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Clinical Reviews in Allergy 1993
Comparative Study Review
Topics: Adult; Asthma; Child; Drug Interactions; Electroencephalography; Humans; Rhinitis; Skin Tests; Terfenadine; Urticaria
PubMed: 8319161
DOI: 10.1007/BF02802292 -
Annals of Neurology Feb 1993
Topics: Adolescent; Adult; Female; Humans; Hypersensitivity; Male; Rhinitis; Terfenadine; Tremor
PubMed: 8434887
DOI: 10.1002/ana.410330216 -
Acta Pharmaceutica (Zagreb, Croatia) Jun 2021Terfenadine is a second-generation H1-antihistamine that despite potentially can produce severe side effects it has recently gained attention due to its anticancer...
Terfenadine is a second-generation H1-antihistamine that despite potentially can produce severe side effects it has recently gained attention due to its anticancer properties. Lately, the subfamily 2 of inward rectifier potassium channels (Kir2) has been implicated in the progression of some tumoral processes. Hence, we characterized the effects of terfenadine on Kir2.x channels expressed in HEK-293 cells. Terfenadine inhibited Kir2.3 channels with a strikingly greater potency (IC50 = 1.06 ± 0.11 μmol L-1) compared to Kir2.1 channels (IC50 = 27.8 ± 4.8 μmol L-1). The Kir2.3(I213L) mutant, possessing a larger affinity for phosphatidylinositol 4,5-bisphosphate (PIP2) than the wild-type Kir2.3, was less sensitive to terfenadine inhibition (IC50 = 13.0 ± 2.9 μmol L-1). Additionally, the PIP2 intracellular application had largely reduced the inhibition of Kir2.1 channels by terfenadine. Our data support that Kir2.x channels are targets of terfena-dine by affecting their interaction with PIP2, which could be regarded as a mechanism of the antitumor properties of terfenadine.
Topics: HEK293 Cells; Histamine H1 Antagonists, Non-Sedating; Humans; Inhibitory Concentration 50; Potassium Channels, Inwardly Rectifying; Terfenadine
PubMed: 33151169
DOI: 10.2478/acph-2021-0017 -
Clinical Pharmacokinetics Jul 1994
Review
Topics: Cytochrome P-450 Enzyme System; Drug Interactions; Fluconazole; Heart; Humans; Itraconazole; Ketoconazole; Prodrugs; Terfenadine
PubMed: 7955768
DOI: 10.2165/00003088-199427010-00001 -
Drug Safety Apr 1993Sedation and impairment of psychomotor performance are well known adverse effects of the traditional antihistamines. These effects appear to be caused by different... (Review)
Review
Sedation and impairment of psychomotor performance are well known adverse effects of the traditional antihistamines. These effects appear to be caused by different mechanisms, but both may have potentially dangerous consequences. while several of the newer antihistamines, such as terfenadine, have overcome the problem of sedation, it is also important to establish their propensity to cause psychomotor impairment. Many single- and multiple-dose studies (mostly in healthy volunteers) have compared the effects of terfenadine on psychomotor performance with those of placebo, as well as traditional and other nonsedating antihistamines. Over half of the studies employed divided-attention tasks that are considered relevant to everyday activities, such as driving. Like several other nonsedating antihistamines, single doses of terfenadine of up to 120 mg did not impair driving performance and generally had no significant effects on other psychomotor tests compared with placebo. In most of the multiple-dose studies, terfenadine 60 mg twice daily was administered for up to 5 days. Again, the effects of terfenadine on psychomotor performance differed little from those of placebo. Thus, the available evidence suggests that the problem of impaired psychomotor performance associated with the older, traditional antihistamines does not apply to terfenadine.
