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Asthma pharmacology
Asthma medicine pharmacology
| Question | Answer |
|---|---|
| List the bronchodilators | SABAS LABAS Xanthine drugs Cysteinyl leokotriene receptor antagonists |
| List the anti-inflammatory agents | Inhaled corticosteroids Cromones Anti-IgE treatments Other Mabs |
| What drugs are used as emergency treatments? | Oxygen Hydrocortisone |
| At what phase of inflammation do relievers act, and what is their role in asthma management? | Immediate phase, immediate relief of bronchospasm. |
| At what phase of inflammation are preventers used and what is their role in asthma management? | Late phase-(influx of Th2 lymphocytes leading to epithelial damage). Preventer medications inhibitor airway inflammation and hyper-reactivity. |
| List the SABA bronchodilators | salbutamol and terbutaline |
| List the LABA bronchodilators | formoterol (eformoterol), indacaterol, salmeterol, vilanterol (only in combo with ICS), olodaterol (only in combo for COPD) |
| List the Xanthine bronchodilators | Theophylline |
| What is Montelukast? | A cysteinyl leukotriene receptor anatagonist (bronchodilator) |
| Explain the pharmacology of SABA's and LABA's | Act on the beta 2 adreno receptor in the lungs. Sends an intraceullar signal via an increase in cellular levels of cAMP to relax the airways by phosphorylating muscle proteins and reducing cellular levels of Ca2+. |
| What is the concern of prolonged use of SAB's? Why? | Desensitisation and down regulation of the beta 2 receptors. -receptors uncouple from adenylate cyclase, internalise and phosphorylate. Results in an overall net loss of receptors. This reduces efficacy of treatment, inc attacks and hospitalisation. |
| What is the dose of salbutamol? | 2 x 100mcg inhalations q4h prn |
| What is the dose of Terbutaline? | 1 x 500mcg every 4-6 hours prn (max 12 in 24 hours) |
| What must LABA's be given in combination with? | ICS Use without has been associated with serious exacerbations and deaths. |
| What is the dosing of Laba's? | Once or twice daily (dose varies for each indivual product) 1 - 30 minute onset of action 12-24 hr duration |
| Which ICS/LABA combo is used for SMART therapy? | Budesonide and Formoterol (maintenance and symptom relief) |
| What are the ADR's of SABA's and LABA's? | Common: tremor, palpitations, headache Inf: hyperglycaemia (high dose), tachycardia, muscle cramps, agitation, insomnia, hyperactivity in children R: paradoxical bronchospasm, allergic reactions - urticaria, angioedema, anaphylaxis, lactic acidosis |
| What are the precautions with SABA's/LABA's? | Cardiac disease at high doses (at normal doses okay) Cardiac arrythmias (exacerbation, low K+, chronotropic effect) Hypokalaemia (high dose and nubelisers) Diabetes (high doses) Hyperthyroidism Lactic acidosis |
| What is the MOA of Xanthines? | Unclear but thought to inhibit phoshodiesterases to inc cAMP, comp antag adenosine A1+A2, activate histone deacetylase, stimulates CNS respiratory (inc diaphragm contractility). Overall smooth muscle relaxation (bronchodilation), CNS stimulation. |
| What is theophylline indicated for? | Maintenance treatment in asthma and copd |
| Why is theophylline rarely used? | Narrow TI (need to monitor plasma drug levels) Need to consider drug/drug interactions, drug disease and anything that might impact elimination of theophylline from the body (excreted renally) |
| Use of theophylline can exacerbate which comorbidities? | GORD, arrythmia, epilepsy |
| What are the ADR's of theophylline? | C: n,v,d, headache, insomnia, irritability, anxiety, tremor, palpitations R: seizures, arrythmias (high conc), tachycardia |
| What is the MOA of LTRA's? | Potent inflammatory mediators that bind to cysteinyl leukotriene receptors and inhibit bronchoconstriction, mucous secretion, vascular permeability and eeisinophil recruitment |
| What are LTRA's indicated for? | Maintenance treatment of asthma. Dose is 10mg once daily |
| Why isn't Montelukast a first line treatment for adults with asthma? | Less effective than a LABA for those not using a low dose ICS Less effective than SABA's for exercise induced asthma No benefit in aspirin tolerant asthma |
| How is montelukast used in children with asthma? | Mainly an alternative to ICS (ICS still more effective in children 6+ with persistant asthma) Montelukast is more effective than a LABA for children with exercise induced asthma to control symptoms. |
| List the coricosteroids for asthma treatment | Beclomethasone Budesonide Ciclesonide Fluticasone propionate Fluticasone furoate Oral prednisolone |
| What are the cromones | Cromoglygate and nedocromil |
| List the MABS used in asthma. Which asthma drug is an Anti-IgE drug? | Omalizumab - Anti Ig E Mepolizuman Benralizumab Dupilumab Reslizumab |
| What is the MOA of corticosteroids? | Inhibits actions of IL-4/5/13 reducing prodn and r/lease of IgE and actvn eisinophils. Secondary actions: reduces proliferation of Th cells = reducing cytokines forming, inhibits induction of COX 2 = inhibition of PGE2 and PGI2 |
| What is the MOA of glucocorticoids? | Inhibits allergen influc of eisinophils into lungs, indirection reduces medaitor release from eisinophils and reduces cytokine release (IL-5 and GMCSF) Upregulates B2 adrenoreceptors, reduces synth of IL-3 = reduces mast cell production |
| How are corticosteroids used in asthma? | Prophylactic management and treatment of asthma Works in late phase of inflammation pathway Reduces airway inflammation and hyper-reactivity Mainstay of treatment for most people with asthma |
| How do the ICS' compare between each other? | No difference insafety Dose between each ICS varies Generally start on the lowest possible dose and adjust, but want to use the lowest possible dose. Fluticasone furoate is 5x more potent than fluticasone p, so FF can be given once daily |
| How are oral corticosteroids used in asthma? | For the management of asthma flares Should be given in the first hour of an asthma flare (adults/kids) Dose: 37.5-50mg d for 5-10 days (adults-prednisolone) 100mg q6h IV (Hydro -adults) 2mg/kg initially -1mg/kg (kids -pred) |
| What are the ADR's of ICS's? | C: dysphonia, oral thrush, bruising, R: allergic reactions (rash, angioedema, bronchospasm) R systemic: adrenal suppression, bone density loss, pneumonia, glaucoma, cataract, skin thinning, growth impairment, tooth enamel dissolved. |
| What is the MOA of anti-IgE MABS? | Antibodies that block IgE activation of receptors on mast cells and other inflammatory cells. Binds to IgE. |
| How are anti IgE drugs used in asthma? | Omalizumab - recombinant humaised MAB that reduces the immune systems response to allergen exposure. Used for maintenance treatment of moderate to severe allergic asthma. For patients that use ICS and have raised IgE serum levels. |
| What is the dose of Omalizumab? | SC injection every 2-4 weeks, maximum 150mg per injection. |
| What is the MOA of the other MABS? | Antibodies that block Il-5 (mepo), or IL-5 receptors (Benra) and reduce eisinophil production and survival. Used for maintenance therapy for severe, refractory asthma as an add on. |
Created by:
LDM
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