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Therapeutics 2 - Fall 2017 > Antihistamines & Allergic Rhinitis > Flashcards

Antihistamines & Allergic Rhinitis Flashcards

1
Q

Describe Synthesis of Histamine

A

Histidine –> CO2 + Histamine

Done in Mast cells and basophils

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2
Q

Histamine containing cells can be found in what parts of the body?

A
  • Mast cells in mucosa places (skin; nose; mouth; lungs; intestinal)
  • Non-Mast Cells Histamine (in nerve terminals and fundus of stomach)
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3
Q

How is Histamine Metabolized

A

2 main enzymes are N-methyl transferase and Diamine Oxidase

another enzyme is a phosphoribosyl transferase

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4
Q

what are the 2 main ways that histamine can be released

A
  • Antigen mediated (antigen binds to IgE)

- Non antigen mediated (thermal or mechanical stress)

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5
Q

What are the steps for Histamine Release

A
  • IgE binds to FcER
  • Antigen binds to IgE
  • Cluster of FcERs
  • influx of Ca2+ via CRAC
    (NEED CALCIUM FOR HISTAMINE RELEASE)
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6
Q

what drugs prevent histamine release

A

cromolyn sodium

Nedocromolin

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7
Q

Beta -Adrenergic or Ach?

can inhibit antigen induced histamine release from mast cells

A

beta adrenergic

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8
Q

Beta -Adrenergic or Ach?

can stimulate histamine release from mast cells

A

Ach

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9
Q

where are H1 receptors found

A

distributed through CV
Respiratory systems
GI
smooth muscle

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10
Q

what GPCR does H1 use

A

Gq (PLC, IP3, DAG, increase Ca2+ –> MLCK will phosphorylate MLC)

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11
Q

H1 receptors can cause smooth muscle ______ AND vaso______

A

muscle contraction; vasoDILATION

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12
Q

how do H1 receptors lead to vasodilation

A

in VASC Endothelial Cells - NO released

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13
Q

H2 Receptor linked to vascular smooth muscle ______ and _____ secretion

A

relaxation; gastric

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14
Q

what GPCR does H2 use

A

Gs (increase adenylate cyclase = increase cAMP)

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15
Q

where is H3 located

A

in CNS

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16
Q

what GPCR does H3 use

A

Gi/Go

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17
Q

what GPCR does H4 use

A

Gi/Go

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18
Q

where is H4 located

A

located on mast cells/basophils/eosinophils

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19
Q

H3 is linked to inhibition of ________

H4 is linked to ___________

A

H3: inhibition of neurotransmitter release
H4: linked to histamine induced chemotaxis

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20
Q

what are the 4 main pharmacological effects of histamine

A
  • cardiovascular
  • Respiratory
  • Acid release in stomach
  • Anaphylaxis
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21
Q

Histamine Regulation of the Heart

A 
Positive Chronotropy (increased heart rate; increased diastolic depoarlization current)
Positive Inotropy (enhance force of contraction)
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22
Q

Histamine Regulation of the Vasculature:

A

Vasodilation

increased capillary permeability

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23
Q

Histamine effects in lungs

A

Bronchoconstriction; Smooth muscle contraction

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24
Q

H1 antagonists are predominantly _______

Full, partial, inverse agonist or neutral antagonist

A

Inverse agonist

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25
Q

what are the first gen. antihistamines

A
  • Diphenhydramine
  • Hydroxyzine
  • Promethazine
  • Brompheniramine
  • cyproheptadine
  • pyrilamine
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26
Q

2 main side effects of first gen antihistamines

A
  • sedation (CNS efffect)

- Anti-cholinergic

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27
Q

what are anticholinergic side effects

A

decrease urination

dry mouth

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28
Q

Anticholinergics = Antimuscarinic = ______-like

A

Atropine

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29
Q

what are some other first gen H1 antagonist side effects

A
  • local anesthetic
  • Anti-serotonin (HA)
  • alpha adrenergic antagonism (hypotension)
  • extrapyramidal (dystonia, akathisia)
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30
Q

what are the 2nd gen antihistamines

A

loratadine
desloratadine
fexofenadine
cetirizine

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31
Q

2nd gen antihistamines:
have decreased ______ solubility
Efflux from ______ by _______

A

decrease lipid;

from CNS; P-glycoprotein transporter

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32
Q

what are the topical H1 receptor antagonists

A

Olopatadine
Azelastine
Ketotifen

33
Q

clinical uses for H1 antagonists

A
  • Seasonal/Perennial allergic rhinoconjunctivitis
  • Chronic urticaria
  • Motion sickness
  • Adjunct w/ epinephrine to treat anaphylaxis
34
Q

Antihistamines are contraindicated for what things?

A

urinary retention

narrow angle glaucoma

35
Q

what are the therapeutic uses for H2 antagonists

A
  • reduce gastric acid secretion

- treat peptic ulcers and GERD

36
Q

Severe side effects of H2 antagonists

A 
CNS dysfunction
Antiandgrogen (gynecomastia, galactorrhea)
impotence
blood dyscrasias
hepatotoxicity
37
Q

First line therapy for mild allergic rhinitis symptoms

A

SGAs (second generation antihistamines)

38
Q

first line therapy moderate to severe symptoms

A

nasal corticosteroids

39
Q

how to add on therapy to monotherapy of Intra-nasal steroid

A
  • add intranasal antihistamine or Oxymetazoline (3 days or less)

(do NOT add oral antihistamine or leukotriene receptor antagonist)

40
Q

how to add on therapy to monotherapy of oral antihistamine

A
  • add oral decongestant
  • leukotriene receptor antagonist
  • do not add intra-nasal steroid (switching to ok but do not add…)
41
Q

how to avoid mold allergen

A

use dehumidifier

vent bathroom/kitchen

42
Q

how to avoid dust mite allergen

A 
use damp washcloth to dust
use dehumidifier
encase pillow/mattress/box spring
wash bedding w/ hot water weekly
remove stuffed animals from bedroom
replace carpet w/ hard surface flooring
43
Q

what are the temporal patterns of allergic rhinitis

A

perennial

Seasonal

44
Q

what are mild allergic rhinitis symptoms

A

normal sleep
no impairment of daily activities
normal work/school functioning
no troublesome symptoms

45
Q

what are moderate to severe allergic rhinitis symptoms

A

one or more of the following:

  • abnormal sleep
  • impairment of daily activities
  • abnormal work/school functioning
  • troublesome symptoms
46
Q

3 phases of pathophysiology of Allergic Rhinitis

A

1) Sensitization (longest phase)
2) early phase response
3) late phase response

47
Q

Pharmacologic options for allergic rhinitis

A 
antihistamines
corticosteroids
decongestants
anticholinergics
mast cell stabilizers
leukotriene modifiers
48
Q

dosing for diphenhydramine

2 -6 yo

A

under drs supervision

49
Q

dosing for diphenhydramine

6 - 11 yo

A

12.5 - 25 mg Q46H

50
Q

dosing for diphenhydramine

12+ yo

A

25 - 50 mg Q46H

51
Q

dosing for cetirizine

6 - 12 mos

A

2.5 mg QD

52
Q

dosing for cetirizine

1 - 5 yo

A

2.5 mg QD or BID

53
Q

dosing for cetirizine

6+ yo

A

5 or 10 mg QD

54
Q

dosing for fexofenadine

2 - 11 yo

A

30 mg BID

55
Q

dosing for fexofenadine

12+ yo

A

60 mg BID or 180 mg QD

56
Q

dosing for loratadine

2 - 6 yo

A

5 mg QD

57
Q

dosing for loratadine

7+ yo

A

10 mg QD

58
Q

Antihistamine Interaction

First generations and ________

A

MAO inhibitors

59
Q

Antihistamine Interaction

Chlorpheniramine and ________

A

phenytoin

60
Q

Antihistamine Interaction

Loratadine and ___________

A

Ketoconazole/Erythromycin

61
Q

Antihistamine Interaction

Fexofenadine and ________

A

grapefruit juice

62
Q

Antihistamine Interaction
First generations and MAO inhibitors:
what is the response?

A

increase in anticholinergic effects

63
Q

Antihistamine Interaction

Chlorpheniramine and Phenytoin: what is the response?

A

increase in phenytoin concentrations

64
Q

Antihistamine Interaction

Loratadine and Ketoconazole/Erythromycin: what is the response

A

increase in loratadine concentrations

65
Q

Antihistamine Interaction

Fexofenadine and grapefruit juice: what is the response

A

increase in fexofenadine concentrations

66
Q

which intranasal corticosteroids are OTC

A

triamcinolone; Fluticasone; budesonide

67
Q

Intranasal Corticosteroids:
Improvement seen in _______
and then max benefit is seen in ______

A

improvement: 3 days
max: 1 -2 weeks

68
Q

pseudoephedrine dosing:

4 - 5 yo

A

15 mg Q46H

69
Q

pseudoephedrine dosing:

6 - 11 yo

A

30 mg Q46H

70
Q

pseudoephedrine dosing:

12+ yo

A

60 mg Q46H

71
Q

MOA of Leukotriene modifiers

A

decrease mucous secretion and increase bronchodilation

72
Q

which antihistamines are alkylamines

A

Brompheniramine; Chlorphenarmine

73
Q

which antihistamines are ethanolamines

A

diphenhydramin; Dimenhydrinate

74
Q

which first gen antihistamine is a phenothiazine

A

promethazine

75
Q

which second gen antihistamine is a piperadine

A

fexofenadine (and 1st gen: cyproheptadine?)

76
Q

which first gen antihistamine is a piperazine

A

hydroxyzine, meclizine, cyclozine

77
Q

which first gen antihisatmine is an ethylenediamine

A

pyrilamine

78
Q

which classes of first gen antihistamines are known to cause sedation

A

ethanolamines and phenothiazines (aka diphenhydramine and promethazine)

Therapeutics 2 - Fall 2017 (22 decks)

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