Drug - Receptor Interactions Flashcards
What is a drug
Chemical substance that interacts with a biological system to create a physiological effect
Drug target sites (4)
Receptors, Ion channels, transport systems, enzymes
What is a receptor
Proteins within the cell membrane
Activated by neurotransmitters/hormones
Defined by agonists & antagonists
Examples of agonist and antagonist drugs targeting receptors
Agonist = acetylcholine
Antagonist = atropine
What is an ion channel
Selective pores allowing ion transfer down the electrochemical gradient
Either voltage sensitive or receptor linked
Examples of drugs targeting ion channels
Calcium channel blockers + LAs
Examples of ion channels
Voltage sensitive = VSCC
Receptor linked = nAChR
What are transport systems
Work against concentration gradients (glucose, ions and NTs) Specificity for certain species
Examples of transport systems
Na+/K+ ATPase
NA ‘uptake 1’
Examples of drugs targeting transport systems
Tricyclic anti-depressants (TCAs)
Cardiac glycosides
What are enzymes
Catalytic proteins that increase rate of reaction
Examples of drugs targeting enzymes/ classes
Enzyme inhibitors = anticholinesterase (neostigmine)
False substrates = methyldopa
Prodrugs = Chloral hydrate (trichloroethanol)
State none specific drug action
Physiochemical properties
> Antacids/osmotic purgatives (↑ water in stool)
Plasma protein binding
How do osmotic purgatives work
Draw water into the stool in order to make it softer
What does the potency of a drug depend on
Affinity (forces involved in the binding of the drug) and Efficacy (activation of the receptor/Intrinsic activity) = conformational change of the receptor