthma symptoms in some people. 7
  8. Amity Institute of Pharmacy Airway innervations • Afferent nerves (sensory) 1. Irritant receptors in upper airways 2. C-fiber receptors in lower airways Stimulated by: exogenous chemicals physical stimuli (cold air) Endogenous inflammatory mediators * Efferent nerves( motor) Parasympathetic supply M3 receptors in smooth muscle and glands 8
  9. Amity Institute of Pharmacy Anti-Asthmatic drugs • Anti- Asthmatic Drugs: • These drugs are used to relieve the acute episodic attacks of asthma like bronchodilators, quick relief medications. • To reduce the frequency of attacks and nocturnal awakenings.(anti-inflammatory drugs , control therapy) • Bronchodilators: • Quick relief medications. • Treat acute episodic attack of asthma. • Short Acting Beta2- agonists • Antimuscarinics • Xanthine preparations 9
  10. Amity Institute of Pharmacy • Anti- inflammatory agents: (control medications or prophylactic therapy) Reduce the frequency of attacks • Corticosteroids • Mast cell stabilizers • Leukotrienes antagonists • Anti-IgE monoclonal antibody • Long acting β2-agonists 10
  11. Amity Institute of Pharmacy Anti-asthmatic drugs • Bronchodilators: (quick relief medications) This are used to relieve acute attack of bronchoconstriction 1. β2-adrenoreceptor agonists 2. antimuscarinics 3.xanthine preparations 11
  12. Amity Institute of Pharmacy • Mechanism of action (β2 adrenoreceptor agonist) • The mechanism of action of beta-2 agonists involves binding to and activating the beta-2 adrenoreceptors, which are coupled to a G protei2n that ultimately leads to the activation of the enzyme adenylate cyclase. Adenylate cyclase then converts ATP to cyclic AMP (cAMP), which activates protein kinase A (PKA) and ultimately leads to relaxation of the smooth muscle cells in the bronchioles. • Inhibit mediators release from mast cells. • Increase mucus clearance. 12
  13. Amity Institute of Pharmacy • Classification of β agonists: • Non Selective β agonists: Epinephrine – isoprenaline • Potent bronchodilator • Rapid action • s.c or inhalation • Has short duration of action 60-90 min • Drug of choice (Hypersensitivity reactions) Selective β2- agonists (Preferable) • Salbutamol • Terbutaline • Salmeterol • Formeterol 13
  14. Amity Institute of Pharmacy Non Selective β agonists: • Disadvantages • Not effective • Hyperglycemia • Cvs side effects : tachycardia, arrhythmia, hypertension • Skeletal muscle tremor • Not suitable for asthmatic patients with hypertension or heart failure. • Contraindications: • CVS patients , diabetic patients 14
  15. Amity Institute of Pharmacy Selective β2- agonists • Drug of choice for acute attack of asthma • Can be given orally, parentrally Short acting β2 agonists • E.g salbutamol,terbutaline Long acting β2 agonists • E.g salmeterol, formeterol Advantage of β2 Agonists • Minimal CVS side effects • Suitable for asthmatic patients with hypertension or heart failure Disadvantages of β2 Agonists Nervousness , tachycardia on over dose Skeletal muscle tremors 15
  16. Amity Institute of Pharmacy Muscarinic antagonists • Ipratropium- tiotropium • Acting by blocking muscarinic receptors • Aerosol inhalation • Quaternary Derivative of atropine • Does not enter diffuse into the blood. • Delayed onset of action • Ipratropium has short duration of action 3-5hr • Titropium has longer duration of action (24hr). • Pharmacodynamics • Are short-acting bronchodilator • Inhibit bronchoconstriction and mucus secretion • Less effective than beta 2 agonists • No anti-inflammatory action • Uses: • Main choice in chronic obstructive pulmonary disease (COPD) • In acute severe asthma combined with beta2 agonists & steroids. 16
  17. Amity Institute of Pharmacy Methylxanthines • Theophylline- aminophylline • Mechanism Of action : • These are phosphodiesterase inhibitors • Increase cAMP – bronchodilation • Adenosine receptors antagonists • Increase diaphragmatic contraction • Stabilization of mast cell membrane. Pharmacological effects: • Bronchial muscle relaxation • Increase contraction of diaphragm- improve ventilation • CVS: increase heart rate, increase force of contraction • GIT: increase gastric acid secretions • Kidney: increase renal blood flow ,weak diuretic action 17
