Mechanism of action
It is a natural substance of the organism that has biological activity in energy metabolism at the level of the mitochondria. It works as a coenzyme in the pyruvate dehydrogenase complexes,? -Ketoglutarate dehydrogenase and in the branches of the chains of the complex of the ac?? – keto dehydrogenase complex. The deficiency of l ác. thioctic or its blockage, which occurs in various intoxications or metabolic disorders, produce pathologically high concentrations of certain degradation products, such as ketone bodies. This situation modifies the oxidative metabolism (aerobic glycolysis) in the following two ways: 1. Pyruvate, product of the degradation of hc. and certain aa. , can only be gradually integrated into the ac cycle. citric through the pyruvate dehydrogenase complex. 2. The gradual conversion of the? -Ketoglutarate dehydrogenase complex decreases the speed of all reactions of the citrus cycles preventing the functioning of the respiratory chain. AC. Thioctic is also a potent antioxidant. It can neutralize a wide variety of different free radicals which damage cells. AC. Thioctic is an important member of the antioxidant network, which consists of vit E, ascorbate and glutathione. It also has the property of regenerating some antioxidants such as glutathione.
Therapeutic indications
Thioctic acid
Tto. etiopathogenic and symptomatic of diabetic peripheral polyneuropathy (motor-sensitive).
Contraindications
Thioctic acid
Patients with known hypersensitivity to ac. thioctic or any of the components of the formulation; Children and adolescents: There is no clinical information available, it should not be used in these age groups.
Warnings and precautions
Thioctic acid
It is recommended that patients with diabetic polyneuropathy refrain from alcohol consumption, as it represents a significant risk factor for the occurrence and progression of clinical symptoms of neuropathy, and may interfere with treatment (also applies to inter- tto.); It is not compatible with sun. Glucose, sun. Ringer, sun. Hartmann, and other sun. which are known to react with thiol groups (SH) or disulfide bridges, since practically insoluble complexes are formed in combination with hc molecules .; Administer only with sun. 0.9% saline (sol. Physiological); Hypersensitivity reactions have been observed after parenteral administration, and sometimes anaphylactic shock, so patients should be carefully monitored and in the case of the appearance of the first symptoms (such as: pruritus, nausea, malaise, etc. .), the tto. should be interrupted immediately, and if appropriate therapeutic measures should be taken; after administration, an abnormal odor can be perceived in the urine, which has no clinical relevance; concomitant food consumption can reduce the absorption of ac. thioctic, therefore, it is advisable to take the full daily dose 1/2 hour before breakfast, especially in patients who show prolonged gastric emptying time; during tto. of diabetic polyneuropathy with ac. Thioctic IV can cause temporary exacerbation of symptoms due to the regeneration processes of damaged nerve fibers. If this occurs, adjuvant medications such as analgesics and in special antidepressant or neuroleptic cases should be administered according to the criteria of the attending physician.
Interactions
The therapeutic effect of cisplatin can be reduced if it is administered concomitantly; because the hypoglycemic effect of insulin or oral hypoglycemic agents can be
intensified, regular monitoring of glucose levels is recommended, particularly at the beginning of treatment, in isolated cases, it may be necessary to reduce the dose of insulin or oral hypoglycemic agents to avoid hypoglycemia symptoms; Regular alcohol consumption represents a significant risk factor for the occurrence and progression of clinical symptoms of neuropathy, and may interfere with treatment. It is recommended that patients with diabetic polyneuropathy refrain from alcohol consumption, as much as possible. (also in the periods of inter-tto.).
Pregnancy
Thioctic acid
Reproductive toxicology studies did not influence fertility or development early embryonic.
Adverse reactions
Thioctic acid
Hypersensitivity reactions, allergic skin reactions, such as hives, pruritus, eczema and rash, as well as systemic reactions and even anaphylactic shock; general disorders, after rapid IV administration, head pressure and respiratory distress have been reported, which may recur spontaneously; nervous system disorders
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