introduction to pharmacology Flashcards
(53 cards)
what is pharmacology?
The study of the action of drugs on the function of living systems
what is a drug?
a chemical substance or natural product that affects the function of cells, organs, systems or the whole body (i.e. is bioactive)
where do drugs come from?
Natural products (i.e. plants, animals)
Serendipity (i.e. by accident)
Changing the structure of an existing molecule (i.e. structure-activity relationships)
Using an existing drug in a new disease (i.e. re-purposing)
Computer-aided design
Studying disease processes
what are the three types of names of drugs?
Chemical – IUPAC name that describes the chemical structure of the drug
Generic – international non-proprietary name given to a molecule
Proprietary – ‘trade’ name(s) given to an approved drug by the manufacturer
what is pharmacokinetics?
what the body does to the drug
- used as a generic term to describe the fate of a drug molecule following administration to a living organism or how a drug molecule is affected by exposure to living cells
what is pharmacodynamics?
what is drug does to the body
- used as a generic term to describe the mechanism of drug action or what happens to cells, organs, systems, etc., as a result of drug exposure
how are proteins involved with drugs?
- drug transporters
- metabolising enzymes
what cells are involved with drugs?
- epithelial cells
- endothelial cells
- hepatocytes
drug administration paths…
what are the different routes of drug penetration into cells?
Diffusion through lipid membrane
- Major route for lipophilic drugs
Diffusion through aqueous channels
- Most drugs too large!
Carrier-mediated transport
- Major route for hydrophilic drugs
Pinocytosis
- Transport of insulin into brain
what does oral absorption of drugs require?
permeation of epithelial cell membrane
what is lipinski’s rule of 5?
an oral drug must have:
- molecular mass less than 500 Daltons
- no more than 5 H-bond donors (total number of N-H and O-H bonds)
- no more than 10 H-bond acceptors (all nitrogen or oxygen atoms)
- an octanol-water partition coefficient log P not greater than 5
basics of drug metabolism…
oral dosing…
what are the drug effects at the level of the cell?
Effects on receptors, ion channels, enzymes, transporters, DNA, etc.
what are the drug effects at the level of the organ/system?
Effects on heart, kidney, cardiovascular system, central nervous system, etc.
what are the drug effects at the level of the organism?
Therapeutic effect on disease state or process; adverse effects or side effects
what are the drug effects at the level of society?
cost , misuse, drug resistance
what are the sites of drug action?
- Human body = 100 trillion cells, 200 different cell types
- Primary tissues: muscle, nerves, epithelial, bone, connective, etc.
- Tissues controlled by: innervation, extracellular fluids, blood supply, exocrine and endocrine secretions
- Many drugs mimic (or block) the action of endogenous molecules (e.g. neurotransmitters, hormones)
- Act at specific sites; receptors, ion channels, enzymes, transporters (all of which are proteins)
what are the particular constituents of cells which drug molecules must bind to to produce an effect?
drug targets
how to drugs act?
- exert a chemical influence on constituents of cells to produce a pharmacological response
- must get close enough to cellular constituents in order that they can interact chemically
- leads to an alteration in molecular / cellular function
what are the protein targets for drug binding?
- receptors
- enzymes
- ion channels
- transporters
- circulating proteins, DNA, bacterial cell wall etc.
what is the main function of receptors?
cell to cell communication
where is cell to cell communication important?
- Neurotransmission (e.g. nerve to nerve; nerve to muscle)
- Effects of chemical mediators in bloodstream (e.g. adrenaline on heart)
- Hormone and growth factor signalling (e.g. action of insulin on muscle)
