Histamine, Serotonin & Ergot Alkaloids Chp 16

Question 1

First Generation H1 antihistamines

Answer 1

Diphenhydramine

Question 2

Effects of first generation antihistamines

Answer 2

reduces/prevents histamine effects on smooth muscle, immune cells; also blocks muscarinic and Alpha adrenoceptors; HIGHLY SELECTIVE

Question 3

Action of first generation antihistamines

Answer 3

competitive antagonism/inverse agonism at H1 receptors

Question 4

Clinical usage of first generation antihistamines

Answer 4

IG-E immediate allergies, especially hay fever, urticaria; often used as. a sedative, anti-emetic, and anti-motion sickness drug

Question 5

Toxicity of Histamines first generation

Answer 5

sedation, muscarinic blockade s/s, orthostatic hypotension, some inhibition of CYP2D6, may prolong action of some beta blockers

Question 6

What is a second generation antihistamine

Answer 6

Cetirizine

Question 7

Action of 2nd generation antihistamines

Answer 7

competiitive antagonism/inverse agonism at H1 receptors

Question 8

effects of cetiriizine

Answer 8

reduces/prevents histamine effects on smooth muscle, immune cells

Question 9

Usage of second generation antihistamine

Answer 9

IG-E immediate allergies

Question 10

Toxicity of 2nd generation antihistamines

Answer 10

sedation and arrhythmias in overdose

Question 11

Serotonin Agonist

Answer 11

5-HT (1B/1D)

Question 12

Example of 5-HT (1B/1D)Agonist

Answer 12

Sumatriptan

Question 13

Action of Sumatriptan

Answer 13

partial agonist at 5-HT (1B/1D)receptors

Question 14

Effects of sumatriptan

Answer 14

not fully understood; may reduce release of calcitonin gene-related peptide and perivascular. edema in cerebral circulation

Question 15

Usage of Sumatriptan

Answer 15

Migraine and cluster HA

Question 16

Toxicity of Sumatriptan

Answer 16

paresthesia, dizziness, coronary vasoconstriction

Question 17

What is the importance of Histamines

Answer 17

mediator of immediate allergic and inflammatory reactions, modest role in anaphylaxis, gastric acid. secretion, and NT and neuromodulator, CV regulation, sleep and arousal, theraml and body wt. regulation

Question 18

H4 blockers

Answer 18

has potential in chronic inflammatory conditions such as asthma, in which eosinophils and mast cells play a role

Question 19

Brain serotonergic neurons are involved in…

Answer 19

mood, sleep, appetite, and temperature regulation, perception to pain, regulation of blood pressure and vomiting

Question 20

Adverse effects of Histamines

Answer 20

Flushing, hypotension, tachycardia, HA, urticaria, bronchoconstrictions, and GI upset

Question 21

H3 selective ligands

Answer 21

value in sleep disorders, narcolepsy, obesity, and cognitive and psychiatric disorders

Question 22

Characteristics of COX 1

Answer 22

“house keeping” functions; gastric epithelial COX

Question 23

Characteristics of COX 2

Answer 23

major source of prostanoids in inflammation and. cancer

Question 24

Lipoxygenase Pathway

Answer 24

gives rise to leukotrienes; associated with asthma, anaphylactic shock, and CV disease; bronchoconstriction

Question 25

Epoxygenases Pathway

Answer 25

vasodilation and decreased BP; anti-thrombitic

Question 26

Isoeicoosanoids

Answer 26

formed nonenzymatically by direct free radical-based action on AA and related lipids substrates; vasoconstrictor; modulate leukocyte and platelet adhesive interactions and angiogenesis

Question 27

Effects of prostaglandins and thromboxanes

Answer 27

effects on smoooth muscle in vasculature, airways, and GI and reproductive tracts

Question 28

CYp450

Answer 28

affects nephron transport functioons

Question 29

Effects of Lipoxygenase & CYp450

Answer 29

blood cells, inflammation, heart, smooth muscle, GI, and airways, renal