Peringatan Keamanan

Second generation antihistamines such as loratadine have very few adverse effects; however, insomnia, headache, fatigue, drowsiness and rash have been reported.A176441 Symptoms of loratadine overdose include gastrointestinal side effects, agitation, drowsiness, tachycardia, and headache.A176441 It is advised to obtain an ECG in the event of loratadine overdose.A176441

Loratadine

DB00455

small molecule approved investigational

Deskripsi

Loratadine is a second generation antihistamine used to manage symptoms of allergic rhinitis.A176435 A lack of sedative and CNS adverse effects make loratadine, along with other second generation antihistamines, preferable over their 1st generation counterparts in many clinical situations.A176441

Struktur Molekul 2D

Berat 382.883
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is approximately 10 hours for loratadine and 20 hours for descarboethoxyloratadine.[A176438]
Volume Distribusi The volume of distribution of loratadine is 120 L/Kg.[L8618]
Klirens (Clearance) The clearance of loratadine after single oral doses of 20 mg and 40 mg are 12 L/h/kg and 9 L/h/kg respectively.[A5506] P-glycoprotein is involved in the clearance of many 2nd generation antihistamines, including loratadine, from the central nervous system. 1st generation antihistamines are not cleared by P-glycoprotein, which may help explain why they have a different central nervous system adverse effect profile compared to their 2nd generation counterparts.[L8618][A175075] It appears that an antihistamine with higher affinity for p-glycoprotein will have a lower incidence of CNS adverse effects.[A175072]

Absorpsi

Loratadine is rapidly absorbed and achieves peak plasma concentration in 1-2 hours, while it's main metabolite achieves peak plasma concentration in 3-4 hours.A176438 In the rapid dissolve formulation, the pharmacokinetic parameters of loratadine are as followsL8486: Cmax = 2.56 ng/ml, Tmax = 1.14 hrs, AUC = 6.14 ng x hr/ml. In the rapid dissolve formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as followsL8486: Cmax = 3.72 ng/ml, Tmax = 1.97 hr, AUC = 49.1 ng x hr/ml. In the conventional formulation, the pharmacokinetic parameters of loratadine are as followsL8486: Cmax = 2.11 ng/ml, Tmax = 1.00 hr, AUC = 4.64 ng x hr/ml In the conventional formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as followsL8486: Cmax = 3.66 ng/ml, Tmax = 1.97 hr, AUC = 48.4 ng x hr/ml

Metabolisme

Loratadine undergoes extensive first pass metabolism in the liver and is primarily metabolized by CYP3A4, CYP2D6, CYP1A1 and CYP2C19. Less involved CYP enzymes include CYP1A2, CYP2B6, CYP2C8, CYP2C9 and CYP3A5.A38842A176444 CYP3A4 and CYP2D6 are mainly responsible for metabolizing loratadine to descarboethoxyloratadine.A176444 This primary metabolite is 4 times more pharmacologically active than loratadine.A176438 In addition, a study demonstrates that descarboethoxyloratadine is first glucuronidated by UGT2B10, then hydroxylated by CYP2C8 to form 3-hydroxydesloratadine.A185855 Further glucuronidation of 3-hydroxydesloratadine facilitates excretion.A185843

Rute Eliminasi

Over a 10 day period, 40% of loratadine is excreted in the urine, and 42% is eliminated in the faeces.L8486

