Drugs Details

Drugs Info of Glyset
Drugs Details
  • Drugs Type  : FDA
  • Date : 13th Mar 2015 10:11 pm
  • Brand Name : Glyset
  • Generic Name : miglitol (Pronunciation: MIG lih tall)
Descriptions

GLYSET Tablets contain miglitol, an oral alpha-glucosidase inhibitor for use in the management of non-insulin-dependent diabetes mellitus (NIDDM). Miglitol is a desoxynojirimycin derivative, and is chemically known as 3,4,5-piperidinetriol, 1-(2hydroxyethyl)-2-(hydroxymethyl)-, [2R-(2α,3β,4α, 5β)]-. It is a white to pale-yellow powder with a molecular weight of 207.2. Miglitol is soluble in water and has a pKa of 5.9. Its empirical formula is C8H17NO5and its chemical structure is as follows:

 

Glyset® (miglitol) Structural Formula Illustration

 

GLYSET is available as 25 mg, 50 mg and 100 mg tablets for oral use. The inactive ingredients are starch, microcrystalline cellulose, magnesium stearate, hypromellose, polyethylene glycol, titanium dioxide, and polysorbate 80.

 

What are the possible side effects of miglitol (Glyset)?

Stop taking miglitol and seek emergency medical attention if you experience an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives).

Other, less serious side effects, are more likely to occur. Continue to take miglitol and talk to your doctor if you experience

  • abdominal pain,
  • diarrhea,
  • flatulence, or
  • a rash.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side...

Read All Potential Side Effects and See Pictures of Glyset »

What are the precautions when taking miglitol (Glyset)?

Before taking miglitol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: intestine/bowel problems (e.g., inflammatory bowel disease, intestinal blockage, digestion/absorption disorders).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease.

You may experience blurred vision, dizziness, or drowsiness due to extremely low or high blood sugar levels. Do not drive, use machinery,...

Read All Potential Precautions of Glyset »

 

This monograph has been modified to include the generic and brand name in many instances.

Indications

GLYSET is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Dosage Administration

There is no fixed dosage regimen for the management of diabetes mellitus with GLYSET Tablets or any other pharmacologic agent. Dosage of GLYSET must be individualized on the basis of both effectiveness and tolerance while not exceeding the maximum recommended dosage of 100 mg 3 times daily. GLYSET should be taken three times daily at the start of each main meal. GLYSET should be started at 25 mg, and the dosage gradually increased both to reduce gastrointestinal adverse effects and to permit identification of the minimum dose required for adequate glycemic control of the patient.

During treatment initiation and dose titration one-hour postprandial plasma glucose may be used to determine the therapeutic response to GLYSET and identify the minimum effective dose for the patient. Thereafter, glycosylated hemoglobin should be measured at intervals of approximately 3 months. The therapeutic goal should be to decrease both postprandial plasma glucose and glycosylated hemoglobin levels to normal or near normal by using the lowest effective dose of GLYSET, either as monotherapy or in combination with a sulfonylurea.

Initial Dosage

The recommended starting dosage of GLYSET is 25 mg, given orally three times daily at the start of each main meal. However, some patients may benefit by starting at 25 mg once daily to minimize gastrointestinal adverse effects, and gradually increasing the frequency of administration to 3 times daily.

Maintenance Dosage

The usual maintenance dose of GLYSET is 50 mg taken 3 times daily, although some patients may benefit from increasing the dose to 100 mg 3 times daily. To allow adaptation to potential gastrointestinal adverse effects, it is recommended that GLYSET therapy be initiated at a dosage of 25 mg 3 times daily, then gradually titrated upward to allow adaptation. After 4 to 8 weeks of the 25 mg 3 times daily regimen, the dosage should be increased to 50 mg 3 times daily for approximately three months, following which a glycosylated hemoglobin level should be measured to assess therapeutic response. If at that time, the glycosylated hemoglobin level is not satisfactory, the dosage may be further increased to 100 mg 3 times daily, the maximum recommended dosage. Pooled data from controlled studies suggest a dose-response for both HbA1c and one-hour postprandial plasma glucose throughout the recommended dosage range. However, no single study has examined the effect on glycemic control of titrating patients' doses upwards within the same study. If no further reduction in postprandial glucose or glycosylated hemoglobin levels is observed with titration to 100 mg 3 times daily, consideration should be given to lowering the dose. Once an effective and tolerated dosage is established, it should be maintained.

Maximum Dosage

The maximum recommended dosage of GLYSET is 100 mg 3 times daily. In one clinical trial, 200 mg 3 times daily gave additional improved glycemic control but increased the incidence of the gastrointestinal symptoms described above.

