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1.
Korean Circulation Journal ; : 960-969, 2017.
Article in English | WPRIM | ID: wpr-123311

ABSTRACT

BACKGROUND AND OBJECTIVES: Dilated cardiomyopathy can be the end-stage of severe cardiac disorders and directly affects the cardiac muscle, inducing cardiomegaly and heart failure (HF). Although a wide variety of animal models are available to study dilated cardiomyopathy, there is no model to assess dilated cardiomyopathy with non-invasive, simple, and large screening methods. METHODS: We developed a dilated cardiomyopathy model in zebrafish larvae using short duration terfenadine, a known cardiotoxic drug that induces ventricular size dilation. Fractional shortening of zebrafish hearts was calculated. RESULTS: We treated zebrafish with 5 to 10 µM terfenadine for 24 hours. In terfenadine-treated zebrafish, blood frequently pooled and clotted in the chamber, and circulation was remarkably reduced. Atria and ventricles were swollen, and fluid was deposited around the heart, mimicking edema. Cardiac contractility was significantly reduced, and ventricular area was significantly enlarged. Heart rate was markedly reduced even after terfenadine withdrawal. Acridine orange staining also showed that terfenadine increased cardiomyocyte apoptosis. A significant increase of natriuretic peptide B (NPPB) mRNA was found in terfenadine-treated zebrafish. A low dose of terfenadine (5–10 µM) did not show mortality in short-term treatment (24 hours). However, moderate dose (35–45 µM) terfenadine treatment reduced zebrafish survival within 1 hour. CONCLUSION: With advantages of rapid sample preparation procedure and transparent observation of the live heart, this model can potentially be applied to large-scale drug screening and toxicity assays for non-ischemic HF.


Subject(s)
Acridine Orange , Apoptosis , Cardiomegaly , Cardiomyopathies , Cardiomyopathy, Dilated , Drug Evaluation, Preclinical , Edema , Heart , Heart Failure , Heart Rate , Larva , Mass Screening , Models, Animal , Mortality , Myocardium , Myocytes, Cardiac , RNA, Messenger , Terfenadine , Zebrafish
2.
Journal of Zhejiang University. Medical sciences ; (6): 155-159, 2014.
Article in Chinese | WPRIM | ID: wpr-336726

ABSTRACT

<p><b>OBJECTIVE</b>To establish a precolumn chiral derivatization method for determination of fexofenadine enantiomers, a chiral substrate of OATP1B1, in cellular model.</p><p><b>METHODS</b>R-(+)-phenylethyl isocyanate was selected as chiral derivatization reagent, which was reacted with fexofenadine to form carbamate derivatives. Enantiomers were identified by LC/MS and separated by RP-HPLC.</p><p><b>RESULTS</b>Under the experimental conditions, the fexofenadine enantiomers were separated completely. The standard curve was linear over the concentration range of 25-100 ng/ml (R(2)=0.9992, 0.9989). Accuracy was 101.1% and 98.3%, intra-precision was 2.4% and 3.1%, inter-precision was 3.1% and 4.0% for D1 and D2, respectively.</p><p><b>CONCLUSION</b>The method established is sensitive and accurate for determination of fexofenadine enantiomers in cells.</p>


Subject(s)
Chromatography, High Pressure Liquid , Methods , Stereoisomerism , Terfenadine
3.
Article in English | IMSEAR | ID: sea-157539

ABSTRACT

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.


