Peringatan Keamanan

Mild (e.g., headache, nausea, confusion), but adverse cardiac events including cardiac arrest, ventricular arrhythmias including torsades de pointes and QT prolongation have been reported. LD50=mg/kg (orally in mice)

Terfenadine

DB00342

small molecule approved withdrawn

Deskripsi

In the U.S., Terfenadine was superseded by fexofenadine in the 1990s due to the risk of cardiac arrhythmia caused by QT interval prolongation.

Struktur Molekul 2D

Berat 471.6734
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3.5 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

On the basis of a mass balance study using 14C labeled terfenadine the oral absorption of terfenadine was estimated to be at least 70%

Metabolisme

Hepatic

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Exercise caution with grapefruit products. Grapefruit is a CYP3A4 inhibitor, and terfenadine is metabolized by CYP3A4. Co-administration may increase terfenadine concentrations and the risk of QT prolongation.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A4 and terfenadine is a substrate of CYP3A4.

Interaksi Obat

1543 Data
Reserpine Reserpine may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Troglitazone Troglitazone may decrease the excretion rate of Terfenadine which could result in a higher serum level.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Terfenadine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Terfenadine.
Erythromycin The serum concentration of Terfenadine can be increased when it is combined with Erythromycin.
Azithromycin The serum concentration of Terfenadine can be increased when it is combined with Azithromycin.
Roxithromycin The serum concentration of Terfenadine can be increased when it is combined with Roxithromycin.
Sirolimus The serum concentration of Terfenadine can be increased when it is combined with Sirolimus.
Dirithromycin The serum concentration of Terfenadine can be increased when it is combined with Dirithromycin.
Telithromycin The serum concentration of Terfenadine can be increased when it is combined with Telithromycin.
Candicidin The serum concentration of Terfenadine can be increased when it is combined with Candicidin.
Clarithromycin The serum concentration of Terfenadine can be increased when it is combined with Clarithromycin.
Josamycin The serum concentration of Terfenadine can be increased when it is combined with Josamycin.
Everolimus The serum concentration of Terfenadine can be increased when it is combined with Everolimus.
Epothilone D The serum concentration of Terfenadine can be increased when it is combined with Epothilone D.
Patupilone The serum concentration of Terfenadine can be increased when it is combined with Patupilone.
6-Deoxyerythronolide B The serum concentration of Terfenadine can be increased when it is combined with 6-Deoxyerythronolide B.
Ixabepilone The serum concentration of Terfenadine can be increased when it is combined with Ixabepilone.
KOS-1584 The serum concentration of Terfenadine can be increased when it is combined with KOS-1584.
Spiramycin The serum concentration of Terfenadine can be increased when it is combined with Spiramycin.
Ridaforolimus The serum concentration of Terfenadine can be increased when it is combined with Ridaforolimus.
Temsirolimus The serum concentration of Terfenadine can be increased when it is combined with Temsirolimus.
AVE9633 The serum concentration of Terfenadine can be increased when it is combined with AVE9633.
Coltuximab ravtansine The serum concentration of Terfenadine can be increased when it is combined with Coltuximab ravtansine.
Cethromycin The serum concentration of Terfenadine can be increased when it is combined with Cethromycin.
Mitemcinal The serum concentration of Terfenadine can be increased when it is combined with Mitemcinal.
Brefeldin A The serum concentration of Terfenadine can be increased when it is combined with Brefeldin A.
Solithromycin The serum concentration of Terfenadine can be increased when it is combined with Solithromycin.
Kitasamycin The serum concentration of Terfenadine can be increased when it is combined with Kitasamycin.
Carbomycin The serum concentration of Terfenadine can be increased when it is combined with Carbomycin.
Doramectin The serum concentration of Terfenadine can be increased when it is combined with Doramectin.
Eprinomectin The serum concentration of Terfenadine can be increased when it is combined with Eprinomectin.
Oleandomycin The serum concentration of Terfenadine can be increased when it is combined with Oleandomycin.
Selamectin The serum concentration of Terfenadine can be increased when it is combined with Selamectin.
Tildipirosin The serum concentration of Terfenadine can be increased when it is combined with Tildipirosin.
Tilmicosin The serum concentration of Terfenadine can be increased when it is combined with Tilmicosin.
Tylosin The serum concentration of Terfenadine can be increased when it is combined with Tylosin.
Tylvalosin The serum concentration of Terfenadine can be increased when it is combined with Tylvalosin.
Bryostatin 1 The serum concentration of Terfenadine can be increased when it is combined with Bryostatin 1.
Lorvotuzumab mertansine The serum concentration of Terfenadine can be increased when it is combined with Lorvotuzumab mertansine.
Epofolate The serum concentration of Terfenadine can be increased when it is combined with Epofolate.
Sagopilone The serum concentration of Terfenadine can be increased when it is combined with Sagopilone.
Mirvetuximab soravtansine The serum concentration of Mirvetuximab Soravtansine can be increased when it is combined with Terfenadine.
Troleandomycin The serum concentration of Terfenadine can be increased when it is combined with Troleandomycin.
Miocamycin The serum concentration of Terfenadine can be increased when it is combined with Miocamycin.
Flurithromycin The serum concentration of Terfenadine can be increased when it is combined with Flurithromycin.
Rokitamycin The serum concentration of Terfenadine can be increased when it is combined with Rokitamycin.
Midecamycin The serum concentration of Terfenadine can be increased when it is combined with Midecamycin.
Mepartricin The serum concentration of Terfenadine can be increased when it is combined with Mepartricin.
Aclidinium The risk or severity of adverse effects can be increased when Terfenadine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Terfenadine.
Mirabegron The risk or severity of urinary retention can be increased when Terfenadine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Terfenadine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Terfenadine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Terfenadine.
Tiotropium The risk or severity of adverse effects can be increased when Terfenadine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Terfenadine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Terfenadine is combined with Umeclidinium.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Terfenadine.
Colchicine The metabolism of Colchicine can be decreased when combined with Terfenadine.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Terfenadine.
Iloperidone The risk or severity of QTc prolongation can be increased when Terfenadine is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Terfenadine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Terfenadine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Terfenadine.
Benzylpenicilloyl polylysine Terfenadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Terfenadine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Terfenadine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Terfenadine.
Glycopyrronium The risk or severity of adverse effects can be increased when Terfenadine is combined with Glycopyrronium.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Terfenadine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Terfenadine.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Terfenadine.
Delavirdine The metabolism of Terfenadine can be decreased when combined with Delavirdine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Terfenadine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Terfenadine.
Bicalutamide The serum concentration of Terfenadine can be increased when it is combined with Bicalutamide.
Posaconazole The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Terfenadine.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Terfenadine is combined with Botulinum toxin type A.
Glucagon Terfenadine may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Terfenadine may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Terfenadine is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Terfenadine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Terfenadine is combined with Ramosetron.
Amphetamine Amphetamine may decrease the sedative activities of Terfenadine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Terfenadine.
Diethylpropion Diethylpropion may decrease the sedative activities of Terfenadine.
Lisdexamfetamine The serum concentration of dextroamphetamine, an active metabolite of Lisdexamfetamine, can be increased when used in combination with Terfenadine.
Mephentermine Mephentermine may decrease the sedative activities of Terfenadine.
MMDA MMDA may decrease the sedative activities of Terfenadine.
Midomafetamine Midomafetamine may decrease the sedative activities of Terfenadine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Terfenadine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Terfenadine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Terfenadine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Terfenadine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Terfenadine.

