Med Chem Flashcards

1
Q

Define drug.

A

A natural, synthetic or semisynthetic substance the results in 1 or more of the following changes within the body: alters incoming sensory sensations, alters mood or emotions or alters the physiological state, including consciousness, metabolic activity level or coordination.

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2
Q

Define LD50.

A

The lethal dose required to kill 50% of the animal test population.

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3
Q

Define ED50.

A

The effective dose required to bring about a measurable effect in 50% of the test animal population.

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4
Q

Define TD50.

A

The toxic dose for 50% of the human test population.

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5
Q

Define therapeutic window.

A

The range of dosages between the minimal dose required to produce a therapeutic effect and a harmful effect due to toxicity at high dosage.

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6
Q

Define side effects.

A

Unintended, unwanted and sometimes harmful or unpleasant effects that appear with a dose within the therapeutic window.

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7
Q

Define tolerance.

A

Occurs as they body’s immune system and target cells adapts to the continued presence of a drug. It raises the risk of dependence and reaching a toxic or lethal dose.

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8
Q

Define agonistic drug.

A

The drug molecule acts in a very similar way to the normal ligand, activating the receptor upon binding and producing a similar biological response.

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9
Q

Define antagonistic drugs.

A

The drug molecule blocks the ligand-binding site and stops the natural ligand from binding and activating the receptor.

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10
Q

Define allosteric drugs.

A

The drug molecule binds to a site on the surface of the protein other than the substrate binding site. This action changes the 3D shape of the protein which may increase or decrease the receptor’s response to the natural substrate (ligand).

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11
Q

Define bioavailability.

A

The fraction of an administered dose of drug that reaches the bloodstream.

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12
Q

Define a prophylactic.

A

A medicine used to treat or prevent the occurrence of a disease or condition.

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13
Q

Define antibiotics.

A

Substances that kill bacteria or inhibit the growth of bacteria.

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14
Q

Define bacteria.

A

Single-celled microorganisms.

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15
Q

What is the beta-lactam ring ?

A

It is a strained 4 membered cyclic amide.

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16
Q

What is the difference between broad-spectrum antibiotics and narrow-spectrum antibiotics ?

A

Broad-spectrum antibiotics are active against a wide range of bacterial diseases/strains while narrow-spectrum antibiotics are active against a small range of bacterial diseases/strains.

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17
Q

What is Penicillin G?

A

The first penicillin to be developed but it had to be injected intravenously because it was hydrolysed by acid in stomach.

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18
Q

Define opiates.

A

Natural narcotic analgesics that are derived from the opium poppy.

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19
Q

Define alkaloids.

A

Nitrogen-containing bases extracted from plants.

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20
Q

Define pro-drug.

A

A biologically inactive compound which can be metabolised into a drug.

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21
Q

Define Placebo.

A

an inert chemical which resembles the drug in apparence and taste but has no bioactive chemicals

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22
Q

What is the placebo effect ?

A

occurs when a placebo promotes the ‘natural healing’ of the human immune and endocrine system

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23
Q

What is synergistic effect?

A

Occurs when the combination of 2 drugs is greater than either individual effect.

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24
Q

Define methadone.

A

A synthetic opioid which is frequently used to treat heroin addicts. It produces many of the same effects as opioids but not euphoria + long-term effects + blocks heroin withdrawal symptoms.

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25
Q

Define dyspepsia.

A

Also known as indigestion and occurs when excess gastric juice is secreted by the stomach and there is reflux into the oesophagus.

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26
Q

Define antacids.

A

Medicines to reduce excess HCl in the stomach.

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27
Q

Define prostaglandin.

A

substances that are responsible for pain and inflammation

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28
Q

Define acidosis.

A

lowering of the pH of blood

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29
Q

What is rational drug design ?

A

The design of drugs to specifically work for their respective targets.

30
Q

Define retrovirus.

A

A virus where the viral DNA becomes integrated to the host’s DNA and may not kill the host unit or cause any obvious illness until years later.

31
Q

What is vitrified ?

A

It means turn into a glass like inert material. Used to dispose of HLW

32
Q

Define green chemistry.

A

Aims to minimise production & use of hazardous chemicals to reduce pollution and conserve natural resources.

33
Q

What is Taxol ?

A

A chemotherapeutic agent also known as paclitaxel. Used to treat cancers of ovary, brain, breasts and lungs.

34
Q

Define chiral auxiliary.

A

A chiral control element temporarily incorporated into the structure of a substrate in order to direct the stereochemistry at new stereogenic centre(s) formed in a reaction. The chiral auxiliary is then removed and may be reused.

35
Q

What is a prochiral molecule?

A

A molecule that can be converted from achiral to chiral in a single step.

36
Q

What is a diastereoselective reaction?

A

A reaction in which in diastereomer is formed in preference to another.

37
Q

Define nuclear medicine.

A

The use of radioactive materials in medicine for diagnostic imaging and therapy.

38
Q

Define targeted radionuclide therapy. What are its side effects? What cancers is it used for ?

A

It involves introducing a radioisotope by injection or ingestion.
Side effect: may damage normal cells.
Used for melanoma, leukemia or breast cancer.

39
Q

Define positron.

A

A particle that has the same mass as an electron but an opposite charge.

40
Q

What is BNCT and what is it used for ?

A

Boron Neutron Capture Therapy. Used for neck and brain cancers.

