Pharmacology/ Pharmacokinetics:
Pharmacodynamics-
Benfotiame increases transketolase activity by increasing the tissue levels of
thiamine diphosphate, prevents the increased UDP- N-acetylglucosamine and
enhances hexosamine pathway activity which is responsible for preventing the
formation of AGEs. Bentofamine normalizes protein kinase activity and prevents
neuclear factor kappaB activation in the retina of diabetes
Potential mechanisms of metformin includes of the myochondrial chain
(complex I), activation of adenosine monophosphate -activated protein kinase
(AMP-K) inhibion of glucogon induced elevation of cyclic adenosine
monophasphate and consequent activation of protein kinase A, inhibition
of mitochondrial glycophosphate dehydrogenase
Pharmocokinetics-
Bentioamine is a lipid -soluble thiamine with higher bioavailability.
Benfotiamine is absorbed via diffusion through the intestinal mucosa.
oral administration acheives higher plasma levels and also
concentrations are maintained for longer time in blood and tissues.
Rationale for Combination-
There is always a need to switch on for combinational therapy in order
to control and reduce the complications of DM which are threatening
and reduces the survival rates in DM patients.
Metformin reduces the elevated glucose levels and benfotamine targets in
reducing AGEs which makes the combination of these two molecules to be
efficacious in treatment of DM.
Metformin is a hydrophyillic molecule that is actively transported
via organic cation transporters in the intestine, liver and kidney
Metformin has a bioavailability of 50-60% under fasting conditions
and is absorbed slowly.Peak plasma concentrations are reached
within 1 to 3 hours.
Metformin is not metabolised and is excreted unchanged in the urine,
with a half-life of about 5 hours
Manufacturer Details