Lecture 1 - introduction

Question 1

What is pharmacology?

Answer 1

The study of mechanisms by which drugs affect the function of living systems

Question 2

Where is morphine derived from?

Answer 2

Poppy - synthesis achieved in 1950s

Question 3

What drug was first sold as a non-addictive form of morphine?

Answer 3

Heroin

Question 4

What is the 4th largest product in the healthcare sector?

Answer 4

Aspirin

Question 5

What can endorphins be referred to as?

Answer 5

a self-made form of pain relief

Question 6

What is a drug?

Answer 6

a chemical (of known structure) which when administered to a living organism produces a biological effect.

Question 7

What are 3 types of drugs?

Answer 7

• synthetic chemical (heroin)
• plant chemical (morphine from poppy)
• biopharmaceutical (generated through the biotech industry)

Question 8

What is a medicine?

Answer 8

A chemical preparation that usually contains one or more drugs, ADMINISTERRED to produce a therapeutic effect

Question 9

What else do medicines contain other than drugs?

Answer 9

• excipients
• stabilizers
• solvents

Question 10

What impact do excipients have on a medicines’ therapeutic effect?

Answer 10

They don’t impact the potency of the drug and its therapeutic effect

Question 11

How might you engineer proteins?

Answer 11

Change the properties of insulin to last longer

Question 12

What is gene therapy?

Answer 12

The addition of genetic material to cells to prevent, alleviate or cure disease

Question 13

Describe what you can use DNA technology for

Answer 13

• therapeutic monoclonal antibodies
• recombinant hormones
• siRNA
• mRNA

Question 14

Describe an example of regenerative medicine

Answer 14

Engineered stem cells to replace irreparably damaged organs

Question 15

Describe what occurs in the first generation in the development of biologics

Answer 15

Copies of endogenous proteins produced by recombinant DNA technology

Question 16

Describe what occurs in the second generation in the development of biologics

Answer 16

‘engineered’ proteins to improve the performance

Question 17

Why would you alter the amino acid sequence of insulin?

Answer 17

Faster-acting hormone - tackle diabetes

Question 18

Why would you alter the amino acid sequence of tissue plasminogen activator analogues?

Answer 18

Longer circulating half-life - tackle thrombolysis

Question 19

Why would you alter the amino acid sequence of interferon analogue?

Answer 19

for superior antiviral action

Question 20

Why would you alter the amino acid sequence of Factor VIII analogue?

Answer 20

smaller molecule, better activity - tackle haemophilia

Question 21

Why would you alter the amino acid sequence of Diphtheria toxin-interleukin-2 protein fusion protein?

Answer 21

Target toxin to appropriate cells - tackles T-cell lymphoma

Question 22

Why would you alter the amino acid sequence of Tumour necrosis factor?

Answer 22

Prolongs half-life - tackles rheumatoid disease

Question 23

What are larger molecules referred to as?

Answer 23

Biologics

Question 24

What is the new biologics?

Answer 24

engineered humanized monoclonal antibodies

Question 25

What is an example of new biologics?

Answer 25

Adalimumab (Humira) - biologic drug to treat rheumatoid arthritis

Question 26

What are more expensive, biologics or small molecule drugs?

Answer 26

Biologics

Question 27

What is pharmacogenetics?

Answer 27

the study of genetic influences on responses to drugs, usually to identify the risk of adverse reactions.

Question 28

What is pharmacogenomics?

Answer 28

use of more complex analysis of individuals genes to guide choice of drug therapy - personalised medicine.

Question 29

What is pharmacoepidemiology?

Answer 29

study of drug effects at a population level

Question 30

What is pharmaco-economics?

Answer 30

Aim to quantify the cost & benefit of drugs

Question 31

What are the 2 general principles underlying the interaction of drugs with living systems?

Answer 31

Drug molecules must exert some CHEMICAL INFLUENCE on at least 1 constituents of cells to produce a pharmacological response. Drug molecule must be BOUND to particular cells to produce an effect.

Question 32

What is the role of a receptor?

Answer 32

Recognise and response to endogenous chemical signals

Question 33

What may be used to identify and class receptors?

Answer 33

Their structure, pharmacology and signaling mechanism

Question 34

What is the effect on specificity when increasing dosage?

Answer 34

Increasing dose will cause it to affect other targets - unwanted side effects, toxicity.

Question 35

What are the 3 ways a drug can interact with a receptor?

Answer 35

- agonists - antagonists - inverse agonists

Question 36

Role of agonist

Answer 36

activation occurs and signalling occurs in cell

Question 37

Role of antagonist

Answer 37

no activation of signalling occurs in cell

Question 38

Role of inverse agonist

Answer 38

binds to receptor and shuts down constitutive activity. This leads to a decrease in signaling.

Question 39

What is an example of receptor that shows 'constitutive activity'?

Answer 39

5HT2A receptor (subtype of serotonin)

Question 40

What type of receptors are Opioid receptors?

Answer 40

G-protein coupled receptors

Question 41

What are examples of agonists of mu-opioid receptors?

Answer 41

- Enkephallins - Endorphins - Morphine - Heroine - Fentanyl

Question 42

What is an example of an antagonist of the mu-opioid receptor?

Answer 42

Naloxone

Question 43

What are blockers?

Answer 43

Drugs that act on channels that lead to permeation becoming blocked

Question 44

What are modulators?

Answer 44

Drugs that act on channels that lead to increased or decreased opening permeability

Question 45

What do local anesthetics bind to?

Answer 45

ion channels to prevent activation

Question 46

Consequence of inhibitor?

Answer 46

normal reaction inhibited

Question 47

Consequence of false substrate?

Answer 47

Abnormal metabolite produced

Question 48

Consequence of prodrug?

Answer 48

active drug produced - prodrug is inactive drug, which when processed by enzyme, becomes activated

Question 49

What 2 drugs bind to an enzyme?

Answer 49

Aspirin & Viagra

Question 50

What is an example of a false substrate?

Answer 50

cocaine - transported where neurotransmitters would usually be

Question 51

What are 2 drugs that bind to a transporter?

Answer 51

- Prozac - Digoxin