Instructions Detralex 500 mg film-coated tablets No. 60
Composition
active ingredient: micronized purified flavonoid fraction (diosmin + flavonoids in the form of hesperidin);
1 tablet contains 500 mg of micronized purified flavonoid fraction, which contains 450 mg of diosmin (90%) and 50 mg of flavonoids in the form of hesperidin (10%);
excipients: gelatin, magnesium stearate, microcrystalline cellulose, sodium starch glycolate (type A), talc, purified water;
film coating: glycerol, macrogol 6000, magnesium stearate, hypromellose, red iron oxide (E 172), sodium lauryl sulfate, titanium dioxide (E 171), yellow iron oxide (E 172).
Dosage form
Film-coated tablets.
Main physicochemical properties: oval-shaped tablet, coated with an orange-pink film coating.
Pharmacotherapeutic group
Angioprotectors. Capillary stabilizing agents. Bioflavonoids. Diosmin, combinations.
ATX code C05C A53.
Pharmacological properties
Pharmacodynamics.
Pharmacology.
Detralex has a venotonic and angioprotective effect, reduces venous distensibility and venostasis, improves microcirculation, reduces capillary permeability and increases their resistance, and also improves lymphatic drainage, increasing lymphatic outflow.
Preclinical pharmacology.
An experimental study on animals using the ischemia/reperfusion model showed that the use of a micronized purified flavonoid fraction has a more pronounced effectiveness in reducing vascular wall permeability and blood plasma leakage compared to simple diosmin. This result is due to the presence of a protective effect on microcirculation of flavonoids, such as hesperidin, diosmetin, linarin and isoroifolin, which are part of the fraction in the form of hesperidin. The reduction in vascular wall permeability and blood plasma leakage observed with the use of a micronized purified flavonoid fraction is more significant than that observed with the use of simple diosmin and each component of the flavonoid fraction separately.
Clinical pharmacology.
The above pharmacological properties have been confirmed in double-blind, placebo-controlled studies using methods that can determine the effect of the drug on venous hemodynamics.
The dose-effect relationship.
A statistically significant dose-dependent effect of the drug was established according to the following venous plethysmographic parameters: venous volume, venous distensibility and venous outflow time. The optimal dose-effect ratio was achieved when taking 2 tablets.
Venotonic activity.
Detralex increases venous tone: a decrease in venous outflow time was demonstrated using venous occlusion plethysmography.
Microcirculatory activity.
In double-blind, placebo-controlled studies, a statistically significant difference between the drug and placebo was demonstrated. In patients with symptoms of capillary fragility, treatment increased their resistance, which was determined by angiostereometry.
The drug also reduces the interaction of leukocytes and endothelium, leukocyte adhesion in postcapillary venules. This reduces the damaging effect of inflammatory mediators on the walls of veins and the leaflets of vein valves.
In clinical practice.
Double-blind placebo-controlled studies have shown the therapeutic activity of the drug in phlebology in the treatment of functional and organic chronic venous insufficiency of the lower extremities, as well as in proctology in the treatment of hemorrhoids.
Pharmacokinetics.
The active substance is excreted mainly in the feces. An average of 14% of the dose is excreted in the urine.
The half-life is 11 hours.
The drug is actively metabolized, as confirmed by the presence of various phenolic acids in the urine.
Indication
Symptomatic treatment of venolymphatic insufficiency (heaviness in the legs, pain, night cramps, edema, trophic disorders, including varicose ulcers).
Symptomatic treatment of hemorrhoids.
Contraindication
Hypersensitivity to the active substance or any excipient.
Interaction with other medicinal products and other types of interactions
No interaction studies have been conducted. No clinically significant drug interactions have been reported during post-marketing use of the drug to date.
Application features
The use of this medicinal product for acute hemorrhoids does not replace specific therapy and does not interfere with the treatment of other proctological diseases. If the symptoms do not disappear quickly during a short course of treatment, a proctological examination should be performed and the therapy reviewed.
