Precautions
The decrease of glyburide in the serum of normal healthy individuals is biphasic; the terminal half-life is about 10 hours. In single dose studies in fasting normal subjects, the degree and duration of blood glucose lowering is proportional to the dose administered and to the area under the drug level concentration-time curve.
How long does it take for glyburide to leave your system?
In single dose studies in fasting normal subjects who were administered glyburide tablets (nonmicronized) in doses ranging from 1.25 mg to 5 mg, the degree and duration of blood glucose lowering is proportional to the dose administered and to the area under the drug level concentration-time curve.
How much glyburide does it take to lower blood sugar?
The chemical classification of glyburide is Sulfonylurea Compounds. The second generation sulfonylureas include glyburide (also known as glibenclamide), gliclazide, glipizide, and glimepiride, which are oral hypoglycemic agents that are widely used in therapy of type 2 diabetes.
What is the chemical classification of glyburide?
Titration to Maintenance Dose. A maintenance dose of 5 mg of Glyburide Tablets provides approximately the same degree of blood glucose control as 250 to 375 mg chlorpropamide, 250 to 375 mg tolazamide, 500 to 750 mg acetohexamide, or 1,000 to 1,500 mg tolbutamide.
How many mg of glyburide is a maintenance dose?
How long does glyburide stay in your system?
Multiple-dose studies with Diaßeta in diabetic patients demonstrate drug level concentration-time curves similar to single- dose studies, indicating no build-up of drug in tissue depots. The decrease of glyburide in the serum of normal healthy individuals is biphasic, the terminal half-life being about 10 hours.
Is glyburide long or short acting?
Long-acting sulfonylureas included glyburide and glimepiride; short-acting sulfonylureas included gliclazide, glipizide and tolbutamide.
How long does it take for glyburide to lower blood sugar?
Generally, Diabeta (glyburide) lowers your blood sugar anywhere from 15 to 60 minutes after taking the dose. This is why it is important to take the medication with your largest meal of the day.
Should I take glyburide in the morning or at night?
Adults—At first, 2.5 milligrams (mg) of glyburide and 500 mg of metformin or 5 mg of glyburide and 500 mg of metformin two times a day, with the morning and evening meals. Your doctor may increase your dose a little at a time until your blood sugar is controlled.
What is the peak time for glyburide?
Single dose studies with Glyburide Tablets in normal subjects demonstrate significant absorption of glyburide within one hour, peak drug levels at about four hours, and low but detectable levels at twenty-four hours.
Is it OK to take glyburide at night?
Bedtime dosing of glyburide resulted in measurable improvement in fasting blood sugar and carbohydrate tolerance curves, but not to a degree justifying general recommendation of this technique in patients with NIDDM with secondary failure to oral agents.
Why is glyburide a high risk medication?
Glyburide has been associated with an increased risk for hypoglycemia and long-term cardiovascular mortality. This may be due to differences in tissue-specific binding of the respective sulfonylureas.
How much does glyburide lower A1C?
Glyburide/metformin tablets caused a superior mean reduction in A1C from baseline (-2.27%) vs. metformin (-1.53%) and glyburide (-1.90%) monotherapy (P = 0.0003). Glyburide/metformin also significantly reduced fasting plasma glucose and 2-h postprandial glucose values compared with either monotherapy.
When should you not take glyburide?
Who should not take Glyburide?low blood sugar.pituitary hormone deficiency.a condition where the adrenal glands produce less hormones called Addison's disease.glucose-6-phosphate dehydrogenase (G6PD) deficiency.hepatic porphyria.a type of blood disorder where the red blood cells burst called hemolytic anemia.alcoholism.More items...
What is the most common side effect of glyburide?
The more common side effects that can occur with glyburide include: diarrhea. dizziness. headache.
How far apart should I take glyburide?
It is usually taken once a day with breakfast or the first main meal of the day. However, in some cases your doctor may tell you to take glyburide twice a day.
Can you just stop taking glyburide?
