Action and mechanism
The main pharmacological effect of oxerutins is the reduction of water filtration speed and microvascular permeability to proteins. Because of their action on the vascular endothelium, with the stabilization of the endothelial membrane and consequent reduction in capillary permeability, oxerutins act clinically on edematous infiltration, pain, trophic disorders and the various pathological manifestations that characterize the picture of chronic venous insufficiency.
Pharmacokinetics
The pharmacokinetics of oxerutins has been studied in mice, rats, dogs, rhesus monkeys and humans. The progressive substitution of hydroxyl groups of the original molecule of the rutin, by hydroxyethyl groups, results in an increase of hydrosolubility, a greater resistance of the molecule to the bacterial degradation in the intestine and a decrease of its fixation to the proteins. The value of this weak and reversible fixation of oxerutins to proteins is approximately 30%. The detection of the glycosides of oxerutins and their corresponding glucuronides in urine and bile (14-20% of a dose administered to rats by mouth) shows that the compound is absorbed. There is an elevated effect of first hepatic step and enterohepatic circulation.
Elimination is mainly through the bile duct (about 65% of the eliminated molecule) and through the urine, and this excretion is practically complete between 24 and 48 hours. Oxerutins do not cross the blood-brain barrier.
After oral or intravenous administration, the passage of oxerutins through the placenta is minimal, with only traces being found in rat or mouse foetuses. Similarly, only traces of oxerutins have been found in milk from lactating rats.
In man, after oral administration of 14C-oxerutins, peak plasma concentrations are found to be between 1-9 hours, with detectable levels observed up to 120 hours after administration. The decrease in concentration occurs biexponentially. 3-6% of the radioactivity administered is excreted in the urine within 48 hours. The apparent elimination half-life varies from 10 to 25 hours, but is relatively constant for the same individual. The elimination of oxerutins by the bile duct, as well as the formation of glucuronide metabolites, has been confirmed in humans.
Indications
- [Poisonous insufficiency] mild. Treatment in adults of symptoms related to mild venous insufficiency of the lower extremities, such as pain, heavy feeling, tightness, tingling and itching in legs with varicose veins or swollen legs.
Dosage
- Adults, oral: Initial dose: 1 sachet/day. Symptom relief usually occurs within the first 2 weeks.
If you do not feel relief after 2 weeks or your symptoms worsen, you should consult your doctor. You can continue treatment for up to 2-3 months.
Rules for correct administration
Dissolve the contents of the envelope in 1 glass of water and then drink.
Contraindications
- Known hypersensitivity to any of the components
Precautions
- Special clinical monitoring should be performed in patients with [PEPTIC ULCER], [HEMORRAGY] or [TRHOMBOPENIA].
Pregnancy
There is no indication that it may have any harmful effect during pregnancy, on the fetus or on the newborn. However, women who plan to become pregnant or are in the first trimester of pregnancy should be advised to take this medication only by prescription.
Breastfeeding
No specific human data are available; discontinuation of treatment during lactation is advised.
Adverse reactions
The following adverse reactions, mainly associated with the use of the oral form, have been reported and are rare (0.01-0.1%) or very rare (<0.01%):
- Digestive: Rare: [FLATULENCE], [DIARRHEA], [GASTRALGY], gastric discomfort and [DYSPEPSY].
- Cardiovascular: Very rare: [RUBORIZATION].
- Neurological/psychological: Very rare: [CEFALEA] and [DIZZY].
- Allergic/Dermatological: Rare: [EXANTHEMATIC ERUPTIONS], [PRURITUDE] and [URTICARY]. Very rare: [ANAPHILAXY], anaphylactoid reactions and [HYPERSENSITIVE REACTIONS]. Skin reactions, the main adverse reactions described with topical use, usually disappear when treatment is stopped.
- General: Very rare: [ASTHENIA].
