Pharmacology 1, 2 and 3 - Intro to drug action, drug movement in the body, elimination Flashcards
What are the 2 compromises of pharmacology and what do they mean?
Pharmacodynamics - what a drug does to the body (biological effects and mechanisms of action)Pharmacokinetics - what the body does to a drug (absorption, distribution, metabolism and excretion)
What selectively of drugs result from?
chemical structure of drugTarget recognising only ligands of a precise type
Examples of targets of drugs? (5)
enzymes, carrier molecule, ion channels, receptors, RNA/DNA
What are receptors?
Macromolecules that mediate the biological actions of hormones and neurotransmitters
2 types of drugs acting on receptors and meaning?
Agonists - a drug that binds to a receptor and produces a cell responseAntagonists - a drug that blocks the actions of agonists
What is a ligand?
A molecule that binds to a receptor
Out of affinity and efficacy, what does an agonist and antagonist posses?
Agonist = affinity and efficacyAntagonist = affinity
How does an agonist work?
A conformational change occurs due to the presence of an agonist molecule making it act and therefore producing a biological response
Affinity?
Strength of association between ligands and receptor
Dissociation rate compared to affinity
Low affinity = high dissociation rate
What are the 2 things that determine affinity
Closer the fitNumber of bonds
Efficacy?
Ability of agonist to provoke a cellular response
Low efficacy?
Low ability to produce a cellular response
Relationship between receptor occupancy and agonist concentration?
As agonist conc. increases, receptor occupancy also increases
EC50?
Concentration of agonist which elicits a half maximal response
Concentration (or dose) response relationship - linear plot - relationship shape
Hyperbolic
Why is it easier to plot the concentration response relationship as the log of the agonist concentration?
It allows you to present data over a wider range of concentrations It is easier to see the max70% of the curve is a straight line
What shape is the response when the concentration response relationship is plotted as a semi-logarithmic plot?
Sigmoidal
What can a highly potent drug do?
Evoke a larger response at lower concentrations
What are partial agonists
Drugs that bind to receptors but only have partial efficacy meaning they cannot evoke the same response as a full agonist
Competitive antagonism?
Binding of agonist and antagonist occur at same (orthosteric) site
Non-competitive antagonism
Agonist binds to orthosteric site and antagonist binds to allosteric site (activation cannot occur if antagonist is bound)
Drug disposition?
The fate of drugs in the body
Determinants of drug disposition
AdsorptionDistributionMetabolismExcretion
Adsorption?
The process by which a drug enters the body from its site of administration
Distribution
The process by which the drug leaves the circulation and enters the tissues perfused by the blood (once inside the tissue, further blood-independant distribution may occur)
Metabolism
The process by which tissue enzymes (particularly in the liver-hepatic metabolism) catalyse the chemical conversion of a drug to a more polar form that is more readily excreted by the body
Excretion
The process that removes the drug from the body (principally the kidneys - renal exertion)
Aside from the liver, where does metabolism also occur?
GI tract and lungs
Aside from the kidneys, where does excretion also occur?
Breath, sweat and milk
What is elimination (sum)?
metabolism + excretion
Where does most absorption occur?
in the Small intestines (due to large SA)
Where is ethanol absorbed
The stomach
name for when unchanged drugs leave the body via the faeces?
Egestion
3 physiochemical factors controlling drug absorption
Solubility (drug must be dissolved to be absorbed)Chemical stability (some drugs are destroyed by the stomach acid or enzymes in the GI tract)Lipid to water partition coefficient (rate of diffusion increases with lipid solubility of drug)
What does ampithatic mean?
Has both polar and non polar parts (drugs must be ampithatic)
In terms of weak/ strong acids/bases, what are many drugs
Weak acids and bases existing in both the ionised and unionised forms