Patients Receiving Sulfonylureas

Sulfonylurea agents may cause hypoglycemia. There was no increased incidence of hypoglycemia in patients who took GLYSET in combination with sulfonylurea agents compared to the incidence of hypoglycemia in patients receiving sulfonylureas alone in any clinical trial. However, GLYSET given in combination with a sulfonylurea will cause a further lowering of blood glucoseand may increase the risk of hypoglycemia due to the additive effects of the two agents. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made (see PRECAUTIONS).

How Supplied

GLYSET Tablets are available as 25 mg, 50 mg, and 100 mg tablets.

 

STRENGTH BOTTLES OF 100: NDC
25 mg 0009-5012-01
50 mg 0009-5013-01
100 mg 0009-5014-01

 

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature].

Distributed by: Pharmacia & Upjohn Co, Division of Pfizer Inc, NY, NY 10017. Manufactured by Bayer HealthCare Pharmaceuticals Inc. Made in Germany. Revised August 2012

This monograph has been modified to include the generic and brand name in many instances.

Side Effects

Gastrointestinal

Gastrointestinal symptoms are the most common reactions to GLYSET Tablets. In U.S. placebo-controlled trials, the incidences of abdominal pain, diarrhea, and flatulence were 11.7%, 28.7%, and 41.5% respectively in 962 patients treated with GLYSET 25 100 mg 3 times daily, whereas the corresponding incidences were 4.7%, 10.0%, and 12.0% in 603 placebo-treated patients. The incidence of diarrhea and abdominal pain tended to diminish with continued treatment.

Dermatologic

Skin rash was reported in 4.3% of patients treated with GLYSET compared to 2.4% of placebo-treated patients. Rashes were generally transient and most were assessed as unrelated to GLYSET by physician investigators.

Abnormal Laboratory Findings

Low serum iron occurred more often in patients treated with GLYSET (9.2%) than in placebo-treated patients (4.2%) but did not persist in the majority of cases and was not associated with reductions in hemoglobin or changes in other hematologic indices.

Postmarketing Experience

The following adverse reactions have been reported during post-approval use of GLYSET. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Gastrointestinal Disorders: ileus (including paralytic ileus), subileus, gastrointestinal pain, nausea, abdominal distention.

  • Pneumatosis Cystoides Intestinalis 
    There have been rare postmarketing reports of pneumatosis cystoides intestinalis associated with the use of alpha-glucosidase inhibitors, including GLYSET. Pneumatosis cystoides intestinalis may present with symptoms of diarrhea, mucus discharge, rectal bleeding, and constipation. Complications may include pneumoperitoneum, volvulus,intestinal obstruction, intussusception, intestinal hemorrhage, and intestinal perforation. If pneumatosis cystoides intestinalis is suspected, discontinue Glyset and perform the appropriate diagnostic imaging.

Read the Glyset (miglitol) Side Effects Center for a complete guide to possible side effects

Learn More »
 
 
 

Interactions

Several studies investigated the possible interaction between miglitol and glyburide. In six healthy volunteers given a single dose of 5 mg glyburide on a background of 6 days treatment with miglitol (50 mg 3 times daily for 4 days followed by 100 mg 3 times daily for 2 days) or placebo, the mean Cmax and AUC values for glyburide were 17% and 25% lower, respectively, when glyburide was given with miglitol. In a study in diabetic patients in which the effects of adding miglitol 100 mg 3 times daily for 7 days or placebo to a background regimen of 3.5 mg glyburide daily were investigated, the mean AUC value for glyburide was 18% lower in the group treated with miglitol, although this difference was not statistically significant. Information on a potential interaction with glyburide was obtained from one of the large U.S. clinical trials (Study 7) in which patients were dosed with either miglitol or placebo on a background of glyburide 10 mg twice daily. At the 6-month and 1-year clinic visits, patients taking concomitant miglitol 100 mg 3 times daily exhibited mean Cmax values for glyburide that were 16% and 8% lower, respectively, compared to patients taking glyburide alone. However, these differences were not statistically significant. Thus, although there was a trend toward lower AUC and Cmax values for glyburide when co-administered with GLYSET, no definitive statement regarding a potential interaction can be made based on the foregoing three studies.

The effect of miglitol (100 mg 3 times daily for 7 days) on the pharmacokinetics of a single 1000 mg dose of metformin was investigated in healthy volunteers. Mean AUC and Cmax values for metformin were 12% to 13% lower when the volunteers were given miglitol as compared with placebo, but this difference was not statistically significant.

In a study with healthy volunteers, co-administration of either 50 mg or 100 mg miglitol 3 times daily together with digoxin reduced the average plasma concentrations of digoxin by 19% and 28%, respectively. However, in diabetic patients under treatment with digoxin, plasma digoxin concentrations were not altered by co-administration of miglitol 100 mg 3 times daily for 14 days.

