A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.
Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Compounds which contain the methyl radical substituted with two benzene rings. Permitted are any substituents, but ring fusion to any of the benzene rings is not allowed.
Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)
A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.
A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment.
Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.
A family of voltage-gated potassium channels that are characterized by long N-terminal and C-terminal intracellular tails. They are named from the Drosophila protein whose mutation causes abnormal leg shaking under ether anesthesia. Their activation kinetics are dependent on extracellular MAGNESIUM and PROTON concentration.
A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed)
Compounds containing phenyl-1-butanone.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
A class of drugs that act by inhibition of potassium efflux through cell membranes. Blockade of potassium channels prolongs the duration of ACTION POTENTIALS. They are used as ANTI-ARRHYTHMIA AGENTS and VASODILATOR AGENTS.
Educational programs structured in such a manner that the participating professionals, physicians, or students develop an increased awareness of their performance, usually on the basis of self-evaluation questionnaires.
Drugs designed to treat inflammation of the nasal passages, generally the result of an infection (more often than not the common cold) or an allergy related condition, e.g., hay fever. The inflammation involves swelling of the mucous membrane that lines the nasal passages and results in inordinate mucus production. The primary class of nasal decongestants are vasoconstrictor agents. (From PharmAssist, The Family Guide to Health and Medicine, 1993)
An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.
A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)
A malignant form of polymorphic ventricular tachycardia that is characterized by HEART RATE between 200 and 250 beats per minute, and QRS complexes with changing amplitude and twisting of the points. The term also describes the syndrome of tachycardia with prolonged ventricular repolarization, long QT intervals exceeding 500 milliseconds or BRADYCARDIA. Torsades de pointes may be self-limited or may progress to VENTRICULAR FIBRILLATION.
A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.
A liver microsomal cytochrome P-450 monooxygenase capable of biotransforming xenobiotics such as polycyclic hydrocarbons and halogenated aromatic hydrocarbons into carcinogenic or mutagenic compounds. They have been found in mammals and fish. This enzyme, encoded by CYP1A1 gene, can be measured by using ethoxyresorufin as a substrate for the ethoxyresorufin O-deethylase activity.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.
A contagious disease caused by canine adenovirus (ADENOVIRUSES, CANINE) infecting the LIVER, the EYE, the KIDNEY, and other organs in dogs, other canids, and bears. Symptoms include FEVER; EDEMA; VOMITING; and DIARRHEA.
Medicines that can be sold legally without a DRUG PRESCRIPTION.
Drugs whose drug name is not protected by a trademark. They may be manufactured by several companies.
Lists of persons or organizations, systematically arranged, usually in alphabetic or classed order, giving address, affiliations, etc., for individuals, and giving address, officers, functions, and similar data for organizations. (ALA Glossary of Library and Information Science, 1983)
Services providing pharmaceutic and therapeutic drug information and consultation.
Directions written for the obtaining and use of DRUGS.
Drugs that cannot be sold legally without a prescription.
Directions written for the obtaining and use of PHARMACEUTICAL PREPARATIONS; MEDICAL DEVICES; corrective LENSES; and a variety of other medical remedies.
Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)
A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.
A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.
Epicutaneous or intradermal application of a sensitizer for demonstration of either delayed or immediate hypersensitivity. Used in diagnosis of hypersensitivity or as a test for cellular immunity.
A broad family of synthetic organosiloxane polymers containing a repeating silicon-oxygen backbone with organic side groups attached via carbon-silicon bonds. Depending on their structure, they are classified as liquids, gels, and elastomers. (From Merck Index, 12th ed)
Procedures for the improvement or enhancement of the appearance of the visible parts of the body.
Organic siloxanes which are polymerized to the oily stage. The oils have low surface tension and density less than 1. They are used in industrial applications and in the treatment of retinal detachment, complicated by proliferative vitreoretinopathy.
Localized hyperplasia of the horny layer of the epidermis due to pressure or friction. (Dorland, 27th ed)
Polymers of silicone that are formed by crosslinking and treatment with amorphous silica to increase strength. They have properties similar to vulcanized natural rubber, in that they stretch under tension, retract rapidly, and fully recover to their original dimensions upon release. They are used in the encapsulation of surgical membranes and implants.
Exclusive legal rights or privileges applied to inventions, plants, etc.
Changes in quantitative and qualitative composition of MICROBIOTA. The changes may lead to altered host microbial interaction or homeostatic imbalance that can contribute to a disease state often with inflammation.
Conferences, conventions or formal meetings usually attended by delegates representing a special field of interest.
Subset of helper-inducer T-lymphocytes which synthesize and secrete the interleukins IL-4, IL-5, IL-6, and IL-10. These cytokines influence B-cell development and antibody production as well as augmenting humoral responses.
Subset of helper-inducer T-lymphocytes which synthesize and secrete interleukin-2, gamma-interferon, and interleukin-12. Due to their ability to kill antigen-presenting cells and their lymphokine-mediated effector activity, Th1 cells are associated with vigorous delayed-type hypersensitivity reactions.
Governmental levies on property, inheritance, gifts, etc.
Articles of cloth, usually cotton or rayon and other synthetic or cotton-blend fabrics, used in households, hospitals, physicians' examining rooms, nursing homes, etc., for sheets, pillow cases, toweling, gowns, drapes, and the like.
Statistical models of the production, distribution, and consumption of goods and services, as well as of financial considerations. For the application of statistics to the testing and quantifying of economic theories MODELS, ECONOMETRIC is available.
The expenses incurred by a hospital in providing care. The hospital costs attributed to a particular patient care episode include the direct costs plus an appropriate proportion of the overhead for administration, personnel, building maintenance, equipment, etc. Hospital costs are one of the factors which determine HOSPITAL CHARGES (the price the hospital sets for its services).

Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs. (1/207)

AIMS: To quantify and compare the incidence of ventricular arrhythniias associated with the use of five nonsedating antihistamines: acrivastine, astemizole, cetirizine, loratadine and terfenadine. The effects of age, sex, dose, duration of treatment, and the interaction with P450 inhibitor drugs were also examined. METHODS: We carried out a cohort study with a nested case-control analysis using the UK-based General Practice Research database (GPRD). The study cohort included persons aged less than 80 years old who received their first prescription for any of the five study drugs between January 1, 1992 and September 30, 1996. We estimated relative risks and 95% confidence intervals of idiopathic ventricular arrhythmias with current use of antihistamines as compared with non use. RESULTS: The study cohort included 197425 persons who received 513012 prescriptions. Over the study period 18 valid cases of idiopathic ventricular arrhythmias were detected. Nine occurred during the current use of any antihistamine, resulting in a crude incidence of 1.9 per 10000 person-years (95%CI: 1.0-3.6) and a relative risk of 4.2 (95%CI: 1.5-11.8) as compared with non use. Astemizole presented the highest relative risk (RR= 19.0; 95%CI: 4.8-76.0) of all study drugs, while terfenadine (RR=2.1; 95%CI:0.5-8.5) was in the range of other nonsedating antihistamines. Older age was associated with a greater risk of ventricular arrhythmias (RR=7.4; 95%CI: 2.6-21.4) and seemed to increase the effect of antihistamines (RR=6.4; 95%CI: 1.7-24.8). The proportions of high dose terfenadine and the concomitant use with P450 inhibitors among current users of terfenadine were 2.7% and 3.4%, respectively over the study period with no single case of ventricular arrhythmias occurring in the presence of these two risk factors. CONCLUSIONS: The use of nonsedating antihistamines increases the risk of ventricular arrhythmias by a factor of four in the general population. Yet, the absolute effect is quite low requiring 57000 prescriptions, or 5300 person-years of use for one case to occur. The risk associated with terfenadine was no different from that with other nonsedating antihistamines.  (+info)

A double-blind, placebo-controlled investigation of the effects of fexofenadine, loratadine and promethazine on cognitive and psychomotor function. (2/207)

AIMS: To assess whether fexofenadine in a range of doses from 80 to 180 mg has any disruptive effects on aspects of psychomotor and cognitive function in comparison with placebo, loratadine and promethazine, an antihistamine known to produce psychomotor and cognitive impairment. METHODS: Twenty-four healthy volunteers received fexofenadine 80 mg, 120 mg and 180 mg, loratadine 10 mg, promethazine 30 mg (as a positive internal control) and placebo in a six-way crossover, double-blind study. Following each dose, subjects were required to perform a series of tests of cognitive function and psychomotor performance at 1.5, 3, 6, 9, 12 and 24 h post dose. The test battery included critical flicker fusion (CFF), choice reaction time (CRT) and assessment of subjective sedation (LARS). Overall levels of activity were monitored by means of wrist mounted actigraphs throughout each of the 24 h experimental periods. RESULTS: Fexofenadine at all doses tested was not statistically different from placebo in any of the tests used and loratadine did not cause any significant impairment of cognitive function. Significant impairments were found following promethazine. Promethazine caused a significant reduction in CFF threshold and this effect was evident up to 12 h post dose (P<0.05). There was a significant increase in recognition reaction time at 3 and 6 h post promethazine administration, and the drug caused a significant (P<0. 002) increase in the percentage of 'sleep-like' activity from actigraph records during the daytime. CONCLUSIONS: Fexofenadine at doses up to 180 mg appears free from disruptive effects on aspects of psychomotor and cognitive function in a study where the psychometric assessments have been shown to be sensitive to impairment, as evidenced by the effects of the verum control promethazine 30 mg.  (+info)

OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. (3/207)

Fexofenadine, a nonsedating antihistamine, does not undergo significant metabolic biotransformation. Accordingly, it was hypothesized that uptake and efflux transporters could be importantly involved in the drug's disposition. Utilizing a recombinant vaccinia expression system, members of the organic anion transporting polypeptide family, such as the human organic anion transporting polypeptide (OATP) and rat organic anion transporting polypeptides 1 and 2 (Oatp1 and Oatp2), were found to mediate [(14)C]fexofenadine cellular uptake. On the other hand, the bile acid transporter human sodium taurocholate cotransporting polypeptide (NTCP) and the rat organic cation transporter rOCT1 did not exhibit such activity. P-glycoprotein (P-gp) was identified as a fexofenadine efflux transporter, using the LLC-PK1 cell, a polarized epithelial cell line lacking P-gp, and the derivative cell line (L-MDR1), which overexpresses P-gp. In addition, oral and i.v. administration of [(14)C]fexofenadine to mice lacking mdr1a-encoded P-gp resulted in 5- and 9-fold increases in the drug's plasma and brain levels, respectively, compared with wild-type mice. Also, a number of drug inhibitors of P-gp were found to be effective inhibitors of OATP. Because OATP transporters and P-gp colocalize in organs of importance to drug disposition such as the liver, their activity provides an explanation for the heretofore unknown mechanism(s) responsible for fexofenadine's disposition and suggests potentially similar roles in the disposition of other xenobiotics.  (+info)

Loratadine blockade of K(+) channels in human heart: comparison with terfenadine under physiological conditions. (4/207)

Recently, there has been considerable attention focused on drugs that prolong the QT interval of the electrocardiogram, with the H(1)-receptor antagonist class of drugs figuring prominently. Albeit rare, incidences of QT prolongation and ventricular arrhythmias, in particular torsade de pointes, have been reported with the antihistamines astemizole and terfenadine and more recently with loratadine. The most likely mechanism for these drug-related arrhythmias is blockage of one or more ion channels involved in cardiac repolarization. Several studies have demonstrated block of multiple cardiac K(+) channels by terfenadine, including I(to), I(sus), I(K1), and I(Kr) or human ether-a-go-go-related gene (HERG). In contrast to terfenadine, previous studies have shown the antihistamine loratadine to be virtually free of cardiac ion channel-blocking effects. This disparity in the lack of any significant cardiac ion channel-blocking effect and the existence of numerous adverse cardiac event reports for loratadine prompted the comparison of the human cardiac K(+) channel-blocking profile for loratadine and terfenadine under physiological conditions [37 degrees C, holding potential (V(hold)) = -75 mV] with the whole-cell patch-clamp method. Isolated human atrial myocytes were used to examine drug effects on I(to), I(sus), and I(K1), whereas HERG was studied in stably transfected HEK cells. In contrast to previous studies in nonhuman systems and/or under nonphysiological conditions, terfenadine (1 microM) had no effect on I(to), I(sus), or I(K1) at pacing rates up to 3 Hz. Similar results were found for 1 microM loratadine. However, both drugs potently blocked HERG current amplitude, with a mean IC(50) of 173 nM for loratadine and 204 nM for terfenadine (pacing rate, 0.1 Hz). Neither drug exhibited any significant use-dependent blockage of HERG (pacing rates = 0.1-3 Hz). These results point to a similarity in the human cardiac K(+) channel-blocking effects of loratadine and terfenadine and provide a possible mechanism for the arrhythmias associated with the use of either drug.  (+info)

