Medication Summary
Most cases of simple acute urticaria can be treated with H1 antihistamine agents.[30] In cases of severe or persistent urticaria, H2 antihistamines may be added and are probably additive to the effect of H1 antihistamines if given simultaneously intravenously.[25] This combination may also be effective orally in a small percentage of patients with chronic urticaria.[23] If the patient with chronic urticaria is refractory to nonsedating antihistamines, doses up to 4 times the recommended maximal dose may be effective.[23] If maximum doses of nonsedating antihistamines are not effective, other therapies should be tried.[31, 32]
Refractory cases of chronic urticaria may improve with glucocorticosteroids. Chronic urticaria may benefit from doxepin, a tricyclic antidepressant with potent antihistamine properties. Because of its significant sedative properties, it should be given at bedtime. Topical therapy with 5% doxepin cream (Zonalon) or capsaicin may also be used in refractory cases. Cyproheptadine may be useful to suppress recurrent cold urticaria. One study showed that the combination of a leukotriene receptor antagonist and a nonsedating antihistamine was superior to the antihistamine alone in treating chronic idiopathic urticaria.[33] Cyclosporine and omalizumab have been shown to be effective in cases of refractory chronic urticaria.[34, 6, 35]
H1-receptor antagonist antihistamines
Class Summary
These agents block the histamine response in sensory nerve endings and blood vessels. They act by competitive inhibition of histamine at the H1 receptor, which mediates wheal and flare reactions, bronchial constriction, mucus secretion, smooth muscle contraction, and edema. Because they have significant anticholinergic activity, especially the older sedating antihistamines, they may cause hypotension, CNS depression, urinary retention, and cardiac arrhythmias, especially in higher therapeutic doses or overdoses.
Hydroxyzine hydrochloride (Atarax, Vistaril)
Sedating peripheral H1 receptor antagonist. Very effective in urticaria. Also may suppress histamine activity in subcortical region of CNS.
Diphenhydramine (Benadryl, Benylin, Diphen)
Sedating peripheral H1 receptor antagonist. Used for symptomatic relief of allergic symptoms caused by histamine released in response to allergens.
Cyproheptadine (Periactin)
Sedating H1 antihistamine for symptomatic relief of allergic symptoms caused by histamine released in response to allergens and skin manifestations.
Cetirizine (Zyrtec)
Selectively inhibits peripheral histamine H1-receptors. Minimally sedating.
Levocetirizine (Xyzal)
Histamine1-receptor antagonist. Active enantiomer of cetirizine. Peak plasma levels reached within 1 h and half-life is about 8 h. Available as a 5-mg breakable (scored) tab. Indicated for seasonal and perennial allergic rhinitis.
Fexofenadine (Allegra)
Selectively inhibits peripheral histamine H1-receptors. Minimally sedating.
Loratadine (Claritin, Alavert)
Selectively inhibits peripheral histamine H1-receptors. Minimally sedating.
Desloratadine (Clarinex)
Long-acting tricyclic histamine antagonist selective for H1-receptor. Major metabolite of loratadine, which after ingestion is extensively metabolized to active metabolite 3-hydroxydesloratadine.
Tricyclic antidepressants (TCAs)
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.
Doxepin (Sinequan, Adapin, Zonalon)
Inhibits histamine and acetylcholine activity and has proven useful in treatment of allergic dermatologic disorders.
Glucocorticoids
Class Summary
These agents decrease the inflammation associated with urticaria resistant to H1- and H2-receptor antihistamine therapy. They do not inhibit mast cell degranulation and are of limited efficacy in acute urticaria. They are often effective in chronic urticaria but should be tapered to the lowest effective dose to prevent long-term complications.
Prednisone (Deltasone, Orasone, Meticorten)
Used in treatment of various allergic and inflammatory diseases. Decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reversing increased capillary permeability.
H2-receptor antagonists
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.
The combination of H1 and H2 antagonists may be useful in acute urticaria as well as chronic idiopathic urticaria not responding to H1 antagonists alone. This combination in IV form also may be useful for itching and flushing in anaphylaxis, pruritus, urticaria, and contact dermatitis.
Famotidine (Pepcid)
H2 antagonist that, when combined with an H1 type, may be useful in treating allergic reactions that do not respond to H1 antagonists alone.
Ranitidine (Zantac)
H2 antagonist that, when combined with an H1 type, may be useful in treating allergic reactions that do not respond to H1 antagonists alone.
Cimetidine (Tagamet)
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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