Chlorcyclizine

DB08936

small molecule approved

Deskripsi

Chlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can be used as an antiemetic.

Struktur Molekul 2D

Berat 300.826
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) about 12 h.
Volume Distribusi After a single oral dose of 2 mg/kg to 4 subjects, average peak plasma concentrations of about 0.05 mg/L and 0.03 mg/L were attained in 5 h for unchanged drug and norchlorcyclizine, respectively. After oral administration of 50 mg 3 times a day for 6 days, plasma concentrations of norchlorcyclizine of 0.05 to 0.11 mg/L were reported on the first day after the cessation of treatment and plasma concentrations of 0.02 to 0.04 mg/L were found on the 10th day after cessation of treatment [Kuntzman et al. 1973].
Klirens (Clearance) -

Absorpsi

Readily absorbed after oral administration and widely distributed throughout the body. Metabolised by N-demethylation to form norchlorcyclizine and by N-oxidation.

Metabolisme

High concentrations of the N-desmethyl metabolite are found in the liver, lungs, kidney, and spleen.

Rute Eliminasi

Slowly excreted in the urine; measurable amounts of norchlorcyclizine have been detected in the urine for up to 3 weeks after the cessation of chronic oral administration. About 0.5% of a single dose is excreted in the urine as the N-oxide.

Interaksi Makanan

1 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may increase the drowsiness caused by chlorcyclizine.

Interaksi Obat

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

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Synthesis reference: Baltzly, R. and Castillo, J.C.; U.S. Patent 2,630,435; March 3, 1953; assigned to Burroughs- Wellcome & Co. (USA.) Inc.
Artikel (PubMed)
  • PMID: 21058326
    Enright BP, Gu YZ, Snyder RD, Dugyala RR, Obert LA, Treinen KA, McIntyre BS, Veneziale RW: Effects of the histamine H1 antagonist chlorcyclizine on rat fetal palate development. Birth Defects Res B Dev Reprod Toxicol. 2010 Dec;89(6):474-84. doi: 10.1002/bdrb.20261.
  • PMID: 14334288
    KUNTZMAN R, KLUTCH A, TSAI I, BURNS JJ: PHYSIOLOGICAL DISTRIBUTION AND METABOLIC INACTIVATION OF CHLORCYCLIZINE AND CYCLIZINE. J Pharmacol Exp Ther. 1965 Jul;149:29-35.

Contoh Produk & Brand

Produk: 19 • International brands: 5
Produk
  • Ahist
    Tablet • 25 mg/1 • Oral • US • OTC
  • Biclora
    Liquid • - • Oral • US • OTC
  • Biclora
    Tablet • - • Oral • US • OTC
  • Biclora
    Liquid • - • Oral • US • OTC
  • biclora-D
    Liquid • - • Oral • US • OTC
  • biclora-D
    Tablet • - • Oral • US • OTC
  • Bonine Kids
    Tablet, chewable • 25 mg/1 • Oral • US • OTC
  • Dallergy
    Tablet, chewable • - • Oral • US • OTC
Menampilkan 8 dari 19 produk.
International Brands
  • Di-Paralene
  • Mantadil
  • Pruresidine
  • Trihistan
  • Zimin — New Chemical

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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