Peringatan Keamanan

LD50=2052mg/kg in mice

Astemizole

DB00637

small molecule approved withdrawn

Deskripsi

Astemizole is a long-acting, non-sedating second generation antihistamine used in the treatment of allergy symptoms. It was withdrawn from market by the manufacturer in 1999 due to the potential to cause arrhythmias at high doses, especially when when taken with CYP inhibitors or grapefruit juice.

Struktur Molekul 2D

Berat 458.5703
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1 day
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly absorbed from the gastrointestinal tract.

Metabolisme

Almost completely metabolized in the liver and primarily excreted in the feces.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Food decreases absorption.

Interaksi Obat

1041 Data
Modafinil The metabolism of Astemizole can be increased when combined with Modafinil.
Armodafinil The metabolism of Astemizole can be increased when combined with Armodafinil.
Phenytoin The metabolism of Astemizole can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Astemizole can be increased when combined with Fosphenytoin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Astemizole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Astemizole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Astemizole.
Colchicine The metabolism of Colchicine can be decreased when combined with Astemizole.
Fentanyl The metabolism of Astemizole can be decreased when combined with Fentanyl.
Iloperidone The risk or severity of QTc prolongation can be increased when Astemizole is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Astemizole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Astemizole.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Astemizole.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Astemizole.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Astemizole.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Astemizole.
Benzylpenicilloyl polylysine Astemizole may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Astemizole.
Metreleptin The metabolism of Astemizole can be increased when combined with Metreleptin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Astemizole.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Astemizole.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Astemizole.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Astemizole.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Astemizole.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Astemizole.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Astemizole.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Astemizole.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Astemizole.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Astemizole.
Crizotinib The metabolism of Astemizole can be decreased when combined with Crizotinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Astemizole.
Bicalutamide The serum concentration of Astemizole can be increased when it is combined with Bicalutamide.
Mirabegron The serum concentration of Astemizole can be increased when it is combined with Mirabegron.
Posaconazole The serum concentration of Astemizole can be increased when it is combined with Posaconazole.
Amphetamine Amphetamine may decrease the sedative activities of Astemizole.
Phentermine Phentermine may decrease the sedative activities of Astemizole.
Benzphetamine Benzphetamine may decrease the sedative activities of Astemizole.
Diethylpropion Diethylpropion may decrease the sedative activities of Astemizole.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Astemizole.
Mephentermine Mephentermine may decrease the sedative activities of Astemizole.
MMDA MMDA may decrease the sedative activities of Astemizole.
Midomafetamine Midomafetamine may decrease the sedative activities of Astemizole.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Astemizole.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Astemizole.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Astemizole.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Astemizole.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Astemizole.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Astemizole.
Metamfetamine Metamfetamine may decrease the sedative activities of Astemizole.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Astemizole.
Ritobegron Ritobegron may decrease the sedative activities of Astemizole.
Mephedrone Mephedrone may decrease the sedative activities of Astemizole.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Astemizole.
Gepefrine Gepefrine may decrease the sedative activities of Astemizole.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Astemizole.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Astemizole.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Astemizole.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Astemizole.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Astemizole.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Astemizole.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Astemizole.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Astemizole.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Astemizole.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Astemizole.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Astemizole.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Astemizole.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Astemizole.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Astemizole.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Astemizole.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Astemizole.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Astemizole.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lomefloxacin is combined with Astemizole.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Astemizole.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Astemizole.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Astemizole.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ofloxacin is combined with Astemizole.
Probucol The risk or severity of QTc prolongation can be increased when Probucol is combined with Astemizole.
Aceprometazine The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Astemizole.
Terlipressin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Astemizole.
Pracinostat The risk or severity of QTc prolongation can be increased when Pracinostat is combined with Astemizole.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Technetium Tc-99m ciprofloxacin is combined with Astemizole.
Garenoxacin The risk or severity of QTc prolongation can be increased when Garenoxacin is combined with Astemizole.
Tedisamil The risk or severity of QTc prolongation can be increased when Tedisamil is combined with Astemizole.
Tucidinostat The risk or severity of QTc prolongation can be increased when Tucidinostat is combined with Astemizole.
Telavancin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Astemizole.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Nemonoxacin is combined with Astemizole.
Antazoline The risk or severity of QTc prolongation can be increased when Antazoline is combined with Astemizole.
Butriptyline The risk or severity of QTc prolongation can be increased when Butriptyline is combined with Astemizole.
Amifampridine The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Astemizole.
Mocetinostat The risk or severity of QTc prolongation can be increased when Mocetinostat is combined with Astemizole.
Entinostat The risk or severity of QTc prolongation can be increased when Entinostat is combined with Astemizole.
CUDC-101 The risk or severity of QTc prolongation can be increased when CUDC-101 is combined with Astemizole.
Simendan The risk or severity of QTc prolongation can be increased when Simendan is combined with Astemizole.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ricolinostat is combined with Astemizole.
Abexinostat The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Astemizole.
Oxatomide The risk or severity of QTc prolongation can be increased when Oxatomide is combined with Astemizole.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Sitafloxacin is combined with Astemizole.
Sultopride The risk or severity of QTc prolongation can be increased when Sultopride is combined with Astemizole.
Nizofenone The risk or severity of QTc prolongation can be increased when Nizofenone is combined with Astemizole.
Bunaftine The risk or severity of QTc prolongation can be increased when Bunaftine is combined with Astemizole.

Target Protein

Histamine H1 receptor HRH1
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Voltage-gated delayed rectifier potassium channel KCNH1 KCNH1
Microtubule-associated protein tau MAPT

Referensi & Sumber

Synthesis reference: Godelieve Irma Christine Maria Heylen, Cornelus Gerardus Maria Janssen, Jurzak Mirek, Henricus Petrus Martinus Maria Van Assouw, "Radiolabeled astemizole and method of making." U.S. Patent US07541476, issued June 02, 2009.
Artikel (PubMed)
  • PMID: 16723379
    Wang X, Hockerman GH, Green HW 3rd, Babbs CF, Mohammad SI, Gerrard D, Latour MA, London B, Hannon KM, Pond AL: Merg1a K+ channel induces skeletal muscle atrophy by activating the ubiquitin proteasome pathway. FASEB J. 2006 Jul;20(9):1531-3. Epub 2006 May 24.
  • PMID: 16816845
    Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr: A clinical drug library screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2.

Contoh Produk & Brand

Produk: 3 • International brands: 8
Produk
  • Hismanal - Tab 10mg
    Tablet • 10 mg / tab • Oral • Canada • Approved
  • Hismanal Suspension 2mg/ml
    Suspension • 2 mg / mL • Oral • Canada • Approved
  • Hismanal Tab 10mg
    Tablet • 10 mg / tab • Oral • Canada • Approved
International Brands
  • Acemiz — Lupin
  • Alerkin — Incobra
  • Astemison
  • Astesen — Senosiain
  • Hismanal — Janssen
  • Histalong — Biofarma
  • Lergibrumizol — Bruluart
  • Stemiz — Cadila HC

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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