[Successful and effective: Montelukast in clinical practice]

[Article in German]

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Montelukast. No current use for asthma.

[Article in English, French]

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Montelukast (Singulair), an antiasthma drug belonging to the leukotriene antagonist family, has two indications: as adjunctive treatment for mild-to-moderate chronic asthma when regular inhaled steroid therapy and short-acting inhaled beta2 stimulants "on demand" are inadequate; and in prevention of effort-induced asthma. The clinical file on montelukast contains no methodologically acceptable comparisons with reference treatments. Several placebo-controlled trials have shown the efficacy of montelukast, with improvement in clinical scores and respiratory function tests in those with chronic asthma and prevention of effort-induced asthma. For chronic asthma, montelukast has not been compared with oral or inhaled long-acting beta2 stimulants or with sustained-release theophylline in patients inadequately controlled by steroid therapy. For effort-induced asthma, only two trials have compared montelukast with salmeterol.On the basis of preliminary results, the authors of both studies concluded that montelukast was superior. Clinical trials showed no clear difference in the frequency of side effects in patients taking montelukast and patients taking placebo. Montelukast, however, might be associated with Churg-Strauss syndrome in rare cases. Montelukast is expensive.

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Correction: montelukast in asthma management

Blake KV.

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[Treatment of ASS-Associated Polyposis (ASSAP) with a cysteinyl leukotriene receptor antagonist - a prospective drug study on its antiinflammatory effects]

[Article in German]

Topfner M.

Universitats-Hals-Nasen-Ohrenklinik Hamburg-Eppendorf. grundman uke.uni-hamburg.de

BACKGROUND: In a high rate of cases with recurrent polyposis an association with ASS-intolerance is detectable despite missing pulmonary symptoms. New examinations of a disturbed arachidonic acid metabolism lead to the development of new therapeutical options. Treatment with leukotriene-receptor antogonists (LTA) showed primarily good results in therapy of ASS-associated asthma. METHODS: 18 patients with ASS-intolerance trias - diagnosed by oral provocation - were treated with the LTA Montelukast, after undergoing sinus surgery. Patients underwent a diagnostic pathway of provocation including four groups: recurrent chronic sinusitis, excessive polyposis, polyposis associated with asthma and anaphylactic symptoms after oral ASS-intake. Clinically we examined the following parameters periodically after sinus surgery: nasal and pulmonal symptoms by scoring levels, recurrency of polypoid hyperplasia by endoscopic follow-ups and serum ECP-levels. To evaluate antiinflammatory tissue effects of LTA EG1/EG2 labelled cells and cytokine levels of Interleukin 5 in mucosa samples of the lower turbinate were analysed under LTA-therapy. RESULTS: Under therapy with LTA we saw a beneficial effect on nasal and pulmonary symptoms and a significant reduction of recurrent polyposis in endoscopic examinations in relation to the untreated group. Results were proven by a permanent reduction of serum ECP-level. A reduction of the rate of EG2-positive cells according to decreased Interleukin 5 levels in the nasal mucosa unter LTA-treatment assumed antiinflammatory effects on ASS-associated polyposis. CONCLUSIONS: We could demonstrate antiinflammatory effects of Leukotriene-Receptor-Antagonists primarily during postoperative treatment of patients with ASS-associated nasal polyps.

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Characterization of the human cysteinyl leukotriene 2 receptor.

Evans JF.

Department of Pharmacology, University of Virginia, School of Medicine, Charlottesville, Virginia 22908, USA.

The contractile and inflammatory actions of the cysteinyl leukotrienes (CysLTs), LTC(4), LTD(4), and LTE(4), are thought to be mediated through at least two distinct but related CysLT G protein-coupled receptors. The human CysLT(1) receptor has been recently cloned and characterized. We describe here the cloning and characterization of the second cysteinyl leukotriene receptor, CysLT(2), a 346-amino acid protein with 38% amino acid identity to the CysLT(1) receptor. The recombinant human CysLT(2) receptor was expressed in Xenopus oocytes and HEK293T cells and shown to couple to elevation of intracellular calcium when activated by LTC(4), LTD(4), or LTE(4). Analyses of radiolabeled LTD(4) binding to the recombinant CysLT(2) receptor demonstrated high affinity binding and a rank order of potency for competition of LTC(4) = LTD(4) LTE(4). In contrast to the dual CysLT(1)/CysLT(2) antagonist, BAY u9773, the CysLT(1) receptor-selective antagonists MK-571, montelukast (Singulair(TM)), zafirlukast (Accolate(TM)), and pranlukast (Onon(TM)) exhibited low potency in competition for LTD(4) binding and as antagonists of CysLT(2) receptor signaling. CysLT(2) receptor mRNA was detected in lung macrophages and airway smooth muscle, cardiac Purkinje cells, adrenal medulla cells, peripheral blood leukocytes, and brain, and the receptor gene was mapped to chromosome 13q14, a region linked to atopic asthma.

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