Schedule H

Oral

• Tablets: 25 mg, 50 mg, 100 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Type 2 Diabetes Mellitus

As adjunct to diet and exercise; may be used as monotherapy or in combination with metformin, sulfonylureas, or insulin.

Parameter Recommendation

Starting dose 25 mg orally three times daily, taken with the first bite of each main meal

Titration Increase to 50 mg three times daily after 4–8 weeks if tolerated; further increase to 100 mg three times daily after additional 4–8 weeks based on response

Usual maintenance dose 50–100 mg three times daily

Maximum dose 100 mg three times daily (patients ≤60 kg: 50 mg three times daily)

Clinical Notes:

• Must be taken with the first bite of each main meal for optimal efficacy

• Primarily reduces postprandial glucose excursions; less effective for fasting hyperglycaemia

• Start low and titrate gradually to minimise gastrointestinal adverse effects

• Minimal risk of hypoglycaemia when used as monotherapy

Secondary Indications – Adults (Off-label, if any)

Indication Dose Duration Notes

Prevention of Type 2 Diabetes in IGT 50–100 mg three times daily Long-term OFF-LABEL; Specialist only; Evidence: STOP-NIDDM trial showed reduced progression from IGT to T2DM; Not standard practice in India

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

NOT APPROVED for routine use in children below 18 years in India.

• Safety and efficacy not established in paediatric population

• Indian regulatory sources (CDSCO, NFI) do not list paediatric indications

Secondary Indications – Paediatrics (Off-label, if any)

Indication Age Dose Notes

Type 2 Diabetes Mellitus in Adolescents ≥10 years Starting: 25 mg once daily with largest meal; Titration: Increase gradually to maximum 50 mg three times daily based on tolerance OFF-LABEL; Specialist paediatric endocrinology supervision only; Limited safety data

Monitoring in Paediatric Use:

• Gastrointestinal tolerability

• Liver function tests

• Postprandial glucose response

• Growth parameters

Not recommended below age 10 years except under specialist supervision in tertiary centres.

• Chronic intestinal diseases associated with marked disorders of digestion or absorption (inflammatory bowel disease, colonic ulceration, partial intestinal obstruction)

• Conditions that may deteriorate due to increased intestinal gas formation (large hernias, intestinal obstruction)

• Hepatic cirrhosis

• Severe renal impairment (eGFR <30 mL/min/1.73 m²)

• Known hypersensitivity to acarbose or any excipient

• Diabetic ketoacidosis

• Malabsorption syndromes

• Gastrointestinal symptoms (flatulence, bloating, diarrhoea) — common initially; usually improve with continued use

• Hepatic enzyme elevation — monitor LFTs in long-term therapy

• Hypoglycaemia risk when combined with insulin or sulfonylureas — must treat with oral glucose (dextrose), not sucrose

• Febrile illness, surgery, or trauma — may need temporary switch to insulin

• Elderly with pre-existing GI disorders — assess carefully before initiation

• Concurrent digestive enzyme preparations — may reduce efficacy

Parameter Details

Risk Category Limited human data; animal studies show no teratogenicity; minimal systemic absorption

Recommendation Not first-line; avoid unless clearly needed

Preferred Alternatives Insulin is preferred for glycaemic control in pregnancy (ICMR, FOGSI guidelines); Metformin acceptable in some cases

When May Be Used Only if benefit outweighs risk and insulin/metformin not suitable; specialist input mandatory

Monitoring Maternal blood glucose (fasting and postprandial); fetal growth surveillance

Parameter Details

Compatibility Likely compatible due to minimal systemic absorption

Drug Levels in Milk Negligible — minimal systemic absorption (<2%)

Preferred Alternatives Metformin or insulin preferred for breastfeeding mothers with T2DM

Infant Monitoring If used, monitor infant for adequate feeding and normal weight gain

Parameter Recommendation

Starting dose 25 mg once or twice daily with meals

Titration Slower titration (every 6–8 weeks); target lowest effective dose

Special Risks Higher incidence of GI adverse effects due to slower GI transit; age-related renal decline may increase accumulation risk

Monitoring Renal function at baseline and periodically; assess for GI contraindications before initiation

