Peringatan Keamanan

Patients experiencing an overdose may present with drowsiness.L7694 Children may become agitated and restless before drowsiness.L7694 Patients should be treated with supportive measures.L7694 Dialysis will not assist in removing the drug from the body.L7694

The maximal nonlethal dose in mice and rats is 240mg/kg.L7694

Levocetirizine

DB06282

small molecule approved

Deskripsi

Levocetirizine is a selective histamine H1 antagonist used to treat a variety of allergic symptoms.A181748,A181790,L7694 It is the R enantiomer of cetirizine.L7694 Levocetirizine has greater affinity for the histamine H1 receptor than cetirizine.L7694

Levocetirizine was granted FDA approval in 1995.L7694

Struktur Molekul 2D

Berat 388.89
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average half life of levocetirizine is 7.05±1.54 hours.[A181727]
Volume Distribusi The volume of distribution of levocetirizine is 0.33±0.02L/kg.[A181727]
Klirens (Clearance) The average clearance of levocetirizine is 0.57±0.18mL/min/kg.[A181727]

Absorpsi

Following a 5mg oral dose of levocetirizine, a Cmax of 0.27±0.04µg/mL with a Tmax of 0.75±0.50h.A181727 The AUC of levocetirizine is 2.31±0.50µg\*h/mL.A181727 Taking levocetirizine with food does not affect the AUC but delays Tmax by 1.25 hours and lowers Cmax by 36%.L7694

Metabolisme

Levocetirizine is poorly metabolized with 85.8% of an oral dose being excreted as the unchanged drug.A181727 Levocetirizine can be metabolized to a dihydrodiol (M2), an N-oxide (M3), a hydroxymethoxy derivative (M4), a hydroxy derivative (M5), an O-dealkylated derivative (M6), a taurine conjugate (M8), and an N-dealkylated and aromatic hydroxylated derivative (M9).A181727 The M5 metabolite can be glucuronidated to form the M1 metabolite and the M9 metabolite can form 4-chloro-4'-hydroxybenzhydryl mercapturates (M10a and M10b).A181727

Rute Eliminasi

168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces.A181727 In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite.A181727 In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite.A181727