Other healthy volunteer studies have demonstrated that miglitol may significantly reduce the bioavailability of ranitidine and propranolol by 60% and 40%, respectively. No effect of miglitol was observed on the pharmacokinetics or pharmacodynamics of either warfarin or nifedipine.

Intestinal adsorbents (e.g., charcoal) and digestive enzyme preparations containing carbohydrate-splitting enzymes (e.g., amylase, pancreatin) may reduce the effect of GLYSET and should not be taken concomitantly.

In 12 healthy males, concomitantly administered antacid did not influence the pharmacokinetics of miglitol.

Read the Glyset Drug Interactions Center for a complete guide to possible interactions

Learn More »
 

This monograph has been modified to include the generic and brand name in many instances.

 
 

Warnings

No information provided.

Precautions

Macrovascular Outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with GLYSET or any other anti-diabetic drug.

General

Hypoglycemia

Because of its mechanism of action, GLYSET, when administered alone, should not cause hypoglycemia in the fasted or postprandial state. Sulfonylureas and insulin can cause hypoglycemia. Because GLYSET Tablets given in combination with a sulfonylurea or insulin will cause a further lowering of blood glucose, it may increase the hypoglycemic potential of the sulfonylurea or insulin. Consider reducing the dose of sulfonylureas or insulin when GLYSET is used in combination with these medications.

Oral glucose (dextrose), whose absorption is not delayed by GLYSET, should be used instead of sucrose (cane sugar) in the treatment of mild-to-moderate hypoglycemia. Sucrose, whose hydrolysis to glucose and fructoseis inhibited by GLYSET, is unsuitable for the rapid correction of hypoglycemia. Severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.

Loss of Control of Blood Glucose

When diabetic patients are exposed to stress such as fever, trauma, infection, or surgery, a temporary loss of control of blood glucose may occur. At such times, temporary insulin therapy may be necessary.

Renal Impairment

Plasma concentrations of GLYSET in renally impaired volunteers were proportionally increased relative to the degree of renal dysfunction. Long-term clinical trials in diabetic patients with significant renal dysfunction (serum creatinine > 2.0 mg/dL) have not been conducted. Therefore, treatment of these patients with GLYSET is not recommended.

Laboratory Tests

Therapeutic response to GLYSET may be monitored by periodic blood glucose tests. Measurement of glycosylated hemoglobin levels is recommended for the monitoring of long-term glycemic control.

Carcinogenesis, Mutagenesis, and Impairment of Fertility

Miglitol was administered to mice by the dietary route at doses as high as approximately 500 mg/kg body weight (corresponding to greater than 5 times the exposure in humans based on AUC) for 21 months. In a two-year rat study, miglitol was administered in the diet at exposures comparable to the maximum human exposures based on AUC. There was no evidence of carcinogenicity resulting from dietary treatment with miglitol.

In vitro, miglitol was found to be nonmutagenic in the bacterial mutagenesis (Ames) assay and the eukaryotic forward mutation assay (CHO/HGPRT). Miglitol did not have any clastogenic effects in vivo in the mouse micronucleus test. There were no heritable mutations detected in dominant lethal assay.

A combined male and female fertility study conducted in Wistar rats treated orally with miglitol at dose levels of 300 mg/kg body weight (approximately 8 times the maximum human exposure based on body surface area) produced no untoward effect on reproductive performance or capability to reproduce. Survival, growth, development, and fertility of the offspring were not compromised.

Pregnancy

Teratogenic Effects - Pregnancy Category B

The safety of GLYSET in pregnant women has not been established. Developmental toxicology studies have been performed in rats at doses of 50, 150 and 450 mg/kg, corresponding to levels of approximately 1.5, 4, and 12 times the maximum recommended human exposure based on body surface area. In rabbits, doses of 10, 45, and 200 mg/kg corresponding to levels of approximately 0.5, 3, and 10 times the human exposure were examined. These studies revealed no evidence of fetal malformations attributable to miglitol. Doses of miglitol up to 4 and 3 times the human dose (based on body surface area), for rats and rabbits respectively, did not reveal evidence of impaired fertility or harm to the fetus. The highest doses tested in these studies, 450 mg/kg in the rat and 200 mg/kg in the rabbit promoted maternal and/or fetal toxicity. Fetotoxicity was indicated by a slight but significant reduction in fetal weight in the rat study and slight reduction in fetal weight, delayed ossification of the fetal skeleton and increase in the percentage of non-viable fetuses in the rabbit study. In the peri-postnatal study in rats, the NOAEL (No Observed Adverse Effect Level) was 100 mg/kg (corresponding to approximately four times the exposure to humans, based on body surface area). An increase in stillborn progeny was noted at the high dose (300 mg/kg) in the rat peripostnatal study, but not at the high dose (450 mg/kg) in the delivery segment of the rat developmental toxicity study. Otherwise, there was no adverse effect on survival, growth, development, behavior, or fertility in either the rat developmental toxicity or peripostnatal studies. There are however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, miglitol should be used during pregnancy only if clearly needed.

Nursing Mothers

Miglitol has been shown to be excreted in human milk to a very small degree. Total excretion into milk accounted for 0.02% of a 100 mg maternal dose. The estimated exposure to a nursing infant is approximately 0.4% of the maternal dose. Although the levels of miglitol reached in human milk are exceedingly low, it is recommended that GLYSET not be administered to a nursing woman.

Pediatric Use

Safety and effectiveness of GLYSET in pediatric patients have not been established.

Geriatric Use

Of the total number of subjects in clinical studies of GLYSET in the United States, patients valid for safety analyses included 24% over 65, and 3% over 75. No overall differences in safety and effectiveness were observed between these subjects and younger subjects. The pharmacokinetics of miglitol were studied in elderly and young males (n=8 per group). At the dosage of 100 mg 3 times daily for 3 days, no differences between the two groups were found.

This monograph has been modified to include the generic and brand name in many instances.

OverDose

Unlike sulfonylureas or insulin, an overdose of GLYSET tablets will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdominal discomfort. Because of the lack of extra-intestinal effects seen with GLYSET, no serious systemic reactions are expected in the event of an overdose.

ContrainDications

GLYSET Tablets are contraindicated in patients with:

  • Diabetic ketoacidosis
  • Inflammatory bowel disease, colonic ulceration, or partial intestinal obstruction, and in patients predisposed to intestinal obstruction
  • Chronic intestinal diseases associated with marked disorders of digestion or absorption, or with conditions that may deteriorate as a result of increased gas formation in the intestine
  • Hypersensitivity to the drug or any of its components.

This monograph has been modified to include the generic and brand name in many instances.

Clinical Pharamacology

Miglitol is a desoxynojirimycin derivative that delays the digestion of ingestedcarbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, GLYSET Tablets reduce levels of glycosylated hemoglobin in patients with Type II (non-insulindependent) diabetes mellitus. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time.

Mechanism of Action

In contrast to sulfonylureas, GLYSET does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal α-glucoside hydrolase enzymes. Membrane-bound intestinal αglucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia.

Because its mechanism of action is different, the effect of GLYSET to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, GLYSET diminishes the insulinotropic and weight-increasing effects of sulfonylureas.

Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance.

Pharmacokinetics

Absorption

Absorption of miglitol is saturable at high doses: a dose of 25 mg is completely absorbed, whereas a dose of 100 mg is 50% - 70% absorbed. For all doses, peak concentrations are reached in 2 to 3 hours. There is no evidence that systemic absorption of miglitol contributes to its therapeutic effect.

Distribution

The protein binding of miglitol is negligible ( < 4.0%). Miglitol has a volume of distribution of 0.18 L/kg, consistent with distribution primarily into the extracellular fluid.

Metabolism

Miglitol is not metabolized in humans or in any animal species studied. No metabolites have been detected in plasma, urine or feces, indicating a lack of either systemic or pre-systemic metabolism.

Excretion

Miglitol is eliminated by renal excretion as unchanged drug. Following a 25 mg dose, over 95% of the dose is recovered in the urine within 24 hours. At higher doses, the cumulative recovery of drug from urine is somewhat lower due to the incomplete bioavailability. The elimination half-life of miglitol from plasma is approximately 2 hours.

Special Populations

Renal Impairment

Because miglitol is excreted primarily by the kidneys, accumulation of miglitol is expected in patients with renal impairment. Patients with creatinine clearance < 25 mL/min taking 25 mg 3 times daily, exhibited a greater than two-fold increase in miglitol plasma levels as compared to subjects with creatinine clearance > 60 mL/min. Dosage adjustment to correct the increased plasma concentrations is not feasible because miglitol acts locally. Little information is available on the safety of miglitol in patients with creatinine clearance < 25 mL/min. Therefore, treatment of these patients with miglitol is not recommended.

Hepatic impairment

Miglitol pharmacokinetics were not altered in cirrhotic patients relative to healthy control subjects. Since miglitol is not metabolized, no influence of hepatic function on the kinetics of miglitol is expected.

Gender

No significant difference in the pharmacokinetics of miglitol was observed between elderly men and women when body weight was considered.

Race

Several pharmacokinetic studies were conducted in Japanese volunteers, with results similar to those observed in Caucasians. A study comparing the pharmacodynamic response to a single 50 mg dose in Black and Caucasian healthy volunteers indicated similar glucose and insulin responses in both populations.

