In the United States, Seldane was brought to market in 1985 as the first nonsedating antihistamine for the treatment of allergic rhinitis.[1][4] In June 1990, evidence of serious ventricular arrhythmias among those taking Seldane prompted the FDA to issue a report on the risk factors associated with concomitant use of the drug with macrolide antibiotics and ketoconazole.[1] Two months later, the FDA required the manufacturer to send a letter to all physicians, alerting them to the problem; in July 1992, the existing precautions were elevated to a black box warning[1] and the issue attracted mass media attention in reports that people with liver disease or who took ketoconazole, an antifungal agent, or the antibiotic erythromycin, could suffer cardiac arrhythmia if they also took Seldane.[4] In January 1997, the same month when the U.S. Food and Drug Administration (FDA) had earlier approved a generic version of Seldane made by IVAX Corporation of Miami, the FDA recommended terfenadine-containing ...
TY - JOUR. T1 - A double-blind evaluation of skin test suppression produced by two doses of terfenadine. AU - Bantz, Eric W.. AU - Dolen, William K.. AU - Nelson, Harold S.. PY - 1987/1/1. Y1 - 1987/1/1. N2 - For some patients, terfenadine, in the currently recommended dose of 60 mg twice daily (bid), may be only modestly effective in the treatment of allergic rhinitis. In a double-blind placebo-controlled crossover study of 12 patients, a larger dose (300 mg bid) was evaluated for its suppression of titrated skin tests to histamine and compound 48/80 to determine whether this regimen might result in greater suppression while it maintained the freedom from side effects of the presently recommended dose. In seven patients, skin test suppression by these two doses of terfenadine, each administered for 3 days, was compared to that produced in an earlier study by 3 days of treatment with chlorpheniramine (8 mg three times a day). The 300 mg bid terfenadine regimen produced significantly greater skin ...
The major finding of these experiments is that terfenadine and astemizole significantly inhibited the IK1 in both guinea pig and rat ventricular myocytes. In the rat myocytes, both drugs also blocked a component of the Ito. Terfenadine, but not astemizole, additionally blocked IK to a small extent. The results of our experiments with terfenadine are consistent with previous studies showing the suppressive effect of terfenadine on the IK in cat and human myocytes.27 28 In cat ventricular myocytes, the IK-associated tail currents on deactivation of the channel were prominent and were markedly suppressed by terfenadine.27 In guinea pig ventricular myocytes, we did not find a similarly large suppression of IK tail current. However, the amplitude of the tail current appears to be somewhat species dependent, ie, quite large in cat, shark, and frog ventricular myocytes and relatively small in human and rodent myocytes.27 28 29 30 31 32 In addition, since deactivation of IK at −40 mV may activate a ...
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... ! Fexofenadine is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms. Fexofenadine, like other second-generation antihistamines, does not readily enter the brain from the blood, and so causes less drowsiness than first generation histamine receptor antagonists; Fexofenadine hydrochloride (brand names include Fexofenadine and Telfast) is an antihistamine drug used in the treatment of hayfever and similar allergy symptoms.
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Fexofenadine hydrochloride is the active ingredient in Allegra tablets and Allegra orally disintegrating tablets, according to RxList. It is also the active ingredient in Allegra oral suspension....
... What is fexofenadine? Fexofenadine hydrochloride (usually shortened to fexofenadine) is often used for hay fever. Its a non-drowsy antihistamine that can help to relieve symptoms of allergies. Some of the other conditions that fexofenadine
Fexofenadine, sold under the brand name Allegra and FX 24 among others is an antihistamine pharmaceutical medication utilized in the treatment of hypersensitivity indications, for example, roughage fever and urticaria. Restoratively, fexofenadine is a particular fringe H1-blocker. Fexofenadine is named a second-age antihistamine since it is less ready to pass the blood-cerebrum hindrance and cause sedation, contrasted with original antihistamines. It has additionally been known as a third-age antihistamine, even though there is some contention related to the utilization of the term.. It was licensed in 1979 and came into restorative use in 1996. Fexofenadine has been fabricated in a nonexclusive structure since 2011. Its typical to take fexofenadine once per day. Kids here and there take it two times every day. Fexofenadine is classed as a non-tired antihistamine, yet a few people still discover it makes them feel very lethargic. Regular reactions incorporate cerebral pains, feeling sluggish, ...
