Acaril

 50 mg Tablet
The White Horse Pharmaceuticals Ltd.
Unit Price: ৳ 15.00 (30's pack: ৳ 450.00)
Indications
  • Type 2 Diabetes Mellitus: Adjunct treatment to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus, especially when diet alone is insufficient.
  • Postprandial Hyperglycemia: Specifically reduces postprandial blood glucose spikes.
  • Off-label Uses: Occasionally used in combination with other antidiabetic agents (e.g., metformin, sulfonylureas) to enhance glycemic control.
  • Not indicated for type 1 diabetes or diabetic ketoacidosis.
Dosage & Administration
  • Initial dose: 25 mg orally three times daily with the first bite of each main meal.
  • Titration: Dose may be increased every 4–8 weeks based on tolerance and efficacy. Common maintenance dose is 50–100 mg three times daily.
  • Maximum dose: Up to 100 mg three times daily for patients weighing less than 60 kg; up to 100 mg or more three times daily for those weighing over 60 kg, not exceeding 300 mg/day.
  • Pediatric use: Safety and efficacy not established in children under 18 years.
  • Elderly: No specific dosage adjustment needed, but monitor for renal function.
  • Renal impairment: Use cautiously in mild to moderate renal impairment; contraindicated in severe renal impairment (eGFR <25 mL/min/1.73 m²).
  • Hepatic impairment: Use with caution; no formal dose recommendations available.
  • Administration: Must be taken with the first bite of each meal for optimal effectiveness.
Mechanism of Action (MOA)

Acarbose is an alpha-glucosidase inhibitor that delays carbohydrate digestion by competitively inhibiting enzymes such as pancreatic alpha-amylase and intestinal brush border alpha-glucosidases. This slows the breakdown of complex carbohydrates into glucose, resulting in a reduction of postprandial hyperglycemia by blunting the rise of blood glucose after meals.

Pharmacokinetics
  • Absorption: Minimal systemic absorption (<2%); acts locally in the gastrointestinal tract.
  • Distribution: Due to negligible absorption, systemic distribution is minimal.
  • Metabolism: Metabolized primarily by intestinal bacteria and digestive enzymes.
  • Excretion: Eliminated mainly via feces as inactive metabolites; a small fraction excreted unchanged in urine.
  • Half-life: Not clinically relevant because of low systemic exposure.
Pregnancy Category & Lactation
  • Pregnancy: Classified as FDA Pregnancy Category B. Animal studies show no fetal harm, but adequate human studies are lacking. Use only if clearly needed.
  • Lactation: Unknown if excreted in human milk; caution is advised during breastfeeding due to lack of data.
  • Note: Benefits should outweigh potential risks when prescribing to pregnant or breastfeeding women.
Therapeutic Class
  • Primary Class: Antidiabetic agent.
  • Subclass: Alpha-glucosidase inhibitor.
Contraindications
  • Hypersensitivity to acarbose or any formulation component.
  • Diabetic ketoacidosis.
  • Cirrhosis.
  • Inflammatory bowel disease (e.g., Crohn's disease, ulcerative colitis).
  • Colonic ulceration or partial intestinal obstruction.
  • Conditions predisposing to intestinal obstruction.
  • Severe renal impairment (eGFR <25 mL/min/1.73 m²).
Warnings & Precautions
  • Hypoglycemia risk: When combined with insulin or sulfonylureas, hypoglycemia risk increases. Treat hypoglycemia with glucose (dextrose), not sucrose, as acarbose inhibits sucrose digestion.
  • Gastrointestinal effects: Flatulence, diarrhea, and abdominal discomfort are common and usually transient.
  • Hepatic effects: Rare cases of elevated liver enzymes have been reported; liver function monitoring recommended if higher doses are used.
  • Renal impairment: Use cautiously in mild to moderate impairment.
  • Patients with gastrointestinal diseases: Use with caution; monitor for signs of bowel obstruction.
  • Early recognition of severe abdominal symptoms is important to rule out serious complications.
Side Effects
  • Common: Flatulence, diarrhea, abdominal pain, and bloating. These effects are dose-dependent and usually decrease over time.
  • Serious/Rare: Elevated liver enzymes, hypersensitivity reactions (rash, angioedema), and intestinal obstruction in predisposed individuals.
  • Side effects typically occur early in treatment.
Drug Interactions
  • Hypoglycemic agents: Increases risk of hypoglycemia with insulin or sulfonylureas.
  • Digestive enzyme inhibitors: Potential interactions affecting carbohydrate digestion.
  • Food: Must be taken with food for effectiveness.
  • Alcohol: No significant interaction, but alcohol may worsen hypoglycemia.
  • Metabolism: No significant CYP450 involvement due to minimal systemic absorption.
Recent Updates or Guidelines
  • Current diabetes guidelines (ADA, EASD) recommend acarbose as a possible adjunct for postprandial glucose control, especially in patients with mild to moderate hyperglycemia.
  • No recent major regulatory changes.
  • Ongoing monitoring of gastrointestinal tolerability emphasized in recent clinical guidance.
Storage Conditions
  • Store at 20°C to 25°C (68°F to 77°F).
  • Protect from moisture and light.
  • Keep in original container tightly closed.
  • Do not freeze.
  • No special refrigeration or reconstitution required.
  • Tablets should be swallowed whole; do not crush or chew.
Available Brand Names