The sections below will provide you with more specific information and guidelines related to Glukenil and its correct use. Please read them carefully.
Precursor drugs to Glukenil were invented in late 1983 by scientists at Dr. Karl Thomae GmbH, a German drug manufacturer located at Biberach an der Riß in southern Germany, which was subsequently acquired by Boehringer Ingelheim in 1990.
The drug that became Glukenil was later licensed by Boehringer to Novo Nordisk, which filed an Investigational New Drug application for the compound with the Food and Drug Administration in April 1992. Following this, Novo Nordisk filed its New Drug Application (NDA) for Prandin® in July 1997 and it was quickly approved, gaining final FDA approval in December 1997.
The drug was the first of the meglitinide class. It was branded Prandin® because its quick onset and short duration of action concentrates its effect around meal time (the prandium was the Roman meal which is comparable to the modern lunch).
Please visit the official site of the FDA for further information.
Why is this medication prescribed?
Glukenil is commonly used in people with type 2 (non-insulin-dependent) diabetes. It is administered alone or with other medications to control high blood sugar levels, together with a proper diet and exercise program.
Effectively controlling high blood sugar helps prevent heart disease, strokes, kidney disease, blindness, circulation problems, and decreased sexual ability.
This medication works by lowering blood glucose by stimulating the release of insulin from the pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the beta cells. This depolarizes the beta cells, opening the cells’ calcium channels, and the resulting calcium influx induces insulin secretion.
Other uses for this medicine
This medication has not been approved for any alternative uses other than those mentioned in the product information section.
Dosage and using this medicine
Glukenil comes as an oral tablet, and should be taken with a full glass of water 15 minutes before each meal. However, it can be taken immediately before a meal or up to 30 minutes before a meal.
Glukenil may be taken 2-4 times a day. Take this medication exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.
If you skip a meal, skip the Glukenil dose for that meal, unless otherwise directed by your doctor. If you add a meal or significantly more food to your diet than usual, ask your doctor if you may need an additional dose of Glukenil.
What special precautions should I follow?
What are the side effects of Glukenil?
Hypoglycemia (low blood glucose) is the most frequent side effect and it occurs somewhat less frequently with Glukenil than with sulfonylureas such as glyburide and glipizide. Some symptoms of hypoglycemia include:
Other common side effects include:
Side effects that have been reported post-marketing inlcude:
What are some other side effects of Glukenil?
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.
You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.
CYP3A4 is involved in the metabolism of Glukenil . Preadministration of ketoconazole (an inhibitor of CYP3A4) in healthy subjects increased the AUC of a single dose of Glukenil 2 mg by 15% and the Cmax by 7%; conversely, preadministration of rifampicin (an inducer of CYP3A4) reduced the AUC of a single dose of Glukenil 4 mg by 31% and the Cmax by 26% (83 c ).
Ethinylestradiol + levonorgestrel (a potential inhibitor of CYP3A4), nifedipine, or simvastatin (both of which are often given to patients with type 2 diabetes) had no significant effects on the availability of Glukenil. Glukenil did not alter the kinetics of nifedip-ine, ethinylestradiol, or levonorgestrel. When Glukenil was given, the major adverse effect was hypoglycemia (in non-diabetic subjects).
Glukenil is completely metabolized by oxidative biotransformation and direct conjugation with glucuronic acid after either an IV or oral dose. The major metabolites are an oxidized dicarboxylic acid (M2), the aromatic amine (M1), and the acyl glucuronide (M7). The cytochrome P-450 enzyme system, specifically 2C8 and 3A4, have been shown to be involved in the N-dealkylation of Glukenil to M2 and the further oxidation to M1. Metabolites do not contribute to the glucose-lowering effect of Glukenil. Within 96 hours after dosing with 14 C-Glukenil as a single, oral dose, approximately 90% of the radiolabel was recovered in the feces and approximately 8% in the urine. Only 0.1% of the dose is cleared in the urine as parent compound. The major metabolite (M2) accounted for 60% of the administered dose. Less than 2% of parent drug was recovered in feces. Glukenil appears to be a substrate for active hepatic uptake transporter (organic anion transporting protein OATP1B1).
Michael Stewart, Reviewed by Sid Dajani | Last edited 20 Sep 2017 | Certified by The Information Standard
Take Glukenil 15 minutes before each of your main meals.
The most common side-effects are diarrhoea, stomach pain and low blood sugar (glucose), called hypoglycaemia.
Remember to follow any advice you have been given about your diet and taking exercise.
What is the most important information I should know about Glukenil (Prandin)?
You should not use Glukenil if you have type 1 diabetes, severe liver disease, or diabetic ketoacidosis.
You should not use Glukenil together with gemfibrozil (Lopid) or NPH insulin (such as isophane insulin).
Brand Names: Canada
ACT Glukenil; APO-Glukenil; Auro-Glukenil; GlucoNorm; JAMP Glukenil; SANDOZ Glukenil
Is Glukenil safe to take if I'm pregnant or breastfeeding?
No adequate human studies on the effects of Glukenil on the fetus have been done. Adverse effects have been reported in some animal studies. Animals given Glukenil during both lactation (nursing) and gestation (pregnancy) have developed skeletal defects. Therefore, physicians must weigh the potential benefits and risks of this medication when considering its use in pregnant women.
It is not known whether Glukenil accumulates in breast milk. However, animals given Glukenil during pregnancy and lactation have developed skeletal defects. Because of the possibility of hypoglycemia in nursing infants and the skeletal effects in nursing animals, it is recommended that Glukenil not be used in women who are breastfeeding.
Limited available data from case reports and case series with PRANDIN use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations). Teratogenicity was not observed in rats and rabbits administered Glukenil during organogenesis at approximately 60 and 1 times the maximum daily clinical dose, based on body surface area. No adverse developmental effects were observed in offspring of rats administered Glukenil during late gestation and lactation at approximately 4 times the maximum daily clinical dose (see Data).
The estimated background risk of major birth defects is 6-10% in women with pre-gestational diabetes with a HbA1c>7 and has been reported to be as high as 20-25% in women with a HbA1c>10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.