certain antihistamines such as astemizole (Hismanal)(no longer available in the U.S.) and terfenadine (Seldane)(no longer available in the U.S. (medlineplus.gov)
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)
Case reports of this complication are particularly common for astemizole and terfenadine. (wikitox.org)
Hismanal2
Astemizole (marketed under the brand name Hismanal, developmental code R43512) was a second-generation antihistamine drug that has a long duration of action. (wikipedia.org)
Astemizole ( hismanal ) was a popular, non sedating, once a day antihistamine for allergy symptoms like runny, itchy nose, itchy eyes , sneezing etc. (healthtap.com)
Histamine H1-receptor antagon1
Astemizole is a histamine H1-receptor antagonist. (wikipedia.org)
Antihistamine1
However, astemizole is an antihistamine that has potential for use as an anti-prion drug. (infectioncontroltoday.com)
Tacrolimus2
The two compounds are already marketed as the drugs tacrolimus and astemizole. (infectioncontroltoday.com)
The first author of the study, Unique Drug Screening Approach for Prion Diseases Identifies Tacrolimus and Astemizole as Antiprion Agents, is Yervand Eduard Karapetyan of The Scripps Research Institute. (infectioncontroltoday.com)
Antagonist1
In contrast, astemizole acts as a histamine H1 receptor (H1R1) antagonist to activate T cells in a non-specific, DC-independent fashion. (bmj.com)
Blood-brain b3
Despite some earlier reports that astemizole does not cross the blood-brain barrier, several studies have shown high permeability and high binding to protein folds associated with Alzheimer's. (wikipedia.org)
Astemizole does not cross the blood-brain barrier , and H1 receptor binding is mostly in the peripheral rather than central nervous system (CNS depression is thus minimal). (wikidoc.org)
Astemizole not only crosses the blood-brain barrier, but works effectively at a relatively low concentration. (infectioncontroltoday.com)
Drugs3
With allergy drugs such as astemizole, how about claritin (loratadine)? (healthtap.com)
With allergy drugs such as astemizole can I take claritin (loratadine)? (healthtap.com)
Results The screening of three drug libraries relevant to known signaling pathways, FDA (Food and Drug Administration)-approved drugs and neuroendocrine factors yielded two major hits, astemizole and ikarugamycin. (bmj.com)
Oral2
Astemizole has an oral LD50 of approximately 2052 mg/kg (in mice). (wikipedia.org)
Astemizole has an oral LD 50 of approximately 2052mg/kg (in mice). (wikidoc.org)
Immune2
Of note, astemizole enhanced the CD8 + /Foxp3 + ratio in the tumor immune infiltrate as well as IFN-γ production by local CD8 + T lymphocytes. (bmj.com)
The combination of astemizole and oxaliplatin was able to cure the majority of mice bearing orthotopic non-small cell lung cancers (NSCLC), then inducing a state of protective long-term immune memory. (bmj.com)
Market1
Astemizole is off the market as it caused arrythmias (irregular heart beats). (healthtap.com)
Effects2
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects. (wikipedia.org)
Perinatal astemizole exposure in the rat throughout gestation: long-term behavioral and anatomic effects associated with reproduction. (bvsalud.org)
Drug1
8. Migliani R, Clouzeau J, Decousser JW, and astemizole before they were with- Ravelomanana N, Rasamoelisoa J, goal in drug therapy decision-making. (cdc.gov)
Action1
So future studies on the mode of action of astemizole may uncover potentially new therapeutic targets for prion diseases and similar disorders. (infectioncontroltoday.com)
Studies1
[2] Recent studies have also suggested anti-malarial properties of astemizole. (wikidoc.org)
Inhibitors1
When astemizole was co-administered with CYP3A4 inhibitors, the plasma of astermizole concentration was higher and may be more likely to cause ADRs. (medscape.com)
Antihistamine drug1
We recently identified astemizole (AST), an antihistamine drug, as a cholesterol trafficking inhibitor from a phenotypic screen. (johnshopkins.edu)
4. The effects of astemizole on histamine-induced weal and flare. (nih.gov)
Cardiotoxicity1
Astemizole: Increased risk of cardiotoxicity and arrhythmias. (pediatriconcall.com)
Prolongation1
showed in the animal models that astemizole at 0.3 mg/kg caused slight prolongation of the QT interval but did not induce any arrhythmias. (medscape.com)
Vitro1
In vitro experiments indicated that both astemizole and demethylated astemizole were strong potassium channel blockers that reduced the conductivity of the delayed rectifier potassium channel (Ikr channel, encoded by hERG ), thereby triggering LQTS. (medscape.com)
CYP3A41
[ 18 ] Orally taken astemizole was O -demethylated by CYP2J2 and CYP3A4 to form demethylated astemizole. (medscape.com)
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects. (wikipedia.org)
Treatment4
2. [Treatment of urticaria with the new H1 antihistaminic astemizole--with special reference to the time of onset of effect and maximum effect]. (nih.gov)
8. [Treatment of chronic urticaria with a new synthetic antihistamine: astemizole]. (nih.gov)
13. Prolonged benefit in the treatment of chronic idiopathic urticaria with astemizole. (nih.gov)
18. Treatment of chronic idiopathic urticaria with astemizole. (nih.gov)