enzymes and transporters Flashcards
What is an enzyme inhibitor
Molecule that binds to an enzyme and decreased it’s activity
What do statins do
Block the rate limiting step in the cholesterol pathway
Class of lipid lowering drug
Prevent CVD
How does RAAS increase blood pressure
Increase the amount of salt and water the body retains
What does inhibiting ACE do
Reduced Ang2 production and therefore causing a reduction in BP
Three main types of protein ports ?
Uniporters -
Symporters
Antiporters
How do uniporters work
Transport one specific type of solute down its conc gradient
How do symporters work
Use the movement in one of the molecules to pull in another molecule against a concentration gradient
What are barbiturates
Increase the permeability of the channel to chloride
Most potent inhibitor of acid secretion
Proton pump inhibitors
What are organophosphates
Irreversible inhibitors of cholinesterase
Two types of enzyme inhibitors and what they do
Irreversible - usually react with the enzyme and change it chemically
Reversible - bind non - covalently
How do anti porters work
One substance moves against its gradient using energy from the second substance moving down its gradient
Give an example of a symporter
Na-k-cl cotransporter moves na k and cl into cells
Moves ions in the same direction
What is the main enzyme involved in drug metabolism
Cytochrome p450
Example of ace inhibitor
Enalapril
Example of cox inhibitor
Aspirin and paracetamol
Example of b2 adrenoreceptor agonist
Salbutamol
What 3 ways can a receptor be sensitised
Uncoupled
Internalised
Degraded
How do diuretics work
They inhibit synporters in the loop of henle
This leads to increased h2o excretion and decreased salt reabsorption and so bp decreases
What enzyme catalyses phase 1 reactions
Cyp450
What is a phase 2 metabolism reaction
Conjugation and glucoronidation
They usually inactivate products and increase hydrophilicity for renal excretion
What happens in a phase 1 reaction
Non conjugation
Aim to increase hydrophilicity
With cyp450
Where would you find b2 receptors
Lungs
Where would you find alpha 1 receptors
Vessels and sphincters