Glyburide and metformin combination controls diabetes but does not cure it. Continue to take glyburide and metformin even if you feel well. Do not stop taking glyburide and metformin without talking to your doctor.
What type of drug is glyburide?
Glyburide belongs to a class of medicines called sulfonylureas. It causes your pancreas to release more insulin into the blood stream. This medicine may be used alone or with another oral medicine such as metformin. This medicine is available only with your doctor's prescription.
Which sulfonylurea is long-acting?
Chlorpropamide is a long-acting sulfonylurea available as 100 mg and 250 mg oral tablets outside the United States. [5][6] Start at 100 mg to 250 mg daily and increase the dose slowly every 5 to 7 days. The maximum daily dose for chlorpropamide is 750 mg.
Is glipizide short or long-acting?
How should this medicine be used? Glipizide comes as tablets and extended-release (long-acting) tablets to take by mouth. The regular tablet is usually taken one or more times a day, 30 minutes before breakfast or meals. The extended-release tablet is usually taken once a day with breakfast.
What is the mode of action of glyburide?
Glyburide, along with others in its class of sulfonylureas, exerts its mechanism of action based on increasing insulin secretion from beta cells in the pancreas. [7] Specifically, sulfonylureas bind to the SUR1 receptors in the membranes of the beta cells of potassium ATP-dependent channels.
Before Taking This Medicine
You should not use glyburide if you are allergic to it, or if: 1. you are being treated with bosentan (Tracleer); 2. you have type 1 diabetes; or 3...
How Should I Take Glyburide?
Glyburide is usually taken with breakfast or the first main meal of the day.Follow all directions on your prescription label and read all medicatio...
What Happens If I Miss A Dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to...
What Happens If I Overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. A glyburide overdose can cause life-threatening hypoglycemia.Sympt...
What Should I Avoid While Taking Glyburide?
If you also take colesevelam, avoid taking it within 4 hours after you take glyburide.Avoid drinking alcohol. It lowers blood sugar and may interfe...
Glyburide Dosing Information
Usual Adult Dose for Diabetes Type 2:Standard glyburide:-Initial dose: 2.5 mg to 5 mg orally once a day-Dose titration: Increase in increments of n...
What Other Drugs Will Affect Glyburide?
Glyburide may not work as well when you use other medicines at the same time. Many other drugs can also affect blood sugar control. This includes p...
How long does it take for glyburide to be absorbed?
Pharmacokinetics. Single dose studies with Glyburide Tablets in normal subjects demonstrate significant absorption of glyburide within one hour, peak drug levels at about four hours, and low but detectable levels at twenty-four hours.
How to monitor glyburide?
Therapeutic response to Glyburide Tablets should be monitored by frequent urine glucose tests and periodic blood glucose tests. Measurement of glycosylated hemoglobin levels may be helpful in some patients.
What is glyburide USP?
Glyburide Tablets, USP contain glyburide, USP, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide, USP is a white, crystalline compound, formulated as Glyburide Tablets, USP of 1.25, 2.5, and 5 mg strengths for oral administration. Inactive ingredients: microcrystalline cellulose, pregelatinized starch (corn starch), sodium starch glycolate (type A potato) and magnesium stearate. In addition, the 2.5 mg contains FD&C yellow No. 6 and the 5 mg contains D&C yellow No. 10, and FD&C blue No. 1.The chemical name for glyburide is 1- [ [p- [2- (5-chloro-o-anisamido)ethyl]phenyl]-sulfonyl]-3-cyclohexylurea and the molecular weight is 493.99. The structural formula is represented below.
What are the reactions to sulfonylurea?
Hematologic Reactions: Leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia (see PRECAUTIONS), aplastic anemia, and pancytopenia have been reported with sulfonylureas.
Does glyburide lower blood glucose?
Glyburide 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. The mechanism by which glyburide lowers blood glucose during long-term administration has not been clearly established.
Is oral hypoglycemic medication associated with cardiovascular mortality?
The administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. This warning is based on the study conducted by the University Group Diabetes Program (UGDP), a long-term prospective clinical trial designed to evaluate the effectiveness of glucose-lowering drugs in preventing or delaying vascular complications in patients with non-insulin-dependent diabetes. The study involved 823 patients who were randomly assigned to one of four treatment groups.
Which drugs cause hyperglycemia?
These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid.
How should I take glyburide?
Glyburide is usually taken with breakfast or the first main meal of the day.
What to know before taking glyburide?
Before taking glyburide, tell your doctor if you are allergic to sulfa drugs, if you have been using insulin or chlorpropamide (Diabinese), or if you have hemolytic anemia (a lack of red blood cells), an enzyme deficiency (G6PD), a nerve disorder, liver disease, or kidney disease.
What other drugs will affect glyburide?
If you also take colesevelam, take your glyburide dose 4 hours before you take colesevelam.
What is glyburide used for?
Glyburide is an oral diabetes medicine that helps control blood sugar levels. Glyburide is used together with diet and exercise to improve blood sugar control in adults with type 2 diabetes mellitus. Glyburide is not for treating type 1 diabetes.
Can you take glyburide with bosentan?
You should not use glyburide if you are being treated with bosentan ( Tracleer ), or if you have diabetic ketoacidosis (call your doctor for treatment). Glyburide is not for treating type 1 diabetes.
How to store a syringe?
Store at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.
Does glyburide cause hives?
Glyburide side effects. Get emergency medical help if you have signs of an allergic reaction to glyburide ( hives, difficult breathing, swelling in your face or throat) or a severe skin reaction ( fever, sore throat, burning in your eyes, skin pain, red or purple skin rash that spreads and causes blistering and peeling).
How long does glyburide last in the body?
The decrease of glyburide in the serum of normal healthy individuals is biphasic; the terminal half-life is about 10 hours.
How long does it take for glyburide to be absorbed?
Pharmacokinetics. Single dose studies with glyburide tablets in normal subjects demonstrate significant absorption within one hour, peak drug levels at about four hours, and low but detectable levels at twenty-four hours.
What should patients know about glyburide?
Information for Patients. Patients should be informed of the potential risks and advantages of glyburide tablets and of alternative modes of therapy. They also should be informed about the importance of adherence to dietary instructions, of a regular exercise program, and of regular testing of urine and/or blood glucose.
What is glyburide tablet?
Glyburide tablets contain micronized (smaller particle size) glyburide, which is an oral blood-glucose-lowering drug of the sulfonylurea class. Glyburide is a white, crystalline compound, formulated as glyburide tablets of 1.25, 2.5, and 5 mg strengths for oral administration.
Why is glyburide considered a secondary failure?
This phenomenon is known as secondary failure, to distinguish it from primary failure in which the drug is ineffective in an individual patient
How to monitor glyburide?
Therapeutic response to glyburide tablets should be monitored by frequent urine glucose tests and periodic blood glucose tests. Measurement of glycosylated hemoglobin levels may be helpful in some patients.
What is the metabolite of glyburide?
The major metabolite of glyburide is the 4-transhydroxy derivative. A second metabolite, the 3-cishydroxy derivative, also occurs. These metabolites contribute no significant hypoglycemic action in humans since they are only weakly active (1/400th and 1/40th as active, respectively, as glyburide) in rabbits.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Pharmacology
Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites
Use: Labeled Indications
Diabetes mellitus, type 2: Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Contraindications
Hypersensitivity to glyburide or any component of the formulation; type 1 diabetes mellitus or diabetic ketoacidosis, with or without coma; concomitant use with bosentan.
Dosage and Administration
Micronized glyburide tablets are not bioequivalent to conventional glyburide tablets; retitration should occur if patients are being transferred to a different glyburide formulation (eg, micronized-to-conventional or vice versa) or from other hypoglycemic agents.
Dietary Considerations
Should be taken with meals at the same time each day (twice-daily dosing may be beneficial if conventional glyburide doses are >10 mg or micronized glyburide doses are >6 mg). Individualized medical nutrition therapy (MNT) based on ADA recommendations is an integral part of therapy.