Clinical Studies

Clinical Experience in Non-Insulin-Dependent Diabetes Mellitus (NIDDM) Patients on Dietary Treatment Only

GLYSET Tablets were evaluated in two U.S. and three non-U.S. controlled, fixed-dose, monotherapy studies, in which 735 patients treated with GLYSET were evaluated for efficacy analyses (see Table 1).

In Study 1, a 1-year study in which GLYSET was evaluated as monotherapy and also as combination therapy, there was a statistically significantly smaller increase in mean glycosylated hemoglobin (HbA1c) over time in the miglitol 50 mg 3 times daily monotherapy arm compared to placebo. Significant reductions in mean fasting and postprandial plasma glucose levels and in mean postprandial insulin levels were observed in patients treated with GLYSET compared with the placebo group.

In Study 2, a 14-week study, there was a significant decrease in HbA1c in patients receiving GLYSET 50 mg 3 times daily or 100 mg 3 times daily compared to placebo. In addition, there were significant reductions in postprandial plasma glucose and postprandial serum insulin levels compared to placebo.

Study 3, was a 6-month dose-ranging trial evaluating GLYSET at doses from 25 mg 3 times daily, to 200 mg 3 times daily. GLYSET produced a greater reduction in HbA1c than placebo at all doses, although the effect was statistically significant at the 100 mg 3 times daily and 200 mg 3 times daily. In addition, all doses of GLYSET produced significant reductions in postprandial plasma glucose and postprandial insulin levels compared to placebo.

Studies 4 and 5 were 6-month studies evaluating GLYSET at 50 and 100 mg 3 times daily, and 100 mg 3 times daily, respectively. As compared to placebo, GLYSET produced reductions in HbA1c, as well as a significant reduction in postprandial plasma glucose in both studies at the doses employed.

Table 1 : Results of Monotherapy Study with GLYSET

STUDY TREATMENT HBA1C (%) 1-HOUR POSTPRANDIAL GLUCOSE (MG/DL)
MEAN CHANGE FROM BASELINE* TREATMENT EFFECT** MEAN CHANGE FROM BASELINE TREATMENT EFFECT**
1 (U.S.) Placebo +0.71 +24
GLYSET 50 mg 3 times daily +0.13 -0.58† -39 -63†
2 (U.S.) Placebo +0.47 +15
GLYSET 50 mg 3 times daily -0.22 -0.69† -52 -67†
GLYSET 100 mg 3 times daily -0.28 -0.75† -59 -74†
3 (non-U.S.) Placebo +0.18 +2
GLYSET 25 mg 3 times daily -0.08 -0.26 -33 -35†
GLYSET 50 mg 3 times daily -0.22 -0.40 -45 -47†
GLYSET 100 mg 3 times daily -0.63 -0.81† -62 -64†
GLYSET 200 mg 3 times daily‡ -0.84 -1.02† -85 -87†
4 (non-U.S.) Placebo +0.01 +8
GLYSET 50 mg 3 times daily -0.35 -0.36† -20 -28†
GLYSET 100 mg 3 times daily -0.57 -0.58† -25 -33†
5 (non-U.S.) Placebo +0.32 +17
GLYSET 100 mg 3 times daily -0.43 -0.75† -38 -55†
* Mean baseline ranged from 7.54 to 8.72% in these studies. 
** The result of subtracting the placebo group average. 
† p ≤ 0.05 
‡ Although results for the 200 mg 3 times daily are presented for completeness, the maximum recommended dosage of GLYSET is 100 mg 3 times daily.

 

Clinical Experience in NIDDM Patients Receiving Sulfonylureas

GLYSET was studied as adjunctive therapy to a background of maximal or near-maximal sulfonylurea (SFU) treatment in three large, double-blind, randomized studies (two U.S. and one non-U.S.) in which 471 patients treated with GLYSET were evaluated for efficacy (see Table 2).

Study 6 included patients under treatment with maximal doses of SFU at entry. At the end of this 14-week study, the mean treatment effects on glycosylated hemoglobin (HbA1c) were -0.82% and -0.74% for patients receiving GLYSET 50 mg 3 times daily plus SFU, and GLYSET 100 mg 3 times daily plus SFU, respectively.

Study 7 was a 1-year study in which GLYSET at 25, 50 or 100 mg 3 times daily was added to a maximal dose of glyburide (10 mg twice daily). At the end of this study, the mean treatment effects on HbA1c of GLYSET when added to maximum glyburide therapy were -0.30%, -0.62%, and -0.73% with 25, 50 and 100 mg 3 times daily dosages of GLYSET, respectively.

