I am diabetic

Absorption
After oral administration, glimepiride is completely (100%) absorbed from the GI tract. Studies with single oral doses in normal subjects and with multiple oral doses in patients with Type 2 diabetes have shown significant absorption of glimepiride within 1 hour after administration and peak drug levels (Cmax) at 2 to 3 hours. When glimepiride was given with meals, the mean Tmax (time to reach Cmax) was slightly increased (12%) and the mean Cmax and AUC (area under the curve) were slightly decreased (8% and 9%, respectively).

Distribution
After intravenous (IV) dosing in normal subjects, the volume of distribution (Vd) was 8.8 L (113 mL/kg), and the total body clearance (CL) was 47.8 mL/min. Protein binding was greater than 99.5%.

Metabolism

Glimepiride is completely metabolized by oxidative biotransformation after either an IV or oral dose. The major metabolites are the cyclohexyl hydroxy methyl derivative (M1) and the carboxyl derivative (M2). Cytochrome P450 2C9 has been shown to be involved in the biotransformation of glimepiride to M1. M1 is further metabolized to M2 by one or several cytosolic enzymes. M1, but not M2, possesses about 1/3 of the pharmacological activity as compared to its parent in an animal model; however, whether the glucose-lowering effect of M1 is clinically meaningful is not clear. Excretion
When 14C-glimepiride was given orally, approximately 60% of the total radioactivity was recovered in the urine in 7 days and M1 (predominant) and M2 accounted for 80-90% of that recovered in the urine. Approximately 40% of the total radioactivity was recovered in feces and M1 and M2 (predominant) accounted for about 70% of that recovered in feces. No parent drug was recovered from urine or feces. After IV dosing in patients, no significant biliary excretion of glimepiride or its M1 metabolite has been observed.

Special Populations

Geriatric
Comparison of glimepiride pharmacokinetics in Type 2 diabetic patients ?65 years and those >65 years was performed in a study using a dosing regimen of 6 mg daily. There were no significant differences in glimepiride pharmacokinetics between the two age groups. The mean AUC at steady state for the older patients was about 13% lower than that for the younger patients; the mean weight-adjusted clearance for the older patients was about 11% higher than that for the younger patients.

Pediatric
The pharmacokinetics of glimepiride (1 mg) were evaluated in a single dose study conducted in 30 Type 2 diabetic patients (Male = 7; Female = 23) between ages 10 and 17 years. The mean AUC(0-last)(338.8�203.1 ng�hr/mL), Cmax (102.4�47.7 ng/mL) and T1/2(3.1�1.7 hours) were comparable to those previously reported in adults (AUC(0-last) 315.2�95.9 ng�hr/mL, Cmax 103.2�34.3 ng/mL and T1/2 5.3�4.1 hours).

Gender
There were no differences between males and females in the pharmacokinetics of glimepiride when adjustment was made for differences in body weight.

Race
No pharmacokinetic studies to assess the effects of race have been performed, but in placebo-controlled studies of Amaryl (glimepiride tablets) in patients with Type 2 diabetes, the antihyperglycemic effect was comparable in whites (n = 536), blacks (n = 63), and Hispanics (n = 63).

Renal Insufficiency
A single-dose, open-label study was conducted in 15 patients with renal impairment. Amaryl (3 mg) was administered to 3 groups of patients with different levels of mean creatinine clearance (CLcr); (Group I, CLcr = 77.7 mL/min, n = 5), (Group II, CLcr = 27.7 mL/min, n = 3), and (Group III, CLcr = 9.4 mL/min, n = 7). Amaryl was found to be well tolerated in all 3 groups. The results showed that glimepiride serum levels decreased as renal function decreased. However, M1 and M2 serum levels (mean AUC values) increased 2.3 and 8.6 times from Group I to Group III. The apparent terminal half-life (T1/2) for glimepiride did not change, while the half-lives for M1 and M2 increased as renal function decreased. Mean urinary excretion of M1 plus M2 as percent of dose, however, decreased (44.4%, 21.9%, and 9.3% for Groups I to III).
A multiple-dose titration study was also conducted in 16 Type 2 diabetic patients with renal impairment using doses ranging from 1-8 mg daily for 3 months. The results were consistent with those observed after single doses. All patients with a CLcr less than 22 mL/min had adequate control of their glucose levels with a dosage regimen of only 1 mg daily. The results from this study suggested that a starting dose of 1 mg Amaryl may be given to Type 2 diabetic patients with kidney disease, and the dose may be titrated based on fasting blood glucose levels.

