LODIAB XR 750/MG PR TAB 60/TAB

Indications

Approved Uses

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus; may be used as monotherapy or in combination with other antidiabetic agents including insulin.

Off-Label Uses

Polycystic ovary syndrome (PCOS); prevention/delay of type 2 diabetes in high‑risk prediabetes; antipsychotic‑associated weight gain/metabolic effects; gestational diabetes (use varies by guideline/region and is not universally approved).

Dosage & Administration

Dosing by Condition

Type 2 diabetes mellitus (XR): Start 750 mg once daily with the evening meal (this product strength); titrate by 750 mg at intervals of ~1-2 weeks based on glycemic response/tolerability; usual maintenance 1500-2000 mg/day; maximum commonly 2000 mg/day for most XR products (some XR formulations allow up to 2250 mg/day-follow local product labeling).

Initial Dose

750mg once daily with the evening meal

Maximum Dose

2250mg per day (extended-release); 3000mg per day (immediate-release)

Children's Dosage

Not approved for children under 10 years. For children 10 years and older (Immediate-Release): Initial dose is 500mg twice daily. Maximum dose is 2000mg per day. Extended-release is not approved for pediatric use.

Dose Adjustment Notes

Titrate gradually (typically every 1-2 weeks) to minimize GI adverse effects; assess renal function before initiation and periodically-do not use if eGFR <30 mL/min/1.73 m², and if eGFR 30-45 mL/min/1.73 m² avoid initiation and reassess risk/benefit if already on therapy (dose reduction may be needed).

How to Take

Take orally once daily with the evening meal; swallow the prolonged‑release tablet whole with water-do not crush, chew, or split/cut.

Side Effects

Common Side Effects

Diarrhea, nausea, vomiting, abdominal discomfort/pain, flatulence, decreased appetite; metallic taste; long‑term use may cause vitamin B12 deficiency.

Side Effect Frequency

Very common (>10%): gastrointestinal effects (e.g., diarrhea, nausea, vomiting, abdominal pain, loss of appetite). Common (1-10%): taste disturbance. Very rare (<0.01%): lactic acidosis; decreased vitamin B12 absorption/low B12 with long-term use; liver function test abnormalities/hepatitis; skin reactions (e.g., erythema, pruritus, urticaria).

Safety & Warnings

Contraindications

Contraindicated in: severe renal impairment (eGFR <30 mL/min/1.73 m²), acute or chronic metabolic acidosis (including diabetic ketoacidosis), and hypersensitivity to metformin.

Warnings & Precautions

Warnings/precautions: lactic acidosis risk-assess/monitor renal function; temporarily withhold for iodinated contrast in at-risk patients and during acute illness/hypoxia/dehydration or major surgery; avoid excessive alcohol; monitor for vitamin B12 deficiency with long-term use; XR tablets must be swallowed whole (do not crush/chew).

Age Restriction

Not recommended/approved for pediatric use (<18 years) for extended-release metformin; immediate-release metformin is approved for children ≥10 years.

Drug Interactions

Drug Interactions

Key interactions: iodinated contrast media (temporary discontinuation in at-risk patients), alcohol (increases lactic acidosis risk), carbonic anhydrase inhibitors e.g., topiramate/acetazolamide (metabolic acidosis risk), cationic/OCT2-MATE inhibitors that raise metformin levels (e.g., cimetidine, dolutegravir, ranolazine, vandetanib), and drugs that worsen glycemia or renal function (e.g., corticosteroids; diuretics/ACEi/ARBs/NSAIDs via renal effects).

Interaction Severity

MAJOR: Iodinated contrast media in at‑risk patients (risk of AKI → metformin accumulation/lactic acidosis; temporarily withhold per eGFR/risk guidance). MODERATE: Alcohol/excessive intake (↑ lactic acidosis risk); carbonic anhydrase inhibitors e.g., topiramate/acetazolamide (↑ metabolic acidosis risk); OCT2/MATE inhibitors (e.g., dolutegravir, ranolazine, cimetidine) can ↑ metformin exposure-monitor and consider dose adjustment. MINOR: None routinely; cimetidine is better considered MODERATE due to clinically meaningful exposure increase in some patients.

