Berlithion 600mg, 30 capsules — Made in Germany — Free Delivery

Pharmacological properties

Pharmacodynamics. Thioctic acid is a vitamin-like substance that is formed in the body and acts as a coenzyme during the oxidative decarboxylation of α-keto acids. Hyperglycemia caused by diabetes mellitus leads to the deposition of glucose on the matrix proteins of blood vessels and the formation of the so-called end products of progressive glycosylation. this process leads to a decrease in endoneural blood flow and endoneural hypoxia / ischemia, which is associated with an increased production of free oxygen radicals that damage peripheral nerves. depletion of the antioxidant glutathione in peripheral nerves has also been noted.

In studies on rats, thioctic acid influenced the biochemical process caused by diabetes mellitus, which was triggered by streptozocin, which reduced the formation of advanced glycosylation end products, improved endoneural blood flow, increased the physiological content of the antioxidant glutathione, which acts in the diabetic nerve affected by the diabetic process, similar to the antioxidant action against free oxygen radicals. These effects are indicative of the ability of thioctic acid to improve peripheral nerve function. This applies to sensory disturbances in diabetic polyneuropathy, which can manifest as dysesthesias and paresthesias, such as, for example, a burning sensation, pain, a feeling of numbness or crawling creeps.

In 1995, a multicenter, placebo-controlled study of the efficacy of thioctic acid for the symptomatic treatment of diabetic polyneuropathy was conducted, in which data on the beneficial effect of thioctic acid on such studied symptoms as burning, paresthesia, numbness and pain were obtained.

Pharmacokinetics. After oral administration, thioctic acid is rapidly absorbed. As a result of significant presystemic metabolism, the absolute bioavailability (in comparison with intravenous administration) of thioctic acid, which is taken orally, is approximately 20%. Due to the rapid distribution in tissues, T½ of thioctic acid in blood plasma is approximately 25 minutes. The relative bioavailability of thioctic acid for oral administration of solid dosage forms is more than 60% in proportion to the drinking solution. Cmax in blood plasma - about 4 μg / ml - was measured 30 minutes after oral administration of 600 mg of thioctic acid. In experiments on animals (rats, dogs), using a radioactive label, it was possible to reveal the predominant excretion by the kidneys (80–90%), namely, in the form of metabolites. In humans, only a small amount of the excreted intact substance is also detected in the urine. Biotransformation occurs mainly through side chain oxidation (β-oxidation) and / or by S-methylation of the corresponding thiols.

Thioctic acid interacts in vitro with ionic metal complexes (for example, with cisplatin). Thioctic acid forms poorly soluble complex compounds with sugar molecules.

Indications

Paresthesia in diabetic polyneuropathy.

Application

Adults. the daily dose is 1 capsule Berlithion 600 capsules (equivalent to 600 mg of thioctic acid), which should be taken as a single dose approximately 30 minutes before the first meal. with intensive paresthesias, treatment with thioctic acid infusion therapy can be started.

Mode of application. Capsules of the preparation Berlithion capsules should be taken on an empty stomach, swallowed whole and washed down with a sufficient amount of liquid. Simultaneous food intake can hinder absorption, therefore, for patients who are characterized by a long time for gastric emptying, it is especially important that the preparation is used half an hour before breakfast. Since diabetic polyneuropathy is a chronic condition, long-term therapy may be necessary. The mainstay of treatment for diabetic polyneuropathy is optimal diabetic control.

Berlithion 600 capsules is not intended for the treatment of children and adolescents due to lack of clinical experience.

Contraindications

Hypersensitivity to thioctic acid or other components of the preparation.

Side effects

To assess the frequency of side effects, the following classification was used: very often ≥1 / 10; often ≥1 / 100-1 / 10; infrequently ≥1 / 1000-1 / 100; rarely ≥1 / 10,000–1 / 1000; very rarely 1 / 10,000; unknown - cannot be estimated based on available data.

Immune system disorders: very rarely - allergic reactions, including skin rashes, hives (urticaria), itching, shortness of breath; unknown - autoimmune insulin syndrome (AIS) (see SPECIAL INSTRUCTIONS), eczema.

Metabolic and nutritional disorders: very rarely - hypoglycemia.

Nervous system disorders: often - dizziness; very rarely - dysgeusia, headache, hyperhidrosis.

Violations of the organ of vision: very rarely - visual impairment.

Digestive tract disorders: often - nausea; very rarely - vomiting, gastrointestinal pain, diarrhea.

General disorders: very rarely - a decrease in blood glucose levels, which is associated with an improvement in glucose absorption. Symptoms similar to hypoglycemic symptoms include dizziness, increased sweating, headache, and blurred vision.

