Option D: Medicinal Chemistry Flashcards

1
Q

What are the five methods of drug administration?

A
  • Orally (through mouth)
  • Parenterally (through injection)
  • Inhalation
  • Rectally
  • Transdermally (through application to skin)
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2
Q

What are the three parenteral methods of drug admministration?

A
  • Subcutaneous (under skin)
  • Intramuscular (into muscle)
  • Intravenous (into vein)
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3
Q

What is the effective dose (ED50)?

A

The minimum amount of bioactive compound required to cause a therapeutic effect in half the population

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4
Q

What is the toxic dose (TD50)?

A

The minimum amount of bioactive compound required to cause an unacceptable adverse effect in half the population

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5
Q

What is the lethal dose (LD50)?

A

The minimum amount of bioactive compound required to kill half the animal population

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6
Q

How is the therapeutic index (TI) measured?

A

TI = TD50 / ED50

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7
Q

What is the therapeutic window?

A

The range of values between ED50 and TD50

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8
Q

What is bioavailability?

A

The fraction of administered dosage that enters the bloodstream (or reaches target organ)

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9
Q

Why do drugs taken orally have a lower bioavailability than drugs administered intravenously?

A
  • Not all drug absorbed
  • Some destroyed by enzymes/stomach acid
  • some metabolised due to first-pass effect (first destination is liver where bioactive compound may be metabolised and cleared)
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10
Q

What is the importance of polar and non-polar groups in drugs?

A
  • Polar groups are soluble in water
  • Non-polar groups can pass through hydrophobic cell membranes and blood-brain barrier
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11
Q

What are side effects?

A

Non-beneficial/unintentional effects a drug has on the body

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12
Q

What is tolerence?

A

When a person needs an ever increasing amount of a drug to gain the desired effect

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13
Q

What is addiction?

A

A compulsion to keep taking a drug

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14
Q

How do drugs interact with the body?

A

Bioactive compound must interact with and fit the biding site of an enzyme or cellular receptor

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15
Q

What are the two ways companies identify a lead compound?

A
  • Screening of a large library of compounds
  • Seeking to improve an existing compound
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16
Q

What are five factors to consider when choosing a compound for clinical trials

A
  • yield of required drug
  • cost to synthesize drug
  • side effects
  • solubility of drug
  • chemical stability of compound
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17
Q

What is the placebo effect and how can it be prevented?

A

Patients report an improvement in condition without taking the drug. This can be prevented by using a placebo (medicine without the active ingredient) and a double-blind trials where neither patients nor doctros know if the patient has a placebo

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18
Q

Which plant is salicylic acid obtained from?

A

Willow bark

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19
Q

What does an analgesic drug do?

A

A drug that relieves pain

20
Q

What does an anti-inflammatory drug do?

A

A drug that reduces swelling

21
Q

What does an antipyretic drug do?

A

A drug that reduces fever symptoms

22
Q

What does an anticoagulant drug do?

A

A drug that thins the blood (reducing blood clotting)

23
Q

How does aspirin relieve pain?

A

It binds irreversibly with COX, preventing it from releasing prostaglandins

24
Q

What is a prostaglandin?

A

A lipid responsible for transmission of pain receptors in the brain

25
Q

What is a prophylactic?

A

A medicine that is taken as a preventative measure

26
Q

What is a synergistic effect?

A

When one drug increases the effectiveness of another

27
Q

How can you improve the solubility of aspirin in water?

A

Deprotonise the carboxylic acid group with NaOH to create a carboxylic salt (soluble ionic compound)

28
Q

Why do most ionic compounds dissolve well in water?

A

Salts form ion-dipole attractions with water molecules and become well solvated

29
Q

How was penicillin discovered?

A

Alexander Fleming left a petri dish with bacteria in open and a blue-green mold formed (penicillium), inhibiting the growth of bacteria

30
Q

Why is a beta-lactam ring very prone to attack by nucleophiles?

A

It has very small bond angles of 90 degrees, creating lots of ring strain

31
Q

How does penicillin kill bacteria?

A
  • opens the beta-lactam ring
  • binds irreversibly with transpeptidase enzyme
  • preventing cross-linking in cell walls and weakening them
  • causing cells to fill with water due to osmotic pressure and burst and die
32
Q

What defense have resistant-bacteria developed to penicillin?

A

Synthesis of penicillinase (deactivates penicillin before it can react with transpeptidase enzyme)

33
Q

What are the three main causes of antibiotic resistance?

A
  • Over-prescription (exposes lots of bacteria to penicillin meaning only
    resistant ones survive and multiply)
  • Poor patience compliance (stop antibiotics course early as they feel better)
  • Agriculture (antibiotics used in livestock to keep animals healthy but still present in meat and dairy)
34
Q

What are MDR bacteria and how should they be treated?

A

Multidrug resistant bacteria that should be treated with a cocktail of drugs

35
Q

What is opium extracted from?

A

Opium poppies

36
Q

How do mild analgesics relieve pain?

A

They block transmission of pain impulses at injury site

37
Q

How do strong analgesics relieve pain?

A

They block opioid receptors in the brain so they can’t receive pain impulses

38
Q

What is a prodrug?

A

An inactive drug which is metabolised into and active drug in the body

39
Q

Which sort of compounds pass easily from the bloodstream into the brain?

A

Non-polar compounds

40
Q

What are withdrawal symptoms?

A

Abnormal physical or psychological features following the abrupt discontinuation of a drug addiction

41
Q

What are the roles of pepsin and hydrochloric acid in gastric juice?

A
  • Pepsin: enzyme that breaks proteins into amino acids and peptides
  • Hydrochloric acid: kills germs, denatures proteins, provides optimum pH
    for enzymes
42
Q

What are antacids?

A

Weak Bronsted-Lowry bases that neutralise excess stomach acid

43
Q

What’s the purpose of antifoaming agents?

A

Allows CO2 to coalesce to help it escape easier

44
Q

What’s the purpose of alginates?

A

Forms a layer on top of gastric acid preventing it from rising into the oesophagus and causing heartburn

45
Q

How do ranitidine, omeprazole and esomeprazole regulate acid secretion?

A
  • Ranitidine: blocks H2-histamine receptors, preventing histamine from releasing stomach acid
  • Omeprazole and esomeprazole: inhibit the proton pump enzyme, preventing the release of H+ ions (lasts longer than ranitidine)