Tolbutamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Tolbutamide is a pure, white, crystalline compound which is practically insoluble in water.
Tolbutamide tablets are indicated as an adjunct to diet to lower the blood glucose in patients with non-insulin-dependent diabetes mellitus (type II) whose hyperglycemia cannot be controlled by diet alone.
In initiating treatment for non-insulin-dependent diabetes, diet should be emphasized as the primary form of treatment. Caloric restriction and weight loss are essential in the obese diabetic patient. Proper dietary management alone may be effective in controlling the blood glucose and symptoms of hyperglycemia. The importance of regular physical activity should also be stressed, and cardiovascular risk factors should be identified and corrective measures taken where possible.
If this treatment program fails to reduce symptoms and/or blood glucose, the use of an oral sulfonylurea or insulin should be considered. Use of tolbutamide tablets must be viewed by both the physician and patient as a treatment in addition to diet, and not as a substitute for diet or as a convenient mechanism for avoiding dietary restraint. Furthermore, loss of blood glucose control on diet alone may be transient, thus requiring only short-term administration of tolbutamide tablets.
During maintenance programs, tolbutamide tablets should be discontinued if satisfactory lowering of blood glucose is no longer achieved. Judgments should be based on regular clinical and laboratory evaluations.
In considering the use of tolbutamide tablets in asymptomatic patients, it should be recognized that controlling the blood glucose in non-insulin dependent diabetes has not been definitely established to be effective in preventing the long-term cardiovascular or neural complications of diabetes.
Published Studies Related to Tolbutamide
No relevant interaction with alprazolam, caffeine, tolbutamide, and digoxin by treatment with a low-hyperforin St John's wort extract. [2005.04]
We evaluated the pharmacokinetic interaction between a low-hyperforin St John's wort (SJW) extract and alprazolam, caffeine, tolbutamide, and digoxin. Previous reports on other SJW products had shown remarkably decreased plasma concentrations of certain co-medicated drugs, which was attributed to an inducing effect of SJW on cytochrome P-450 (CYP) and p-glycoprotein (p-gp) activity...
Is acarbose equivalent to tolbutamide as first treatment for newly diagnosed type 2 diabetes in general practice? A randomised controlled trial. [2004.01]
We performed a double blind randomised controlled trial in general practice to assess equivalence between tolbutamide and acarbose with respect to the effect on mean HbA(1c) in newly diagnosed patients with type 2 diabetes. Secondary objectives were to compare the effects of both treatments on fasting and post-load blood glucose and insulin levels, lipids, and adverse events...
Tolbutamide, flurbiprofen, and losartan as probes of CYP2C9 activity in humans. [2003.01]
The metabolic activity of CYP2C9 in 16 subjects expressing four different genotypes (CYP2C9*1/*1, *1/*2, *1/*3, and *2/*2) was evaluated. Single oral doses of tolbutamide, flurbiprofen, and losartan were administered in a randomized, crossover design...
Effects of CYP2C19 and CYP2C9 genetic polymorphisms on the disposition of and blood glucose lowering response to tolbutamide in humans. [2002.03]
Several recent in-vitro data have revealed that CYP2C19, in addition to CYP2C9, is also involved in the 4-methylhydroxylation of tolbutamide. We evaluated the relative contribution of CYP2C9 and CYP2C19 genetic polymorphisms on the disposition of blood glucose lowering response to tolbutamide in normal healthy Korean subjects in order to reappraise tolbutamide as a selective in-vivo probe substrate of CYP2C9 activity...
Fluvoxamine inhibits the CYP2C9 catalyzed biotransformation of tolbutamide. [2001.01]
OBJECTIVE: Our objective was to examine the interaction between fluvoxamine and tolbutamide to confirm that fluvoxamine inhibits CYP2C9... CONCLUSION: Fluvoxamine is a moderate inhibitor of CYP2C9 in vivo.
Clinical Trials Related to Tolbutamide
A Drug Interaction Study of Tasisulam in Patients With Advanced Cancer or Lymphoma [Terminated]
Drug Drug Interaction Study Between BI 201335 and BI 207127 in Chronic Hepatitis C Infected Patients [Completed]
To evaluate the drug-drug interactions between BI 201335 and BI 207127 as well as their
combined effect on CYP probe drug substrates and on tenofovir and raltegravir in treatment
naive or prior treatment relapse patients with chronic hepatitis C infection.
A Study to Assess Effect of JNJ-54861911 on Pharmacokinetics of Cocktail Representatives for Cytochrome P450 (CYP) 3A4, CYP2B6, CYP2C9, and CYP1A2 Substrates [Completed]
The purpose of this study is to assess the effects of single and multiple once daily doses
of 50 milligram (mg) of JNJ-54861911 on pharmacokinetics (PK) (study of the way a drug
enters and leaves the blood and tissues over time) of caffeine, midazolam, and tolbutamide
in healthy male participants.
AZD2066 Cocktail Study [Completed]
Multiple Doses of BI 207127 NA, BI 201335 NA Followed by the Combination of BI 207127 NA and BI 201335 NA in Healthy Male Volunteers [Terminated]
Study to investigate the pharmacokinetic drug-drug interaction potential of BI 207127 NA and
BI 201335 NA on each other at steady-state and to quantify the effect of BI 207127 NA, and
BI 207127 NA combined with BI 201335 NA, on the activity of CYP 2C9 and CYP 3A4 using the
probe substrates tolbutamide (CYP 2C9) and midazolam (CYP 3A4).
Page last updated: 2007-10-18