Neuropharmacology Flashcards
focuses on the basic chemical composition and processes of the nervous system
Neurochemistry
is the study of compounds that selectively affect the nervous system
- The presynaptic neuron releases an endogenous (internal) substance – a neurotransmitter
Neuropharmacology
any substance that binds to receptor
- Endogenous ligands bind to a receptor and activate a change (e.g. opens an ion channel)
Ligand
- When a drug activates the receptor, it’s acting as an…
- the other only produce a small response
agonist
Partial agonists
When a drug binds to a receptor without activating it and blocks it, is an…
antagonist
They don’t – they just spread throughout the body and bind to their receptors when they find them
How do drugs know where to go?
the collective name for all the factors that affect the movement of a drug into, through, and out of the body
Pharmacokinetics
free to act on the target
bioavailable
produces active metabolites that may produce side effects
- A drug’s effect depend on the dose, where it binds, and what it does
Biotransformation
the degree of chemical attraction between a ligand and a receptor
Binding Affinity
the ability of a bound ligand to activate the receptor
Efficacy (intrinsic activity)
is a graph of the relationship between drug doses and the effects
A Dose-Response Curve (DRC)
tight junctions between the cells of blood vessels in the CNS prevent the movement of large molecules; can limit drug availability
Blood-Brain Barrier
Reduced Efficacy of the Drug
Repeated Drug Treatments May Result in Drug Tolerance
organ systems become more effective at eliminating the drug
Metabolic Tolerance
target tissue may alter its sensitivity to the drug by changing the number of receptors
Functional Tolerance
in response to an agonist – fewer receptors
Down-Regulation
in response to an antagonist – more receptors
Up-Regulation
tolerance to one drug is generalized to other drugs in its class
Cross-Tolerance
depends on absorption
by the gut, which is somewhat slower than most other routes and
affected by digestive factors such as acidity of the stomach and the
presence of food.
- slow to moderate
ingestion
take advantage of the rich
vascularization of the nose and lungs to convey drugs directly into the
bloodstream
- moderate to fast
inhalation
- under the skin tend to have the slowest effects because they must diffuse into nearby tissue in order to reach the bloodstream
- intravenous have very
rapid effects because the drug is placed directly into circulation - moderate to fast
peripheral injection
directly into the central nervous system and are used in order to circumvent the blood-brain barrier, to
rule out peripheral effects, or to directly affect a discrete brain
location.
- fast to very fast
central injection
