BRONCHIAL ASTHMA
1. Bronchodilators
a. Sympathomimetics
SABA
- Salbutamol
- Short Acting
- Given by inhalational route
- Terbutaline
- Used in acute attacks
LABA
- Formoterol
- Fast acting
- Used for acute attacks and prophylaxis
- Salmeterol
- Slow acting
- Only used for prophylaxis
- Metro → Long acting
- Slow → Salme
- Fast → Forme
VLABA → COPD only
- Olodaterol
- Vilanterol
- Carmoterol
- Karma (Carmeterol) for Old (Olodaterol) Villains (Vilanterol)
Adverse Effects of b2 Agonists
- T - Tachycardia
- T - Tremors
- Most common side effect
- T - Tolerance
- Mainly with long-acting beta 2 agonists
- T - T wave changes
- Because of hypokalaemia
- These drugs can cause hyperglycaemia (but never hypoglycemia)
b. Parasympatholytics
- M3 Blockers
- Ipratropium
- Tiotropium
- ► Given by inhalational route
c. Phosphodiesterase 3 Inhibitors
- Theophylline and aminophylline
- aka Methylxanthines
- Given orally or by intravenous route
- Not available by inhalational route
- MOA of Bronchodilatation
- Inhibit PDE 3 >> 4
- Thereby ↑ cAMP
- S/E due to PDE inhibition
- Nausea, Vomiting, Diarrhea
- Headache
- Arrhythmias
- Note: Sildenafil → PDE 5 ⛔
- Adenosine A1 receptor antagonist
- S/E due to Adenosine A1 antagonism
- Arrhythmias
- Diuresis
- Epileptic seizures
- MOA of Anti inflammation
- PDE 4⛔
- ↑ IL 10
- Histone deacetylase stimulation → similar to steroid
- Theophylline is metabolized by microsomal enzymes
- Prone to drug interactions
- Enzyme inducers
- Like smoking
- Decrease the effect
- Therefore smokers require higher doses
- Enzyme inhibitors
- Like ciprofloxacin, clarithromycin and erythromycin
- Can result in toxicity
- Seizures, arrhythmias etc.
New drugs COPD :
- Roflumilast : PDE4 ⛔
- Ensifentrine : Both PDE3 ⛔ and PDE4 ⛔
- Rough (Roflumilast) Siphon (Ensifen)
2. Drugs affecting LTs
a. Steroids
- DOC for prophylaxis
- Also used in acute attack
- Along with bronchodilators
- Fluticasone: Most potent
- MOA: Steroids produce annexin-1 → ⛔ Phospholipase A2 → reduction in bronchoconstriction (does not actively cause bronchodilation)
- MOA of systemic steroids
- To ↑↑ the sensitivity of b2 agonists
- Preferred by inhalational route
- MC side effect is oropharyngeal candidiasis, hoarseness of voice
- Topical Nystatin or clotrimazole is used to treat candidiasis
- Gargling after every dose will prevent this adverse effect
- Soft steroids
- Ciclesonide
- Beclomethasone
- Mnemonic: soft people → ikkili aakum → beclo ciclo
- Inactive orally ; activated in the lungs
- ↓risk of oropharyngeal candidiasis
Potency Level | Group |
Super high-potency | Group I |
High-potency | Group II, III |
Medium-potency | Group IV |
Lower mid-potency | Group V |
Low-potency | Group VI |
Least potency | Group VII |
b. LOX inhibitors
- Zileuton
- Mnemonic: ↓Leu - on → Leucotriene - Number
c. LT Receptor antagonists
- Zafirlukast
- Montelukast
- Black box warning: ↑↑ Suicidal ideation
3. Mast Cell Stabilizers
- Sodium Cromoglycate
- Nedocromil
- Ketotifen
- Mnemonic: Mast cell Stabilise cheyyan → chromium (sod chromoglycate, nedochromil) paint adikkam OR Tiffen lu vakkam (Ketotifen)
- Only used for prophylaxis
- Given by inhalational route
4. Omalizumab
- Monoclonal antibody against IgE
- Used for
- Urticaria
- prophylaxis of severe persistent Bronchial asthma
- Not effective in atopic dermatitis
- Given subcutaneously
- Kochinu asthma (asthma) vannapo maran Om Kreem (Om) kuttichathaennu prnj ammumma
5. Anti Interleukins
- In severe eosinophilic BA
- Anti-IL-5:
- Reslizumab
- Mepolizumab
- Mnemonic: Me poli Rasam → 5 benz rally (benralizumab) cheyyum
- Anti-IL-5 Receptor (IL-5R):
- Benralizumab
- Anti-IL-4 Receptor (IL-4R):
- Dupilumab
- out of 5 infront of reception, 4 are duplicate
- IL-13 inhibitor:
- Tralokinumab,
- Lebrikizumab
GINA (GLOBAL INITIATIVE FOR ASTHMA) GUIDELINES
Therapy Type | Drug of Choice (DOC) |
Acute Attack (Rescue Therapy) | Inhalational formoterol + Low dose inhaled corticosteroids |
Maintenance Therapy | Formoterol + Low dose ICS |
Anticholinergics (M3 Muscarinic Antagonists)
SAMA (Short-Acting Muscarinic Antagonists)
- Ipratropium
- Dosing: QID
IAMA (Intermediate-Acting Muscarinic Antagonists)
- Aclidinium
- Dosing: BD
LAMA (Long-Acting Muscarinic Antagonists)
- Tiotropium → OD
- Umeclidinium (Latest)
- Revefenacin (Latest)
Clinical Use
a. Bronchial Asthma
- Used as add-on drugs
b. COPD
- DOC: Tiotropium
- MOA: M3 Antagonist
- Treats bronchoconstriction due to:
- Parasympathetic overactivity (reversible component)
- Fibrosis/sclerosis (irreversible component)
- Side Effects
- Dry mouth
- Worsening of BPH
Antitussives
Dry Cough Management → Centrally Acting Agents
⛔ medullary cough center
- Opioids:
- Mild-moderate:
- Codeine
- Pholcodine
- Hydrocodone
- Severe (e.g., Bronchial CA):
- Methadone
- Morphine
- Non-Opioids:
- Mnemonic: Dry (Dextromethorphan, Diphenhydramine) Leaky (Levopropoxyphene) Nose (Noscapine)
- Dextromethorphan (most common)
- NMDA ⛔
- Side effects: Hallucinations (risk of abuse)
- Diphenhydramine
- Noscapine
- Levopropoxyphene
Productive Cough Management
- Expectorant:
- Guaifenesin
- Mucolytics: Liquefy mucous
- N-acetyl cysteine: Breaks disulfide bond
- Ambroxol/bromhexine: Depolymerize mucopolysaccharide
Productive Cough Syrup:
- Syrup: Guaifenesin + ambroxol/bromhexine + salbutamol
If codeine is coming to the market in combination with dextromethorphan as an anti tussive, this combination ____________
A. Should not be used due to risk of addiction
B. Can be used as both have different mechanism of action
C. Should not be used as it is irrational
D. Can be used to treat cough effectively
B. Can be used as both have different mechanism of action
C. Should not be used as it is irrational
D. Can be used to treat cough effectively
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