Acute Urticaria Medication

  • Author: Henry K Wong, MD, PhD; Chief Editor: Michael A Kaliner, MD   more...
 
Updated: Jun 14, 2011
 

Medication Summary

Use of antihistamines is the mainstay of therapy. In acute cases, a short course of steroids can be very effective. Long-term treatment with steroids should be avoided, if possible, but may be necessary in severe cases. A number of other classes of medicines have been found to be effective, mostly on an experimental basis. If urticaria does not respond to antihistamine treatment (with the possible addition of a short course of steroids), then referral to a specialist is indicated.[67, 36, 49, 68, 69]

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H1 Antagonists (first-generation antihistamines)

Class Summary

Primary agents used for urticaria.[10] The older, first-generation H1 antagonists (eg, diphenhydramine, hydroxyzine) are effective in reducing the lesions and pruritus but can produce adverse effects, such as drowsiness and anticholinergic effects.[46]

The first-generation agents can be useful if administered at bedtime because the sedative effects can help with sleep; however, the patient must be warned that the sedation and cognitive effects may continue until the next day. Any patient who is taking a medication that has potential sedative effects should be cautioned about driving and operating heavy machinery. Commonly used first-generation agents include diphenhydramine, hydroxyzine, doxepin, chlorpheniramine, and cyproheptadine.

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Diphenhydramine (Benadryl, Benylin)

 

Diphenhydramine is a common first-generation agent that is available without a prescription in the United States and can be used to control pruritus. It acts by competitive inhibition of histamine at the H1 receptor, which mediates the wheal-and-flare reactions.

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Cyproheptadine (Periactin)

 

Cyproheptadine is a first-generation agent and historically has been a drug of choice for prophylaxis of primary acquired cold-induced urticaria.

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Chlorpheniramine (Chlor-Trimeton)

 

Chlorpheniramine is a first-generation agent and is one of the safest antihistamines to use during pregnancy.

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Hydroxyzine (Atarax, Vistaril, Vistazine)

 

Hydroxyzine is used for control of pruritus. It is an effective first-generation agent but frequently produces sedation, particularly with higher doses. Historically, it has been considered a drug of choice for cholinergic urticaria. SC and IV are not recommended administration routes. Hydroxyzine also may suppress histamine activity in the subcortical region of the CNS.

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H1 Antagonists (second-generation antihistamines)

Class Summary

The newer second-generation antihistamines are nonsedating in most patients, with very few adverse effects reported. These agents are preferred for chronic urticaria, with first-generation agents reserved for acute or refractory cases. Commonly used H1 antagonists currently available in the United States are cetirizine, levocetirizine, desloratadine, loratadine, and fexofenadine.

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Loratadine (Claritin, Alavert)

 

Loratadine selectively inhibits peripheral histamine H1 receptors. It is tolerated very well, with a rate of sedation that is not significantly different from that of placebo. The once-daily dosing makes it convenient.

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Fexofenadine (Allegra)

 

Fexofenadine is a second-generation agent that is effective in urticaria. It is tolerated very well, with a rate of sedation that is not significantly different from that of placebo. Fexofenadine competes with histamine for H1 receptors on the GI tract, blood vessels, and respiratory tract, reducing hypersensitivity reactions.

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Desloratadine (Clarinex)

 

Desloratadine is a long-acting tricyclic histamine antagonist selective for H1 receptors. It is a major metabolite of loratadine, which, after ingestion, is metabolized extensively to active metabolite 3-hydroxydesloratadine.

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Levocetirizine (Xyzal)

 

Levocetirizine is a histamine1-receptor antagonist and an active enantiomer of cetirizine. Peak plasma levels are reached within 1 hour, and the half-life is about 8 hours. It is available as a 5-mg breakable (scored) tab and is indicated for uncomplicated skin manifestations of chronic idiopathic urticaria

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Cetirizine (Zyrtec)

 

Cetirizine is a second-generation agent that is frequently used in urticaria. It acts by competitive inhibition of histamine at the H1 receptor. Once-daily dosing makes it convenient, and sedation occurs in approximately 10% of patients. Dosing qhs may be useful if sedation is a problem. Although the standard dose is 5-10 mg qd, some specialists increase this to 10 mg bid for chronic urticaria that is not responding to the usual FDA-approved maximum dose.