Hepatic Impairment
No studies were performed in patients with hepatic insufficiency.

Other Populations
There were no important differences in glimepiride metabolism in subjects identified as phenotypically different drug-metabolizers by their metabolism of sparteine. The pharmacokinetics of glimepiride in morbidly obese patients were similar to those in the normal weight group, except for a lower Cmax and AUC. However, since neither Cmax nor AUC values were normalized for body surface area, the lower values of Cmax and AUC for the obese patients were likely the result of their excess weight and not due to a difference in the kinetics of glimepiride.

Product Description

Most important information about Amaryl

Possible Side Effects

More information about AMARYL (Glimepiride):

Amaryl-Metformin Combination Therapy

Amaryl-Insulin Combination Therapy

FDA MedWatch Alerts

To buy Amaryl click HERE: My Family Drugstore

What is the most important information I should know about Amaryl?
Treatment with glimepiride may increase the risk of death from cardiovascular disease compared to treatment of diabetes with diet alone or diet plus insulin. Discuss with your doctor the risks and benefits of treatment with glimepiride.
Know the signs and symptoms of low blood sugar (hypoglycemia), which include headache, drowsiness, weakness, dizziness, fast heartbeat, sweating, tremor, and nausea. Carry a piece of hard candy or glucose tablets with you to treat episodes of low blood sugar.
Follow diet, medication, and exercise routines closely. Changing any of them can affect your blood sugar levels.
Do not change your dose of glimepiride without first talking to your doctor.
Avoid alcohol. It lowers blood sugar and may interfere with your diabetes treatment.
What should I discuss with my doctor before taking Amaryl?
Some medical conditions may interact with Amaryl. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding
• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
• if you have allergies to medicines, foods, or other substances
• if you have had a severe allergic reaction (eg, a severe rash, hives, breathing difficulties, dizziness) to any other sulfonamide medicine, such as acetazolamide, celecoxib, certain diuretics (eg, hydrochlorothiazide), glipizide, probenecid, sulfamethoxazole, valdecoxib, or zonisamide
• if you have a history of stroke or liver, kidney, thyroid, heart, or blood vessel problems
• if you have stomach or bowel problems (eg, stomach or bowel blockage, stomach paralysis), drink alcohol, or have had poor nutrition
• if you have type 1 diabetes, very poor health, a high fever, a severe infection, severe diarrhea, or high blood acid levels, or have had a severe injury
• if you have a history of certain hormonal problems (eg, adrenal or pituitary problems, syndrome of inappropriate secretion of antidiuretic hormone [SIADH]), or low blood sodium levels
• if you will be having surgery

You may not be able to take amaryl, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.
Patients 65 years of age and older may have a stronger reaction to glimepiride and may require a reduced dose.
Glimepiride is in the FDA pregnancy category C. This means that it is not known whether glimepiride will be harmful to an unborn baby. Insulin is usually the drug of choice to control diabetes during pregnancy. Do not take glimepiride without first talking to your doctor if you are pregnant or could become pregnant during treatment.
It is not known whether glimepiride passes into breast milk. Do not take glimepiride without first talking to your doctor if you are breast-feeding a baby.

