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Chemistry > D.1 Pharmaceutical Products and Drug Action > Flashcards

D.1 Pharmaceutical Products and Drug Action Flashcards

1
Q

What is the therapeutic index (TI) in animal studies?

A

Lethal Dose of a drug for 50% of the population (LD50) divided by the minimum effective dose for 50% of the population (ED50)
(LD50) / (ED50)

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2
Q

What is the therapeutic index (TI) in humans?

A

Toxic dose of a drug for 50% of the population (TD50)
divided by the minimum effected dose for 50% of the population (ED50)
(TD50) / (ED50)

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3
Q

What is the therapeutic window?

A

The range of dosages between ineffective amounts of drug and a toxic dose of the drug.

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4
Q

Consideration of drug administration?

A

Dosage, tolerance, addiction and side-effects

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5
Q

What is bioavailability?

A

The fraction of the administered dosage that reaches the target part of the human body

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6
Q

What does bioavailability depend on?

A

Solubility, polarity of molecules, and functional groups present

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7
Q

What reduces the bioactivity of hydroxyl, carboxyl, and amino groups?

A

They are polar and usually soluble in water
Can be absorbed through GI (gastrointestinal) tract into the bloodstream
May not pass across non-polar membranes easily -> reduces their bioactivity

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8
Q

What is dosage?

A

How much of a drug to administer

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9
Q

Main steps in development of synthetic drugs

A
  1. Identifying need and structure
  2. Synthesis
  3. Yield
  4. Extraction
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10
Q

Drug-receptor interaction

A

based on structure of the drug and the site of activity

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11
Q

Why should animal and human test of drugs be kept to a minimum?

A

For ethical and environmental reasons

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12
Q

What is medicinal chemistry?

A

Discovery, digan, development of bioactive compound that can be used to therapeutically alleviate symptoms of conditions, cure diseases or help diagnose medical issues.

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13
Q

Determination of risks and benefits of drugs

A

medicines go through a variety of tests to determine their effectiveness and safety before being made commercially available.

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14
Q

List the effects of medicines and drugs on the functioning of the body

A
  1. Alters the physiological state, consciousness, activity level, or coordination.
  2. Alters incoming sensory senation
  3. Alters mood or emotions
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15
Q

What is the therapeutic effect?

A

Beneficial effect of medical treatment

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16
Q

What is the placebo effect?

A

Phenomenon where a patient believing they are given a medication experience the benefits even when not taking the medicine.

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17
Q

What must be used during the development of new drugs?

A

Placebo to compare the results of drug vs. placebo (no drug)

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18
Q

What is the Therapeutic Index (TI) in relation to the Therapeutic Window?

A

The relative margin of safety of a drug for a particular treatment. TW can be quantized as TI.

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19
Q

TI in animals

A

(LD50) / (ED50)

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20
Q

TI in humans

A

(TD50) / (ED50)

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21
Q

What happens when TI is large?

A

This would happen when there is a small ED50 and a large LD50
(Large difference between the therapeutic amount and toxic amount)
Meaning that it takes a large amount of the drug to overdose

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22
Q

What happens when TI is small?

A

This would happen when there is a large ED50 and a small LD50
(Small difference between the therapeutic amount and toxic amount)
Meaning that it takes a small amount of the drug to overdose

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23
Q

Why is a high TI desirable in a drug?

A

High TI means that there is a greater amount needed of the specific drug to overdose, meaning it is hard to overdose.

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24
Q

What is the TI order of Morphine, penicillin, cocaine, ethanol, and warfarin? As well as their therapeutic effects?

A

in decreasing value of therapeutic index (highest and the top)
1. Penicillin -> antibiotic
2. Morphine -> analgesic
3. Cocaine -> stimulant
4. Ethanol -> depressant
5. Warfarin -> anticoagulant in blood

25
Q

How does tolerance build up?

A

Over time and with regular use

26
Q

What does tolerance mean in the effect of a drug?

A

over time the user may need increasing amounts of a drug to achieve the same desired physiological effect.

27
Q

What is the risk of a tolerance build-up?

A

Increases health hazards and risk of fatal overdose

28
Q

What can happen if a user takes the same amount of a drug after a long period of time?

A

tolerance may have decreased, size of the dose that the user used may be enough for an overdose.

29
Q

What is a side effect?

A

The unwanted responses of a drug.
To achieve the main effect, side effects must be tolerated.

30
Q

Which organs are usually damaged as a side effect of medication and why?

