Anti-Asthma Drugs Flashcards
what do chemokine do in mast cells
attract inflammatory mediators to the area
what are the types of bronchodilators
beta2 adrenergic receptor agonists
theophylline
muscarinic receptor antagonists
leukotriene receptor antagonists
where are beta2 receptor also found apart from on smooth muscle cells
mucous glands in the bronchiole wall and on ciliated epithelial cells that line the lumen of the bronchioles - stimulates mucus secretion and increases the beat frequency of cilia which together increases mucucillary clearance
what kind of receptors are beta2 adrenergic receptors
G protein coupled receptors
what are G protein coupled receptors mediated by
signalling cascades that are activated downstream of aGTP binding protein (G protein)
what is the G protein involved in the beta2 adrenergic receptor mechanism
the Gs protein
what enzyme does the Gs protein activate
adenylate cyclase
what are the natural agonists of the beta2 receptors
noradrenaline released from sympathetic nerve terminals or adrenaline
what does the endogenous agonist binding to the receptor site cause
a conformational change in the receptor protein
what does adenylate cyclase catalyse
the conversion of ATP into the second messenger, cAMP
what does cAMP bind to
protein kinase A causing it to be activated
what does protein kinase A do
phosphorylates several proteins that promote the relaxation of smooth muscle
what is the enzyme that metabolises cAMP called
phosphodiesterase which hydrolyses phosphodiester bonds to generate cAMP
how can the activity of phosphodiester be blocked
drugs known as phospohodiester inhibitors, resulting in an elevation of cAMP levels and stimulation of downstream events in the pathway
what is an example of a phosphodiesterase inhibitor
theophylline
how does a beta2 adrenergic antagonist work
when the beta blocker is bound to the receptor it does not interact with the Gs protein and stimulate the signalling cascade. compete with the beta2 agonist for binding to the receptor site and when they are bound they prevent the agonist from binding and having an effect.
examples of SABA
salbutamol and terbutaline
how long do SABA drugs work for
3-5 hours
how often do you use SABA
as needed
examples of LABA
salmeterol and formoterol
how long do LABA work for
8-12 hours
how often are LABA given
twice daily
examples of Ultra LABA
vilanterol and indacaterol
how long to ultraLABA work for
around 24 hours
how often are ultraALABA used for
once daily
what drugs can be combined with a corticosteroid
ultra LABAs
side effects of beta2 agonists
tremor caused by activation of the skeletal muscles
rise to headaches
lowers blood pressure and triggers a reflex tachycardia
what is aminophylline made by
combining theophylline with ethylene diamine and is more water soluble and used when the drug is given intravenously
what is theophylline
a phosphodiesterase inhibitor
what is adenosine
produced in all cells as the final product of ATP
extracellular conc is highly regulated but can be increased dramatically when the energy demand of a cell increases in cases such as inflammation
In the long term thought to contribute to athsma