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Large complex polygons were generated by shortening effect ascribing the differences in APDs with numerous points lying distant from the identity type of the Poincar plot. Moreover, while 0. 01 and 0. 1 mM terfenadine did not somewhat increase STV during 0. 5 Hz, higher levels induced a decrease that became significant at 10 mM. Additionally, throughout the transition towards the steady state reduction in APD in Ivacaftor solubility LVMMs, terfenadine induced a marked upsurge in temporal BVR at 1 Hz. Figure 2A shows that before the shortening effect of 1 mM terfenadine, the progression towards the plateau phase of the AP, although not APD, was affected. Even though between 198 and records 170, the best shift of the development phase became more pronounced, and the plateau phase was depressed, APD wasnt afflicted, and terfenadine caused the loss in AP dome. During the transition to the steady-state decline in APD, large variations in effective APDs were seen. Four out-of 10 myocytes showed this ...
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4723 Background: ATN is an oral selective endothelin A receptor antagonist in phase 3 clinical development for treatment of hormone-refractory prostate cancer. ATN is not a p-glycoprotein (Pgp) substrate, but inhibits Pgp with an IC50 ∼12 μM (|50-fold the mean plasma Cmax for 10 mg/d ATN, although maximal intestinal concentrations may be 80 μM). The antihistamine FEX is a sensitive probe Pgp substrate; in clinical trials, Pgp inhibitors erythromycin and ketoconazole increased FEX AUC |2-fold. METHODS To assess the effect of ATN on FEX PK, a phase 1 open label study was conducted in 12 healthy subjects (10 M and 2 F; mean±SD 27±9 yrs, 75±10 kg). Subjects received FEX 120 mg PO on Days 1 and 8, and ATN 10 mg PO QD from Day 3 through 9. Blood and urine samples for FEX assay were collected predose and over 48 h after each FEX dose. Plasma and urine concentrations of FEX were determined using validated LC/MS/MS methods. RESULTS FEX PK are summarized (mean±SD; N=11) in the following table. [Figure
Use of any drugs known to induce or inhibit hepatic drug metabolism (examples of inducers: barbiturates, carbamazepine, phenytoin, glucocorticoids, rifampin/rifabutin; examples of inhibitors: antidepressants, cimetidine, diltiazem, erythromycin, ketoconazole, MAO inhibitors, neuroleptics, verapamil, quinidine), use of an investigational drug or participation in an investigational study within 30 days prior to administration of the study medication ...
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Telfast (Fexofenadine 120mg) contains the active ingredient fexofenadine hydrochloride which is an antihistamine. It is suitable for adolescents over the age of
This study supports the need to model the dynamic nature of hERG channel pharmacology, especially trapping, to explain why some drugs with similar hERG-blocking potency have different proarrhythmic liabilities. Together with multichannel pharmacology, our IKr-dynamic ORd model was able to stratify all CiPA training compounds into their corresponding TdP risk groups.. A unique feature of our approach is the use of a continuous parameter (Vhalf-trap) to represent the tendency of a drug to be trapped on hERG channel closing. Although the Vhalf-trap parameters appear consistent with previous classifications of compounds as either trapped or nontrapped by block recovery experiments, as in the case of dofetilide,26 bepridil, cisapride,11 and verapamil,21 some discrepancies exist. For instance, quinidine and terfenadine were considered nontrapped and trapped, respectively, in previous block recovery experiments11,26; however, quinidine seems to be more trapped than terfenadine based on their Vhalf-trap ...
Back DJ, Stevenson P, Tjia JF. Comparative effects of two antimycotic agents, ketoconazole and terbinafine on the metabolism of tolbutamide, ethinyloestradiol, cyclosporin and ethoxycoumarin by human liver microsomes in vitro. Br J Clin Pharmacol 1989; 28: 166-70PubMedCrossRefGoogle Scholar ...
The phenomenon of different assays providing different results for the same enzyme is most notable for CYP3A4 activity, as recent publications indicate. Wang et al. (2000) examined the mutual inhibition among the four commonly used CYP3A4 substrates testosterone, terfenadine, midazolam, and nifedipine. They found that although testosterone partially inhibits hydroxylation of terfenadine and midazolam, it does not inhibit nifedipine oxidation. Based on a study of the modulatory effect of 34 compounds on 10 commonly used CYP3A4-mediated reactions,Kenworthy et al. (1999) reported that the effect is substrate-dependent. Haloperidol, for example, activates dextromethorphan N-demethylation by 20%, but it inhibits nifedipine oxidation by 96%, even though CYP3A4 catalyzes both reactions. Stresser et al. (2000) showed that the extent of substrate dependence for the quantitative inhibition parameters (IC50) is as large as 195-fold among four tested CYP3A4 reactions.. The in vitro experimental conditions ...
