Acarbose

Name: Acarbose

How should I take acarbose?

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Take acarbose with the first bite of a main meal, unless your doctor tells you otherwise.

Your blood sugar will need to be checked often, and you may need other blood tests at your doctor's office.

If you take acarbose with insulin or other diabetes medications, your blood sugar could get too low.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, confusion, irritability, dizziness, or feeling shaky. Always keep a source of dextrose (D-glucose) with you in case you have low blood sugar. When taking acarbose, dextrose will work better than cane sugar or table sugar in treating hypoglycemia. Sources of dextrose include honey, dates, raisins, plums, dried prunes, grapes, or glucose tablets. Be sure your family and close friends know how to help you in an emergency.

If you have severe hypoglycemia and cannot eat or drink, use a glucagon injection. Your doctor can prescribe a glucagon emergency injection kit and tell you how to use it.

Also watch for signs of high blood sugar (hyperglycemia) such as increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, and weight loss.

Check your blood sugar carefully during times of stress, travel, illness, surgery or medical emergency, vigorous exercise, or if you drink alcohol or skip meals. These things can affect your glucose levels and your dose needs may also change. Do not change your medication dose or schedule without your doctor's advice.

Acarbose is only part of a complete treatment program that may also include diet, exercise, weight control, regular blood sugar testing, and special medical care. Follow your doctor's instructions very closely.

Store at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.

Uses for Acarbose

Diabetes Mellitus

Used as monotherapy as an adjunct to diet and exercise for the management of type 2 (noninsulin-dependent) diabetes mellitus (NIDDM) in patients whose hyperglycemia cannot be controlled by diet and exercise alone.1 6 14 47

Also used as adjunct to diet and exercise in combination with metformin, a sulfonylurea, or insulin for management of type 2 diabetes mellitus in patients whose hyperglycemia cannot be controlled with acarbose, metformin, insulin, or sulfonylurea monotherapy, diet, and exercise.1 3 6 14 23 26 44 47

Metformin generally recommended over other antidiabetic agents for initial oral antidiabetic therapy because of absence of weight gain or hypoglycemia, relatively lower expense and greater efficacy, and generally low adverse effect profile.110

ADA and other clinicians prefer addition of an insulin, a sulfonylurea, or a thiazolidinedione over an α-glucosidase inhibitor (e.g., acarbose), pramlintide, exenatide, or a meglitinide (e.g., repaglinide, nateglinide) as second-line therapy in patients inadequately controlled on metformin monotherapy because of relatively lesser efficacy, limited clinical data, frequent GI adverse effects, and/or greater cost with the latter agents.110

Acarbose should not be used as sole antidiabetic therapy in patients whose diabetes is complicated by ketoacidosis with or without coma (e.g., type 1 [insulin-dependent, IDDM] diabetes mellitus); instead, such patients should receive insulin.1 57

Proper Use of acarbose

Follow carefully the special meal plan your doctor gave you. This is the most important part of controlling your condition, and is necessary if the medicine is to work properly. Also, exercise regularly and test for sugar in your blood or urine as directed.

For acarbose to work properly it must be taken at the beginning of each main meal.

Dosing

The dose of acarbose will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of acarbose. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For type 2 diabetes:
      • Adults—At first the dose is 25 milligrams (mg) three times a day, at the start of each main meal. Your dose may then be adjusted by your doctor.
      • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of acarbose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you finish a meal and you have forgotten to take the medicine, do not take the missed dose. Instead, take the next dose at the beginning of your next meal, as scheduled.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using acarbose

Your doctor will want to check your progress at regular visits , especially during the first few weeks you take acarbose.

