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TARGET AUDIENCE
This CME activity is intended for physicians, medical
students, nurse practitioners, and physician assistants who
manage children with acute illness in either the emergency
department (ED) or office-based settings. Pediatric emergency physicians, emergency physicians, pediatricians, and family practitioners will find this information especially useful.
LEARNING OBJECTIVES
After completion of the article, the reader should be
able to:
1. Discuss the role histamine plays in allergic responses.
2. Describe differences between first- and second-generation
antihistamines based on pharmacology and side effect
profiles.
3. Identify the second-generation antihistamines and their
relative strengths and weaknesses.
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143
As a result of their selective engineering, the secondgeneration antihistamines do not bind muscarinic receptors
and therefore do not have anticholinergic side effects. Most
are not active on serotonergic receptors and do not affect
appetite or cause weight gain.33 Few case reports of
ingestions of the newer antihistamines exist in children.
As a result, there are no good guidelines directing management of pediatric poisonings from these agents. One high
dose loratidine (Claritin) exposure in a 6-year-old resulted
in minor hypertension and tachycardia which was managed with supportive measures alone.34 Three other reports
have documented overdoses of cetirizine (Zyrtec). No
cardiovascular effects were noted and patients experienced only sedation35,36 and, in one case, agitation.37 All
children underwent conservative management and suffered
no sequelae.
SPECIFIC AGENTS
Cetirizine (Zyrtec)
Although cetirizine (Zyrtec) is a second-generation
antihistamine, it retains some of the sedative side effects of
its parent compound, hydroxyzine (Atarax). The drug is not
metabolized by the liver, which may explain its rapid onset
of activity and lack of interaction with many other medications.38,39 Cetirizine (Zyrtec) has been found to be among the
most effective antihistamines in preventing allergic skin
reactions.40 42 It has, by far, the most documented antiallergic effects independent of its antihistaminic effects at
approved dosages.43 It has been shown to decrease eosinophilic infiltration of the skin44,45 and diminish the late phase
response.44 46 It is approved for use by children as young as
6 months old.
Loratidine (Claritin)
TABLE 1. Characteristics of First- and Second-Generation
Antihistamines
Generic Name
Trade Name
First-generation
Antihistamines
Diphenhydramine
Clemastine
Chlorpheniramine
Hydroxyzine
Promethazine
Second-generation
Antihistamines
Loratidine
Certizirine
Fexofenadine
Desloratidine
144
Half-life (hours)
Benadryl
Tavist
Chlor-Trimeton
Atarax
Phenergan
Claritin
Zyrtec
Allegra
Clarinex
Loratidine (Claritin) is the only member of the secondgeneration antihistamines to be approved for over the counter
use. It is metabolized by the cytochrome P450 system47 to
descarboethoxyloratidine. Loratidine (Claritin) has a slightly slower onset of action compared with other secondgeneration antihistamines.39,48,49
Fexofenadine (Allegra)
7.511
710
1115
2530
Desloratidine (Clarinex)
Desloratidine (Clarinex), the primary active metabolite
of loratidine (Claritin), recently gained FDA approval in 2001.
n 2004 Lippincott Williams & Wilkins
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Indications
Forms
Cetirizine
SAR, PAR, CU
Tabs: 5, 10 mg
Syrup: 5 mg/5 cc
Loratidine
SAR, PAR, U
Fexofenadine
SAR, CIU
Tabs/reditabs: 10 mg
Syrup: 5 mg/5 cc
Tabs: 30, 60, 180 mg
Desloratidine
Tabs/reditabs: 5 mg
Dosage
Cost
>12 years: 10 mg qd
611 years: 5 mg qd
6 months to 5 years: 2.5 mg qd
>6 years: 10 mg qd
26 years: 5 mg qd
>12 years: 60 mg bid or 180 mg qd
611 years: 30 mg bid
>12 years: 5 mg qd
$57.53
$52.95
$31.00
$32.97/$38.97
$13.75
$61.74/$62.03
$38.99
$68.49
CIU indicates chronic idiopathic urticaria; CU, chronic urticaria; PAR, perennial allergic rhinitis; SAR, seasonal allergic rhinitis; U, urticaria.
