Pharmacology (intro & pharmacodynamics)

a drug is a chemical … of known structure other than a … or an essential … ingredient, which, when … to a living organism, produces a … effect

substance, nutrient, dietary, administered, biological

a medicine is a chemical … which usually contains one or more … and is … to a living organism with the intention of producing a … effect

preparation, drugs, administered, therapeutic

drugs have to be … and not … and they may be … or obtained from … or … or can be products of … …

administered, endogenous, synthetic, plants or animals, genetic engineering

medicines usually contain other substances besides the active drug such as …, … and … to make them more convenient to use

excipients, stabilisers and solvents

drug molecules must exert … … on one or more cell … in order to produce a … response

chemical influence, constituents, pharmacological

drug molecules must get so … to cell constituents that the two interact … in such a way that the … of the cell constituent is altered

close, chemically, function

what is the study of what the drug does to the body called?

pharmacodynamics

what is the study of what the body does to the drug called?

pharmacokinetics

pharmacodynamics refer to the physiological and biochemical process of … … … of drugs

mechanism of action

pharmacokinetics refer to the changes in … of a drug through physiological processes

concentration

affinity is the strength of … between ligand and receptor

association

efficacy is the ability of an … to invoke a cellular …

agonist, response

if the dissociation rate is fast is the affinity high or low?

if the dissociation rate is slow is the affinity high or low?

low

high

4 main types of drug targets

1. receptors

2. enzymes

3. carrier molecules

4. ion channels

receptor is used to denote any protein molecule whose function is to … and … to … chemical signals

recognise and respond, endogenous

most receptors are functionally … in absence of the … mediator or …

silent, endogenous, drug

activation of a receptor alters the receptor’s … towards the cell and elicits a … response through … signalling or … changes

behaviour, tissue, transmembrane, intracellular

agonists bind to and … the receptor or increase the … of the … ligand to do so

activate, ability, endogenous

antagonists bind the receptor without causing … and … the effect of agonists

activation, block

affinity is the … of a drug to … to the receptor

tendency, bind

efficacy is the … of a drug to … the receptor

tendency, activate

name for agonists which possess 100% efficacy

full agonists

name for agonists which posess intermediate levels of efficacy

partial agonists

agonists possess both … and …

affinity and efficacy

antagonists possess … but not …

affinity, efficacy

specific binding = … binding - … binding

total, nonspecific

to get specific binding we perform the radioligand binding study in presence of a … concentration of ligand (without …) which prevents drug binding

saturating, radioligand

Bmax is the … … which tells you the maximum amount of … that are bound by the …

maximum binding, receptors, drug

the plateau at Bmax on a concentration vs specific binding plot tells you that …

there are no more receptors left to bind

radioligand binding study

1. step 1: … samples of tissue with increasing … of radioactive drug until … is reached (i.e. when the rates of … and … of radioactive drug are equal)

2. step 2: remove … (leave behind only tissue and … …)

3. put remaining radiolabelled tissue in … fluid

4. read amount of radioactivity in tissue which gives the … binding

1. incubate, concentrations, equilibrium, association and dissociation

2. supernatant, bound radioactivity

3. scintillation

4. total

use the log scale for the … to produce a graph from which Kd can be read - Kd is the … … which is the … of drug at which half of the … are bound and at which half of … is reached

concentration, dissociation constant, concentration, receptors, Bmax

Kd is used to measure drug … and the lower the Kd the … the affinity

affinity, higher

to get the bidning curve graph we plot … … vs … … against eachother

receptor occupancy, drug concentration

the binding curve defines the relationship between drug … and the amount of drug …

concentration, bound

the binding curve allows for estimations of drug …, … … (Bmax) and … …

affinity, binding capacity and dissociation constant

a dose-response curve plots the amount of a substance … (the dose) against the … or … effect, whereas a concentration-effect curve plots the … … of the substance at the … site or in a fluid (such as … … or a cell … …) against the resulting effect

administered, biological or clinical, actual concentration, target, blood plasma, culture medium

the dose-response and concentration-effect curves are used to measure …

efficacy

the dose-response curve is done in … and the concentration-effect curve is done in …

vivo, vitro

the dose-response and concentration-effect curves let us estimate the … … (Emax) that a drug can produce, and … or …

maximal response, EC50 or ED50

ED50/EC50 measure the amount of drug needed to reach half of the … … (Emax) which is called potency

maximal response

the lower the EC50/ED50 the … the potency

higher

EC50 is the … of a drug or ligand that produces 50% of its maximum possible … …

ED50 is the … of a drug required to produce the desired … effect in 50% of a tested population

concentration, biological response

dose, therapeutic

applying a log to the drug concentration transforms the graph from a … to a … curve

hyperbola, sigmoidal

in this graph both A and B are … agonists because they both reach … at a high enough concentration meaning they have the same … however they have different … because the EC50 or A is … than that of B

full, Emax, efficacy, potency, lower

from this curve we can see A is a more … agonist that B but has equal …

potent, efficacy

for a drug to be useful it must show a high degree of binding site …

specificity

protein drug targets also generally show a high degree of … … meaning they bind only molecules of a certain precise type

ligand specificity

TCAs (… …) block … … but produce side effects due to ability to block various other receptors such as … and … receptors producing … … and … respectively as side effects

tricyclic antidepressants, monoamine transporters, muscarinic and histamine, dry mouth and drowsiness

TCAs work as antidepressants by blocking reuptake of … neurotransmitters like … and …

monoamine, serotonin and norepinephrine

generally the lower the … of a drug and the higher the … needed to produce an effect of interest the more likely that … … sites of action will assume significance and produce side effects

potency, dose, off target