GO - Targets identified from studying the effects of drugs and toxins Flashcards Preview

CH344 > GO - Targets identified from studying the effects of drugs and toxins > Flashcards

Flashcards in GO - Targets identified from studying the effects of drugs and toxins Deck (28):
1

Put these steps for the drug discovery process in order:
1. Lead optimisation
2. Marketing authorisation
3. Target identification
4. Formulation development
5. Lead generation
6. Pharmaceutical and Toxicity profiling
7. Target validation

3, 7, 5, 1, 6, 4, 2

2

For a drug molecule to exert a pharmacological effect, an interaction between the ___ and the _____ must occur.

drug molecule
target molecule

3

This interaction between the drug molecule and target molecule requires:

1 - functional groups on both target molecule and drug molecule
2 - appropriate orientation in space of the drug functional groups relative to the target molecule functionality.
3. and can be explained in terms of bonding and reactivity between the two molecules.

4

State the bond types and order them from strongest to weakest.

Covalent
Ionic
Ion-dipole
Hydrogen
Hydrophobic
VWF

5

What is a pharmacophore

The combination of parameters essential for activity

6

Pharmacophoric descriptors are used to define a pharmacophores, including:

ionic, H-bonding, hydrophobic and eletrostatic interaction sites, define by atoms, ring centers and virtual points

7

The pharmacophore can be considered:
- the largest common denominator shared by a set of. inactive molecules
- the largest common denominator shared by a set of. active molecules
- the largest common numerator shared by a set of. active molecules
- the smallest common denominator shared by a set of. active molecules

- the largest common denominator shared by a set of. active molecules

8

Structurally relevant (but different) molecules from natural resources frequently have similar ( but subtly different) ________, such as ________

biological activities
duration of action

9

Where did drugs come from in the past?

Food and toxins

10

What are two ways in which you can improve pharmacodynamic activity?

1. Greater potency --> same effect with lower dose
2. Greater selectivity --> fewer s/es due to interaction with other targets

11

Most drugs have 'side effects'. This is often the result of...

activity on other targets.

12

Opium alkaloids are obtained from the latex of....

Papaver somniferum

13

What properties are opium alkaloids known for?

sedating and analgesic.

14

Name a few opium alkaloids.

Noscapine
Thebaine
Papaverine
Morphine
Codiene

15

How is morphine administered

Subcutaneous injection

16

What activity does morphine show?

- analgesic
- antitussive
- reduced gastric motility
- respiratory depressant

17

Morphine side effects

- Constipation
- Nausea and vomiting
- Drowsiness
- Respiratory depression

18

What is an opiate antagonist?

Nalaxone

19

Order the functional groups in order of polarity.

Amide > Acid > Alcohol > Ketone > Aldehyde > Amine > Ester > Ether > Alkene > Alkane

20

What is the general term for opioid peptides

Endorphins

21

Higher affinity for analgesic receptors =

greater potency

22

Change susceptibility to metabolising enzymes =

change in duration of action

23

Changing lipophilicity will

change penetration of CNS

24

u-receptors are associated with all the main pharmacological effects of morphine:

- analgesia
- respiratory depression
- emesis
- tolerance
- withdrawal symptoms
- reduce gastric motility

25

k- selective agonists produce....

they lack....

produce:
- diuresis
- sedation
- analgesia
- dysphoria

lack:
- constipation
- respiratory depression
- addictive effects

26

selective k- opioids with only peripheral action may be useful in relieving.....

inflammation and its associated pain

27

d- selective agonists produce

- analgesia
- convulsant activity

28

Is Fentanyl or Morphine more potent? By how much? and because of what?

Fentanyl.
500 times more
greater lipophilicity