Benfotiamine

• 6 - (4 -amino-2 -methyl-5 -pyrimidinyl )-3- benzoylthio -5 -formyl -4-methyl -5 -aza -3- hexenyl dihydrogenphosphate
• Benfotiamine
• Benfotiaminum
• Benphothiamine

A11DA03

Provitamin

Fixed

155-165 ° C (dec.)

15 g · kg -1 ( LD50, mouse, oral)

Template: Infobox chemical / molecular formula search available

Benfotiamine is a fat- soluble precursor ( prodrug ) of vitamin B1 and is rapidly cleaved in the organism to the effective vitamin B1. The fat- soluble benfotiamine is different from the water-soluble vitamin B1 in that it included a significantly higher proportion (about 5-7 times higher ) in the body ( absorbed ) is. Due to its high bioavailability is benfotiamine both the prevention and the treatment of a vitamin B1 deficiency.

• 5.1 Diabetic Neuropathy
• 5.2 Diabetic Retinopathy
• 5.3 kidney protection
• 5.4 cardioprotection

Chemical Properties

Isomerism

Benfotiamine is a compound of two because of the different possibilities of substitution at the C = C double bond isomers, fine ( E, Z)- isomers exist. These isomers differ in their chemical and physical properties and physiological effects. By a suitable synthetic strategies or separation processes can be selectively separate the individual isomers and isolate pure.

Bioavailability

At equimolar doses of 100 mg benfotiamine (about 210 micromol thiamine) thiamine mononitrate and a five-fold higher AUC and an approximately seven -fold increase in maximum plasma concentration gave, after Benfotiamingabe.

Mechanism of Action

In diabetics, various pathogenic pathways are activated by the elevated blood glucose level: the Hexosaminstoffwechselweg, the protein kinase C pathway, the formation of " advanced glycation end products " ( AGEs - advanced glycation end products ) and the Polyolstoffwechselweg. Benfotiamine inhibits this nerve and vascular damaging metabolic pathways by activating a key enzyme of glucose metabolism, the transketolase. The transketolase leads excess glucose increased the innocuous pentose phosphate pathway and thus to withdraw it, the pathogenic pathways.

Areas of application

Treatment of neuropathy ( nervous disorder ), and cardiovascular disorders, which are caused by lack of vitamin B1. Therapy or prophylaxis of clinical vitamin B1 deficiency states, where it can not be corrected nutritionally.

Studies on the therapeutic use

Diabetic Neuropathy

A consequence of disease that often occurs in diabetics, the peripheral sensory neuropathy. Due to the increased blood sugar, the nerve fibers are inter alia damage in the legs and arms. As a result, it may lead to abnormal sensations such as tingling, stinging or burning. In addition, the sentience of the affected parts of the body - mainly on the feet - completely subside. As a possible consequence, which can adjust " diabetic foot".

Some studies in diabetic patients on very low thiamine. Compared to healthy subjects, the thiamine in plasma were decreased in diabetic patients by an average of 75 percent. This deficit may be the above-mentioned pathogenic pathways and thereby promote the development and progression of diabetic complications such as neuropathy. Treatment of symptomatic diabetic polyneuropathy consists of the optimal blood glucose control and symptomatic therapy. Substitution with benfotiamine is a pathogenetically oriented therapy approach dar. efficacy and tolerability were demonstrated in some pilot studies.

Diabetic retinopathy

Diabetes is a common cause of blindness. An in vitro study from 2009 shows that benfotiamine and thiamine prevent apoptosis of pericytes. In the early stage of retinopathy benfotiamine may possibly act regulating.

Kidney protection

Adverse metabolic products ( AGEs sa ) fall increasingly also in a peritoneal dialysis treatment. They damage the peritoneum and the rest of the kidney. Characterized the duration of the dialysis treatment will be limited. In an animal study from 2011 benfotiamine protected the peritoneum and the kidneys from these harmful effects.

Heart protection

Hyperglycemia affects damaging and debilitating effect on the heart. In a study in rats benfotiamine improved the resistance of the heart cells to diabetes-related damage. Treatment with the provitamin, the survival rate of diabetic rats was significantly increased after a heart attack: benfotiamine slowed apoptosis of cardiac cells and promoted the formation of new blood vessels.

Deficiency ( hypovitaminosis )

( Similar to those of thiamine / vitamin B1)

Symptoms:

• Disorders of carbohydrate metabolism and nervous system (including polyneuropathy )
• Irritability and depression
• Drowsiness, blurred vision, loss of appetite, lack of concentration, muscle atrophy
• Anemia (anemia)
• Frequent headaches
• Memory impairment ( Korsakoff's syndrome), confusion
• Heart failure, edema, tachycardia, low blood pressure, shortness of breath ( dyspnea)
• Decreased production of antibodies in infections
• Disturbed energy production

Diseases:

• Beriberi, Wernicke's encephalopathy, Strachan syndrome