How does acarbose work to control blood sugar levels. What are the proper dosage instructions for acarbose. What are the potential side effects and precautions when taking acarbose. How should acarbose be stored and disposed of properly. What should patients know about acarbose and hypoglycemia management.

Understanding Acarbose: Mechanism of Action and Uses

Acarbose is a medication primarily prescribed for the management of type 2 diabetes. It belongs to a class of drugs known as alpha-glucosidase inhibitors. The primary function of acarbose is to slow down the digestion of complex carbohydrates, thereby helping to control blood sugar levels, particularly after meals.

How does acarbose work? Acarbose inhibits enzymes in the small intestine that are responsible for breaking down complex carbohydrates into simple sugars. By delaying this process, acarbose helps prevent rapid spikes in blood glucose levels that typically occur after eating carbohydrate-rich foods. This mechanism of action makes acarbose an effective tool in the overall management of type 2 diabetes when used in conjunction with diet and, in some cases, other diabetes medications.

Key Benefits of Acarbose

• Helps control post-meal blood sugar spikes
• Can be used alone or in combination with other diabetes medications
• May reduce the risk of diabetes-related complications when used as part of a comprehensive treatment plan
• Does not cause weight gain, which is beneficial for many diabetes patients

Is acarbose suitable for all types of diabetes? While acarbose is primarily prescribed for type 2 diabetes, it is not typically used for type 1 diabetes management. The medication’s effectiveness is most pronounced in individuals whose blood sugar levels are particularly high after meals.

Proper Administration and Dosage of Acarbose

Acarbose is available in tablet form and is typically taken three times daily. The correct administration of acarbose is crucial for its effectiveness and to minimize potential side effects.

Dosage Guidelines

• Initial dose: Usually 25 mg three times daily, taken with the first bite of each main meal
• Dose may be gradually increased to 50 mg or 100 mg three times daily, based on individual response and tolerability
• Maximum recommended dose: 100 mg three times daily

Why is timing important when taking acarbose? The effectiveness of acarbose is closely tied to meal timing. Taking the medication with the first bite of a meal ensures that it is present in the digestive system when carbohydrates begin to be processed, maximizing its blood sugar-lowering effect.

Can acarbose be taken on an empty stomach? Acarbose should not be taken on an empty stomach. It is specifically designed to work in conjunction with food intake, particularly meals containing carbohydrates. Taking it without food may lead to unnecessary side effects without providing the intended benefits.

Potential Side Effects and Precautions

While acarbose is generally well-tolerated, like all medications, it can cause side effects in some individuals. Understanding these potential side effects and knowing when to seek medical attention is crucial for patients taking acarbose.

Common Side Effects

• Flatulence (gas)
• Abdominal discomfort or pain
• Diarrhea
• Soft stools

Why do these gastrointestinal side effects occur? The side effects associated with acarbose are primarily related to its mechanism of action. By inhibiting the breakdown of complex carbohydrates in the small intestine, more undigested carbohydrates reach the large intestine. This can lead to increased gas production and changes in bowel habits.

Serious Side Effects

While rare, some patients may experience more serious side effects that require immediate medical attention:

• Severe abdominal pain
• Jaundice (yellowing of the skin or eyes)
• Unusual bleeding or bruising
• Signs of liver problems (e.g., persistent nausea, vomiting, dark urine)

When should patients contact their healthcare provider about side effects? Patients should seek medical advice if they experience persistent or severe gastrointestinal symptoms, signs of liver problems, or any other unusual or concerning symptoms while taking acarbose.

Drug Interactions and Contraindications

Acarbose can interact with various medications and may not be suitable for all patients. Understanding potential drug interactions and contraindications is essential for safe and effective use of acarbose.

Medications That May Interact with Acarbose

• Digestive enzymes (e.g., amylase, pancreatin)
• Activated charcoal
• Certain antibiotics
• Other diabetes medications, particularly those that can cause hypoglycemia

How do these interactions affect acarbose’s effectiveness? Some medications, such as digestive enzymes, may reduce the effectiveness of acarbose by counteracting its carbohydrate-blocking action. Others, like certain diabetes medications, may increase the risk of hypoglycemia when used in combination with acarbose.

Contraindications

Acarbose may not be suitable for individuals with:

• Inflammatory bowel disease
• Intestinal obstruction or predisposition to intestinal obstruction
• Chronic intestinal diseases associated with marked digestion or absorption disorders
• Severe liver or kidney disease
• Diabetic ketoacidosis

Why are these conditions contraindicated with acarbose use? These conditions can either be exacerbated by acarbose’s effects on the digestive system or may interfere with the proper metabolism and excretion of the medication, potentially leading to adverse effects.

Managing Hypoglycemia While Taking Acarbose

Hypoglycemia, or low blood sugar, is a potential risk for individuals taking diabetes medications, including acarbose. Understanding how to recognize and manage hypoglycemia is crucial for patients on acarbose therapy.

