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The Pediatric Forum |

Diphenhydramine in Infants

F. Estelle R. Simons, MD
[+] Author Affiliations

Copyright 2007 American Medical Association. All Rights Reserved. Applicable FARS/DFARS Restrictions Apply to Government Use.

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Arch Pediatr Adolesc Med. 2007;161(1):105-105. doi:10.1001/archpedi.161.1.105-a
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The randomized controlled trial by Merenstein et al1 demonstrating lack of an infant sleep response to diphenhydramine is a welcome addition to the pediatric literature. Old, first-generation H1 antihistamines such as diphenhydramine are widely used and are assumed to be effective and safe because they are available without prescription. However, these medications were introduced long before regulatory agencies mandated prospective, randomized, placebo-controlled, double-blind studies of the efficacy and safety of new chemical entities.2 The diphenhydramine dose recommended for infants and young children is based on anecdotal experience rather than on prospective pharmacokinetic and pharmacodynamic studies. The dose recommended for sleep is similar to the dose recommended for the treatment of allergic rhinitis or urticaria symptoms.

Although Merenstein et al1 describe diphenhydramine as a safe medication, diphenhydramine toxicity became apparent shortly after the drug was introduced into the pharmacopeia more than half a century ago.3 Like other first-generation H1 antihistamines, even in recommended doses it may lead to a variety of adverse effects. It crosses the blood-brain barrier, blocks the neurotransmitter effect of histamine at H1 receptors in the central nervous system, and potentially causes sedation. In infants and young children, it may have paradoxical stimulatory central nervous system effects, with resulting irritability, nervousness, excitation, insomnia, and seizures.2 4 Fatalities after overdose continue to be reported, and it has been used as an agent of infanticide.4

It may be relevant to note that in 2004, the Food and Drug Administration added a boxed warning to the labeling for the first-generation H1 antihistamine promethazine, including a contraindication for use in children younger than 2 years of age because of continued reports of serious adverse events, such as respiratory depression and central nervous system reactions, including seizures.5

AUTHOR INFORMATION

Correspondence: Dr Simons, The University of Manitoba, 820 Sherbrook St, Winnipeg, Manitoba, Canada R3A 1R9 (lmcniven@hsc.mb.ca).

Financial Disclosure: None reported.

Merenstein  D, Diener-West  M, Halbower  AC, Krist  A, Rubin  HR. The trial of infant response to diphenhydramine: the TIRED study—a randomized, controlled, patient-oriented trial. Arch Pediatr Adolesc Med 2006;160707- 712
PubMed
Simons  FER. Advances in H1-antihistamines. N Engl J Med 2004;3512203- 2217
PubMed
Wyngaarden  JB, Seevers  MH. The toxic effects of antihistaminic drugs. JAMA 1951;145277- 282
PubMed
Baker  AM, Johnson  DG, Levisky  JA.  et al.  Fatal diphenhydramine intoxication in infants. J Forensic Sci 2003;48425- 428
PubMed
Starke  PR, Weaver  J, Chowdhury  BA. Boxed warning added to promethazine labeling for pediatric use. N Engl J Med 2005;3522653
PubMed

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Merenstein  D, Diener-West  M, Halbower  AC, Krist  A, Rubin  HR. The trial of infant response to diphenhydramine: the TIRED study—a randomized, controlled, patient-oriented trial. Arch Pediatr Adolesc Med 2006;160707- 712
PubMed
Simons  FER. Advances in H1-antihistamines. N Engl J Med 2004;3512203- 2217
PubMed
Wyngaarden  JB, Seevers  MH. The toxic effects of antihistaminic drugs. JAMA 1951;145277- 282
PubMed
Baker  AM, Johnson  DG, Levisky  JA.  et al.  Fatal diphenhydramine intoxication in infants. J Forensic Sci 2003;48425- 428
PubMed
Starke  PR, Weaver  J, Chowdhury  BA. Boxed warning added to promethazine labeling for pediatric use. N Engl J Med 2005;3522653
PubMed

Correspondence

January 1, 2007
Dan Merenstein, MD; Marie Diener-West, PhD; Ann C. Halbower, MD; Alex Krist, MD, MPH; Haya R. Rubin, MD, PhD
Arch Pediatr Adolesc Med. 2007;161(1):105-105.
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