Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

IB > Medicinal Chem > Flashcards

Medicinal Chem Flashcards

1
Q

Define effective dose (ED50)

A

Dosage required to produce a therapeutic effect for 50% of tested population

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Define toxic dose (TD50)

A

Dosage required to produce a toxic effect for 50% of tested population

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Define lethal dose (LD50)

A

Dosage required to kill 50% of tested ANIMAL population

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Define therapeutic index

A

Ratio measuring the relative safety of a drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Formula for therapeutic index, differentiating between therapeutic index for animal studies and human studies

A

Animal studies = Lethal Dose/Effective Dose
Human studies = Toxic Dose/Effective Dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Define therapeutic window

A

Range of concentration of drug in the blood for it to produce the therapeutic effect without causing toxic effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Why is a narrow therapeutic window problematic?

A

Toxic levels are easily reached

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Define side effects

A

Adverse effects of drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Define tolerance

A

When the body becomes less responsive to the drugs and a larger dosage is required to produce the same effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why is a high dosage dangerous

A

Can increase the risk of dependence and increase the possibility of reaching the lethal dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Define addiction

A

Psychological or physical dependence on drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Give several withdrawal symptoms

A
  • Depression
  • Anxiety
  • Fever
  • Cold sweats
  • Nausea
  • Insomnia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Define bioavailability

A

Fraction of administered dosage that reaches target part of human body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Why does oral administration of drugs give low bioavailability?

A

Drugs can be broken down by the digestive system before they are absorbed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Ethical considerations faced by medical researchers
when developing medications

A
  • Risk to benefit ratio
  • Animal testing
  • Effects on environment
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Administration of drugs that gives the highest bioavailability is ___

A

Intravenous injection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Outline how pulmonary administration works

A

Rapid absorption into blood through the lungs which have a large surface area

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Give the equation for the conversion of salicylic acid into aspirin

A

Salicylic acid + Ethanoic anhydride –> Aspirin + Ethanoic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Reagent, catalyst and conditions for conversion of salicylic acid into aspirin

A

Reagent: Ethanoic anhydride, (CH3CO)2O
Catalyst: Concentrated sulfuric acid or phosphoric acid
Condition: Water bath

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

The conversion of salicylic acid into aspirin is a ___ reaction

A

Nucleophilic substitution/Condensation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

How does aspirin relieve pain?

A

Relieves pain by preventing the production of prostaglandins at site of pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Other than relieving pain, what therapeutic effects does aspirin have?

A
  • Anti-inflammatory (Prevents swelling)
  • Anti-pyretic (Reduces fever)
  • Anti-coagulant (Decreases blood’s ability to clot)
  • Reduces risk of strokes and heart attacks
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Side effects of aspirin

A
  • Excessive bleeding and ulceration of stomach (Synergistic effect when taken with alcohol)
  • Acidosis (Decrease in blood pH)
  • Reye’s syndrome in young children
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Define synergistic effect

A

Effect of 2 or more drugs on the body that is greater than their individual effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Outline a method to separate aspirin from a non-acidic mixture

A
  • Add NaOH to convert aspirin to its water-soluble salt
  • Separate immiscible layers
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Outline a method to purify aspirin

A

Recrystallisation using ethanol as a solvent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Why does isolation of the aspirin involve the addition of ice-cold water?

A

Aspirin has low solubility in water at low temperatures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Why is aspirin not stored in hot, humid locations?

A

Water causes hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Methods to confirm the identity of aspirin

A
  • Melting point
  • 1H NMR
  • Mass spectrometry
  • X-ray crystallography
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Methods to confirm the identity of PURE aspirin

A
  • Melting point is higher
  • Melting point is closer to literature value
  • Smaller range of melting point values
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Why is aspirin SLIGHTLY soluble in water?

A
  • Polar hydroxyl group
  • Non-polar large benzene ring
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Method to increase the solubility of aspirin in water

A
  • React aspirin with NaOH to turn it into an ionic salt
  • Ionic compounds are more soluble than covalent compounds
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Give the equation for the conversion of aspirin, C6H4(OCOCH3)COOH, into its water-soluble ionic salt

A

C6H4(OCOCH3)COOH (s) + NaOH (aq) –> C6H4(OCOCH3)COONa (aq)
+ H2O

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Why is aspirin a better alternative than paracetamol?

A

Paracetamol has a narrow therapeutic window and smaller therapeutic index

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Why is aspirin a better alternative than ibuprofen?

A

Ibuprofen can increase the risk of stomach bleeding

36
Q

How does penicillin combat bacterial infection?

A
  • Highly strained beta-lactam ring opens up
  • Irreversibly inhibits enzyme responsible for the cross-linking of bacterial cell wall
  • Results in a weakened cell wall
  • Causes bacterial cell to burst due to the high osmotic pressure caused by water from the surroundings entering the cell
37
Q

How can we mitigate the resistance of bacteria to penicillin?

A
  • Modify side chain
  • Prevents enzyme in bacteria from deactivating penicillin
38
Q

How do opiates relieve pain?

A

Block transmission of pain by binding to opioid receptors in the brain

39
Q

Other than relieving pain, what therapeutic effects do opiates have?

A

Cough suppression effects

40
Q

Why are opiates addictive?

A
  • Releases dopamine
  • Gives a feeling of euphoria
  • Interacts with opioid receptors in the brain
41
Q

Functional groups present in morphine, codeine and diamorphine are ___

A
  • Benzene
  • Amino
  • Ether
42
Q

Solubility of opiate derivatives:
Morphine > Codeine > Diamorphine
Explain why

A
  • Morphine has 2 hydroxyl groups
  • 1 of the hydroxyl groups in morphine is replaced with an ether group in codeine
  • Both hydroxyl groups in morphine are replaced with ester groups in diamorphine
  • Non-polar compounds cross the hydrophobic blood-brain barrier more easily
43
Q

Method to synthesise codeine from morphine

A

React with iodomethane (CH3I) in alkaline solution

44
Q

The synthesis of codeine from morphine is a ___ reaction

A

Nucleophilic substitution

45
Q

Why does codeine have to be metabolised into morphine first?

A
  • Steric hindrance of methyl group
  • Codeine cannot bind directly to opioid receptors
46
Q

Method to synthesise diamorphine from morphine

A

Heat morphine with ethanoic anhydride

47
Q

The synthesis of diamorphine from morphine is a ___ reaction

A

Condensation

48
Q

Outline the role of hydrochloric acid in the stomach

A
  • Provides denature proteins
  • Provides the optimum condition for pepsins and other enzymes to digest food
  • Kills bacteria ingested with food
49
Q

Outline the role of hydrogen carbonates and gastric mucus in the stomach

A

Prevents the gastric juice from digesting the stomach

50
Q

Effect of excess HCl in the stomach

A
  • Indigestion
  • Gastritis
  • Peptic ulcer
51
Q

How does an antacid combat excess HCl in the stomach?

A

Quickly reduces the acidity of the gastric juice by neutralising excess acid and increasing the pH

52
Q

Why do antacids usually contain a mixture of 2 or more ingredients?

A
  • Counteract undesirable side effects
  • Some ingredients might be slower
53
Q

Define the role of antifoaming agents in antacids

A

Relieve bloating by allowing CO2 to coalesce and leave as flatulence

54
Q

Define the role of alginates in antacids

A

Produces protective layer that floats on stomach content and prevents heartburn

55
Q

Outline how Ranitidine and Zantac work

A

Binds to H2 histamine receptor which stops the production of acid
- Binds to same H2 receptors as histamine –> Blocks histamine binding to H2 receptor

56
Q

Outline how Omeprazole and Esomeprazole work

A

Binds to gastric proton pump thus preventing the release of H+ ions into the stomach

57
Q

Outline how metabolites work

A

Drugs are changed into the active form (metabolites) after being processed by the body

58
Q

Reasons for making drugs in different forms (metabolites)

A
  • Avoid side effect
  • Longer shelf life
  • Easier storage
  • Allow drug to be more soluble in water
  • Target drugs for specific areas
59
Q

Why is it important to maintain the pH of the body within certain strict limits

A

To ensure enzymes function correctly

60
Q

Define a buffer solution

A

Solution which resists changes in pH when small amounts of acid or alkali are added to them

61
Q

Data booklet:
pH = pKa + log [A-]/[HA]
What do A- and HA mean?

A

[A-] = Concentration of conjugate base
[HA] = Concentration of acid

62
Q

Difference between virus and bacteria

A
  • Bacteria have cell walls and viruses do not
  • Bacteria perform living functions on their own and viruses do not without a host cell
  • Bacteria affected by antibiotics while viruses are not
63
Q

Why are viruses considered non-living organisms?

