Peringatan Keamanan

The LD50 of diosmin is >3g/kg in animal studies, with an LD50 of great than 3000 mg/kg in rats.A233150 No cases of overdose have been reported, however, an overdose is likely to result in gastrointestinal effects such as nausea, dyspepsia, vomiting, and diarrhea.L33040

Diosmin

DB08995

small molecule approved investigational

Deskripsi

Chronic venous insufficiency is a common condition the western population. Compression and pharmacotherapy are frequently used to manage chronic venous insufficiency, improving circulation and symptoms of venous disease.A232885

Diosmin is a bioflavonoid isolated from various plants or synthesized from hesperidin. It is used for the improvement of capillary fragility or venous insufficiency, including chronic venous insufficiency (CVI) and hemorrhoids. Diosmin is widely available over-the-counter and demonstrates a favourable a favorable safety profile.A232890,T840,L33040

Struktur Molekul 2D

Berat 608.5447
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Diosmin half-life ranges from 26 to 43 hours.[A232473] One study using a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method after a single 900 mg dose of diosmin demonstrated a half-life of 60.2±85.7 hours in healthy volunteers.[A233150]
Volume Distribusi A pharmacokinetic study of 5 adults revealed a volume of distribution of 62.1±7.9 L.[L32848]
Klirens (Clearance) -

Absorpsi

Diosmin is rapidly absorbed in the gastrointestinal tract.A232473 After a 900 mg single oral dose in a study using liquid chromatography with tandem mass spectrometry (LC-MS/MS) method, Cmax was 4.2±3.8 ng·mL-1, Tmax was 18.7±9.9 hours, and AUC0~96 was 185.4±166.2 ng·mL-1 in healthy volunteers.A233150 Another pharmacokinetic study of 5 adults revealed a Cmax of 417±94.1 ng/dL.L32848

Metabolisme

Degradation products of diosmin such as alkyl-phenolic acids confirm a metabolic pattern similar to that of other flavonoids.A232473

Rute Eliminasi

Pharmacokinetic data show absence of urinary elimination for diosmin and its aglycone diosmetin. Minor metabolites are found to be eliminated in the urine as glucuronic acid conjugates.A232473

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

456 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Diosmin.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Diosmin.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Diosmin.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Diosmin.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Diosmin.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Diosmin.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Diosmin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Diosmin.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Diosmin.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Diosmin.
Silodosin The excretion of Silodosin can be decreased when combined with Diosmin.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Diosmin.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Diosmin.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Diosmin.
Vincristine The excretion of Vincristine can be decreased when combined with Diosmin.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Diosmin.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Diosmin.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Diosmin.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Diosmin.
Morphine The serum concentration of Morphine can be increased when it is combined with Diosmin.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Diosmin.
Clobazam The serum concentration of Clobazam can be increased when it is combined with Diosmin.
Mefloquine The serum concentration of Mefloquine can be increased when it is combined with Diosmin.
Quinine The serum concentration of Quinine can be increased when it is combined with Diosmin.
Toremifene The serum concentration of Toremifene can be increased when it is combined with Diosmin.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Diosmin.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Diosmin.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Diosmin.
Loperamide The excretion of Loperamide can be decreased when combined with Diosmin.
Vardenafil The serum concentration of Vardenafil can be increased when it is combined with Diosmin.
Clomifene The serum concentration of Clomifene can be increased when it is combined with Diosmin.
Tipranavir The serum concentration of Tipranavir can be increased when it is combined with Diosmin.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Diosmin.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Diosmin.
Saquinavir The serum concentration of Saquinavir can be increased when it is combined with Diosmin.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Diosmin.
Posaconazole The serum concentration of Posaconazole can be increased when it is combined with Diosmin.
Darunavir The serum concentration of Darunavir can be increased when it is combined with Diosmin.
Paliperidone The serum concentration of Paliperidone can be increased when it is combined with Diosmin.
Mibefradil The serum concentration of Mibefradil can be increased when it is combined with Diosmin.
Belinostat The serum concentration of Belinostat can be increased when it is combined with Diosmin.
Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Diosmin.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Diosmin.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Diosmin.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Diosmin.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Diosmin.
Cethromycin The serum concentration of Cethromycin can be increased when it is combined with Diosmin.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Diosmin.
Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Diosmin.
Ticagrelor The serum concentration of Ticagrelor can be increased when it is combined with Diosmin.
Linagliptin The serum concentration of Linagliptin can be increased when it is combined with Diosmin.
Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Diosmin.
Canagliflozin The serum concentration of Canagliflozin can be increased when it is combined with Diosmin.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Diosmin.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Diosmin.
Umeclidinium The serum concentration of Umeclidinium can be increased when it is combined with Diosmin.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Diosmin.
Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Diosmin.
Technetium Tc-99m sestamibi The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Diosmin.
Dasabuvir The serum concentration of Dasabuvir can be increased when it is combined with Diosmin.
Methylene blue The serum concentration of Methylene blue can be increased when it is combined with Diosmin.
Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Diosmin.
Paritaprevir The serum concentration of Paritaprevir can be increased when it is combined with Diosmin.
Selexipag The serum concentration of Selexipag can be increased when it is combined with Diosmin.
Elbasvir The serum concentration of Elbasvir can be increased when it is combined with Diosmin.
Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Diosmin.
Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Diosmin.
Tucatinib The serum concentration of Tucatinib can be increased when it is combined with Diosmin.
Selumetinib The serum concentration of Selumetinib can be increased when it is combined with Diosmin.
Voclosporin The serum concentration of Voclosporin can be increased when it is combined with Diosmin.
Tezacaftor The serum concentration of Tezacaftor can be increased when it is combined with Diosmin.
Lasmiditan The serum concentration of Lasmiditan can be increased when it is combined with Diosmin.
Talinolol The serum concentration of Talinolol can be increased when it is combined with Diosmin.
Fostemsavir The serum concentration of Fostemsavir can be increased when it is combined with Diosmin.
Revefenacin The serum concentration of Revefenacin can be increased when it is combined with Diosmin.
Valspodar The serum concentration of Valspodar can be increased when it is combined with Diosmin.
Lemborexant The serum concentration of Lemborexant can be increased when it is combined with Diosmin.
Duvelisib The serum concentration of Duvelisib can be increased when it is combined with Diosmin.
Glasdegib The serum concentration of Glasdegib can be increased when it is combined with Diosmin.
Elagolix The serum concentration of Elagolix can be increased when it is combined with Diosmin.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Diosmin.
Gilteritinib The serum concentration of Gilteritinib can be increased when it is combined with Diosmin.
Omadacycline The serum concentration of Omadacycline can be increased when it is combined with Diosmin.
Fedratinib The serum concentration of Fedratinib can be increased when it is combined with Diosmin.
Grapiprant The serum concentration of Grapiprant can be increased when it is combined with Diosmin.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Diosmin.
Darolutamide The serum concentration of Darolutamide can be increased when it is combined with Diosmin.
Enfortumab vedotin The serum concentration of Enfortumab vedotin can be increased when it is combined with Diosmin.
Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Diosmin.
Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Diosmin.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Diosmin.
Tenofovir The serum concentration of Tenofovir can be increased when it is combined with Diosmin.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Diosmin.
Ripretinib The serum concentration of Ripretinib can be increased when it is combined with Diosmin.
Trilaciclib The serum concentration of Trilaciclib can be increased when it is combined with Diosmin.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Diosmin.
Daptomycin The serum concentration of Daptomycin can be increased when it is combined with Diosmin.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Diosmin.
Tivozanib The serum concentration of Tivozanib can be increased when it is combined with Diosmin.
Loncastuximab tesirine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Diosmin.