Target Protein

Histamine H1 receptor HRH1
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M5 CHRM5
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M2 CHRM2
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Synthesis reference: Timothy G. Fawcett, Christian T. Goralski, David W. Ziettlow, "Preparation of polymorphically pure terfenadine." U.S. Patent US4742175, issued April, 1975.

Contoh Produk & Brand

Produk: 11 • International brands: 12
Produk
  • Allergy Relief
    Tablet • 60 mg / tab • Oral • Canada • Approved
  • Allergy Relief Once A Day Allergy Caplet 120mg
    Tablet • 120 mg • Oral • Canada • Approved
  • Apo-terfenadine Tab 120mg
    Tablet • 120 mg / tab • Oral • Canada • Generic • Approved
  • Apo-terfenadine Tablets 60mg
    Tablet • 60 mg / tab • Oral • Canada • Generic • Approved
  • Novo-terfenadine Tab 60mg
    Tablet • 60 mg / tab • Oral • Canada • Generic • Approved
  • Seldane - Sus 30mg/5ml
    Suspension • 30 mg / 5 mL • Oral • Canada • Approved
  • Seldane - Tab 60mg
    Tablet • 60 mg / tab • Oral • Canada • Approved
  • Seldane 120mg Once-A-day Caplets
    Tablet • 120 mg / tab • Oral • Canada • Approved
Menampilkan 8 dari 11 produk.
International Brands
  • Bronal — Galenika
  • Daylert — Micro Labs
  • Seldane
  • Servinin — Novartis
  • Teldane
  • Terfed — Cipla
  • Terfenadin AL — Aliud
  • Terfenadine FLX — Accord Healthcare
  • Terfin — Interbat
  • Ternadin — Dunar

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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