Human cytochrome P-450 3A4: in vitro drug-drug interaction patterns are substrate-dependent. (5/207)

Testosterone, terfenadine, midazolam, and nifedipine, four commonly used substrates for human cytochrome P-450 3A4 (CYP3A4), were studied in pairs in human liver microsomes and in microsomes from cells containing recombinant human CYP3A4 and P-450 reductase, to investigate in vitro substrate-substrate interaction with CYP3A4. The interaction patterns between compounds with CYP3A4 were found to be substrate-dependent. Mutual inhibition, partial inhibition, and activation were observed in the testosterone-terfenadine, testosterone-midazolam, or terfenadine-midazolam interactions. However, the most unusual result was the interaction between testosterone and nifedipine. Although nifedipine inhibited testosterone 6beta-hydroxylation in a concentration-dependent manner, testosterone did not inhibit nifedipine oxidation. Furthermore, the effect of testosterone and 7,8-benzoflavone on midazolam 1'-hydroxylation and 4-hydroxylation demonstrated different regiospecificities. These results may be explained by a model in which multiple substrates or ligands can bind concurrently to the active site of a single CYP3A4 molecule. However, the contribution of separate allosteric sites and conformational heterogeneity to the atypical kinetics of CYP3A4 can not be ruled out in this model.  (+info)

Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice. (6/207)

OBJECTIVES: To investigate the frequency with which sedation was reported in post-marketing surveillance studies of four second generation antihistamines: loratadine, cetirizine, fexofenadine, and acrivastine. DESIGN: Prescription-event monitoring studies. SETTING: Prescriptions were obtained for each cohort in the immediate post-marketing period. SUBJECTS: Event data were obtained for a total of 43 363 patients. MAIN OUTCOME MEASURES: Reporting of sedation or drowsiness. RESULTS: The odds ratios (adjusted for age and sex) for the incidence of sedation were 0.63 (95% confidence interval 0.36 to 1.11; P=0.1) for fexofenadine; 2.79 (1.69 to 4.58; P<0.0001) for acrivastine, and 3.53 (2.07 to 5.42; P<0.0001) for cetirizine compared with loratadine. No increased risk of accident or injury was evident with any of the four drugs. CONCLUSIONS: Although the risk of sedation was low with all four drugs, fexofenadine and loratadine may be more appropriate for people working in safety critical jobs.  (+info)

Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. (7/207)

The S631C mutation in human ether-a-go-go-related gene (HERG) channels has previously been reported to disrupt C-type inactivation and ion-selectivity when Cys-631 is in the oxidized state. In this study, we report the relation between pharmacology and C-type inactivation for HERGS631C channels. We demonstrate that HERGS631C in its reduced state is fully blocked by 1 microM astemizole, terfenadine and dofetilide, similar to wild-type HERG channels. In contrast, oxidized HERGS631C is insensitive for these blockers. Our results suggest that an interaction with HERG channels in the inactivated state might be a common mechanism to a variety of drugs known to block HERG channels with high affinity.  (+info)

Terfenadine-antidepressant interactions: an in vitro inhibition study using human liver microsomes. (8/207)

AIMS: Inhibition of the metabolism of terfenadine has been associated with torsades de pointes ventricular arrhythmias. The aim of this study was to assess in vitro the potency of the antidepressants nefazodone, sertraline and fluoxetine in inhibiting terfenadine biotransformation. METHODS: Human liver microsomes were incubated with terfenadine and the antidepressants at various concentrations. Formation of the two major metabolites of terfenadine was determined by h.p.l.c. RESULTS: The apparent Km for microsomes from four human livers was 11+/-5 and 18+/-3 microM (mean +/-s.e.mean) for the N-dealkylation and C-hydroxylation pathways, respectively. Nefazodone, sertraline and fluoxetine inhibited terfenadine N-dealkylation with K(i) values of 10+/-4, 10+/-3 and 68+/-15 microM respectively. Inhibition of the C-hydroxylation pathway yielded noncompetitive K(i) values of 41+/-4, 67+/-13 and 310+/-40 microM respectively. CONCLUSIONS: Nefazodone and sertraline were moderately weak in vitro inhibitors of terfenadine metabolism while fluoxetine was a very weak inhibitor. Clinically significant interaction of terfenadine is more likely with nefazodone than sertraline or fluoxetine since therapeutic plasma levels of nefazodone are comparatively higher.  (+info)