Symptoms of Hypoglycemia

• Shakiness or trembling
• Sweating
• Rapid heartbeat
• Confusion or difficulty concentrating
• Dizziness or lightheadedness
• Hunger
• Irritability or mood changes

How does acarbose affect hypoglycemia management? Unlike some other diabetes medications, acarbose does not directly cause hypoglycemia. However, when used in combination with insulin or sulfonylureas, it can contribute to low blood sugar episodes. Importantly, the standard treatment for hypoglycemia (consuming simple sugars) may not be as effective in patients taking acarbose.

Managing Hypoglycemia in Acarbose Users

For individuals experiencing hypoglycemia while on acarbose:

1. Use glucose tablets or gel as the preferred treatment
2. Avoid using table sugar, as acarbose will inhibit its breakdown
3. Monitor blood glucose levels closely
4. Seek medical attention if symptoms persist or worsen

Why is glucose the preferred treatment for hypoglycemia in acarbose users? Glucose is a simple sugar that can be absorbed directly into the bloodstream, bypassing the digestive enzymes inhibited by acarbose. This makes it a more effective and rapid treatment for low blood sugar in individuals taking this medication.

Long-Term Benefits and Considerations of Acarbose Therapy

While acarbose is primarily used for blood sugar control, its long-term use may offer additional benefits for individuals with type 2 diabetes. Understanding these potential advantages, as well as long-term considerations, can help patients and healthcare providers make informed decisions about acarbose therapy.

Potential Long-Term Benefits

• Reduced risk of cardiovascular complications
• Improved glycemic control over time
• Potential delay in the progression of type 2 diabetes
• Weight neutral effect, which may be beneficial for overweight or obese patients

How does acarbose contribute to these long-term benefits? By consistently controlling post-meal blood sugar spikes, acarbose may help reduce the overall burden of hyperglycemia on the body. This sustained glucose control can potentially lead to a lower risk of diabetes-related complications, particularly those affecting the cardiovascular system.

Long-Term Considerations

Patients and healthcare providers should consider the following factors when evaluating long-term acarbose therapy:

• Regular monitoring of liver function
• Potential need for vitamin B12 supplementation
• Ongoing assessment of gastrointestinal tolerance
• Periodic evaluation of overall diabetes management plan

Why is ongoing monitoring important for long-term acarbose users? Regular check-ups and monitoring help ensure that the medication remains safe and effective over time. They allow healthcare providers to adjust treatment plans as needed and address any emerging concerns promptly.

Proper Storage and Disposal of Acarbose

Proper storage and disposal of acarbose are essential for maintaining its effectiveness and ensuring safety. Understanding the correct procedures can help patients maximize the benefits of their medication while minimizing potential risks.

Storage Guidelines

• Store acarbose at room temperature, away from excessive heat and moisture
• Keep the medication in its original container, tightly closed
• Store away from direct sunlight
• Keep out of reach of children and pets

Why is proper storage important for acarbose? Correct storage helps maintain the medication’s potency and prevents degradation that could affect its effectiveness. It also reduces the risk of accidental ingestion by children or pets.

Disposal Instructions

When disposing of unused or expired acarbose:

1. Do not flush down the toilet or pour down the drain unless instructed to do so
2. Use community drug take-back programs when available
3. If no take-back program is available, mix the medication with an undesirable substance (e.g., used coffee grounds), seal in a plastic bag, and dispose of in household trash
4. Remove or destroy any personal information on the empty medication container before disposal

Why is proper disposal of acarbose important? Correct disposal methods help prevent environmental contamination and reduce the risk of accidental ingestion or misuse by others. It’s part of responsible medication management and contributes to overall community safety.

Acarbose in Combination Therapy for Type 2 Diabetes

While acarbose can be effective as a monotherapy for some patients with type 2 diabetes, it is often used in combination with other diabetes medications. Understanding the role of acarbose in combination therapy can help patients and healthcare providers optimize diabetes management strategies.

Common Combination Therapies

• Acarbose with metformin
• Acarbose with sulfonylureas
• Acarbose with insulin
• Acarbose with DPP-4 inhibitors

How does combining acarbose with other medications enhance diabetes management? Each class of diabetes medication works through different mechanisms. By combining acarbose with other drugs, healthcare providers can target multiple aspects of blood sugar control, potentially leading to better overall glycemic management.

Considerations for Combination Therapy

When using acarbose in combination with other diabetes medications, healthcare providers and patients should consider:

• Increased risk of hypoglycemia, especially when combined with insulin or sulfonylureas
• Potential for drug interactions
• Need for more frequent blood glucose monitoring
• Adjustments in dosage of individual medications

Why is careful monitoring important in combination therapy? Combining multiple diabetes medications can increase the complexity of treatment and the potential for side effects or interactions. Close monitoring allows for timely adjustments to the treatment plan, ensuring optimal efficacy and safety.

