Respiratory pharmacology - including asthma and COPD. Based on Rang and Dale Pharmacology.
Muscarinic receptors which facilitate ACh transmission on nicotinic receptors, localised in the bronchial ganglia post-synaptic cells
Inhibitory autoreceptors, which mediate negative feedback effects on ACh release by postganglionic cholinergic nerves
Mediate contraction of brachial smooth muscle and secretion of glands
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Montelucast
Zafirlukast
Salbutamol
Theophylline
Enprophylline
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Spontaneous rhythmic discharges from the respiratory centre of the medulla
Spontaneous rhythmic discharges from the respiratory centre of the cerebellum
Continual stimulation from the pons
Continual stimulation from the medulla
Spasmodic stimulation from the motor region
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B2-adrenoceptor agonists - theophylline - muscarinic receptor agonists - cysteinyl-leukotriene receptor antagonists
Cysteinyl-leukotriene receptor antagonists - B2 adrenoceptor agonists - theophylline - muscarinic receptor agonists
B2-adrenoceptor agonists - theophylline / muscarinic receptor agonists - cysteinyl-leukotriene receptor antagonists
Theophylline - muscarinic receptor agonists - B2 adrenoceptor agonists - cysteinyl-leukotriene receptor antagonists
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Metered-dose inhaler, with boosts of oral glucorticoids if severe or rapidly deteriorating
Orally, with boosts of inhaled glucorticoids if severe or rapidly deteriorating
Metered-dose inhaler
Orally
IV infusion
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Muscarinic receptors which facilitate ACh transmission on nicotinic receptors, localised in the bronchial ganglia post-synaptic cells
Inhibitory autoreceptors, which mediate negative feedback effects on ACh release by postganglionic cholinergic nerves
Mediate contraction of brachial smooth muscle and secretion of glands
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Beclometasone dipropionate
Budesonide
Fluticaone propionate
Salbutamol
Theophylline
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Unclear. Believed part is due to the inhibition of phosphdiesterase isoenzymes, which increase cAMP.
Unclear. Believed to be due to an action at the Beta adrenoceptors
Decreases the level of circulating adrenaline.
Side effects: nausea, vomiting, anorexia, nervousness, tremour, dysrhythmia in high concentrations, seizures at slightly above normal range.
Side effects: excessive somnolence, fatigue and lethargy, lack of concentration, pigmentation of the skin and bradycardia.
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Ipratropium
Oxitropium
Salbutamol
Theophylline
Zafirlukast
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Muscarinic receptors which facilitate ACh transmission on nicotinic receptors, localised in the bronchial ganglia post-synaptic cells
Inhibitory autoreceptors, which mediate negative feedback effects on ACh release by postganglionic cholinergic nerves
Mediate contraction of brachial smooth muscle and secretion of glands
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Noradrenaline
Excitatory peptides
Nitric Oxide (NO)
Adrenaline
Acetylcholine
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It depresses the exaggerated neuronal reflexes - ie. it suppresses the response of senxory C fibres to capsaicin irritant and may inhibit the release of preformed T cell cytokines
It binds to B2 adrenoceptor molecules and causes sustained agonist action
It suppresses the release of inflammatory cytokines from mast cells
It decreases circulating adrenaline
It blocks parasympathetic innervation
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PCO2 at the medullary chemoreceptors
PO2 at the aortic and carotid bodies
PCO2 at the aortic body
PCO2 at the aortic and carotid body
PO2 at the carotid body
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Decreased FEV1
Decreased VC
Cough
Wheeze
Difficulty breathing out
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Spirometry FEV1
Peak expiratory flow meter
Spirometry VC
Spirometry RC
Bronchodilator spirometry
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Circulating adrenaline
Sympathetic nerve stimulation
Circulating acetylcholine
Parasympathetic nerve stimulation
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B2 adrenoceptor agonists
Cysteinyl-leukotriene receptor antagonists
Muscarinic receptor agonists
Muscarinic receptor antagonists
Xanthines
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Codeine
Dextromethorphan
Pholcodeine
Morphine
Salbutamol
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On the mast cells
In the airways
In the epithelium
On the glands
In the alveoli
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Relax bronchial constriction caused by parasympathetic stimulation
Increases bronchial constriction caused by sympathetic stimulation
Inhibits augmentation of mucous secretion
Increases augmentation of mucous secretion
Increases the mucocillary clearance of bronchial secretions
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A syndrome of chronic bronchitis and emphysema
Chronic bronchitis: inflammation of the bronchi and bronchioles due to cigarette smoke or air pollution.