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H2 antagonists (antihistamines)

Class Summary

These are reversible, competitive blockers of histamine at H2 receptors, particularly those in gastric parietal cells. The H2 antagonists are highly selective, do not affect H1 receptors, and are not anticholinergic agents. They block the vasodilation mediated by the H2 receptors in blood vessels, possibly leading to less edema formation in urticaria.

When used as single agents for urticaria, they are not effective. However, the combination of an H1 antagonist with an H2 antagonist is more effective than an H1 antagonist alone.[48, 49] Any of the H2 blockers can be used. Two of the most commonly used agents are ranitidine and cimetidine.

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Famotidine (Pepcid)

 

Famotidine is an H2 antagonist that, when combined with an H1 type, may be useful in treating allergic reactions that do not respond to H1 antagonists alone.

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Cimetidine (Tagamet)

 

Cimetidine is an H2 antagonist that, when combined with an H1 antagonist, may be useful in treating itching and flushing in urticaria and contact dermatitis that do not respond to H1 antagonists alone. Use in addition to H1 antihistamines.

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Ranitidine (Zantac)

 

Ranitidine is an H2 antagonist that, when combined with an H1 type, may be useful in treating urticaria when urticaria is not responsive to H1 antagonists alone.

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Corticosteroids

Class Summary

In instances of acute or chronic urticaria in which antihistamines may fail, even at high doses, or adverse effects may be problematic, mediators other than histamine may be involved. In such situations, corticosteroids may be administered. If not, then consider the possibility of another disease process (eg, malignancy, mastocytosis,[70] vasculitis). Corticosteroids may also be used in urticarial vasculitis, which usually does not respond to antihistamines.

A short course of an oral corticosteroid (administered daily for 5-7 d, with or without a taper) or a single dose of a long-acting injectable steroid is not usually associated with long-term sequelae and can be helpful when used for an acute episode of urticaria nonresponsive to antihistamines.[23]

Because of adverse effects of chronic or recurrent use of systemic corticosteroids, the long-term use of these agents should be avoided, when possible. If urticaria is severe and cannot be safely controlled with other medications, low-dose therapy and/or alternate day therapy can be considered.

A large number of preparations are available. Representative examples are prednisolone, methylprednisolone, and prednisone.

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Prednisolone (Pediapred, Prelone, Delta-Cortef)

 

Prednisone is a commonly used oral agent that must be metabolized to the active metabolite prednisolone for effect. Conversion may be impaired in liver disease. It is useful in cases that have not responded to traditional antihistamine. For extensive, symptomatic urticaria, a burst of prednisone over 4 days can lead to marked improvement and control of symptoms. Prednisone decreases inflammation by suppressing migration of polymorphonuclear leukocytes and by reversing increased capillary permeability.

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Methylprednisolone (Medrol, Depo-Medrol, Solu-Medrol)

 

Methylprednisolone is used for the treatment of severe urticaria reactions. It reverses increased capillary permeability.

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Prednisone (Deltasone, Orasone, Meticorten)

 

Prednisolone is available in both tablet and liquid forms. It reduces capillary permeability.

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Sympathomimetic Agents

Class Summary

These agents cause vasoconstriction and reduction in vascular dilation, which contributes to urticaria formation.

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Epinephrine (Adrenalin, Sus-Phrine, Epi-Pen, Ana-Guard, Twinject)

 

Epinephrine is DOC for the treatment of severe or generalized urticaria as part of an anaphylactic reaction. The alpha-agonist effects of this medication increase peripheral vascular resistance and reverse peripheral vasodilatation, vascular permeability, and systemic hypotension. Conversely, the beta-agonist effects of epinephrine produce bronchodilatation, cause positive inotropic and chronotropic cardiac activity, and result in an increased production of intracellular cAMP. Any patient who has had a potentially life-threatening allergic reaction should have injectable epinephrine available for use at all times (eg, portable Epi-Pen). Intramuscular administration of epinephrine is preferred over subcutaneous.

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Leukotriene Receptor Antagonist

Class Summary

In recent years, leukotriene receptor antagonists (eg, montelukast) have been added to antihistamines to control urticaria.

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Montelukast (Singulair)

 

Montelukast is a potent and selective antagonist of leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1. It prevents or reverses some of the pathologic features associated with the inflammatory process mediated by leukotrienes C4, D4, and E4. It is available as a tablet, chewable tablet, or PO granules. Granules may be administered directly in the mouth or dissolved in 1 tsp of cold or room-temperature baby formula, breast milk, or food (stable with applesauce, carrots, rice, or ice cream).