In Study 8, the addition of GLYSET 100 mg 3 times daily to a background of treatment with glyburide produced an additional mean treatment effect on HbA1c of -0.66%.

Table 2 : Results of Combination Therapy with GLYSET Plus Sulfonylurea (SFU)

STUDY TREATMENT HBA1C
(%)
1-HOUR POSTPRANDIAL GLUCOSE (MG/DL)
MEAN CHANGE FROM BASELINE* TREATMENT EFFECT** MEAN CHANGE FROM BASELINE TREATMENT EFFECT**
6 (U.S.) Placebo + SFU +0.33 --- -1 ---
GLYSET 50 mg 3 times daily + SFU -0.49 -0.82† -69 -68†
GLYSET 100 mg 3 times daily + SFU -0.41 -0.74† -73 -72†
7 (U.S.) Placebo + SFU +1.01 --- 48 ---
GLYSET 25 mg 3 times daily+ SFU +0.71 -0.30 -2 -50†
GLYSET 50 mg 3 times daily+ SFU +0.39 -0.62† -13 -61†
GLYSET 100 mg 3 times daily+ SFU +0.28 -0.73† -33 -81†
8 (non-U.S.) Placebo + SFU +0.16 --- +10 ---
GLYSET 100 mg 3 times daily+ SFU -0.50 -0.66† -36 -46†
* Mean baseline ranged from 8.56 to 9.16% in these studies. 
** The result of subtracting the placebo group average. 
† p ≤ 0.05

 

Figure 1 : HbAc (%) Mean Change From Baseline: Treatment Effect Pooled Results from Controlled Fixed-Dose Studies in Tables 1 and 2

HbAc (%) Mean Change From Baseline -  Illustration

 

Figure 2 : 1-Hour Postprandial Plasma Glucose Mean Change From Baseline: Treatment Effect Pooled Results from Controlled Fixed-Dose Studies in Table 1 and 2

Plasma Glucose Mean Change From Baseline - Illustration

 

Because of its mechanism of action, the primary pharmacologic effect of miglitol is manifested as a reduction in postprandial plasma glucose, as shown previously in all of the major clinical trials. GLYSET was statistically significantly different from placebo at all doses in each of the individual studies with respect to effect on mean one-hour postprandial plasma glucose, and there is a dose response from 25 to 100 mg 3 times daily for this efficacy parameter.

This monograph has been modified to include the generic and brand name in many 

Patient Information

The following information should be provided to patients:

  • GLYSET should be taken orally three times a day at the start of each main meal. It is important to continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose.
  • GLYSET itself does not cause hypoglycemia when administered to patients in the fasted state. Sulfonylurea drugs and insulin, however, can lower blood sugar levels and cause symptoms or life-threatening hypoglycemia. Because GLYSET given in combination with a sulfonylurea or insulin will cause a further lowering of blood sugar, it may increase the hypoglycemic potential of these agents. The risk of hypoglycemia, its symptoms and treatment, and conditions thatpredispose to its development should be well understood by patients and responsible family members. Because GLYSET prevents the breakdown of table sugar, a source of glucose (dextrose, D-glucose) should be readily available to treat symptoms of low blood sugar when taking GLYSET in combination with a sulfonylurea or insulin.
  • If side effects occur with GLYSET, they usually develop during the first few weeks of therapy. They are most commonly mild-to-moderate dose-related gastrointestinal effects, such as flatulence, soft stools, diarrhea, or abdominal discomfort, and generally diminish in frequency and intensity with time. Discontinuation of drug usually results in rapidresolution of these gastrointestinal symptoms.

Physician Counseling Information for Patients

In initiating treatment for type 2 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. Use of GLYSET or other antidiabetic medications must be viewed by both the physician and patient as a treatment in addition to diet and not as a substitution 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 GLYSET or other antidiabetic medications. Maintenance or discontinuation of GLYSET or other antidiabetic medications should be based on clinical judgment using regular clinical and laboratory evaluations.

This monograph has been modified to include the generic and brand name in many instances.

Consumer Overview Uses

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

MIGLITOL - ORAL

 

(MIG-lih-tall)

 

COMMON BRAND NAME(S): Glyset

 

USES: Miglitol is used along with a proper diet and exercise program to control high blood sugar in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems. Proper control of diabetes may also lessen your risk of a heart attack or stroke. Miglitol works by slowing the absorption of carbohydrates from your diet, so that your blood sugar does not rise as much after a meal.

 

HOW TO USE: Take this medication by mouth, usually 3 times daily with the first bite of a meal, or as directed by your doctor. The dosage is based on your medical condition and response to therapy.

Use this medication regularly in order to get the most benefit from it. Remember to use it at the same times each day.

