Acrivastine

DB09488

small molecule approved

Deskripsi

Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia.

Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D.

Struktur Molekul 2D

Berat 348.4382
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life for acrivastine was 1.9 ± 0.3 hours following single oral doses and increased to 3.5 ± 1.9 hours at steady state. The terminal half-life for the propionic acid metabolite was 3.8 ± 1.4 hours.
Volume Distribusi 0.46 ± 0.05 L/kg
Klirens (Clearance) 2.9 ± 0.7 mL/min/kg

Absorpsi

Acrivastine was absorbed rapidly from the combination capsule following oral administration and was as bioavailable as a solution of acrivastine. After administration of SEMPREX-D Capsules, maximum plasma acrivastine concentrations were achieved at 1.14 ± 0.23 hour.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

A mass balance study in 7 healthy volunteers showed that acrivastine is primarily eliminated by the kidneys. Over a 72-hour collection period, about 84% of the administered total radioactivity was recovered in urine and about 13% in feces, for a combined recovery of about 97%.

Interaksi Obat

1058 Data
Benzylpenicilloyl polylysine Acrivastine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Acrivastine.
Amphetamine Amphetamine may decrease the sedative activities of Acrivastine.
Phentermine Phentermine may decrease the sedative activities of Acrivastine.
Benzphetamine Benzphetamine may decrease the sedative activities of Acrivastine.
Diethylpropion Diethylpropion may decrease the sedative activities of Acrivastine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Acrivastine.
Mephentermine Mephentermine may decrease the sedative activities of Acrivastine.
MMDA MMDA may decrease the sedative activities of Acrivastine.
Midomafetamine Midomafetamine may decrease the sedative activities of Acrivastine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Acrivastine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Acrivastine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Acrivastine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Acrivastine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Acrivastine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Acrivastine.
Metamfetamine Metamfetamine may decrease the sedative activities of Acrivastine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Acrivastine.
Ritobegron Ritobegron may decrease the sedative activities of Acrivastine.
Mephedrone Mephedrone may decrease the sedative activities of Acrivastine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Acrivastine.
Gepefrine Gepefrine may decrease the sedative activities of Acrivastine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Acrivastine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Acrivastine.
Leuprolide The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Goserelin.
Erythromycin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Moxifloxacin.
Ranolazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Ranolazine.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Sulfisoxazole.
Methadone The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Methadone.
Diltiazem The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Diltiazem.
Clozapine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Droperidol.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Chlorpromazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Acrivastine.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Ciprofloxacin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Atropine.
Chloroquine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Chloroquine.
Efavirenz The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Efavirenz.
Adenosine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Cinoxacin.
Loperamide The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Loperamide.
Granisetron The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Flecainide.
Clarithromycin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Clarithromycin.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Levacetylmethadol.
Saquinavir The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Saquinavir.
Mibefradil The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Mibefradil.
Probucol The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Telavancin.
Pazopanib The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Pazopanib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nemonoxacin.
Panobinostat The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Panobinostat.
Nilvadipine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Antazoline.
Crizotinib The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Crizotinib.
Bedaquiline The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Eperisone.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

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Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Semprex D
    Capsule • - • Oral • US • Approved
  • Semprex-D
    Capsule • - • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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