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Mitiglinide
Indications, Uses, Dosage, Drugs Interactions, Side effects
Mitiglinide
Medicine Type :
Allopathy
Allopathy
Prescription Type:
Prescription Required
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Schedule H
Pharmacological Class:
Meglitinides Derivatives, Therapy Class:
Antidiabetic Agent, Approved Countries
Italy, Spain, the United Kingdom, China, Germany, South Korea and Japan.
Mitiglinide is an anti-diabetic agent belonging to the pharmacological class of Meglitinides Derivatives.
Mitiglinide is approved for use in Japan but has not yet gained FDA approval for treating type 2 diabetes mellitus, particularly for individuals who experience post-meal elevations in blood glucose levels. It helps reduce the blood sugar levels by increasing insulin release from the pancreas in response to meals.
Mitiglinide is rapidly absorbed following oral administration, reaching peak plasma concentrations within 1 to 1.5 hours. It is mainly metabolized in the liver, and its metabolites are eliminated primarily through the kidneys.
Mitiglinide's most common side effects include diarrhoea, nausea, dizziness, headache, malaise and hypoglycemia.
Mitiglinide is available in the form of oral tablets.
The molecule is available in Italy, Spain, the United Kingdom, China, Germany, South Korea and Japan.
Mitiglinide is an Anti-diabetic Agent belonging to the pharmacological class of Meglitinides Derivatives.
Mitiglinide is thought to increase the production of insulin by attaching itself to and obstructing ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells (Kir6.2/SUR1 complex). Calcium influx is stimulated through voltage-gated calcium channels when potassium channels close, resulting in depolarization. The exocytosis of insulin granules is then triggered by high intracellular calcium.
Data duration of Mitiglinide action lasting about 2- 4 hr after each dose.
The onset of Mitiglinide action is shown typically within 30 minutes.
The Data of Tmax of Mitiglinide is typically within 0.5-1 hour after oral administration.
The Data of Cmax of Mitiglinide typically achieved within 0.23-0.28 hours after oral administration.
Mitiglinide is available in the form of oral tablets.
Tablets: To be swallowed whole with water/liquid. Do not chew, crush or break it.
As the physician recommends, take the medication orally three times daily; it is best taken before meals.
- Mitiglinide manages type 2 diabetes by helping regulate blood sugar levels.
- It regulates and lowers blood sugar levels by stimulating insulin release from the pancreas after meals.
- Mitiglinide can be used in combination with other antidiabetic medications to achieve better glycemic control in individuals with type 2 diabetes.
Mitiglinide helps in the control of type 2 diabetes. Stimulating insulin secretion, especially after meals, helps regulate blood sugar. Better glycemic control results from this, lowering the possibility of hyperglycemia. It works well for controlling post-meal glucose increases, which is crucial for the general management of diabetes. By enabling individualized dosage with meals, improving patient adherence, and promoting improved long-term blood sugar management, Mitiglinide offers therapeutic flexibility.
- Mitiglinide is indicated for type 2 diabetic patients whose response to the following medicines is insufficient in improving postprandial plasma glucose transition: diet management combined with exercise therapy alone, Utilization of α-glucosidase inhibitors, nutrition, and exercise.
- Mitiglinide is indicated when fasting blood glucose levels are equal to or greater than 126 mg/dL or postprandial blood glucose levels are similar to or greater than 200 mg/dL within a 1- or 2-hour period.
Orally: Mitiglinide is available as a tablet that can be taken orally. Mitiglinide should be taken before meals, usually within 5 minutes before eating. It is best to take it regularly at a fixed time each day following the physician's prescribed schedule for regular and evenly spaced intervals because the dose and duration of therapy are individualized per specific conditions to achieve the most effective and successful treatment outcome.
The dosage and duration of treatment should be as per the treating physician's clinical judgment.
Tablets: 5mg, 10 mg or 20 mg
Mitiglinide is available in the form of oral tablets.
Dose Adjustment in Adult Patients:
Adults should typically take 10 mg of mitiglinide three times a day before meals.
The dosage should be changed depending on the symptoms.
Mitiglinide should be used in treating Type 2 Diabetes Mellitus, along with appropriate nutritional limits.
There are no specific dietary restrictions when taking Mitiglinide. It is crucial to follow a good balanced and healthy diet.
Taking Mitiglinide just or up to 30 minutes before a meal is advised; skipping meals or delaying meals while on this medication can lead to low blood sugar (hypoglycemia). Also, limit or avoid the intake of alcohol, as it can interfere with blood sugar regulation.
