Peringatan Keamanan

Oral ingestion of up to 60x the recommended dose has been reported, although no fatal overdoses of ketotifen have been described.A231209 Symptoms of ketotifen overdosage may include significant sedation, confusion, disorientation, tachycardia, hypotension, convulsions, hyperexcitability (particularly in children), and/or reversible coma.L32283 If ingestion is recent, consider the use of gastric lavage or activated charcoal.L32283 Other treatments should be supportive and administered as necessary based on symptoms.

Physostigmine may be useful to mitigate anticholinergic effects, and short-acting barbiturates or benzodiazepines may be used if the patient presents with excitation or convulsions.L32283

Ketotifen

DB00920

small molecule approved

Deskripsi

Ketotifen is a benzocycloheptathiophene derivativeA231204 with potent antihistaminic and mast cell stabilizing properties. It has a similar structure to some other first-generation antihistamines such as cyproheptadine and azatadine.A231204

Ketotifen was first developed in Switzerland in 1970 by Sandoz Pharmaceuticals and was initially marketed for the treatment of anaphylaxis.A231204 In the US, it is now used in an over-the-counter ophthalmic formulation for the treatment of itchy eyes associated with allergies,L32278 and in Canada a prescription-only oral formulation is available and indicated as an add-on therapy for children with atopic asthma.L32283 In addition, oral ketotifen is used in Mexico and across Europe for the treatment of various allergic symptoms and disorders,A231204 including urticaria, mastocytosis, and food allergy.

Struktur Molekul 2D

Berat 309.425
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ketotifen clearance is biphasic - the half-life of the distribution phase is approximately 3-5 hours and the half-life of the elimination phase is 22 hours.[A231214]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Following oral administration, absorption is relatively quick (with a Tmax of ~3 hours) and nearly complete as judged by plasma concentrations and urinary excretion levels - despite this, oral bioavailability is only ~50% due to a significant first-pass effect in the liver.L32283

Metabolisme

Ketotifen is extensively metabolized in humansA231214 and three distinct metabolites have been detected in human urine. The main metabolite is the N-glucuronide, comprising roughly 50% of urinary drug product,A231214 with the N-demethylated nor-ketotifen and the 10-hydroxyl derivative comprising 2% and <1%, respectively.L32283 Nor-ketotifen appears to be equally as active as its parent drug,L32283 though the clinical relevance of this is unclear given the relatively small proportion in which nor-ketotifen is found in the plasma. Formation of the N-glucuronide metabolite is carried out by several UGT enzymes, including UGT1A3, UGT1A4, and UGT2B10.A32560

Rute Eliminasi

More than 60% of an administered dose is excreted in the urine, primarily as metabolitesL32283 - of this material, <1% is found as unchanged drug, while the glucuronide and pharmacologically active nor-ketotifen metabolites account for 50% and 10%, respectively.A231214

Interaksi Makanan

1 Data
  • 1. Take with or without food. The co-administration of food does not significantly affect ketotifen disposition.

