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Animal studies showed that these compounds lowered blood glucose levels. Some less toxic derivatives, synthalin A and synthalin B, were used for diabetes treatment, but after the discovery of insulin, their use declined. Biguanides were reintroduced into Type 2 diabetes treatment in the late 1950s.
Phenformin is an antidiabetic drug from the biguanide class. It was marketed as DBI by Ciba-Geigy, but was withdrawn from most markets in the late 1970s due to a high risk of lactic acidosis, which was fatal in 50% of cases. Phenformin was developed in 1957 by Ungar, Freedman and Seymour Shapiro, working for the U.S. Vitamin Corporation ...
High blood lactic acid level is a concern if the medication is used in overly large doses or prescribed in people with severe kidney problems. [ 23 ] [ 24 ] Metformin is a biguanide anti- hyperglycemic agent. [ 16 ]
Even less safe are drugs such as digoxin, a cardiac glycoside; its therapeutic index is approximately 2:1. [12] Other examples of drugs with a narrow therapeutic range, which may require drug monitoring both to achieve therapeutic levels and to minimize toxicity, include dimercaprol, theophylline, warfarin and lithium carbonate.
The ED50 is commonly used as a measure of the reasonable expectancy of a drug effect, but does not necessarily represent the dose that a clinician might use. This depends on the need for the effect, and also the toxicity. The toxicity and even the lethality of a drug can be quantified by the TD 50 and LD 50 respectively. Ideally, the effective ...
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Structure of chlorhexidine, a bisbiguanide antiseptic.. Bisbiguanides are a class of chemically related compounds known for their bactericidal properties. Generally considered to be of the generic formula: R 1 R 2 N.C(:NR 6)NH.C(:NH)NH.CH 2 X--(CH 2) 3 NH.C(:NH)NH.C(:NR 7)NR 3 R 4 V. [1] These compounds include the antiseptics chlorhexidine and alexidine.