pharmacology Flashcards
what is a drug
this is a chemical that is used to prevent , diagnose, treat or cure pathological issues.
drug action
drug binding onto a molecule.
drug affinity
ability of a drug to bind onto a receptor and elicit a response
efficacy
ability of a drug to cause a response after binding onto a receptor.
factors that pharmacological effect depend on
affinity
efficacy
residence time
what is meant by residence time
total time spent by the drug on the receptor
factors that can influence receptor response
1.polymorphic variation - different people have different genes that code for the receptor proteins .
2.age -older people less receptors that are expressed.
3.disease
4.drug treatment for example clonidine is a drug for hypertension and addition of this molecule is seen as not balancing in homeostasis.
agonist receptors
they bind to the receptor and they cause a response
antagonists ligand
bind to the receptor and causes no activation
competitive ligand
competes with the other ligands for site for binding while the non - competitive changes the shape of the binding site.
pharmacodynamics
effects of the drug on a specific site
what is meant by pharmacokinetics
what the body does to the drug that is ADME
Biophase
the effect site of the drug (the physical region in which the
drug target is located)
bioavailability
this is the extent and rate at which the drug reaches its site of action
how is bioavailability measured
measured by injecting the drug in the systemic circulation through IV administration.
best routes of administration
IV
SC/IM
PR/PO
what is meant by half life of a drug
that is the time it takes to reach half it concentration in the blood.
methods of drug lost
through barriers that is why IV route is usually the best option .
bioavailability and the mode of administration
IV has the highest bioavailability because there is no loss of the drug
what is the benefit of a half life
adjustment of a dose
concentration max interpretation
too low means there is no therapeutic effect while too high means toxicity.
what is meant by therapeutic index
this is the ratio of the the dose that causes therapeutic effect to the dose that causes toxicity
narrow therapeutic index
prescription with care
very large therapeutic effect
not so many problems
movement of the drug from the plasma
-plasma to interstitial fluid
then to intracellular fluid which has to cross the cell membrane .
-sometimes has to cross other fluids such as CSF, peritoneal , humours etc.
movement of plasma to interstitial fluid
filtration
paracellular movement
filtration
transcellular movement
from the interstitial fluid to the intracellular
types of barriers to be crossed during drug penetration
passage through the basement membrane to the epithelial cell
types of movement that occur
movement by diffusion
facilitated diffusion
active transport
factors that affect movement of drugs into the cell
1.lipophilicity
2.ionisation
3.blood supply and perfusion.
4.size of a drug
5.existence of some transport mechanism.
6.
elimination of a drug
this refers to metabolism and excretion
body`s mechanism of preventing the exposure to alien molecules.
1.blood brain barrier
2.physical removal of a drug through urine, blood , sweat and breath.
3.characteristics that promote entry limit exit such as size , lipophilic or not etc.
metabolism are easily excreted than parent
metabolites render the drug more polar