Drug Interactions
Ajmaline: Sulfonamides may enhance the adverse/toxic effect of Ajmaline. Specifically, the risk for cholestasis may be increased. Monitor therapy
What is a glyburide?
Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects. Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects.
Where is glyburide excreted?
Glyburide is inactivated by the liver to 4-trans-hydroxyglyburide and 3-cis-hydroxyglyburide; 50% of these compounds is excreted in the urine and 50% in the bile.
Is glyburide a first generation drug?
Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects. To date it has a low frequency of clinically significant interactions with other drugs.
Can glyburide be used for renal disease?
Glyburide should not be prescribed for patients with liver disease or significant renal disease. Because glyburide is a potent hypoglycemic agent, it should be prescribed in small initial doses, particularly for elderly patients with diabetes.
Is glyburide the same as tolbutamide?
Glyburide, a second-generation hypoglycemic sulfonylurea, is 200 times as potent as tolbutamide. This increase is due to greater intrinsic hypoglycemic potency of the molecule rather than to a prolonged biologic half-life.
Is sulfonylurea a replacement for sulfonylurea?
It is a useful medication for patients with type II diabetes whose hyperglycemia is not adequately reduced by dietary management and exercise. It can be used as the initial drug in these patients or as the replacement drug for those with primary or secondary failure during therapy with first-generation sulfonylureas.
Does glyburide cause insulin secretion?
Although glyburide is a potent stimulator of pancreatic insulin secretion after short- term administration, an additional mechanism of action during long-term administration is to decrease the resistance of muscle and liver to the action of insulin.
How long does it take for glyburide to work?
Oral Route. Following oral administration, glyburide is rapidly and completely absorbed from the GI tract. The onset of action occurs within 2 hours, with a maximal decrease in serum glucose occurring within 3 to 4 hours. The micronized formulation is not bioequivalent to the conventional glyburide products.
Where is glyburide metabolized?
Glyburide is metabolized completely in the liver to 2 metabolites. CYP2C9 is thought to be primarily responsible for the biotransformation of glyburide in vivo, with CYP3A4 playing a minor role. The major metabolite of glyburide is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites are not thought to significantly contribute to the drug's hypoglycemic action in humans since they are only weakly active (1/400th and 1/40th as active, respectively, as glyburide) in rabbits. Glyburide is excreted as metabolites in the bile and urine, approximately 50% by each route. This dual excretory pathway is qualitatively different from that of other sulfonylureas, which are excreted primarily in the urine. The terminal elimination half-life of glyburide (conventional formulation) is 10 hours. The blood glucose lowering effect persists for 24 hours following a single morning doses in nonfasting diabetic patients. Under conditions of repeated administration in diabetic patients, however, there is no reliable correlation between blood drug levels and fasting blood glucose levels.
When transferring patients from oral hypoglycemic agents other than chlorpropamide, is a transition period necessary?
When transferring patients from oral hypoglycemic agents other than chlorpropamide, no transition period is necessary. When transferring from chlorpropamide, use care during the first 2 weeks because the prolonged action of chlorpropamide and subsequent overlapping drug effects may provoke hypoglycemia.
Does sulfonylurea cause myocardial infarction?
The largest of the trials, the United Kingdom Prospective Diabetes Study (UKPDS), has demonstrated that intensive therapy with sulfonylureas does not increase the risk of myocard ial infarction or diabetes-related death when compared to conventional therapy. In this trial, lowering blood glucose with sulfonylurea therapy did not significantly effect cardiovascular complications. A 16% reduction (not statistically significant) in the risk of combined fatal or nonfatal myocardial infarction and sudden death has been reported. In a follow-up study to the UKPDS, researchers found that after 10-years of resuming typical care, patients originally randomized to intensive therapy with sulfonylureas or insulin had a 15% relative reduction (RR 0.85, 95% CI 0.74—0.97; p=0.01) in the risk of myocardial infarction and a 13% relative decrease (RR 0.87, 95% CI 0.76—0.96; p=0.007) in the risk of death from any cause as compared to patients originally randomized to conventional therapy; it should be noted that these reductions in cardiovascular risks persisted even though HbA1c concentrations were similar in the 2 groups after 1 year of follow-up. In contrast, the University Group Diabetes Program (UGDP) has previously reported that the administration of oral sulfonylureas increases cardiovascular mortality compared with dietary management alone, or dietary management and insulin therapy. The UGDP study has been widely criticized for study limitations including a small sample size (i.e., 200 patients per treatment group). Despite the controversy regarding these findings, the results of the UGDP study serve as a basis for the manufacturers' warning of possible risk of cardiovascular mortality associated with the use of oral sulfonylureas.