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

1645 Data
Buprenorphine Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Hydrocodone Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Levocetirizine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Levocetirizine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Mirtazapine Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Orphenadrine Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Pramipexole Levocetirizine may increase the sedative activities of Pramipexole.
Ropinirole Levocetirizine may increase the sedative activities of Ropinirole.
Rotigotine Levocetirizine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Levocetirizine.
Sodium oxybate Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Thalidomide Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Benzylpenicilloyl polylysine Levocetirizine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Levocetirizine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Levocetirizine.
Ethanol Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Levocetirizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Levocetirizine.
Fluvoxamine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Levocetirizine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Levocetirizine is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Seproxetine.
Levomilnacipran Levocetirizine may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Indalpine The risk or severity of adverse effects can be increased when Levocetirizine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Levocetirizine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Levocetirizine is combined with Alaproclate.
Citalopram The risk or severity of QTc prolongation can be increased when Levocetirizine is combined with Citalopram.
Escitalopram The risk or severity of adverse effects can be increased when Levocetirizine is combined with Escitalopram.
Amphetamine Amphetamine may decrease the sedative activities of Levocetirizine.
Phentermine Phentermine may decrease the sedative activities of Levocetirizine.
Benzphetamine Benzphetamine may decrease the sedative activities of Levocetirizine.
Diethylpropion Diethylpropion may decrease the sedative activities of Levocetirizine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Levocetirizine.
Mephentermine Mephentermine may decrease the sedative activities of Levocetirizine.
MMDA MMDA may decrease the sedative activities of Levocetirizine.
Midomafetamine Midomafetamine may decrease the sedative activities of Levocetirizine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Levocetirizine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Levocetirizine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Levocetirizine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Levocetirizine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Levocetirizine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Levocetirizine.
Metamfetamine Metamfetamine may decrease the sedative activities of Levocetirizine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Levocetirizine.
Ritobegron Ritobegron may decrease the sedative activities of Levocetirizine.
Mephedrone Mephedrone may decrease the sedative activities of Levocetirizine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Levocetirizine.
Gepefrine Gepefrine may decrease the sedative activities of Levocetirizine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Levocetirizine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Levocetirizine.
Trospium Trospium may increase the anticholinergic activities of Levocetirizine.
Oxyphenonium Oxyphenonium may increase the anticholinergic activities of Levocetirizine.
Benzatropine The risk or severity of QTc prolongation can be increased when Benzatropine is combined with Levocetirizine.
Ipratropium Ipratropium may increase the anticholinergic activities of Levocetirizine.
Metixene Metixene may increase the anticholinergic activities of Levocetirizine.
Buclizine The risk or severity of QTc prolongation can be increased when Buclizine is combined with Levocetirizine.
Trihexyphenidyl Trihexyphenidyl may increase the anticholinergic activities of Levocetirizine.
Oxyphencyclimine Oxyphencyclimine may increase the anticholinergic activities of Levocetirizine.
Procyclidine Procyclidine may increase the anticholinergic activities of Levocetirizine.
Profenamine Profenamine may increase the anticholinergic activities of Levocetirizine.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Levocetirizine.
Methscopolamine bromide Methscopolamine bromide may increase the anticholinergic activities of Levocetirizine.
Tridihexethyl Tridihexethyl may increase the anticholinergic activities of Levocetirizine.
Anisotropine methylbromide Anisotropine methylbromide may increase the anticholinergic activities of Levocetirizine.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Levocetirizine.
Nicardipine The metabolism of Levocetirizine can be decreased when combined with Nicardipine.
Pirenzepine Pirenzepine may increase the anticholinergic activities of Levocetirizine.
Homatropine methylbromide Homatropine methylbromide may increase the anticholinergic activities of Levocetirizine.
Benzquinamide Benzquinamide may increase the anticholinergic activities of Levocetirizine.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Levocetirizine.
Propantheline Propantheline may decrease the excretion rate of Levocetirizine which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Levocetirizine which could result in a higher serum level.
Biperiden Biperiden may increase the anticholinergic activities of Levocetirizine.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Levocetirizine.
Methantheline Methantheline may increase the anticholinergic activities of Levocetirizine.
Cycrimine Cycrimine may increase the anticholinergic activities of Levocetirizine.
Glycopyrronium Glycopyrronium may increase the anticholinergic activities of Levocetirizine.
Tolterodine The risk or severity of QTc prolongation can be increased when Tolterodine is combined with Levocetirizine.
Oxybutynin Oxybutynin may increase the anticholinergic activities of Levocetirizine.
Flavoxate Flavoxate may decrease the excretion rate of Levocetirizine which could result in a higher serum level.
Diphenidol Diphenidol may increase the anticholinergic activities of Levocetirizine.
Tiotropium Tiotropium may decrease the excretion rate of Levocetirizine which could result in a higher serum level.
Solifenacin The risk or severity of QTc prolongation can be increased when Solifenacin is combined with Levocetirizine.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11758635
    Benedetti MS, Plisnier M, Kaise J, Maier L, Baltes E, Arendt C, McCracken N: Absorption, distribution, metabolism and excretion of 14Clevocetirizine, the R enantiomer of cetirizine, in healthy volunteers. Eur J Clin Pharmacol. 2001 Oct;57(8):571-82.
  • PMID: 21918368
    Mosges R, Konig V, Koberlein J: The effectiveness of levocetirizine in comparison with loratadine in treatment of allergic rhinitis--a meta-analysis. Allergol Int. 2011 Dec;60(4):541-6. doi: 10.2332/allergolint.10-OA-0300. Epub 2011 Sep 25.
  • PMID: 7614779
    Desager JP, Horsmans Y: Pharmacokinetic-pharmacodynamic relationships of H1-antihistamines. Clin Pharmacokinet. 1995 May;28(5):419-32. doi: 10.2165/00003088-199528050-00006.

Contoh Produk & Brand

Produk: 141 • International brands: 1
Produk
  • 24HR Allergy Relief
    Tablet, coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet, coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet, coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • OTC • Approved
  • Allergy Relief 24HR
    Tablet • 5 mg/1 • Oral • US • Generic • OTC • Approved
Menampilkan 8 dari 141 produk.
International Brands
  • Xusal

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul