Fundamental Principles of Pharmacology I

Question 1

Definition of drugs

Answer 1

Exogenous molecules that mimic or block the action of endogenous molecules or systems
Even though they are derived from exogenous sources, they may be chemically identical, related or distinct from endogenous molecules

Question 2

Definition of phamacodynamics

Answer 2

What a drug does to an organism

The sum of all the actions of a drug

Question 3

Definition of phamacokinetics

Answer 3

What the organism does to the drug (ADME)

Determines how quickly a drug acts

Question 4

Definition of intraarterial (IA)

Answer 4

Liquid injected into an artery, v rare in human medicine

Question 5

Definition intracerebroventricular (ICV)

Answer 5

Injected into the cerebral ventricles

Question 6

Definition of intradermal

Answer 6

Injected into the skin layer (liquid/suspension)

Question 7

Definition of intrathecal (IT)

Answer 7

Injected into the membranes that enclose the spinal cord

Question 8

Definition of transcutaneous

Answer 8

Fine powder blaster through the skin under pressure using a device or by diffusion from an adherent pathc

Question 9

Definition of proprietary name

Answer 9

Brand name

Question 10

Definition of common name

Answer 10

Active ingredient in a drug

Question 11

Definition of chemical name

Answer 11

Tells you the chemical composition

Question 12

Definition of assay

Answer 12

Investigative procedure for qualitatively assessing or quantitatively measuring the presence, amount or functional activity of the analyte

Question 13

Definition of chemical library

Answer 13

Compound library, collection of stored chemicals with associated info such as the chemical structure, purity, quantity and physiochemical characteristics

Question 14

Definition of combinatorial chemistry

Answer 14

Synthetic methods that make it possible to prepare a large no of compounds in a single process

Question 15

What are drugs

Answer 15

Exogenous molecules that mimic/block the action of endogenous molecules or systems

Can be

• chemically identical to an endogenous molecule
• related to an endogenous molecule
• chemically distinct from any endogenous molecule

Question 16

How do drugs function

Answer 16

The lock and key model

Drug molecule with complementary shape to the receptor binds
This binding produces an effect

Question 17

What are the 3 types of pharmacological receptor

Answer 17

Physiological receptor
Other proteins
Nucleic acids

Question 18

Describe how physiological receptors work

What are examples of these receptors

Answer 18

Endogenous proteins that are the receptors for endogenous chemical signalling compounds (hormones, NT)

Adrenergic, cholinergic, SNS, PNS

Question 19

Describe how other proteins function as receptors

What are examples of these receptors

Answer 19

Enzymes, ion channels

Drugs bind to specific sites on proteins, prevent them from functioning or stimulate them

Question 20

Describe how nucleic acids can function as receptors

Answer 20

Drugs bind to regulatory sites on nucleic acids to influence gene expression or protein synthesis

Question 21

Describe how agonists and antagonists function

Answer 21

Agonists bind to the complementary receptor => response

Antagonists bind to the complementary receptor => prevents receptor from being activated

Question 22

Describe how reversible and irreversible drugs function

Why is the type of binding important

Answer 22

Reversible drugs
-Ionic and can have hydrophobic interactions between the receptor and the drug

Irreversible drugs
-Covalent bonds cannot be broken easily

Determines drugs primary effects

Question 23

What is the difference between pharmacokinetics and pharmacodynamics

Answer 23

Pharmacodynamics, what a drug does to an organism
The sum of all the actions of a drug

Pharmacokinetics, what the organism does to the drug (ADME)
Determines how fast a drug acts

Question 24

What is absorption

What is it influenced by

Answer 24

How much drug entrees the system and the speed of entry

• Chemical properties of drug
• Molecular size
• Lipid solubility/ionization
• Chemical, metabolic vulnerability
• Routes of administration
• Properties of the patient

Question 25

How does the route of administration affect the absorption of a drug

Answer 25

Each route has a different barrier to absorption - IV, no barriers - PO, absorbed by the gut => into the bloodstream => metabolized by the liver

Question 26

How do the properties of the patient affect the absorption of a drug

Answer 26

- Fat, thin (affects lipophilic drugs) - Light, heavy (heavy people may need a larger dose) - Fed, empty stomach (affects absorption in GI) - Healthy, ill (hepatic disease => impaired metabolism, renal disease => impaired excretion)

Question 27

What is distribution | What is it influenced by

Answer 27

What happens after absorption In order to achieve its effects, drug may need to diffuse through tissue/carried in blood - Blood soluble - Stick to proteins or cells - Does it concentrate in fats or aqueous solutions - Does the patient have adequate circulation

Question 28

What is metabolism and excretion | What is it influenced by

Answer 28

Duration of action determined by metabolism and excretion If excreted rapidly, may have short duration of action - Location of metabolism and excretion - Health of liver and kidney - Whether metabolites are toxic

Question 29

What are the 5 ways of categorizing drugs

Answer 29

``` Proprietary name, brand name Common name, active ingredient Chemical name, chemical composition Therapeutic use, its function Mechanism, how it works ```

Question 30

Describe the preclinical pathway in making a new drug

Answer 30

Basic research info (science behind a biological process) Idea (Based off scientific theory) Hypothesis (Forms basis of idea for drug) Assay systems (Combining natural products, compound libraries, combinatorial chemistry => starting chemicals => assay system) Once an active chemical is found Optimized Tested on animal models Becomes a drug candidate

Question 31

Describe Phase 0 in a clinical trial

Answer 31

Subtherapeutic doses in humans to work out pharmacokinetics Can include tests on humanized animals Not expected to have an effect

Question 32

Describe Phase 1 in a clinical trial

Answer 32

Small scale involving 20-80 healthy volunteers Understand properties, side effects and safety Tolerability and dose findings found here

Question 33

Describe Phase 2 in a clinical trial

Answer 33

Medium scale involving 100-300 patient volunteers | Understand side effects and safety and effectiveness

Question 34

Describe Phase 3 in a clinical trail

Answer 34

Large scale involving 1000-3000 patient volunteers More uncontrolled variables Understand side effects and confirms effectiveness Comparisons with currently available medicines

Question 35

Who can you register a new drug with

Answer 35

UK, Medicines and Healthcare Regulatory Agency (MHRA) EU, European Medicines Agency (EMA) US, Food and Drug Admin (FDA)

Question 36

Describe Phase 4 in a clinical trial

Answer 36

Post registration studies, every prescription is still a test Test on different populations for long term safety