Block A Lecture 2: Where do Drugs Act? Flashcards
What are the top 2 receptor types which are targets for drugs?
G protein-coupled receptors (GPCRs) - 30%
Nuclear hormone receptors - 4%
(Lecture 2, Part 1, Slide 3)
What do agonists and antagonists do to cell activity?
An agonist enhances cellular activity whereas an antagonist blocks cellular activity
(Lecture 2, Part 1, Slide 5)
How can new drugs often be made?
By tweaking the structure of already existing drugs to try improve on their pharmacological properties
(Lecture 2, Part 1, Slide 7)
Is salbutamol an agonist or antagonist?
Agonist (beta-2 adrenergic receptor)
(Lecture 2, Part 1, Slide 8)
What is the first step of salbutamol’s mechanism of action to combat asthma?
Salbutamol activates ß-2 adrenergic receptors in the smooth muscle of bronchioles in the lung
(Lecture 2, Part 1, Slide 8)
What happens in salbutamol’s mechanism of action after it activates ß-2 adrenergic receptors in the smooth muscle of bronchioles?
ß-2 adrenergic receptors, activate the enzyme adenylyl cyclase
(Lecture 2, Part 1, Slide 8)
What happens in salbutamol’s mechanism of action after ß-2 adrenergic receptors activates the adenylyl cyclase?
It converts ATP into cyclic adenosine monophosphate (cAMP)
(Lecture 2, Part 1, Slide 8)
What happens in salbutamol’s mechanism of action after adenylyl cyclase converts ATP into cyclic adenosine monophosphate (cAMP)?
cAMP inhibits calcium release, resulting in smooth muscle relaxation
(Lecture 2, Part 1, Slide 8)
Are anti-histamines antagonists or agonists?
Antagonists
(Lecture 2, Part 1, Slide 11)
What are anti-histamines antagonists for?
Histamine H1 receptors
(Lecture 2, Part 1, Slide 11)
What do antihistamines treat?
Allergic reactions
(Lecture 2, Part 1, Slide 14)
Are drugs mainly agonists or antagonists?
Antagonists
(Lecture 2, Part 1, Slide 15)
What are beta blockers antagonists for?
Beta 1 receptors
(Lecture 2, Part 1, Slide 15)
What are beta blockers used to treat?
Heart arrythmias (irregular heart beat)
(Lecture 2, Part 1, Slide 15)
What do antagonists of histamine H2 receptors treat?
Stomach ulcers
(Lecture 2, Part 1, Slide 15)
What do antagonists of angiotensin II receptors treat?
High blood pressure (by lowering it)
(Lecture 2, Part 1, Slide 15)
What do antagonists of purinergic (P2y12) receptors on platelets treat and how?
Heart attacks - by inhibiting platelet aggregation
(Lecture 2, Part 1, Slide 15)
Is the contraceptive pill an agonist or antagonist?
Agonist
(Lecture 2, Part 1, Slide 16)
What type of drug is aspirin?
An enzyme inhibitor
(Lecture 2, Part 2, Slide 5)
What is the full chemical name of aspirin?
Acetyl Salicylic Acid
(Lecture 2, Part 2, Slide 6)
What does aspirin inhibit?
It inhibits both isoforms of the cyclo-oxygenase inhibitor (COX inhibitor), COX-1 and COX-2
(Lecture 2, Part 2, Slide 7)
What is the cyclo-oxygenase inhibitor responsible for?
Converting arachidonic acid into TXA2 and PGE 2 prostaglandins
(Lecture 2, Part 2, Slide 7)
What is PGE2?
A prostaglandin involved in inflammation
(Lecture 2, Part 2, Slide 9)
What mediates the creation of PGE2?
COX-2
(Lecture 2, Part 2, Slide 9)