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22 Cards in this Set
- Front
- Back
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Name some β2 receptor agonists |
Salbutamol, salmeterol, forometerol |
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How do β-2 antagonists work |
Function via cyclic AMP- dependent relaxation of the smooth muscle Long acting β-adrenoceptor agonists have lipophilic groups attached which interact with exo sites on receptor binding site |
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What beta receptors are on the heart and lung? |
B1 on the heart B2 on the lung |
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Name other actions of adrenoceptor agonists |
Cholinergic transmission- inhibition if cholinergic acetylcholine release Inhibition of inflammatory mediator release- greater potency than smooth muscle relaxation and involves mast cell stabilisation, lymphocyte actuvation resulting in reduced plasma histamine, PAF, chemotactic factors Vascular permeability- suggestion its reduced by b-adrenoceptor agonist Mucociliary clearance- increase in ciliary beats to clear mucus |
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For therapeutics whats the routes of administration |
Inhaled, oral and intravenous/intramuscular |
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Explain each route of administration |
Inhaled- metered dose inhaler is commonly used( only 10% of drug enters the lung) for people who cant use this others include nebulisers Oral route- only non-catecholamines are effective via this route, side effects make this route last option but could be effectivr for small airway bronchodilation Intravenous/intramuscular- necessary for acute asthma. Given as a drip or as a bolus injection. Most commonly used with terbutaline |
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Problems with b2 adrenoceptor agonist |
When given systemically they elicit vasodilatopn via cyclic amp dependent relaxation of smooth muscle, the consequences are increased blood flow and fall in systemic vascular resistance. Fall in bp can cause reflex increased CO and tachycardia(can be dude to direct action on heart adrenoceptors) Increase metabolic processes like increased glucose, fatty ackds, ketone bodies and high density lipoprotein Increase in tremor associated with relaxation of slow contracting skeletal muscle |
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What are anti-allergic drugs |
Glucocorticoid: anti-inflammatory, inhibit PLA2 activity Widely used by inhalation(beclamatasone, budesonide, fluticasone proprionate) as prophylactic therapy- Many argue glucocorticoids should be the first line therapy in asthma |
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Anti allergenic drugs effects on permeability increasing mediators |
LTC4, LTD4, LTE4 secretion inhibited PAF synthesis inhibited PGE1 synthesis blocked and bradykinin formation inhibited O2 free radical formation inhibited |
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in what cell types what are the primary effector systems |
Alveolar macrophages( migration, IgG and complement decreased) Mast cells(decrease histamine release) Endothelial cells(decrease adhesive response, reduction in vascular permeability) Basophils(local influx inhibited) |
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Name the secondary recruited systems effected with anti allergenic drugs |
Neutrophils (IgG receptor decreased, increased apoptosis, decreased adherence to endothelium) Eosinophils(decreased adherence and chemotaxis) Lymphocytes( increased apoptosis and decreased differentiation, reduction in T4 helper cells and B cycle) Monocytes(migration inhibited, cell death, reduced production, reduced IgE receptor) |
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What is leukotriene B4 |
Neutrophil chemoatrractant |
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What do leukotriene c4 and b4 do and what inhibits it |
Cause bronchoconstriction increased bronchial reactivity, mucosal edema and mucus hypersecretion Leukotriene D4 inhibits these effects- zafirlukast and montelukast |
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What does zileuton do |
5-lipoxygenase is the enzyme involved in leukotriene synthesis- zileuton inhibits this and reduced the frequency of asthma exacerbations Liver toxitiy is a major side effect of zileuton so zarfirulast is better it has a bit of hepatoxicity but less than zileuton |
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What is montelukast unique side effect |
Eosinophillia and churg strauss syndrome |
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Xanthines are commonly used anti-asthmatic drugs, what is their mechanism |
Adenosine antagonist- blocks the inhibitory action of adenosine upon adenyl cyclade thus allow intracellular cAMP to accumulate and promote relaxation Phosphodiesterase inhibitor- blocks reduction in intracellular cyclic AMP and relax smooth muscle Effects catecholamines (increases release) shown to antagonise actions of PGE2 and PGF2α |
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Problems with oral theophylline |
Side effects include anorexia, vomiting and mild CNS stimulation Doses should be low to avoid gastroadominal problem .CNS stimulation is a problem when maintenance administration is increased too quickly, serious toxicity is a risk of seizures. Intravenous routes increase arrhythmia, palpitations, tachycardia at doses above 30mg/l |
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Name some anti muscarinics |
Ipratropium-M3 receptor Tiotropium- Primarily M2 and M3 receptor |
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What are anti muscarinics used in the treatment od ans whats side effetcs |
Treatment of COPD And potential use in asthma Se- dry mouth, exacerbation of natrow angle glaucoma and myasthenia gravis |
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Characteristics of protease inhibitors |
Helpful in patients with emphysema caused by alpha 1 anti-trypsin deficiency Side effects- anaphylaxis and low grade fever (especially in patients with IGA deficiency |
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What do tralokinab and lebrikizumab do |
Anti IL-13 IL-13 is produced by Th2 cells and activates eosinophils and mast cells in the allergic response |
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What are mepoluzimab and omalizumab do |
Anti IL-5 ANTI-IgE |