Product Description

Pharmacokinetics

Possible Side Effects

More information about AMARYL (Glimepiride):

Amaryl-Metformin Combination Therapy

Amaryl-Insulin Combination Therapy

FDA MedWatch Alerts

To buy Amaryl click HERE: My Family Drugstore

Drug Name
Amaryl (Glimepiride)

Generic Name
Glimepiride (glye-MEP-i-ride)

Manufacturer / Distributor
Aventis Pharmaceuticals

Looks like
Glimepiride is available with a prescription under the brand name Amaryl. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.

• Amaryl 1 mg-pink, flat-faced, oblong tablets
• Amaryl 2 mg-green, flat-faced, oblong tablets
• Amaryl 4 mg-blue, flat-faced, oblong tablets

Dosage Form
Tablets

Route Of Administration
ORAL

Imprint Code
AMA;RYL

Size
10mm

Alternatives
Glucotrol XL

Drug Uses
Amaryl is an anti-diabetic drug (sulfonylurea-type) used along with a proper diet and exercise program to control high blood sugar. It is used in patients with type 2 diabetes (non-insulin-dependent diabetes). It works by stimulating the release of your body’s natural insulin. Effectively controlling high blood sugar.
Helps prevent:

• heart disease,
• strokes,
• kidney disease,
• blindness,
• and circulation problems, as well as sexual function problems (impotence).

Drug class
Amaryl is an oral blood sugar-lowering drug in a class of medicines for controlling diabetes called sulfonylureas. Amaryl is related to other sulfonylureas including:

• glyburide (Micronase; Diabeta),
• glipizide (Glucotrol),
• tolbutamide (Orinase)
• and tolazamide (Tolinase).

Amaryl is used in type II diabetes, the most common type of diabetes that is found in 90% of patients with diabetes. In type II diabetes, insulin usually is not necessary to control the blood sugar. Instead, diet and oral medications often are sufficient. Intolerance to sugar that results in elevated blood sugar is caused by reduced insulin secretion by the pancreas and resistance to insulin’s effects by the body’s cells. Amaryl lowers the sugar level in the blood by stimulating insulin to be secreted from the pancreas into the blood. Insulin causes sugar to leave the blood and enter cells throughout the body.

Contains
Amaryl (glimepiride tablets) is an oral blood-glucose-lowering drug of the sulfonylurea class. Glimepiride is a white to yellowish-white, crystalline, odorless to practically odorless powder formulated into tablets of 1-mg, 2-mg, and 4-mg strengths for oral administration.
Amaryl Tablets contain:

• the active ingredient glimepiride
• and the following inactive ingredients: lactose (hydrous), sodium starch glycolate, povidone, microcrystalline cellulose, and magnesium stearate.

In addition, Amaryl 1-mg tablets contain Ferric Oxide Red,
Amaryl 2-mg tablets contain Ferric Oxide Yellow and FD&C Blue #2 Aluminum Lake,
and Amaryl 4-mg tablets contain FD&C Blue #2 Aluminum Lake.

Chemical formula
Chemically, glimepiride is identified as 1 – [[p - [2 - (3 - ethyl - 4 - methyl - 2 - oxo - 3 - pyrroline - 1 - carboxamido)ethyl]phenyl]sulfonyl] – 3 – (trans – 4 – methylcyclohexyl)urea. The CAS Registry Number is 93479-97-1.

Mechanism of Action
The primary mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells. In addition, extrapancreatic effects may also play a role in the activity of sulfonylureas such as glimepiride. This is supported by both preclinical and clinical studies demonstrating that glimepiride administration can lead to increased sensitivity of peripheral tissues to insulin. These findings are consistent with the results of a long-term, randomized, placebo-controlled trial in which Amaryl therapy improved postprandial insulin/C-peptide responses and overall glycemic control without producing clinically meaningful increases in fasting insulin/C-peptide levels. However, as with other sulfonylureas, the mechanism by which glimepiride lowers blood glucose during long-term administration has not been clearly established.
Amaryl is effective as initial drug therapy. In patients where monotherapy with Amaryl or metformin has not produced adequate glycemic control, the combination of Amaryl and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different primary mechanisms of action. This complementary effect has been observed with metformin and other sulfonylureas, in multiple studies.