In conclusion, acarbose plays a valuable role in the management of type 2 diabetes, both as a standalone therapy and in combination with other medications. Its unique mechanism of action, focusing on post-meal blood sugar control, makes it a useful tool in the diabetes management arsenal. However, like all medications, it requires careful consideration of dosing, potential side effects, and long-term management strategies. Patients taking acarbose should work closely with their healthcare providers to ensure safe and effective use of the medication, tailoring the treatment plan to their individual needs and circumstances. With proper use and monitoring, acarbose can contribute significantly to improved glycemic control and potentially reduce the risk of diabetes-related complications.

Acarbose: MedlinePlus Drug Information

pronounced as (ay’ car bose)

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Acarbose is used (with diet only or diet and other medications) to treat type 2 diabetes (condition in which the body does not use insulin normally and therefore cannot control the amount of sugar in the blood) . Acarbose works by slowing the action of certain chemicals that break down food to release glucose (sugar) into your blood. Slowing food digestion helps keep blood glucose from rising very high after meals.

Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.

Acarbose comes as a tablet to take by mouth. It is usually taken three times a day. It is very important to take each dose with the first bite of each main meal. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take acarbose exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Continue to take acarbose even if you feel well. Do not stop taking acarbose without talking to your doctor.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

Before taking acarbose,

• tell your doctor and pharmacist if you are allergic to acarbose or any other drugs.
• tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially 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, and vitamins.
• tell your doctor if you have or have ever had ketoacidosis, cirrhosis, or intestinal disease such as inflammatory bowel disease or bowel obstruction.
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking acarbose, call your doctor.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acarbose.

Be sure to follow all exercise and dietary recommendations made by your doctor or dietitian. It is important to eat a healthful diet.

Alcohol may cause a decrease in blood sugar. Ask your doctor about the safe use of alcoholic beverages while you are taking acarbose.

Take the missed dose as soon as you remember it. If you will be having a snack soon, take a dose with the snack. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

When used in combination with insulin or other medications used to treat diabetes, acarbose may cause excessive lowering of blood sugar levels.

If you have any of these symptoms, glucose products (Insta-Glucose or B-D Glucose tablets) should be used and you should call your doctor.

Because acarbose blocks the breakdown of table sugar and other complex sugars, fruit juice or other products containing these sugars will not help to increase blood sugar. It is important that you and other members of your household understand this difference between acarbose and other medications used to treat diabetes.

• shakiness
• dizziness or lightheadedness
• sweating
• nervousness or irritability
• sudden changes in behavior or mood
• headache
• numbness or tingling around the mouth
• weakness
• pale skin
• hunger
• clumsy or jerky movements

If hypoglycemia is not treated, severe symptoms may develop. Be sure that your family, friends, and other people who spend time with you know that if you have any of the following symptoms, they should get medical treatment for you immediately.

• confusion
• seizures
• loss of consciousness

Call your doctor immediately if you have any of the following symptoms of hyperglycemia (high blood sugar):

• extreme thirst
• frequent urination
• extreme hunger
• weakness
• blurred vision

If high blood sugar is not treated, a serious, life-threatening condition called diabetic ketoacidosis could develop.

Call your doctor immediately if you have any of the these symptoms:

• dry mouth
• upset stomach and vomiting
• shortness of breath
• breath that smells fruity
• decreased consciousness

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

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Last Revised – 12/15/2017

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Acarbose Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Uses

Acarbose is used 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. Acarbose works in your intestines to slow the breakdown and absorption of carbohydrates from foods that you eat. This effect helps lessen your blood sugar rise after a meal.

How to use Acarbose

Take this medication by mouth as directed by your doctor, usually 3 times daily with the first bite of a meal. The dosage is based on your medical condition and response to treatment. To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor’s instructions carefully.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Tell your doctor if your condition does not get better or if it gets worse (your blood sugar is too high or too low).

Side Effects

Diarrhea, gas, or abdominal discomfort/pain may occur as your body adjusts to this medication during the first few weeks. These side effects usually lessen with time. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Remember that this medication has been prescribed because your doctor 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.

Tell your doctor right away if you have any serious side effects, including: signs of liver problems (such as nausea/vomiting that doesn’t stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).

Acarbose does not usually cause low blood sugar (hypoglycemia). Low blood sugar may occur if this drug is prescribed with other diabetes medications, or if you do not consume enough calories from food, or if you do unusually heavy exercise. Talk with your doctor or pharmacist about whether the dose of your other diabetes medication(s) needs to be lowered.

Symptoms of low blood sugar include sudden sweating, shaking, fast heartbeat, hunger, blurred vision, dizziness, or tingling hands/feet. Do not use table sugar or drink non-diet soda to relieve these symptoms because acarbose slows the breakdown of table sugar. Carry glucose tablets or gel with you to treat low blood sugar. If 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. Tell your doctor right away about the reaction and the use of this product. To help prevent low blood sugar, eat meals on a regular schedule and do not skip meals. Check with your doctor or pharmacist to find out what you should do if you miss a meal.

