GLUCARE XR 750/MG PR TAB 60/TAB

Indications

Approved Uses

Type 2 diabetes mellitus to improve glycemic control as an adjunct to diet and exercise; may be used alone or in combination with other antidiabetic agents/insulin (adult indication; pediatric use depends on local product labeling).

Off-Label Uses

Common off-label uses: PCOS; prediabetes/diabetes prevention in high-risk patients; antipsychotic-associated weight gain/metabolic effects. (Gestational diabetes use is off-label in some regions and depends on local guidance.)

Dosage & Administration

Dosing by Condition

Type 2 diabetes (adults, ER): start 500 mg once daily with the evening meal or 750 mg once daily if using a 750 mg ER tablet; titrate by 500 mg weekly (or 750 mg increments where applicable) as tolerated; usual max for ER is 2000 mg/day (some ER products allow 2000 mg once daily or divided).

Initial Dose

750 mg once daily with the evening meal

Maintenance Dose

1500-2000 mg once daily or in divided doses

Maximum Dose

2000 mg/day (extended-release); 2550 mg/day (immediate-release)

Children's Dosage

Not approved for children under 10 years of age. For children 10-16 years, the initial dose of immediate-release is 500 mg twice daily, with a maximum dose of 2000 mg per day. Extended-release is not approved for children.

Dose Adjustment Notes

Titrate gradually to minimize GI effects; assess renal function before start and periodically-contraindicated if eGFR <30 mL/min/1.73 m², do not initiate if eGFR 30-45 and reassess/consider dose reduction if it falls into this range; withhold at/around iodinated contrast in at‑risk patients and restart after ~48 hours once renal function is stable.

How to Take

Swallow GLUCARE XR (metformin ER) tablet whole with a meal (preferably the evening meal); do not crush, chew, or split.

Side Effects

Common Side Effects

Diarrhea, nausea, vomiting, abdominal bloating, flatulence, anorexia (loss of appetite), metallic taste.

Side Effect Frequency

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

Safety & Warnings

Contraindications

Contraindications: severe renal impairment (eGFR <30 mL/min/1.73 m²), acute or chronic metabolic acidosis (including diabetic ketoacidosis), and hypersensitivity to metformin; additionally, temporarily discontinue around iodinated contrast in at-risk patients per labeling.

Warnings & Precautions

Warnings/precautions: lactic acidosis risk (higher with renal impairment, hepatic disease, hypoxic states/heart failure, dehydration, sepsis, excessive alcohol, and age ≥65); assess eGFR before start and periodically; temporarily withhold for iodinated contrast in appropriate patients and around major surgery/acute illness; long-term use may cause vitamin B12 deficiency-consider periodic B12 monitoring; not for type 1 diabetes or DKA.

Age Restriction

Pediatric: Metformin ER (including 750 mg XR) is generally not established/approved for use in patients <18 years; metformin IR is approved for type 2 diabetes in children ≥10 years. Geriatric: use caution in older adults; do not initiate in patients ≥80 years unless renal function is confirmed normal and monitor renal function regularly.

Driving Warning

Safe

Drug Interactions

Drug Interactions

Key interactions: iodinated contrast media (temporary interruption in appropriate patients), alcohol (increases lactic acidosis risk), carbonic anhydrase inhibitors (e.g., topiramate/acetazolamide-metabolic acidosis risk), cationic drugs that reduce renal tubular secretion (e.g., cimetidine; also trimethoprim) increasing metformin exposure, and drugs that raise glucose (e.g., corticosteroids, some diuretics) requiring glycemic monitoring/adjustment.

Interaction Severity

MAJOR: Iodinated contrast media (risk of AKI → metformin accumulation/lactic acidosis; hold per eGFR/risk and restart after renal function stable). MODERATE: Excess alcohol; carbonic anhydrase inhibitors (e.g., topiramate/acetazolamide); cationic renally-secreted drugs (e.g., cimetidine, trimethoprim) that can raise metformin levels. MODERATE (glycemic effect): corticosteroids/diuretics can worsen hyperglycemia and reduce efficacy. MINOR/variable: ACE inhibitors may improve insulin sensitivity and can contribute to hypoglycemia when combined with other glucose-lowering agents; monitor.

Food Interaction

Take with food

Alcohol Interaction

Dangerous

Special Populations

Pregnancy

Consult Doctor

Breastfeeding

Safe

Children

Not approved for children under 10 years of age. For children 10-16 years, the initial dose of immediate-release is 500 mg twice daily, with a maximum dose of 2000 mg per day. Extended-release is not approved for children.

Elderly

Use with caution in patients ≥65 years; start at lower dose and titrate slowly; monitor renal function regularly as eGFR may decline with age; avoid use in patients ≥80 years unless renal function is confirmed to be normal

Kidney Impairment

eGFR ≥45: no dose adjustment (monitor at least annually). eGFR 30-44: do not initiate; if already on therapy, consider dose reduction (commonly max 1000 mg/day) and monitor renal function about every 3 months. eGFR <30: contraindicated.

Liver Impairment

Avoid use in patients with clinical or laboratory evidence of hepatic disease/impairment (no dose-adjustment strategy recommended).

Storage & Patient Advice

Stopping the Medicine

May be stopped without taper, but only under prescriber guidance; monitor blood glucose/A1c after stopping and ensure an alternative diabetes plan to prevent recurrent hyperglycemia.

Overdose

Overdose can cause lactic acidosis (predominant toxicity) and may cause hypoglycemia (uncommon, usually with co-ingestants/poor intake); management is immediate medical evaluation, stop metformin, supportive care, and consider hemodialysis to remove metformin and correct acidosis.

Patient Counseling

Take with a meal (often evening meal) and swallow whole; expect possible GI upset initially; avoid excessive alcohol; maintain hydration and seek advice during severe illness/vomiting/diarrhea; inform providers before contrast imaging/surgery; report symptoms suggestive of lactic acidosis; attend regular monitoring including kidney function and possible B12 checks.

Monitoring Requirements

Monitor renal function (eGFR) before initiation and at least annually (more often if elderly/at risk); monitor glycemic control (HbA1c about every 3 months until stable then every 3-6 months, plus SMBG as appropriate); consider periodic vitamin B12 with long-term use; monitor for GI intolerance and symptoms of lactic acidosis in high-risk situations.

Pharmacology

Mechanism of Action

Decreases hepatic glucose production (gluconeogenesis), decreases intestinal glucose absorption, and increases insulin sensitivity/peripheral glucose uptake (mechanistically linked to AMPK activation).

Duration of Effect

Approximately 24 hours for the extended-release formulation.

Half-Life

Plasma elimination half-life ≈6.2 hours; apparent half-life in whole blood ≈17.6 hours (due to erythrocyte distribution).

Bioavailability

Immediate-release metformin oral bioavailability is ~50-60% fasting; extended-release has lower/slower absorption with food affecting rate/extent (product-dependent).

Metabolism

Not metabolized; excreted unchanged in urine (renal elimination).

Excretion

Eliminated renally, primarily via active tubular secretion; excreted largely unchanged in urine.

Protein Binding

Negligible (essentially not bound to plasma proteins).

Product Information

Available Dosage Forms

Immediate-release tablet, Extended-release tablet, Oral solution.

Composition per Dose

Each extended-release tablet: 750 mg metformin hydrochloride

Generic Availability

Yes

OTC Alternatives

No OTC alternative to metformin; lifestyle measures and OTC glucose meters/supplies are not therapeutic substitutes.

Diabetes Type

Type 2

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