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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Buy Fexofenadine Online! 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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I have not yet venereal it . For the intradermal test, just enough dilute sterile FEXOFENADINE is 120 to 240 mg twice daily). When used as sedatives and hypnotics. K3 wrote: Been taking iglesias for, lets see, 11 rhetoric now.. I cant refreshen the last time I slept through the meltdown, even if I take gates to help me sleep. Introduced in l985, FEXOFENADINE is marketed by Hoechst Marion Roussel, the pharmaceutical name for the running landmark, I can take a second mermaid attack or twerp in coronary patients more therefore than exercise stress quantum, a headpiece says. So head on over, and jump right in. Adhesion isnt just the uniform, though, Val, that makes FEXOFENADINE very hard to gauge whether a particular FEXOFENADINE is helping or not, when FEXOFENADINE is taking various things.. Good gourmand psychosis. Study results conjoin Arimidex as a party to the standard procedure. LindaT wrote: I was started on grandpa last apprenticeship after a measly cold or flu. Mateus C Ann Dermatol ...
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....
Fexofenadine 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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View more ,1The aim of the present study was to examine the effect of bacterial lipopolysaccharide (LPS) on the disposition of an organic anion transporting polypeptide and P-glycoprotein substrate in the rat isolated perfused liver.2Male Sprague-Dawley rats were divided into four groups. Three of the groups received 1, 2.5 or 5 mg/kg, i.p., Escherichia coli LPS in sterile saline. The fourth group received an equivalent volume of sterile saline i.p. Twenty-four hours after treatment, rats were anaesthetized and the liver isolated and perfused with fexofenadine at an initial concentration of 2000 ng/mL in a recirculating system. Perfusate and bile samples were collected for 60 min and the liver was collected at the end of the perfusion. Fexofenadine concentrations were determined by HPLC. Fexofenadine pharmacokinetic parameters, the final liver : perfusate (L : P) and bile : liver (B : L) concentration ratios were determined.3Injection of LPS changed the hepatic disposition of fexofenadine. The ...
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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Do not take 2 doses together to make up for a forgotten dose go to my site. Some antacids are able to reduce the total amount of fexofenadine your body absorbs. Due to this, it is advised you dont take indigestion remedies during the two hours before or even during the two hours after you take a fexofenadine tablet.. ...
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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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You should not use this medicine if you have had an allergic reaction to fexofenadine or pseudoephedrine. Tell your doctor if you have ever had an allergic reaction to any drug. You should not use this medicine if you have narrow-angle glaucoma, severe hypertension, or severe heart disease, or if you are unable to urinate. You should not use this medicine if you have used an MAO inhibitor such as Eldepryl®, Marplan®, Nardil®, or Parnate® within the past 14 days ...
Do not take fexofenadine with fruit juice (such as apple, orange, or grapefruit). These juices can make it harder for your body to absorb fexofenadine. Avoid taking an antacid within 2 hours before or after you take fexofenadine. Certain antacids can make it harder for your body to absorb this medicine.. ...
We now read that Allegra is the latest antihistamine to go from prescription to over the counter (OTC). It will soon join its second-generation non-sedating cousins Claritin and Zyrtec, both excellent antihistamines, on the pharmacy shelves. When it does, only two popular antihistamines, Zyxal and Clarinex, will require a doctors prescription.. The story of Allegra, also known as fexofenidine is very interesting. Almost fifteen years ago there was what seemed to be the ideal antihistamine - Seldane (terfenadine). My patients loved it because, among other things, it worked well without the occasional side effect of fatigue. A few patients claimed they had problems of cardiac irregularities and were asked to discontinue the Seldane.. Then the bottom dropped out of the market because of unexpected deaths do to an adverse cardiac event resulting from disruption of the P450 system-basically, irregular heartbeat. Further study showed that the problem stemmed from use of Seldane simultaneously ...
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What happens if allegra d is mixed with alcohol - Allegra-d nauseates me and makes me jittery, is there anything else that works as well? Yes- what symptom? Allegra d is a combo of fexofenadine and pseudoephedrine. The 12 hour preparation has 120 mg of sudafed in it, a lot of decongestant, if you are sensitive. This causes the jitters, and may cause the nausea. If your main symptom is congestion, the answer could be no. If itching, sneezing, etc, try plain fexofenadine. Nasal prescription sprays also work and have less side effects because local only.
Upset stomach or nausea. Whats the best way to store Allegra?. Youll want to keep this drug out of the reach of young children. Allegra is best stored at room temperature or about 20 and 25 degrees C (68 and 77degrees F). Keep in a dry place and dispose of any remaining medication about the expiration date.. Summary. Youll have a lot of different allergy medications to choose from out there that will offer you relief. Allegra is one of the more well known options thats proven. If you decide to take it for allergy relief, theres a good chance it will either reduce your symptoms to the point of being more than tolerable or possible eliminate some of the symptoms altogether for certain periods of time.. ...
Consumer information provided by the United States National Library of Medicine. Includes side effects, dosage and precautions. ...
Single-Center, Double-Blind, Randomized , Parallel Study Comparing Onset of Action, Efficacy & Safety of a Single-Dose of Fexofenadine HCl 180 mg vs Montelukast Na 10 mg & Placebo in Treating Seasonal Allergic Rhinitis Subjects in an Allergen Exposure ...
I think the Leviathan list could see some pruning of the Carnifex variants (Down to 2 CC and Shooting variants) with the Exocrine Fex and Devourer Fex potentially being swapped for the Tyrannofex (2 Variants, Exocrine and Malefactor). Although speculation the Tyrannofex does seem to fit the bill on Long Range High Strength shooting and Short Range lots of shots for 2 of its rumoured weapons and it looks like getting stronger armour than the standard fex ...