It is very important to follow carefully any instructions from your health care team about:

  • Alcohol—Drinking alcohol may cause severe low blood sugar. Discuss this with your health care team.
  • Other medicines—Do not take other medicines during the time you are taking acarbose unless they have been discussed with your doctor. This especially includes nonprescription medicines such as aspirin, and medicines for appetite control, asthma, colds, cough, hay fever, or sinus problems.
  • Counseling—Other family members need to learn how to prevent side effects or help with side effects if they occur. Also, patients with diabetes may need special counseling about diabetes medicine dosing changes that might occur because of lifestyle changes, such as changes in exercise and diet. Furthermore, counseling on contraception and pregnancy may be needed because of the problems that can occur in patients with diabetes during pregnancy.
  • Travel—Keep a recent prescription and your medical history with you. Be prepared for an emergency as you would normally. Make allowances for changing time zones and keep your meal times as close as possible to your usual meal times.

In case of emergency—There may be a time when you need emergency help for a problem caused by your diabetes. You need to be prepared for these emergencies. It is a good idea to wear a medical identification (ID) bracelet or neck chain at all times. Also, carry an ID card in your wallet or purse that says that you have diabetes and a list of all of your medicines.

Acarbose does not cause hypoglycemia (low blood sugar). However, low blood sugar can occur if you take acarbose with another type of diabetes medicine, delay or miss a meal or snack, exercise more than usual, drink alcohol, or cannot eat because of nausea or vomiting. Symptoms of low blood sugar must be treated before they lead to unconsciousness (passing out). Different people may feel different symptoms of low blood sugar. It is important that you learn which symptoms of low blood sugar you usually have so that you can treat it quickly.

Symptoms of low blood sugar include anxiety; behavior change similar to being drunk; blurred vision; cold sweats; confusion; cool, pale skin; difficulty in thinking; drowsiness; excessive hunger; fast heartbeat; headache (continuing); nausea; nervousness; nightmares; restless sleep; shakiness; slurred speech; or unusual tiredness or weakness.

If symptoms of low blood sugar occur, eat glucose tablets or gel or honey, or drink fruit juice to relieve the symptoms. Table sugar (sucrose) or regular (nondiet) soft drinks will not work. Also, check your blood for low blood sugar. Glucagon is used in emergency situations when severe symptoms such as seizures (convulsions) or unconsciousness occur. Have a glucagon kit available, along with a syringe and needle, and know how to use it. Members of your household also should know how to use it.

Hyperglycemia (high blood sugar) may occur if you do not take enough or skip a dose of your antidiabetic medicine, overeat or do not follow your meal plan, have a fever or infection, or do not exercise as much as usual.

Symptoms of high blood sugar include blurred vision; drowsiness; dry mouth; flushed, dry skin; fruit-like breath odor; increased urination; ketones in urine; loss of appetite; stomachache, nausea, or vomiting; tiredness; troubled breathing (rapid and deep); unconsciousness; or unusual thirst.

If symptoms of high blood sugar occur, check your blood sugar level and then call your doctor for instructions.

How is this medicine (Acarbose) best taken?

Use acarbose as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take with the first bite of each meal.
  • Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.
  • If you take charcoal or digestive enzyme preparations, talk to your doctor about how to take them with acarbose.

What do I do if I miss a dose?

  • Skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.

How do I store and/or throw out Acarbose?

  • Store at room temperature.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.

Acarbose Description

Acarbose Tablets are an oral alpha-glucosidase inhibitor for use in the management of type 2 diabetes mellitus. Acarbose is an oligosaccharide which is obtained from fermentation processes of a microorganism, Actinoplanes utahensis, and is chemically known as O-4,6-dideoxy-4-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-α-D-glucopyranosyl-(1→4)-O-α-D-glucopyranosyl-(1→4)-D-glucose. It is a white to off-white powder with a molecular weight of 645.6. Acarbose is soluble in water and has a pKa of 5.1. Its empirical formula is C25H43NO18 and its chemical structure is as follows:

Acarbose Tablets are available as 25 mg, 50 mg and 100 mg tablets for oral use. The inactive ingredients are corn starch, magnesium stearate, microcrystalline cellulose and colloidal silicon dioxide.

