L6 - Neuropharmacology Flashcards
What is Neuropharmacology?
The drug and toxin induced changes in the function of cells in the nervous system
What are the two branches of Neuropharmacology?
Behavioural
Molecular
What is Pharmacokinetics?
Branch of pharmacology dedicated to the determination of the fate of substances administered to a living organism
What does Pharmacokinetics mainly deal with?
Absorption of the Chemical
Distribution in the body
Metabolism
Excretion
What is Pharmacodynamics?
Physiological effects of drugs in the body
What does Phharmacodynamics mainly deal with?
Dose-Response Relationships
Activity/Response profiles
Mechanism of Action
List examples of routes of drug administration
Oral Intravenous Intraperitaneal Sub-cutaneous Sub-lingual Intra-nasal Inhalation Into ventricle Local injections
In order for a drug to pass into the brain it must be..
Have a molecular weight less than 500
Be highly lipophillic or be actively transported
What does high potency mean?
You only need a low concentration of the drug to elicit a maximal response
What does high efficacy mean?
The size of the effect you obtain is large
What is an EC50?
The concentration needed to evoke half maximal response
Why would you perform a second messenger assay?
To try to discover what the drug is causing to happen in the cell
What methods do big companies use to discover drugs?
Purification from a natural source followed by structural and chemical derivation e.g. Aspirin
Derivation of natural enzyme substrates or NTs e.g. L-Dopa
Utlization of X-ray structures of putative drug target for computer assisted drug design e.g. AMPA antagonists
High throughput screening followed by chemical optimization (Most favoured)
How do we condition fear in Rats?
Use the Fear Potentiated Startle method (FPS) . Which involves the association of a signal with a loud noise.
How do we test innate fear in rats?
Using the light dark box which uses the Rat’s natural tendency to explore a new environment and aversive properties of a brightly lit open area
What is anxiety?
Inappropriate expression of fear
What is a mood?
Sustained emotional state
How were brain areas of emotional processing discovered?
Lesion studies both experimental and opportuinistic
An insular cortex lesion would have what effect?
The inability to experience disgust
An amygdala lesion would have what effect?
Learned fear response is eliminated Innate fear response in inhibited Hypersexuality Decreased aggresion General suppressed emotion
What are the centres for fear and aversion in the human brain?
Pre-frontal cortex
Anterior and posterior cingulate cortex
Insular cortex
Amygdala
What is the neual circuit for emotion
The papez circuit
List possible sites for drug action
NT synthesizing enzymes Synaptic vesicle transporters Reuptake transporters Degradative enzymes Transmitter gated ion channls GPCRs g-proteins G-protein gated ion channels 2nd messenger cascades
Where do Benzodiazepines act?
At an allosteric binding site between the alpha and gamma subunits on a GABAareceptor/
What is Diazepam more commonly known as?
Valium
What is Diazepam commonly used to treat?
Anxiety Insomnia Seizures Alcohol withdrawal Muscle Spasms
What is Alprazolam more commonly known as?
Xanax
What is Alprazolam commonly used to treat?
Moderate anxiety disorders
Panic attacks
Adjunctive treatment for anxiety associated with depression
What can GABA hypofunction/Glutamate hyperfunction cause?
Anxiety
Drug Abuse
Schizophrenia
Epilepsy
What can Glutamate hypofunction cause?
Depression
Schizophrenia
What are the most common Anti-depressants?
Tricyclics -target NA and 5HT uptake
Serotonin and NA reuptake inhibitors (SNRIs)
Selective serotonin reuptake inhibitors (SSRIs)
Monoamine oxidase inhibitors