Interaksi Obat

74 Data
Benzylpenicilloyl polylysine Ketotifen may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Ketotifen.
Amphetamine Amphetamine may decrease the sedative activities of Ketotifen.
Phentermine Phentermine may decrease the sedative activities of Ketotifen.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Ketotifen.
Benzphetamine Benzphetamine may decrease the sedative activities of Ketotifen.
Diethylpropion Diethylpropion may decrease the sedative activities of Ketotifen.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Ketotifen.
Mephentermine Mephentermine may decrease the sedative activities of Ketotifen.
MMDA MMDA may decrease the sedative activities of Ketotifen.
Midomafetamine Midomafetamine may decrease the sedative activities of Ketotifen.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Ketotifen.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Ketotifen.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Ketotifen.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Ketotifen.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Ketotifen.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Ketotifen.
Metamfetamine Metamfetamine may decrease the sedative activities of Ketotifen.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Ketotifen.
Ritobegron Ritobegron may decrease the sedative activities of Ketotifen.
Mephedrone Mephedrone may decrease the sedative activities of Ketotifen.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Ketotifen.
Gepefrine Gepefrine may decrease the sedative activities of Ketotifen.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Ketotifen.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Ketotifen.
Pitolisant The therapeutic efficacy of Pitolisant can be decreased when used in combination with Ketotifen.
Norepinephrine The therapeutic efficacy of Norepinephrine can be increased when used in combination with Ketotifen.
Epinephrine The therapeutic efficacy of Epinephrine can be increased when used in combination with Ketotifen.
Droxidopa The therapeutic efficacy of Droxidopa can be increased when used in combination with Ketotifen.
Levonordefrin The therapeutic efficacy of Levonordefrin can be increased when used in combination with Ketotifen.
Protokylol The therapeutic efficacy of Protokylol can be increased when used in combination with Ketotifen.
Racepinephrine The therapeutic efficacy of Racepinephrine can be increased when used in combination with Ketotifen.
Theodrenaline The therapeutic efficacy of Theodrenaline can be increased when used in combination with Ketotifen.
Deoxyepinephrine The therapeutic efficacy of Deoxyepinephrine can be increased when used in combination with Ketotifen.
Ephedrine The therapeutic efficacy of Ephedrine can be increased when used in combination with Ketotifen.
Hyoscyamine Ketotifen may increase the anticholinergic activities of Hyoscyamine.
Troglitazone The risk or severity of thrombocytopenia can be increased when Troglitazone is combined with Ketotifen.
Glimepiride The risk or severity of thrombocytopenia can be increased when Glimepiride is combined with Ketotifen.
Acarbose The risk or severity of thrombocytopenia can be increased when Acarbose is combined with Ketotifen.
Metformin The risk or severity of thrombocytopenia can be increased when Metformin is combined with Ketotifen.
Rosiglitazone The risk or severity of thrombocytopenia can be increased when Rosiglitazone is combined with Ketotifen.
Acetohexamide The risk or severity of thrombocytopenia can be increased when Acetohexamide is combined with Ketotifen.
Miglitol The risk or severity of thrombocytopenia can be increased when Miglitol is combined with Ketotifen.
Chlorpropamide The risk or severity of thrombocytopenia can be increased when Chlorpropamide is combined with Ketotifen.
Nateglinide The risk or severity of thrombocytopenia can be increased when Nateglinide is combined with Ketotifen.
Tolazamide The risk or severity of thrombocytopenia can be increased when Tolazamide is combined with Ketotifen.
Repaglinide The risk or severity of thrombocytopenia can be increased when Repaglinide is combined with Ketotifen.
Phenformin The risk or severity of thrombocytopenia can be increased when Phenformin is combined with Ketotifen.
Glyburide The risk or severity of thrombocytopenia can be increased when Glyburide is combined with Ketotifen.
Glipizide The risk or severity of thrombocytopenia can be increased when Glipizide is combined with Ketotifen.
Gliclazide The risk or severity of thrombocytopenia can be increased when Gliclazide is combined with Ketotifen.
Tolbutamide The risk or severity of thrombocytopenia can be increased when Tolbutamide is combined with Ketotifen.
Pioglitazone The risk or severity of thrombocytopenia can be increased when Pioglitazone is combined with Ketotifen.
Gliquidone The risk or severity of thrombocytopenia can be increased when Gliquidone is combined with Ketotifen.
Mitiglinide The risk or severity of thrombocytopenia can be increased when Mitiglinide is combined with Ketotifen.
Sitagliptin The risk or severity of thrombocytopenia can be increased when Sitagliptin is combined with Ketotifen.
Glisoxepide The risk or severity of thrombocytopenia can be increased when Glisoxepide is combined with Ketotifen.
Glymidine The risk or severity of thrombocytopenia can be increased when Glymidine is combined with Ketotifen.
Buformin The risk or severity of thrombocytopenia can be increased when Buformin is combined with Ketotifen.
Vildagliptin The risk or severity of thrombocytopenia can be increased when Vildagliptin is combined with Ketotifen.
Voglibose The risk or severity of thrombocytopenia can be increased when Voglibose is combined with Ketotifen.
Alogliptin The risk or severity of thrombocytopenia can be increased when Alogliptin is combined with Ketotifen.
Dapagliflozin The risk or severity of thrombocytopenia can be increased when Dapagliflozin is combined with Ketotifen.
Saxagliptin The risk or severity of thrombocytopenia can be increased when Saxagliptin is combined with Ketotifen.
Linagliptin The risk or severity of thrombocytopenia can be increased when Linagliptin is combined with Ketotifen.
Canagliflozin The risk or severity of thrombocytopenia can be increased when Canagliflozin is combined with Ketotifen.
Glibornuride The risk or severity of thrombocytopenia can be increased when Glibornuride is combined with Ketotifen.
Benfluorex The risk or severity of thrombocytopenia can be increased when Benfluorex is combined with Ketotifen.
Empagliflozin The risk or severity of thrombocytopenia can be increased when Empagliflozin is combined with Ketotifen.
Gemigliptin The risk or severity of thrombocytopenia can be increased when Gemigliptin is combined with Ketotifen.
Evogliptin The risk or severity of thrombocytopenia can be increased when Evogliptin is combined with Ketotifen.
Carbutamide The risk or severity of thrombocytopenia can be increased when Carbutamide is combined with Ketotifen.
Metahexamide The risk or severity of thrombocytopenia can be increased when Metahexamide is combined with Ketotifen.
Bexagliflozin The risk or severity of thrombocytopenia can be increased when Bexagliflozin is combined with Ketotifen.