Clinical Trials

Clinical Experience from Dose Finding Studies in Type 2 Diabetes Mellitus Patients on Dietary Treatment Only

Results from six controlled, fixed-dose, monotherapy studies of Acarbose Tablets in the treatment of type 2 diabetes mellitus, involving 769 Acarbose Tablets-treated patients, were combined and a weighted average of the difference from placebo in the mean change from baseline in glycosylated hemoglobin (HbA1c) was calculated for each dose level as presented below:

Table 1
Mean Placebo-Subtracted Change in HbA1c in Fixed-Dose Monotherapy Studies
Dose of Acarbose Tablets* N Change in HbA1c p-Value
* Acarbose Tablets were statistically significantly different from placebo at all doses. Although there were no statistically significant differences among the mean results for doses ranging from 50 to 300 mg t.i.d., some patients may derive benefit by increasing the dosage from 50 to 100 mg t.i.d. † Although studies utilized a maximum dose of 200 or 300 mg t.i.d., the maximum recommended dose for patients < 60 kg is 50 mg t.i.d.; the maximum recommended dose for patients > 60 kg is 100 mg t.i.d.
25 mg t.i.d. 110 -0.44 0.0307
50 mg t.i.d. 131 -0.77 0.0001
100 mg t.i.d. 244 -0.74 0.0001
200 mg t.i.d.† 231 -0.86 0.0001
300 mg t.i.d.† 53 -1.00 0.0001

Results from these six fixed-dose, monotherapy studies were also combined to derive a weighted average of the difference from placebo in mean change from baseline for one-hour postprandial plasma glucose levels as shown in the following Figure.

Figure 1
* Acarbose Tablets were statistically significantly different from placebo at all doses with respect to effect on one-hour postprandial plasma glucose.
** The 300 mg t.i.d. Acarbose Tablets regimen was superior to lower doses, but there were no statistically significant differences from 50 to 200 mg t.i.d.
Dose of Acarbose Tablets (t.i.d.)*

Clinical Experience in Type 2 Diabetes Mellitus Patients on Monotherapy, or in Combination with Sulfonylureas, Metformin or Insulin

Acarbose Tablets were studied as monotherapy and as combination therapy to sulfonylurea, metformin, or insulin treatment. The treatment effects on HbA1c levels and one-hour postprandial glucose levels are summarized for four placebo-controlled, double-blind, randomized studies conducted in the United States in Tables 2 and 3, respectively. The placebo-subtracted treatment differences, which are summarized below, were statistically significant for both variables in all of these studies.

Study 1 (n=109) involved patients on background treatment with diet only. The mean effect of the addition of Acarbose Tablets to diet therapy was a change in HbA1c of -0.78%, and an improvement of one-hour postprandial glucose of -74.4 mg/dL.

In Study 2 (n=137), the mean effect of the addition of Acarbose Tablets to maximum sulfonylurea therapy was a change in HbA1c of -0.54%, and an improvement of one-hour postprandial glucose of -33.5 mg/dL.

In Study 3 (n=147), the mean effect of the addition of Acarbose Tablets to maximum metformin therapy was a change in HbA1c of -0.65%, and an improvement of one-hour postprandial glucose of -34.3 mg/dL.

Study 4 (n=145) demonstrated that Acarbose Tablets added to patients on background treatment with insulin resulted in a mean change in HbA1c of -0.69%, and an improvement of one-hour postprandial glucose of -36.0 mg/dL.

A one year study of Acarbose Tablets as monotherapy or in combination with sulfonylurea, metformin or insulin treatment was conducted in Canada in which 316 patients were included in the primary efficacy analysis (Figure 2). In the diet, sulfonylurea and metformin groups, the mean decrease in HbA1c produced by the addition of Acarbose Tablets was statistically significant at six months, and this effect was persistent at one year. In the Acarbose Tablets-treated patients on insulin, there was a statistically significant reduction in HbA1c at six months, and a trend for a reduction at one year.

