Amaryl 4mg Tablets
It is used to lower blood sugar in patients with high blood sugar (diabetes).
Drug Class
Antidiabetic agent
Pharmacologic Class
Sulfonylurea
Pregnancy Category
Category C
FDA Approved
Dec 1995
DEA Schedule
Not Controlled
Overview
What is this medicine?
Glimepiride is a medication used to treat type 2 diabetes. It helps your body make more insulin, a hormone that lowers blood sugar. It also helps your body use insulin more effectively. It's usually taken once a day with your first meal.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with a meal, preferably with the first meal of the day if you're taking it once daily. Establish a routine by taking your medication at the same time every day. It's also important to know what to do if you don't eat as much as usual or if you skip a meal.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember, with a meal. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with a meal, preferably with the first meal of the day if you're taking it once daily. Establish a routine by taking your medication at the same time every day. It's also important to know what to do if you don't eat as much as usual or if you skip a meal.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember, with a meal. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Follow a healthy diet plan recommended by your doctor or a dietitian.
- Engage in regular physical activity as advised by your healthcare provider.
- Monitor your blood sugar levels regularly as instructed.
- Do not skip meals, especially after taking your medication, to avoid low blood sugar (hypoglycemia).
- Carry a source of fast-acting sugar (e.g., glucose tablets, hard candy, fruit juice) to treat low blood sugar.
- Limit or avoid alcohol consumption, as it can increase the risk of low blood sugar.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 1-2 mg orally once daily with breakfast or first main meal. Maintenance: 1-4 mg orally once daily.
Dose Range:
1 - 8 mg
Condition-Specific Dosing:
Type 2 Diabetes Mellitus:
Initial: 1-2 mg orally once daily. Titrate in increments of 1-2 mg at 1-2 week intervals based on blood glucose response. Maximum dose: 8 mg orally once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Safety and efficacy not established in pediatric patients)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed, but monitor closely.
Moderate:
Initial dose 1 mg orally once daily. Titrate cautiously. Maximum dose 4 mg orally once daily.
Severe:
Initial dose 1 mg orally once daily. Titrate cautiously. Maximum dose 4 mg orally once daily.
Dialysis:
Not recommended for use in dialysis patients due to risk of prolonged hypoglycemia; consider alternative agents.
Hepatic Impairment:
Mild:
Initial dose 1 mg orally once daily. Titrate cautiously.
Moderate:
Initial dose 1 mg orally once daily. Titrate cautiously.
Severe:
Not recommended due to increased risk of hypoglycemia; consider alternative agents.
Pharmacology
Mechanism of Action
Glimepiride is a sulfonylurea antidiabetic agent that lowers blood glucose by stimulating the release of insulin from the beta cells of the pancreatic islets. It also appears to increase the sensitivity of peripheral tissues to insulin and decrease hepatic glucose production. Its primary mechanism involves binding to the sulfonylurea receptor on the pancreatic beta-cell membrane, leading to closure of ATP-sensitive potassium channels, depolarization of the cell, and opening of voltage-gated calcium channels. The influx of calcium triggers insulin exocytosis.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
2-3 hours
FoodEffect:
Food decreases the rate of absorption (increased Tmax and decreased Cmax) but does not significantly affect the extent of absorption (AUC).
Distribution:
Vd:
8.8 L
ProteinBinding:
>99.5% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
5-9 hours (terminal half-life)
Clearance:
Not available
ExcretionRoute:
Approximately 60% via urine (as metabolites), 40% via feces (as metabolites)
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
2-4 hours
DurationOfAction:
Approximately 24 hours (allows for once-daily dosing)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Shortness of breath
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms of low blood sugar include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions, such as red, swollen, blistered, or peeling skin; skin irritation (with or without fever); red or irritated eyes; or sores in the mouth, throat, nose, or eyes
Other Possible Side Effects
Most people taking this medication will not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Upset stomach
Dizziness, tiredness, or weakness
Headache
Flu-like symptoms
Weight gain
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Shortness of breath
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Symptoms of low blood sugar include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other severe skin reactions, such as red, swollen, blistered, or peeling skin; skin irritation (with or without fever); red or irritated eyes; or sores in the mouth, throat, nose, or eyes
Other Possible Side Effects
Most people taking this medication will not experience serious side effects, but some may occur. If you notice any of the following side effects, contact your doctor if they bother you or do not go away:
Upset stomach
Dizziness, tiredness, or weakness
Headache
Flu-like symptoms
Weight gain
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Symptoms of low blood sugar (hypoglycemia): sweating, shaking, fast heartbeat, hunger, dizziness, confusion, irritability, headache, blurred vision. If these occur, consume 15-20 grams of fast-acting carbohydrate.
- Symptoms of high blood sugar (hyperglycemia): increased thirst, frequent urination, increased hunger, fatigue, blurred vision. Report these to your doctor.
- Signs of allergic reaction: rash, hives, swelling of face/lips/tongue/throat, difficulty breathing.
- Signs of liver problems: yellowing of skin or eyes (jaundice), dark urine, pale stools, persistent nausea or vomiting, severe stomach pain.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
A known sulfa allergy.