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Zafirlukast

 

Zafirlukast inhibits the effects by leukotriene receptors, whose activity has been associated with airway edema, smooth muscle contraction, and cellular activity associated with the symptoms.

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Tricyclic Antidepressants

Class Summary

These agents are a complex group of drugs that have central and peripheral anticholinergic effects, as well as sedative effects, and block the active reuptake of norepinephrine and serotonin. Some TCAs (eg, doxepin) have antihistamine effects, blocking both the H1 and H2 receptors and have been used in the treatment of allergic reactions, especially urticaria.

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Doxepin (Sinequan, Adapin, Zonalon)

 

Doxepin inhibits histamine and acetylcholine activity and has proven to be useful in the treatment of allergic dermatologic disorders. It has both H1 antagonist activity and H2 antagonist activity that is far more potent than traditional antihistamines. It also has antidepressant properties attributed to blocking MAO.

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Contributor Information and Disclosures
Author

Henry K Wong, MD, PhD  Associate Professor of Dermatology, Ohio State University College of Medicine

Henry K Wong, MD, PhD is a member of the following medical societies: American Academy of Dermatology, American Association of Immunologists, International Society for Cutaneous Lymphomas, and Society for Investigative Dermatology

Disclosure: EISAI Consulting fee Speaking and teaching; Amgen Consulting fee Speaking and teaching; Abbott Labs Honoraria Speaking and teaching; Centocor Honoraria Speaking and teaching; Celgene Grant/research funds None

Coauthor(s)

Jeffrey P Callen, MD  Professor of Medicine (Dermatology), Chief, Division of Dermatology, University of Louisville School of Medicine

Jeffrey P Callen, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Dermatology, American College of Physicians, and American College of Rheumatology

Disclosure: Amgen Honoraria Consulting; Abbott Honoraria Consulting; Electrical Optical Sciences Consulting fee Consulting; Celgene Honoraria Safety Monitoring Committee; GSK - Glaxo Smith Kline Consulting fee Consulting; TenXBioPharma Consulting fee Safety Monitoring Committee

Kevin P Connelly, DO  Clinical Assistant Professor, Department of Pediatrics, Division of General Pediatrics and Emergency Care, Virginia Commonwealth University School of Medicine; Medical Director, Paws for Health Pet Visitation Program of the Richmond SPCA; Pediatric Emergency Physician, Emergency Consultants Inc, Chippenham Medical Center

Kevin P Connelly, DO is a member of the following medical societies: American Academy of Pediatrics, American College of Osteopathic Pediatricians, and American Osteopathic Association

Disclosure: Nothing to disclose.

Steven A Conrad, MD, PhD  Chief, Department of Emergency Medicine; Chief, Multidisciplinary Critical Care Service, Professor, Department of Emergency and Internal Medicine, Louisiana State University Health Sciences Center

Steven A Conrad, MD, PhD is a member of the following medical societies: American College of Chest Physicians, American College of Critical Care Medicine, American College of Emergency Physicians, American College of Physicians, International Society for Heart and Lung Transplantation, Louisiana State Medical Society, Shock Society, Society for Academic Emergency Medicine, and Society of Critical Care Medicine

Disclosure: Nothing to disclose.

Daniel J Hogan, MD  Clinical Professor of Internal Medicine (Dermatology), Nova Southeastern University College of Osteopathic Medicine; Investigator, Hill Top Research, Florida Research Center

Daniel J Hogan, MD is a member of the following medical societies: Alpha Omega Alpha, American Academy of Dermatology, American Contact Dermatitis Society, and Canadian Dermatology Association

Disclosure: Nothing to disclose.

Shih-Wen Huang, MD  Professor Emeritus, Pulmonology and Allergy, Department of Pediatrics University of Florida College of Medicine

Shih-Wen Huang, MD, is a member of the following medical societies: American Academy of Allergy Asthma and Immunology

Disclosure: Nothing to disclose.

Harumi Jyonouchi, MD  Associate Professor, Division of Pulmonary Allergy/Immunology and Infectious Diseases, Department of Pediatrics, UMDNJ-New Jersey Medical School

Harumi Jyonouchi, MD is a member of the following medical societies: American Academy of Allergy Asthma and Immunology, American Academy of Pediatrics, American Association of Immunologists, American Medical Association, Clinical Immunology Society, New York Academy of Sciences, Society for Experimental Biology and Medicine, Society for Mucosal Immunology, and Society for Pediatric Research

Disclosure: Nothing to disclose.

