Drugs. 2005;65(2):215-28.
Efficacy and tolerability of newer antihistamines in the treatment of allergic conjunctivitis.
Bielory L, Lien KW, Bigelsen S.
Department of Medicine, Pediatrics and Ophthalmology, Division of Allergy, Immunology and Rheumatology, UMDNJ-New Jersey Medical School, Immuno-Ophthalmology Service, 90 Bergen Street, DOC Suite 4700, Newark, NJ 07103, USA. bielory@umdnj.edu.

Treatment for allergic conjunctivitis has markedly expanded in recent years, providing opportunities for more focused therapy, but often leaving both physicians and patients confused over the variety of options. As monotherapy, oral antihistamines are an excellent choice when attempting to control multiple early-phase, and some late-phase, allergic symptoms in the eyes, nose and pharynx. Unfortunately, despite their efficacy in relief of allergic symptoms, systemic antihistamines may result in unwanted adverse effects, such as drowsiness and dry mouth. Newer second-generation antihistamines (cetirizine, fexofenadine, loratadine and desloratadine) are preferred over older first-generation antihistamines in order to avoid the sedative and anticholinergic effects that are associated with first-generation agents. When the allergic symptom or complaint, such as ocular pruritus, is isolated, focused therapy with topical (ophthalmic) antihistamines is often efficacious and clearly superior to systemic antihistamines, either as monotherapy or in conjunction with an oral or intranasal agent.Topical antihistaminic agents not only provide faster and superior relief than systemic antihistamines, but they may also possess a longer duration of action than other classes including vasoconstrictors, pure mast cell stabilisers, NSAIDs and corticosteroids. Many antihistamines have anti-inflammatory properties as well. Some of this anti-inflammatory effect seen with 'pure' antihistamines (levocabastine and emedastine) may be directly attributed to the blocking of the histamine receptor that has been shown to downregulate intercellular adhesion molecule-1 expression and, in turn, limit chemotaxis of inflammatory cells. Some topical multiple-action histamine H(1)-receptor antagonists (olopatadine, ketotifen, azelastine and epinastine) have been shown to prevent activation of neutrophils, eosinophils and macrophages, or inhibit release of leukotrienes, platelet-activating factors and other inflammatory mediators. Topical vasoconstrictor agents provide rapid relief, especially for redness; however, the relief is often short-lived, and overuse of vasoconstrictors may lead to rebound hyperaemia and irritation. Another class of topical agents, mast cell stabilisers (sodium cromoglicate [cromolyn sodium], nedocromil and lodoxamide), may be considered; however, they generally have a much slower onset of action. The efficacy of mast cell stabilisers may be attributed to anti-inflammatory properties in addition to mast cell stabilisation. In the class of topical NSAIDs, ketorolac has been promoted for ocular itching but has been found to be inferior for relief of allergic conjunctivitis when compared with olopatadine and emedastine. Lastly, topical corticosteroids may be considered for severe seasonal ocular allergy symptoms, although long-term use should be avoided because of risks of ocular adverse effects, including glaucoma and cataract formation.

BMJ. 2002 Jan 19;324(7330):144-6.
Randomised controlled trial of butterbur and cetirizine for treating seasonal allergic rhinitis.
Schapowal A; Petasites Study Group.
Allergy Clinic, Hochwangstrasse 3, CH-7302 Landquart, Switzerland.

OBJECTIVES: To compare the efficacy and tolerability of butterbur (Petasites hybridus) with cetirizine in patients with seasonal allergic rhinitis (hay fever). DESIGN: Randomised, double blind, parallel group comparison. SETTING: Four outpatient general medicine and allergy clinics in Switzerland and Germany. PARTICIPANTS: 131 patients were screened for seasonal allergic rhinitis and 125 patients were randomised (butterbur 61; cetirizine 64). INTERVENTIONS: Butterbur (carbon dioxide extract tablets, ZE 339) one tablet, four times daily, or cetirizine, one tablet in the evening, both given for two consecutive weeks. MAIN OUTCOME MEASURES: Scores on SF-36 questionnaire and clinical global impression scale. RESULTS: Improvement in SF-36 score was similar in the two treatment groups for all items tested hierarchically. Butterbur and cetirizine were also similarly effective with regard to global improvement scores on the clinical global impression scale (median score 3 in both groups). Both treatments were well tolerated. In the cetirizine group, two thirds (8/12) of reported adverse events were associated with sedative effects (drowsiness and fatigue) despite the drug being considered a non-sedating antihistamine. CONCLUSIONS: The effects of butterbur are similar to those of cetirizine in patients with seasonal allergic rhinitis when evaluated blindly by patients and doctors. Butterbur should be considered for treating seasonal allergic rhinitis when the sedative effects of antihistamines need to be avoided.

Allerg Immunol (Paris). 1989 Oct;21(8):312-3, 316, 318.
Importance of Zyrtec in the treatment of chronic urticaria and allergic rhinopathies apropos of 1168 cases seen by hospital practitioners
Billardon M.
Laboratoires Nanterre, France.

