also decrease hepatic metabolism of lactate and have a negative ionotropic effect on the heart, both of which elevate lactate levels (11).
Reasonable combinations of drugs include a sulfonylurea plus metformin, a sulfonylurea plus an -glucosidase inhibitor, a sulfonylurea plus a thiazolidinedione, metformin plus repaglinide, biguanide
plus [alpha]-glucosidase inhibitor, and metformin plus a thiazolidinedione (Lin and Sun 2010).
In the early 1970s, Professor Vladimir Dilman originally developed the idea that antidiabetic biguanides
may be promising as geroprotectors and anticancer drugs ("metabolic rehabilitation").
Drugs which increase peripheral utilisation, called Biguanides
, are the preferred drugs to start with.
and thiazolidinediones (TZDs) are insulin sensitizers and enhance insulin action.
Metformin, which belongs to the class of oral antihyperglycemic agents known as the biguanides
, lowers glucose levels by decreasing hepatic glucose production and decreasing peripheral insulin resistance.
Although the exact mechanism for causing lactic acidosis is not understood, it is postulated that biguanides
induce it by inhibiting certain microsomal enzymes involved in glucose metabolism (3).
One study revealed that biguanides
, phenformin and metformin were associated with embryo death, although metformin was observed to be less toxic than phenformin in mouse whole embryo culture (8).
work by: 1) inhibiting the normal hepatic glucose output 2) interfering with intestinal absorption of glucose from ingested carbohydrates, and 3) increasing peripheral glucose uptake.
5%) of the oral antidiabetic medicines prescribed during the study period were biguanides
, followed by sulfonylureas (44.
Description: phenoxyethanol (and) benzoic acid (and) dehydroacetic acid (and) ethylhexylglycerin (and) polyaminopropyl biguanides
8) Five classes of oral hypoglycemic agents are currently available: the sulfonylureas, the nonsulfonylurea insulin secretagogues, the biguanides
, the [alpha]-glucosidase inhibitors, and the thiazolidinediones.
He notes there are several medications on the market to help control Type II diabetes, such as sulfonylureas, which help the pancreas produce more insulin; biguanides
, which lessens the amount of glucose the liver produces; and thiazolidinediones, which helps make blood cells more receptive to insulin.
Metformin belongs to a class of medicines known as biguanides
, which have been used for decades to treat type two diabetes - the form of the disease that normally affects the middle-aged or elderly.
It is thought that agents that increase the cellular AMP/ATP ratio, such as the antidiabetic biguanides
metformin and phenformin, inhibit mTORC1 through AMPK activation of TSC1/2-dependent or -independent mechanisms.