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What is a receptor made out of?

Protein

What is potentiate?

To make stronger

What is inhibit?

To slow or stop

What is exogenous?

Coming from outside the body

What does mimic mean?

To imitate

What is the margin of safety?

LD1: ED99

What is "safety"?

It measures the potential of the drug to cause adverse effects that vary from predictibale and tolerable side effects to serious and unpredicatable toxicities.

What is Therapeutic index?

The ratio of LD50:ED50 to determine the relative safety of the drug.

What are 3 actions that result from drug-receptor binding?

Agonist (direct); Agonist (indirect); Antagonist

What is ED50?

A dose of drug that produces the desired effects in 50% of the subjects

What is efficacy?

A maximum effect obtainable with additional doses producing no more effect

What is slope?

The amount of change in dose needed to produce a difference in effect

Define the function of Agonist (direct)

Drug binds to receptor site normally occupied by NT and mimics the action of the NT (ex. Meth, Heroin)

What is variability?

Individual differences in a drug response

What is "potency"?

The absolute number of molecules of a drug required to elicit a response, a measurement of the dose required.

When a NT hits a receptor site is it reversible? What happens?

The NT activates the neuron while it's attached and changes the structure of the protein

What is Peak?

The plot on a curve that indicates the maximal effect or efficacy that can be produced by the drug.

What are the four elements of receptor structure?

Ion channel receptors (1st messenger); Carrier proteins; G Protein coupled receptors (2nd messengers); enzymes (acetylcholine esterase; monoamine oxidase)

Define "potent"

The lowest dose that achieves the same level of response as a higher dose of a second drug. (Ex. Codeine vs. Morphine)

Define the function of agonist (indirect)

Drug binds to a near-by receptor site normally occupied by NT and facilitates NT binding (modulator or regulator) [Ex. Caffeine]

What is endogenous?

Naturally occurring in the body

what is the term for measurments of the degree the drug produces the therapeutic results that are claimed by the manufacturer in the general population?

Effectiveness

Where is potency measured on a graph?

On the horizontal axis

Where is dose measured on a graph?

On the horizontal axis

Where is response measured on a graph?

On the vertical axis

Define the function of an Antagonist

The drug binds to a receptor site normally occupied by NT and blocks access of the NT, prohibiting the normal fuctioning of the cell (ex. Narcan)

What is disrupt?

To alter/change

What affects intensity?

he best fit to the receptor & the percentage of receptors occupied by the drug

What is LD50?

The lethal dose in 50% of the experimental animals receiving a certain drug

What is a ligand?

A Neurotransmitter

What is pharmacodynamics

It is the basic principly of pharmacology that the pharmacological, physiological or behavioral effects induced by a drug follow from their interaction with receptors

What is the fuction of a receptor?

A binding site for endogenous NT's or exogeneous drugs

What is drug-receptor binding?

It is the occupation of a receptor by a drug or other molecular substance

Is drug-receptor binding reversible?

Yes in most cases

The interactions between the pahrmacological, phisiological, or behavioral effects that happen because of the drugs interation with the receptors is the study of what?

Pharmacodynamics

In most cases what is reversible?

Binding

Where would you find a receptor?

Embedded in the postsynaptic membrane

What is a complex structure?

A Receptor

Although binding is reversible, what can still happen before it reverses?

The NT activates the neuron while it's attached and changes the structure of the protein

A drug can affect the signal by binding to what?

The receptor meant for a NT or to a nearby, related site

Drugs do not create unique effects means...

Drugs cannot do anything your body can't do on its own

Drugs don't produce distinctive effects they...

Mimic, copy, potentiate, disrupt, inhibit or block the natural neuronal functions that are normally the action of the NT

If a receptor is usually occupied by a NT, then what can bind to the site, Prohibiting normal physiological functioning of the cell?

Antagonist (drug)

What does not cause effect, but instead just blocks, and gets in the way?

Antagonist (drug)

What is it called when a drug binds to a NT receptor site and mimics the actions of that NT?

Direct Agonist

Which Agonist is the one that binds to NT receptor site and mimics the action of the NT that normally occupies it?

Direct Agonist

Which Agonist is the one that binds to a near-by NT receptor site and facilitates NT binding? (Modulator or Regulator)

Indirect Agonist

What kind of Agonist hijacks the receptor sites that have other Neurotransmitters in it?

Direct Agonist

What kind of Agonist is not as strong?

Indirect Agonist

Where is slope measured on the graph?

On the vertical axis

Which one of the 4 elements of receptor structure is first messenger?

Ion Channels Receptors

Which one of the 4 elements of receptor structure is second messenger?

G Protein-Coupled Receptors

Which one of the 4 elements of receptor structure is missing: Ion Channel Receptors, Carrier Proteins, G Protein-Coupled receptors

Enzymes

If it ends in (ase) it must be directly related to...

Enzymes

Acetylcholine esterase is a...

Enzyme that breaks down Ach

Monoamine Oxidase is an enzyme that breaks down what?

DA, NE, 5HT

Receptors exhibit high specificity for...

One particular NT & certain drug molecules

What do certain drugs have for certain receptors?

An affinity (relationship)

What are Receptors built to have a specific relationship with?

A Neurotransmitter

What two things will determine the intensity of a drugs effect by eliciting the greatest response from the cell?

The best fit to the receptor & the percentage of receptors occupied by the drug

Response is...

On the vertical axis

Potent means

Its concentrated, it takes less

The graph plots the dose against what?

Percentage of people who display a characteristic or typical effect

The intensity or magnitude of the response in a single person is plotted against?

Dose

What is the complete number of molecules of a drug necessary to elicit a response, a measurement of the amount (dose) required?

Potency

If you're as high as you're going to get no matter how much more doses you take, you've achieved what?

Maximum Efficacy

When you consider the different ways people respond to a drug because of their individual factors, you are considering what?

Variability

If you are considering a less safe drug that produces a greater effect with only a small increase in dose, vs. a drug that takes many doses to greatly increase the effect, you are considering what part of the graph?

Slope

When you have reached the maximum efficacy of a drug, "you are as high as you're going to get." on the graph, the plot on the curve that indicates this is called what?

Peak

What does Effectiveness measure?

How many percentages of people are getting therapeutic results from a drug that the manufacturer claims is effective

What does safety measure?

The likeliness of a drug to cause side effects, and if those side effects are ones that can be dealt with or ones that can cause death or other serious illness

Effects that change depending on the needs & desires of the user, & are related to the principle and predictable pharmacological action of the drug are...

Unwanted RELATED side effects or drug toxicity

Effects that change depending on the needs & desires of the user, & are unrelated to the expected actions of the drug are...

Are UN RELATED side effects or drug toxicity

Main effects are ______, while side effects are _________

Desired & Undesired

When are side effects usually apparent?

Well before the maximum effect of the drug is detected

What is independent from the reason a drug is taken?

Side Effects

If you think your high when you're not you are probably experiencing what?

The Placebo Effect

What type of drug does not mean a more effective drug it just means a drug that produces an effect at a somewhat lower dose?

Potent

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