Interacting Drug Mechanism / Effect Recommendation

Digestive enzymes (pancreatin, amylase, lipase) Reduce acarbose efficacy by enhancing carbohydrate digestion Avoid concurrent use

Oral sucrose (table sugar) Acarbose inhibits sucrase; sucrose ineffective for treating hypoglycaemia Use oral glucose (dextrose) tablets or solution for hypoglycaemia treatment

Charcoal / Adsorbents May reduce acarbose absorption Avoid concurrent administration

Interacting Drug Mechanism / Effect Recommendation

Insulin / Sulfonylureas Additive hypoglycaemic effect Monitor blood glucose closely; educate patient to use glucose (not sucrose) for hypoglycaemia

Metformin Combined GI adverse effects possible Monitor tolerability; stagger dose escalation

Digoxin May reduce digoxin bioavailability Monitor digoxin levels if clinically indicated

Cholestyramine May alter GI pH and transit affecting acarbose Separate administration by at least 2 hours

Neomycin May exacerbate GI adverse effects Monitor closely if concurrent use unavoidable

Antacids (aluminium/magnesium containing) May affect efficacy Separate administration by at least 2 hours

• Flatulence (most common; dose-related)

• Abdominal distension and bloating

• Diarrhoea

• Borborygmi (rumbling bowel sounds)

• Abdominal pain/discomfort

• Nausea

Note: GI symptoms typically decrease with continued use and dietary compliance.

Adverse Effect Clinical Action

Hepatitis / Elevated transaminases Discontinue acarbose; monitor LFTs until normalised; usually reversible

Fulminant hepatitis (rare) Discontinue immediately; urgent hepatology referral

Ileus (rare, especially with high doses) Discontinue; supportive care

Severe hypoglycaemia (when combined with insulin/sulfonylureas) Treat with oral glucose (NOT sucrose); may require IV dextrose if severe

4–8 weeks after initiation/dose change Postprandial glucose response; assess GI tolerability

Every 3 months (first year) LFTs if on doses >50 mg TID

Long-term LFTs every 6 months; HbA1c every 3 months; renal function annually or as indicated

Monotherapy:

• Glucobay (Bayer Zydus Pharma)

• Rebose (Intas)

• Acarb (Glenmark)

• Acbose (USV)

• Acarose (Sun Pharma)

• Glucar (Micro Labs)

Fixed-Dose Combinations:

• With Metformin: Glucobay M, Acarb M, Rebose MF

• Not included in current NLEM; pricing not NPPA-controlled

• Cost varies across brands and regions

• FDCs with metformin slightly more expensive

• Acarbose is most effective for isolated postprandial hyperglycaemia — not useful for fasting glucose correction; consider for patients with predominant post-meal spikes

• Always initiate at low dose (25 mg once daily or with largest meal) and titrate slowly over weeks to minimise GI intolerance — most dropouts occur due to flatulence

• Critical patient education: Hypoglycaemia (when combined with insulin/sulfonylureas) must be treated with oral glucose tablets or dextrose solution, NOT sucrose-containing foods (sweets, sugar) as acarbose delays sucrose absorption

• GI side effects typically improve over 4–8 weeks with continued use and dietary compliance (reducing rapidly fermentable carbohydrates)

• Monitor LFTs especially at doses exceeding 50 mg TID — hepatotoxicity is rare but documented

• Avoid in patients with significant GI pathology (IBD, malabsorption) — drug mechanism worsens symptoms

Acarbose; type 2 diabetes; alpha-glucosidase inhibitor; postprandial hyperglycaemia; GI adverse effects; hepatic monitoring; renal-caution; oral antidiabetic; Schedule H

RxIndia v1.0 — 04 Apr 2025

• CDSCO approved product information

• Indian Pharmacopoeia (IP)

• National Formulary of India (NFI)

• National List of Essential Medicines (NLEM India, 2022) — referenced for inclusion status

• API Textbook of Medicine — Diabetes Mellitus chapter

• ICMR Guidelines for Management of Type 2 Diabetes (2018)

• AIIMS Endocrinology Treatment Protocols

• Goodman & Gilman's: The Pharmacological Basis of Therapeutics

• STOP-NIDDM Trial (for off-label IGT indication reference)