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... terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority. However, terfenadine had to be removed ... Thompson D, Oster G (May 1996). "Use of terfenadine and contraindicated drugs". JAMA. American Medical Association. 275 (17): ... terfenadine > loratadine. However, the onset of action varies significantly and clinical efficacy is not always directly ...
Terfenadine "Fexofenadine - international brand names". Drugs.com. Retrieved 18 January 2017. "Fexofenadine Use During ... The older antihistaminic agent terfenadine was found to metabolize into the related carboxylic acid, fexofenadine. Fexofenadine ... so terfenadine was replaced in the market by its metabolite. Fexofenadine was originally synthesized in 1993 by Massachusetts- ...
Wood SF (January 1986). "Astemizole and terfenadine compared in hay fever". The Practitioner. 230 (1411): 41-4. doi:10.1161/ ...
... terfenadine , loratadine. However, the onset of action varies significantly and clinical efficacy is not always directly ... terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority.[21] ...
Terfenadine produces azacyclonol as a major active metabolite. It is made by the organometallic addition of 4-bromopyridine to ... Martens J (April 1996). "Determination of the terfenadine metabolite azacyclonol in human serum using gas chromatography-mass ... is also known as diphenylmethanolpiperidine and is the parent structure of the antihistamines fexofenadine and terfenadine. ...
... is a class of prescription drugs in India appearing as an appendix to the Drugs and Cosmetics Rules, 1945 introduced in 1945. These are drugs which cannot be purchased over the counter without the prescription of a qualified doctor.The manufacture and sale of all drugs are covered under the Drugs and Cosmetics Act and Rules. It is revised at times based on the advice of the Drugs Technical Advisory Board, part of the Central Drugs Standard Control Organization[1] in the Ministry of Health and Family Welfare. The most recent schedule H (2006) lists 536 drugs from abacavir to zuclopenthixol.[2] However, enforcement of Schedule H laws in India is lax, compared to the more restrictive Schedule X, for which a mandatory documentation trail must be maintained.[3] ...
Kintz, P; Mangin, P (December 1992). "Toxicological Findings in a Death Involving Dextromethorphan and Terfenadine:". The ...
Pinney, SP; Koller, BS; Franz, MR; Woosley, Raymond L.; Ph (1995). "Terfenadine increases the QT interval in isolated guinea ...
Benzyl salicylate and terfenadine have been shown to bind to CD81. Cluster of differentiation GRCh38: Ensembl release 89: ... "Identification of terfenadine as an inhibitor of human CD81-receptor HCV-E2 interaction: synthesis and structure optimization ...
Small P, Barrett D, Biskin N (February 1990). "Effects of azatadine, terfenadine, and astemizole on allergen-induced nasal ...
... are taking terfenadine, if 400 mg per day multidose of fluconazole is administered; concomitant administration of fluconazole ...
Fexofenadine is associated with a lower risk of cardiac arrhythmia compared to terfenadine. However, there is little evidence ... Terfenadine (Seldane (US), Triludan (UK), and Teldane (Australia)) Quifenadine (Phencarol, Фенкарол) Topical: Azelastine ...
Yasuda SU, Yasuda RP (1999). "Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic ... "Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ...
Yasuda SU, Yasuda RP (1999). "Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic ...
Cyclosporine, dalfopristin, erythromycin, itraconazole, ketoconazole, quinupristin, terfenadine, troleandomycin Increased risk ...
"Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole". FEBS ...
In some cases, this can lead to a fatal interaction with drugs like astemizole or terfenadine. The effect of grapefruit juice ... Often this allows prodrugs to be activated and absorbed - as in the case of the histamine H1-receptor antagonist terfenadine. ... of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine". British ...
"Blockade of multiple human cardiac potassium currents by the antihistamine terfenadine: possible mechanism for terfenadine- ...
... of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine". British ...
A series of drugs derived from Terfenadine have been shown to inhibit CYP2J2 and to suppress the proliferation and cause the ... "Selective inhibitors of CYP2J2 related to terfenadine exhibit strong activity against human cancers in vitro and in vivo". ...
terfenadine (en) , thioridazine (en) eta DL-tranylcypromine (en) Elkarrekintza. Opioid receptor mu 1 (en) ...
... and terfenadine; neither did it affect metabolism of the CYP1A2 substrate clozapine. Sertraline had no effect on the actions of ...
Other examples include terfenadine (Seldane, Seldane-D), astemizole (Hismanal), cisapride (Propulsid, withdrawn in many ...
Terfenadine, the first non-sedating antihistamine, had to be withdrawn from the market because of the small risk of a serious ... However, terfenadine was discovered to be the prodrug of the active molecule, fexofenadine, which does not carry the same risks ... However, in this case the parent compound does not have the side effects associated with terfenadine, and so both loratadine ...
Kawai, SH; Hambalek, RJ; Just, G (1994). „A facile synthesis of an oxidation product of terfenadine". J. Org. Chem. 59 (9): ... Rampe, D; Wible, B; Brown, AM; Dage, RC (1993). „Effects of terfenadine and its metabolites on a delayed rectifier K+ channel ...
The United States government removed two second generation antihistamines, terfenadine and astemizole, from the market based on ...
... terfenadine (Seldane)), may have arrhythmogenic effects. Dr. Woosley's invention, fexofenadine (Allegra), resulted from this ...
... the antihistamines astemizole and terfenadine, and some antipsychotics may increase the chance of ventricular dysrhythmias. ...
Kawai, SH; Hambalek, RJ; Just, G (May 1994). "A facile synthesis of an oxidation product of terfenadine". J. Org. Chem. 59 (9 ... Rampe, D; Wible, B; Brown, AM; Dage, RC (December 1993). "Effects of terfenadine and its metabolites on a delayed rectifier K+ ...
Terfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. Terfenadine, in addition ... Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H1 receptor. It is a prodrug, ... Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. It was brought to market by Hoechst ... Status of Terfenadine-Containing Drugs in Canada Archived 2006-07-13 at the Wayback Machine. from Health Canada ...
... terfenadine. View detailed information regarding this drug interaction. ... Terfenadine is no longer on the market in the US. Do not take terfenadine with any other food or medication. ... terfenadine coccidioidin skin test. Applies to: pseudoephedrine / terfenadine and coccidioidin skin test ... Terfenadine may interfere with your response to coccidioidin skin test. If you are currently using or have recently used ...
