Lectures 6-10 Flashcards
What would a peak using the patch clamp technique represent?
open state receptors
What are inverse agonists?
The show affinity but negative efficacy
What are GABA(A) receptors?
ligand gated Cl- channels in the brain
What is benzodiazepine?
GABA(A) agonist
It increases the affinity of the GABA binding site for GABA
It hence increases openings
What is the significance of Glutamate-gated chloride receptors?
They’re common in the nervous system
They’re targeted by anti-parasitic drugs
What are competitive antagonists?
What effect do they have?
They bind reversibly at the site of the natural agonist
They produce a parallel shift to the right of the agonist dose
What is important about an SERD’s structure?
It reflects oestrogen’s structure
What is fulvestrant?
A selective oestrogen receptor degrader
What is the difference between biosimilars and generics?
Biosimilars are modelled after drugs using living organisms, where generics are synthetic drugs
Give three examples of drugs that use physio-chemical properties
General anaesthetics
Laxatives
Osmotic diuretics
Define drug potency
drug activity expressed in terms of the amount required to produce an effect of given intensity
What are cardiomyocytes used for?
Decreasing blood pressure
What is the therapeutic window?
the region between the toxic and effective drug concentrations
What is AVD?
Apparent Volume of Distribution
The volume of fluid to dilute the absorbed dose to the concentration found in plasma
AVD = dose/[plasma]
What is thiopentone
A short acting barbiturate, causing unconsciousness within 30-40 seconds
What are the stages of biotransformation?
1 - oxidation using cytochrome p450 transmembrane enzymes in the ER to form -OH groups
2 - conjugation (forms small soluble molecules)
What is a prodrug?
A drug with active metabolites