Amaryl

Amaryl (glimepiride) is a second-generation sulfonylurea oral antidiabetic medication indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It functions primarily by stimulating insulin secretion from the pancreatic beta cells and increasing peripheral tissue sensitivity to insulin. This medication is a cornerstone in the management of hyperglycemia, particularly when metformin alone is insufficient or not tolerated. Proper use under medical supervision can significantly reduce the risk of diabetes-related complications.

Features

• Active Ingredient: Glimepiride
• Drug Class: Sulfonylurea
• Available Strengths: 1 mg, 2 mg, 4 mg tablets
• Administration: Oral, once daily
• Onset of Action: Within 1 hour
• Duration of Action: Up to 24 hours
• Bioavailability: Approximately 100%
• Protein Binding: >99.5%
• Metabolism: Hepatic (via CYP2C9)
• Excretion: Renal (60%) and fecal (40%)

Benefits

• Effective HbA1c Reduction: Demonstrated to lower hemoglobin A1c by an average of 1.5–2.0% in clinical studies.
• Convenient Once-Daily Dosing: Supports medication adherence and simplifies treatment regimens.
• Beta-Cell Specific Action: Binds with high affinity to sulfonylurea receptors, promoting glucose-dependent insulin secretion.
• Extrapancreatic Effects: Enhances peripheral glucose uptake and utilization in muscle and adipose tissue.
• Cardiovascular Safety Profile: No increased risk of cardiovascular mortality observed in long-term studies compared to other sulfonylureas.
• Flexible Combination Therapy: Can be effectively combined with metformin, DPP-4 inhibitors, or insulin when needed.

Common use

Amaryl is prescribed for the management of type 2 diabetes mellitus in adult patients when glycemic control cannot be achieved through diet and exercise alone. It is typically used as monotherapy or in combination with other oral antidiabetic agents like metformin. In some cases, it may be combined with basal insulin when dual therapy proves insufficient. It is not indicated for type 1 diabetes or diabetic ketoacidosis.

Dosage and direction

The initial recommended dose is 1–2 mg once daily, administered with the first main meal of the day (typically breakfast). Dose titration should occur in increments of 1–2 mg at 1–2 week intervals based on glycemic response. The usual maintenance dose is 1–4 mg daily; some patients may require up to 8 mg daily. Maximum recommended dose is 8 mg once daily. Patients transferring from other oral hypoglycemic agents should undergo careful dose conversion under medical supervision. Renal or hepatic impairment may require dose adjustment.

Precautions

• Regular monitoring of blood glucose and HbA1c is essential
• Higher risk of hypoglycemia, particularly in elderly patients, those with renal/hepatic impairment, or malnourished individuals
• May cause hemolytic anemia in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency
• Stress situations (e.g., fever, trauma, infection, surgery) may require temporary insulin therapy
• Photosensitivity reactions have been reported; advise sun protection measures
• Periodic liver function tests recommended during long-term therapy
• Educate patients about recognizing and managing hypoglycemic symptoms

Contraindications

• Hypersensitivity to glimepiride or other sulfonylureas/sulfonamides
• Type 1 diabetes mellitus
• Diabetic ketoacidosis, with or without coma
• Severe renal impairment (eGFR <30 mL/min/1.73m²)
• Severe hepatic impairment
• Pregnancy and breastfeeding
• Concomitant use with bosentan

Possible side effect

Common (≥1/100):

• Hypoglycemia
• Headache
• Dizziness
• Nausea
• Asthenia

Uncommon (≥1/1000, <1/100):

• Visual disturbances
• Transient liver enzyme elevations
• Pruritus
• Urticaria
• Gastrointestinal disturbances (abdominal pain, diarrhea)

Rare (<1/1000):

• Leukopenia
• Thrombocytopenia
• Aplastic anemia
• Hemolytic anemia
• Hyponatremia
• Severe cutaneous reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
• Hepatitis
• Photosensitivity reactions
• Disulfiram-like reactions with alcohol

Drug interaction

Potentiates hypoglycemic effect:

• Insulin and other antidiabetic agents
• ACE inhibitors
• Allopurinol
• Anabolic steroids
• Chloramphenicol
• Coumarin derivatives
• Cyclophosphamide
• Disopyramide
• Fenfluramine
• Fluconazole
• MAO inhibitors
• Miconazole
• Para-aminosalicylic acid
• Pentoxifylline
• Phenylbutazone
• Oxyphenbutazone
• Probencid
• Salicylates
• Sulfinpyrazone
• Sulfonamides
• Tetracyclines
• Trimethoprim
• Beta-blockers
• Alcohol

Reduces hypoglycemic effect:

• Acetazolamide
• Barbiturates
• Corticosteroids
• Diazoxide
• Diuretics
• Epinephrine
• Glucagon
• Isoniazid
• Nicotinic acid
• Estrogens
• Progestogens
• Phenothiazines
• Phenytoin
• Rifampicin
• Somatropin
• Sympathomimetics
• Thyroid hormones

May increase risk of hypoglycemia or hyperglycemia:

• Beta-blockers, clonidine, guanethidine, and reserpine

Other significant interactions:

• Bosentan (contraindicated)
• CYP2C9 inhibitors/inducers may affect glimepiride metabolism

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If remembered near the time of the next dose, skip the missed dose and resume the regular schedule. Do not double the dose to make up for a missed dose. Monitor blood glucose levels more frequently until the next scheduled dose.

Overdose

Symptoms primarily include severe hypoglycemia: sweating, tremor, anxiety, blurred vision, hunger, palpitations, nausea, fatigue, which may progress to seizures, coma, and neurological impairment. Management includes immediate glucose administration (oral or intravenous depending on consciousness level). Continuous glucose monitoring and supportive care are essential. Hemodialysis is not effective due to high protein binding. Hospitalization may be required for severe cases or prolonged hypoglycemia.

Storage

Store at room temperature (15–30°C or 59–86°F) in the original container. Protect from light and moisture. Keep tightly closed. Do not store in bathroom or near sink. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Discard any tablets that appear discolored or damaged.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Individual patient needs may vary. Always consult with a qualified healthcare professional before starting, changing, or stopping any medication. The prescribing physician should be aware of the patient’s complete medical history and concurrent medications. Patients should not self-adjust doses without medical supervision.

Reviews

Clinical studies demonstrate Amaryl’s efficacy in glycemic control with once-daily dosing convenience. The ADOPT study showed durable glycemic control over several years. The RECAP study confirmed its effectiveness in real-world settings with significant HbA1c reductions. Many endocrinologists appreciate its predictable pharmacokinetics and lower hypoglycemia risk compared to older sulfonylureas. Patient satisfaction surveys indicate good tolerability and preference for once-daily regimen. Long-term safety data from post-marketing surveillance supports its continued use in type 2 diabetes management.