Symptoms of high blood sugar (hyperglycemia) include thirst, increased urination, confusion, drowsiness, flushing, rapid breathing, and fruity breath odor. If these symptoms occur, tell your doctor right away. Your 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: diarrhea that doesn’t stop, constipation, blood/mucus in stool.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: 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 or at www.fda.gov/medwatch.

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

Precautions

Before taking acarbose, 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.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: intestine/bowel problems (such as inflammatory bowel disease, blockage, ulcers), kidney problems, liver disease.

You may experience blurred vision, dizziness, or drowsiness due to extremely low or high blood sugar. 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 alcohol while taking this medication because it can increase your risk of developing low blood sugar.

It may be harder to control your blood sugar when your body is stressed (such as due to fever, infection, injury, or surgery). Consult your doctor because this may require a change in your treatment plan, medications, or blood sugar testing.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

Pregnancy may cause or worsen diabetes. Discuss a plan with your doctor for managing your blood sugar while pregnant. Your doctor may change your diabetes treatment during your pregnancy (such as diet and medications including insulin).

It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Some products that may interact with this drug are: charcoal products taken by mouth, digestive enzyme products (such as amylase, pancreatin), pramlintide.

Beta blocker medications (such as metoprolol, propranolol, glaucoma eye drops such as timolol) may prevent the fast/pounding heartbeat you would usually feel when your blood sugar falls too low (hypoglycemia). Other symptoms of low blood sugar, such as dizziness, hunger, or sweating, are not affected by these drugs.

Many drugs can affect your blood sugar, making it harder to control. 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 regularly as directed and share the results with your doctor. Tell your doctor right away if you have symptoms of high or low blood sugar. (See also Side Effects section.) Your doctor may need to adjust your diabetes medication, exercise program, or diet.

Does Acarbose interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications 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.

Images

acarbose 100 mg tablet

Color: whiteShape: roundImprint: 54 251

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 50 mg tablet

Color: whiteShape: roundImprint: 54 737

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 25 mg tablet

Color: whiteShape: roundImprint: 54 311

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 100 mg tablet

Color: whiteShape: roundImprint: 320 cor

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 50 mg tablet

Color: whiteShape: roundImprint: 319 cor

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 25 mg tablet

Color: whiteShape: roundImprint: 318 cor

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 100 mg tablet

Color: whiteShape: roundImprint: HP 149

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 50 mg tablet

Color: whiteShape: roundImprint: HP 148

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 25 mg tablet

Color: whiteShape: roundImprint: HP 147

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 50 mg tablet

Color: whiteShape: roundImprint: P211 50

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 100 mg tablet

Color: whiteShape: roundImprint: P212 100

This medicine is a white, round, tablet imprinted with “54 251”.

acarbose 25 mg tablet

Color: whiteShape: roundImprint: P210 25

This medicine is a white, round, tablet imprinted with “54 251”.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Acarbose – description of the substance, pharmacology, use, contraindications, formula

Contents

• Structural formula

• Russian name

• English title

• Latin name

• chemical name

• Gross formula

• Pharmacological group of the substance Acarbose

• Nosological classification

• CAS code

• pharmachologic effect

• Characteristic

• Pharmacology

• Application of the substance Acarbose

• Contraindications

• Use during pregnancy and lactation

• Side effects of the substance Acarbose

• Interaction

• Overdose

• Dosage and administration

• Precautionary measures

• Information sources

Structural formula

Russian name

Acarbose

English name

Acarbose

Latin name

Acarbosum 62 Acarbosi)

Chemical name

[1S-(1alpha,4alpha,5beta,6alpha) ]-0-4,6-Dideoxy-4-[[4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-alpha-D-glucopyranosyl-(1-4) -0-alpha-D-glucopyranosyl-(1-4)-D-glucose

Gross formula

C ₂₅ H ₄₃ NO ₁₈

Pharmacological group of the substance Acarbose

Hypoglycemic synthetic and other agents

Nosological classification

ICD-10 code list

CAS code

56180-94-0

Pharmacological action

Pharmacological action –

hypoglycemic .

Characteristics

Oral alpha-glucosidase inhibitor indicated for the treatment of type 2 diabetes mellitus; oligosaccharide, which is obtained during the fermentation of the microorganism Actinoplanes utahensis .

White to off-white powder, molecular weight 645.6. Acarbose is water soluble and has a pKa of 5.1.

Pharmacology

Pharmacodynamics

Acarbose is a complex oligosaccharide that delays the digestion of carbohydrates, resulting in a smaller rise in blood glucose after meals. As a consequence of lowering plasma glucose levels, acarbose lowers HbA1 levels _c in patients with type 2 diabetes mellitus. Systemic non-enzymatic glycosylation of proteins, reflected by the level of HbA1 _c , depends on the average concentration of glucose in the blood over time.

