AstemizoleSeldaneAntihistamineMetabolismFexofenadineConcentrationsTheophyllineCYP3A4CardiotoxicDrugsWithdrawnGrapefruitEliminationAsthmaPlasmaDrugEffectsResultsBloodMethodPatientsBenefitTorsades de poinActive metabolite of terfenadine1996DosesLiverAntagonistTroglitazoneSevereLineHeartTreatmentDoctor
Astemizole3
- Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. (drugbank.com)
- With allergy drugs such as astemizole or terfenadine, how about taking claritin (loratadine)? (healthtap.com)
- In a comparative study the new H 1 -receptor antagonists, astemizole, terfenadine and cetirizine were more effective than older drugs, with a lesser adverse effect profile. (soton.ac.uk)
Seldane4
- In the United States, terfenadine as Seldane was brought to market in 1985 as the first non-sedating antihistamine for the treatment of allergic rhinitis. (wikipedia.org)
- 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)
- 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)
- When drugs that cause LQTS, such as terfenadine (Seldane), enter the market, millions of people are put at serious risk. (ca.gov)
Antihistamine6
- Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. (wikipedia.org)
- 53 Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H1 receptor. (wikipedia.org)
- Terfenadine, in addition to its antihistamine effects, also acts as a potassium channel blocker (Kv11.1 encoded by the gene hERG). (wikipedia.org)
- A pharmacologist known as Richard Kinsolving noticed that terfenadine showed a structural resemblance to the antihistamine diphenhydramine, so terfenadine was tested as an antihistamine. (wikipedia.org)
- Terfenadine is an antihistamine for the treatment of allergy symptoms. (drugbank.com)
- Objective: Because of anecdotal reports and uncontrolled trials showing antihistamine efficacy in CFS, we evaluated the clinical efficacy of the antihistamine terfenadine (60 mg twice daily) in a placebo-controlled study. (umn.edu)
Metabolism4
- Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is not measurable in the plasma. (wikipedia.org)
- The metabolism of 1,2-Benzodiazepine can be decreased when combined with Terfenadine. (drugbank.com)
- The metabolism of Terfenadine can be increased when combined with Abatacept. (drugbank.com)
- Inhibition of terfenadine metabolism by CYP3A4: evidence for substrate inhibition reflects multiple binding sites. (manchester.ac.uk)
Fexofenadine3
- In the U.S., Terfenadine was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation. (drugbank.com)
- The active metabolite of terfenadine is fexofenadine. (drugbank.com)
- Fexofenadine is a pharmacologically active metabolite of terfenadine. (medicines.org.uk)
Concentrations2
- Plasma concentrations of the cardiotoxic agent terfenadine and the active antihistaminic metabolite terfenadine carboxylate were determined over 8 hours. (nih.gov)
- Co-administration may increase terfenadine concentrations and the risk of QT prolongation. (drugbank.com)
Theophylline1
- Theophylline, Terfenadine and Erythromycin: Zafirlukast plasma concentration is reduced. (pediatriconcall.com)
CYP3A43
- The addition of, or a dosage increase in, these CYP3A4 inhibitors makes it harder for the body to metabolize and remove terfenadine. (wikipedia.org)
- Grapefruit is a CYP3A4 inhibitor, and terfenadine is metabolized by CYP3A4. (drugbank.com)
- This herb induces CYP3A4 and terfenadine is a substrate of CYP3A4. (drugbank.com)
Cardiotoxic1
- Terfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. (wikipedia.org)
Drugs1
- Terfenadine-containing drugs were subsequently removed from the Canadian market in 1999, and are no longer available for prescription in the UK. (wikipedia.org)
Withdrawn1
- Lethal reactions can be the reasons that some medications are withdrawn from the market (such as troglitazone and terfenadine). (msdmanuals.com)
Grapefruit5
- To investigate the single dose-response effects of grapefruit juice on terfenadine disposition and electrocardiographic measurements. (nih.gov)
- Twelve healthy males received 250 ml water or regular- or double-strength grapefruit juice with 60 mg terfenadine in a randomized crossover trial. (nih.gov)
- No differences in the pharmacokinetics of terfenadine and terfenadine carboxylate were observed between the two strengths of grapefruit juice. (nih.gov)