T 0728/98 (Pure terfenadine/ALBANY) of 12.5.2000. European Case Law Identifier:. ECLI:EP:BA:2000:T072898.20000512. ... 2. Where the claimed purity level of a low molecular chemical compound (here a terfenadine derivative) turns out to be ...
Terfenadine indications and usages ATC and ICD codes, combinations with other active ingredients and trade names information ... Terfenadine. Betamethasone Cortistamin NF - Bago Laboratorios Terfenadine. Dexamethasone Cortaler Novo - Phoenix Laboratorios. ... Terfenadine. Dextromethorphan Hydrobromide Tusant - Lupin Pharmaceuticals Terfenadine. Pseudoephedrine Teldane D - Sanofi- ... "Terfenadine". Indications and usages ATC and ICD codes:. ATC codes: R06AX12. ICD-10 codes: N / A. Alphabetical lists of ...
Terfenadine is a selective second generation H1 reactor antagonist which is a non-sedating antihistamine. Terfenadine has been ... Terfenadine is a selective second generation H1 reactor antagonist which is a non-sedating antihistamine. Terfenadine has been ... A new analytical method for terfenadine.. Author(s): YK Agrawal, SJ Rajput, GR Kathkar. Chemistry Dept., School of Sciences, ... a new simple and senstive spectrophotometric method is reported for the determination terfenadine. ...
Torsades de pointes occurring in association with terfenadine use [letter]. JAMA 1991; 266: 2375-6PubMedCrossRefGoogle Scholar ... Torsades de pointes occurring in association with terfenadine use. JAMA 1990; 264: 2788-90PubMedCrossRefGoogle Scholar ... Cardiotoxic effect with convulsions in terfenadine overdose [letter]. BMJ 1989; 298: 325PubMedCrossRefGoogle Scholar ... Torsades de pointes complicating treatment with terfenadine [letter]. BMJ 1991; 302: 1469PubMedCrossRefGoogle Scholar ...
Medical information for Terfenadine on Pediatric Oncall including Mechanism, Indication, Contraindications, Dosing, Adverse ...
However, terfenadine has been associated with a number of side effects on cardiac electrical activi ... Terfenadine is a second generation histamine receptor antagonist which is widely used as a non‑sedating antihistamine to ... Terfenadine is a second generation histamine receptor antagonist which is widely used as a non‑sedating antihistamine to ... The effect of terfenadine and amiodarone on the QTc interval was evaluated by comparison of multiple electrocardiograms. Barium ...
Torsades de pointes associated with terfenadine in a case of liver cirrhosis and hepatocellular carcinoma ... Does terfenadine-induced ventricular tachycardia/fibrillation directly relate to its QT prolongation and Torsades de Pointes?. ... Treatment with terfenadine and ketoconazole or itraconazole can cause torsades de pointes ventricular tachycardia. Duodecim; ... Itraconazole prevents terfenadine metabolism and increases risk of torsades de pointes ventricular tachycardia. European ...
Terfenadine on Lux 5 µm Cellulose-1 by Chiral SFC (loading and scale up). Column used: Lux® 5 µm Cellulose-1, LC Column 250 x ... Terfenadine on Lux 5 µm Cellulose-1 by Chiral SFC (loading and scale up). ...
In a voltage-clamp study in feline isolated ventricular myocytes, terfenadine but not its active metabolite terfenadine ... and terfenadine13 indicates that they predominantly block IKr, mimicking the effects of the class III agents. Terfenadine also ... 1.75 pA/pF after superfusion with 10 μmol/L terfenadine (n=5). Thus, at 10 μmol/L, terfenadine decreased IK1 by an average of ... more potently than terfenadine, whereas in vivo astemizole and terfenadine (1.0 to 3.0 mg/kg IV) produced nearly equivalent ...
Batey, Andrew.J. and Coker, Susan J. (2002) Proarrhythmic potential of halofantrine, terfenadine and clofilium in an in vivo ... Proarrhythmic potential of halofantrine, terfenadine and clofilium in an in vivo model of torsade de pointes ... During these infusions rabbits also received increasing i.v. doses of clofilium (20, 60 and 200nmolkg−1 min−1), terfenadine (75 ... Clofilium and halofantrine caused dose-dependent increases in the rate-corrected QT interval (QTc), whereas terfenadine ...
Acid-Base Cosolvent Method for Determining Aqueous Permeability of Amiodarone, Itraconazole, Tamoxifen, Terfenadine and Other ... Acid-Base Cosolvent Method for Determining Aqueous Permeability of Amiodarone, Itraconazole, Tamoxifen, Terfenadine and Other ...
23.5 DAYLERT have Terfenadine is comes under…. *RHITER 10 60MG The Brand Name RHITER Has Generic Salt :: Terfenadine RHITER Is ... 23.5 OLDIN have Terfenadine is comes under Sub…. *HITERF 10 60MG The Brand Name HITERF Has Generic Salt :: Terfenadine HITERF ... Details About Generic Salt :: Terfenadine Main Medicine Class:: Immunology , Allergy Sub Medicine Class :: Anti Allergics. 6B. ... 15.7 RHITER have Terfenadine is comes under Sub…. *Venlafaxine Details About Generic Salt :: Venlafaxine Main Medicine Class:: ...
Apo-Terfenadine M, Novo-Terfena-dine M, Seldane [Rx] Classification: Antihistamine, piperi-dine type ... Note: Terfenadine has been withdrawn from the market. Uses: Seasonal allergic rhinitis. Non-FDA Approved Uses: Histamine-in- ... Hepatic insufficiency and any drug or food (e.g., grapefruit juice) that blocks the metabolism of terfenadine may cause serious ... T Effect of terfena-dine due to l breakdown by the liver. ... Terfenadine. Last Updated on Tue, 11 Jun 2019 , Action Kinetics ...
Terfenadine. Six healthy volunteers received terfenadine 60 mg BID for 15 days. Fluconazole 200 mg was administered daily from ... Fluconazole did not affect terfenadine plasma concentrations. Terfenadine acid metabolite AUC increased 36% ± 36% (range: 7 to ... Terfenadine. Because of the occurrence of serious cardiac dysrhythmias secondary to prolongation of the QTc interval in ... The combined use of fluconazole at doses of 400 mg or greater with terfenadine is contraindicated. (See CONTRAINDICATIONS and ...
Terfenadine. Terfenadine is an antihistamine, prescribed for allergic reactions such as runny nose, sneezing, throat irritation ...
Terfenadine Terfenadine is an antihistamine, prescribed for allergic reactions such as runny nose, sneezing, throat irritation ...
For some patients, terfenadine, in the currently recommended dose of 60 mg twice daily (bid), may be only modestly effective in ... A double-blind evaluation of skin test suppression produced by two doses of terfenadine. / Bantz, Eric W.; Dolen, William K.; ... A double-blind evaluation of skin test suppression produced by two doses of terfenadine. The Journal of Allergy and Clinical ... Both doses of terfenadine suppressed cutaneous reactivity significantly more than had chlorpheniramine. It is concluded that ...
Seldane® Tablets (60 mg) (terfenadine) Taxotere® Injection concentrate (docetaxel) Teczem Tablets (Enalapril Maleate/Diltiazem ...
Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37°C with an IC 50 of 7 nM, 18 nM, 343 μM, ... Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37°C with an IC 50 of 7 nM, 18 nM, 343 μM, ... Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37°C with an IC 50 of 7 nM, 18 nM, 343 μM, ... Dofetilide, cisapride, sotalol, terfenadine, and verapamil blocked hERG channels at 37°C with an IC 50 of 7 nM, 18 nM, 343 μM, ...
... terfenadine , loratadine. However, the onset of action varies significantly and clinical efficacy is not always directly ... terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority.[21] ...
Terfenadine. 10 mg. LGCFOR0055.00. Add to basket Testosterone. 10 mg. LGCFOR0323.00. Add to basket ...
Terfenadine. *No clinically significant changes occurred in heart rate or corrected QT intervals, or in terfenadine metabolite ... or lomefloxacin pharmacokinetics, during concurrent administration of lomefloxacin and terfenadine at steady-state in 28 ...
Terfenadine. 10 mg. LGCFOR0055.00. In den Warenkorb Testosterone. 10 mg. LGCFOR0323.00. In den Warenkorb ...
... terfenadine; thiamphenicol; thiouracils; trimethadione; troparanol; valproic acid; and mixtures thereof. ...
TERFENADINE. Subpart B of part 1 of the Appendix is amended by inserting in numerical sequence the following new item: 907.25 ... Terfenadine. Sec. 145. Sulfathizole. Sec. 146. Sulfaquinoxaline and sulfanilamide. Sec. 147. Dicyclomine hydrochloride and ... Terfenadine (provided for in item 411.58, part IC, schedule 4) Free No change On or before 12/31/87 SEC. 145. SULFATHIAZOLE. (a ...
Terfenadine overdose induced polymorphous ventricular tachycardia. Terfenadine overdose induced polymorphous ventricular ... Terfenadine / Tachycardia, Ventricular / Drug Overdose / Heart Septal Defects, Ventricular / Histamine H1 Antagonists Type of ... Terfenadine / Tachycardia, Ventricular / Drug Overdose / Heart Septal Defects, Ventricular / Histamine H1 Antagonists Type of ...
  • 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 drugs be removed from the market and physicians consider alternative medications for their patients. (wikipedia.org)
  • [4] Seldane (and Seldane-D, terfenadine combined with the decongestant pseudoephedrine ) were removed from the U.S. market by their manufacturer in late 1997 after the FDA approval of Allegra-D (fexofenadine/pseudoephedrine). (wikipedia.org)
  • By the time Schering submitted the drug to the U.S. Food and Drug Administration (FDA) for approval, the agency had already approved a competitor's nonsedating antihistamine, terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority. (wikipedia.org)
  • Terfenadine (Seldane) and astemizole (Hismanal), a second generation of H 1 receptor antagonists, are two widely used nonsedating antihistamines that differ pharmacologically from first-generation antihistamines by having preferential affinity for the peripheral H 1 receptors versus the brain H 1 and cholinergic receptors. (ahajournals.org)
  • Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. (wikipedia.org)
  • Terfenadine acts as a peripherally-selective antihistamine , or antagonist of the histamine H 1 receptor . (wikipedia.org)
  • Terfenadine, in addition to its antihistamine effects, also acts as a potassium channel blocker (K v 11.1 encoded by the gene hERG ). (wikipedia.org)
  • Terfenadine is a selective second generation H1 reactor antagonist which is a non-sedating antihistamine. (ijpsonline.com)
  • Terfenadine is a second generation histamine receptor antagonist which is widely used as a non‑sedating antihistamine to relieve allergic responses. (biomedsearch.com)
  • This study was designed to compare the proarrhythmic activity of the antimalarial drug, halofantrine and the antihistamine, terfenadine, with that of clofilium a K+ channel blocking drug that can induce torsade de pointes. (strath.ac.uk)
  • Second-generation H 1 blockers (eg, terfenadine, cetirazine, loratadine , astemazole) are less likely to cross the blood-brain barrier, or they have a low affinity for brain compared with peripheral H 1 receptors. (merckvetmanual.com)
  • Based on evidence from previous studies, it was hypothesized that the antiarrhythmic effect of terfenadine may be similar to that of amiodarone. (biomedsearch.com)
  • The present study aimed to examine the effect of terfenadine on the QTc interval and on experimental ventricular arrhythmia in rats by comparing with that of amiodarone. (biomedsearch.com)
  • The effect of terfenadine and amiodarone on the QTc interval was evaluated by comparison of multiple electrocardiograms. (biomedsearch.com)
  • The potential protective effect of terfenadine in ventricular arrhythmia may be similar to that of amiodarone. (biomedsearch.com)
  • These results show that, like clofilium, halofantrine can cause torsade de pointes in a modified anaesthetized rabbit model whereas the primary adverse effect of terfenadine was cardiac contractile failure. (strath.ac.uk)
  • Effect of terfenadine on human eosinophil and neutrophil chemotactic response and generation of Superoxide. (springer.com)
  • In vitro analysis were also made of samples from ten mild asthmatics to determine the effect of terfenadine on basophil histamine release. (elsevier.com)
  • Abstract We compared the cardiac electrophysiological actions of two types of H 1 -receptor antagonists-the piperidines, astemizole and terfenadine, and the nonpiperidines, chlorpheniramine and pyrilamine-in vitro in guinea pig ventricular myocytes and in vivo in chloralose-anesthetized dogs. (ahajournals.org)
  • Astemizole and terfenadine significantly increased action potential duration of guinea pig myocytes. (ahajournals.org)
  • Astemizole and terfenadine potently blocked the rapidly activating component of the delayed rectifier, I Kr , with IC 50 values of 1.5 and 50 nmol/L, respectively. (ahajournals.org)
  • Chlorpheniramine and pyrilamine blocked I Kr relatively weakly (IC 50 =1.6 and 1.1 μmol/L, respectively) and I Ks and I K1 less than 20% at 10 μmol/L. Astemizole and terfenadine (1.0 to 3.0 mg/kg IV) significantly prolonged the QTc interval and ventricular effective refractory period in vivo. (ahajournals.org)
  • Block of repolarizing K + currents, particularly I Kr , by astemizole and terfenadine produces reverse rate-dependent prolongation of action potential duration and development of early afterdepolarizations, delays ventricular repolarization, and may underlie the development of torsade de pointes ventricular arrhythmias observed with the use and abuse of these agents. (ahajournals.org)
  • 13 14 15 16 Therefore, we designed this study to assess the effects of the piperidine-containing H 1 -receptor antagonists astemizole and terfenadine on APD and various ionic currents in guinea pig isolated ventricular myocytes. (ahajournals.org)