Terfenadine has been reported to cause cardiac death. Hence, we investigated its pro-arrhythmic potential in various in vitro models. Pro-arrhythmic effects of terfenadine were investigated in rabbit isolated hearts and left ventricular wedge preparations. Also, using whole-cell patch-clamp recording, we examined its effect on the human ether-à-go-go-related gene (hERG) current ...
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Allegra has antihistamine properties which are used to treat seasonal allergy symptoms such as sneezing, runny nose, itchy throat, or itchy, watery eyes.
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Rev. May200ai Brief Summary ALLEGRA0 (fexofenadine hydrochloride) Capsules and Tablets INDICATIONSAND USAGESeasonal Allergic Rhinitis A LlGRAis indicated for the relief of symp toms associated with seasonal allergic rhinitis in adults and children 6 years of age and older. Symptoms Ireated effectively were sneezing, rhinorrhea. itchy nose/palate/throat, idhy/watery/red eves Chronic Idiooathi Urticaia ALLEGRAis indicatedfor treatment of uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. It significantly reduces pruritus and the number of wheals. CONTRAINDICATIONS AILEGRAis con traindicated in patients with known hypersensitivityto any of its ingredients PRECAUTIONSDrug Interaction with Erythromycn and Ketoconazole Fexolenadinmehydrochloride has been shown to exhihit minimal (cal 5)iimetabolism. However, co administration ol fexofenadine hydrochloride with ketoconazole and erythronmrin led to increased plasma levels of fexofenadine ...
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We investigated the involvement of serine protease and proteinase-activated receptor 2 (PAR2) in dermatophyte-induced itch in mice. An intradermal injection of an extract of the dermatophyte Arthroderma vanbreuseghemii (ADV) induced hind-paw scratching, an itch-related behavior. ADV extract-induced scratching was inhibited by the opioid receptor antagonists naloxone and naltrexone, the serine protease inhibitor nafamostat mesylate, and the PAR2 receptor antagonist FSLLRY-NH2. ADV extract-induced scratching was not inhibited by the H1 histamine receptor antagonist terfenadine or by mast cell deficiency. Heat pretreatment of the ADV extract markedly reduced the scratch-inducing and serine protease activities. Proteolytic cleavage within the extracellular N terminus of the PAR2 receptor exposes a sequence that serves as a tethered ligand for the receptor. The ADV extract as well as tryptase and trypsin cleaved a synthetic N-terminal peptide of the PAR2 receptor. The present results suggest that ...
Although increased serum histamine levels and H1R expression in the plaque are seen in atherosclerosis, it is not known whether H1R activation is a causative factor in the development of the disease, or is a host defense response to atherogenic signals. In order to elucidate how pharmacological inhibition of histamine receptor 1 (H1R) signaling affects atherogenesis, we administered either cetirizine (1 and 4 mg/kg. b.w) or fexofenadine (10 and 40 mg/kg. b.w) to ApoE2/2 mice maintained on a high fat diet for three months. Mice ingesting a low dose of cetirizine or fexofenadine had significantly higher plaque coverage in the aorta and cross-sectional lesion area at the aortic root. Surprisingly, the higher doses of cetirizine or fexofenadine did not enhance atherosclerotic lesion coverage over the controls. The low dose of fexofenadine, but not cetirizine, increased serum LDL cholesterol. Interestingly, the expression of iNOS and eNOS mRNA was increased in aortas of mice on high doses of ...
Summary of Facts and Submissions. I. The appeal lodged on 15 April 1998 lies from the decision of the Examining Division posted on 23. February 1998 refusing European patent application No. 96 200 338.0 (European publication No. 723 958).. II. The decision under appeal was based on a main request comprising claims 1 to 9 as originally filed and on three auxiliary requests. Independent original claim 1 according to the main request read as follows:. 1. A substantially pure piperidine derivative compound of the formulae:. FORMULA. or. FORMULA. wherein. R1 is hydrogen or hydroxy;. R2 is hydrogen;. or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;. R3 is -COOH or -COOR4;. R4 is an alkyl with 1 to 6 carbon atoms;. A, B and D can be one or more different substituents of their rings and are individually hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents or a salt thereof.. II. The Examining Division found that the present application lacked ...
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