Mechanism of action

Unlike sulfonylurea derivatives, acarbose does not increase insulin secretion. The antihyperglycemic effect of acarbose is the result of competitive reversible inhibition of pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolase enzymes. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the small intestine lumen, while intestinal membrane-bound alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In patients with diabetes, this enzyme inhibition leads to a delay in glucose absorption and a reduction in postprandial hyperglycemia.

Due to the difference in mechanism of action, the effect of acarbose on enhancing glycemic control is additive to that of sulfonylurea derivatives, insulin or metformin when used in combination. In addition, acarbose reduces the insulinotropic effect of sulfonylurea derivatives and their effect on weight gain.

Acarbose does not have lactase inhibitory activity and therefore cannot cause lactose intolerance.

Pharmacokinetics

Absorption

Less than 2% of an oral dose of acarbose is absorbed as active drug, while the total absorption of acarbose and its metabolites is 35%. On average, 51% of the dose was excreted in the feces in unabsorbed form within 96 hours after ingestion. Because acarbose acts locally in the GI tract, such low systemic bioavailability of the parent compound is therapeutically desirable. After oral administration to healthy volunteers ¹⁴ C-labeled acarbose, peak plasma radioactivity concentrations were reached 14-24 hours after dosing, while peak concentrations of the active drug were reached after approximately 1 hour. These differences are associated with the absorption of metabolites, which are formed under the influence of intestinal bacteria or enzymatic hydrolysis.

Metabolism

Acarbose is metabolized exclusively in the gastrointestinal tract, mainly by intestinal bacteria, but also by digestive enzymes. Some of these metabolites (approximately 34% of the dose) were absorbed and subsequently excreted in the urine. At least 13 metabolites have been isolated chromatographically from urine samples. The main metabolites have been identified as derivatives of 4-methylpyrogallol. One metabolite (formed by cleavage of a glucose molecule from acarbose) also has alpha-glucosidase inhibitory activity. This metabolite, together with the parent compound excreted in the urine, accounts for less than 2% of the total administered dose.

Excretion

The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. With intravenous acarbose, 89% of the dose was excreted in the urine as active drug within 48 hours. Less than 2% of the oral dose was excreted in the urine as active drug (i.e. parent compound and active metabolite). This is consistent with the low bioavailability of acarbose. 1/2″>T _1/2 of acarbose from plasma in healthy volunteers is approximately 2 hours. Therefore, when taken orally 3 times a day, accumulation of drugs does not occur.

Special patient groups

Children. The safety and efficacy of acarbose in children have not been established.

Old age. Of the total number of patients in US clinical trials of acarbose, 27% were 65 years of age or older and 4% were 75 years of age or older. There were no differences in safety and efficacy between this group of patients and younger adults. The mean AUC and max”>C _max of acarbose were approximately 1.5 times higher in the elderly compared to young volunteers, however, these differences were not statistically significant.

Renal failure. In patients with severe renal insufficiency (Cl creatinine <25 ml / min / 1.73 m ² ), the values ​​of max “> C _max and AUC of acarbose were approximately 5 and 6 times higher, respectively, than in volunteers with normal renal function

Race Race-specific pharmacokinetic studies of acarbose have not been conducted Controlled clinical trials conducted in the USA in patients with type 2 diabetes mellitus reduced HbA1 levels _c was the same in Caucasians (n=478) and African Americans (n=167), the best response was observed in Hispanics (n=132).

Clinical Studies

Clinical dose titration studies in diet-only patients with type 2 diabetes in 769 patients treated with acarbose in fixed doses of 50 to 300 mg 3 times a day found that the maximum the recommended dose for patients weighing less than 60 kg is 50 mg 3 times a day; The maximum recommended dose for patients weighing more than 60 kg is 100 mg 3 times a day.

In four placebo-controlled, double-blind, randomized studies conducted in the USA, patients with type 2 diabetes mellitus received acarbose monotherapy or acarbose in combination with a sulfonylurea, metformin, or insulin. The effects of treatment on HbA1 _c and glucose levels 1 hour after meals are summarized below.

Study 1 (n=109) included patients who received only a diet during treatment. The median effect of adding acarbose to dietary therapy was a change in HbA1 _c by -0.78% and glucose improvement 1 hour postprandial by -74.4 mg/dl.

In Study 2 (n=137), when acarbose was added to the highest dose of a sulfonylurea, the mean change in HbA1 _from was −0. 54% and the improvement in glucose 1 hour postprandial was −33.5 mg/dL.

In Study 3 (n=147), similar changes when acarbose was added to the maximum dose of metformin were −0.65% and −34.3 mg/dL.

Study 4 (n=145) showed that adding acarbose to patients on insulin treatment resulted in a mean change in HbA1 _c by -0.69% and blood glucose 1 hour after a meal by -36 mg/dL.