Subject(s)
Acetates/administration & dosage , Acetates/analogs & derivatives , Acetates/pharmacology , Adult , Drug Combinations , Female , Humans , India , Male , Middle Aged , Quinolines/administration & dosage , Quinolines/analogs & derivatives , Quinolines/pharmacology , Product Surveillance, Postmarketing , Rhinitis, Allergic/drug therapy , Rhinitis, Allergic/epidemiology , Terfenadine/administration & dosage , Terfenadine/analogs & derivatives , Terfenadine/pharmacology , Treatment Outcome
4.
Journal of Rhinology ; : 20-25, 2013.
Article in Korean | WPRIM | ID: wpr-14327

ABSTRACT

BACKGROUND: Montelukast is a type 1 cysteinyl-leukotrienes receptor antagonist that has been widely used in allergic disease. However, the effect of combination of leukotriene receptor antagonist and antihistamine is controversial. The aim of this study was to compare the effect of combination treatment of montelukast and antihistamine, fexofenadine, over antihistamine alone in patients with allergic rhinitis (AR). SUBJECTS AND METHODS: Retrospective chart review of 60 patients with AR was undertaken. Patients were classified into combination group (montelukast and fexofenadine, n=28) and antihistamine only group (fexofenadine, n=32) according to treatment modalities. Questionnaire survey was performed and allergic symptoms (VAS scale, 5pointscale), and SNOT (sinonasal outcome test)-20 score were obtained before and after the treatment. RESULTS: Mean follow-up duration was 6.7+/-4.6weeks. There was no significant difference in demographic data between two groups. Allergic symptoms and SNOT-20 score(nasal, QOL domain) were improved significantly in both groups after the treatment (all p 0.05, respectively). CONCLUSION: A combination treatment of montelukast and fexofenadine showed more efficacies in nasal obstruction than single fexofenadine treatment in patients with AR. Therefore, montelukast could be used effectively with antihistamine in patients with AR complaining nasal congestion.


Subject(s)
Humans , Acetates , Estrogens, Conjugated (USP) , Follow-Up Studies , Nasal Obstruction , Quinolines , Receptors, Leukotriene , Retrospective Studies , Rhinitis , Rhinitis, Allergic, Perennial , Terfenadine , Surveys and Questionnaires
5.
Pakistan Journal of Pharmacology. 2011; 28 (1): 43-49
in English | IMEMR | ID: emr-178290

ABSTRACT

Fexofenadine hydrochloride is a piperidine derivative. It is indicated to relive signs and symptoms that are related with seasonal allergic rhinitis, such as rhinorrhea, sneezing, nose, throat and itchy eyes. In the present research work a liquid chromatographic method was developed for the determination of Fexofenadine in tablets and the dissolution method by UV/VIS spectrophotometer was also developed. Method was developed by using Lichrospher 10 micro m [C18] column. The mobile phase is composed of acetonitrile-5mM ammonium acetate buffer [50:50, v/v] pumped at a flow rate of 1 ml/min. The UV detector was operated at 254nm. The method was validated for system suitability, accuracy/recovery, linearity, system precision, method precision, ruggedness, robustness, limit of detection and limit of quantitation. Similarly, for dissolution method difference concentrations of standard and sample solutions were prepared i.e. 65 micro g/ml, 35 micro g/ml, 17.5 micro g/ml, 8.75 micro g/ml and 4.375 micro g/ml. The proposed HPLC method was easy, precise and fewer time consuming. The linearity for the dissolution method was found to be acceptable. The correlation coefficient of standard solutions was 0.9979 similarly the correlation coefficient of sample solutions was 0.9963


Subject(s)
Terfenadine/analysis , Chromatography, High Pressure Liquid , Chemistry, Pharmaceutical
6.
Annals of Dermatology ; : S329-S332, 2011.
Article in English | WPRIM | ID: wpr-165618

ABSTRACT

Fexofenadine (Allegra(R) 180) is a second-generation antihistamine. It is widely used as anti-allergic drug, which suppresses various allergic reactions mediated by histamines. A few cases of H1-antihistamine-induced urticaria have been reported. Herein, we report a rare case of fexofenadine-induced urticaria which was confirmed by a prick test, oral provocation test, and flow cytometry assisted-basophil activation test.


