Basics 1

Question 1

What is Pharmacology?

Answer 1

The science concerned with the understanding of interactions b/w chemical substances and living systems

Question 2

What is medical pharmacology?

Answer 2

relates this understanding to human beings and the practice of medicine

Question 3

Pharmacy

Answer 3

deals with the chemical and physical properties of drugs, their formulations and packaging.

Question 4

What is a drug?

Answer 4

any substance that when administered to a living organism, brings about fxnl changes as a consequence of interactions at the molecular level.

Question 5

What can drugs be?

Answer 5

Inorganic
Small/Large organic molecules
Bio-macromolecules
Recombinant proteins, antibodies, polysaccharides, nucleic acids . etc

Question 6

Drugs can exist as diff types of stereoisomers ?

Answer 6

many drugs are administered as a RACEMIC mixture of the drug molecules’s stereoisomer. Typically, only 1 stereoisomer of a drug molecule will be significantly pharmacologically active. INTERACTIONS B/W BIOMOLECULES IS STEREOSPECIFIC

Question 7

Drug size and molecular weight

Answer 7

7(lithium) to over 50K.

100 usually poorlu absorbed and distributed

Question 8

Drug shape

Answer 8

Structural Isomer-same mol. formula, but bonded together in a different order.
May be chain, position, or functional group isomers.
Stereoisomers-same formula and sequece of bonded atoms, but diff 3D shape.
Chiral enantiomers-non-superimposable mirror images. Many receptors/drugs prefer some enantiomers over others. . . most chiral drugs are still provided as RACEMIC MIXTURES b/c it’s expensive to separate.

Question 9

What is pharmacokinetics?

Answer 9

"what the body does to the drug" Study of fate of drugs once ingested and the variability of drug response in varying patient populations. "ADME"
Absorption
Distribution
Metabolism/biotransformation
Elimination

Question 10

Routes of administration: What is the local effect?

Answer 10

at or near the site of administration

Question 11

Routes of administration: What is the systemic effect?

Answer 11

At site or sites near and distant to site of administration.

Question 12

What are the 2 broad categories of routes of administration?

Answer 12

Enteral and parenteral

Question 13

What is enteral administration?

Answer 13

delivery of drugs via the GI route:
Oral
Sublingual
Rectal

Question 14

What is parenteral administration?

Answer 14

Delivery of drugs NOT via the GI tact!
Injections
Subcutaneous
Intradermal
Intramuscular
Intravenous
Cutaneous-topical/transdermal
Mucous membrane admin-eyes, nose, ear, vaginally, urethral .etc .anything not taken orally or rectally.

Question 15

What is Drug absorption?

Answer 15

process by which unchanged drug proceeds from the site of admin to the site of measurement w/in the body (systemic circ.)

Question 16

What is the quantitative measurement of Drug Absorption?

Answer 16

Bioavailability

Question 17

What is bioavailability?

Answer 17

the fraction of a drug dose reaching the systemic circulation unchanged when administered by any route. (differs depending on route of admin.

Question 18

Why is the IV bioavailability of ALL DRUGS 100%?

Answer 18

b/c they are injected directly into the blood stream/systemic circulation.

Question 19

What are the 3 major areas that drugs are distributed to the body?

Answer 19

Therapeutic sites of action
Tissue réservoirs
Unwanted sites of action

Question 20

What are therapeutic sites of action?

Answer 20

Tissues/organs of the body where you want the drug to go so that it can function as a proper prophylactic, therapeutic, diagnostic agent.

Question 21

What is a tissue reservoir?

Answer 21

other tissues/organs of the body where the drug can be stored “DRUG DEPOT”

Question 22

What are unwanted sites of action?

Answer 22

tissues/organs where the drug is able to elicit effects that you do not necessarily desire->responsible for adverse effects and toxicities…

Question 23

What is volume of distribution (VD)?

Answer 23

Quatitative measurement of drug distribution

Question 24

How does conversion of a drug into different chemical substance effect it?

