1 - Cells, Diffusion, Basics

Question 1

Defines the dose of drug that is lethal to 1% of population compared with dose therapeutically effective in 99% (LD1/ED99).

Answer 1

Certain Safety Index

Question 2

The difference of content between one side of the cell membrane and the other; the larger the difference, the faster the diffusion.

Answer 2

Concentration Gradient

Question 3

These describe the extent of biological or behavioural effect produced by a given drug dose on a population. Plotted on a semi-log scale, it has an S-shape. At low doses, drug-induced effect is slight because very few receptors are occupied. The ____ ____ is the smallest dose that produces a measurable effect. As the dose of drug increases more receptors activate and a greater biological response occurs.

___ __ is the dose that produces half of maximal effect (the more potent drug is the one for which it is lower) and ___ ___ occurs at a dose where we assume receptors are maximally occupied.

These graphs show that with increasing doses, the effect increases steadily until the maximum effect is reached.

Answer 3

Dose–Response Curve | Threshold Dose | ED50 | ED100

Question 4

The reduction in a cellular response to a molecule due to a decrease in number of receptors on cell surface. The process of reduces / suppresses a response to a stimulus.

Answer 4

Down-Regulation

Question 5

Refers to specific molecular changes produced by a drug when it binds to a particular target site or receptor.

Answer 5

Drug Action

Question 6

All drugs have multiple effects and can be sorted/identified in any of several ways depending on the trait of interest.

Answer 6

Drug Category

Question 7

Molecular changes from drug action lead to more widespread alterations in physiological or psychological functions.

Answer 7

Drug Effects

Question 8

Effects of drug are determined by 2 primary factors and are qualified by other issues (2)

Answer 8

• How muach drug reaches its target sites, where it has biological action, and
• how quickly the drug reaches those sites.

qualified by

• Nonspecific characteristics of individuals/environments;
• Frequency/history of prior use — time gap; same dose may overdose/kill

Question 9

Inflammation of heart lining

Answer 9

Endocarditis

Question 10

A network of tubules within the liver cell cytoplasm. Liver enzymes primarily responsible for metabolizing psychoactive drugs are located here.

Answer 10

Endoplasmic Reticulum

Question 11

Drugs pass through the liver and become subject to metabolism/biotransformation

Answer 11

First Pass Effect

Question 12

Family of proteins that act as molecular switches inside cells. Involved in transmitting signals from variety of stimuli outside cell to interior.

GNBP

Answer 12

Guanine Nucleotide-Binding Proteins. G proteins.

Question 13

These bind to a receptor and initiate a biological action that is the opposite of what would be produced by an agonist.

Answer 13

Inverse Agonists

Question 14

Any molecule that binds to a receptor with some selectivity.

Answer 14

Ligand

Question 15

Concerned with drug-induced changes in the functioning of cells in the nervous system.

Answer 15

Neuropharmacology

Question 16

Its goal is to identify chemical substances acting on the nervous system which alter behaviour that is disturbed due to injury, disease, or environmental factors. Also interested in using chemical agents as probes to gain understanding of neurobiology of behaviour.

Answer 16

Neuropsychopharmacology

Question 17

Drugs that reduce effects of agonists in ways other than competing for receptors. May impair agonist action by binding to portion of receptor other than agonist-binding site, by disturbing cell membrane supporting the receptor, or by interfering with intracellular processes that were initiated by the agonist–receptor association.

ex: the analgesic dose–response curve of morphine is distorted and the same maximum effect is not likely to be reached.

Answer 17

Non-Competitive Antagonists

Question 18

Demonstrate efficacy that is less than that of a full agonist but more than that of an antagonist at a given receptor.

Answer 18

Partial Agonist

Question 19

A substance tends to move from an area of high concentration to an area of low concentration until the concentration is equal across the space.

Answer 19

Passive diffusion

How our cells breath; CO2 leaks out and oxygen goes in same way.

Question 20

The study of physiological and biochemical interactions of drug molecules with target tissue responsible for the ultimate effects of a drug. Drugs have biological effects because they interact with receptors on target tissues.

Answer 20

Pharmacodynamics

Question 21

Study of genetic basis for variability in drug response in individuals. Goals are identify genetic factors that confer susceptibility to specific side effects and to predict good/poor therapeutic response. It should be possible for clinician to select most appropriate drug for individual based on this study.