Subject(s)
Basophil Degranulation Test , Flow Cytometry , Hypersensitivity , Terfenadine , Urticaria
7.
Annals of Dermatology ; : S371-S374, 2011.
Article in English | WPRIM | ID: wpr-165607

ABSTRACT

Aquagenic urticaria is a rare form of physical urticaria, in which contact with water evokes wheals. A 19-year-old man and a 4-year-old boy complained of recurrent episodes of urticaria. Urticaria appeared while taking a bath or a shower, in the rain, or in a swimming pool. Well-defined pin head to small pea-sized wheals surrounded by variable sized erythema were provoked by contact with water on the face, neck, and trunk, regardless of its temperature or source. Results from a physical examination and a baseline laboratory evaluation were within normal limits. Treatment of the 19-year-old man with 180 mg fexofenadine daily was successful to prevent the wheals and erythema. Treatment with 5 ml ketotifen syrup bid per day resulted in improvement of symptoms in the 4-year-old boy.


Subject(s)
Humans , Young Adult , Baths , Erythema , Head , Ketotifen , Neck , Physical Examination , Child, Preschool , Rain , Swimming Pools , Terfenadine , Urticaria , Water
8.
Indian J Dermatol Venereol Leprol ; 2008 Jul-Aug; 74(4): 361-3
Article in English | IMSEAR | ID: sea-52178

ABSTRACT

BACKGROUND: Histamine is the major mediator of allergic reactions. Newer H1 antihistaminics like levocetirizine, fexofenadine, and desloratadine are used in the treatment of seasonal and perennial allergic rhinitis and urticaria. The ability to block the cutaneous response to intradermal histamine is used to evaluate the potential of antihistamines. AIMS: To compare the potency, onset, and duration of action of the commonly used antihistamines-levocetirizine, fexofenadine, and desloratadine. METHODS: Thirty volunteers were given three single doses of levocetirizine, fexofenadine and desloratadine at weekly intervals. A pretest was performed by using the intradermal histamine prick test. After administration of the drugs, the intradermal test was repeated at (1/2), 1, 2, 3, 6 and 24 h, and the sizes of the wheal were measured. The mean values were taken and were compared by using Levene's t-test. RESULTS: At 30 min, fexofenadine showed a statistically significant suppression of wheal size compared to levocetirizine and desloratadine. Two and three hours after administration, levocetirizine and fexofenadine showed statistically significant inhibition of wheal size while only levocetirizine had this effect after six hours when compared to desloratadine. Desloratadine showed greater inhibition of wheal size at the end of 24 h when compared to levocetirizine and fexofenadine but this was not statistically significant. CONCLUSIONS: Fexofenadine had the earliest onset of action while levocetirizine showed maximum inhibition of wheal response after three and six hours.


Subject(s)
Adolescent , Adult , Cetirizine/pharmacology , Histamine/administration & dosage , Histamine H1 Antagonists, Non-Sedating/pharmacology , Humans , Injections, Intradermal , Loratadine/analogs & derivatives , Middle Aged , Terfenadine/analogs & derivatives , Time Factors , Urticaria/chemically induced , Young Adult
9.
Saudi Medical Journal. 2008; 29 (3): 333-339
in English | IMEMR | ID: emr-90133

ABSTRACT

The interaction of natural products and drugs is a common hidden problem encountered in clinical practice. The interactions between natural products and drugs are based on the same pharmacokinetic and pharmacodynamic principles as drug-drug interactions. Clinically important interactions appear to involve effects on drug metabolism via cytochrome P-450 isoenzymes, impairment of hepatic or renal function, and other possible mechanisms. To effectively counsel patients on interactions involving natural products, physicians, and pharmacists should be familiar with the most commonly used products, and have access to information on more obscure products. In this review, we describe details of drugs interaction with natural products and its impact on drug therapy management


Subject(s)
Humans , Herb-Drug Interactions , Cytochrome P-450 Enzyme System , Citrus paradisi/adverse effects , Felodipine/pharmacokinetics , Terfenadine/pharmacokinetics , Itraconazole/pharmacokinetics , Cisapride/pharmacokinetics , Spinacia oleracea/adverse effects , Solanum lycopersicum/adverse effects , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics
10.
Korean Journal of Dermatology ; : 151-159, 2008.
Article in Korean | WPRIM | ID: wpr-187500

