Properties
What is it?
DETRALEX® 1000mg 1. Name of the medicinal product DETRALEX 1000mg, film-coated tablet 2. Qualitative and quantitative composition Micronized purified flavonoid fraction ............................ 1000,000 mg, consisting of: Diosmin 90%.................................................................................................. 900,000 mg Flavonoids in the form of hesperidin: 10% ................................................... 100,000 mg Average mass fraction of impurities............................................................................ 40,000 mg Information about one film-coated tablet For a full list of excipients, see section 6.1. See also: TURBO MICRON - TURBO MICRON G 500mg 60 tablets GMP 3. Pharmaceutical form Film-coated tablet. The score line is for facilitating the ingestion of the tablet and not for dividing it into equal doses. 4. Clinical particulars 4.1. Therapeutic indications Treatment of symptoms related to veno-lymphatic insufficiency (feeling of heaviness in the legs, pain, morning syndrome of tired legs) Treatment of functional symptoms associated with acute hemorrhoidal attack 4.2. Posology and method of administration Usual dosage: 1 tablet per day, preferably in the morning with meals. Hemorrhoidal attack: 3 tablets per day for the first 4 days, then 2 tablets per day for 3 days. DETRALEX — how to take the drug for hemorrhoids, see the blog. 4.3. Contraindications Hypersensitivity to the active substance or to any of the excipients (listed in section 6.1). 4.4. Special warnings and precautions for use When taking the product, taking this product for symptomatic treatment of acute hemorrhoids does not exclude the need for treatment of other anal diseases. If symptoms do not disappear quickly, a proctological examination and review of treatment are necessary. 4.5. Interactions with other medicinal products and other forms of interaction Drug interaction studies have not been conducted, and no clinically significant drug interactions have been described to date in the post-marketing period. 4.6. Fertility, pregnancy and lactation Pregnancy Data on the use of micronized purified flavonoid fraction in pregnant women are limited or absent. Animal studies have not revealed reproductive toxicity (see paragraph 5.3). For safety reasons, it is not recommended to use DETRALEX during pregnancy. Lactation It is unknown whether the active substance or its metabolites are excreted in breast milk. The risk to newborns and infants cannot be excluded. The decision to discontinue breastfeeding or to discontinue/not start treatment with DETRALEX should be made taking into account the benefits of breastfeeding for the child and the benefits of therapy for the woman. Fertility Reproductive system toxicity studies have not revealed any effects on the fertility of male and female rats (see section 5.3). 4.7. Effects on ability to drive and use machines Studies on the effect of flavonoid fraction on the ability to drive vehicles and operate machinery have not been conducted. Nevertheless, based on the overall safety profile of the flavonoid fraction, DETRALEX has no effect or a very negligible effect on this ability. 4.8. Undesirable effects Brief description of the safety profile of the product Adverse effects observed during clinical trials of DETRALEX were mild. Adverse effects are mainly related to gastrointestinal events (diarrhea, dyspepsia, nausea, vomiting). Table of adverse reactions The following adverse effects and events are described with the following frequencies: very common (≥1/10); common (≥1/100 - <1/10); uncommon (≥1/1,000 - <1/100); rare (≥1/10,000 - <1/1,000); very rare (<1/10,000), frequency unknown (cannot be estimated from available data) Organ system class | Frequency | Preferred term -------------------|-----------|---------------- Nervous system disorders | Rare | Dizziness, Headache, Asthenia Gastrointestinal disorders | Common | Diarrhea, Dyspepsia, Nausea, Vomiting | Uncommon | Colitis | Frequency unknown* | Abdominal pain Skin and subcutaneous tissue disorders | Rare | Pruritus, Rash, Urticaria | Frequency unknown* | Isolated swelling of the face, lips, eyelids. In very rare cases - angioedema. * Post-marketing use experience 4.9. Overdose Symptoms Data on overdose of DETRALEX are limited. The most frequent adverse reactions in case of overdose were gastrointestinal disorders (diarrhea, nausea, abdominal pain) and skin disorders (pruritus, rash). Treatment Symptomatic treatment is carried out in case of overdose. 5. Pharmacological properties 5.1. Pharmacodynamic properties Pharmacotherapeutic group: Venotonic and angioprotective agents, ATC code: C05CA53 Pharmacology: DETRALEX acts on the cardiovascular system: o At the venous level, it reduces venous distensibility and venous congestion; o At the microcirculation level, it normalizes capillary permeability and increases their resistance. Clinical pharmacology: In double-blind, controlled studies using objective quantitative methods to study the effect of the drug on venous hemodynamics, the pharmacological properties of the drug in humans have been confirmed. o Dose-effect relationship: A statistically significant relationship between dose and effect was shown for the following parameters of venous plethysmography: volume, distension, and emptying time. The best dose-effect relationship is achieved with 2 tablets. o Venotonic activity: The drug increases venous tone: venous occlusion plethysmography, performed with a mercury tensometric recorder, showed a decrease in venous emptying time. o Microcirculatory activity: Double-blind, controlled studies showed a statistically significant difference between the given drug and placebo. In patients with signs of capillary fragility, treatment increases capillary resistance, as confirmed by the angiosteriometry method. In clinical practice: Double-blind, placebo-controlled studies have shown the therapeutic activity of the drug in phlebology for chronic functional and organic venous insufficiency of the lower extremities. 5.2. Pharmacokinetic properties After oral administration of the 14C-labeled diosmin in humans: - The drug is mainly excreted in the feces: excretion in urine accounts for an average of 14% of the administered dose. - The half-life is 11 hours. - The drug is actively involved in metabolism, as evidenced by the presence of various phenolic acids in urine. 5.3. Preclinical safety data No toxicity or lethal effects, as well as behavioral, biological, anatomical, or histological disorders, were observed in mice, rats, and monkeys after single or short-term and regular long-term oral administration of high doses. Studies in rats and rabbits did not reveal embryotoxicity or teratogenic effects. Fertility properties are not altered. No mutagenic potential was detected in in-vitro and in-vivo studies. 6. Pharmaceutical properties 6.1. List of excipients Sodium starch glycolate, microcrystalline cellulose, gelatin, magnesium stearate, talc. Film coating: titanium dioxide (E 171), glycerol, sodium lauryl sulfate, macrogol 6000, hypromellose, iron oxide yellow (E 172), iron oxide red (E 172), magnesium stearate. 6.2. Incompatibilities Unknown 6.3. Shelf life 4 years. 6.4. Special precautions for storage Store at a temperature not exceeding +30°C. 6.5. Description of the packaging and its contents 18, 30, 60 film-coated tablets in blister packs (PVC and aluminum). Not all pack sizes may be marketed. 6.6. Special precautions for disposal and use There are no special requirements for disposal and use. Dispensing category: Pharmaceutical product group III, available without a prescription.