Is glyburide bioequivalent to glyburide?
In some patients, twice daily dosing will provide better control, and doses are usually given with breakfast and dinner.#N#Micronized and conventional formulations of glyburide are not bioequivalent and should not be substituted for one another.
Is metformin safe for T2DM?
Safety and efficacy have not been established for type 2 diabetes mellitus (T2DM); not FDA-approved. Not a first-line therapy in pediatric patients for T2DM. In one study, metformin monotherapy, glyburide monotherapy and metformin and glyburide combined therapy (range of glyburide dosing: 1.25 mg to 5 mg PO twice daily) were compared in pediatric patients 9 to 16 years of age with T2DM. After 26 weeks, the mean hemoglobin A1C declined in all 3 groups. However, combination therapy failed to show superiority over use of either drug alone. In general, sulfonylureas are not superior to metformin for T2DM in this age group, and, they may cause weight gain and exhibit higher rates of hypoglycemia. More study is needed of use as add-on therapy to metformin.
Can type 2 diabetics be switched to glyburide?
SWITCHING FROM INSULIN: Some type 2 DM patients treated with insulin can be switched successfully to glyburide therapy. For patients being treated with less than 40 units/day of insulin, begin with a usual starting dose of glyburide and monitor closely.
How long does it take for glyburide to be absorbed?
Single dose studies with glyburide tablets (micronized) in normal subjects demonstrate significant absorption of glyburide within one hour, peak drug levels at about two to three hours, and low but detectable levels at twenty-four hours.
When should you retitrate glyburide?
Patients should be retitrated when transferred from glyburide tablets (nonmicronized) or Diabeta® or other oral hypoglycemic agents.
How often should I take glyburide?
When transferring patients receiving more than 40 units of insulin daily, they may be started on a daily dose of glyburide tablets (micronized) 3 mg concomitantly with a 50% reduction in insulin dose. Progressive withdrawal of insulin and increase of glyburide tablets (micronized) in increments of 0.75 to 1.5 mg every 2 to 10 days is then carried out. During this conversion period when both insulin and glyburide tablets (micronized) are being used, hypoglycemia may occur. During insulin withdrawal, patients should test their urine for glucose and acetone at least three times daily and report results to their physician. The appearance of persistent acetonuria with glycosuria indicates that the patient is a Type I diabetic who requires insulin therapy.
How to monitor micronized glyburide?
Therapeutic response to micronized glyburide tablets should be monitored by frequent urine glucose tests and periodic blood glucose tests. Measurement of glycosylated hemoglobin levels may be helpful in some patients.
What is a 3mg glyburide?
Glyburide Tablets, USP (micronized) 3mg- is a light blue oval shaped tablet, bisected on one side, debossed with "M04" and "3.0", and with "M OVA" on the other side; and supplied as follows:
Is glyburide a hypoglycemic drug?
Some patients who are initially responsive to oral hypoglycemic drugs, including glyburide, may become unresponsive or poorly responsive over time. Alternatively, glyburide may be effective in some patients who have become unresponsive to one or more other sulfonylurea drugs.
Does glyburide lower blood glucose?
Glyburide 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. The mechanism by which glyburide lowers blood glucose during long-term administration has not been clearly established. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonylurea hypoglycemic drugs. The combination of glyburide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms.