ABSTRACT

BACKGROUND: Fexofenadine (Allegra(R)) is a H1-receptor selective antihistamine which exhibits consistent efficacy and safety in the treatment of allergic diseases. We thought that fexofenadine may be useful in treatment of the pruritus associated with eczema. OBJECTIVE: The purpose of this study was to evaluate the efficacy and safety of fexofenadine in the treatment of pruritus associated with eczema. METHODS: In this study, patients with atopic and allergic contact dermatitis were divided into a group given fexofenadine 180 mg once daily with topical prednicarbate treatment group or a topical prednicarbate treatment only group, for 1 week. The primary efficacy parameter was the mean change from baseline in pruritus score, and the secondary parameters were the mean change in the incidence of scratching, the mean change in visual analogue scale (0~100 mm) of pruritus, and a comparison of patient satisfaction. RESULTS: 435 patients were included and the mean age was 32.9 years old. The mean pruritus score at baseline was 3.55 point in fexofenadine group and 3.51 point in the control group. Regarding the mean change in pruritus score, fexofenadine significantly decreased the severity of pruritus compared with the control group (p<0.05). There were no significant differences in the decrease in the incidence of scratching between the two groups. A decrease in pruritus levels utilizing visual analogue scale was significant in the fexofenadine group (p<0.05) and patient satisfaction was significantly higher in the fexofenadine group (p=0.0192). There was no significant difference in the incidence of adverse events between two groups (p=0.6237). CONCLUSION: Fexofenadine administered 180 mg once daily in combination with topical prednicarbate treatment was effective and well tolerated in this study.


Subject(s)
Humans , Dermatitis, Allergic Contact , Dermatitis, Atopic , Eczema , Incidence , Patient Satisfaction , Prednisolone , Pruritus , Terfenadine
11.
Korean Journal of Epidemiology ; : 128-136, 2008.
Article in Korean | WPRIM | ID: wpr-728955

ABSTRACT

PURPOSE: To estimate the prevalence of co-prescribing contraindicated drugs for elderly patients in Busan. METHODS: We used the Health Insurance Review Agency (HIRA) claims database. Study population consisted of elderly patients who visited clinics or hospitals in Busan metropolitan city from January 1, 2000 to December 31, 2001. Contraindicated drugs were defined as 162 combinations of contraindicated drugs announced by the Korea Ministry of Health and Welfare in 2004. The co-prescription of contraindicated drugs was defined as prescribing two or more contraindicated drugs in combination in the same prescription. The prevalence of co-prescribing contraindicated drugswas estimated as proportion of co-prescribed patients out of the study patients. We estimated and age-adjusted prevalence and its 95% confidence interval of co-prescription of contraindicated drugs among the elderly patients in Korean population in 2001. RESULTS: The study elderly patients were 262,952 with 2,483,227 prescriptions. Among the study patients 1,208 (4.6%) were prescribed contraindicated drugs in combination. A total of 16,255 patients were estimated as the number of co-prescribed patients among the Korean elderly in 2001. Age-standardized prevalence of co-prescription to the Korean elderly was estimated to be 45 per 10,000 persons. The most frequently prescribed combinations were cisapride & amitriptyline, roxithromycin & ergoloid mesylate, and terfenadine & erythromycin, and the frequency were 325 (16.8%), 149 (7.7%), and 132 (6.8%),respectively. CONCLUSIONS: The contraindicated drugs were co-prescribed to the elderly patients in Korea. Many of these co-prescriptions should be avoided if unnecessary. The patients should be carefully monitored if they were inevitably prescribed the contraindicated drugs.