Target Protein

Histamine H1 receptor HRH1
6-phosphogluconate dehydrogenase, decarboxylating PGD

Referensi & Sumber

Synthesis reference: Roy W. Bryant, Ravi Parihar, Thomas Rowe, Susan Caballa, "Methods of Making and Using Stable Pharmaceutical Compositions Comprising Ketotifen and Naphazoline." U.S. Patent US20110312998, issued December 22, 2011.
Artikel (PubMed)
  • PMID: 9733660
    Hawes EM: N+-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group. Drug Metab Dispos. 1998 Sep;26(9):830-7.
  • PMID: 23611809
    Kato Y, Izukawa T, Oda S, Fukami T, Finel M, Yokoi T, Nakajima M: Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97. doi: 10.1124/dmd.113.051565. Epub 2013 Apr 23.
  • PMID: 24267353
    Sokol KC, Amar NK, Starkey J, Grant JA: Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol. 2013 Dec;111(6):433-6. doi: 10.1016/j.anai.2013.10.003. Epub 2013 Oct 25.
  • PMID: 6113023
    Jeffreys DB, Volans GN: Ketotifen overdose: surveillance of the toxicity of a new drug. Br Med J (Clin Res Ed). 1981 May 30;282(6278):1755-6. doi: 10.1136/bmj.282.6278.1755.
  • PMID: 2226222
    Grant SM, Goa KL, Fitton A, Sorkin EM: Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders. Drugs. 1990 Sep;40(3):412-48. doi: 10.2165/00003495-199040030-00006.

Contoh Produk & Brand

Produk: 126 • International brands: 2
Produk
  • Alaway
    Solution / drops • 0.25 mg/1mL • Ophthalmic • US • OTC • Approved
  • Alaway
    Solution • - • Ophthalmic • US • OTC • Approved
  • Alaway
    Solution • - • Ophthalmic • US • OTC • Approved
  • Alaway Preservative Free
    Solution / drops • 0.35 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • Allergy Eye
    Solution / drops • 0.25 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • Allergy Eye
    Solution / drops • 0.25 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • Allergy Eye Drops
    Solution / drops • 0.35 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
  • Allergy Eye Drops
    Solution / drops • 0.35 mg/1mL • Ophthalmic • US • Generic • OTC • Approved
Menampilkan 8 dari 126 produk.
International Brands
  • Totifen — Patron
  • Zasten — Novartis

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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