Interaksi Obat

713 Data
Reserpine Reserpine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Loratadine which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Loratadine which could result in a higher serum level.
Tamoxifen Tamoxifen may decrease the excretion rate of Loratadine which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Loratadine which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Loratadine which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Loratadine which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Loratadine which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Loratadine which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Loratadine which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Loratadine which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Loratadine which could result in a higher serum level.
Cyclosporine Cyclosporine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Erythromycin The serum concentration of Loratadine can be increased when it is combined with Erythromycin.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Quinidine Quinidine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Nifedipine Loratadine may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Loratadine which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Loratadine which could result in a higher serum level.
Benzylpenicilloyl polylysine Loratadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Loratadine.
Amphetamine Amphetamine may decrease the sedative activities of Loratadine.
Phentermine Phentermine may decrease the sedative activities of Loratadine.
Benzphetamine Benzphetamine may decrease the sedative activities of Loratadine.
Diethylpropion Diethylpropion may decrease the sedative activities of Loratadine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Loratadine.
Mephentermine Mephentermine may decrease the sedative activities of Loratadine.
MMDA MMDA may decrease the sedative activities of Loratadine.
Midomafetamine Midomafetamine may decrease the sedative activities of Loratadine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Loratadine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Loratadine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Loratadine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Loratadine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Loratadine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Loratadine.
Metamfetamine Metamfetamine may decrease the sedative activities of Loratadine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Loratadine.
Ritobegron Ritobegron may decrease the sedative activities of Loratadine.
Mephedrone Mephedrone may decrease the sedative activities of Loratadine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Loratadine.
Gepefrine Gepefrine may decrease the sedative activities of Loratadine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Loratadine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Loratadine.
Rosiglitazone The metabolism of Rosiglitazone can be decreased when combined with Loratadine.
Torasemide The metabolism of Torasemide can be decreased when combined with Loratadine.
Dapsone The metabolism of Dapsone can be decreased when combined with Loratadine.
Morphine The metabolism of Morphine can be decreased when combined with Loratadine.
Sulfadiazine The metabolism of Sulfadiazine can be decreased when combined with Loratadine.
Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Loratadine.
Piroxicam The metabolism of Piroxicam can be decreased when combined with Loratadine.
Diclofenac The metabolism of Diclofenac can be decreased when combined with Loratadine.
Amodiaquine The metabolism of Amodiaquine can be decreased when combined with Loratadine.
Paramethadione The metabolism of Paramethadione can be decreased when combined with Loratadine.
Naproxen The metabolism of Naproxen can be decreased when combined with Loratadine.
Tazarotene The metabolism of Tazarotene can be decreased when combined with Loratadine.
Repaglinide The metabolism of Repaglinide can be decreased when combined with Loratadine.
Almotriptan The metabolism of Almotriptan can be decreased when combined with Loratadine.
Irbesartan The metabolism of Irbesartan can be decreased when combined with Loratadine.
Selegiline The metabolism of Selegiline can be decreased when combined with Loratadine.
Fluvastatin The metabolism of Fluvastatin can be decreased when combined with Loratadine.
Tolbutamide The metabolism of Tolbutamide can be decreased when combined with Loratadine.
Pioglitazone The metabolism of Pioglitazone can be decreased when combined with Loratadine.
Ketamine The metabolism of Ketamine can be decreased when combined with Loratadine.
Lapatinib The metabolism of Lapatinib can be decreased when combined with Loratadine.
Mestranol The metabolism of Mestranol can be decreased when combined with Loratadine.
Aminophenazone The metabolism of Aminophenazone can be decreased when combined with Loratadine.
Antipyrine The metabolism of Antipyrine can be decreased when combined with Loratadine.
Licofelone The metabolism of Licofelone can be decreased when combined with Loratadine.
Beraprost The metabolism of Beraprost can be decreased when combined with Loratadine.
Eltrombopag The metabolism of Eltrombopag can be decreased when combined with Loratadine.
Muraglitazar The metabolism of Muraglitazar can be decreased when combined with Loratadine.
Ketobemidone The metabolism of Ketobemidone can be decreased when combined with Loratadine.
Seratrodast The metabolism of Seratrodast can be decreased when combined with Loratadine.
Benzyl alcohol The metabolism of Benzyl alcohol can be decreased when combined with Loratadine.
Perospirone The metabolism of Perospirone can be decreased when combined with Loratadine.
Riociguat The metabolism of Riociguat can be decreased when combined with Loratadine.
Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Loratadine.
Olodaterol The metabolism of Olodaterol can be decreased when combined with Loratadine.
Lobeglitazone The metabolism of Lobeglitazone can be decreased when combined with Loratadine.
Netoglitazone The metabolism of Netoglitazone can be decreased when combined with Loratadine.
Rivoglitazone The metabolism of Rivoglitazone can be decreased when combined with Loratadine.
Ciglitazone The metabolism of Ciglitazone can be decreased when combined with Loratadine.
Propacetamol The metabolism of Propacetamol can be decreased when combined with Loratadine.
Balaglitazone The metabolism of Balaglitazone can be decreased when combined with Loratadine.
Testosterone cypionate The metabolism of Testosterone cypionate can be decreased when combined with Loratadine.
Testosterone enanthate The metabolism of Testosterone enanthate can be decreased when combined with Loratadine.
Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Loratadine.
Istradefylline The metabolism of Istradefylline can be decreased when combined with Loratadine.
Dexibuprofen The metabolism of Dexibuprofen can be decreased when combined with Loratadine.
Trimethadione The metabolism of Trimethadione can be decreased when combined with Loratadine.
Ketorolac The metabolism of Ketorolac can be decreased when combined with Loratadine.
Propofol The metabolism of Propofol can be decreased when combined with Loratadine.
Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Loratadine.
Azelastine The metabolism of Azelastine can be decreased when combined with Loratadine.
Domperidone The risk or severity of QTc prolongation can be increased when Loratadine is combined with Domperidone.
Capravirine The metabolism of Capravirine can be decreased when combined with Loratadine.
Glasdegib The risk or severity of QTc prolongation can be increased when Loratadine is combined with Glasdegib.
Anastrozole The metabolism of Anastrozole can be decreased when combined with Loratadine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Loratadine.

Target Protein

Histamine H1 receptor HRH1
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Synthesis reference: Alberto Stampa, Pelayo Camps, Gloria Rodriguez, Jordi Bosch, Maria del Carmen Onrubia, "Process for the preparation of loratadine." U.S. Patent US6084100, issued July 04, 2000.
Artikel (PubMed)
  • PMID: 14655812
    See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6.
  • PMID: 9444440
    Menardo JL, Horak F, Danzig MR, Czarlewski W: A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4.
  • PMID: 1977506
    Howarth PH: Histamine and asthma: an appraisal based on specific H1-receptor antagonism. Clin Exp Allergy. 1990 Aug;20 Suppl 2:31-41.
  • PMID: 11291777
    Baroody FM, Naclerio RM: Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27.
  • PMID: 29371864
    Tenn MW, Steacy LM, Ng CC, Ellis AK: Onset of action for loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the Environmental Exposure Unit: a post hoc analysis of total symptom score. Allergy Asthma Clin Immunol. 2018 Jan 16;14:5. doi: 10.1186/s13223-017-0227-4. eCollection 2018.
  • PMID: 2525847
    Barenholtz HA, McLeod DC: Loratadine: a nonsedating antihistamine with once-daily dosing. DICP. 1989 Jun;23(6):445-50.
  • PMID: 29670310
    Randall KL, Hawkins CA: Antihistamines and allergy. Aust Prescr. 2018 Apr;41(2):41-45. doi: 10.18773/austprescr.2018.013. Epub 2018 Apr 3.
  • PMID: 23723474
    Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832.
Menampilkan 8 dari 16 artikel.

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