Treatment biguanides

Ghlorhexidine Gluconate. Chlorhexidine gluconate [18472-51 -0] (l,l -hexamethylene bis[5-(p-chlorophenyl) biguanide] di-D-gluconate) is used as an antimicrobial against both aerobic and anaerobic bacteria ia the oral cavity. It is used as a therapeutic supplement ia the treatment of gingivitis, periodontal disease, and dental caries. A mouth riase form is available as a 0.12 wt% aqueous solution (288). 

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. 

VI.a.2.4. Diaminopyrimidines. Pyrimethamine is a dihydrofolate reductase inhibitor, like the biguanides, and is structurally related to trimethoprim. It is seldom used alone. Pyrimethamine in fixed combinations with dapsone or sulfadoxine is used for treatment and prophylaxis of chloroquine-resistant falciparum malaria. The synergistic activities of pyrimethamine and sulfonamides are similar to those of trimethoprim/sulfonamide combinations. Resistant strains of Plasmodium falciparum have appeared world wide. Prophylaxis against falciparum... 

The lower frequency of lactic acidosis during treatment with metformin compared with other biguanides may be caused by its short non-polar hydrophobic side chains substituted with two CH3 groups. This has a lower affinity for hydrophobic structures, such as phospholipids in mitochondrial and cellular membranes, than the longer monosubstituted side-chains of the other biguanides (64). 

Guariglia A, Gonzi GL, Regolisti G, Vinci S. Treatment of biguanide-induced lactic acidosis reproposal of the physiological approach and review of the literature. Ann Ital Med Int 1994 9(l) 35-9. 

Hydroxoaquobis(biguanide)chromium(III) sulfate forms violet crystals which are sparingly soluble in water and do not lose any water even when heated to 120°. On treatment with hot caustic solution the substance is converted into tris(biguanidato) chromium which separates as ruby-red crystals. The chloride of the hydroxoaquo compound may be prepared as rose-red crystals by treating the sulfate with the calculated amount of barium chloride. 

Larkin DF, Kilvington S, Dart JK. Treatment of Acanthamoeba keratitis with polyhexamethylene biguanide. Ophthalmology 1992 99(2) 185-191. 

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