Acidic blood problems, such as acidosis.
Type 1 diabetes, as this medication is not intended to treat this condition.
Additionally, please note that:
This medication is not suitable for children and should not be administered to them.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist.
To ensure safe use, you must verify that it is safe to take this medication with all your other medications and health conditions.
Do not initiate, discontinue, or modify the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
A known sulfa allergy.
Acidic blood problems, such as acidosis.
Type 1 diabetes, as this medication is not intended to treat this condition.
Additionally, please note that:
This medication is not suitable for children and should not be administered to them.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist.
To ensure safe use, you must verify that it is safe to take this medication with all your other medications and health conditions.
Do not initiate, discontinue, or modify the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. To manage your condition effectively, follow the diet and exercise plan recommended by your doctor.
Be aware that this drug can cause low blood sugar, which may lead to severe consequences, including seizures, loss of consciousness, long-lasting brain damage, and even death. Consult your doctor to discuss ways to prevent and manage low blood sugar.
Regularly check your blood sugar levels as instructed by your doctor. If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you may be at a higher risk of developing anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent. Your doctor will monitor your condition through regular blood tests, so be sure to follow their instructions and discuss any concerns with them.
Avoid driving if you have experienced low blood sugar, as it can increase your risk of being involved in an accident. Before consuming alcohol, consult your doctor to understand the potential risks and interactions with this medication.
If you are taking colesevelam, take it at least 4 hours after taking this drug to minimize potential interactions. Be aware that stress, such as fever, infection, injury, or surgery, can affect your blood sugar control. Changes in physical activity, exercise, or diet can also impact your blood sugar levels.
This medication may increase the risk of death from heart disease. Discuss this potential risk with your doctor to understand the benefits and risks associated with this medication. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. They will help you weigh the benefits and risks of this medication for both you and your baby.
Be aware that this drug can cause low blood sugar, which may lead to severe consequences, including seizures, loss of consciousness, long-lasting brain damage, and even death. Consult your doctor to discuss ways to prevent and manage low blood sugar.
Regularly check your blood sugar levels as instructed by your doctor. If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you may be at a higher risk of developing anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent. Your doctor will monitor your condition through regular blood tests, so be sure to follow their instructions and discuss any concerns with them.
Avoid driving if you have experienced low blood sugar, as it can increase your risk of being involved in an accident. Before consuming alcohol, consult your doctor to understand the potential risks and interactions with this medication.
If you are taking colesevelam, take it at least 4 hours after taking this drug to minimize potential interactions. Be aware that stress, such as fever, infection, injury, or surgery, can affect your blood sugar control. Changes in physical activity, exercise, or diet can also impact your blood sugar levels.
This medication may increase the risk of death from heart disease. Discuss this potential risk with your doctor to understand the benefits and risks associated with this medication. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor. They will help you weigh the benefits and risks of this medication for both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe hypoglycemia (extremely low blood sugar)
- Confusion
- Slurred speech
- Seizures
- Loss of consciousness
- Coma
What to Do:
Immediately consume a fast-acting carbohydrate. If the person is unconscious or unable to swallow, call 911 or emergency medical services. Glucagon injection may be necessary. Call 1-800-222-1222 (Poison Control Center) for further advice.
Drug Interactions
Major Interactions
- Bosentan (increased risk of hepatotoxicity)
- Miconazole (oral, IV, topical - severe hypoglycemia)
- Fluconazole (increased glimepiride levels, hypoglycemia)
- NSAIDs (e.g., ibuprofen, naproxen - increased hypoglycemic effect)
- Salicylates (e.g., aspirin - increased hypoglycemic effect)
- Sulfonamides (e.g., sulfamethoxazole/trimethoprim - increased hypoglycemic effect)
- Beta-blockers (mask hypoglycemia symptoms, enhance hypoglycemic effect)
- Alcohol (potentiates hypoglycemic effect)
Moderate Interactions
- Corticosteroids (decrease hypoglycemic effect)
- Thiazide diuretics (decrease hypoglycemic effect)
- Thyroid products (decrease hypoglycemic effect)
- Estrogens/Oral Contraceptives (decrease hypoglycemic effect)
- Phenytoin (decrease hypoglycemic effect)
- Nicotinic acid (decrease hypoglycemic effect)
- Sympathomimetics (decrease hypoglycemic effect)
- Calcium channel blockers (decrease hypoglycemic effect)
- Isoniazid (decrease hypoglycemic effect)
- Chloramphenicol (increased hypoglycemic effect)
- Coumarin derivatives (e.g., warfarin - increased hypoglycemic effect, altered INR)
- MAOIs (increased hypoglycemic effect)
- Probenecid (increased hypoglycemic effect)
- Rifampin (decreased glimepiride levels, reduced efficacy)
Minor Interactions
- Antacids (may slightly alter absorption, generally not clinically significant)
Monitoring
Baseline Monitoring
Fasting Plasma Glucose (FPG)
Rationale: To establish baseline glycemic control and guide initial dosing.
Timing: Prior to initiation of therapy.
Hemoglobin A1c (HbA1c)
Rationale: To establish baseline long-term glycemic control and set treatment goals.