Subject(s)
Aged , Humans , Amitriptyline , Cisapride , Drug Combinations , Drug Utilization Review , Ergoloid Mesylates , Erythromycin , Insurance, Health , Korea , Prescriptions , Prevalence , Roxithromycin , Terfenadine
12.
Experimental & Molecular Medicine ; : 284-294, 2007.
Article in English | WPRIM | ID: wpr-201426

ABSTRACT

The role of mast cells in tumor growth is still controversial. In this study we analyzed the effects of both histamine and pre-formed mediators spontaneously released by mast cells on the growth of two human hepatocellular carcinoma cell lines, HA22T/VGH and HuH-6, with different characteristics of differentiation, biological behavior and genetic defects. We showed that total mast cell releasate, exocytosed granules (granule remnants) and histamine reduced cell viability and proliferation in HuH-6 cells. In contrast, in HA22T/VGH cells granule remnants and histamine induced a weak but significant increase in cell growth. We showed that both cell lines expressed histamine receptors H1 and H2 and that the selective H1 antagonist terfenadine reverted the histamine-induced inhibition of HuH-6 cell growth, whereas the selective H2 antagonist ranitidine inhibited the histamine-induced cell growth of HA22T/VGH cells. We demonstrated that histamine down-regulated the expression of beta-catenin, COX-2 and survivin in HuH-6 cells and that this was associated with caspase-3 activation and PARP cleavage. On the contrary, in HA22T/VGH cells expression of survivin and beta-catenin increased after treatment with granule remnants and histamine. Overall, our results suggest that mediators stored in mast cell granules and histamine may affect the growth of liver cancer cells. However, mast cells and histamine may play different roles depending on the tumor cell features. Finally, these data suggest that histamine and histamine receptor agonists/antagonists might be considered as "new therapeutic" drugs to inhibit liver tumor growth.


Subject(s)
Animals , Female , Humans , Rats , Apoptosis , Carcinoma, Hepatocellular/metabolism , Caspase 3/metabolism , Cell Line, Tumor , Cell Proliferation , Cell Survival , Cells, Cultured , Cyclooxygenase 2/metabolism , Enzyme Activation , Exocytosis , Histamine/pharmacology , Histamine Antagonists/pharmacology , Liver Neoplasms/metabolism , Mast Cells/physiology , Microtubule-Associated Proteins/metabolism , Neoplasm Proteins/metabolism , Poly(ADP-ribose) Polymerases/metabolism , Ranitidine/pharmacology , Rats, Wistar , Receptors, Histamine/metabolism , Terfenadine/pharmacology , beta Catenin/metabolism
13.
Asian Pac J Allergy Immunol ; 2005 Dec; 23(4): 169-74
Article in English | IMSEAR | ID: sea-36672

ABSTRACT

Allergic rhinitis is one of the most common chronic disorders in children. It is also one of the most common causes of absence from school. This study reports on the efficacy and safety of a twice-daily oral dose of fexofenadine HCl 30 mg in Asian children aged 6-11 years diagnosed with seasonal or perennial allergic rhinitis. A total of 100 children with a history of allergic rhinitis for more than one year and a positive prick skin test response to at least one of the common aeroallergens in Thailand were enrolled in this multi-center, open-label, non comparative study. The severity of individual symptoms such as sneezing, rhinitis, etc. and adverse events were recorded in diary cards by the patients in form of scores as well as by the investigator at each visit. The total symptom score (TSS) with or without blocked nose at baseline, week 1 and week 2 was recorded. The TSS was defined as the sum of the individual symptom scores except for the nasal blockage score, as nasal blockage was not expected to respond to antihistamine treatment. Only patients with a total symptom score > or = 6 were included in the study. There was a statistically significant improvement at p < 0.01 for the TSS with or without blocked nose and for each symptom score such as blocked nose, sneezing, rhinorrhea, itchy nose/palate and/or throat, and itchy/watery/red eyes from baseline to week 1 and week 2. Additionally, there was a statistically significant improvement between week 1 and week 2 for itchy nose/palate and/or throat and itchy/watery/red eyes (p < 0.05). The Kappa measure of agreement was statistically significant at p < 0.001 between investigator's and patient's/parent's assessment, indicating the same degree of satisfaction with the overall effectiveness of the treatment. Fexofenadine 30 mg bid is effective in reducing the total symptom score of allergic rhinitis including blocked nose and is generally well tolerated. It is not cardiotoxic and is safe for pediatric patients as young as 6 years of age.


