Principles Pharmacology Flashcards
Pharmacodynamics
What a drug does to the body.
Pharmacokinetics
What the body does to a drug.
Drug
Any synthetic, or natural, substance of known structure used in the treatment, prevention, or diagnosis of disease.
Medicine
A chemical preparation containing one, or more, drugs used with the intention of causing a therapeutic effect.
Agonists
Drugs that bind to a receptor to produce a cellular response.
Antagonists
Drugs that block the actions of an agonist by binding to the same receptor.
Affinity
Is the strength of association between the ligand and the receptor.
Efficacy
Is the ability of an agonist to produce a cellular response.
EC50
Is the concentration of a drug that produces 50% of the maximal effect. This tells us how potent the drug is.
LD50
The concentration of a drug that produces a lethal dose in 50% of the population.
Basal Activity
is the receptor activity that occurs even when there is no agonist around.
Inverse Agonist
Simply eliminates basal activity (binds to receptors and stabilises them).
Competitive Antagonism
When we have both agonist and antagonist and they bind to the same site on the receptor, they will compete for that side.
Non-Competitive Antagonism
Some antagonists can form covalent bonds with the active site on the receptor and this irreversibly blocks it. This is a non-competitive process because the irreversible antagonist cannot be displaced by the agonist which leads to a reduction in the maximal effect and this reduction in agonist efficacy.
Allosteric Antagonist
They bind to the site different from the agonist binding site and induce conformational change which prevents the agonist from activating the receptor.
Therapeutic Index
Not everyone will experience the same effect from the same dose of drug. The therapeutic index helps measure the relative safety of a drug.
Zero-Order Kinetics
The amount of drug eliminated is independent of drug concentration in the body.
First-Order Kinetics
Most drugs are eliminated by first order kinetics. The rate of elimination is directly proportional to the concentration of the drug in the body.
Steady State
Rate of drug administration = rate of drug elimination (equilibrium).
Absorption
the process by which a drug enters the body from its site of administration and enters the general circulation (note the lumen of the G.I. tract is outside the body).
Distribution
the transport of drug by the general circulation. Drugs most often leave the blood and enter perfused tissues. Once within a tissue further, reversible, distribution dictated by a concentration gradient, may occur by diffusion (or carrier-mediated transport).
Metabolism
the process by which tissue enzymes (principally in the liver – hepatic metabolism) catalyse the chemical conversion of a frequently lipid soluble drug to an often less active and more polar form that is more readily excreted from the body.
Excretion
the processes that remove the drug, or its metabolites, from the body (principally the kidneys – renal excretion), but other routes may be important for specific agents.
The Micturition Reflex
an example of the coordinated activity of the sympathetic and parasympathetic divisions of the ANS in terms of bladder control.