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Study > Medicinal Chemistry > Flashcards

Medicinal Chemistry Flashcards

1
Q

drug

A

any chemical that affects the body

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2
Q

bioavailability

A

how much a drug reaches its target in the body

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3
Q

effective dose

A

the minimum amount required for the therapeutic effect for 50% of the population

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4
Q

toxic dose

A

the amount causing unacceptable effects for 50% of the population

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5
Q

therapeutic index

A

the ratio of the toxic dose to the effective dose for humans. the ratio of the lethal dose to the effective dose for animals – the larger the window, the better

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6
Q

How is aspirin made?

A

salicin –> salicylic acid –> aspirin. for the second arrow, an acid catalyst is needed (ex. ethanoic anhydride ) – there is more detail about this I need to add

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7
Q

Aspirin

A

mild analgesic that intercepts pain stimulus at the source

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8
Q

Side effects of aspirin

A

reduces blood clotting, which can be used against stroke and heart attacks. It can cause irritation/ulceration in the stomach & intestines, liver/brain disorders in children, and allergies. It also shows synergy when taken with alcohol.

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9
Q

Penicillin

A

antibiotics produced by fungi, cyclic amide ( beta-lactam 4-membered ring ), that reacts with bacterial enzyme transpeptidase, inactivating it, and interfering w/ bacterial cell wall synthesis

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10
Q

opiates

A

natural narcotic analgesics derived from the opium poppy that intercept the pain response of humans before the perception of pain is received

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11
Q

narcotic effects

A

influences mood and behaviour

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12
Q

side effects of opiates

A

the feeling of contentment, addiction/dependence, constipation, cough suppression, pupil constriction

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13
Q

features of addiction

A

withdrawal symptoms – craving, sweat/chills, anxiety, irritability, muscle aches, increased heart rate, nausea, vomiting, diarrhea

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14
Q

what features of a drug molecule make it easier for it to cross the blood-brain barrier

A

less polar molecules, hydrophobic molecules. Large hydrophilic molecules cannot easily cross barriers.

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15
Q

codeine

A

an opioid pain reliever used to treat mild to moderately severe pain. less effective than morphine as it binds more weakly to opioid receptors in the brain

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16
Q

morphine

A

used to treat severe pain. Esterification of morphine makes diamorphine ( heroin ) and etherification of morphine makes codeine

17
Q

diamorphine

A

narcotic analgesics used in the treatment of severe pain (heroin)

18
Q

buffer

A

mixture of a weak acid and one of its salts or a weak base and one of its salts that resists changes in pH due to small amounts of added acid or alkali

19
Q

What happens when there is excess stomach acid?

A

It can lead to indigestion and ulceration

20
Q

histamine

A

hormone that produces acid production in the stomach

21
Q

What are the 4 different methods to reduce acid production?

A
  1. block histamine receptors
  2. inhibiting the release of acid from parietal cells using the enzyme H+/K+ ATPase
  3. using a proton pump inhibitor
  4. neutralizing the acid with a base
22
Q

omeprazole

A

treat excess acid in the stomach. proton pump inhibitor

23
Q

What are the typical bases used to neutralize the acid?

A

Ca(OH)2, Mg(OH)2, Al(OH)3, NaHCO3, Na2CO3

24
Q

How do antiviral drugs work?

A

Either alter the cell host genetic material so the virus cannot use the cells to multiply or block the neuraminidase enzyme activity within the host cell

25
Q

Virus

A

small making it difficult to target w/ drugs, contains DNA or RNA, simple w/ nuclear material & protein coat, only replicates by taking over the host cell, has rapid multiplication & genetic mutation

26
Q

What is the life cycle of a virus?

A

1) The virus attaches to the surface of the host cell
2) viral DNA/RNA enters the host cell
3) viral DNA/RNA replicates and new viral protein is formed
4) new viral particles are assembled
5) host cell burst releasing new virus

27
Q

Oseltamivir

A

antiviral medication is used to treat infections caused by viruses. It is a neuraminidase inhibitor made from shikimic acid, found in star anise

28
Q

Zanamivir

A

antiviral medication is used to prevent and treat infections caused by influenza. it is a neuraminidase inhibitor

29
Q

AIDS

A

acquired immune deficiency syndrome (AIDS) is a chronic condition caused by HIV

30
Q

HIV

A

Human immunodeficiency virus (HIV) attacks the body’s immune system and affects the white blood cells. It is a retrovirus containing RNA which is difficult to treat, mutates rapidly, and can lay dormant for long periods of time.

31
Q

How to treat HIV and AIDS?

A

use antiretroviral drugs. it will suppress the virus but cannot eliminate it.

32
Q

What is the largest waste product of the pharmaceutical industry?

A

Solvent – any substance that is capable of dissolving one or several substances

33
Q

Which solvents are best to use in terms of environmental impact?

A

low toxicity, safe to use, does not harm the environment when released or burned

34
Q

Good solvents

A

ethanol, water, carbon dioxide

35
Q

Bad solvents

A

tetrachloromethane, benzene

36
Q

Chlorinated solvents

A

industrial chemicals that are useful in organic synthesis – low reactivity, good solubility properties, but damage the ozone layer, cause organ damage, and release toxic compounds

37
Q

levels of waste

A

high-level waste – releases high levels of ionizing radiation for a long time
low-level waste – releases low levels of ionizing radiation for a short time

38
Q

antibiotic resistance

A

caused by widespread use of antibiotics which creates bacterial superbugs resistant to antibiotics

39
Q

antibiotics

A

medicines that fight bacterial infections in people and animals

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