A syndrome of cough, then productive cough, then wheezing and breathlessness due to airflow limitation
Emphysema: distension and damage of lung tissue beyond the respiratory bronchioles (bronchiectasis)
Sudden-onset cough, relieved by bronchodilators
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Blood vessels (causing constriction)
Glands (inhibiting secretion)
Glands (increasing secretion)
Blood vessels (causing dilation)
Adrenal gland causing increased circulating adrenaline affecting smooth muscle in the lungs
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Orally
Inhalation
IV
Act on the cysteinyl-leukotriene receptors, causing bronchodilatation, and preventing aspirin-sensitive and exercise-induced asthma and reducing sputum eosinophilia
Act on the cysteinyl-leukotriene receptors, causing bronchodilatation, and decreasing allergenic reactivity by acting on the irritant receptors
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Causes bronchoconstriction
Causes bronchodilation
Causes increased secretion of glands
Causes increased respiratory rate
Causes decreased respiratory rate
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Salbutamol
Formoterol
Terbutaline
Salmeterol
Bambuterol
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Anti-asthmatic bronchodilation
Increased alertness, tremor and nervousness
Affect sleep and increase respiratory rate
Increase heart rate and vasodilatation
Weak diuretic effect
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Oropharyngeal candidiasis
Dysphonia
Adrenal suppression with regular large doses
Cushing syndrome in oral Rx
Cardiac arrhythmias
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Excitatory neuropeptides - eg. substance P and neurokinin A
Nitric Oxide (NO)
Adrenaline
Released from Sensory C fibres
Released from irritant receptors
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Salmeterol
Formoterol
Fenoterol
Pirbuterol
Reprotelol
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Main benefit: few unwanted side effects and is generally safe and well tolerated.
Main benefit: quick effects, causing rapid bronchodilatation and relief of symptoms
Used as an adjunct to B2-adrenoceptor antagonists and steroids
Used as a primary treatment for severe asthma
Used as a second-line therapy with B2 adrenoceptor antagonists
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Given prophylactically
Allergen-induced, exercise induced and irritant induced asthma
In those patients who respond (is not possible to predict who will, but more commonly children)
cold-air induced, drug induced asthma
Useful in all asthmatics, in acute bronchospasm
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Pontine CNS centre
Vagal afferents from the lungs
Chemoreceptors on aortic and carotid bodies
Medullary chemoreceptors
Motor area
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Decrease the formation of cytokines, in particular the Th2 cytokines and decrease eosinophilic recruitment and activation
Decrease IgE production and IgE receptor expression and inhibit vasodilatation by suppressing PGE2 and PGI2 though induction of COX-2
Decrease spasmogens LTC4 and LTD4, decrease chemotactins LTB4 and platelet activating factor and therefore decreasing recruitment and activation of inflam cells
Can upregulate B2 adrenoceptors and decrease mediator release from eosinophils
Long term Rx reduces the early phase response to allergens and prevents exercise-induced asthma
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An ill-defined effect on the brainstem, suppressing the 'cough centre'
Inhibit release of excitatory neuropeptides through action on mew receptors on sensory nerves in the bronchi
Decreasing nerve conduction from the 'cough centre' to the motor centre of the brain
Decreasing the ability of nerves in the respiratory system to respond to stimuli
Paralysing the abdominal muscles and accessory muscles of respiration
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In the alveoli
In the airways
On mast cells
In the epithelium
In smooth muscle
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Ipratropium bromide
Salbutamol
Oral prednisolone
Beclometasone dipropionate, budesonide and fluticasone propionate
Theophylline
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Slowly adapting stretch receptors
Adrenoceptors
Unmyelinated senory C fibres
Muscarinic receptors
Rapidly adapting irritant receptors associated with myelinated vagal fibres
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B2 receptors of the smooth muscle
B2 receptors of the alveoli
B2 receptors of the vasculature
Decreasing mediator release from mast cells
Increasing mucous clearance in the cilia
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