Tolazamide metabolites

Tolazamide (Y) Tolinase 100, 250, 500 100-250 100 250 1,000 Up to 24 hours Metabolized in liver metabolite less active than parent compound renally eliminated... 

Tolazamide is slowly absorbed and its hypoglycemic action only becomes manifest after several hours. Its is metabolized in the liver with an elimination half-life of about 7 hours. However several of its metabolites retain hypoglycemic activity. Its duration of action is shorter than that of chlorpropamide. 

Tocainide hydrochloride, 1028 Toclase, 431 Tocomine, 329 Tocopherol acetate, 329 Tocopheryl acetate, 329 Tofenacin, 1028 (metabolite), 833 Tofenacin hydrochloride, 1028 Tofranil, 679 Tofranil-PM, 679 Togiren, 589 Toilax, 397 Tokols, 329 Tolanase, 1029 Tolazamide, 1029 Tolazoline, 1029 Tolazoline hydrochloride, 1029 Tolbutamide, 1030 Tolbutamide sodium, 1030 Tolbutone, 1030 Tolectin, 1032 Tolerance to drugs, 298 Tolerzide, 663 Tolerzide, 971 Tolfenamic acid, 1031 Tolglybutamide, 1030... 

Metabolism/ elimination Acetohexamide, chlorpropamide, tolazamide, glyburide glimepiride weakly active metabolites. Glipizide, tolbutamide inactive metabolites. Inactive metabolites Predominantly inactive metabolites Excreted unchanged in urine Extensively metabolized in liver to metabolites Acarbose inactive metabolites. Miglitol excreted unchanged in urine. 

Tolazamide, U5P. Tolazamide. l-(hexahydrn-l/f-azcpin-l-yl)-3-(/r-tolylsulfonyl)urea (Tolinase). is an analogue of tolbutamide and is reported to be effective, in general, under the same eireumstanccs in which tolbutamide is useful. Tolazamide, however, appears to be more potent than tolbutamide and is nearly equal in potency to chlorpropamide. In studies with radioactive tolazamide, investigators found that 85% of an oral dose appeared in the urine as metabolites that were more soluble than tolazamide itself. 

Tolazamide p-Carboxytolazamide (a) Two hydroxy derivatives (a.i) p-Toluenesulphonamide (a) One unknown metabolite... 

Mechanism of Action. Based on the radiactive studies it has been observed that nearly 85% of an oral dose usually appears in the urine as its corresponding metabolites which were certainly more water-soluble than the parent tolazamide itself. 

In contrast, tolbutamide and tolazamide undergo a more rapid benzylic oxidation, leading to an inactive benzoic acid derivative (Fig. 32.4). An alternative hydroxylation of the aliphatic ring of tolazamide to an active metabolite results in a prolonged duration of action relative to tolbutamide. 

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