Acarbose 100mg Tablets

Manufacturer ROXANE Active Ingredient Acarbose(AY car bose) Pronunciation AY car bose
It is used to lower blood sugar in patients with high blood sugar (diabetes).
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Drug Class
Antidiabetic agent
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Pharmacologic Class
Alpha-glucosidase inhibitor
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Pregnancy Category
Category B
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FDA Approved
Dec 1995
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Acarbose is a medication used to help control high blood sugar in people with type 2 diabetes. It works by slowing down the digestion of carbohydrates (sugars and starches) in your gut, which helps to prevent a sharp rise in blood sugar after meals.
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How to Use This Medicine

Taking Your Medication Correctly

To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with the first bite of each meal. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.

If you are taking charcoal or digestive enzyme preparations, consult with your doctor about how to take them in conjunction with this medication to ensure safe and effective use.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding the bathroom. Keep the lid tightly closed to maintain the medication's potency.

What to Do If You Miss a Dose

If you miss a dose, skip it and return to your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Take acarbose with the first bite of each main meal (breakfast, lunch, and dinner).
  • Continue to follow your doctor's recommended diet and exercise plan.
  • If you experience low blood sugar (hypoglycemia) while taking acarbose with other diabetes medications (like insulin or sulfonylureas), treat it with pure glucose (dextrose) tablets or gel, not regular table sugar or sugary drinks, as acarbose will block the breakdown of table sugar.
  • Be aware that common side effects include gas, bloating, and diarrhea, especially when starting the medication or increasing the dose. These usually lessen over time.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 25 mg three times daily (TID) with the first bite of each main meal. Maintenance: 50 mg or 100 mg TID with the first bite of each main meal.
Dose Range: 25 - 100 mg

Condition-Specific Dosing:

Type 2 Diabetes Mellitus: Initial: 25 mg TID. Titrate at 4-8 week intervals based on postprandial glucose and tolerability. Max dose: 50 mg TID for patients weighing ≤ 60 kg; 100 mg TID for patients weighing > 60 kg.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment required, but use with caution.
Moderate: No specific dose adjustment required, but use with caution.
Severe: Contraindicated in patients with creatinine clearance < 25 mL/min.
Dialysis: Contraindicated.

Hepatic Impairment:

Mild: No specific dose adjustment required.
Moderate: No specific dose adjustment required.
Severe: No specific dose adjustment required, but monitor liver enzymes periodically. Contraindicated in patients with cirrhosis.

Pharmacology

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Mechanism of Action

Acarbose is an oral alpha-glucosidase inhibitor. It competitively inhibits alpha-glucosidase enzymes (e.g., sucrase, maltase, glucoamylase, dextranase) in the brush border of the small intestine. This inhibition delays the digestion of complex carbohydrates (polysaccharides, oligosaccharides, and disaccharides) into absorbable monosaccharides (glucose). The delayed absorption of glucose results in a lower and more prolonged postprandial blood glucose rise.
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Pharmacokinetics

Absorption:

Bioavailability: <2% (systemic)
Tmax: 1 hour (for parent drug, unabsorbed); 14-24 hours (for active metabolites)
FoodEffect: Must be taken with the first bite of each main meal to exert its local effect in the intestine.

Distribution:

Vd: Not well-defined due to minimal systemic absorption
ProteinBinding: Not significant
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 2 hours (for absorbed active metabolites)
Clearance: Not well-defined due to minimal systemic absorption
ExcretionRoute: Renal (approximately 51% of absorbed dose); Fecal (approximately 51% of the administered dose as unabsorbed drug)
Unchanged: <2% (systemically absorbed unchanged drug)
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Pharmacodynamics

OnsetOfAction: Within minutes of ingestion (local effect)
PeakEffect: Peak reduction in postprandial glucose occurs within 1-2 hours after a meal.
DurationOfAction: Duration of effect is limited to the presence of food in the GI tract, typically 2-4 hours after a meal.

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Attention Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Low blood sugar (hypoglycemia), which can occur when this medication is used with other diabetes medications. Symptoms may include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or some fruit juices.
Liver problems, which have rarely occurred with this medication and can be fatal. If you experience any of the following symptoms, contact your doctor immediately:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people may not experience any side effects or may only have mild ones. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:

Stomach pain
Diarrhea
Gas

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Symptoms of severe hypoglycemia (if on combination therapy): severe confusion, seizures, loss of consciousness.
  • Severe or persistent gastrointestinal symptoms: severe abdominal pain, persistent diarrhea, bloody stools.
  • Signs of liver problems: unusual tiredness, dark urine, yellowing of the skin or eyes (jaundice), nausea, vomiting, upper right abdominal pain.
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have kidney disease, as this may affect how your body processes the medication.
* If you have any of the following health conditions:
+ Diabetic acidosis or other diabetic complications
+ Digestion problems, such as inflammatory bowel disease
+ Bowel blockage or an increased risk of bowel blockage
+ Liver disease
+ Malabsorption syndrome
+ Ulcers in the colon

This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you experience low blood sugar, do not operate a vehicle, as this increases your risk of being involved in an accident.