Consumer Overview Side Effect

SIDE EFFECTS: Diarrhea, gas, upset stomach, or stomach pain may occur in the first few weeks of treatment as your body adjusts to this medication but usually improve with time. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Miglitol does not cause low blood sugar (hypoglycemia). However, this effect can occur if you also take other anti-diabetic drugs (e.g., sulfonylureas, insulin) and if you do not consume enough calories (from food, juices, fruit, etc.). The symptoms include chills, cold sweat, blurred vision, dizziness, drowsiness, shaking, rapid heart rate, weakness, headache, fainting, tingling of the hands or feet, or hunger. Do not use table sugar or drink non-diet soda to relieve these symptoms because miglitol delays the breakdown of table sugar. Carry glucose tablets or gel with you to treat low blood sugar. If you are in a situation where you don't have these reliable forms of glucose, eat some honey or drink a glass of orange juice to quickly raise your blood sugar level. Tell your doctor immediately about the reaction. To help prevent hypoglycemia, eat meals on a regular schedule and do not skip meals.

Check with your doctor or pharmacist about what you should do if you miss a meal.

Symptoms of high blood sugar (hyperglycemia) include thirst, increased urination, confusion, drowsiness, flushing, rapid breathing, or fruity breath odor. If these symptoms occur, tell your doctor immediately. Your medication dosage may need to be increased or you may need other drugs.

This medication may rarely cause a serious intestinal condition (pneumatosis cystoides intestinalis). Tell your doctor right away if you develop: persistent diarrhea, constipation, blood/mucus in stool.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

Read the Glyset (miglitol) Side Effects Center for a complete guide to possible side effects

Learn More »
 

PRECAUTIONS: Before taking miglitol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: intestine/bowel problems (e.g., inflammatory bowel disease, intestinal blockage, digestion/absorption disorders).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease.

You may experience blurred vision, dizziness, or drowsiness due to extremely low or high blood sugar levels. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages because it can increase the risk of developing hypoglycemia.

During times of stress, such as fever, infection, injury or surgery, it may be more difficult to control your blood sugar. Consult your doctor, as a change in your medication or how often you test your blood sugar may be required.

This medication should be used only when clearly needed during pregnancy. Your doctor may substitute insulin for this drug during your pregnancy. Follow all instructions carefully. Discuss the risks and benefits with your doctor.

This drug passes into breast milk. Consult your doctor before breast-feeding.

Consumer Overview Missed Dose

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop, or change the dosage of any medicine before checking with them first.

This drug should not be used with the following medications because very serious interactions may occur: activated charcoal, drugs that help digestion (e.g., amylase, pancreatin).

If you are currently using any of these medications listed above, tell your doctor or pharmacist before starting miglitol.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: pramlintide.

Beta-blocker medications (e.g., metoprolol, propranolol, glaucoma eye drops such as timolol) may prevent the fast/pounding heartbeat you would usually feel when your blood sugar level falls too low (hypoglycemia). Other symptoms of low blood sugar such as dizziness, hunger, or sweating are unaffected by these drugs.

Many drugs can affect your blood sugar levels, making it more difficult to control your blood sugar. Before you start, stop, or change any medication, talk with your doctor or pharmacist about how the medication may affect your blood sugar. Check your blood sugar levels regularly as directed by your doctor. Tell your doctor about the results and of any symptoms of high or low blood sugar. (See also Side Effects section.) Your doctor may need to adjust your anti-diabetic medication, exercise program, or diet.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

 

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

 

NOTES: Do not share this medication with others.

It is recommended that you attend a diabetes education program to understand diabetes and all the important aspects of its treatment including meals/diet, exercise, personal hygiene, medications, and getting regular eye, foot and medical exams.

Keep all medical appointments. Laboratory and/or medical tests (e.g., kidney function tests, fasting and after-meal blood glucose levels, hemoglobin A1c) should be performed periodically to monitor for side effects and response to therapy. Regularly check your blood sugar levels if so directed by your doctor or pharmacist.

 

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

STORAGE: Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

 

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

 

Information last revised March 2014. Copyright(c) 2014 First Databank, Inc.

Patient Detailed Side Effect

Brand Names: Glyset

Generic Name: miglitol (Pronunciation: MIG lih tall)

  • What is miglitol (Glyset)?
  • What are the possible side effects of miglitol (Glyset)?
  • What is the most important information I should know about miglitol (Glyset)?
  • Who should not take miglitol (Glyset)?
  • How should I take miglitol (Glyset)?
  • What happens if I miss a dose (Glyset)?
  • What happens if I overdose (Glyset)?
  • What should I avoid while taking miglitol (Glyset)?
  • What other drugs will affect miglitol (Glyset)?
  • Where can I get more information?