Subject(s)
Anti-Allergic Agents/administration & dosage , Asian People , Child , Female , Histamine H1 Antagonists/administration & dosage , Humans , Male , Multicenter Studies as Topic , Rhinitis, Allergic, Perennial/drug therapy , Rhinitis, Allergic, Seasonal/drug therapy , Terfenadine/administration & dosage , Treatment Outcome
14.
Asian Pac J Allergy Immunol ; 2005 Mar; 23(1): 35-9
Article in English | IMSEAR | ID: sea-36658

ABSTRACT

The main objective of this study was to investigate the ability of histamine receptor antagonists to modulate tryptase release from human colon mast cells induced by histamine. Enzymatically dispersed cells from human colon were challenged with histamine in the absence or presence of the histamine receptor antagonists, and the tryptase release was determined. It was found that histamine induced tryptase release from colon mast cells was inhibited by up to approximately 61.5% and 24% by the H1 histamine receptor antagonist terfenadine and the H2 histamine receptor antagonist cimetidine, respectively, when histamine and its antagonists were added to cells at the same time. The H3 histamine receptor antagonist clobenpropit had no effect on histamine induced tryptase release from colon mast cells at all concentrations tested. Preincubation of terfenadine, cimetidine or clobenpropit with cells for 20 minutes before challenging with histamine did not enhance the ability of these antihistamines to inhibit histamine induced tryptase release. Apart from terfenadine at 100 microg/ml, the antagonists themselves did not stimulate tryptase release from colon mast cells following both 15 minutes and 35 minutes incubation periods. It was concluded that H1 and H2 histamine receptor antagonists were able to inhibit histamine induced tryptase release from colon mast cells. This not only added some new data to our hypothesis of self-amplification mechanisms of mast cell degranulation, but also suggested that combining these two types of antihistamine drugs could be useful for the treatment of inflammatory bowel disease (IBD).


Subject(s)
Calcimycin/pharmacology , Cells, Cultured , Cimetidine/pharmacology , Colon/drug effects , Histamine/pharmacology , Histamine H1 Antagonists/pharmacology , Histamine H2 Antagonists/pharmacology , Humans , Imidazoles/pharmacology , Ionophores/pharmacology , Mast Cells/drug effects , Serine Endopeptidases/metabolism , Serine Proteinase Inhibitors/pharmacology , Terfenadine/pharmacology , Thiourea/analogs & derivatives , Tryptases
15.
Article in English | IMSEAR | ID: sea-40504

ABSTRACT

BACKGROUND AND OBJECTIVE: Non-sedating antihistamines (loratadine, fexofenadine, and cetirizine) have been widely used in Thailand. This study examined the time-of-onset and compared the 95% inhibitory effect of these agents on histamine-induced cutaneous reaction so as to understand the diversity of their efficacy. PATIENTS AND METHOD: Thirty-one atopic patients were randomized into 4 treatment groups, placebo (n = 7), loratadine (n = 8), fexofenadine (n = 8), and cetirizine (n = 8). They were pricked with histamine every 30 min for 4 hrs. The percentage change of the wheal/flare area was calculated. RESULTS: All active treatments showed wheal suppression superior to placebo after 210 min for loratadine (P = 0.04); 90 min for fexofenadine (P = 0.009); and 60 min for cetirizine (P = 0.02), while flare suppression was significantly marked after 150 min (P = 0.0008) for loratadine; 90 min for fexofenadine (P = 0.0001), and 60 min for cetirizine (P = 0.006). All drugs except loratadine demonstrated a 95% suppression of wheal superior to the placebo (P = 0.001 for fexofenadine; P = 0.0001 for cetirizine). Only fexofenadine exhibited a 95% suppression of flare statistically superior to placebo (P = 0.02). Discrepancies among the effects of these 3 antihistamines were also detected. DISCUSSION AND CONCLUSION: All antihistamines tested repressed the wheal-and-flare area superbly over the placebo within 4 hours. Cetirizine exerted the fastest onset, and it also appeared to be the most efficacious inhibitor. The heterogeneity of their efficacy probably stems from their diverse physicochemical properties, which have also been discussed.


