Lecture 1 And 2 Flashcards Preview

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Flashcards in Lecture 1 And 2 Deck (21):
1

One person trials

Focus on individual response to treatment rather than average from group

2

Drawback of imprecision medicine

Very few people derive benefits from the drugs they take

3

100,000 genome project

NHS genome sequencing programme

Some patients will benefit as a conclusive diagnosis can be given for rare/inherited diseases or because most suitable treatment can be chosen

4

Pharmacokinetics

What the body does to a drug
Measures changes in drug concentration with time in one or more regions of body
Focuses on how much drug you should take

5

Pharmacodynamics

What drug does to the body
Biological effects and mechanisms of action

6

3 classes of GPCR

Rhodopsin like
Secretin and adhesion
Glutamate

7

4 major classes of drug targets

Receptors
Ion channels
Enzymes
Transporters

8

Most GPCRs are

Class A
Rhodopsin like

9

How are the classes of GPCRs different?

Have different orthosteric sites

10

First crystal structure of GPCR bound to diffusible ligand

Human beta2 adrenoceptor

Target for salbutamol- asthma

11

Purinergic receptors

P2Y1
P2Y12
Bind ADP in very different binding pockets despite belonging to same family

12

How do we study nociceptor activation?

DRG neuron culture
Electrophysiology eg. Patch clamp

13

Key molecular target in nociceptors
Application

Na channels
Targeted by local anaesthetic- LAs block channel and stop APs firing. Enter cell and bind to site inside pore- very effective

14

Problem with local anaesthetic

Not selective
Systemic application would have many toxic effects

15

Voltage gated sodium channels are encoded by....different genes and are......., giving a opportunity for

9
Structurally diverse
Selectivity

16

Which sodium channel is the target for pain disorders and where is it expressed?

Nav1.7
Spinal cord

17

Relationship between Nav1.7 and SCN9A

SCN9A encodes Nav1.7

18

Carbamazepine

Anti epileptic drug
Na channel inhibitor
IEM patients with 2 different types of mutation in Nav1.7 experiences reduced pain time

19

Pfizer

Trialed a Nav1.7 antagonist on subjects with 4 different Nav1.7 mutations
Heat pad elicited pain and rates on scale
Significant but variable results

20

Largest drug class

Small molecules
Eg diazepam (Valium)

21

Antibody-drug conjugate

mAb targets toxic drug to its target