What is miglitol (Glyset)?

 

Miglitol delays the digestion of carbohydrates (forms of sugar) in your body. This decreases the amount of sugar that passes into your blood after a meal and prevents periods of hyperglycemia (high blood sugar).

Miglitol is used to treat non-insulin-dependent (Type II) diabetes mellitus.

Miglitol may also be used for purposes other than those listed in this medication guide.

Glyset 100 mg

round, white, imprinted with 100, GLYSET

What are the possible side effects of miglitol (Glyset)?

 

Stop taking miglitol and seek emergency medical attention if you experience an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives).

Other, less serious side effects, are more likely to occur. Continue to take miglitol and talk to your doctor if you experience

  • abdominal pain,
  • diarrhea,
  • flatulence, or
  • a rash.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

Read the Glyset (miglitol) Side Effects Center for a complete guide to possible side effects

Learn More »
 

What is the most important information I should know about miglitol (Glyset)?

 

Take each dose of miglitol with the first bite of a main meal.

Know the signs and symptoms of low blood sugar, which include headache, drowsiness, weakness, dizziness, fast heartbeat, sweating, tremor, and, nausea. Carry glucose tablets, paste, or another glucose or dextrose substance to treat episodes of low blood sugar.

Side Effects Centers
  • Glyset

Patient Detailed How Take

Who should not take miglitol (Glyset)?

 

Before taking this medication, tell your doctor if you have

  • an inflammatory bowel disease, such as ulcerative colitis or Chron's disease; or any other disease of the stomach or intestines;
  • ulcers of the colon;
  • a blockage or obstruction in your intestines; or
  • kidney disease.

You may not be able to take miglitol, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Call your doctor if you develop a fever or an infection, or if you experience a serious injury. You may require insulin for a period of time to control your blood sugar levels.

Miglitol is in the FDA pregnancy category B. This means that it is not expected to harm an unborn baby. Do not take miglitol without first talking to your doctor if you are pregnant.

Miglitol passes into breast milk and may affect a nursing infant. Do not take miglitol without first talking to your doctor if you are breast-feeding a baby.

How should I take miglitol (Glyset)?

 

Take miglitol exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass of water.

Take each dose with the first bite of a main meal.

Store miglitol at room temperature away from moisture and heat.

Side Effects Centers
  • Glyset

Patient Detailed Avoid Taking

What happens if I miss a dose (Glyset)?

 

Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication.

What happens if I overdose (Glyset)?

 

Seek emergency medical attention.

An overdose of this medication is unlikely to occur. Symptoms of an overdose are unknown, but stomach pain, gas, bloating, and diarrhea might be expected.

What should I avoid while taking miglitol (Glyset)?

 

Follow your doctor's diet and exercise recommendations to help control your blood sugar levels.

Use alcohol cautiously. Alcohol may affect your blood sugar levels.

What other drugs will affect miglitol (Glyset)?

 

Digestive-enzyme supplements such as pancreatin (amylase, protease, lipase) in products such as Arco-Lase, Cotazym, Donnazyme, Pancrease, Creon, Ku-Zyme, and others may decrease the effects of miglitol. These medications should not be taken at the same time as miglitol.

Before taking this medication, tell your doctor if you are taking any of the following medicines:

  • propranolol (Inderal);
  • ranitidine (Zantac, Zantac 75);
  • digoxin (Lanoxin, Lanoxicaps),
  • another diabetes medicine such as glyburide (Micronase, Diabeta, Glynase), glipizide (Glucotrol), tolbutamide (Orinase), metformin (Glucophage), and others;
  • a thiazide diuretic (water pill) such as hydrochlorothiazide (HCTZ, Hydrodiuril, others), chlorothiazide (Diuril), chlorthalidone (Thalitone), indapamide (Lozol), and others;
  • a steroid medication such as prednisone (Deltasone), methylprednisolone (Medrol), and others;
  • an estrogen (Premarin, Ogen, and others) or an estrogen-containing birth control pill;
  • a thyroid medication (Synthroid, Levoxyl, and others);
  • phenytoin (Dilantin); or
  • a calcium channel blocker such as verapamil (Calan, Verelan, Isoptin), diltiazem (Cardizem, Dilacor XR), nifedipine (Procardia, Adalat), and others.

The drugs listed above may interact with miglitol or affect blood sugar levels. You may require a dosage adjustment or special monitoring during treatment if you are taking any of the medicines listed above.

Drugs other than those listed here may also interact with miglitol or affect your condition. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines.

Where can I get more information?

 

Your pharmacist has more information about miglitol written for health professionals that you may read.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2013 Cerner Multum, Inc. Version: 1.05. Revision date: 12/15/2010.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

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