Subject(s)
Adolescent , Adult , Cetirizine/pharmacokinetics , Female , Histamine H1 Antagonists, Non-Sedating/pharmacokinetics , Humans , Loratadine/pharmacokinetics , Male , Middle Aged , Terfenadine/analogs & derivatives , Urticaria/drug therapy
17.
RBM rev. bras. med ; 60(3): 121-130, mar. 2003. ilus, tab, graf
Article in Portuguese | LILACS | ID: lil-347200

ABSTRACT

As interaçöes medicamentosas que causam alteraçöes no metabolismo e biodisponibilidade das drogas têm sido parcialmente explicadas pelas atividades que estas drogas exercem sobre as isoenzimas do sistema citocromo P450 (CYP). Alguns estudos recentes, poréem, sugerem que novos sistemas transportadores ded droga chamados glicoproteína P (P-gp,P-glycoprotein) e polipeptidio transportador de ânions orgânicos (OATP, organic anion transporting polypeptide) porem causar o efluxo e influxo celular de várias classes de medicamentos. Estes mecanismos podem contribuir para as interaçöes medicamentosas por mecanismos independentes do metabolismo oxidativo via CYP. Alguns modelos experimentais criados para avaliar a funçäo da P-gp ou OATP demonstraram que pode haver alteraçöes desses transportadores com efeito significativo sobre a biodisponibilidade de rogas. Assim, a interferência sobre estes sistemas de transporte P-gp e OATP surge como um novo mecanismo potencialmente relacionado a interaçöes medicamentosas ae alimentares.au


Subject(s)
Drug Interactions , ATP Binding Cassette Transporter, Subfamily B, Member 1/adverse effects , Terfenadine
18.
Rev. invest. clín ; 54(3): 192-197, mayo-jun. 2002.
Article in Spanish | LILACS | ID: lil-332928

ABSTRACT

OBJECTIVE: To determine the frequency of concurrent use of cisapride, astemizole and terfenadine with macrolides and azole antimitotics, drug combinations that have been reported in the literature as producing a pharmacological interaction associated with potentially fatal ventricular arrhythmias. MATERIAL AND METHODS: A retrospective analysis of a total of 72,444 prescriptions generated by 611 physicians during a 6 months period for ambulatory patients, was performed. The database included a register of automatic alerts produced every time a predetermined drug combination was detected. RESULTS: 145 potentially risk situations were detected, with an incidence rate to 2.1 cases per 1,000 prescriptions, which increases to 6.2 when prescriptions for terfenadine, astemizole, and cisapride were included, with 12, 9 y 5, respectively. Only 36 physicians (6) wrote prescriptions producing alerts, and about half (45) were pediatricians. The same physician prescribed both drugs in 31 of the cases. CONCLUSION: The use of drug combinations associated with a high risk of potentially fatal ventricular arrhythmias is relatively high in Mexico. An electronic online detecting system showed to be useful in preventing this kind of potential pharmacological interactions.