Food Interaction

Take with food (preferably the evening meal).

Alcohol Interaction

Avoid

Special Populations

Pregnancy

Category B (old FDA); Not recommended without risk/benefit assessment

Breastfeeding

Contraindicated (per some sources); Use with caution

Children

Not approved for children under 10 years. For children 10 years and older (Immediate-Release): Initial dose is 500mg twice daily. Maximum dose is 2000mg per day. Extended-release is not approved for pediatric use.

Elderly

Start at lower doses and titrate cautiously. Monitor renal function regularly as eGFR declines with age. Contraindicated if eGFR <30 mL/min/1.73m². Avoid use in patients ≥80 years unless renal function is confirmed to be normal.

Kidney Impairment

eGFR ≥45: no adjustment; eGFR 30-44: do not initiate-if already on metformin, consider dose reduction (commonly max 1000 mg/day) and monitor renal function more frequently; eGFR <30: contraindicated.

Liver Impairment

Avoid/not recommended in hepatic impairment (no dose-adjustment strategy; generally do not use due to lactic acidosis risk).

Storage & Patient Advice

Stopping the Medicine

Can be stopped without tapering, but should not be discontinued without prescriber advice because glycemic control may worsen.

Overdose

Overdose can cause metformin-associated lactic acidosis (GI symptoms, malaise, myalgias, respiratory distress/hyperventilation, hypothermia, hypotension, bradyarrhythmias, altered mental status); management is emergency care with immediate discontinuation, supportive treatment, and hemodialysis to remove metformin and correct acidosis.

Patient Counseling

Take once daily with the evening meal; swallow whole-do not crush/chew/split. GI upset is common initially and often improves; report severe/persistent symptoms. Avoid excessive alcohol. Tell providers before iodinated-contrast imaging or major surgery (may need temporary interruption). Seek urgent care for possible lactic acidosis symptoms (e.g., rapid breathing, severe weakness, unusual muscle pain, abdominal pain, hypothermia). You may see an empty tablet shell in stool (normal with XR). Keep follow-up for HbA1c, kidney function, and periodic vitamin B12 assessment.

Monitoring Requirements

Glycemic control (HbA1c about every 3 months until stable then at least every 6 months; SMBG as clinically indicated); renal function (eGFR) at baseline and at least annually, more often if eGFR <60 or in elderly; vitamin B12 level periodically (e.g., every 2-3 years or sooner if anemia/neuropathy); assess for GI intolerance and symptoms of lactic acidosis when clinically indicated.

Pharmacology

Mechanism of Action

Decreases hepatic glucose production (gluconeogenesis), decreases intestinal glucose absorption, and improves insulin sensitivity/increases peripheral glucose uptake; does not stimulate insulin secretion (mechanistically linked to AMPK activation among other pathways).

Duration of Effect

Approximately 24 hours with once-daily prolonged-release dosing; full therapeutic effect may take up to 2 weeks.

Half-Life

Plasma elimination half-life ~6 hours (commonly ~4-8.7 h); longer apparent half-life in whole blood (~17 hours) due to erythrocyte distribution.

Bioavailability

Approximately 50-60% absolute oral bioavailability (metformin overall; XR may have similar or slightly lower systemic exposure than IR depending on formulation and fed state).

Metabolism

Not metabolized; eliminated largely unchanged via renal excretion (active tubular secretion).

Excretion

Eliminated unchanged in urine via renal tubular secretion and glomerular filtration; negligible metabolism.

Protein Binding

Negligible (essentially not bound to plasma proteins).

Product Information

Available Dosage Forms

Immediate-release tablet, prolonged-release (extended-release) tablet, oral solution

Composition per Dose

Each prolonged-release tablet: 750mg metformin hydrochloride

Generic Availability

Yes

OTC Alternatives

No OTC alternative

Diabetes Type

Type 2

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