M Scott Linscott, MD, FACEP  Professor, Division of Emergency Medicine, Professor of Surgery (Clinical), University of Utah School of Medicine

M Scott Linscott, MD, FACEP is a member of the following medical societies: American College of Emergency Physicians, Society for Academic Emergency Medicine, and Utah Medical Association

Disclosure: Nothing to disclose.

Umer Najib, MD  Clinical Research Fellow, Department of Medicine, Division of Allergy and Inflammation, Beth Israel Deaconess Medical Center

Disclosure: Nothing to disclose.

Robert A Schwartz, MD, MPH  Professor and Head, Dermatology, Professor of Pathology, Pediatrics, Medicine, and Preventive Medicine and Community Health, University of Medicine and Dentistry of New Jersey-New Jersey Medical School

Robert A Schwartz, MD, MPH is a member of the following medical societies: Alpha Omega Alpha, American Academy of Dermatology, American College of Physicians, and Sigma Xi

Disclosure: Nothing to disclose.

Javed Sheikh, MD  Assistant Professor of Medicine, Harvard Medical School; Clinical Director, Division of Allergy and Inflammation, Clinical Director, Center for Eosinophilic Disorders, Beth Israel Deaconess Medical Center

Javed Sheikh, MD is a member of the following medical societies: American Academy of Allergy Asthma and Immunology and American College of Allergy, Asthma and Immunology

Disclosure: Nothing to disclose.

Specialty Editor Board

Stephen C Dreskin, MD, PhD  Professor of Medicine, Departments of Internal Medicine, Director of Allergy, Asthma, and Immunology Practice, University of Colorado Health Sciences Center

Stephen C Dreskin, MD, PhD is a member of the following medical societies: American Academy of Allergy Asthma and Immunology, American Association for the Advancement of Science, American Association of Immunologists, American College of Allergy, Asthma and Immunology, Clinical Immunology Society, and Joint Council of Allergy, Asthma and Immunology

Disclosure: Genentech Consulting fee Consulting; American Health Insurance Plans Consulting fee Consulting; Johns Hopkins School of Public Health Consulting fee Consulting; Array BioPharma Consulting fee Consulting

Francisco Talavera, PharmD, PhD  Adjunct Assistant Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference

Disclosure: Medscape Salary Employment

Pamela L Dyne, MD  Professor of Clinical Medicine/Emergency Medicine, University of California, Los Angeles, David Geffen School of Medicine; Attending Physician, Department of Emergency Medicine, Olive View-UCLA Medical Center

Pamela L Dyne, MD is a member of the following medical societies: American Academy of Emergency Medicine, American College of Emergency Physicians, and Society for Academic Emergency Medicine

Disclosure: Nothing to disclose.

Dirk M Elston, MD  Director, Department of Dermatology, Geisinger Medical Center

Dirk M Elston, MD is a member of the following medical societies: American Academy of Dermatology

Disclosure: Nothing to disclose.

Chief Editor

Michael A Kaliner, MD  Clinical Professor of Medicine, George Washington University School of Medicine; Chief, Section of Allergy and Immunology, Washington Hospital Center; Medical Director, Institute for Asthma and Allergy

Michael A Kaliner, MD is a member of the following medical societies: American Academy of Allergy Asthma and Immunology, American Association of Immunologists, American College of Allergy, Asthma and Immunology, American Society for Clinical Investigation, American Thoracic Society, and Association of American Physicians

Disclosure: Alcon Consulting fee Consulting; Greer Consulting fee Consulting; Sanofi Consulting fee Consulting; Schering/Merck Consulting fee Consulting; Teva Consulting fee Consulting; Meda Honoraria Speaking and teaching; Ista Consulting

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Urticaria associated with a drug reaction.
Urticaria developed after bites from an imported fire ant.
Local urticaria on a patient with latex allergy who was touched with a latex glove.
Urticaria from drug reaction.
Photograph of dermographism.
Pressure urticaria (dermatographia) developed after strokes.
Acute urticaria associated with dermatographism.
Urticaria associated with acute group A beta-hemolytic streptococci infection.
Acute urticaria in a toddler affecting the face. Likely cause is postviral syndrome.
 
 
 
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