Subject(s)
Humans , Male , Female , Infant , Child, Preschool , Child , Adolescent , Adult , Middle Aged , Online Systems , Terfenadine , Astemizole , Cisapride , Arrhythmias, Cardiac/chemically induced , Drug Information Services/organization & administration , Triazoles/adverse effects , Pilot Projects , Risk , Incidence , Retrospective Studies , Astemizole , Cisapride , Drug Utilization , Histamine H1 Antagonists , Mexico , Anti-Bacterial Agents/adverse effects , Antifungal Agents/adverse effects , Arrhythmias, Cardiac/epidemiology , Arrhythmias, Cardiac/prevention & control , Diagnosis-Related Groups , Drug Interactions , Drug Prescriptions/statistics & numerical data , Managed Care Programs/organization & administration , Pharmaceutical Services/organization & administration
19.
Asian Journal of Andrology ; (6): 291-294, 2002.
Article in English | WPRIM | ID: wpr-300921

ABSTRACT

<p><b>AIM</b>To investigate the role of fexofenadine, a mast cell blocker, on semen quality in the treatment of infertile men.</p><p><b>METHODS</b>The study included 16 Turkish idiopathic infertile men with azoospermia or oligozoospermia who underwent testicular biopsy to examine mast cells containing tryptase. In all patients, a complete medical history, clinical examination, semen analysis and serum hormone assay were carried out. The biopsy specimens were immunohistochemically stained with antihuman tryptase for mast cells. The number of total mast cells per seminiferous tubule was calculated and recorded as mast cell index. The patients were divided into two groups according to their mast cell index: the higher (> or =1, n=9) and the lower (<1, n=7) index groups. Fexofenadine was administered orally at a dose of 180 mg/day for 4 to 9 months. Pre- and post-treatment semen parameters, including total motile sperm counts (TMC) were recorded and compared. Spontaneous pregnancies after the treatment were registered.</p><p><b>RESULTS</b>There was no statistically significant difference in TMC between the pre-treatment and post-treatment values in patients with higher and lower mast cell index (P> or =0.05). In both groups, nobody had a significant response to the treatment and there was no spontaneous pregnancy after the treatment.</p><p><b>CONCLUSION</b>Although testicular dysfunction is closely associated with increased number of testicular mast cells, fexofenadine, a mast cell blocker, appears not having any benefit in the treatment of Turkish infertile men with a significant increase in testicular mast cells.</p>


Subject(s)
Adult , Humans , Male , Middle Aged , Biopsy, Needle , Follicle Stimulating Hormone , Blood , Histamine H1 Antagonists , Therapeutic Uses , Infertility, Male , Drug Therapy , Pathology , Mast Cells , Pathology , Semen , Physiology , Serine Endopeptidases , Metabolism , Sperm Count , Sperm Motility , Terfenadine , Therapeutic Uses , Testis , Pathology , Tryptases , Turkey
20.
Article in English | IMSEAR | ID: sea-40561

ABSTRACT

Fexofenadine is a non-sedating antihistamine indicated for relieving symptoms from allergic conditions with a rapid onset of action without cardiotoxic risks. Controlled studies showed that fexofenadine 180 mg daily provides significant relief of symptoms of chronic idiopathic urticaria (CIU). The purpose of this study was to demonstrate the efficacy and safety of fexofenadine 60 mg twice daily in Thai patients with CIU in a multicenter trial. Patients were assigned to receive twice daily doses of fexofenadine 60 mg for 6 weeks. Patients rated symptom severity every night, investigators rated patients' signs and symptoms at recruitment and at 1, 3 and 6 weeks. Ninety eight out of 108 patient (90.7%) completed the study. The patients reported 95 per cent improvement and, of those, 91 per cent had very favorable responses (excellent 15%, very good 42%, good 30%, fair 8%). The objective assessment by their physicians paralleled those responses. Fexofenadine provided a rapid clinical response that was significantly superior to before treatment in relieving symptoms of CIU (p < 0.001). Adverse events occurred in 20 cases (18.5%), mostly mild headache and drowsiness. Fexofenadine 60 mg twice daily provides effective relief of the symptoms of CIU with minimal adverse events.


Subject(s)
Adolescent , Adult , Aged , Aged, 80 and over , Chronic Disease , Female , Histamine H1 Antagonists/administration & dosage , Humans , Male , Middle Aged , Terfenadine/administration & dosage , Thailand , Urticaria/drug therapy
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