PBL Flashcards
Name the 4 types of bronchodilators
- Beta 2 adrenergic receptor agonists
- theophylline
- muscarinic receptor antagonists
- leukotriene receptor antagonists
what are the types of beta 2 adrenergic receptor agonists? and give examples
- Short-acting - salbutamol
- longer acting - salmeterol
- ultra-long acting
what type of receptor is the beta 2 adrenoreceptor and what is its activation cascade?
G protein coupled receptors -
binding of an agonist causes the recruitment of adenylate cyclase which converts ATP to cAMP, this activates PKA.
PKAa will cause downstream protein phosphorylation causing muscle relaxation
What are the common side effects of salbutamol?
tremor and tachycardia - due to the receptors in heart and skeletal muscle
What two features characterise asthma what what does this result in?
characterised by: 1. inflammation in the airways 2. hyper-reactivity of the bronchioles, e.g. to irritant chemicals, cold air, stimulant drugs etc. Results in: 1. bronchoconstriction 2. mucus production
Describe the development of asthma
IgE mediated gypersensitivity reaction. IgE made by plasma cells coat the surface of mast cells. presentation of an antigen to these mast cells causes cross linking of 2 IgE receptors leading to degranulation
What is the mechanism of action of theophylline?
phosphodiesterase inhibitor. Phosphodesterase will convert cAMP to AMP. blocking this coversion will increase intracellular cAMP this in tern will activate more PKA causing downstream protein phosphorylation and therefore muscle relaxation
what is the mechanism of action of muscarinic receptor antagonists?
competetive inhibition of ach receptors on smooth muscle cells. means fewer muscarininc receptors are activated, and smooth muscle stays relaxed and airways remain open
what is the definition of potency?
the concentration of a drug that it takes to cause a particular effect
what is the definition of affinity?
how tightly something binds
what is the definition of efficacy?
the magnitude of the effect a drug can achieve at saturation
what is psycho-somatic?
relating to the interaction of mind and body
what is the brain region involved in pattern generation in breathing
pre-botsinger
also involved ventral and dorsal and pontine
what are the sensory inputs that control breathing?
chemoreceptors
lungs and airways
chest wall
where are the peripheral chemoreceptors located and what do they primarily sense?
carotid bodies and aortic arch - primarily sensitive to decreases in the partial pressure of oxygen, however also sensitive to changes in pH and CO2