A study on acarbose alone or in combination with a sulfonylurea, metformin, or insulin treatment was conducted in Canada in 316 patients. In the diet, sulfonylurea, and metformin groups, the mean reduction in HbA1 _c induced by acarbose supplementation was statistically significant at 6 months, and this effect was maintained for 1 year. Patients treated with acarbose and insulin experienced a statistically significant decrease in HbA1 _c after 6 months and a downward trend after 1 year.

Carcinogenicity, Mutagenicity, Fertility

Eight carcinogenicity studies have been conducted on acarbose. Six studies were performed in rats (two strains, Sprague-Dawley and Wistar) and two studies were performed in hamsters. In the first study, Sprague-Dawley rats were fed acarbose at high doses (up to about 500 mg/kg) for 104 weeks. The use of acarbose has led to a significant increase in the incidence of kidney tumors (adenoma and adenocarcinoma) and benign Leydig cell tumors. This study was repeated with a similar result.

Further studies were performed to separate the direct carcinogenic effects of acarbose from the indirect effects resulting from carbohydrate deficiency caused by the high doses of acarbose used in the studies. In one study in Sprague-Dawley rats, acarbose was mixed with food, but carbohydrate deprivation was prevented by adding glucose to the diet. In another 26-month study in Sprague-Dawley rats, acarbose was administered by gavage daily after meals to avoid pharmacological effects. In both of these studies, there was no increase in the incidence of kidney tumors found in the original studies. Acarbose was also given with food and by gavage in two separate studies in Wistar rats. None of these studies found an increase in the incidence of kidney tumors. There was also no evidence of carcinogenicity in two studies of feeding hamsters with and without glucose supplementation.

Acarbose did not induce DNA damage in vitro”> in vitro in the Chinese hamster cell chromosome aberration assay, microbiological test (Ames test), or DNA binding assay. In vivo no DNA damage was detected in the dominant lethal test mutations in male mice or in the mouse micronucleus test

Fertility studies conducted in dietary acarbose-fed rats showed no adverse effects on fertility or overall reproductive capacity.

Substance use Acarbose

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

Contraindications

Hypersensitivity; diabetic ketoacidosis or cirrhosis of the liver; inflammatory bowel disease, colon ulcer, partial intestinal obstruction or predisposed to it; chronic intestinal diseases associated with severe digestive or absorption disorders, as well as conditions that may worsen as a result of increased gas formation in the intestines.

Use in pregnancy and lactation

FDA fetal category B.

Pregnancy

The safety of acarbose in pregnant women has not been established. Reproduction studies have been performed in rats at doses up to 480 mg/kg (corresponding to 9 times the human dosage based on blood drug levels) and have not found any evidence of impaired fertility or harm to the fetus due to acarbose. In rabbits, a decrease in maternal body weight, probably as a result of the pharmacodynamic activity of high doses of acarbose in the intestine, could be responsible for a slight increase in the number of embryo losses. However, in rabbits given acarbose at 160 mg/kg (corresponding to 10 times the human dose based on body surface area), there was no evidence of embryotoxicity, and there was no evidence of teratogenicity at 32 times the human dose. (based on body surface area). However, there are no adequate and well-controlled studies of acarbose in pregnant women. Because animal reproduction studies are not always predictive of human response, acarbose should only be used during pregnancy if absolutely necessary. Because current information strongly suggests that abnormal blood glucose levels during pregnancy are associated with a higher rate of birth defects as well as increased neonatal morbidity and mortality, most experts recommend using insulin during pregnancy to maintain blood glucose levels as low as possible. as close to normal as possible.

Lactation

A small amount of radioactivity has been found in the milk of lactating rats after administration of radiolabeled acarbose. It is not known whether acarbose is excreted in breast milk in women. Because many drugs are excreted in breast milk, acarbose should not be given to nursing women.

Side effects of the substance Acarbose

Digestive tract

Gastrointestinal symptoms are the most common reaction to the use of acarbose. In placebo-controlled studies in the United States, the incidence of abdominal pain, diarrhea, and flatulence was 19, 31 and 74%, respectively, in 1255 patients treated with acarbose 50-300 mg 3 times a day, while among 999 patients treated with placebo, the corresponding frequency was 9, 12 and 29%. In a one-year safety study during which patients kept diaries of gastrointestinal symptoms, abdominal pain and diarrhea returned to pre-treatment levels over time, and the frequency and intensity of flatulence decreased over time. The increase in gastrointestinal symptoms in patients treated with acarbose is a manifestation of the mechanism of action and is associated with the presence of undigested carbohydrates in the lower gastrointestinal tract.

Failure to follow the prescribed diet may increase intestinal side effects. If, despite adherence to the prescribed diabetic diet, severe warning symptoms develop, it is necessary to consult a doctor and reduce the dose temporarily or permanently.

Elevated serum transaminases (see Precautions).

