Histamine and Serotonin

Question 1

Name the 5 H1 receptor antagonists.

Answer 1

1. Diphenhydramine
2. Tripelennamine
3. Cyclizine
4. Promethazine
5. Chlorpheniramine

Question 2

What are the general properties of the 1st generation H1 receptor antagonists?

Answer 2

rapidly absorbed, widely distributed, rapidly metabolized, OTC, many actions outside of H1 receptor antagonism

Question 3

What are the clinical uses for H1 receptor anatagonists?

Answer 3

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

Question 4

What is Tripelennamine primarily used for?

Answer 4

OTC sleep aid

Question 5

What is Cyclizine primarily used for?

Answer 5

motion sickness

Question 6

What is Promethazine primarily used for?

Answer 6

Anti-emetic

Question 7

What is Chlorpheniramine usually a component of?

Answer 7

cold medications; less sedating than others so in day time medications

Question 8

Which two H1 receptor antagonists exhibit anti-muscarinic effects and sedation?

Answer 8

diphenhydramine and promethazine

Question 9

Name the 4 2nd generation H1 receptor antagonists.

Answer 9

Loratidine, fexofenadine, Azelastine and Certirizine

Question 10

What can all 2nd generation H1 receptor antagonists be used to treat?

Answer 10

Allergic rhinitis

Question 11

Which of the following is available as an intranasal spray or opthalmic solution to treat allergic rhinitis and allergic conjunctivitis respectively? Loratidine, fexofenadine, Azelastine and Certirizine

Answer 11

Azelastine

Question 12

Do the 2nd generation H1 receptor antagonists produce sedation?

Answer 12

NO

Question 13

Do the 2nd generation H1 receptor antagonists cross the BBB?

Answer 13

NO

Question 14

Which of the 2nd generation H1 receptor antagonists can cause cardiovascular side effects at high doses?

Answer 14

loratidine and fexofenadine

Question 15

Which type of drug are Cimetidine, Ranitidine, Famotidine and Nizatidine?

Answer 15

H2 receptor antagonist; blocks gastric acid secretion (primarily nocturnally)

Question 16

What are the H2 receptor antagonists used to treat?

Answer 16

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

Question 17

Which of the H2 receptor anatagonists has the most side effects? the least?

Answer 17

most-Cimetidine

least-Nizatidine

Question 18

Which of the following can cause anti-androgen effects and can inhibit P-450 oxidative enzymes? Cimetidine, Ranitidine, Famotidine or Nizatidine

Answer 18

Cimetidine

Question 19

Which of the following can cause liver toxicity? Cimetidine, Ranitidine, Famotidine or Nizatidine

Answer 19

Ranitidine

Question 20

Which of the following can cause CNS dysnfunction? Cimetidine, Ranitidine, Famotidine or Nizatidine

Answer 20

ALL

Question 21

What is the mechanism of Cyproheptadine and what is it used to treat?

Answer 21

antihistaminic and antiserotinergic; skin allergies (anti-5HT1) and diarrhea of carcinoid system (anti-5HT2)

Question 22

What are the side effects of cyproheptadine?

Answer 22

anti-muscarinic effects and sedation

Question 23

What is the mechanism of Ketanserin and what is used to treat?

Answer 23

selective 5HT-2A, 2C antagonists and a1, H1 antagonist; antihypertensive and antiplatelet aggregation

Question 24

What is the mechanism of Odansetron and what is used to treat?

Answer 24

5HT3 receptor antagonist; nausea and vomiting in chemo

Question 25

As a class, what type of receptors do the Ergot Alkaloids effect and what side effects can they produce?

Answer 25

5HT and a-adrenergic; hallucinations and smooth muscle contraction (vascular and uterine)

Question 26

Name the 4 ergot alkaloids.

Answer 26

Ergotamine, Methysergide, Ergonovine, and Bromocriptine

Question 27

Which 3 receptors is ergotamine a partial agonist of and what is it used to treat?

Answer 27

5HT 1, 2 and a-adrenergic; prodrome of migraines

Question 28

Which 2 receptors does methysergide interact with?

Answer 28

5HT1-partial agonist | 5HT2- antagonist

Question 29

What is ergonovine used to treat?

Answer 29

postpartum hemorrhage

Question 30

Which receptor does Bromocriptine interact with and what is it used to treat?

Answer 30

dopamine agonst; hyperprolactinemia

Question 31

What are triptans and which receptors do they interact with?

Answer 31

non ergot serotinin analogs; 5HT1B, D receptor agonist

Question 32

What are triptans used to treat?

Answer 32

migraines

Question 33

What are the side effects of ergotamine?

Answer 33

Nausea and vomitting, cumulative and prolonged vasoconstriction

Question 34

What are the side effects of methysergide?

Answer 34

GI disturbances, inflammatory fibrosis (chronic use), hallucinations; withdrawn from market because of these

Question 35

What are the effects of histamine on the lungs and through what receptor does it work?

Answer 35

bronchoconstriction; H1

Question 36

What are the effects of histamine on vascular smooth muscle and through what receptor does it work?

Answer 36

post capillary venule dilation, terminal arteriole dilation and venoconstriction; H1

Question 37

What are the effects of histamine on vascular endothelial cells and through what receptor does it work?

Answer 37

contraction and separation of endothelial cells; H1

Question 38

What are the effects of histamine on the nervous system and through what receptor does it work?

Answer 38

sensitization of afferent nerve terminals causing pain and itching: H1

Question 39

What are the effects of histamine on the heart and through what receptor does it work?

Answer 39

minor increase in HR and contractility; H2

Question 40

What are the effects of histamine on the stomach and through what receptor does it work?

Answer 40

increases gastric acid secretion; H2

Question 41

What are the effects of serotonin on the GI tract?

Answer 41

contraction of GI smooth muscle

Question 42

What are the effects of serotonin on the cardiovascular system?

Answer 42

vasoconstriction of smooth muscle, vasodilator in skeletal muscle and heart, reflex bradycardia and platelet aggregation

Question 43

What are the effects of serotonin on the nervous system?

Answer 43

sensitization of sensory receptors causing pain and itching