Clinical Pharmacology Review for Primary Health Care Providers: I. Antihistamines

Seunghoon Han

doi:10.12793/tcp.2014.22.1.13

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Han: Clinical Pharmacology Review for Primary Health Care Providers: I. Antihistamines

Original Article

Translational and Clinical Pharmacology 2014;22(1):13-18.

Published online: 30 June 2014

DOI: https://doi.org/10.12793/tcp.2014.22.1.13

Clinical Pharmacology Review for Primary Health Care Providers: I. Antihistamines

Seunghoon Han^∗

Department of Clinical Pharmacology and Therapeutics, Seoul St. Mary's Hospital, The Catholic University of Korea, Seoul 137–701, Korea

^∗Correspondence: S. Han; Tel: +82-2-2258-7326, Fax: +82-2-2258-7876, E-mail: waystolove@catholic.ac.kr

Received 31 May 2014 Accepted 31 May 2014

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Primary health care providers play a critical role in maintaining public health, and the appropriate use of pharmaceutical products is one of the major parts of their practice. This series of articles, entitled ‘Clinical Pharmacology Review for Primary Health Care Providers,' is intended to help primary health care providers select more appropriate prescriptions for frequently used drugs based on up-to-date information. We expect that this effort will contribute to improvements in public health and diminish unnecessary drug use.

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Table 1.

Pharmacokinetic and pharmacodynamic characteristics of single-dose oral antihistamines in healthy young adults

Generation	Drug	Onset of action (h)	t_max (h)	Half-life (h)	Duration of action (h)	Drug interaction	Dose adjustment
1	Chlorpheniramine	0.5 – 3	2 – 3.6	20 – 36	24	Possible	NA
	Clemastine	2	NA	10 – 12	NA	Possible	NA
	Diphenhydramine	2	0.7 – 2.7	7 – 11	12	Possible	H
	Hydroxyzine	2	1.7 – 2.5	16 – 24	24	Possible	H
2	Cetirizine	1 – 3	0.5 – 1.5	7 – 10	≥ 24	Unlikely	H, R
	Desloratadine	2	1 – 3	27	≥ 24	Unlikely	H, R
	Ebastine	2	1.5∗	10 – 20∗	≥ 24	Possible	H, R
	Fexofenadine	2	2.5	14	24	Unlikely for CYP Possible for p-glycoprotein	R
	Levocetirizine	NA	0.3 – 1.3	5.5 – 8.5	≥ 24	Unlikely	H, R
	Loratadine	1 – 3	0.9 – 1.5	12 – 15	24	Unlikely	H, R
	Mizolastine	1	1.5	13	24	Possible	H

t_max, time between oral administration and peak plasma concentration; NA, No available information; H, Hepatic impairment; R, Renal impairment ∗With >50% coefficient of variation

Table 2.

Side effects of antihistamines according to the blocked receptors

H1 (histamine) receptor	Muscarinic receptor	α- adrenergic receptor	Serotonergic receptor	Cardiac channels
↓ CNS neurotransmission	urinary retention	hypotension (postural)	↑ appetite	QT prolongation
Sleepiness	sinusoidal tachycardia	dizziness		Ventricular arrhythmia
↓ cognitive function		reflex tachycardia
↑ appetite

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