block a lecture 2 Flashcards
where do drugs act
what drug has a similar structure to adrenaline
salbutamol
what receptor does salbutamol work on
smooth muscle receptors
(beta 2 receptor)
what does salbutamol interact with once activating beta 2 receptor
GCPR
what response occurs after salbutamol activated receptor and interacts with GCPR
converts ATP into cAMP causing inhibition of calcium
what does the inhibition of calcium do
relaxation of the airways allowing more air into lungs
what type of agonist is salbutamol
b2 selective agonist for the. receptor
what type of antagonists are antihistamines
histamine H1 antagonist
how is histamine released during hay fever
T cell hypersensitivity (Th2)
too much IgE produced
IgE interacts with receptor on mast cells
promoting release of histamine stored in granules
driving inflamm response
mechanism of action of mepyramine
H1 blockers
needs to be selective for H1 (GCPR directed)
what type of antagonists used for heart arrythmias
beta blockers
(b1 antagonists)
what type of antagonists used for treatment of stomach ulcers
antagonists of histamine H2 receptors
what type of antagonists used to lower blood pressure
antagonists of angiotensin II receptor
what type of antagonists used for heart attacks (inhibits platelet aggregation)
antagonist of purinergic (P2Y12) receptor on platelets
example of a steroid hormone receptor drug
the pill
oestrogen and progesterone analogues (agonists)
what receptor is the pill directed at
nuclear receptors
what is an enzyme
proteins which drive chemical reactions inside the cell
essential for cell function
name of the acid that is aspirin
acetyl salicylic acid
who discovered/synthesised aspirin and when
1897 felix hoffman
what is a cox inhibitor
cyclo-oxygenase inhibitor
how does aspirin work as a COX inhibitor
takes arachidonic acid into catalytic site and oxidases it
converted into PGH2 volatile, then into TXA2 and PGE2
aspirin gets into site and acetyl serine residues and cyclooxigenates preventing formation of TXA2 and PGE2
what is PGE2
prostaglandin
involved in inflammation
mediated by COX-2
what is TXA2
thromboxane A2
prostaglandin like product
involved in platelet aggregation during clotting
mediated by COX-1
what dosage of aspirin for inflammation, period pain, headaches etc
300mg
how does low dose aspirin work in the prevention of secondary heart attacks
inhibiting COX-1 in platelets
not a statin
dosage of aspirin when using for prevention of secondary heart attacks
75mg
what is an ACE inhibitor
angiotensin converting enzyme inhibitor
what system is ACE a part of
renin angiotensin system
what is angiotensin II
a peptide
what does ACE do
convert ang I to ang II
ang II works on GCPR
what was the venom of brazilian pit viper found to do
reduce blood pressure
pharm companies made non peptide analogues of the venom, why was this
cannot make peptide drugs as they would be broken down in the liver
ACE inhibitors as medication
blood pressure meds
prevents angiotensin II being formed
less vasoconstriction= lower blood pressure
ACE inhibitors as medication
blood pressure meds
prevents angiotensin II being formed
less vasoconstriction= lower blood pressure
what do statins do
lower cholesterol and prevents heart attacks
what does sildenafil inhibit
inhibits the enzyme which breakdown cGMP- helps with erectile dysfunction (PDE5 inhibitor)
what does nevirapine inhibit and treat
non nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1
used to treat patients with HIV and AIDS
how does penicillin inhibit bacteria
kills bacteria through binding of the beta lactam ring to DD-transpeptidase