41
Q

What radiation does lutetium-177 emit and what tumours is it good for?

A

Emits beta and gamma radiation. Good for small tumours as it has a shorter penetration range than Yttrium-90.

42
Q

What radiation does Yttrium-90 emit ?

A

Beta radiation.

43
Q

What is Bragg peak effect ?

A

When the absorption of protons reaches a maximum within a narrow range, deep inside the patient’s body.

44
Q

What does the m in Technetium-99m mean ?

A

Metastable nuclide. Means that the nucleons in its nucleus are at a higher energy level than the stable Tc nucleus.

45
Q

What are the side effects of radiotherapy ?

A

Hair loss, nausea, fatigue, loss of appetite, sterility, DNA mutation.

46
Q

What is a fractionating column ?

A

A column packed with beads, resin, glass tubes & rings to provide large surface area for liquids & vapour to be in contact. The most efficient fractionating columns are long and densely packed.

47
Q

What are theoretical plates in fractional distillation ?

A

The number of steps which can be drawn on the b.p composition diagram.

48
Q

Define mole fraction.

A

The amount in moles of one component divided by the total amount in moles in the solution or mixture.

49
Q

State Raoult’s law.

A

In a mixture of 2 miscible liquids at equilibrium, each component will exert a vapour pressure proportional to its mole fraction.

50
Q

Define steroids.

A

Molecules that contain 4 rings fused together.

51
Q

What are aspirin’s properties and what is its mode of action?

A

Properties: antipyretic, anti-inflammatory, blood thinner.
Mode of action: works directly at the site of injury by inhibiting the enzyme that catalyses the formation of prostaglandins which prevents transmission of pain.

52
Q

What are the side effects of aspirin and what is the synergistic effect with alcohol?

A

Side effects: bleeding of stomach lining, when very large dose is taken acidosis.
Synergistic effect with alcohol: increased risk of bleeding of stomach lining.

53
Q

How is aspirin synthesised?

A

From the esterification of salicylic acid & ethanoic anhydride.

54
Q

What is penicillin and what is its mode of action?

A

Penicillin is an antibiotic.
Mode of action: penicillin inhibits the enzyme that catalyses the formation of cross-links in bacterial cell walls. Without these cross-links, bacterial cell walls are permeable to water so water enters by osmosis & cell bursts.

55
Q

How does the enzyme penicillinase cause antibiotic resistance and how to prevent it?

A

It breaks the peptide bond in the beta-lactam ring. But its activity can be reduced with inhibitors like clavulanic acid or different side chains.

56
Q

What are effects of opiates and what is their mode of action? Why are they addictive?

A

Short-term effects: euphoria, analgesic properties, vasodilation.
Long-term effects: reduced appetite, risk of HIV, constipation.
Mode of action: cross the blood-brain barrier & bind to opioid receptors in the brain which prevents transmission of pain.
Addictive because there are withdrawal effects.

57
Q

What are the distinct functional groups of morphine, diamorphine and codeine?

A

Morphine: 2 -OH
Codeine: 1 additional ether
Diamorphine: 2 ester groups.

58
Q

What is the common structural feature of morphine, diamorphine & codeine?

A

Phenylamine chemical moiety gives it rigidity & allows it to interact strongly with opioid receptors.

59
Q

What is Ranitidine/Zantac?

A

Inhibits the secretion of HCl due to its similar structure to histamine.

60
Q

What are omeprazole/prisolec & esomeprazole/nexium? How do they work ?

A

Synthetic proton pump inhibitors. Bind to proton pump enzyme by binding to a specific amino acid through a disulphide bond.

61
Q

How do antiviral medication work?

A
  • Prevent genetic material from being injected into the host cell (prevents replication),
  • inhibits the uncoating process (prevents replication),
  • inhibits replication,
  • prevent newly-replicated viruses from being released,
  • inhibits reverse transcriptase in retroviruses.
62
Q

How is HIV treated?

A

With a cocktail of drugs because retroviruses mutate fast.

63
Q

How do oseltamivir (Tamiflu) and zanamivir (Relenza) work?

A

Competitive inhibitors for neuronimidase which prevents the new viruses from leaving the host cell.

64
Q

What is the green synthesis of oseltamivir?

A

Genetically modified E.Coli undergo fermentation and the cells are broken down to form shikimic acid.

65
Q

What is the green synthesis of Taxol?

A

It is extracted from the needles of the European Yew tree because the needles regrow.

66
Q

What radiation do Pb-212 and Ra-223 emit?

A

Alpha.

67
Q

What is TLC and what are its advantages?

A

It is a thin layer of powdered solid (aluminium or silica) on a glass/plastic sheet.
Advantages : solvent front moves quicker than normal paper chromatography & a variety of mixtures/solvents can be used.

68
Q

What radiation does Technetium-99m emit ?

A

Gamma

69
Q

What are some ethical implications of nuclear medicine ?

A
  • poses risk of cancer to health worker.
  • lack of education.
  • proper disposal of radioactive waste.
70
Q

Why is Technetium-99m the most common radioisotope ?

A
  • Half life of 6 hours is long enough for scan to occur but short enough to not expose the body to too much radiation
  • decay released gamma rays which are less likely to be absorbedy by cells
71
Q

How do you synthesise codeine from morphine ?

A

CH3I in alkaline solution