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What is pharmacodynamics
Effect of drugs on the body
What is pharmacokinetics
what the body does to the drug
What are the 2 different classes of drugs
. Naturally occurring
. Synthetic
What does pharmacodynamics allow us to determine in terms of patients (3)
. Appropriate dosage range
. Compare efficacy
. Compare safety
What does the acronym ADME stand for in terms of pharmacokinetics
. Absorption
. Distribution
. Metabolism
. Excretion (of the drug in body)
What does pharmacokinetics allow us to do in terms of patients (2)
. Design and optimise treatment regimes
. Such as the route, frequency and duration
,What are the 4 types of considerations that must be made when designing a drug
. Hydrophobicity
. Ionisation of drug
. Conformation of target
. Stereochemistry of drug
What are nuclear receptors a type of
Intracellular receptors
What are the different classes of nuclear receptors and what distinguishes them
(3 defining characteristics)
. Class 1 - cytoplasm, ligands endocrine and homodimers
. Class 2 - nucleus, ligands lipids, heterodimer
Not all drugs need a recep some act viva psycho-chem properties
What are the 4 targets for drug action
receptors, ion channels, carrier molecules, enzymes
What is drugs interaction w target dependant on (2)
. Shape
. Charge distribution
Why is charge distribution important in terms of drug binding
. Too tightly binding could cause an irreversible binding which is bad
. Too loose of a binding causes a low affinity so drug doesn't really work and is bad
What do antagonists do
block receptors - usually inhibit action
What to agonists do?
, Can act as a pseudosubstrate - promote action usually
What are the two dose-response relationships
Graded and quantal
What is a graded dose-response relationship
describe the effect of various doses of a drug on a singular individual
What is a quantal dose-response relationship
show the effect of various doses of a drug on a population of individuals
used to calculate ED50, TD50, LD50
What do quantal dose response curves look like (visually)
A bell curve
Why are dose response curves used?
Allows estimation of Emax and allows the estimation of conc or dose required to
produce 50% of maximal dose
What does EC50 mean?
Concentration of drug that produces 50% of maximal response
What is efficacy?
maximal effect a drug can produce.
What is the potency of a drug?
The amount of a drug that must be given in order to produce a particular response
What does a lower Kd indicate
A tighter ligand-receptor interaction (higher affinity)
If one drug has a higher potency than another drug what differs