Target Protein

Aryl hydrocarbon receptor AHR

Referensi & Sumber

Synthesis reference: Rajiv Sakhardande, Manmohan Nimbalkar, Navin Khatri, Subarao Patil, Santosh Bhalekar, Rajendra Patil, Pandharinath Firake (2011). Process for the preparation of diosmin (WO2010092592A2).IFI CLAIMS PATENT SERVICES.https://patents.google.com/patent/WO2010092592A2/en
Artikel (PubMed)
  • PMID: 30228853
    Feldo M, Wozniak M, Wojciak-Kosior M, Sowa I, Kot-Wasik A, Aszyk J, Bogucki J, Zubilewicz T, Bogucka-Kocka A: Influence of Diosmin Treatment on the Level of Oxidative Stress Markers in Patients with Chronic Venous Insufficiency. Oxid Med Cell Longev. 2018 Aug 28;2018:2561705. doi: 10.1155/2018/2561705. eCollection 2018.
  • PMID: 1551741
    Cova D, De Angelis L, Giavarini F, Palladini G, Perego R: Pharmacokinetics and metabolism of oral diosmin in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1992 Jan;30(1):29-33.
  • PMID: 31547271
    Feldo M, Wojciak-Kosior M, Sowa I, Kocki J, Bogucki J, Zubilewicz T, Kesik J, Bogucka-Kocka A: Effect of Diosmin Administration in Patients with Chronic Venous Disorders on Selected Factors Affecting Angiogenesis. Molecules. 2019 Sep 12;24(18). pii: molecules24183316. doi: 10.3390/molecules24183316.
  • PMID: 23886889
    Barreca D, Lagana G, Bruno G, Magazu S, Bellocco E: Diosmin binding to human serum albumin and its preventive action against degradation due to oxidative injuries. Biochimie. 2013 Nov;95(11):2042-9. doi: 10.1016/j.biochi.2013.07.014. Epub 2013 Jul 22.
  • PMID: -
    Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods.
  • PMID: 31487997
    Sliva J: Diosmin - still an important modality in the treatment of venous insufficiency. Vnitr Lek. 2019 Summer;65(7-8):524-526.
  • PMID: 24934505
    Milano G, Leone S, Fucile C, Zuccoli ML, Stimamiglio A, Martelli A, Mattioli F: Uncommon serum creatine phosphokinase and lactic dehydrogenase increase during diosmin therapy: two case reports. J Med Case Rep. 2014 Jun 16;8:194. doi: 10.1186/1752-1947-8-194.
  • PMID: 30203575
    Boisnic S, Branchet MC, Gouhier-Kodas C, Verriere F, Jabbour V: Anti-inflammatory and antiradical effects of a 2% diosmin cream in a human skin organ culture as model. J Cosmet Dermatol. 2018 Oct;17(5):848-854. doi: 10.1111/jocd.12778. Epub 2018 Sep 10.
Menampilkan 8 dari 15 artikel.
Textbook
  • ISBN: 978-0-12-813822-9
    Ronald Watson, Victor Preedy (2019). Bioactive Food as Dietary Interventions for Diabetes (2nd ed.). Academic Press.

Contoh Produk & Brand

Produk: 5 • International brands: 12
Produk
  • Analpram Advanced
    Kit • - • Oral; Topical • US
  • Analpram Advanced
    Kit • - • Oral; Topical • US
  • Analpram Advanced
    Kit • - • Topical • US
  • Bruselix Bruising
    Tablet • - • Oral • US
  • Vasculera
    Tablet • - • Oral • US
International Brands
  • Barosmin
  • Dalfon — Servier
  • Detralex
  • Diosven
  • Dioven
  • Diovenor
  • Flebosmil
  • Flebosten
  • Insuven
  • Litosmil

Sekuens Gen/Protein (FASTA)

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