- A normal amount of regular-strength grapefruit juice produced maximum single-dose effects on terfenadine and carboxylic acid metabolite pharmacokinetics. (nih.gov)
- This study further enhances the awareness of the potential for a serious interaction between grapefruit juice and terfenadine. (nih.gov)
Elimination1
- However, terfenadine carboxylate apparent elimination half-life (t1/2) was not altered. (nih.gov)
Asthma1
- In a controlled trial terfenadine did not confer any significant benefit in the treatment of chronic asthma. (soton.ac.uk)
Plasma5
- Terfenadine plasma peak drug concentration (Cmax) was also higher. (nih.gov)
- Terfenadine carboxylate area under the plasma drug concentration-time curve (AUC), Cmax, and time to reach Cmax (tmax) were increased by both strengths of juice. (nih.gov)
- This work describes the methodology for the analysis of terfenadine and the acid metabolite of terfenadine in plasma using high-performance liquid chromatography. (nih.gov)
- The use of solid-phase extraction allows the use of robotic or manual sample preparation for the efficient clean-up of terfenadine and terfenadine acid metabolite from plasma. (nih.gov)
- This explains the limited reduction of early bronchoconstriction by terfenadine, despite the plasma histamine rise being unchanged. (soton.ac.uk)
Drug1
- He is one of the authors of the article 'Toursade de Pointes Occurring in Association with Terfenadine Use' reporting this significant drug interaction. (xtalks.com)
Effects1
- Terfenadine was highly specific with no anti-methacholine, prostaglandin D 2 or leukotriene D 4 effects in asthmatic airways. (soton.ac.uk)
Results1
- Conclusion: Although this trial involved a small number of patients, the results suggest that terfenadine is unlikely to be of clinical benefit in treating CFS symptoms. (umn.edu)
Blood1
- Terfenadine competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. (drugbank.com)
Method1
- A new analytical method for terfenadine. (ijpsonline.com)
Patients1
- Methods: Thirty patients with CFS were enrolled in a 2-month, double-blind, placebo- controlled trial of terfenadine. (umn.edu)
Benefit1
- No therapeutic benefit from terfenadine could be detected in terms of symptom amelioration, improved physical or social functioning, health perceptions, or mental health. (umn.edu)
Torsades de poin1
- Terfenadine was removed from the market because of associated episodes of torsades de pointes, yet therapeutic dosages only extended the QT interval by 6 msec. (aafp.org)
Active metabolite of terfenadine2
19961
- Benton RE, Honig PK, Zamani K, Cantilena LR & Woosley RL (1996): Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. (nature.com)
Doses1
- Terfenadine itself, however, is cardiotoxic at higher doses, while its major active metabolite is not. (wikipedia.org)
Liver1
- Terfenadine and risk of acute liver disease. (nih.gov)
Antagonist1
- 53 Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H1 receptor. (wikipedia.org)
Troglitazone2
- Further experiments to study the effects of Terfenadine (10 μM), Tolcapone (88 μM), Trovafloxacin (150 μM with or without 1 μg/mL lipopolysaccharide), Troglitazone (28 μM), Rosiglitazone (0.8 μM), Pioglitazone (3 μM), and caffeine (600 μM) were carried out over 10 days. (nih.gov)
- Lethal reactions can be the reasons that some medications are withdrawn from the market (such as troglitazone and terfenadine). (msdmanuals.com)
Severe1
- Severe exacerbation of psoriasis due to terfenadine. (nih.gov)
Line1
- 50 μm in B. ( C ) Time course of onset of 2:1 or higher grade AV block in response to atrial pacing (bars) or terfenadine (line) expressed as a percentage of the embryos studied. (zfin.org)
Heart1
- C ) silent heart mutant embryos develop 2:1 block at 48 hpf in response to terfenadine treatment, as demonstrated in this plot of atrial and ventricular fluorescence intensity. (zfin.org)
Treatment2
- Terfenadine is an antihistamine formerly used for the treatment of allergic conditions. (wikipedia.org)
- B ) endothelin 1 morphant fish develop normal AV conduction block on treatment with terfenadine at 48 hpf. (zfin.org)
Doctor1
- Did Their Church Parents A Professional Or Levitra Prescription Without Maybe Doctor Influenced Them 20mg Their Generic mg op de eerste dag en vervolgens eenmaal daags 400 mg totdat u wordt gezegd dat u moet stoppen Ter behandeling. (ultimateunderground.com)