Drugs part 2 Flashcards
Structure of adrenoceptors
G protein coupled receptors
single polypeptide chain, 7 transmembrane alpha helices
alpha 1 adrenoceptor
binds to noradrenaline
Gq associated
alpha subunit dissociates and binds to phospholipase C
generates IP3 and DAG
IP3 binds to receptor on ER, causes calcium release
DAG activates PKC
Alpha 2 adrenoceptor
Gi protein (inhibitory)
alpha subunit inhibits to adenylyl cyclase
decreased PKA
beta 1,2 and 3 adrenoceptors
Noradrenaline
Gs protein
stimulates adenylyl cyclase
increased PKA
Where are beta 1 adrenoceptors found and what do they do?
Heart
increase heart rate, conduction velocity and increased contraction
What do beta 2 adrenoceptors cause?
dilation of blood vessls and bronchi
ciliary muscle relaxation
Which adrenoceptors cause blood vessel constriction?
Alpha 1 and 2
When can dobutamine be used as an adrenoceptor agonist?
beta 1 receptor agonist
heart failure, heart block
What are the differences between nicotinic and muscarinic AChRs?
Nicotinic receptors are ionotropic - acts as a channel for positively charged ions (sodium) to flow to cause depolarisation, all are excitatory
Muscarinic receptors are G protein coupled receptors, can be excitatory or inhibitory
M1 Muscarinic receptors
neural, including ganlia in stomach
IP3 pathway
M2 muscarinic receptors
cardiac
inhibits cAMP pathway
M3 muscarinic receptors
smooth muscle
increases IP3 stimulation
clinical uses of antimuscarinic drugs
asthma
bradycardia
to decrease gut motility
urinary incontinence
Drugs for GORD (supression of acid)
proton pump inhibitors (omeprazole)
H2 blockers - blockers histimine which stimulates acid secretion
Antacids increase pH
alginates form a physical barrier
What is helicobacter pylori and what can it cause?
gram negative bacteria
peptic ulcers disease - gastritis
hypergastrinaemia - increases gastrin release and decrease somatostatin release