Table 2: Effect of Acarbose Tablets on HbA1c
HbA1c(%)*
Study Treatment Mean Baseline Mean change from baseline† Treatment Difference p-Value
* HbA1c Normal Range: 4 to 6% † After four months treatment in Study 1, and six months in Studies 2, 3, and 4 ‡ SFU, sulfonylurea, maximum dose § Although studies utilized a maximum dose of up to 300 mg t.i.d., the maximum recommended dose for Patients ≤ 60 kg is 50 mg t.i.d.; the maximum recommended dose for patients > 60 kg is 100 mg t.i.d. ¶ Metformin dosed at 2000 mg/day or 2500 mg/day # Results are adjusted to a common baseline of 8.33% Þ Mean dose of insulin 61 U/day
1 Placebo Plus Diet 8.67 +0.33 - -
Acarbose Tablets 100 mg t.i.d. Plus Diet 8.69 -0.45 -0.78 0.0001
2 Placebo Plus SFU‡ 9.56 +0.24 - -
Acarbose Tablets 50 to 300§ mg t.i.d. Plus SFU‡ 9.64 -0.30 -0.54 0.0096
3 Placebo Plus Metformin¶  8.17 +0.08# - -
Acarbose Tablets 50 to 100 mg t.i.d Plus Metformin¶ 8.46 -0.57# -0.65 0.0001
4 Placebo Plus InsulinÞ 8.69 +0.11 - -
Acarbose Tablets 50 to 100 mg t.i.d. Plus InsulinÞ 8.77 -0.58 -0.69 0.0001
Table 3: Effect of Acarbose Tablets on Postprandial Glucose
One-Hour Postprandial Glucose (mg/dL)
Study Treatment Mean Baseline Mean change from baseline* Treatment Difference p-Value
* After four months treatment in Study 1, and six months in Studies 2, 3, and 4 † SFU, sulfonylurea, maximum dose ‡ Although studies utilized a maximum dose of up to 300 mg t.i.d., the maximum recommended dose for patients ≤ 60 kg is 50 mg t.i.d.; the maximum recommended dose for patients > 60 kg is 100 mg t.i.d. § Metformin dosed at 2000 mg/day or 2500 mg/day ¶ Results are adjusted to a common baseline of 273 mg/dL # Mean dose of insulin 61 U/day
1 Placebo Plus Diet 297.1 +31.8 - -
Acarbose Tablets 100 mg t.i.d. Plus Diet 299.1 -42.6 -74.4 0.0001
2 Placebo Plus SFU† 308.6 +6.2 - -
Acarbose Tablets 50 to 300‡ mg t.i.d. Plus SFU† 311.1 -27.3 -33.5 0.0017
3 Placebo Plus Metformin§  263.9 +3.3¶ - -
Acarbose Tablets 50 to 100 mg t.i.d Plus Metformin§ 283.0 -31.0¶ -34.3 0.0001
4 Placebo Plus Insulin# 279.2 +8.0 - -
Acarbose Tablets 50 to 100 mg t.i.d. Plus Insulin# 277.8 -28.0 -36.0 0.0178
Figure 2

Figure 2: Effects of Acarbose Tablets (■) and Placebo (•) on mean change in HbA1c levels from baseline throughout a one-year study in patients with type 2 diabetes mellitus when used in combination with: (A) diet alone; (B) sulfonylurea; (C) metformin; or (D) insulin. Treatment differences at 6 and 12 months were tested:
* p < 0.01; # p = 0.077.

PRINCIPAL DISPLAY PANEL - 50 mg Tablet Bottle Label

NDC 69543-121-10

Acarbose
Tablets 50 mg

Rx only

100 Tablets

VIRTUS
PHARMACEUTICALS

Pronunciation

(AY car bose)

Monitoring Parameters

Postprandial glucose, hemoglobin A1c (at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change [ADA 2017a]), serum creatinine; serum transaminase levels every 3 months during the first year of treatment and periodically thereafter.

Patient information

Patients should be told to take PRECOSE orally three times a day at the start (with the first bite) of each main meal. It is important that patients continue to adhere to dietary instructions, a regular exercise program, and regular testing of urine and/or blood glucose.