Topics: Clinical Trials as Topic; Drug Administration Schedule; Humans; Psychomotor Performance; Terfenadine
PubMed: 8481218
DOI: 10.2165/00002018-199308040-00006 -
Journal of Investigational Allergology... Dec 1991This double-blind, double-dummy, parallel-group study was undertaken in 40 patients with seasonal allergic rhinoconjunctivitis during the 1990 hay fever season. The... (Clinical Trial)
Clinical Trial Randomized Controlled Trial Review
This double-blind, double-dummy, parallel-group study was undertaken in 40 patients with seasonal allergic rhinoconjunctivitis during the 1990 hay fever season. The patients were randomized and treated for seven days with either 120 mg terfenadine or 10 mg loratadine, each drug taken once daily in the morning. The severity of nasal congestion, rhinorrhea, sneezing, nasopharyngeal itching, and itchy, watery, red eyes was evaluated before and at the end of treatment. The global severity of symptoms was ranked daily by the patient on a diary card. Both treatment groups experienced a significant improvement of symptoms after treatment (p < 0.01), without any significant difference between the two study drugs. Terfenadine and loratadine significantly improved symptom severity by 69 and 55% compared with the baseline values, respectively. Headache and fatigue were reported in three loratadine-treated patients, and sedation in one patient. No side effects were observed in patients receiving terfenadine. This study confirmed that terfenadine 120 mg once daily is a safe and effective treatment for hay fever.
Topics: Adolescent; Adult; Double-Blind Method; Female; Humans; Loratadine; Male; Middle Aged; Rhinitis, Allergic, Seasonal; Safety; Terfenadine
PubMed: 1669595
DOI: No ID Found -
Drugs in R&D 2007Fexofenadine, an active metabolite of the second-generation histamine H1 receptor antagonist (antihistamine) terfenadine, does not have the disadvantage of QT... (Comparative Study)
Comparative Study Review
Fexofenadine, an active metabolite of the second-generation histamine H1 receptor antagonist (antihistamine) terfenadine, does not have the disadvantage of QT prolongation. In addition, unlike first-generation antihistamines, it is associated with few CNS adverse effects. Chemically, fexofenadine has a zwitterionic structure that makes it an interesting molecule for use as an oral drug. Fexo-fenadine has negligible hepatic metabolism in humans, and is recovered mainly in the faeces in an unchanged form after oral administration. The absolute oral bioavailability of fexofenadine in humans is not known because of a lack of studies of intravenous administration of this agent. Its apparent elimination half-life (t1/2) ranges from 3 to 17 hours and is highly dependent on study design, i.e. the length of blood sampling. This large discrepancy might be associated with a 'flip-flop' phenomenon caused by slow absorption of the zwitterionic molecule. This review summarises the available literature related to the absorption, elimination and excretion of fexofenadine and terfenadine. Based on these data, the volume of distribution, t1/2 and oral bioavailability of fexofenadine in humans are estimated. Understanding these pharmacokinetic aspects of this drug might be very useful for medicinal chemists utilising fexofenadine/terfenadine as an example for designing zwitterionic compounds to combat cardiotoxicity and other issues related to basic and lipophilic molecules.
Topics: Animals; Anti-Allergic Agents; Biological Availability; Biotransformation; Blood Proteins; Half-Life; Histamine H1 Antagonists, Non-Sedating; Humans; Terfenadine
PubMed: 17767395
DOI: 10.2165/00126839-200708050-00004 -
The Western Journal of Medicine Dec 1994
Topics: Astemizole; Drug Information Services; Drug Interactions; Humans; Terfenadine; United States; United States Food and Drug Administration
PubMed: 7856171
DOI: No ID Found -
The Annals of Pharmacotherapy Nov 1993
Topics: Adult; Drug Interactions; Electrocardiography, Ambulatory; Fluoxetine; Humans; Male; Tachycardia, Sinus; Terfenadine
PubMed: 8286821
DOI: 10.1177/106002809302701119 -
Journal of Pharmacokinetics and... Apr 2021
Topics: Dose-Response Relationship, Drug; Drug Approval; Drug Recalls; Electrocardiography; Humans; Long QT Syndrome; Models, Biological; Software; Terfenadine
PubMed: 33826074
DOI: 10.1007/s10928-021-09754-z