Pharm Exam 2: Antihistamines And Migraine

Front 1

Histamine acts on:

Back 1

Small diameter sensory neurons

Front 2

Three modalities transmitted by small diameter sensory neurons

Back 2

Temperature
Noxious
Itch

Front 3

Histamine is decarboxylatd from:

Back 3

Histidine

Front 4

Histamine is synthesized and stored in:

Back 4

Mast cells
Enterochromaffin cells

Front 5

Two main histamine receptors

Back 5

H1 and H2

Front 6

H1 Receptor

Back 6

Smooth muscle
Vascular endothelium
Brain

Front 7

H2 Receptor

Back 7

Gastric mucosa
Cardiac muscle
Brain

Front 8

Use of H1 Agonist

Back 8

Test for bronchosensitivity

Front 9

H1 Agonist - Name 3

Back 9

2-methylhistamine
Histamine
2-(3-Bromphenyl)

Front 10

H1 Receptor Antagonist - 1st generation (name 2)

Back 10

Diphenhydranine
Chlorpheniramine

Front 11

H1 Receptor Antagonist - 2nd generation (name 4)

Back 11

Cetirizine
Loratidine
Desloratadine
Fexofenadine

Front 12

H2 Receptor Antagonist (Name 4)

Back 12

Cimetidine
Famotidine
Ranitidine
Nizatidine

Front 13

Use for H2 Receptor Antagonist

Back 13

Treat PUD and gastric irritation

Front 14

6 major physiologic actions of histamine

Back 14

1. Allergic response
2. CV effects
3. Bronchoconstriction
4. Increase in gastric acid secretion (H2)
5. Itch
6. Anaphylaxis

Front 15

Allergic response mediated by histamine

Back 15

Rhinitis and urticaria (hives)

Front 16

Cardiovascular effects mediated by histamine

Back 16

Vasodilation
Increased vascular permeability
Histamine injection triple response (red spot, flare, wheal)
Increased contraction of heart

Front 17

Anaphylaxis

Back 17

Severe hypotension
Bronchoconstriction
Epiglottal swelling

Front 18

Antihistamine are/are not effective in treating bronchoconstriction.

Back 18

Not effective

Front 19

Type of antagonist of H1 Antagonists

Back 19

Reversible, competitive inhibitor

Front 20

Properties of first generation H1 Antagonist

Back 20

1. Highly lipid soluble
2. Drowsiness and sedation
3. Some anti-muscarinic activity

Front 21

Why use 1st generation H1 antagonist in sleep aids

Back 21

Highly lipid soluble - readily distribute to CNS
Produce drowsiness and sedation

Front 22

Why use 1st generation H1 antagonist in first line treatment of Parkinson's

Back 22

Some antimuscarinic activity can help with early manifestations of Parkinsons

Front 23

Properties of 2nd generation H1 Antagonist

Back 23

1. Ionized at pH 7.4 - less readily into CNS
2. Highly bound to albumin - less readily into CNS
3. Less drowsiness and sedation
4. No antimuscarinic activity

Front 24

Name 6 1st generation H1 Antagonist

Back 24

1. Diphenhydramine
2. Chlorpheniramine
3. Pyrilamine
4. Hydroxyzine
5. Promethazine
6. Doxepin

Front 25

Major side effect of 1st generation H1 Antagonist

Back 25

Drowsiness and sedation

Front 26

Name four 2nd generation H1 antagonist

Back 26

Cetirizine
Loratadine
Desloratadine
Fexofenadine

Front 27

2nd generation H1 antagonists metabolism

Back 27

CYP450 pathway
Consider drug drug interactions of those also metabolized by CYP450

Front 28

Do/do not get anticholinergic effects w/ 2nd generation H1 antagonist

Back 28

Don't get anticholinergic effects

Front 29

Difference in side effects between 1st and 2nd generation H1 antagonist

Back 29

2nd generation = minimal drowsiness and sedation

Front 30

Use for promethazine

Back 30

Treatment of nausea and vomiting
Antimuscarinic effects

Front 31

Use for diphenhydramine aside from OTC use

Back 31

First line treatment of Parkinsons disease
Antimuscarinic effects

Front 32

Two 1st generation antihistamines used for prophylaxis and treatment of motion sickness

Back 32

Promethazine and diphenhydramine

Front 33

5HT is derived from which amino acid

Back 33

Tryptophan

Front 34

Name two important 5HT receptor subtypes

Back 34

5HT1B, 5HT1D

Front 35

Function of 5HT1B Receptor

Back 35

Autoreceptor
Regulate presynaptic function

Front 36

Function of 5HT1D Receptor

Back 36

Vasoconstriction

Front 37

Ergot alkaloids act on which 5HT receptor subtype

Back 37

5HT2A, 5HT2B

Front 38

Function of 5HT2 Receptor

Back 38

Smooth muscle contraction
(Think uterine SM contraction)

Front 39

Prophylaxis of migraine

Back 39

Beta-blocker
TCA

Front 40

4 Characteristics of Migraine

Back 40

1. Unilateral HA lasting 4-72 hours
2. Pulsating and aggravated by movement
3. Nausea or photophobia
4. Preceded by visual aura (commonly)

Front 41

Rx therapy for migraine

Back 41

5HT1B/5HT1D Agonist

Front 42

Disorder of neurogenic inflammation

Back 42

Migraine

Front 43

Neurogenic inflammation of migraine mediated by:

Back 43

CT gene related peptide (CGRP)
Substance P

Front 44

Three possible components of Migraine

Back 44

1. Neurogenic inflammation
2. Cortical speading depression
3. Central sensitization

Front 45

Triptans

Back 45

5HT1 receptor agonist

Front 46

Name 5 triptans (5HT1 receptor agonist)

Back 46

sumatriptan
naratriptan
rizatriptan
Zolmitriptan
Almotriptan

Front 47

Where do triptans work?

Back 47

5HT1 receptors especially 5HT1B AND 5HT1D

Front 48

Triptans are/are not useful in prophylaxis and long term use in treatment of migraines

Back 48

Not useful

Front 49

2 Proposed mechanisms of action of triptans on migraines

Back 49

1. Direct vascoconstriction of intracranial blood vessels 5HT1D)
2. Presynaptic inhibition on sensory neurons (5HT1B)

Front 50

Rare complication of triptans

Back 50

Serious CV complications:
Coronary artery spasm (due to SM constriction, activation of 5HT2R)--> ischemia, arrhythmia

Front 51

Contraindication to triptans

Back 51

History of ischemic/vasospastic coronary artery disease
Cerebrovascular or peripheral vascular disease
Uncontrolled HT
Patients on MAO-I

Front 52

Do not give naratriptan to:

Back 52

Patients with severe renal or hepatic disease