How Taken
Take amaryl exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.
Take each dose with a full glass of water.
Amaryl is usually taken once a day, with breakfast or the first main meal. Follow your doctor’s instructions.
It is important to take amaryl regularly to get the most benefit.
Your healthcare provider may recommend regular monitoring of blood sugar levels with blood or urine tests.
Do not change your dose of glimepiride without first talking to your doctor.

Dosage and Administration
ADULTS
The usual starting dose is 1 to 2 milligrams taken once daily with breakfast or the first main meal. The maximum starting dose is 2 milligrams.
If necessary, your doctor will gradually increase the dose 1 or 2 milligrams at a time every 1 or 2 weeks. Your diabetes will probably be controlled on 1 to 4 milligrams a day; the most you should take in a day is 8 milligrams. If the maximum dose fails to do the job, your doctor may add Glucophage to your regimen. Weakened or malnourished people and those with adrenal, pituitary, kidney, or liver disorders are particularly sensitive to hypoglycemic drugs such as Amaryl and should start at 1 milligram once daily. Your doctor will increase your medication based on your response to the drug.

CHILDREN
Safety and effectiveness in children have not been established.

Usual Starting Dose
The usual starting dose of Amaryl as initial therapy is 1-2 mg once daily, administered with breakfast or the first main meal. Those patients who may be more sensitive to hypoglycemic drugs should be started at 1 mg once daily, and should be titrated carefully.
No exact dosage relationship exists between Amaryl and the other oral hypoglycemic agents. The maximum starting dose of Amaryl should be no more than 2 mg.

Usual Maintenance Dose
The usual maintenance dose is 1 to 4 mg once daily. The maximum recommended dose is 8 mg once daily. After reaching a dose of 2 mg, dosage increases should be made in increments of no more than 2 mg at 1-2 week intervals based upon the patient’s blood glucose response. Long-term efficacy should be monitored by measurement of HbA1c levels, for example, every 3 to 6 months.

Missed Dose
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Overdose
Seek emergency medical attention if you think you have used too much of this medicine. Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center ( http://www.aapcc.org/findyour.htm ), or emergency room immediately.
Symptoms of a glimepiride overdose include hunger, nausea, anxiety, cold sweats, weakness, drowsiness, unconsciousness, and coma.

Storage
Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

How Supplied
Amaryl Tablets are available in the following strengths and package sizes:

• 1 mg (pink, flat-faced, oblong with notched sides at double bisect, either imprinted with “AMA RYL” on one side) or imprinted with “AMA RYL” on one side and the Hoechst logo on both sides of the bisect on the other side)
  [Bottles of 100] [(NDC 0039-0221-10)]
• 2 mg (green, flat-faced, oblong with notched sides at double bisect, either imprinted with “AMA RYL” on one side) or imprinted with “AMA RYL” on one side and the Hoechst logo on both sides of the bisect on the other side)
  [Bottles of 100] [(NDC 0039-0222-10)]
  [Unit Dose Cartons (100)] [(NDC 0039-0222-11)]
• 4 mg (blue, flat-faced, oblong with notched sides at double bisect, either imprinted with “AMA RYL” on one side, or imprinted with “AMA RYL” on one side and the Hoechst logo on both sides of the bisect on the other side)
  [Bottles of 100] [(NDC 0039-0223-10)]
  [Unit Dose Cartons (100)] [(NDC 0039-0223-11)]

Most important information about Amaryl

Pharmacokinetics

Possible Side Effects

More information about AMARYL (Glimepiride):

Amaryl-Metformin Combination Therapy

Amaryl-Insulin Combination Therapy

FDA MedWatch Alerts

To buy Amaryl click HERE: My Family Drugstore