Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

How is Histamine Metabolized

A

2 main enzymes are N-methyl transferase and Diamine Oxidase

another enzyme is a phosphoribosyl transferase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what drugs prevent histamine release

A

cromolyn sodium

Nedocromolin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Beta -Adrenergic or Ach?

can inhibit antigen induced histamine release from mast cells

A

beta adrenergic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Beta -Adrenergic or Ach?

can stimulate histamine release from mast cells

A

Ach

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

where are H1 receptors found

A

distributed through CV
Respiratory systems
GI
smooth muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what GPCR does H1 use

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

H1 receptors can cause smooth muscle ______ AND vaso______

A

muscle contraction; vasoDILATION

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

how do H1 receptors lead to vasodilation

A

in VASC Endothelial Cells - NO released

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

H2 Receptor linked to vascular smooth muscle ______ and _____ secretion

A

relaxation; gastric

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what GPCR does H2 use

A

Gs (increase adenylate cyclase = increase cAMP)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

where is H3 located

A

in CNS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what GPCR does H3 use

A

Gi/Go

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what GPCR does H4 use

A

Gi/Go

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

where is H4 located

A

located on mast cells/basophils/eosinophils

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

H3 is linked to inhibition of ________

H4 is linked to ___________

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what are the 4 main pharmacological effects of histamine

A
  • cardiovascular
  • Respiratory
  • Acid release in stomach
  • Anaphylaxis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Histamine Regulation of the Heart

A 
Positive Chronotropy (increased heart rate; increased diastolic depoarlization current)
Positive Inotropy (enhance force of contraction)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Histamine Regulation of the Vasculature:

A

Vasodilation

increased capillary permeability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Histamine effects in lungs

A

Bronchoconstriction; Smooth muscle contraction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

H1 antagonists are predominantly _______

Full, partial, inverse agonist or neutral antagonist

A

Inverse agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
what are the first gen. antihistamines
- Diphenhydramine - Hydroxyzine - Promethazine - Brompheniramine - cyproheptadine - pyrilamine
26
2 main side effects of first gen antihistamines
- sedation (CNS efffect) | - Anti-cholinergic
27
what are anticholinergic side effects
decrease urination | dry mouth
28
Anticholinergics = Antimuscarinic = ______-like
Atropine
29
what are some other first gen H1 antagonist side effects
- local anesthetic - Anti-serotonin (HA) - alpha adrenergic antagonism (hypotension) - extrapyramidal (dystonia, akathisia)
30
what are the 2nd gen antihistamines
loratadine desloratadine fexofenadine cetirizine
31
2nd gen antihistamines: have decreased ______ solubility Efflux from ______ by _______
decrease lipid; | from CNS; P-glycoprotein transporter
32
what are the topical H1 receptor antagonists
Olopatadine Azelastine Ketotifen
33
clinical uses for H1 antagonists
- Seasonal/Perennial allergic rhinoconjunctivitis - Chronic urticaria - Motion sickness - Adjunct w/ epinephrine to treat anaphylaxis
34
Antihistamines are contraindicated for what things?
urinary retention | narrow angle glaucoma
35
what are the therapeutic uses for H2 antagonists
- reduce gastric acid secretion | - treat peptic ulcers and GERD
36
Severe side effects of H2 antagonists
``` CNS dysfunction Antiandgrogen (gynecomastia, galactorrhea) impotence blood dyscrasias hepatotoxicity ```
37
First line therapy for mild allergic rhinitis symptoms
SGAs (second generation antihistamines)
38
first line therapy moderate to severe symptoms
nasal corticosteroids
39
how to add on therapy to monotherapy of Intra-nasal steroid
- add intranasal antihistamine or Oxymetazoline (3 days or less) (do NOT add oral antihistamine or leukotriene receptor antagonist)
40
how to add on therapy to monotherapy of oral antihistamine
- add oral decongestant - leukotriene receptor antagonist - do not add intra-nasal steroid (switching to ok but do not add...)
41
how to avoid mold allergen
use dehumidifier | vent bathroom/kitchen
42
how to avoid dust mite allergen
``` 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
what are the temporal patterns of allergic rhinitis
perennial | Seasonal
44
what are mild allergic rhinitis symptoms
normal sleep no impairment of daily activities normal work/school functioning no troublesome symptoms
45
what are moderate to severe allergic rhinitis symptoms
one or more of the following: - abnormal sleep - impairment of daily activities - abnormal work/school functioning - troublesome symptoms
46
3 phases of pathophysiology of Allergic Rhinitis
1) Sensitization (longest phase) 2) early phase response 3) late phase response
47
Pharmacologic options for allergic rhinitis
``` antihistamines corticosteroids decongestants anticholinergics mast cell stabilizers leukotriene modifiers ```
48
dosing for diphenhydramine | 2 -6 yo
under drs supervision
49
dosing for diphenhydramine | 6 - 11 yo
12.5 - 25 mg Q46H
50
dosing for diphenhydramine | 12+ yo
25 - 50 mg Q46H
51
dosing for cetirizine | 6 - 12 mos
2.5 mg QD
52
dosing for cetirizine | 1 - 5 yo
2.5 mg QD or BID
53
dosing for cetirizine | 6+ yo
5 or 10 mg QD
54
dosing for fexofenadine | 2 - 11 yo
30 mg BID
55
dosing for fexofenadine | 12+ yo
60 mg BID or 180 mg QD
56
dosing for loratadine | 2 - 6 yo
5 mg QD
57
dosing for loratadine | 7+ yo
10 mg QD
58
Antihistamine Interaction | First generations and ________
MAO inhibitors
59
Antihistamine Interaction | Chlorpheniramine and ________
phenytoin
60
Antihistamine Interaction | Loratadine and ___________
Ketoconazole/Erythromycin
61
Antihistamine Interaction | Fexofenadine and ________
grapefruit juice
62
Antihistamine Interaction First generations and MAO inhibitors: what is the response?
increase in anticholinergic effects
63
Antihistamine Interaction | Chlorpheniramine and Phenytoin: what is the response?
increase in phenytoin concentrations
64
Antihistamine Interaction | Loratadine and Ketoconazole/Erythromycin: what is the response
increase in loratadine concentrations
65
Antihistamine Interaction | Fexofenadine and grapefruit juice: what is the response
increase in fexofenadine concentrations
66
which intranasal corticosteroids are OTC
triamcinolone; Fluticasone; budesonide
67
Intranasal Corticosteroids: Improvement seen in _______ and then max benefit is seen in ______
improvement: 3 days max: 1 -2 weeks
68
pseudoephedrine dosing: | 4 - 5 yo
15 mg Q46H
69
pseudoephedrine dosing: | 6 - 11 yo
30 mg Q46H
70
pseudoephedrine dosing: | 12+ yo
60 mg Q46H
71
MOA of Leukotriene modifiers
decrease mucous secretion and increase bronchodilation
72
which antihistamines are alkylamines
Brompheniramine; Chlorphenarmine
73
which antihistamines are ethanolamines
diphenhydramin; Dimenhydrinate
74
which first gen antihistamine is a phenothiazine
promethazine
75
which second gen antihistamine is a piperadine
fexofenadine (and 1st gen: cyproheptadine?)
76
which first gen antihistamine is a piperazine
hydroxyzine, meclizine, cyclozine
77
which first gen antihisatmine is an ethylenediamine
pyrilamine
78
which classes of first gen antihistamines are known to cause sedation
ethanolamines and phenothiazines (aka diphenhydramine and promethazine)

Therapeutics 2 - Fall 2017 (22 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions