GLUCARE XR 500/MG 60/TAB

Indications

Approved Uses

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

Off-Label Uses

Polycystic ovary syndrome (PCOS); diabetes prevention in high-risk prediabetes; antipsychotic-associated weight gain/insulin resistance (selected patients).

Dosage & Administration

Dosing by Condition

Type 2 diabetes mellitus (extended-release): start 500 mg orally once daily with the evening meal; increase by 500 mg weekly as tolerated; usual effective dose 1000-2000 mg once daily; maximum 2000 mg/day (some ER products allow 2000 mg once daily).

Initial Dose

500 mg orally once daily with the evening meal.

Maintenance Dose

1000-2000 mg once daily or in divided doses

Maximum Dose

2000 mg/day (extended-release); 3000 mg/day (immediate-release)

Children's Dosage

Extended-release form is not approved for children under 18 years. Immediate-release is approved for children 10 years and older.

Dose Adjustment Notes

Titrate by 500 mg increments no more frequently than weekly to reduce GI effects; assess renal function before start and periodically-contraindicated if eGFR <30 mL/min/1.73 m², and initiation is generally not recommended if eGFR 30-45 (if already on therapy, consider dose reduction and close monitoring).

How to Take

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

Side Effects

Common Side Effects

Diarrhea, nausea, vomiting, abdominal bloating, flatulence, anorexia, metallic taste.

Side Effect Frequency

Very common (≥10%): gastrointestinal effects (diarrhea, nausea, vomiting, abdominal pain; appetite loss may occur). Common (1-10%): taste disturbance. Very rare (<0.01%): lactic acidosis, hepatitis, skin reactions (e.g., erythema/pruritus/urticaria). Frequency not known/long-term: decreased vitamin B12 absorption leading to B12 deficiency.

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. (Not absolute contraindications but important precautions/temporary holds: iodinated contrast in at-risk patients, hypoxic states, and severe hepatic impairment).

Warnings & Precautions

Warnings/precautions: lactic acidosis risk-assess eGFR before start and periodically; avoid/withhold during acute illness causing dehydration or hypoxia and before/after iodinated contrast in at-risk patients; avoid excessive alcohol; use caution in age ≥65 due to renal decline; long-term therapy may cause vitamin B12 deficiency-consider periodic B12 monitoring; not indicated for type 1 diabetes or treatment of DKA.

Age Restriction

Extended-release formulation: Not approved under 18 years

Drug Interactions

Drug Interactions

Key interactions: iodinated contrast media (temporary withholding in at-risk patients), alcohol (increases lactic acidosis risk), cimetidine/other OCT2/MATE inhibitors (increase metformin exposure), carbonic anhydrase inhibitors e.g., topiramate (increase acidosis risk), diuretics (may worsen renal function/dehydration), corticosteroids (raise glucose/oppose effect), and other glucose-lowering agents (additive hypoglycemia risk when combined).

Interaction Severity

MAJOR: Iodinated contrast media (temporarily discontinue metformin at/around the time of contrast in at-risk patients and reassess renal function before restarting); Alcohol/excessive alcohol intake (increases lactic acidosis risk). MODERATE: Carbonic anhydrase inhibitors (e.g., topiramate/acetazolamide), cimetidine, and drugs that can impair renal function or worsen glycemia (e.g., diuretics, corticosteroids).

Food Interaction

Take with food (preferably the evening meal).

Alcohol Interaction

Use caution: excessive alcohol increases lactic acidosis risk

Special Populations

Pregnancy

Category B (old system); Risk Summary: Disease-associated maternal and/or embryo/fetal risk; Limited human data; Animal data show no adverse effects

Breastfeeding

Use with caution: present in human milk; monitor infant for GI effects, assess risk/benefit

Children

Extended-release form is not approved for children under 18 years. Immediate-release is approved for children 10 years and older.

Elderly

Start at lowest available dose and titrate cautiously; monitor renal function closely due to age-related decline in eGFR; contraindicated if eGFR <30 mL/min/1.73m²

Kidney Impairment

eGFR ≥60: no adjustment; monitor at least annually. eGFR 45-59: continue/initiate with routine monitoring (every 3-6 months if risk factors). eGFR 30-44: do not initiate; if already on metformin, consider dose reduction (often max 1000 mg/day) and monitor every 3 months. eGFR <30: contraindicated.

Liver Impairment

Avoid in severe hepatic impairment or significant active liver disease; mild-to-moderate impairment: no specific dose adjustment but use with caution due to lactic acidosis risk.

Storage & Patient Advice

Missed Dose

Take the missed dose with food as soon as remembered; if it is close to the next dose, skip the missed dose and resume the regular schedule-do not double doses.

Stopping the Medicine

Can be stopped abruptly if clinically necessary, but should generally be done under prescriber guidance with a plan to monitor glucose and arrange alternative therapy to avoid hyperglycemia.

Overdose

Overdose primarily causes lactic acidosis (often with nonspecific symptoms such as malaise, myalgias, abdominal distress, respiratory distress, somnolence; may progress to hypothermia, hypotension, bradyarrhythmias, altered mental status). Management: stop metformin, urgent hospital care/supportive treatment; hemodialysis is effective to remove metformin and correct acidosis.

Patient Counseling

Take once daily with the evening meal; swallow whole (do not crush/chew/split); the tablet shell may appear in stool; limit/avoid alcohol; inform providers before iodinated-contrast imaging or major surgery (may need temporary hold); seek urgent care for symptoms of lactic acidosis (e.g., severe weakness, muscle pain, trouble breathing, abdominal pain, persistent vomiting, feeling cold); keep follow-up for kidney function and periodic vitamin B12 monitoring.

Monitoring Requirements

Renal function (eGFR) at baseline and at least annually (more often if risk factors/elderly); glycemic control (HbA1c about every 3 months until stable then every 3-6 months, plus SMBG as appropriate); vitamin B12 periodically (e.g., every 1-2 years or if anemia/neuropathy); hepatic function if clinically indicated.

Pharmacology

Mechanism of Action

Decreases hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake/utilization (AMPK activation is a key mechanistic pathway).

Duration of Effect

Approximately 24 hours.

Half-Life

Plasma elimination half-life ≈6.2 hours; whole-blood half-life ≈17.6 hours (reflecting erythrocyte distribution).

Bioavailability

Approximately 50-60% (metformin oral bioavailability; ER has similar overall exposure but slower absorption vs immediate-release).

Metabolism

Not metabolized (no hepatic metabolism); excreted unchanged.

Excretion

Primarily renal excretion as unchanged drug (≈90% within 24 hours).

Protein Binding

Negligible

Product Information

Available Dosage Forms

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

Composition per Dose

Each extended-release tablet: 500 mg metformin hydrochloride

Generic Availability

Yes

OTC Alternatives

No OTC alternative

Diabetes Type

Type 2

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