Efficacy and Safety of Montelukast Plus Fexofenadine Fixed Dose Combination in Allergic Rhinitis : Results of Post-Marketing Study In India.

Background:Allergic rhinitis is one of the most common conditions in clinical practice. Motelukast and second generation antihistamine fexofenadine are routinely used in the management of allergic rhinitis. Individually both drugs have been found to be effective in allergic rhinitis. Fixed dose combination of montelukast 10 mg plus fexofenadine 120 mg is available in India is also used in the treatment of allergic rhinitis. Objective: To evaluate the efficacy and safety of montelukast and fexofenadine fixed dose combination in the management of patients with allergic rhinitis. Material and methods: Post marketing observational study was conducted in 809 patients from all over India. All the patients were treated with montelukast 10 mg plus fexofenadine 120 mg fixed dose combination once daily for 14 days. The primary outcome criteria was the change in total symptom score (Sum of total nasal symptom score and total ocular symptom score) at the end of study compared to baseline. The secondary outcome criteria included change in total nasal symptom score (nasal congestion, rhinorrhea, nasal itching, and sneezing) and total ocular symptom score (Itching/burning eyes, tearing/ watering eyes and eye redness) at the end of study compared to baseline and physician’s and patient’s global assessment for efficacy and tolerability. The patients were evaluated at baseline, day 7 and day 14 for efficacy evaluation while the safety parameters were assessed at screening and day 14. Results: The fixed dose combination of fexofenadine plus montelukast was significantly effective in reducing total symptom score, total nasal symptom score and total ocular symptom score (p<0.0001 for all parameters). The global assessment of efficacy evaluation by both patient and investigators demonstrated “excellent to good” efficacy in >95% of patients. Most of the study population reported “good” tolerability with the fixed drug combination. No adverse events were reported in the study. Conclusion: The fixed dose combination of fexofenadine plus montelukast was found to be efficacious and well tolerated in allergic rhinitis in Indian adult patients.

Montelukast Induced Hypertriglyceridemia.

Montelukast a LT4 receptor antagonist is a prophylactic agent used in chronic asthma, to improve asthma control and reduce the frequency of asthma exacerbation. Advantage of Montelukast is, it is well tolerated in both adult and children upto 6 years of age. Suspected adverse effect reported to U.K, CSM follow the launch of Montelukast are anaphylaxis, angioedema, urticaria, chest pain, vertigo, athralgia, fever. Further suspected side effects are nightmare, palpitation, and sweating and Churg Strauss syndrome. Hypertriglyceridemia associated with this agent is rarely found in any published medical report or literature. This is a case of a male patient who was suffering from chronic asthma since childhood, developed allergic rhinitis since November´10. He developed hypertriglyceridemia and associated lipid profile abnormality after taking Montelukast and was also receiving salbutamol inhalation since childhood. His lipid profile before Montelukast administration was normal. Routine investigation done 4 months following drug intake shows serum triglyceride to be 732mg/dl.Montelukast was immediately withdrawn, but salbutamol was continued The triglyceride level reaches near the base line 4 months following drug withdrawal. This case highlights a rare case of Montelukast induced hypertriglyceridemia. Physician should be vigilant of the fact that Montelukast can induce hypertriglyceridemia following therapy with it.

case of Churg-Strauss syndrome treated with Montelukast

To report a case of Churg-Strauss syndrome who had asthma and allergic rhinitis treated with montelukast. A nonsmoking 59-year-old woman presented with fever, hemoptysis and dyspnea. Past medical history included allergic rhinitis and asthma which were diagnosed 18 years ago. The asthma was treated successfully with inhaled salmeterol and beclamethasone. She also received montelukast [10 mg/day] for 3 years. Although her chest X-ray was normal a week earlier, she had widespread bilateral pulmonary infiltrates on admission. She had leukocytosis [12.5 x 109/l] with eosinophilia [15.6%]. Her total IgE count was 550 U/ml. Testing for protoplasmic-staining antineutrophil cytoplasmic antibodies was positive. Bronchoalveolar lavage could not be performed due to bronchospasm and severe hypoxemia; however, mucosal biopsies were obtained, which revealed eosinophil leukocytes in the lumen and walls of small vessels. She was diagnosed to have Churg-Strauss syndrome and had remarkable clinical improvement on day 5 with high-dose of oral prednisolone [50 mg/day]. Radiological improvement was detected at the end of the second week. This case shows the importance of being aware that leukotriene receptor antagonists could cause Churg-Strauss syndrome, in spite of the uncertainty about its mechanism

New 4-substituted phenoxy quinolines of possible antimierobial activity

New series of semicarbazone and substituted thiosemicarbazones [3a-d], 7-chloro-4-[p-[4-aryl-3-cyano-2-oxo[1H] pyridin-6-yl] phenoxy] quinolines [4a-f], 7-chloro-4-[p-[4-aryl-3-cyano-2-imino[1H] pyridin-6-yl] phenoxy]quinolines [5a-e] and 7-chloro-4-[p-[4-aryl-3-cyano-2-thioxo [1H] pyridin-6-yl] phenoxy] quinoline [6a-c], were synthesized for the purpose of antimicrobial evaluation against Gram +ve, Gram -ve bacteria, yeast and fungi

Synthesis of some new 4-methylquinolines of possible biological activity

Some new 4,8-dimethyl-2 [p-[3-cyano-2-thioxo-4-arylpyridin-6-yl] anilinoquinolines [3a-d] and 7-chloro-4-methyl-2-[4-hydroxy] anilinoquinolines Mannich bases [5,6a-c] were synthesized for the purpose of antimicrobial evaluation against bacteria, yeast, and fungi. Some representative examples showed activity against these microorganisms

Synthesis of certain substituted quinolines as potential DNA complexing agents

Two series of 2,4,6-trisubstituted quinoline derivatives were prepared for potential DNA complexing activity. The first series comprises the preparation of 4-arylaminoquinoline derivatives 9-24 by amination of 4-chloroquinolines 5-8, while, the second series involves the preparation of the amide derivatives of cinchoninic acid 27-30 by amidation of 2-phenyl-4-cinchonoyl chloride 26. Three new compounds were tested for in vitor cytotoxic activity

Synthesis of some substituted 9-anilinoacridines and 4-anilinoquinolines of possible antitumor activity

3-amino-4-methoxybenzoie acid methyl ester and 3-amino- 4-methoxy-6- methane sulphonamidobenzoic acid methyl ester were condensed with 4, 7-dichloroquinoline, 4-chloroquinaldine, 9-chloroacridine and 2-methoxy-6,9-dichloro acridine. The anilide esters obtained were reduced to the corresponding alcohols from which the N-methylcarbamate derivatives were prepared as possible antitumour agents