The Effects Of Metformin And Diabinese On Female Sex Hormone Of Type 2 Diabetes Mellitus Patients
[UNIVERSITY OF ILORIN TEACHING HOSPITAL (UITH), ILORIN, KWARA STATE]

2.4 DIABINESE (CHLORPROPAMIDE)
Diabinese (chlorpropamide), is an oral blood-glucose-lowering drug of the sulfonylurea class. Chlorpropamide is 1-[(pChlorophenyl)sulfonyl]-3-propylurea(Medrikovaet al., 2012.Chlorpropamide is a white crystalline powder, that has a slight odor. It is practically insoluble in water at pH 7.3 (solubility at pH 6 is 2.2 mg/mL). It is soluble in alcohol and moderately soluble in chloroform. The molecular weight of chlorpropamide is 276.74(Medrikova et al., 2012. Diabinese is available as 100 mg and 250 mg tablets.
2.4.1      CLINICAL PHARMACOLOGY OF DIABINESE
Diabinese appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets(Medrikova et al., 2012. The mechanism by which Diabinese lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity (Helseth et al., 2009).
Diabinese may also prove effective in controlling certain patients who have experienced primary or secondary failure to other sulfonylurea agents. A method developed which permits easy measurement of the drug in blood is available on request. Chlorpropamide does not interfere with the usual tests to detect albumin in the urine(Medrikova et al., 2012).
Diabinese is absorbed rapidly from the gastrointestinal tract. Within one hour after a single oral dose, it is readily detectable in the blood, and the level reaches a maximum within two to four hours. It undergoes metabolism in humans and it is excreted in the urine as unchanged drug and as hydroxylated or hydrolyzed metabolites. The biological half-life of chlorpropamide averages about 36 hours. Within 96 hours, 80–90% of a single oral dose is excreted in the urine. However, long-term administration of therapeutic doses does not result in undue accumulation in the blood, since absorption and excretion rates become stabilized in about 5 to 7 days after the initiation of therapy (Davidson and Peters, 2017). Diabinese exerts a hypoglycemic effect in healthy subjects within one hour, becoming maximal at 3 to 6 hours and persisting for at least 24 hours. The potency of chlorpropamide is approximately six times that of tolbutamide. Some experimental results suggest that its increased duration of action may be the result of slower excretion and absence of significant deactivation.