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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
How does tolerance build up?
Over time and with regular use
26
What does tolerance mean in the effect of a drug?
over time the user may need increasing amounts of a drug to achieve the same desired physiological effect.
27
What is the risk of a tolerance build-up?
Increases health hazards and risk of fatal overdose
28
What can happen if a user takes the same amount of a drug after a long period of time?
tolerance may have decreased, size of the dose that the user used may be enough for an overdose.
29
What is a side effect?
The unwanted responses of a drug. To achieve the main effect, side effects must be tolerated.
30
Which organs are usually damaged as a side effect of medication and why?
Most drugs are concentrated, metabolized, and excreted by kidneys and liver. Side effects can damage these organs.
31
What are the physiological effects of a drug?
The therapeutic effect that is intended Along with the side-effects that are unintended
32
What is dependence?
When a person continues to use a drug because they don't feel right without it. An intense craving for the drug.
33
What is physical dependence?
When the body cannot perform normally without the drug.
34
Symptoms of physical dependence
fever convulsions (Withdrawal) can be fatal
35
What is Psychological dependence?
The drug becomes central to a person's thoughts and they can't stop using it or thinking about it. (Addiction)
36
Ways of administering drugs
1. Orally -> pills 2. Inhalation -> ventilin 3. Rectal -> through anus 4. Injected a. intravenous b. intramuscular c. subcutaneous 5. Topical
37
Why are there different methods for drug administration?
Methods vary in the speed at which the medicine reaches the blood.
38
What are the levels of the skin tissue?
1. Epidermis 2. Dermis 3. Subcutaneous tissue 4. Muscle 5. Vein
39
Where are subcutaneous, intravenous, and intramuscular administrations injected?
Subcutaneous -> injected directly under surface of the skin Intravenous -> injected directly into bloodstream Intramuscular -> injected directly into a muscle
40
What affects oral bioavailability?
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
What is the first-pass effect?
The relatively low bioavailability of a drug taken orally. 20 - 40% of an orally ingested drug may reach bloodstream.
42
Why is there low bioavailability in orally ingested drugs?
After swallowing, drugs pass into digestive system. Enzymes may alter them chemically. Then passed in blood to liver where further metabolic breakdown occurs
43
What is the difference in dosage between oral and IV?
Oral needs to be about 4x higher than IV
44
First-pass metabolism pathway
1. Swallowed drug 2. Digestive system 3. Hepatic portal system 4. Liver 5. Rest of the body
45
Why is water solubility important?
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
Why is lipid solubility important?
Lipid solubility helps in the passage of the drug through membranes during absorption
47
Factors that affect solubility
Presence of polar groups or functional groups that can undergo ionisation
48
What do functional groups affect
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
What is a receptor agonist?
Drug binds to cell-membrane protein receptor, mimicking effect of normal molecule causes a series of reactions in cell
50
What is a receptor antagonist?
Drug binds to cell-membrane protein repector so normal messenger can't prevents particular responses in the cell
51
A drug should be... (receptor)
specific and bind to only one particular type fo receptor
52
What do drug-receptor interactions depend on?
chemical fit between drug and receptor, better fit = greater drug activity
53
What bonding is involved in drug-receptor interactions?
non-covalent, ionic, hydrogen, dispersion forces, hydrophobic interactions
54
What is the process of drug-receptor interactions?
biological receptor and drug molecule are seperate -> recognition and binding cause spramolecular complex -> physiological response
55
What is the drug discovery stage?
identification of a compound that shows promising activity toward target. slow, inefficient and expensive most compounds don't get past this stage
56
What is used in clinical testing for drugs? Why?
rats, mice, guinea pigs, 3 species to determine LD50
57
Process of drug development
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
Down sides of drug developemt
expensive industry is selective about what diseases/conditions to go after 10-12 yrs, lengthy process
59
steps in synthetic drug develpment
1. structure 2. synthesis 3. yeild 4. extraction

Chemistry (2 decks)

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