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Biguanides administration

Aromatic biguanides such as proguanil (181) have been found useful as antimalarial agents. Investigation of the metabolism of this class of drugs revealed that the active compound was in fact the triazine produced by oxidative cyclization onto the terminal alkyl group. The very rapid excretion of the active entity means that it cannot be used as such in therapy. Consequently, treatment usually consists in administration of either the metabolic precursor or, alternately, the triazine as some very insoluble salt to provide slow but continual release of drug. [Pg.280]

The only biguanide approved by the Food and Drug Administration (FDA) and currently available in the United States is metformin. Metformin was approved in the United States in 1995, although it has been used extensively in Canada and Europe since 1959. This agent is thought to lower blood... [Pg.656]

Sitagliptin is a dipeptidylpeptidase-4 inhibitor that increases insulin secretion and lowers glucagon secretion. Sitagliptin is available for oral administration. It is indicated in patients with type 2 diabetes mellitus in combination with either metformin (biguanide) or a sulphonylurea or a thiazolidinedione. [Pg.154]

Biguanides are used as an oral drug for the management of mild to moderately severe, noninsulin-depend-ent (type II) diabetes mellitus in obese patients who are usually above 40 years of age. It is important that for the administration of this drug the disease should have adult onset. [Pg.271]

Phenformin is the only biguanide to have been marketed in the United States and removed from the market by the US Food and Drug Administration (FDA) in 1977 because of its association with the development of lactic acidosis, a metabolic aberration that results in mortality in 50-75% of cases. Ethanol intake before the administration of phenformin therapeutic doses or excessive dose appears to predispose the patient to the development of lactic acidosis with a serious outcome. Phenformin and its other relative biguanides are still sold in European and other countries worldwide. [Pg.272]

Lactic acidosis due to biguanides may be treated with judicious doses of sodium bicarbonate. Excessive bicarbonate administration may worsen intracellular acidosis. [Pg.95]


See other pages where Biguanides administration is mentioned: [Pg.80]    [Pg.168]    [Pg.1428]    [Pg.396]    [Pg.147]    [Pg.284]    [Pg.21]    [Pg.469]    [Pg.377]    [Pg.187]   
See also in sourсe #XX -- [ Pg.141 ]




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