Answer 21

Pharmacogenetics

Question 22

These collectively contribute to bioavailability (5)

Answer 22

Pharmacokinetic Factors/Components of DrugAction

1. Routes of administration
2. Absorption and distribution
3. Binding
4. Inactivation
5. Excretion

Question 23

Scientific Study of the actons of drugs and their effects on a living organism

Answer 23

Pharmacology

Question 24

2 drugs act in distinct ways but interact in a way that reduce each other’s effectiveness.

One may act on receptors in heart to increase heart rate, and 2nd may act on distinct receptors in brain-stem to slow heart rate.

Answer 24

Physiological Antagonism

Question 25

Absolute amount of drug necessary to produce a specific affect. Differences among 3 drugs can be seen by comparing each ED₅₀.

Answer 25

Potency

Question 26

Combination of 2 drugs produces effects greater than sum of individual effects. Often involves issues of pharmacokinetics like altered metabolic rate/competition for depot binding, which may elevate free drug blood levels in unexpected ways.

Answer 26

Potentiation

Question 27

Usual analogy of a lock and key suggests only a limited group of these neurochemicals or drugs can bind to a particular receptor protein to initiate a cellular response.

Answer 27

Receptor Agonists

Question 28

A key may fit in a lock but not turn; a ligand may be recognized by a receptor but not initiate a biological action. These ligands are considered to have low efficacy and block the receptor; they bind to receptors but fail to initiate an intracellular effect, thereby reducing the effects of the agonists.

Answer 28

Receptor Antagonists / Competative Antagonists

Question 29

Receptor proteins for a drug or neurotransmitter with different characteristics in different target tissues.

Answer 29

Receptor Subtypes

Question 30

Large protein molecules located on cell surface or within cells that are initial sites of action of ligands.

Answer 30

Receptors

Question 31

Where the drug does its work. May be different from site of drug effect.

Answer 31

Site of drug action

Question 32

Morphine taken internally leads to *pinpoint* *pupils*. The ____ \_\_\_\_ ____ \_\_\_\_ is distant from the site of initial action.

Answer 32

Site of Drug Effect

Question 33

Those based on the physical and biochemical interactions of a drug with a target site in living tissue.

Answer 33

Specific Drug Effects

Question 34

Desired blood concentration of a drug achieved when the absorption/distribution phase is equal to the metabolism/excretion phase. Approached after a period of time queal to 5 half-lives.

Answer 34

Steady State

Question 35

Involves taking multiple blood samples to directly measure plasma levels of drug after drug has been administered. Done to identify optimim dosage to maximize positive potential and minimize side effects. Especially important for dugs with serious side effects and when there are changes in an individual's pharmacokinetics due to aging, hormonal shifts, stress, new medications, or other events.

Answer 35

Therapeutic Drug Monitoring

Question 36

Desired outcome/effects of the drug's use. \_\_\_ The drug–receptor interaction produces desired physical or behavioural changes. SSRI - more serotonin/calming

Answer 36

Therapeutic Effects

Question 37

Calculates Drug Safety by looking at cumulative % of population experiencing particular drug-induced response.

Answer 37

Therapeutic Index

Question 38

2 principal types of receptors

Answer 38

**Extracellular**: Most drugs and neurotransmitters remain outside cell and bind to receptors on exterior cell surface **Intracellular**: Many hormones capable of entering cell before acting on an intracellular receptor that changes expression of specific genes within nucleus.

Question 39

Increase in a cellular response to a molecular stimulus due to increase in number of receptors on cell surface. The process increases response to a stimulus.

Answer 39

Up-Regulation

Question 40

Pharmacologically inert compound administered to an individual

Answer 40

Placebo

Question 41

All effects other than the desired physical or behavioural changes

Answer 41

Side Effects

Question 42

Explainations for Placebo Effect

Answer 42

* **Pavlovian Conditioning** * **Social Learning​** —Conscious expectations of outcomes * **Genetic Variants** (runners who like running may ave greater natural opioid response → higher placebo response

Question 43

Amount of drug in the blood that is free to bind at target sites.

Answer 43

Bioavailability

Question 44

Expecting treatment failure when an inert substance is given along with verbal suggestions of negative outcome produces negative reporting (increased stress hormones). Warnings about side-effects can lead to greaeteer side effect occurance.

Answer 44

Nocebo Effect

Question 45

Drug unrelated to the drug being tested but not completely innert so as to produce some side-effects. When the study drug is certain to have side-effects this helps conceal the true placebo group.

Answer 45

"Active" Placebo