  18. Amity Institute of Pharmacy Pharmacokinetics: • it is metabolized by cyt p450 enzymes in liver • Half life = 8 hours • Drug interaction -Enzyme inducers: as phenobarbitone-rifampicin-- increase metabolism of theophylline-- decrease half life. Uses: • Second line drug in asthma (theophylline) • For status asthmatics( aminophylline, given slow infusion) Side effects: • Low therapeutic index narrow safety margin • Cvs effects: hypotension, arrhythmia • GIT effects: nausea & vomiting • CNS effects: tremors, nervousness, insomnia, convulsions 18
  19. Amity Institute of Pharmacy • Glucocorticoids: MOA: -Inhibition of phospholipase A2 -decrease prostaglandin and leukotrienes -decrease number of inflammatory cells in airways. -Mast cell stabilization- decrease histamine release -Decrease capillary permeability and mucosal edema. -Inhibition of antigen-antibody reaction -Upregulate beta2 receptors (have additive effects to beta2 agonists) Routes of administration: -inhalation Eg: budesonide & fluticasone, beclomethasone -given by inhalation,given by metered-dose inhaler -have first pass metabolism -best choice in asthma, less side effects • orally: prednisone, methyl prednisolone • Injection: hydrocortisone, dexamethasone. • Systemic corticosteroids are reserved for a; • Status asthmaticus (i.v) • Using inhaled beta2 agonists 3 times /week • Or waking one night/week. 19
  20. Amity Institute of Pharmacy *Side effects due to systemic corticosteroids: -adrenal suppression -growth retardation in children -Osteoporosis -fluid retention, weight gain ,hypertension -hyperglycemia -susceptibility to infections -glaucoma -cataract -fat distribution, wasting of the msucles -psychosis 20
  21. Amity Institute of Pharmacy Mast Cell Stabilizers: • E.g: Cromolyn-Nedocromil • Act by stabilization of mast cell membrane. • Given by inhalation(aerosol, microfine powder, nebulizers) • Have poor oral absorption • Pharmacodynamics: • Not bronchodilators • Are not effective in acute attack of asthma • Prophylactic anti inflammatory drug • Reduce bronchial hyper reactivity. Uses: -prophylactic therapy in asthma -allergic rhinitis. -conjunctivitis. Side effects: -Bitter taste -Minor upper respiratory tract irritation(burning sensation , nasal congestion) 21
  22. Amity Institute of Pharmacy Leukotrienes’s antagonists • Leukotrienes: -produced by the action of 5-lipoxygenase on arachidonic acid -synthesized by inflammatory cellsfound in the airways(eosinophils, macrophages, mast cell) -Leukotriene –B4: chemotaxis of neurophills *Cysteinyl leukotrienes C4,D4 &E4: Bronchoconstriction Increase bronchial hyper-activity Mucosal edema, mucus hypersecretion. Leukotriene receptor antagonist: E.g: zafirlukast, montelukast, pranlukast -are selective , reversibile, antagonists of cysteinyl leukotriene receptors -taken orally -are bronchodilators -have anti-inflammatory action Less effective than inhaled corticosteroids Use: not effective to relieve acute attack of asthma Prophylaxis of mild to moderate asthma Aspirin-induced asthma Antigen and exercise inducd asthma 22
  23. Amity Institute of Pharmacy • Omalizumab: • Is a monoclonal antibody directed against human IgE • Prevents IgE binding with its receptors on mast cells & basophils. • Decrease release of allergic mediators • Used for treatment of allergic asthma • Expensive not first line therapy. 23
  24. Amity Institute of Pharmacy Drugs Used in COPD • COPD is a chronic irreversible airflow obstruction, lung damage and inflammation of the air sacs(alveoli). • Smoking is a high risk factor. 24 Treatment: – Inhaled bronchodilators – Inhaled glucocorticoids – Oxygen therapy -Antibiotics specifically macrolides such as azithromycin to reduce the number of exacerbations. -Lung transplantation
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  27. Amity Institute of Pharmacy • References: • KD. Tripathi 8th edition. • Leung, J. M., & Sin, D. D. (2017). Asthma-COPD overlap syndrome: pathogenesis, clinical features, and therapeutic targets. BMJ (Clinical research ed.), 358, j3772. • Hoshino, T., Toda, R., & Aizawa, H. (2009). Pharmacological treatment in asthma and COPD. Allergology international : official journal of the Japanese Society of Allergology, 58(3), 341–346. 27
  28. Amity Institute of Pharmacy • Thank You!! 28