Coincidences in the age of rational drug design

Question 1

What is pharmacology?

Answer 1

Pharmacology is the discipline dealing with the intended interactions of drugs and human.

Question 2

What is toxicology?

Answer 2

Toxicology is the discipline dealing with the unintended interactions of drugs and human.

Question 3

What is meant by randomisation in study design?

Answer 3

The allocation to treatment is by chance.

Question 4

What is meant by placebo control in study design?

Answer 4

All patients are treated but not each drug contains the active compound.

Question 5

What is meant by double blinding in study design?

Answer 5

Neither patients nor study team know to which group patients have been allocated.

Question 6

What is meant by multicentering in study design?

Answer 6

The study is being conducted at several locations.

Question 7

Dimethyl fumarate is a prodrug. What is the active metabolite?

Answer 7

Monomethyl fumarate

Question 8

What is a prodrug?

Answer 8

A prodrug is a inactive medication that is metabolized in the body into its active form.

Question 9

What are the four phases of drug development?

Answer 9

1. Phase:
   -> First tests in 10-100 healthy humans
   -> Takes a few months up to one year
2. Phase:
   -> First tests in 50-500 patiens
   -> Takes 1-2 years
3. Phase:
   -> Tests in a few hundred to a few thousand patients
   -> Takes 3-5 years
4. Phase:
   -> Post-marketing tests
   -> Patients in treatment with approved drug

Question 10

What is phytotherapy?

Answer 10

Treatment of diseases with plant-based medicines
-> Use of non-purified plant extracts

Question 11

What is the half-life of monomethyl fumarate?

Answer 11

1,5 hours

Question 12

What are the side effects of dimethyl fumarate?

Answer 12

1. Gastrointestinal disorder
2. Lymphopenia
3. PML
4. Flush (heat and red skin)

Question 13

How is dimethyl fumarate working?

Answer 13

1. Dimethyl fumarate (DMF) is converted into monomethyl fumarate (MMF)
2. MMF binds to Keap1 and activates NRF2 (transcription factor)
3. MMF binds to the HCA2-receptor on neutrophil granulocytes and macrophages
4. Decreased secretion of pro-inflammatory cytokines
5. Increased neutoprotection

Question 14

For the treatment of which diseases is DMF used?

Answer 14

1. Multiple Sklerose
2. Psoriasis (Schuppenflechte)