10. Targeting Local Mediators

Question 1

Where is histamine stored?

Answer 1

Mast cell and basophil granules

Question 2

What causes the release of histamine?

Answer 2

Complement

IgE

Question 3

What type of receptors are histamine receptors?

Answer 3

GCPRs

Question 4

What effects does activation of the H1 receptor have?

Answer 4

Contraction of smooth muscle
Vasodilation
Increased vascular permeability

Question 5

What effect does histamine have in anaphylaxis?

Answer 5

Reduced CO and shock

Question 6

What is the MOA of antihistamines?

Answer 6

Inverse agonists to the H1 receptor

Question 7

What is the difference between first and second generation antihistamines?

Answer 7

First gen can cross the BBB and cause sedation, anti-emesis and dry mouth
Second gen can’t cross BBB

Question 8

Name a first generation antihistamine

Answer 8

Diphenhydramine

Question 9

Name a second generation antihistamine

Answer 9

Cetirizine

Question 10

What effect does 5-HT have on the body?

Answer 10

Vasodilation in undamaged vessels and vasoconstriction in damaged ones
Causes pain and itching by activating sensory nerves
Drives organ dysfunction in sepsis

Question 11

Which 5-HT receptor is not a GPCR?

Answer 11

5-HT3

Question 12

What condition are 5-HT1 agonists used to treat?

Answer 12

Migraines

Question 13

Name a 5-HT1 agonist?

Answer 13

Ergotamine

Question 14

What are NO donors used for?

Answer 14

Prevent reperfusion injury in the heart by inhibiting neutrophils

Question 15

What is the difficulty with NO targeting treatment?

Answer 15

Tolerance can develop

Nitrate free periods must be taken to prevent this