Peringatan Keamanan

Information regarding desloratadine overdose is limited, although somnolence has been reported. In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis.

In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD50), doses that represent 120 and 290 times the human exposure based on the recommended daily oral dose. In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.

Desloratadine

DB00967

small molecule approved investigational

Deskripsi

Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratidine (a second generation histamine). Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

Struktur Molekul 2D

Berat 310.821
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Desloratadine has a mean plasma elimination half-life of approximately 27 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Desloratadine administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean Tmax of approximately 3 hours, a mean steady-state Cmax of 4 ng/ml, and a mean steady-state AUC of 56.9 ng\*hr/ml. A similar profile was observed using 10 ml of an oral solution containing 5 mg of desloratadine. Food was found not to affect desloratadine absorption.

Metabolisme

Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine, which is subsequently glucuronidated.

Rute Eliminasi

Approximately 87% of a 14C-desloratadine dose was equally recovered in urine and feces as metabolic products.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1150 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Desloratadine.
Buprenorphine Desloratadine 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 Desloratadine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Hydrocodone Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Desloratadine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Desloratadine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
Mirtazapine Desloratadine 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 Desloratadine.
Orphenadrine Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Desloratadine 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 Desloratadine.
Pramipexole Desloratadine may increase the sedative activities of Pramipexole.
Ropinirole Desloratadine may increase the sedative activities of Ropinirole.
Rotigotine Desloratadine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Desloratadine.
Sodium oxybate Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Desloratadine 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 Desloratadine.
Thalidomide Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Desloratadine.
Benzylpenicilloyl polylysine Desloratadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Desloratadine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Desloratadine.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Desloratadine is combined with Botulinum toxin type A.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Desloratadine is combined with Botulinum toxin type B.
Ethanol Desloratadine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Desloratadine 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 Desloratadine.
Fluvoxamine The risk or severity of adverse effects can be increased when Desloratadine is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Desloratadine is combined with Duloxetine.
Sertraline The risk or severity of adverse effects can be increased when Desloratadine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Desloratadine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Desloratadine is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Desloratadine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Desloratadine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Desloratadine is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Desloratadine is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Desloratadine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Desloratadine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Desloratadine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Desloratadine is combined with Alaproclate.
Paroxetine The risk or severity of adverse effects can be increased when Desloratadine is combined with Paroxetine.
Amphetamine Amphetamine may decrease the sedative activities of Desloratadine.
Phentermine Phentermine may decrease the sedative activities of Desloratadine.
Benzphetamine Benzphetamine may decrease the sedative activities of Desloratadine.
Diethylpropion Diethylpropion may decrease the sedative activities of Desloratadine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Desloratadine.
Mephentermine Mephentermine may decrease the sedative activities of Desloratadine.
MMDA MMDA may decrease the sedative activities of Desloratadine.
Midomafetamine Midomafetamine may decrease the sedative activities of Desloratadine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Desloratadine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Desloratadine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Desloratadine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Desloratadine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Desloratadine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Desloratadine.
Metamfetamine Metamfetamine may decrease the sedative activities of Desloratadine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Desloratadine.
Ritobegron Ritobegron may decrease the sedative activities of Desloratadine.
Mephedrone Mephedrone may decrease the sedative activities of Desloratadine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Desloratadine.
Gepefrine Gepefrine may decrease the sedative activities of Desloratadine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Desloratadine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Desloratadine.
Naltrexone The risk or severity of adverse effects can be increased when Desloratadine is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Desloratadine is combined with Bezitramide.
Morphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Morphine.
Codeine The risk or severity of adverse effects can be increased when Desloratadine is combined with Codeine.
Hydromorphone The risk or severity of adverse effects can be increased when Desloratadine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Desloratadine is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Desloratadine is combined with Butorphanol.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Desloratadine is combined with Dextropropoxyphene.
Pentazocine The risk or severity of adverse effects can be increased when Desloratadine is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Desloratadine is combined with Sufentanil.
Alfentanil The risk or severity of adverse effects can be increased when Desloratadine is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Desloratadine is combined with Fentanyl.
Nalbuphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Desloratadine is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Desloratadine is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Desloratadine is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Desloratadine is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Desloratadine is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Desloratadine is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Desloratadine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Desloratadine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Desloratadine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Desloratadine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Desloratadine is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Desloratadine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Desloratadine is combined with DPDPE.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Synthesis reference: Zoltan Toth, "Processes for preparation of polymorphic forms of desloratadine." U.S. Patent US20040242619, issued December 02, 2004.
Artikel (PubMed)
  • PMID: 10784544
    Mann RD, Pearce GL, Dunn N, Shakir S: Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice. BMJ. 2000 Apr 29;320(7243):1184-6.
  • PMID: 12917016
    Glass DJ, Harper AS: Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine. BMC Fam Pract. 2003 Aug 13;4:10. Epub 2003 Aug 13.
  • PMID: 14655812
    See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6.
  • PMID: 18336052
    Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30.
  • PMID: 19539095
    Bachert C: A review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clin Ther. 2009 May;31(5):921-44. doi: 10.1016/j.clinthera.2009.05.017.
  • PMID: 17902729
    DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83.
  • PMID: 20067329
    Bachert C, Maurer M: Safety and efficacy of desloratadine in subjects with seasonal allergic rhinitis or chronic urticaria: results of four postmarketing surveillance studies. Clin Drug Investig. 2010;30(2):109-22. doi: 10.2165/11530930-000000000-00000.
  • PMID: 12642846
    Simons FE, Prenner BM, Finn A Jr: Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol. 2003 Mar;111(3):617-22.

Contoh Produk & Brand

Produk: 241 • International brands: 1
Produk
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerinaze
    Tablet, multilayer, extended release • - • Oral • EU • Approved
  • Aerius
    Syrup • 0.5 mg / mL • Oral • Canada • OTC • Approved
  • Aerius
    Tablet • 5 mg • Oral • Canada • OTC • Approved
Menampilkan 8 dari 241 produk.
International Brands
  • Claramax

Sekuens Gen/Protein (FASTA)

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