INDICATIONS
Allergic Rhinitis
Allergic rhinitis affects up to 30% of adolescents52 and
is responsible for over 2 million missed school days each
year.53 It can be differentiated into 2 categories based on the
duration and timing of symptoms. Seasonal allergic rhinitis
(SAR), commonly known as hay fever, is triggered by weed,
grass, and tree pollens, whereas perennial allergic rhinitis
(PAR) is present year round.54 Second-generation antihistamines have proven to be potent and safe in controlling
allergic rhinitis symptoms such as watery eyes, nasal pruritis,
and rhinorrhea 32,5456 even in preschool children.57 Multiple
studies have shown the combination of newer antihistamines
and pseudoephedrine to be more effective than either
component alone in alleviating nasal congestion associated
with allergic rhinitis.54,58,59
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145
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CME EXAM
Instructions for the Pediatric Emergency Care CME Program Examination
To earn CME credit, you must read the designated article and complete the examination below, answering at least 80%
of the questions correctly. Mail a photocopy of the completed answer sheet to the Office of Continuing Education, Wolters
Kluwer Health, 530 Walnut Street, 2nd Floor East, Philadelphia, PA 19106. Only the first answer form will be considered for
credit and must be received by Wolters Kluwer Health by April 15, 2004. Answer sheets will be graded and certificates will be
mailed to each participant within six to eight weeks after WKH receipt. The answers for this examination will appear in the
May 2004 issue of Pediatric Emergency Care.
Credits
Wolters Kluwer Health designates this educational activity for a maximum of 1 category 1 credit toward the AMA
Physicians Recognition Award. Each physician should claim only those credits that he/she actually spent in the educational
activity.
Accreditation
Wolters Kluwer Health is accredited by the Accreditation Council for Continuing Medical Education to provide
continuing medical education for physicians.
CME EXAMINATION
February 2004
Please mark your answers on the ANSWER SHEET.
New Oral Antihistamines in Pediatrics, Horowitz and Reynolds
1. Which is the only non sedating antihistamine to be
approved for three indications?
a) cetirizine
b) hydroxyzine
c) loratidine
d) fexofenadine
e) desloratidine
2. As compared to the first generation antihistamines, the
second generation:
a) cross the blood brain barrier more easily
b) are all only available by prescription
c) are larger and highly lipophobic molecules
d) should not be used with antifungal agents
e) bind muscarinic receptors
3. The cheapest second-generation antihistamine is:
a) Certirizine
b) Loratidine
c) Desloratidine
d) Fexotendadine
4. A study suggests that early treatment of an atopic child
with which antihistamine may prevent asthma:
a) Certirizine
b) Loratidine
c) Diphenhydramine
5. Which second-generation antihistamine is approved for
use in children as young as 6 months old:
a) Cetirizine
b) Fexofenadine
c) Loratidine
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147
1.
A B C D E
2.
3.
4.
A B C D E
A B C D E
A B C D E
5.
A B C D E
Your evaluation of this CME activity will help guide future planning. Please respond to the following questions.
1. Did the content of the article(s) meet the stated learning objectives?
[ ] Yes
[ ] No
2. On a scale of 1 to 5, with 5 being the highest, how do you rank the overall quality of this educational activity as it pertains to
your practice?
[]5
[]4
[]3
[]2
[]1
3. As a result of meeting the learning objectives of this educational activity, will you be changing your practice behavior in a
manner that improves your patient care? If yes, please explain.
[ ] Yes
[ ] No
4. Did you perceive any evidence of bias for or against any comercial products? If so, please explain.
[ ] Yes
[ ] No
5. Please state one or two topics that you would like to see addressed in future issues.
6. How long did it take you to complete this CME activity?
__________hour(s) __________minutes
Mail by April 15, 2004 to
Office of Continuing Education
Wolters Kluwer Health
530 Walnut Street, 2nd Floor East
Philadelphia, PA 19106
148
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