Monitor your blood sugar levels as directed by your doctor. Additionally, have your blood work checked as recommended by your doctor, and discuss the results with them. Adhere to the diet and exercise plan outlined by your doctor to maintain optimal blood sugar control.

Be aware that stress, such as fever, infection, injury, or surgery, can make it more challenging to manage your blood sugar levels. Changes in physical activity, exercise, or diet can also impact your blood sugar control.

This medication may interfere with certain laboratory tests. Therefore, it is crucial to inform all your healthcare providers and laboratory personnel that you are taking this drug. If you are pregnant, planning to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Acute overdose of acarbose is not expected to cause hypoglycemia if not taken with sulfonylureas or insulin. However, it may lead to transient increases in flatulence, diarrhea, and abdominal discomfort.

What to Do:

In case of overdose, contact a poison control center immediately (1-800-222-1222) or seek emergency medical attention. Avoid food or drinks containing carbohydrates for 4-6 hours after an overdose.

Drug Interactions

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Moderate Interactions

  • Intestinal adsorbents (e.g., charcoal): May reduce the effect of acarbose.
  • Digestive enzyme preparations (e.g., amylase, pancreatin): May reduce the effect of acarbose.
  • Thiazides, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers, and isoniazid: May cause hyperglycemia and reduce the glucose-lowering effect of acarbose.

Monitoring

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Baseline Monitoring

HbA1c

Rationale: To establish baseline glycemic control.

Timing: Prior to initiation of therapy.

Serum Creatinine / eGFR

Rationale: To assess renal function, as acarbose is contraindicated in severe renal impairment.

Timing: Prior to initiation of therapy.

Liver Enzymes (ALT, AST)

Rationale: To establish baseline liver function, as transient elevations have been reported.

Timing: Prior to initiation of therapy.

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Routine Monitoring

HbA1c

Frequency: Every 3-6 months

Target: Individualized, typically <7%

Action Threshold: If target not met, consider dose adjustment or additional therapy.

Postprandial Blood Glucose

Frequency: Periodically, as needed for dose titration

Target: Individualized, typically <180 mg/dL 1-2 hours post-meal

Action Threshold: If consistently elevated, consider dose adjustment.

Liver Enzymes (ALT, AST)

Frequency: Every 3 months during the first year of treatment, then periodically (e.g., annually) or as clinically indicated.

Target: Within normal limits

Action Threshold: If persistently elevated, consider dose reduction or discontinuation.

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Symptom Monitoring

  • Symptoms of hypoglycemia (if used with sulfonylureas or insulin): sweating, tremor, dizziness, confusion, hunger.
  • Gastrointestinal side effects: flatulence, diarrhea, abdominal pain/cramping, bloating.
  • Symptoms of liver injury: unusual fatigue, dark urine, yellowing of skin/eyes (jaundice), nausea, vomiting, abdominal pain.

Special Patient Groups

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Pregnancy

Acarbose is Pregnancy Category B. Studies in animals have shown no evidence of harm to the fetus. However, there are no adequate and well-controlled studies in pregnant women. Acarbose should be used during pregnancy only if clearly needed.

Trimester-Specific Risks:

First Trimester: No specific increased risk identified, but limited human data.
Second Trimester: No specific increased risk identified, but limited human data.
Third Trimester: No specific increased risk identified, but limited human data.
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Lactation

It is not known whether acarbose is excreted in human milk. Due to the potential for adverse effects in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Generally not recommended.

Infant Risk: Risk unknown due to lack of data; potential for gastrointestinal effects in infant if excreted in milk.
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Pediatric Use

Safety and effectiveness of acarbose in pediatric patients (under 18 years of age) have not been established. Use is not recommended.

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Geriatric Use

No specific dose adjustment is required based on age alone. However, elderly patients may have age-related decline in renal function, which should be assessed before initiating therapy and monitored periodically, as acarbose is contraindicated in severe renal impairment.

Clinical Information

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Clinical Pearls

  • Acarbose must be taken with the first bite of each main meal to be effective.
  • It does not cause hypoglycemia when used as monotherapy, but can increase the risk when combined with insulin or sulfonylureas.
  • If hypoglycemia occurs while on acarbose (especially with other antidiabetics), treat with pure glucose (dextrose), not sucrose (table sugar), as acarbose inhibits sucrose breakdown.
  • Gastrointestinal side effects (flatulence, diarrhea, abdominal discomfort) are common, especially at the start of therapy or with dose increases, but often improve with continued use and dietary adjustments.
  • Liver enzymes should be monitored periodically, especially during the first year of treatment.
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Alternative Therapies

  • Metformin (Biguanide)
  • Sulfonylureas (e.g., Glipizide, Glyburide, Glimepiride)
  • Thiazolidinediones (TZDs) (e.g., Pioglitazone, Rosiglitazone)
  • DPP-4 Inhibitors (e.g., Sitagliptin, Saxagliptin)
  • GLP-1 Receptor Agonists (e.g., Liraglutide, Semaglutide)
  • SGLT2 Inhibitors (e.g., Canagliflozin, Dapagliflozin, Empagliflozin)
  • Insulin
  • Meglitinides (e.g., Repaglinide, Nateglinide)
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Cost & Coverage

Average Cost: Varies, typically $20-$100 per 30 tablets
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.