What is Diosmin Hesperidin in English?
Diosmin and hesperidin are citrus-derived flavonoid compounds used primarily for treating venous disorders, with diosmin being a flavone glycoside that is often semi-synthetically produced from hesperidin, a flavanone naturally abundant in citrus fruits. 1, 2
Chemical Identity and Source
Diosmin is chemically described as 7-[[6-O-(6-Deoxy-α-L-mannopyranosyl)-ß-D-glucopyranosyl]oxy]-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-4H-1-benzopyran-4-one, with molecular formula C28H32O15 and molecular weight 608.5 1
Hesperidin is a naturally occurring flavanone glycoside found in citrus rinds that serves as the precursor for pharmaceutical diosmin production 2, 3
Both compounds are flavonoids—phytochemicals extracted from citrus fruits—with diosmin often obtained through semi-synthetic conversion of hesperidin 4, 5
Pharmaceutical Formulations
Micronized Purified Flavonoid Fraction (MPFF) is the most studied preparation, containing 90% diosmin and 10% hesperidin (9:1 ratio), marketed as Daflon® 4, 2
Pure diosmin formulations contain 600 mg of diosmin glycoside per tablet, often combined with alkaline compounds (alka4-complex) to manage blood pH 1
The micronization process reduces particle size to enhance absorption, though clinical studies show 600 mg of non-micronized diosmin achieves equivalent efficacy to 1000 mg of MPFF 3
Primary Clinical Uses
Chronic venous disorders (CVD): Both compounds manage venous inflammation, reduce polymorphonuclear leukocyte accumulation, and decrease edema caused by deteriorating venous vessel walls 1, 4
Hemorrhoidal disease: MPFF received the highest recommendation (1B) in guidelines for treating hemorrhoids, with significant improvement in discomfort, bleeding, and edema within 7 days 1, 4
Venous ulcers: Treatment with diosmin plus standard compression therapy increases ulcer resolution rates (70% for ulcers <3 cm vs 50% with standard care alone) and reduces time to healing 1
Mechanism of Action
After oral administration, diosmin is converted to diosmetin in the intestine, which is absorbed and subsequently esterified into glucuronide conjugates for urinary excretion 2
The compounds contain flavonoids (including hesperidin and hesperetin) that can decrease activity of cytochrome P450 3A4 (CYP3A4) and other metabolic enzymes 6, 2
Diosmin demonstrates anti-inflammatory, antioxidant, antidiabetic, and antifibrotic effects through multiple pathways including glycation inhibition 6, 2
Important Drug Interactions
Grapefruit juice effects: While hesperidin may increase bioavailability of drugs like diltiazem through CYP450 3A4 inhibition, this has not been specifically attributed to the diosmin-hesperidin combination 1
Metabolic enzyme inhibition: Diosmin significantly delays half-life and increases AUC of chlorzoxazone (CYP2E1 substrate), diclofenac, and metronidazole (both CYP2C9 substrates) 1
No evidence of drug incompatibility has been observed when combined with drugs for various clinical disorders, though caution is warranted given the metabolic enzyme effects 1
Safety Profile
Both compounds are Generally Recognized as Safe (GRAS) by FDA standards and demonstrate favorable safety profiles in toxicological studies 1, 2
Adverse effects are typically mild, including gastrointestinal disturbances such as nausea and vomiting, with few serious reactions reported in clinical trials 3
The formulations are suitable for vegans and do not contain common allergens (fructose, glucose, lactose, gluten, tree nuts, peanuts) 1