Timing: Prior to initiation of therapy.
Renal Function (e.g., eGFR, serum creatinine)
Rationale: Glimepiride is renally excreted; impairment requires dose adjustment.
Timing: Prior to initiation of therapy.
Hepatic Function (e.g., ALT, AST)
Rationale: Glimepiride is metabolized in the liver; impairment requires dose adjustment.
Timing: Prior to initiation of therapy.
Routine Monitoring
Fasting Plasma Glucose (FPG)
Frequency: Daily (patient self-monitoring) or at least weekly (clinician review) during dose titration, then periodically (e.g., monthly) once stable.
Target: <130 mg/dL (individualized)
Action Threshold: >130 mg/dL consistently (consider dose adjustment or add-on therapy); <70 mg/dL (assess for hypoglycemia, consider dose reduction).
Hemoglobin A1c (HbA1c)
Frequency: Every 3-6 months.
Target: <7% (individualized)
Action Threshold: >7% (consider dose adjustment or add-on therapy); <6.5% with frequent hypoglycemia (consider dose reduction).
Symptoms of Hypoglycemia
Frequency: Continuously (patient education and self-monitoring).
Target: N/A
Action Threshold: Any occurrence of symptoms (e.g., sweating, tremor, confusion, hunger, dizziness) requires immediate action (consume fast-acting carbohydrate) and subsequent evaluation of treatment regimen.
Renal Function (e.g., eGFR, serum creatinine)
Frequency: Annually, or more frequently in patients with existing renal impairment or risk factors.
Target: Stable, within normal limits or as appropriate for patient's baseline.
Action Threshold: Significant decline in eGFR (consider dose reduction or discontinuation).
Hepatic Function (e.g., ALT, AST)
Frequency: Periodically, especially if symptoms of liver dysfunction develop.
Target: Within normal limits.
Action Threshold: Significant elevation (investigate cause, consider discontinuation).
Symptom Monitoring
- Symptoms of hypoglycemia (e.g., sweating, tremor, palpitations, anxiety, hunger, confusion, dizziness, headache, blurred vision, slurred speech, irritability, mood changes, unsteadiness, fatigue, seizures, unconsciousness)
- Symptoms of hyperglycemia (e.g., increased thirst, increased urination, increased hunger, fatigue, blurred vision)
- Signs of allergic reaction (e.g., rash, itching, hives, swelling of face/lips/tongue/throat, difficulty breathing)
- Symptoms of liver problems (e.g., dark urine, pale stools, yellowing of skin/eyes, persistent nausea/vomiting, abdominal pain)
Special Patient Groups
Pregnancy
Generally not recommended during pregnancy. Insulin is the preferred treatment for diabetes during pregnancy. Glimepiride is classified as Pregnancy Category C (older classification) due to potential for fetal harm (e.g., hypoglycemia in neonates).
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity, though human data are limited and conflicting. Risk of hypoglycemia in the mother.
Second Trimester:
Risk of prolonged severe neonatal hypoglycemia if used near term. Insulin is preferred for glycemic control.
Third Trimester:
High risk of severe and prolonged neonatal hypoglycemia if used, especially in the last trimester. Discontinue at least 2 weeks before expected delivery.
Lactation
Not recommended during breastfeeding. Glimepiride and its metabolites are excreted into breast milk. There is a potential for serious adverse reactions, including hypoglycemia, in a breastfed infant.
Infant Risk:
L3 (Moderate risk) - Potential for hypoglycemia in the infant. Monitor infant for signs of hypoglycemia (e.g., lethargy, poor feeding, jitteriness).
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Use is generally not recommended due to lack of data and potential for hypoglycemia.
Geriatric Use
Use with caution in elderly patients due to increased risk of hypoglycemia, particularly in those with impaired renal or hepatic function. Start with a low dose (1 mg) and titrate slowly. Monitor blood glucose closely.
Clinical Information
Clinical Pearls
- Always take glimepiride with breakfast or the first main meal of the day to minimize the risk of hypoglycemia.
- Educate patients thoroughly on the symptoms and management of hypoglycemia.
- Patients should carry a source of fast-acting carbohydrate (e.g., glucose tablets, juice) at all times.
- Avoid alcohol consumption as it can potentiate the hypoglycemic effect.
- Monitor renal function regularly, especially in elderly patients or those with pre-existing kidney disease, as dose adjustments are necessary.
- Be aware of drug interactions, particularly with other medications that can affect blood glucose levels (e.g., beta-blockers, corticosteroids, NSAIDs).
- Consider alternative agents in patients with severe renal or hepatic impairment due to increased risk of prolonged hypoglycemia.
Alternative Therapies
- Metformin (first-line for most Type 2 DM patients)
- Other Sulfonylureas (e.g., Glipizide, Glyburide)
- DPP-4 Inhibitors (e.g., Sitagliptin, Saxagliptin)
- GLP-1 Receptor Agonists (e.g., Liraglutide, Semaglutide)
- SGLT2 Inhibitors (e.g., Canagliflozin, Dapagliflozin)
- Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
- Insulin
Cost & Coverage
Average Cost:
$10 - $30 per 30 tablets (generic 4mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.