PRECOSE itself does not cause hypoglycemia even when administered to patients in the fasted state. Sulfonylurea drugs and insulin, however, can lower blood sugar levels enough to cause symptoms or sometimes life-threatening hypoglycemia. Because PRECOSE 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. Hypoglycemia does not occur in patients receiving metformin alone under usual circumstances of use, and no increased incidence of hypoglycemia was observed in patients when PRECOSE was added to metformin therapy. The risk of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be well understood by patients and responsible family members. Because PRECOSE prevents the breakdown of table sugar, patients should have a readily available source of glucose (dextrose, D-glucose) to treat symptoms of low blood sugar when taking PRECOSE in combination with a sulfonylurea or insulin.

If side effects occur with PRECOSE, they usually develop during the first few weeks of therapy. They are most commonly mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort, and generally diminish in frequency and intensity with time.

Acarbose Brand Names

Acarbose may be found in some form under the following brand names:

  • Precose

Side Effects of Acarbose

Serious side effects have been reported with acarbose. See the “Acarbose Precautions” section.

Common side effects of acarbose include the following:

  • Abdominal pain
  • Diarrhea
  • Flatulence

This is not a complete list of acarbose side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

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

Acarbose Interactions

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

  • other medications for diabetes
  • digoxin (Lanoxin)
  • diuretics ('water pills')
  • estrogens
  • isoniazid
  • medications for high blood pressure or colds
  • oral contraceptives
  • pancreatic enzymes
  • phenytoin (Dilantin)
  • steroids
  • thyroid medications
  • vitamins

This is not a complete list of acarbose drug interactions. Ask your doctor or pharmacist for more information.

Inform MD

Before taking acarbose, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

  • are allergic to acarbose or to any of its ingredients
  • have kidney problems
  • have liver problems
  • have gastrointestinal problems
  • are pregnant or breastfeeding

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Acarbose and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if acarbose crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using acarbose.

Adverse Effects

>10%

abdominal pain (19%)

diarrhea (31%)

elevated serum transaminases

flatulence (74%)

Postmarketing Reports

Gastrointestinal: Fulminant hepatitis with fatal outcome, ileus/subileus, jaundice and/or hepatitis and associated liver damage

Hypersensitive skin reactions: rash, erythema, exanthema and urticaria

Edema

Thrombocytopenia

Pneumatosis cystoides intestinalis

Patient Handout

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What is the most important information i should know about acarbose (precose)?

Do not use this medication if you are allergic to acarbose, or if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin). You also should not use acarbose if you have inflammatory bowel disease, an ulcer or blockage in your intestines, or cirrhosis of the liver.

Before taking acarbose, tell your doctor if you have liver disease, or any type of stomach or intestinal disorder.

Take acarbose with the first bite of a main meal, unless your doctor tells you otherwise.

Your medication needs may change if you become sick or injured, if you have a serious infection, or if you have any type of surgery. Do not change your dose or stop taking acarbose without first talking to your doctor.

If you take acarbose with insulin or other diabetes medications, your blood sugar could get too low. Low blood sugar (hypoglycemia) can occur if you skip a meal, exercise too long, drink alcohol, or are under stress. Symptoms include headache, hunger, weakness, sweating, tremors, irritability, or trouble concentrating.

Carry hard candy or glucose tablets with you in case you have low blood sugar. Other sugar sources include orange juice and milk. Be sure your family and close friends know how to help you in an emergency.

Acarbose is only part of a complete program of treatment that may also include diet, exercise, weight control, foot care, eye care, dental care, and testing your blood sugar. Follow your diet, medication, and exercise routines very closely. Changing any of these factors can affect your blood sugar levels.

In Summary

Commonly reported side effects of acarbose include: abdominal pain, diarrhea, and flatulence. See below for a comprehensive list of adverse effects.

For the Consumer

Applies to acarbose: oral tablet

Along with its needed effects, acarbose may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur while taking acarbose:

Rare
  • Yellow eyes or skin

Some side effects of acarbose may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Abdominal or stomach pain
  • bloated feeling or passing of gas
  • diarrhea

Precautions

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

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