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Pharmacodynamics & Pharmacokinetics, Transmembrane, No. Sub units,…
Pharmacodynamics & Pharmacokinetics
Drug Evaluation
Phase 2: drug tried on informed pt.
Phase 3: drug used in vast clinical market
Phase 1: chemicals tested on human volunteers
Phase 4: continual evaluation of the drug
Preclinical Trials: chemicals tested on lab animals
Pharmacokinetics
what the body does to the drug
PK determines the speed of onset, efficacy & duration of action of a drug
PK considerations:
onset of drug action,
duration of drug action (half-life)
timing of peak effect
metabolism or biotransformation of the drug
site of excretion
Route of Admin. influences ADME
Distribution
Metabolism (First Pass Effect): important to drugs given orally as they are metabolised by the liver
Absorption: movement of drug from site of admin into blood supply
Elimination
Bioavailability
% of administered drug that reaches systemic circulation. E.g. administer 100mg of a drug, 75mg entered systemic circulation/blood plasma, therefore bioavailability is 75% (75/100)
Half-Life
time it takes for the max. plasma conc. to reduce by 1/2. Measure on a graph using the max. point & point which conc. is 1/2 what you started with
PK assay amount of drug bound or response:
fractional response
conc. of drug
4 Target Proteins: Receptors, Ion channels, Enzymes, Carrier Proteins
Ion Channels
Blockers: drug sits in channel so nothing can move in/out
Modulators: modulates the ability of the drug to open/close the channel
Enzymes
Inhibitor: stops from making product
False Substrate: uses energy to make a diff. product
Pro-drug: not the active drug, piggy backs to get active drug as product
Receptor agonist; bind to & activates receptor brings about biological response
Receptor Antagonist: binds to receptors & prevents agonists binding, keeps receptor in inactive state
Log Dose Curves (LDRs)
test low conc. of drugs & compare to response, until they get a plateau/ 100% response.
Potency = EC50 (lower the EC50 more potent a drug is
Efficacy: max. effect @ plateau
Slope: indicates if small change in conc. brings about big diff. in response
ED50= dose of drug required to produce specified effect in 50% pop.
LD50= dose of drug producing toxic effect in 50% pop.
Therapeutic index= LD50/ED50
KLP
1
1
catalytic/kinase
NR
0
1
DNA binding
GPCR
7
1
g protein coupling
LGIC
4
4-5
channel pose
Pharmacodynamics
what the drug does to the body
Transmembrane
No. Sub units
Special Domain