This was a phase IV prospective trial involving out-patients from 80 hospital respiratory diseases and ENT departments, and 40 hospital dermatology departments. More than 1,000 cases were collected and used to evaluate the efficacy of Zyrtec at the dose of 10 mg per day. The aim of the trial was to assess the rapidity of action and good acceptability of treatment for 10 days and 2 weeks respectively in cases of seasonal and perennial rhinopathy. Similarly, in pruritic allergic skin disorders, the aim was to measure the degree of activity and acceptability of treatment for 2 weeks. Overall evaluation of results provided clinical evidence of satisfactory rapidity of action with an appreciable acceptability level. This prospective study confirms the good therapeutic index of Zyrtec as a new anti-allergic agent.

Ann Allergy Asthma Immunol 2002 Dec;89(6):589-98
The comparison of the efficacy and safety of cetirizine, oxatomide, ketotifen, and a placebo for the treatment of childhood perennial allergic rhinitis
Lai DS, Lue KH, Hsieh JC, Lin KL, Lee HS
Department of Pediatrics, Chung Shan Medical University Hospital, Taichung, Taiwan, ROC.

BACKGROUND: There has been no study comparing the long-term effects of ketotifen, oxatomide, and cetirizine for the treatment of perennial allergic rhinitis among children. OBJECTIVE: We conducted a study to compare the efficacy of the three agents for the treatment of perennial allergic rhinitis among children. METHODS: The study consisted of a double-blind, placebo-controlled, randomized design, comprising 69 perennial allergic rhinitis patients with mite allergy, aged 6 to 12 years, randomly assigned to 1 of 4 test treatment groups for 3 months: 19 in the cetirizine group (10 mg daily), 18 in the ketotifen group (1 mg, twice daily), 16 in the oxatomide group (1 mg/kg, twice daily), and 16 in the placebo group. We used the nasal symptom score of diary card and the Pediatric Rhinoconjunctivitis Quality of Life Questionnaire and eosinophil cation protein peripheral blood total eosinophil count and immunoglobulin E level, eosinophil proportion from a nasal smear, and nasal peak expiratory flow rate to evaluate the effect of the four agents. RESULTS: Cetirizine was significantly more effective at reducing the mean rhinorrhea score compared with oxatomide for both weeks 8 and 12 (P < 0.01). Before the end of week 12, cetirizine was significantly more effective than ketotifen (P < 0.01). Cetirizine and oxatomide significantly decreased the mean Pediatric Rhinoconjunctivitis Quality of Life Questionnaire score compared with the placebo for week 12 (P < 0.05). CONCLUSIONS: Cetirizine was more effective than oxatomide and ketotifen for the relief of nasal congestion and rhinorrhea, and was responsible for significantly decreasing the eosinophil representation of a posttreatment nasal smear.

Drug information

GENERIC NAME: cetirizine
BRAND NAME: Zyrtec

DRUG CLASS AND MECHANISM: Cetirizine is the fourth addition to a new generation of allergy medications called "non- sedating" antihistamines or histamine (H-1) receptor blockers. These new antihistamines are called non-sedating because they cause less sedation than their predecessors; however, cetirizine is more sedating than the other non-sedating antihistamines.

Antihistamines block the effects of histamines. Histamines cause symptoms of allergy when released by allergic reactions in the body. Antihistamines block the ability of histamine to promote the allergy symptoms. For further information, please read the Allergic Rhinitis article.

PREPARATIONS: 5mg and 10mg oral tablets.

STORAGE: Store in a dry place at 15-30 degrees C (59- 86 F).

PRESCRIBED FOR: Cetirizine is used by people who suffer from allergic symptoms such as sneezing, itchy nose (allergic rhinitis) and itchy eyes. It also has been used to treat hives.

DOSING: Cetirizine should be taken at doses specifically directed by a physician. Cetirizine can be taken with food.

DRUG INTERACTIONS: Cetirizine should be taken only in doses prescribed. Increasing the dose can be dangerous. When taking cetirizine with theophylline the dose of theophylline may need to be reduced. Cetirizine occasionally can cause sleepiness . Cetirizine can be taken with erythromycin or ketaconazole without the increased risk of heart irregularities common to other non-sedating antihistamines. Cetirizine also can be used to treat children.

SIDE EFFECTS: Sleepiness occurs in 14% of patients. Dry mouth, nausea, headache, fatigue, jitteriness and sore throat are infrequently reported with cetirizine.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.

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MILGAMMA

Substance (drage): 250 mcg cyancobalaminum, 50 mg benfotiaminum.
Substance (injection): 1 mg cyancobalaminum, 100 mg pyridoxinum chloratim, 100 mg thiaminium chloratum, 20 mg lidocainium chloratum / 2 ml
Substance (capsules): 250 mcg cyancobalaminum, 40 mg benfotiaminum, 90 mg pyridoxinium chloratum

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