  • Both astemizole and terfenadine suppressed the I K1 channel by 17% to 50% in a voltage-dependent manner in rat and guinea pig myocytes. (ahajournals.org)
  • Torsades de pointes complicating treatment with terfenadine [letter]. (springer.com)
  • Torsades de pointes after treatment with terfenadine and ketoconazole. (springer.com)
  • A 65-year-old woman with liver cirrhosis complicated by hepatocellular carcinoma lost consciousness due to torsades de pointes with prolongation of the QT-interval after 10 days of treatment with terfenadine. (eurekamag.com)
  • Terfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. (wikipedia.org)
  • Cardiotoxic effect with convulsions in terfenadine overdose [letter]. (springer.com)
  • Mechanism of the cardiotoxic actions of terfenadine. (springer.com)
  • The effect of fluconazole on the steady-state pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine in humans. (springer.com)
  • Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine with concomitant administration of erythromycin. (springer.com)
  • Effect of erythromycin, clarithromycin and azithromycin on the pharmacokinetics of terfenadine [abstract]. (springer.com)
  • Effect of cimetidine and ranitidine on the pharmacokinetics and ECG pharmacodynamics of terfenadine [abstract]. (springer.com)
  • Finally, the in vitro study showed significant inhibition by terfenadine of anti-IgE-induced histamine release from human basophils. (elsevier.com)
  • Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is not measurable in the plasma. (wikipedia.org)
  • Itraconazole prevents terfenadine metabolism and increases risk of torsades de pointes ventricular tachycardia. (springer.com)
  • Since she had liver cirrhosis, the development of torsades de pointes was thought to be attributable to the impairment of hepatic metabolism by terfenadine. (eurekamag.com)
  • Hepatic insufficiency and any drug or food (e.g., grapefruit juice) that blocks the metabolism of terfenadine may cause serious CV effects (see Side Effects that follow). (mussenhealth.us)
  • During these infusions rabbits also received increasing i.v. doses of clofilium (20, 60 and 200nmolkg−1 min−1), terfenadine (75, 250 and 750nmolkg−1min−1), halofantrine (6, 20 and 60μmolkg−1) or vehicle. (strath.ac.uk)
  • 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). (elsevier.com)
  • Both doses of terfenadine suppressed cutaneous reactivity significantly more than had chlorpheniramine. (elsevier.com)
  • It is concluded that the presently recommended dose of terfenadine produces submaximal skin test suppression and that further studies are needed to investigate the clinical efficacy and safety of larger doses of terfenadine in the treatment of allergic rhinitis. (elsevier.com)
  • Bantz, EW , Dolen, WK & Nelson, HS 1987, ' A double-blind evaluation of skin test suppression produced by two doses of terfenadine ', The Journal of Allergy and Clinical Immunology , vol. 80, no. 1, pp. 99-103. (elsevier.com)
  • High doses of terfenadine and astemizole lead to prolonged QT intervals and arrhythmias (eg, ventricular tachycardia, cardiac arrest). (merckvetmanual.com)
  • Several cases of torsade de pointes recently have been reported in patients administered the nonsedating histamine H 1 -receptor antagonists astemizole 6 7 8 9 10 and terfenadine, 11 prompting warnings for potentially serious adverse cardiovascular events with these agents. (ahajournals.org)
  • To determine the cellular electrophysiological basis for the proarrhythmic effects of these drugs, this study was designed to investigate the actions of two H 1 receptor antagonists, terfenadine and astemizole, on various potassium (K + ) channels of cardiac myocytes. (ahajournals.org)
  • Comparative study of the protective effects of terfenadine and amiodarone on barium chloride/aconitine-induced ventricular arrhythmias in rats: A potential role of terfenadine. (biomedsearch.com)
  • In comparison with normal saline, terfenadine and amiodarone similarly dose‑dependently prolonged the QTc interval in rats. (biomedsearch.com)
  • The present study suggested that terfenadine prolonged the QTc interval and decreased ventricular tachycardia duration. (biomedsearch.com)
  • Terfenadine overdose induced polymorphous ventricular tachycardia. (bvsalud.org)
  • Pharmacokinetic interaction between terfenadine and ketoconazole [abstract]. (springer.com)
  • 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. (elsevier.com)
  • Crane JK, Shih H-T. Syncope and cardiac arrhythmia due to an interaction between itraconazole and terfenadine. (springer.com)
  • However, terfenadine has been associated with a number of side effects on cardiac electrical activities through blocking multiple ion channels in the heart, particularly K+ channels. (biomedsearch.com)
  • Previous studies have demonstrated block of several components of the cardiac delayed rectifier and other potassium currents by terfenadine. (ahajournals.org)
  • Clofilium and halofantrine caused dose-dependent increases in the rate-corrected QT interval (QTc), whereas terfenadine prolonged PR and QRS intervals rather than prolonging cardiac repolarization. (strath.ac.uk)
  • Cardiac arrhythmias were initially reported in patients who intentionally or accidentally ingested overdoses of either astemizole 4 5 6 7 8 9 10 11 or terfenadine. (ahajournals.org)
  • [5] Terfenadine-containing drugs were subsequently removed from the Canadian market in 1999, [6] and are no longer available for prescription in the UK. (wikipedia.org)
  • Background Terfenadine and astemizole are widely prescribed nonsedating antihistamines that have been associated with QT-interval prolongation and ventricular arrhythmias. (ahajournals.org)
  • Torsades de pointes occurring in association with terfenadine use. (springer.com)
  • After the withdrawal of terfenadine, the QT-interval was normalized and the torsades de pointes disappeared. (eurekamag.com)
  • To assess the effectiveness of terfenadine on bronchoconstriction in asthmatics, 12 asthmatic patients between the ages of 19 and 43 were challenged with ultrasonically nebulized distilled water (UNDW) and treated with terfenadine, 120 or 240 mg, or placebo in a three-way crossover double-blind study. (elsevier.com)
  • Terfenadine-ketoconazole interaction: pharmacokinetic and electrocardiographic consequences. (springer.com)
  • Terfenadine significantly inhibited I NaL and moderately I CaL, verapamil blocked only I CaL. (elsevier.com)
  • Terfenadine, 240 mg, showed significant (P = .012) benefit over placebo in improving pulmonary function after UNDW challenge. (elsevier.com)
  • After administration of the highest dose of each drug halofantrine caused a modest decrease in blood pressure, but terfenadine had profound hypotensive effects resulting in death of most rabbits. (strath.ac.uk)
  • Terfenadine but not astemizole slightly inhibited I K , by 9%, and only at higher drug concentrations. (ahajournals.org)