A

Viruses lack cell structure and do not grow or reproduce

64
Q

Ways in which antiviral drugs work

A
  • Prevents attachment of virus to host cell
  • Blocks enzyme activity in the host cell so viruses cannot use it to multiply
  • Prevents new virus from leaving host cell
65
Q

Outline how Oseltamivir and Zanamivir work

A
  • Blocks NA viral enzyme which allows viruses to pass through cell membrane
  • Prevents virus from leaving host cell so it cannot infect other cells
66
Q

Functional groups present in both Oseltamivir and Zanamivir are ___

A
  • Carboxamide
  • Ether
  • Carbonyl
  • Amino
  • Alkenyl
67
Q

Why is oseltamivir inactive in its original form?

A
  • Presence of ester group
  • Turned into acidic metabolite once ester is hydrolysed in body
68
Q

Difficulties with eradicating AIDS/HIV virus include ___

A
  • Virus mutates quickly (can adapt to drugs)
  • Makes people vulnerable to other infections
  • Virus attacks immune system
  • Each kind of virus requires special drugs
  • Difficult to attack virus without attacking host cell
69
Q

Source of pharmacologically active compounds (waste)

A
  • Incorrect disposal of drugs in hospitals and pharmacological industries
  • Incorrect disposal of waste products from pharmacological industries in particular organic and/or chlorinated solvents
  • Use of antibacterial drugs in agriculture and animal husbandry
70
Q

Detrimental effects of pharmacologically active compounds (waste) in the environment

A
  • Increased resistance of bacteria to current drugs
  • Carcinogenic
  • Cause damage to internal organs of living organisms
  • Changes in metabolism and behaviours of organism
71
Q

Environmental effect of chlorinated solvents

A

Contribute to greenhouse gases and ozone depletion

72
Q

Why must chlorinated solvents be incinerated at high temperatures?

A

To prevent the formation of carcinogens

73
Q

Preventive/corrective measures for pharmacologically active compounds (waste)

A
  • Ensure proper treatment of drugs before disposal
  • Restrict antibiotic therapy to bacterial infections
  • Controlled use in agriculture
  • Use of alternative solvents such as supercritical fluid
74
Q

Define low-level nuclear waste

A

Nuclear waste that has low radioactivity and usually contains isotopes with short half-lives

75
Q

Source of low-level nuclear waste

A

Contaminated surgical/clinical instruments

76
Q

Outline the proper disposal of low-level nuclear waste

A
  • Stored on site until decay activity is safe and then disposed of as ordinary waste
  • Incineration
77
Q

Define high-level nuclear waste

A

Nuclear waste that has high radioactivity and usually contains isotopes with longer half-lives

78
Q

Source of high-level nuclear waste

A

Nuclear reactors

79
Q

Outline the proper disposal of high-level nuclear waste

A
  • Vitrification
  • Storage underground in concrete bunkers
80
Q

Dangers of high-level nuclear waste

A
  • Carcinogenic
  • Can cause birth defects
  • Weaken immune system
  • Cause DNA mutation in living organisms especially in bacteria
81
Q

Outline some principles of green chemistry

A
  • Minimise number of steps in synthesis
  • Maximise atom economy
  • Use as little solvent and energy as possible
  • Recover/reuse solvents
  • Use water as a solvent
82
Q

How can antibiotic use affect the environment?

A
  • Leads to antibiotic resistance in bacteria/microorganisms
  • Destroys useful bacteria
83
Q

Outline the synthesis of oseltamivir using green chemistry

A
  • Synthesis from petrochemicals involves huge quantity of materials and generates large amounts of waste
  • Current synthesis uses shikimic acid, a natural product extracted from Chinese star anise or fermentation of glucose by GM bacteria
  • Current synthesis cuts down on number of steps and reduces energy consumption
84
Q

Common hazardous solvents

A
  • Methanol
  • Formaldehyde
  • Chlorinated solvents
  • Benzene
85
Q

Give some green solutions to the problem of organic solvent waste

A
  • Use of alternative solvents such as supercritical fluids
  • Use of water as solvent
  • Use solvent-free reactions
  • Recycle waste solvents
  • Catalysis that leads to better/higher yield
  • Reducing number of steps

IB (2 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions