Micronized

Micronized Uses, Dosage, Side Effects, Food Interaction and all others data.

Glibenclamide is an orally effective hypoglycaemic agent that reduces blood sugar concentration by stimulating secretion of endogenous insulin from the pancreatic β-cells. It stimulates the mobilization of endogenous insulin with a lower dosage and with few incidence of side effects that any available anti-diabetic. Hypoglycaemic action associated with short-term therapy appears to include reduction of basal hepatic glucose production and enhancement of peripheral insulin action at target sites.

Micronized is a second generation sulfonylurea that stimulates insulin secretion through the closure of ATP-sensitive potassium channels on beta cells, raising intracellular potassium and calcium ion concentrations. Glibenclamide has a long duration of action as it is given once daily, and a wide therapeutic index as patients are started at doses as low as 0.75mg but that can increase as high as 10mg or more. Patients taking glyburide should be cautioned regarding an increased risk of cardiovascular mortality as seen with tolbutamide, another sulfonylurea.

Trade Name Micronized
Availability Prescription only
Generic Glyburide
Glyburide Other Names Glibenclamida, Glibenclamide, Glibenclamidum, Glyburide
Related Drugs Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir
Type Oral
Formula C23H28ClN3O5S
Weight Average: 494.004
Monoisotopic: 493.143819418
Protein binding

Glyburide is 99.9% bound to protein in plasma with >98% accounted for by binding to serum albumin.

Groups Approved
Therapeutic Class Sulfonylureas
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Micronized
Micronized

Uses

Glibenclamide is used in the treatment of non insulin dependent diabetes melitus (NIDDM). It is ineffective in completely pancreatectomized patients and in juvenile-onset type of diabetes, in which the pancreas has lost all or nearly all of its capacity to secrete insulin. Such patients require insulin and attempts to control them with oral therapy are dangerous and doomed to failure.

Micronized is also used to associated treatment for these conditions: Gestational Diabetes Mellitus (GDM), Glycemic Control, Type 2 Diabetes Mellitus

How Micronized works

Micronized belongs to a class of drugs known as sulfonylureas. These drugs act by closing ATP-sensitive potassium channels on pancreatic beta cells. The ATP-sensitive potassium channels on beta cells are known as sulfonylurea receptor 1 (SUR1).

Under low glucose concentrations, SUR1 remains open, allowing for potassium ion efflux to create a -70mV membrane potential.

Normally SUR1 closes in response to high glucose concentrations, the membrane potential of the cells becomes less negative, the cell depolarizes, voltage gated calcium channels open, calcium ions enter the cell, and the increased intracellular calcium concentration stimulates the release of insulin containing granules.

Micronized bypasses this process by forcing SUR1 closed and stimulating increased insulin secretion.

Dosage

Micronized dosage

Initially stabilization dosage: Glibenclamide half tablet (2.5 mg) should be taken initially during or immediately after breakfast. 3-5 days after initiation of the drug, the blood sugar level and urine sugar level should be checked. Daily dose of ½ tablet (2.5 mg) may be continued as maintenance therapy if good control has been achieved. If the result is not good, increment of daily dose in steps of ½ tablet (2.5 mg) is necessary at intervals of 3-5 days up to a maximum of 3 tablets. Daily doses in excess of 10 mg may be taken in 2 divided doses. Patients should be given ½ to 1 tablet of Glibenclamide in changing over from other oral anti-diabetics with a similar action.

Change over from insulin to Glibenclamide:The mildly diabetic patient whose insulin requirement is fewer than 20 units daily, can be started on the initial dosage of Glibenclamide with immediate discontinuation of insulin. If the insulin requirement is moderate or high, the changeover should be made gradually by giving insulin and Glibenclamide simultaneously and slowly cutting down the dose of insulin.

When insulin requirements are increased as in fever, surgical interventions or trauma, the Glibenclamide alone is inadequate and the patient must be given insulin to carry him or her through such critical situation.

This changeover from insulin to Glibenclamide is strictly for NIDDM of fairly recent onset which is being controlled on small doses of insulin. This should preferably be done in hospital or with daily medical supervision.

Side Effects

Glibenclamide is well tolerated. Few side effects that may arise include nausea, vomiting, epigastric pain, dizziness, weakness, paraesthesia and headache. Allergic skin reactions and haemopoietic reactions (leukopenia, thrombocytopenia, etc.) are occasionally observed.

Toxicity

The oral LD50 in rats is >3200mg/kg, in mice is >1500mg/kg, in rabbits is >10,000mg/kg, and in guinea pigs is >1500mg/kg.

Patients experiencing an overdose may present with hypoglycemia. Mild hypoglycemia should be treated with oral glucose and adjustments to drug doses or meal schedules. Severe hypoglycemia may present with coma, seizure, and neurological impairment. This should be treated immediately in hospital with intravenous glucose and monitoring for 24-48 hours.

Precaution

Weight reduction is of the greatest importance in the treatment of diabetes. A vigorous effort must be made by the patient and the physician to reduce the patient's weight as an integral part of diabetic treatment, irrespective of the drug chosen.

Interaction

Alcohol, cyclophosphamide, dicoumarol, monoamino oxidase inhibitors, phenylbutazone, propranolol and other beta-adrenergic blocking agents and certain long-acting sulphonamides may enhance the hypoglycemic effect of Glibenclamide

Food Interaction

  • Avoid alcohol. Alcohol increases the risk of hypoglycemia.
  • Take before a meal. Take 30-60 minutes before breakfast.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Volume of Distribution

Elderly patients have a volume of distribution of 19.3-52.6L, while younger patients have a volume of distribution of 21.5-49.3L.

Elimination Route

Elderly patients taking glyburide reached a Cmax of 211-315ng/mL with a Tmax of 0.9-1.0h, while younger patients reached a Cmax of 144-302ng/mL with a Tmax of 1.3-3.0h. Patients taking glyburide have and AUC of 348ng*h/mL.

Half Life

Elderly patients have a terminal elimination half life of 4.0-13.4h, while younger patients have a terminal elimination half life of 4.0-13.9h.

Clearance

Elderly patients have a clearance of 2.70-3.55L/h, while younger patients have a clearance of 2.47-4.11L/h.

Elimination Route

Unlike other sulfonylureas, glyburide is 50% excreted in the urine and 50% in the feces. Micronized is mainly excreted as the metabolite 4-trans-hydroxyglyburide.

Pregnancy & Breastfeeding use

There is no information on the use of Glibenclamide in human pregnancy but it has been in wide, general use for many years without apparent ill consequence. Animal studies have shown no hazard. It has not yet been established whether Glibenclamide is transferred to human milk. However, other sulphonylureas have been found in milk and there is no evidence to suggest that Glibenclamide differs from the group in this respect.

Contraindication

Severe metabolic de-compensation with acidosis, pre-comatose states and diabetic coma, severe renal or hepatic dysfunction or serious impairment of typhoid or adrenal function; pregnancy, diabetes mellitus complicated by fever, trauma or gangrene.

Acute Overdose

Symptoms: Hypoglycaemia.

Management: Mild hypoglycaemic symptoms without loss of consciousness or neurologic findings may be treated with oral glucose and adjust drug dosage and/or meal patterns.

Storage Condition

Should be stored in a dry place below 30˚ C.

Innovators Monograph

You find simplified version here Micronized

Micronized contains Glyburide see full prescribing information from innovator Micronized Monograph, Micronized MSDS, Micronized FDA label

FAQ

What is Micronized used for?

Micronized is a medication used to treat diabetes mellitus type 2. It is recommended that it be taken together with diet and exercise. It may be used with other antidiabetic medication.

How safe is Micronized?

Micronized can increase your risk of a heart attack or stroke. This can sometimes be fatal. Tell your doctor if you have a heart condition before you start taking this drug.

How does Micronized work?

Micronized lowers blood sugar by causing the pancreas to produce insulin (a natural substance that is needed to break down sugar in the body) and helping the body use insulin efficiently. 

What are the common side effects of Micronized?

Common side effects of Micronized are include:

  • Skin swelling.
  • Hives.
  • Rash.
  • Drug rash.
  • Itching.
  • Photosensitivity reaction.
  • Heartburn.
  • Vasculitis.

Is Micronized safe during pregnancy?

Micronized is thought to be safe for use during pregnancy for treatment of gestational diabetes mellitus (GDM).

Is Micronized safe during breastfeeding?

The exposure of infants to second-generation sulfonylureas (eg, glipizide, glyburide) through breast milk is expected to be minimal, based on the limited data available. Women with type 2 diabetes treated with sulfonylureas should not be discouraged from breastfeeding.

Can I drink alcohol with Micronized?

Avoid drinking alcohol. It lowers blood sugar and may interfere with your diabetes treatment. Micronized could make you sunburn more easily.

What is the best time to take Micronized ?

It is usually taken once a day with breakfast or the first main meal of the day.

How much can I take Micronized daily?

The dose is usually not more than 20 mg of Micronized and 2000 mg of Micronized per day.

How long does Micronized take to work ?

Micronized lowers your blood sugar anywhere from 15 to 60 minutes after taking the dose.

How long does stay in my system ?

The decrease of Micronized in the serum of normal healthy individuals is biphasic, the terminal half-life being about 10 hours.

Can I just stop taking Micronized?

Do not stop taking Micronized and metformin without talking to your doctor.

Can I take Micronized for a long time?

Micronized oral tablet is used for long-term treatment. It comes with serious risks if you don't take it as prescribed. If you miss doses or don't take it at all: If you don't take Micronized as prescribed by your doctor, your blood sugar levels won't be controlled.

Is Micronized bad for my heart?

Micronized should be avoided in all cardiac patients. Micronized can increase your risk of a heart attack or stroke. This can sometimes be fatal. Tell your doctor if you have a heart condition before you start taking this drug.

Is Micronized bad for my kidneys?

Micronized use should be avoided in patients with severe kidney impairment.

Who should not take Micronized?

You should not use Micronized if you are being treated with bosentan (Tracleer), or if you have diabetic ketoacidosis (call your doctor for treatment). Micronized is not for treating type 1 diabetes.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention. A glyburide overdose can cause life-threatening hypoglycemia. Symptoms of severe hypoglycemia include extreme weakness, nausea, tremors, sweating, confusion, trouble speaking, fast heartbeats, or seizure.

What happen If I stop taking Micronized?

If you stop taking Micronized your blood sugar levels won't be controlled. This can lead to complications from diabetes, such as nerve damage, heart disease, heart attack, stroke, and eye damage.

Can Micronized affects my liver?

Micronized may build up in your body, which can cause lower blood sugar levels. For people with liver disease: Your doctor may lower your dosage of Micronized if you have liver damage or liver disease.

*** Taking medicines without doctor's advice can cause long-term problems.
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