Pharmacology: Chapter 1

Front 1

Pharmaceutic

Back 1

The drug becomes a solution so it can cross the biological membrane.

Front 2

Excipients

Back 2

Used in drug preparation to allow the drug to take a particular size and shape and to enhance drug dissolution.

Front 3

Disintegration

Back 3

The breakdown of a tablet into smaller particles.

Front 4

Dissolution

Back 4

The dissolving of smaller particles into the GI fluid before absorption.

Front 5

Pharmacokinetics

Back 5

The process of drug movement to achieve drug action.

Hint 5

Absorption, Distribution, Metabolism (or biotransformation), and excretion( or elimination)

Front 6

Absorption

Back 6

The movement of drug particles from the GI tract to the body fluids by passive absorption, active absorption, or pinocytosis.

Front 7

Passive absorption

Back 7

Occurs mostly by diffusion (movement from higher concentration to lower concentration)

Hint 7

No energy required!

Front 8

Active absorption

Back 8

Requires a carrier such as an enzyme or protein to move the drug against a concentration gradient.

Hint 8

Requires energy!

Front 9

Remember

Back 9

Drugs that are lipid soluble and nonionized are absorbed faster than water soluble and ionized.

Front 10

First-pass effect

Back 10

Process in which the drug passes to the liver first.

Hint 10

Hepatic first pass

Front 11

Bioavailability

Back 11

The percentage of administered drug dose that reaches the systemic circulation.

Hint 11

Subcategory of absorption

Front 12

Factors that alter Bioavailability

Back 12

1) the drug form (e.g., tablet, capsule,sustained release, etc)

2) route of administration ( e.g., oral, rectal, suppository, inhalation)

3) GI mucosa and motility

4) food and other drugs, and

5) changes in liver metabolism caused by liver distinction or inadequate hepatic blood flow.

Front 13

Distribution

Back 13

Process by which the drug becomes available to body fluids and body tissues.

Hint 13

Influenced by blood flow, drug affinity to tissue, and the protein-binding effect

Front 14

Protein-binding effect

Back 14

As drugs are distributed in the plasma, many are bound to varying degrees (percentages) with protein ( primarily albumin)

Front 15

Free drugs

Back 15

(Drugs not bound to a protein) are active and can cause a pharmacological response

Front 16

Metabolism

Back 16

Process by which the body inactivates or biotransforms a drug

Front 17

Half-life (t1/2)

Back 17

The time it takes for one half of the drug concentration to be eliminated

Front 18

Elimination ( or excretion )

Back 18

Exiting of drug from the body through the main route,kidneys (urine), or other routes such as; bile, feces,lungs,saliva, sweat, and breast milk.

Front 19

Creatinine clearance (CLcr)

Back 19

Common test used to determine reanal function and blood urea nitrogen (BUN)

Hint 19

Compares the level of creatinine in the urine with the level of creatinine in the blood.

Front 20

Creatinine

Back 20

A metabolic by-product of muscle that is excreted by the kidneys

Front 21

Pharmacodynamics

Back 21

The study of the way the drugs affect the body.

Front 22

Primary and secondary effect

Back 22

The primary effect is desirable while the secondary effect may be desirable or undesirable.

Front 23

Onset of action

Back 23

The time it takes to reach minimum effective concentration(MEC) after a drug is administered

Front 24

Peak action

Back 24

Occurs when drug reaches the highest blood or plasma concentration

Front 25

Duration of action

Back 25

The length of time the drug has a pharmacological effect

Front 26

Time-response curve

Back 26

Evaluate three drug parameters of action: the onset of duration, peak action, and duration of action.

Front 27

Weak vs. Strong Agonist

Back 27

Two drug agonist attach to the receptor site. The drug agonist that has the exact fit is a strong agonist, and is more biologically active than the weak agonist.

Front 28

Receptor families

Back 28

1) kinase-linked receptors, 2) ligand-gated ion channels, 3) G protein- coupled receptor systems, 4) nuclear receptors.

Front 29

Kinase-linked receptors

Back 29

The ligand-binding domain for drug binding is on the cell surface. The drug activates the enzyme (inside the cell), and a response is initiated

Front 30

Ligand-gated ion channels

Back 30

The channel spans the cell membrane and with this type of receptor, the channel opens, allowing for the flow of ions into and out of the cells (primarily sodium and calcium)

Front 31

G protein- coupled receptor systems

Back 31

There are three components to this receptor response: 1) the receptor 2) the G protein 3) the effector that is either an enzyme or an ion channel.

Hint 31

Drug>receptors>G protein>effect

Front 32

Nuclear receptors

Back 32

Found in the cell nucleus ( not on the surface) of the cell membrane. Activation of receptors through transcription factors is prolonged. With the first three receptor groups, activation of the receptors is rapid

Front 33

Agonist

Back 33

Drugs that produce a response

Front 34

Antagonist

Back 34

Drugs that block a response

Front 35

Non specific drugs

Back 35

Drugs that affect various sites and have properties of nonspecificity

Front 36

Nonselective drugs

Back 36

Drugs that affect various receptors or have properties of nonselectivity

Front 37

Four categories of drug action

Back 37

1) stimulating or depression 2) replacement 3) inhibiting or killing or organisms 4) irritation

Front 38

Therapeutic index (TI)

Back 38

Estimates the margin of safety of a drug through the use of a ratio that measures the effect (therapeutic) dose (ED) and the lethal dose (LD)

Front 39

Therapeutic range (therapeutic range)

Back 39

The level of drug between the minimum effective concentration in the plasma for obtaining desired drug action and minimum toxic concentration (the toxic effect)

Front 40

Peak drug level

Back 40

The highest plasma concentration of the drug at a specific time

Front 41

Trough levels

Back 41

The lowest level of plasma concentration of a drug, and it measures the rate at which the drug is eliminated.

Front 42

Loading dose

Back 42

When immediate drug response is desired, a large initial dose is given to achieve a rapid minimum effective concentration in the plasma

Front 43

Side effects

Back 43

Physiological effects not related to desired drug effects

Front 44

Adverse reactions

Back 44

More severe than the side effects

Front 45

Toxic effects (or toxicity)

Back 45

Identified by monitoring the plasma (serum) therapeutic range of the drug.

Front 46

Pharmacogenetics

Back 46

The scientific discipline studying how the effects of some drug action varies from predicted drug response because of genetic factors of hereditary influence

Front 47

Tolerance

Back 47

A decrease responsiveness over the course of therapy

Front 48

Tachyphalaxis

Back 48

A rapid decrease in response to the drug (acute tolerance)

Front 49

Placebo effect

Back 49

A physiological benefit from a compound that may not have tee chemical structure of a drug effect