In cases of venous circulation disorders, it is more effective to combine therapy with adherence to the following lifestyle recommendations:
Excipients.
Sodium level.
Detralex contains less than 1 mmol sodium (23 mg) per tablet, i.e. it is almost sodium-free.
Use during pregnancy or breastfeeding
There are no or limited data from the use of micronized purified flavonoid fraction in pregnant women.
Animal studies have not demonstrated reproductive toxicity.
As a precautionary measure, it is advisable to avoid using the drug during pregnancy.
Breast-feeding.
It is not known whether the active substance or its metabolites pass into breast milk.
A risk to newborns/infants cannot be excluded.
A decision on whether to discontinue breast-feeding or to discontinue/abstain from therapy with this medicinal product should be made taking into account the benefit of breast-feeding for the child and the benefit of therapy for the mother.
Fertility.
Reproductive toxicity studies in animals showed no effect on fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies of the effect of the flavonoid fraction on the ability to drive or operate other mechanisms have not been conducted. However, in accordance with the general safety profile of the flavonoid fraction, Detralex does not affect or has a negligible effect on this ability. In case of detection of side effects of the drug (see section "Adverse reactions"), caution should be exercised.
Method of administration and doses
For oral use.
It is intended for adults.
Venolymphatic insufficiency.
The recommended dose is 2 tablets per day: 1 tablet in the afternoon and 1 tablet in the evening with meals. After a week of use, you can take 2 tablets per day once with meals.
The usual recommended duration of treatment is up to 3 months. Longer durations of treatment, 6 to 12 months, have been well tolerated in clinical studies.
Hemorrhoidal disease.
Treatment of acute hemorrhoid episodes: 6 tablets per day for 4 days, then 4 tablets per day for the next 3 days. Take with meals. Divide the daily number of tablets into 2–3 doses. Maintenance therapy - 2 tablets per day with a treatment duration of up to 3 months.
Children
There are no data on the use of Detralex in children.
Overdose
Symptoms
There is limited data on overdose with this medicinal product. The most common adverse reactions reported in overdose were gastrointestinal reactions (such as diarrhoea, nausea, abdominal pain) and skin reactions (such as pruritus, rash).
Treatment
Treatment of overdose should include therapy of clinical symptoms.
Adverse reactions
During clinical studies, moderate side effects were observed with the use of micronized purified flavonoid fraction, mainly from the gastrointestinal tract (diarrhea, dyspepsia, nausea, vomiting).
The following adverse reactions have been reported and are classified according to frequency: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (< 1/10000); frequency unknown (cannot be estimated from the available information).
Nervous system: rarely: dizziness, headache, malaise.
Gastrointestinal disorders: common: diarrhea, dyspepsia, nausea, vomiting; uncommon: colitis; frequency unknown*: abdominal pain.
Skin and subcutaneous tissue disorders: rarely: itching, rash, urticaria; frequency unknown*: isolated swelling of the face, lips, eyelids, in exceptional cases - Quincke's edema.
*Post-marketing surveillance.
Reporting of suspected adverse reactions. Reporting of suspected adverse reactions during the post-marketing period of a medicinal product is important. This allows for continuous monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions through the national reporting system.
Expiration date
4 years.
Storage conditions
Does not require any special storage conditions. Keep out of the reach of children.
Packaging.
15 tablets in a blister of aluminum foil and PVC film; 2 or 4 blisters in a cardboard box.
Vacation category
Without a prescription.
Producer
Servier Industry Laboratories/Les Laboratoires Servier Іndustrie.
Location of the manufacturer and its business address.
905 route de Saran, 45520 Gidy, France/905 route de Saran, 45520 Gidy, France.
Applicant.
LE LABORATORIES SERVIER/Les Laboratoires Servier.
Location of the applicant.
50, rue Carnot, 92284 Suresnes Сedex, France/50, rue Carnot, 92284 Suresnes Сedex, France.
For any information regarding the medicinal product, please contact Servier Ukraine LLC by phone: (044) 490 3441, fax: (044) 490 3440.