Answer 24

may inactivate the drug, maintain drug activity, or activate the activate the drug

Question 25

What is the major organ and enzyme involved in drug metabolism?

Answer 25

Liver! Cytochrome P450 (CYP) enzymes- located in SER of hepatocytes

Question 26

Drug Excretion

Answer 26

passing the drug out of the body. Renal excretion is the most important-via urine. Others include: intestines, lungs,skin, body secretions, etc, gaseous

Question 27

How do you measure drug excretion?

Answer 27

Clearance of a drug (CL)

Question 28

Pharmacodynamics?

Answer 28

``` "what the drug does to the body" study of effects, actions, and mechanisms of action of drugs: Receptors Mediators Targets Toxicity ```

Question 29

Mechanism of action

Answer 29

Drugs interact with MOLECULES within tissues and organs, (which causes changes in the tissues/organs) . . not whole tissues/organs. how the drug works at the molecular level

Question 30

Drug receptor

Answer 30

any cell component to which a drug binds to initiate the chain of biochemical events leading to the drug's observed effects. Usually cellular bio-macromolecules/proteins: regulatory proteins,ion channels,cell surface/cytoplamic receptors, enzymes, carrier proteins, and structural proteins. Note: a single drug may posses more than receptor and may affect them in different ways/diff degrees ie, may be determined by selectivity

Question 31

Via what type of bonds do drugs bind to their receptors

Answer 31

NON-covalent bonds: hydrogen bonds van der Waals attractions Ionic bonds Weaker non-covalent bonds require a better fit, and are reversible. Covalent bonds/very strong involve less selectivity and an irreversible interaction

Question 32

What are bound drugs? (know these well)

Answer 32

Agonist->full and partial Antagonist Inverse Agonist

Question 33

What is a full agonist?

Answer 33

a drug when bound to its receptor, activates the receptor to produce a maximal response.

Question 34

What is a partial agonist?

Answer 34

drug when bound to its receptor, activates the receptor to produce a response below the maximal level

Question 35

What is an antagonist?

Answer 35

drug when bound to the receptor, fails completely to produce any activation of that receptor-inibits/blocks/decreases agonist mediated responses of the receptor/ action.

Question 36

What is an inverse agonist?

Answer 36

drug that when bound to a constitutively active receptor (display biological activity in absence of any ligand), decreases the basal activity of that receptor.

Question 37

How do bound drugs exert their functions on their receptors?

Answer 37

through interaction with ACTIVE SITE/LIGAND BINDING site of a molecule or through direct interaction with an ALLOSTERIC site.

Question 38

In terms of inhibition drug receptors, how do antagonist and inverse agonists function?

Answer 38

Irreversible (suicide) inhibition Competetive inhibition Non-competetive inhibition Uncompetetive inhibition

Question 39

What is pharmacological action?

Answer 39

the functional or physiological modifications caused by the drug's interaction with its receptor(s)->leads to pharmacological effect

Question 40

What is pharmacological effect?

Answer 40

the observed effect which has been produced by the drug

Question 41

What is an example of a mechanism of action?

Answer 41

Drug X functions as a full agonist of cardiac beta-receptors

Question 42

What is an example of pharmacological action?

Answer 42

Drug X increases the freq of spontaneous depolarizations of the SA node of the heart.

Question 43

What is an example of pharmacological effect?

Answer 43

Drug X induces tachycardia.

Question 44

What is toxicology?

Answer 44

studies the adverse effects of drugs, the mechanisms of these effects , and the conditions that surround these effects.

Question 45

What are contraindications and precautions?

Answer 45

A condition which makes the use of a particular inadvisable. Absolute contraindication:absolutely inadvisable Relative contraindication: somewhat inadvisable, but does not rule it out (PRECAUTION) Often seen in anti-psychotics or seizure medicine that can harm the fetus.

Question 46

What are congeners & "me too" drugs?

Answer 46

Drugs that are similar to a drug that already exist. ie, just has an extra hydroxyl group.