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Anti Asthmatic Drugs:

Classification: Name Bronchodilators 1. sympathomimetics a) Selective beta agonists Short acting Salbutamol turbutaline Long acting salmetrol fenoterol formoterol pirbuterol b) non selective agents adrenaline isoprenaline ephedrine 2. methylxanthines theophylline aminophyllin 3. anticholenergics ipratropium bromide atropine Anti inflammatory agents: 1. systemic glucocorticoids eg. Hydrocortisone, prednisolone 2. inhalational beclomethasone budesonide fluticasone triamcinolone Mast cell stabilizers disodium cromoglycate nedocromil Dose Route

Prepared By Navjot Brar, Lecturer, Med Surg

ketotifen Leukotriene receptor antagonists montelukast zafirlukast leukotriene pathway inhibitors

Ze339 Zileuton

Anti IgE antibody omalizumab

Mechanism of Actionit acts in the following ways 1. Salbutamol Stimulates 2 receptors of the bronchial smooth muscle Stimulation of the Adenylate Cyclase enzyme Increased intracellular cyclic-AMP (also reduction of the intracellular calcium) Smooth muscle relaxation Bronchodilatation occurs. 2. Salbutamol Acts on the 2 receptor of the mast cell c-AMP production Stabilization of the mast cell membrane No Histamine release No bronchoconstriction. 3. Salbutamol increases the muco-ciliary action of the lung. 4. Decreases micro-vascular permeability of the lung.

Mechanism of Action of Theophylline

Prepared By Navjot Brar, Lecturer, Med Surg

1. Combines with the adenosine receptor (PI) and acts as antagonist of adenosine thus prevents it to cause contraction of the bronchial smooth muscle. 2. Combines and inactivates phospho-diesterase enzyme and degradation of the cyclic-AMP stops. CAMP accumulates in the bronchial smooth muscle and causes bronchodilatation. C-AMP has negative effect on the release of the calcium from the endoplasmic reticulum.

Mechanism of action of adrenaline:

Mechanism of Action of cholenergics Vagal nerve innervation acetyle choline muscarinic receptor bronchoconstriction

Prepared By Navjot Brar, Lecturer, Med Surg

Anticholinergics act here by inhibiting the muscarinic receptors Ipratropium Bromide (atropine methyl nitrate) Advantages Disadvantages given orally, only inhalation

o Can reach in high doses in the bronchial o Cannot be airway. (expensive) o Do not readily enter CNS. o Has less systemic effect. o Useful adjuvant to other drugs like Salbutamol Pharmacological effects Lungbronchodilatation

o Bronchodilatation effect is not great o Full effect after long use

CNScortical stimulation, excitement, mental exhaustion and fatigue. Loss of sleep. Stimulate medullary respiratory and vomiting center. CVSpositive ionotropic and chronotropic effects. CO, HR, force of contraction. At large doses it causes cerebral vaso-constriction. In high leveltoxicitycardiac arrhythmia, tachycardia Kidneydiabetic action. renal blood supply and GFR. Na+ and other electrolyte absorption. Skeletal musclediaphragmatic contraction is stimulated. fatigue of the skeletal muscle. Causes tremor. GIT gastric acid secretion. IndicationsBronchial asthma, COPD, apnea / preterm infant apnea. Comparison between Salbutamol ( beta agonists) and Aminophylline( methylxanthines) as antiasthma drug Points Mechanism Action Onset of action Salbutamol Aminophylline

of Selective stimulation of the 2 Competitive inhibition of the bronchial adrenoceptor of bronchial smooth muscle adenosine receptors and causes and causes bronchodilatation bronchodilatation Slower Rapid

Prepared By Navjot Brar, Lecturer, Med Surg

Duration of Longer action Therapeutic Larger index In acute asthma Suitable in inhaler form Drug of choice Side effects Mildest asthmatic with intermittent attack Tremor, headache, cardiac arrhythmia

Shorter Narrow Suitable in IV form Severe acute asthma asthma Headache, vomiting and chronic

Anti-inflammatory drugs
Glucocorticoids o Phospholipase A2 blocker o Acts by inhibiting the PG secretion, no leukotriens secretion o Decrease permeability to capillaries exudation and transudation Corticosteroids anti-inflammatory drug (inhalation, tablet, IV). Betamethasone Inhaler / long acting Beclomethasone Prednisone Tablet / intermediate acting Prednisolone Hydrocortisone IV / short acting

