ACTION AND MECHANISM

Venotonic and vasoprotective. It produces venoconstriction, increasing vascular resistance and decreasing their permeability.

In animals, it exerts a double action on the venous return system:

- at the level of the veins and venules: increases parietal tonicity and exerts an antistatic action;

- at the microcirculation level: normalizes capillary permeability and strengthens capillary resistance.

In humans, double-blind controlled studies have confirmed venotonic activity: it increases venous tone: venous occlusion plethysmography with a mercury ring has shown a decrease in venous emptying times.

It has also demonstrated activity on microcirculation: in patients with signs of capillary fragility, it increases capillary resistance measured by angiosterometry.

SENIORS

In one study, no significant differences in adverse effects were found between geriatric and younger patients. Accepted use.

PATIENT ADVICE

- It is recommended to take the tablets after lunch and dinner.

- This medicine is intended for the short-term treatment of venous insufficiency, for periods of less than 2-3 months.

CONTRAINDICATIONS

- Hypersensitivity to diosmin or other flavonoids.

PREGNANCY

There is no evidence of any harmful effects on humans. Experimental studies have not revealed any teratogenic effects.

Extreme caution should be exercised when prescribing to pregnant women.

PHARMACOKINETICS

The pharmacokinetics of diosmin are linear.

Oral route:

- Absorption: Diosmin is rapidly transformed by the intestinal flora and absorbed in its aglycone form (diosmetin). Bioavailability: Approx. 57.9%.

- Distribution: extensive (Vd: 62.1 L).

- Metabolism: Diosmetin is rapidly and extensively degraded to phlebotonic acids or their derivatives conjugated with glycine, which are eliminated in the urine. Predominant metabolite: hydroxyphenylpropionic acid (which is eliminated mainly conjugated). Smaller metabolites: other phenolic acids corresponding to 1-hydroxy-4-methoxybenzoic acid, 3-methoxy-4-hydroxyphenylacetic acid and 3,4-dihydroxybenzoic acid.

- Elimination: Relatively rapid. In studies with radiolabeled diosmin, 34% of the dose was recovered in urine and feces after the first 24 h, and approximately 86% was recovered in urine and feces after the first 48 h.

INDICATIONS

- Short-term relief (2 to 3 months) of edema and symptoms related to chronic [VENOUS INSUFFICIENCY].

LACTATION

It is not known whether this drug is excreted in breast milk; however, minimal excretion in breast milk (1%) was observed in an animal model study. In the absence of conclusive data on its transfer into breast milk, its use during breastfeeding is not recommended.

CHILDREN

There is insufficient clinical experience in this age group. Not recommended.

RULES FOR CORRECT ADMINISTRATION

Take with meals (midday and dinner).

POSOLOGY

- Adults: Usual therapeutic dose: 2 tablets a day, divided into two doses, one tablet at midday and another at night, with meals.

- Children and adolescents < 18 years: not recommended.

- Elderly: no dosage adjustment required.

Treatment duration : 2-3 months maximum.

ADVERSE REACTIONS

Adverse effects of diosmin are generally infrequent, mild and transient.

Adverse reactions are described according to each frequency interval, considering very frequent (>10%), frequent (1-10%), unfrequent (0.1-1%), rare (0.01-0.1%), very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data).

-Digestive: frequent: [NAUSEA], [VOMITING], [DYSPEPSIA], [DIARRHEA].

-Neurological/psychological: rare: [HEADACHE], malaise, [VERTIGO].

-Allergic/dermatological: rare: [SKIN RASHES], [ITCHING], [URTICARIA].

OVERDOSE

No cases of overdose have been reported. The wide therapeutic range of this specialty means that the risk of poisoning is practically zero.