Suspected adverse reactions reported. Reports of suspected adverse reactions following preparation registration are important. This allows you to continue monitoring the benefit / risk ratio of the preparation. Health professionals are asked to report any suspected adverse reactions.

Special instructions

The main factor in the effective treatment of diabetic polyneuropathy is the optimal correction of the patient's blood glucose level. at the beginning of the treatment of polyneuropathy due to regeneration processes, a short-term increase in paresthesia with a feeling of "creeping" is possible. when using thioctic acid in patients with diabetes mellitus, frequent monitoring of blood glucose levels is necessary. in some cases, it is necessary to reduce the dose of antidiabetic preparations in order to prevent the development of hypoglycemia.

Berlithion 600 capsules contain sorbitol, so they should not be used in patients with such a rare hereditary disease as fructose intolerance.

One case of AIS has been reported with thioctic acid treatment. Patients with a specific genotype for HLA (Human Leukocyte Antigen System), such as the HLA-DRB1 * 04: 06 and HLA-DRB1 * 04: 03 alleles, are more likely to develop AIS when treated with thioctic acid. The HLA-DRB1 * 04: 03 allele (the ratio of the possible propensity to AIS is 1.6) is predominantly common among representatives of the Caucasian race, in addition, the prevalence in southern Europe is greater than in northern Europe. Allele HLA-DRB1 * 04: 06 (the ratio relative to the possible propensity to AIS - 56.6) is predominantly common among patients in Japan and Korea. The possibility of developing AIS in patients taking thioctic acid should be taken into account, with a differential diagnosis of spontaneous hypoglycemia (see SIDE EFFECTS).

Use during pregnancy and lactation

Fertility Reproductive toxicity studies have not found any evidence of an effect on fertility.

Pregnancy. The preparation should be used during pregnancy only after a careful assessment of the benefit / risk ratio.

Lactation. There are no data on the penetration of thioctic acid or its metabolites into breast milk. A decision should be made whether to stop breastfeeding or to discontinue the preparation, taking into account the benefits of breastfeeding for the baby and the benefits of therapy for the woman.

The ability to influence the reaction rate when driving or operating other mechanisms. During treatment, care must be taken when driving vehicles, working with mechanisms or engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, due to the possibility of adverse reactions such as hypoglycemia, dizziness and visual impairment.

Interactions

The effectiveness of cisplatin decreases with simultaneous treatment with thioctic acid.

Thioctic acid is a metal chelator and therefore, according to the basic principles of pharmacotherapy, it should not be used simultaneously with metal compounds (for example, with food additives containing iron, magnesium, or dairy products, since they contain calcium). If the total daily dose of the preparation Berlithion is used 30 minutes before breakfast, then food supplements containing iron and magnesium can be taken in the afternoon or evening.

It is possible to enhance the glucose-lowering effect of insulin or oral antidiabetic agents, therefore, especially at the initial stage of treatment with thioctic acid, careful monitoring of blood glucose levels is shown. In some cases, it may be necessary to reduce the dose of insulin or an oral antidiabetic agent to avoid symptoms of hypoglycemia.

Regular consumption of alcoholic beverages is a significant risk factor for the development and progression of the clinical picture of neuropathy and, thus, can also interfere with the effectiveness of treatment with the preparation Berlithion. Therefore, patients with diabetic polyneuropathy are strongly advised to stop drinking alcohol. This also applies to periods when therapy is not carried out.

Overdose

Overdose may cause nausea, vomiting, and headache. after accidental ingestion or attempted suicide with oral administration of thioctic acid in doses of 10–40 g in combination with alcohol, significant intoxication occurred, in some cases with a lethal outcome. the clinical picture of poisoning is initially manifested by psychomotor agitation or impaired consciousness, and in the future its course is accompanied by attacks of generalized seizures and the development of lactic acidosis. in addition, hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation syndrome, bone marrow suppression and multiple organ failure have been described in cases of intoxication with high doses of thioctic acid.

Treatment. Even if severe preparation intoxication is suspected (for example, taking more than 10 capsules of 600 mg for adults or a dose of more than 50 mg / kg of body weight in children), immediate hospitalization is recommended and taking measures in accordance with general principles in case of accidental poisoning (for example, induction of vomiting, washing stomach, intake of activated carbon). Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication should be carried out in accordance with the principles of modern intensive care and carried out symptomatically. To date, the expediency of using hemodialysis, hemoperfusion or filtration methods within the framework of the forced withdrawal of thioctic acid has not been confirmed.

Storage conditions

Store at a temperature not exceeding 25 ° c.