Other laboratory abnormalities

A slight decrease in hematocrit occurred more frequently in patients treated with acarbose than in patients treated with placebo, but was not associated with a decrease in Hb levels.

Low serum calcium and low plasma vitamin B levels ₆ have been associated with acarbose therapy but are considered either questionable or of no clinical significance.

Post-marketing data

Additional adverse effects reported in worldwide post-marketing experience include fatal fulminant hepatitis, skin hypersensitivity reactions (eg, rash, erythema, exanthema, and urticaria), edema, ileus/partial bowel obstruction, jaundice and / or hepatitis and associated liver damage, thrombocytopenia and cystoid intestinal pneumatosis (see “Precautions”).

Cystoid intestinal pneumatosis. There have been rare post-marketing reports of cystoid intestinal pneumatosis associated with the use of alpha-glucosidase inhibitors, including acarbose. Cystic intestinal pneumatosis may present with symptoms of diarrhea, mucus discharge, rectal bleeding, and constipation. Complications may include accumulation of gas in the abdomen, volvulus, intestinal obstruction, intussusception and bleeding, and intestinal perforation. If cystoid intestinal pneumatosis is suspected, acarbose should be discontinued and appropriate diagnostic tests performed.

Interactions

Some drugs may cause hyperglycemia and lead to loss of blood glucose control. These drugs include thiazides and other diuretics, corticosteroids, phenothiazines, thyroid medications, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, CCBs, and isoniazid. With the simultaneous use of such drugs and acarbose, careful monitoring of the patient’s condition should be established for loss of control of blood glucose levels. When such drugs are discontinued in patients receiving acarbose in combination with sulfonylurea derivatives or insulin, patients should be carefully monitored for signs of hypoglycemia.

The use of acarbose in patients receiving sulfonylurea derivatives or insulin, which can cause hypoglycemia, may lead to a further decrease in blood glucose levels and increase the likelihood of hypoglycemia. If hypoglycemia occurs, appropriate adjustments should be made to the dosage of these drugs. Very rarely, isolated cases of hypoglycemic shock have been reported in patients receiving acarbose therapy in combination with sulfonylurea derivatives and/or insulin.

Intestinal adsorbents (eg charcoal) and digestive enzymes that break down carbohydrates (eg amylase, pancreatin) may reduce the effect of acarbose and should not be taken concomitantly.

Acarbose has been shown to alter the bioavailability of digoxin when co-administered, which may require dose adjustment of digoxin.

Studies in healthy volunteers have shown that acarbose does not affect the pharmacokinetics and pharmacodynamics of nifedipine, propranolol or ranitidine.

Acarbose does not affect the absorption or distribution of glyburide in diabetic patients.

When used simultaneously with acarbose, the AUC of metformin did not change compared to placebo, however, max “> C _max decreased by approximately 20%, which is associated with a delay in the absorption of metformin. There is no clinically significant interaction between acarbose and metformin.

Overdose

Symptoms: unlike sulfonylurea derivatives or insulin, an overdose of acarbose will not lead to hypoglycemia.Overdose can lead to a temporary increase in flatulence, diarrhea and abdominal discomfort, which will soon disappear.

Treatment: in case of overdose, the patient should not be given drinks or foods containing carbohydrates (polysaccharides, oligosaccharides and disaccharides) for the next 4-6 hours.

Dosage and administration

Inside. Dosage should be individualized based on efficacy and tolerability, with the maximum recommended dose not exceeding 100 mg 3 times daily.

Precautions

Macrovascular complications

No clinical studies have been conducted to establish conclusive evidence for a reduction in the risk of macrovascular complications with acarbose or any other antidiabetic drug.

Hypoglycemia

When used alone, acarbose should not cause fasting or postprandial hypoglycemia. Sulfonylureas or insulin may cause hypoglycemia. Since acarbose, when combined with sulfonylurea derivatives or insulin, causes a further decrease in blood glucose levels, this may increase the likelihood of hypoglycemia. Hypoglycemia does not usually occur in patients receiving metformin alone, and there has been no increase in the incidence of hypoglycemia in patients when acarbose was added to metformin therapy.

For the treatment of mild to moderate hypoglycemia, glucose (dextrose) should be used instead of sucrose, the absorption of which is not inhibited by acarbose. Sucrose, whose hydrolysis to glucose and fructose is inhibited by acarbose, is not suitable for rapid correction of hypoglycemia. In severe hypoglycemia, intravenous glucose infusion or glucagon injection may be required.

Elevated serum transaminases

ALT) up to 1. 8 times ULN, more than 1.8 times ULN, and more than 3 times ULN was observed in 14%, 6%, and 3%, respectively, in the acarbose-treated groups compared with 7, 2, and 1%, respectively, in patients receiving placebo. Although these differences were statistically significant, transaminase elevations were asymptomatic, reversible, more common in females, and generally not associated with other signs of liver dysfunction. In addition, this increase in serum transaminases appeared to be dose-dependent. In US studies, with acarbose doses up to the maximum approved dose of 100 mg 3 times daily, treatment-related increases in AST and/or ALT levels of any grade were similar between acarbose-treated and placebo-treated patients (p≥ 0.496).