A

Most drugs are concentrated, metabolized, and excreted by kidneys and liver. Side effects can damage these organs.

31
Q

What are the physiological effects of a drug?

A

The therapeutic effect that is intended
Along with the side-effects that are unintended

32
Q

What is dependence?

A

When a person continues to use a drug because they don’t feel right without it.
An intense craving for the drug.

33
Q

What is physical dependence?

A

When the body cannot perform normally without the drug.

34
Q

Symptoms of physical dependence

A

fever
convulsions
(Withdrawal)
can be fatal

35
Q

What is Psychological dependence?

A

The drug becomes central to a person’s thoughts and they can’t stop using it or thinking about it.
(Addiction)

36
Q

Ways of administering drugs

A
  1. Orally -> pills
  2. Inhalation -> ventilin
  3. Rectal -> through anus
  4. Injected
    a. intravenous
    b. intramuscular
    c. subcutaneous
  5. Topical
37
Q

Why are there different methods for drug administration?

A

Methods vary in the speed at which the medicine reaches the blood.

38
Q

What are the levels of the skin tissue?

A
  1. Epidermis
  2. Dermis
  3. Subcutaneous tissue
  4. Muscle
  5. Vein
39
Q

Where are subcutaneous, intravenous, and intramuscular administrations injected?

A

Subcutaneous -> injected directly under surface of the skin
Intravenous -> injected directly into bloodstream
Intramuscular -> injected directly into a muscle

40
Q

What affects oral bioavailability?

A

Formulation of tables
Their solubility
How easily they are absorbed through intestinal wall
Susceptibility to being broken down by enzymes in gut and liver

41
Q

What is the first-pass effect?

A

The relatively low bioavailability of a drug taken orally.
20 - 40% of an orally ingested drug may reach bloodstream.

42
Q

Why is there low bioavailability in orally ingested drugs?

A

After swallowing, drugs pass into digestive system. Enzymes may alter them chemically.
Then passed in blood to liver where further metabolic breakdown occurs

43
Q

What is the difference in dosage between oral and IV?

A

Oral needs to be about 4x higher than IV

44
Q

First-pass metabolism pathway

A
  1. Swallowed drug
  2. Digestive system
  3. Hepatic portal system
  4. Liver
  5. Rest of the body
45
Q

Why is water solubility important?

A

For circulation in the aqueous solution in the blood. Only individual molecules of a drug can pass through wall of intestine. Water is the medium of GI.

46
Q

Why is lipid solubility important?

A

Lipid solubility helps in the passage of the drug through membranes during absorption

47
Q

Factors that affect solubility

A

Presence of polar groups or functional groups that can undergo ionisation

48
Q

What do functional groups affect

A

Bioavailability, particularly acid-base groups
pKa and pKb values determine charges carried out at different pH values, therefore reactivity and solubility in parts of the body

49
Q

What is a receptor agonist?

A

Drug binds to cell-membrane protein receptor, mimicking effect of normal molecule
causes a series of reactions in cell

50
Q

What is a receptor antagonist?

A

Drug binds to cell-membrane protein repector so normal messenger can’t
prevents particular responses in the cell

51
Q

A drug should be… (receptor)

A

specific and bind to only one particular type fo receptor

52
Q

What do drug-receptor interactions depend on?

A

chemical fit between drug and receptor, better fit = greater drug activity

53
Q

What bonding is involved in drug-receptor interactions?

A

non-covalent, ionic, hydrogen, dispersion forces, hydrophobic interactions

54
Q

What is the process of drug-receptor interactions?

A

biological receptor and drug molecule are seperate -> recognition and binding cause spramolecular complex -> physiological response

55
Q

What is the drug discovery stage?

A

identification of a compound that shows promising activity toward target.
slow, inefficient and expensive
most compounds don’t get past this stage

56
Q

What is used in clinical testing for drugs? Why?

A

rats, mice, guinea pigs, 3 species to determine LD50

57
Q

Process of drug development

A

discovery research (3 yrs)
development research (6 yrs)
-> phase 1 (50-100 subjects)
-> phase 2 (200-400 subjects)
-> phase 3 (3000+ subjects(placebo50% and drug 50%)
regulatory review (2 yrs)
- launch product
post marketing monitoring (1 yr)

58
Q

Down sides of drug developemt

A

expensive
industry is selective about what diseases/conditions to go after
10-12 yrs, lengthy process

59
Q

steps in synthetic drug develpment

A
  1. structure
  2. synthesis
  3. yeild
  4. extraction

Chemistry (2 decks)

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