Resp Flashcards
What are bronchodilators
Medications which relieve bronchoconstriction caused by conditions that affect air passageways and alveoli.
Alpha and beta adrenoceptors and muscarinic acetylcholine receptors (mAChRs) are…
G-protein coupled receptors
Alpha1 affect
Blood vessels, gut, liver, bladder, sweat glands, iris
Alpha2 affect
Presynaptically on all adrenergic nerve terminals, post-pancreas
Beta1 affect
Heart muscle, gut, juxtaglomerular apparatus
Beta2 affect
Bronchioles, skeletal muscle, pancreas, mast cells, liver, uterus
Beta3 affect
Adipose tissue, heart
Alpha1 receptors activate:
Phospholipase C (PLC) producing inositol trisphosphate (IP3) and diacylglycerol (DAG)
Alpha2 receptors inhibit
Adenylate cyclase thus decreasing cyclic adenosine monophosphate (cAMP)
All subtypes of beta receptors stimulate…
Adenylate cyclase thus increasing cAMP
Alpha1 receptor activation results in
Vasoconstriction, pupil dilation, decreasing peristalsis and decreasing voiding, sweating, hepatic glycogenolysis
Alpha2 receptor activation results in
Autoinhibition of transmitter release (NA and acetylcholine receptor release from autonomic nerves)
Beta1 receptor activation results in
Increased cardiac rate and force, relaxation of GI smooth muscle (decreasing peristalsis), renin release and lipolysis
Beta2 receptor activation results in
Bronchodilation, vasodilation, relaxation of uterine smooth muscle, hepatic glycogenolysis, increased insulin secretion, fine muscle tremor
Beta3 receptor activation results in
Lipolysis
Selective alpha1 agonists
Phenylephrine and oxymetazoline
Selective alpha2 agonists
Clonidine
Selective beta1 agonists
Dobutamine
Selective beta2 agonists
Salbutamol, formoterol, terbutaline and salmeterol used mainly in asthma
The drug class of choice for an immediate phase asthmatic attack and what does it do?
Beta2 adrenoceptor agonist- dilate the bronchi by a direct action on the beta2 adrenoceptors in the bronchial smooth muscle causing relaxation
What do beta2 adrenoceptor agonists inhibit
Inhibit mediator release from mast cells and decrease mucus production
What are the main short-acting drugs in the beta2 adrenoceptor agonist class?
Salbutamol and terbutaline
How are salbutamol and terbutaline administered?
Typically administered by inhalation (aerosol, powder, nebuliser) but can be given by IV in severe attacks
Characteristics of salbutamol and terbutaline:
Rapid onset of action, within a few minutes; effect lasts for 3-5 hours