In approximately 3 million patient-years of international post-marketing experience with acarbose, 62 cases of elevated serum transaminases >500 IU/L (29 of which were associated with jaundice) have been reported. Forty-one of these 62 patients were treated with 100 mg 3 times daily or more, and 33 of the 45 weight-measured patients were <60 kg. Of the 59 follow-up cases, hepatic dysfunction improved or disappeared after acarbose was discontinued in 55 cases and unchanged in 2. Fatal cases of fulminant hepatitis have been reported and have not been associated with acarbose.

Loss of blood glucose control

When patients with diabetes are exposed to stress such as fever, injury, infection, or surgery, temporary loss of blood glucose control can occur. In such cases, temporary insulin therapy may be required.

Interference with laboratory tests

Therapeutic response to acarbose should be monitored by periodic blood glucose testing. For long-term glycemic control, HbA1 measurement is recommended _c .

Acarbose, especially at doses greater than 50 mg 3 times a day, may cause an increase in serum transaminases and, in rare cases, hyperbilirubinemia. It is recommended to check serum transaminase levels every 3 months during the first year of treatment and periodically thereafter. If an increase in transaminase levels is observed, a reduction in dosage or discontinuation of therapy may be indicated, especially if the increase persists.

Renal failure

Plasma concentrations of acarbose in volunteers with renal insufficiency increased in proportion to the increase in the degree of renal dysfunction. Long-term clinical trials have not been conducted in diabetic patients with significant renal impairment (serum creatinine >2 mg/dL), and treatment of such patients with acarbose is not recommended.

Summary www.rxlist.com and www.drugs.com, 2020.

Alpha-glucosidase inhibitors to prevent or slow the progression of type 2 diabetes and related complications in people at increased risk for diabetes 2 th type

Survey Question

Can alpha-glucosidase inhibitors prevent or slow the development of type 2 diabetes and related complications in people at increased risk of developing type 2 diabetes?

Relevance

People with moderately elevated glucose levels are often at increased risk of developing type 2 diabetes. Therefore, to prevent type 2 diabetes, these people are often advised to increase physical activity and reduce calorie intake. Alpha-glucosidase inhibitors (acarbose, miglitol, voglibose) are used to lower blood glucose levels in people with type 2 diabetes. It is currently unknown whether alpha-glucosidase inhibitors should be given to individuals with moderately elevated blood glucose levels. We wanted to find out if alpha-glucosidase inhibitors could prevent or slow down the development of type 2 diabetes in people with mildly elevated glucose levels. We searched the medical literature for randomized controlled trials (clinical trials in which people are randomly assigned to one of two or more treatment groups) lasting at least one year that investigated alpha-glucosidase inhibitors in participants with glucose levels. above normal but below diagnostic criteria for type 2 diabetes.

Study profile

We found 10 randomized controlled trials representing 11,814 participants, 8 of which tested acarbose and 2 tested voglibose. The duration of the trials varied from one to six years.

This evidence is current to December 2017.

Main results

When acarbose was compared with placebo (a substance not thought to have a therapeutic effect), 670 of 4014 participants (17%) who received acarbose developed type 2 diabetes compared to 812 of 3994 participants (20%) who received placebo. Most of the data for this comparison came from trials involving people with heart disease. When comparing acarbose with no intervention, seven of 75 participants (9%) who received acarbose developed type 2 diabetes, compared with 18 of 65 participants (28%) in the no intervention group. Treatment with acarbose did not reduce or increase the risk of death from any cause, death from heart disease, serious side effects, stroke, or heart failure. Compared with placebo, acarbose reduced the risk of myocardial infarction (one of 742 participants (0.1%) who received acarbose had a myocardial infarction compared to 15 of 744 participants (2%) who received placebo). Treatment with acarbose showed an increased risk of non-serious side effects (mainly gastrointestinal events) compared with placebo: In 751 of 775 people (97% who received acarbose had non-serious side effects compared to 723 of 775 people (93%) who received placebo.

One trial compared voglibose with placebo and another compared voglibose with diet and exercise. When comparing voglibose with placebo, 50 of 897 participants (5.6%) who received voglibose developed type 2 diabetes compared to 106 of 881 participants (12%) who received placebo.

One trial with 90 participants compared acarbose with diet and exercise, and another trial with 98 participants compared acarbose with metformin. For these comparisons, there were no significant differences in any of the outcomes.

None of the trials reported on lower limb amputations, blindness or severe vision loss, kidney disease, health-related quality of life, time to progression to type 2 diabetes, or socioeconomic outcomes (such as absence from work or expenses).