1. NDRB 36

What is neuropsychopharmacology?

The study of how drugs affect the nervous system mood thinking behavior and mental processes

What is pharmacokinetics (PK)?

How drugs move through the body

What is pharmacodynamics (PD)?

How the body responds to drugs and drug receptor interactions

Drugs act at several target sites and produce multiple effects depending on how they move through the body. What is this called?

Pharmacokinetics

What is a therapeutic effect?

The desired physical or behavioral effect produced by a drug

What are side effects?

Any effects other than the intended therapeutic effect

What is the placebo effect an example of?

A nonspecific psychological effect due to mind body interactions

What is a placebo?

A pharmacologically inert substance that can still produce effects because of expectation and belief

Possible explanations for placebo effects?

Conscious expectation social learning and Pavlovian conditioning

What are the four principles of pharmacokinetics in order?

Absorption Distribution Metabolism Excretion (ADME)

What is bioavailability?

The amount of drug in the blood available to bind targets

What factors contribute to bioavailability?

Route of administration absorption distribution metabolism excretion binding and inactivation

What route of administration is fastest and most accurate?

Intravenous (IV)

Which route involves absorption through the lungs?

Inhalation

Which route provides slower more even absorption over time?

Intramuscular (IM)

What is subcutaneous administration?

Injection just beneath the skin

What is intraperitoneal administration?

Injection into the abdominal cavity commonly used in lab animals

What is the blood brain barrier (BBB)?

The separation between brain capillaries and the brain or CSF that limits substance entry into the brain

What is cerebrospinal fluid (CSF)?

Fluid surrounding the brain and spinal cord

Figure 1.4 x axis?

Time (hours)

Figure 1.4 y axis?

Drug concentration in blood (μg/kg)

Main point of Figure 1.4?

Different routes of administration produce different rates of absorption peak concentrations and durations of action

Compare IV and IM administration using ADME.

IV enters the bloodstream immediately producing the fastest rise and highest concentration while IM must first be absorbed from muscle causing a slower rise and longer duration

Compare IM oil and SC administration.

IM oil absorbs more slowly producing a lower but much longer lasting blood concentration than SC administration

Why is half life important in neuropsychopharmacology?

It determines how long a drug remains in the body and helps determine dosing intervals

What is half life?

The time required for 50 percent of a drug to be removed from the body

What is first order kinetics?

A constant percentage of drug is eliminated over time causing exponential decay

Example of first order kinetics?

Amphetamine

What is zero order kinetics?

A constant amount of drug is eliminated over time regardless of concentration

Example of zero order kinetics?

Alcohol

What is a receptor?

A protein that binds specific ligands and produces a cellular response

Why do receptors bind specific ligands?

Because of molecular shape compatibility or the lock and key model

True or False All drugs bind membrane bound receptors.

False

What type of receptor is the NMDA receptor?

A ligand gated non selective cation channel and ionotropic glutamate receptor

True or False NMDA is a selective cation channel.

False

What ions pass through NMDA receptors?

Primarily sodium potassium and calcium ions

What is an agonist?

A drug that binds and activates a receptor producing a biological effect

What is an antagonist?

A drug that binds a receptor but does not activate it and blocks agonists

What is a partial agonist?

A ligand that activates a receptor but produces less than the maximum response

What is an inverse agonist?

A ligand that produces the opposite effect of an agonist while blocking agonist actions

What is a competitive antagonist?

A drug that competes with an agonist for the same receptor binding site without activating the receptor

Can competitive antagonists be overcome?

Yes by increasing agonist concentration

What is one reason a high concentration of an agonist could overcome a competitive antagonist?

The agonist and antagonist compete for the same binding site so excess agonist is more likely to bind the receptor

What is a noncompetitive antagonist?

An antagonist that reduces agonist effects by binding elsewhere or interfering with receptor function

Can increasing agonist concentration overcome a noncompetitive antagonist?

No

Example of a competitive antagonist?

Naloxone blocking morphine or opioid receptors

How can drugs act as agonists in the brain?

Increase neurotransmitter synthesis increase neurotransmitter release or prolong neurotransmitter action in the synapse

What is up regulation?

An increase in receptor number usually after prolonged absence of stimulation

What is down regulation?

A decrease in receptor number after chronic receptor activation

What is a dose response curve?

A graph showing the relationship between drug dose and biological response

Why are dose response curves important in neuropsychopharmacology?

They allow researchers to measure and compare potency efficacy and effective dosage ranges

What is the threshold dose?

The smallest dose that produces a measurable effect

What is ED50?

The dose that produces 50 percent of the maximum effect

What is ED100?

The dose that produces the maximum effect

What happens if the dose increases beyond ED100?

No further therapeutic effect occurs because receptors are already maximally occupied

What does comparing ED50 values tell us?

Differences in drug potency

If Drug A has a lower ED50 than Drug B which is more potent?

Drug A

PK vs PD?

PK is what the body does to the drug and PD is what the drug does to the body

What does ADME stand for?

Absorption Distribution Metabolism Excretion

Fastest route of administration?

Intravenous (IV)

What determines dosing interval?

Half life

Can a competitive antagonist be overcome by more agonist?

Yes

Can a noncompetitive antagonist be overcome by more agonist?

No

NMDA receptor type?

Ligand gated non selective cation channel ionotropic glutamate receptor

Placebo effect?

A nonspecific psychological effect due to mind body interaction