*** cannot suddenly stop these drugs, tapering of the dose to avoid withdrawal syndrome and to avoid precipitating acute problems. Action of Corticosteroids neutrophil, RBC, platelet eosinophil, lymphocyte, monocyte

Prepared By Navjot Brar, Lecturer, Med Surg

Monocyte IL1, TNF, Pyrogen Lymphocyte IL2 T-Lymphocyte TNF (responsible for septicemic shock syndrome)

IL1 fever, PAF, PG, Neutrophil and Lymphocytes IL2 CD8, T-cell TNF Cytokinin

Mast cell stabilizer

Na-chromoglycate, Nedocromil-Na o Reduces the hyper-reactivity of the bronchial o Prevention of another attack tree o Prevents eosinophilic and neutrophilic o Stabilizes the mast cell of the bronchial airway chemotaxis o They should be given only by inhalation o Also reduce the irritation of airway nerve endings o No bronchodilator effects o As tablets in advance to minimize or reduce risk Indication o Prophylaxis in allergic bronchial asthma. o Allergic rhinitis o Allergic conjunctivitis

Leukotriens pathway inhibitor

leukotriens are produced from the action of 5-lipoxegenase on arachidonic acid by variety of cells like basophiles, eosinophils, monocytes etc. They are of 2 categories o 5-lipoxegenase enzyme inhibitor (Zileuton) o LTD4 receptor antagonist (Zafirleukast, Monteleukast) *** these drugs are effective when given orally and have important role in aspirin induced asthma.

Prepared By Navjot Brar, Lecturer, Med Surg

Side-effects of anti asthmatics inhalation

Corticosteroids: Oral Candidiasis or Thrush: Leukotriene modifiers: Dysphonia (Hoarseness): Stomach upset Reflex Cough and Headache Bronchospasm Liver test abnormalities Poor Growth Skin rashes Decreased Bone Density: Rarely, Churg Strauss Disseminated Varicella syndrome Infection (chickenpox that spreads to organs) Bad taste in mouth Easy Bruising Cough Cataracts and Glaucoma Itching or Sore Throat Adrenal Gland Suppression Headache Viral illness Sneezing or stuffy nose Upper Respiratory Tract Shortness of breath Infections Wheezing Sinusitis Sore Throat Headache

Anaphylaxis: A very small (0.2%) number of patients taking Xolair injections may experience this potentially life threatening condition. Symptoms of anaphylaxis may include:

Sudden onset of asthma like symptoms such as wheezing, cough, shortness of breath, or trouble breathing. Feeling dizzy or faint Hives Changes in your voice, swelling of the tongue, or difficulty swallowing

a. Oropharyngeal candediasis (steroid causes immuno-suppresion)advised for frequent mouthwash b. Patient may have harshness / coarse voice Side-effects of tablet Peptic ulcer, glaucoma, osteoporosis, hypertension, aggravation of diabetes mellitus. Contraindications:

Prepared By Navjot Brar, Lecturer, Med Surg

Known hypersensitivity Lung cancer Bone marrow depression Cardiac dysrrythmias

Treatment steps
1. Occasional use of short acting 2 agonists 2. Low dose inhaled steroids (or other anti-inflammatory drugs) 3. High dose of inhaled steroid or low dose inhaled steroid plus long acting inhaled 2 agonist 4. High dose inhaled steroids and regular bronchodilators 5. Addition of regular oral steroid therapy Management of Acute Severe Asthmathe aim of management is to prevent death, to restore pulmonary function, to maintain optimum pulmonary function and to prevent early relapse. Status Asthmaticusacute emergency condition. Immediate treatment in Status Asthmaticus 1. 2. 3. 4. 5. Oxygengiven at highest concentration possible High dose of inhaled 2 agonistSalbutamol 2.5-5 mg as nebulizer and repeated every 30min Systemic corticosteroidsIV hydrocortisone or oral prednisolone (if patient can swallow) If severity persists then additional measurements used Monitoring of the patient

Prepared By Navjot Brar, Lecturer, Med Surg