Katzung Pharm Ch 1

Front 1

Pharmacology

Back 1

Defines as a study of substances that interact with living systems through chemical processes.

Front 2

Medical Pharmacology

Back 2

The science of substances used to prevent, diagnose, and treat diseases. Deliberate therapeutic application

Front 3

Toxicology

Back 3

The branch of pharm that deals with the undesirable effects of chemicals on living systems

Front 4

Materia Medica

Back 4

The science of drug preparation and the medical use of drugs (precursor to pharm)

Front 5

Pharmacogenomics

Back 5

the relation of the individual's genetic makeup to his response to specific drugs- close to becoming a practical form of therapy.

Front 6

agonist

Back 6

activator

Front 7

antagonist

Back 7

inhibitor

Front 8

receptor

Back 8

regulatory molecule that interacts with a drug molecule (agonist/antagonist)

Front 9

Chemical antagonist

Back 9

interact with other drugs

Front 10

osmotic agents

Back 10

interact almost exclusively with water molecules.

Front 11

xenobiotics

Back 11

chemicals synthesized outside of the body
(xenos=stranger)

Front 12

Toxins

Back 12

Poisons of biological origin

Front 13

Drug Size

Back 13

Range from MW 7-60,000 but average range is 100-1000. Too small and it wont fit in the receptor and too large and it cant move about the body

Front 14

Covalent Bonds

Back 14

Very strong and usually irreversible in biological conditions, ex: aspirin and COX; DNA-alkylating agents chemotherapy.

Front 15

Electrostatic Bonds

Back 15

More common, vary from relatively strong to weaker hydrogen bonds and very weak van der Waals forces. All are weaker than covalent bonds

Front 16

Hydrophobic bonds

Back 16

Quite weak and important in the interaction of highly lipid soluble drugs with cell membranes

Front 17

Chirality

Back 17

Stereoisomerism; Usually one enantomer is more potent than another. One is also usually more susceptible to degradation by drug-metabolizing enzymes than the other. Drug transporters are stereoselective.

Front 18

Rational Drug Design

Back 18

using the characteristics of a known receptor to design a drug to fit that receptor.

Front 19

Pharmocodynamics

Back 19

Actions of the drug on the body. Determine the group and classification of the drug

Front 20

Pharmocokinetics

Back 20

The actions of the body on the drug. Govern absorption, distribution, and elimination of drugs

Front 21

Pharmacodynamic Principles

Back 21

Drug+Receptor-effector-->drug-receptor-effector complex-->effect
D+R-->drug-receptor complex-->effector molecule-->effect
D+R-->D-R complex-->activation of coupling molecules-->effector molecule-->effect
Inhibition of metabolism of endogenous activator-->increased activator--> increased effect

Front 22

Agonist

Back 22

Drugs that bind to and activate the receptor , which directly or indirectly brings about the effect

Front 23

Receptor activation

Back 23

Brings about a change in conformation . Some receptors incorporate effector machinery in the same molecule, so that the drug binding brings about the effect directly. Others are linked through intervening coupling molecules to a separate effector molecule.

Front 24

Pharmacologic antagonist

Back 24

bind to a receptor and compete with and prevent binding by other molecules. (ex: atropine blocking acetlycholine receptors)

Can be overcome by increasing the amount of agonist

Front 25

Allosteric inhibitor

Back 25

Bind to the same receptor molecule, but do not prevent binding of the agonist. More agonist wont overcome the allosteric inhibitor

Front 26

Constitutive activity

Back 26

Receptor activation occurring in the absence of agonist. May depend on receptor density, concentration of coupling molecules and the number of effectors in the system

Front 27

Full-agonist

Back 27

When administered at concentrations sufficient to saturate the pool, activate their receptor-effector system to the maximum extent capable.
Cause a shift of almost all the receptor pool to the Ra-D pool

Front 28

Partial agonist

Back 28

Do not evoke as great as a response as full-agonist. They do not stabilize the Ra configuration as fully.

Front 29

Intrinsic efficacy

Back 29

How well a drug stabilizes a Ra configuration. Low would be an example of a partial agonist

Front 30

Neutral antagonism

Back 30

Binds to the receptor site causes no change in the system (have no effect) until an agonist is present. Then the antagonist will block the receptor sites for the agonist and lower the effect.

Front 31

Inverse agonist

Back 31

The drug as a much higher affinity for the inactive state therefore stabilizing the Ri-D pool thereby reducing any constitutive activity. Effects are then opposite the effects of a normal agonist.

Front 32

Receptors

Back 32

Endogenous molecules that must be selective in choosing ligands (drugs) and must change its function when bound.

Front 33

Prodrug

Back 33

precursor chemical that is readily absorbed and distributed and then converted into the active drug by biological processes

Front 34

Pharmacokinetic movement of drugs

Back 34

Must be Absorbed into the blood, Distributed to its site of action, Permeate through barriers and Eliminated at a reasonable rate.

Front 35

Permeation

Back 35

-Aqueous Diffusion
-Lipid Diffusion
-Special Carriers
-Endocytosis/exocytosis

Front 36

Aqueous Diffusion

Back 36

Occurs within larger aqueous departments of the body (interstitial space, cytosol...) and across the endothelial membrane tight junction and endothelial lining of BV. Driven by concentration gradients and electrical fields if charged.

Front 37

Lipid Diffusion

Back 37

Most important limiting factor for drug permeation because they separate the aqueous compartments. Lipid:Aqueous partition coefficient of a drug is how readily it moves between aqueous and lipid media. (can also be dependent on pH)

Front 38

Special Carriers

Back 38

These molecules exist for substances that are too large or insoluble to diffuse passively. (peptides, AA and glucose). Use active transport/facilitated diffusion. Is inhibitable. Tend to be less selective when expelling foreign molecules

Front 39

Multi-drug resistance-associated protein

Back 39

transporter from the ABC family (ATP-binding cassette) excrete some drugs and their metabolites into urine and bile. Also responsible for some resistance in tumors to chemo drugs.

Front 40

Endocytosis/Exocytosis

Back 40

For very large substances.
-Bound to surface receptor
-Engulfed
-Carried into the cell by pinching off of new vesicle
-Released inside the cytosol
ex: intrinsic factor(B12)
Exo:
ex: neurotransmitter substances in nerve endings.

Front 41

Fick's Law of Diffusion

Back 41

The passive flux of molecules down a concentration gradient
Flux(molecules/unit time)= (C1 x C2) x Area x Permeability Coefficient /Thickness
C1=higher C2=lower concentration

Front 42

Henderson-Hasselbalch Equation

Back 42

log(Pronated/Unpronated)=pKa-pH
Used for weak acids and bases

Adjusting the pH of a solution (in the kidney) can change the reabsorption of that drug