Lecture 1 - introduction Flashcards

1
Q

What is pharmacology?

A

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

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2
Q

Where is morphine derived from?

A

Poppy - synthesis achieved in 1950s

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3
Q

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

A

Heroin

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4
Q

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

A

Aspirin

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5
Q

What can endorphins be referred to as?

A

a self-made form of pain relief

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6
Q

What is a drug?

A

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

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7
Q

What are 3 types of drugs?

A
  • synthetic chemical (heroin)
  • plant chemical (morphine from poppy)
  • biopharmaceutical (generated through the biotech industry)
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8
Q

What is a medicine?

A

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

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9
Q

What else do medicines contain other than drugs?

A
  • excipients
  • stabilizers
  • solvents
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10
Q

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

A

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

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11
Q

How might you engineer proteins?

A

Change the properties of insulin to last longer

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12
Q

What is gene therapy?

A

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

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13
Q

Describe what you can use DNA technology for

A
  • therapeutic monoclonal antibodies
  • recombinant hormones
  • siRNA
  • mRNA
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14
Q

Describe an example of regenerative medicine

A

Engineered stem cells to replace irreparably damaged organs

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15
Q

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

A

Copies of endogenous proteins produced by recombinant DNA technology

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16
Q

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

A

‘engineered’ proteins to improve the performance

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17
Q

Why would you alter the amino acid sequence of insulin?

A

Faster-acting hormone - tackle diabetes

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18
Q

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

A

Longer circulating half-life - tackle thrombolysis

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19
Q

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

A

for superior antiviral action

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20
Q

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

A

smaller molecule, better activity - tackle haemophilia

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21
Q

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

A

Target toxin to appropriate cells - tackles T-cell lymphoma

22
Q

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

A

Prolongs half-life - tackles rheumatoid disease

23
Q

What are larger molecules referred to as?

A

Biologics

24
Q

What is the new biologics?

A

engineered humanized monoclonal antibodies

25
Q

What is an example of new biologics?

A

Adalimumab (Humira) - biologic drug to treat rheumatoid arthritis

26
Q

What are more expensive, biologics or small molecule drugs?

A

Biologics

27
Q

What is pharmacogenetics?

A

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

28
Q

What is pharmacogenomics?

A

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

29
Q

What is pharmacoepidemiology?

A

study of drug effects at a population level

30
Q

What is pharmaco-economics?

A

Aim to quantify the cost & benefit of drugs

31
Q

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

A

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.

32
Q

What is the role of a receptor?

A

Recognise and response to endogenous chemical signals

33
Q

What may be used to identify and class receptors?

A

Their structure, pharmacology and signaling mechanism

34
Q

What is the effect on specificity when increasing dosage?

A

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

35
Q

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

A
  • agonists
  • antagonists
  • inverse agonists
36
Q

Role of agonist

A

activation occurs and signalling occurs in cell

37
Q

Role of antagonist

A

no activation of signalling occurs in cell

38
Q

Role of inverse agonist

A

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

39
Q

What is an example of receptor that shows ‘constitutive activity’?

A

5HT2A receptor (subtype of serotonin)

40
Q

What type of receptors are Opioid receptors?

A

G-protein coupled receptors

41
Q

What are examples of agonists of mu-opioid receptors?

A
  • Enkephallins
  • Endorphins
  • Morphine
  • Heroine
  • Fentanyl
42
Q

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

A

Naloxone

43
Q

What are blockers?

A

Drugs that act on channels that lead to permeation becoming blocked

44
Q

What are modulators?

A

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

45
Q

What do local anesthetics bind to?

A

ion channels to prevent activation

46
Q

Consequence of inhibitor?

A

normal reaction inhibited

47
Q

Consequence of false substrate?

A

Abnormal metabolite produced

48
Q

Consequence of prodrug?

A

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

49
Q

What 2 drugs bind to an enzyme?

A

Aspirin & Viagra

50
Q

What is an example of a false substrate?

A

cocaine - transported where neurotransmitters would usually be

51
Q

What are 2 drugs that bind to a transporter?

A
  • Prozac
  • Digoxin