The dietary restriction should be individualized as per patient requirements.
Mitiglinide may be contraindicated in the following conditions:-
- Patient with Type 1 diabetes mellitus, diabetic coma or pre-coma, or severe ketosis. [It is imperative to administer intravenous fluid or insulin to treat hyperglycemia promptly.]
- Patient who has experienced significant trauma before or after surgery or severe infections. [Controlling blood glucose levels using insulin injections is preferable. As a result, these patients shouldn't receive this medication.]
- Anyone who has previously experienced hypersensitivity to any of the product's constituents.
- Pregnant women or those who may get pregnant.
- Caution should be exercised when administering Mitiglinide to the following patient groups: those with hepatic dysfunction, renal dysfunction, ischemic heart disease, pituitary or adrenal insufficiency, and those with gastroenteropathy such as diarrhoea and vomiting.
- Mitiglinide should not be administered in cases of malnutrition, starvation, insufficient food intake, or frailty.
- During the maintenance of Mitiglinide treatment, regular monitoring of blood glucose levels and the patient's condition is essential. Alternative treatments should be considered if satisfactory effects are not achieved after two to three months.
- Mitiglinide has a rapid onset of insulin secretagogue activity at the same site as sulfonylurea-type agents. Due to unconfirmed additive/synergistic clinical effects and safety when combined with sulfonylurea-type agents, Mitiglinide should not be combined.
- The effectiveness and safety of concomitant use of Mitiglinide with insulin sensitizers (e.g., pioglitazone hydrochloride) or biguanides (e.g., metformin) have not been confirmed.
Alcohol Warning
It is unsafe to consume Mitiglinide with alcohol.
Breast Feeding Warning
Avoid use during breastfeeding.
Pregnancy Warning
It is not recommended for use during pregnancy.
Food Warning
Mitiglinide should be taken with meals and avoid excessive alcohol intake.
The adverse reactions related to Mitiglinide can be categorized as
- Common Adverse Effects: Hypoglycemia, upper respiratory tract infections, and headache
- Less Common Adverse Effects: Abdominal pain, diarrhoea, constipation, and dizziness.
- Rare Adverse Effects: Thrombocytopenia, leukopenia, anaemia, hypersensitivity reactions, and liver dysfunction.
The clinically relevant drug interactions of Mitiglinide are briefly summarized here.
May enhance the hypoglycemic effect when combined with insulin preparation, biguanides (like metformin), α-glucosidase inhibitors (like voglibose), insulin sensitizers (like pioglitazone HCl), salicylates (like aspirin), clofibrate, sulfanilamide (like sulfamethoxazole), β-adrenergic blocking agents (like propranolol), MAOIs, anabolic hormone (like mestanolone), and tetracyclines (like tetracycline HCl, minocycline HCl). Epinephrine, adrenocortical hormones (e.g., methylprednisolone), ovarian hormones (e.g., ethinylestradiol) & thyroid hormones, nicotinic acid, INH, pyrazinamide, phenothiazines (e.g., chlorpromazine), diuretics (e.g., thiazide, chlorthalidone, ethacrynic acid), phenytoin, and guanethidine sulphate may lessen the hypoglycemic effect.
The most common side effects of Mitiglinide include:
- Weight gain
- Hypoglycemia
- Edema
- Constipation
- Abdominal distension
- Pregnancy
Mitiglinide has not yet gained FDA approval
Women who are pregnant or may become pregnant should not take mitiglide. Mitiglinide can pass the placental barrier, according to research done on rats. Furthermore, in one case, a neonatal rat dam passed away, and the possibility that hypoglycemia—which may have been brought on by the pharmacological effects of GLUFAST (Mitiglinide)—played a role in the incident could not be rejected. As such, it is not advised to use mitigatriline while pregnant.
- Nursing Mothers
Breastfeeding mothers on Mitiglinide should not continue. This is due to the fact that rat studies have verified that mitiglinide is present in breast milk, which has raised concerns over possible exposure to nursing infants. As such, it is best to refrain from nursing while using mitiglinide.
- Pediatric Use
As per the FDA, safety and effectiveness in the pediatric population have not been established.
- Geriatric Use
Mitiglinide should be administered with caution to older individuals, as their physiological functions are commonly compromised. To guarantee the medication's efficacy and safety in this population, treatment may be initiated at a lower dose, usually 5 mg each, and blood glucose levels will be closely monitored.
The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Mitiglinide.
Overconsumption of Mitiglinide is unknown.There is no specific antidote or treatment for excessive intake of Mitiglinide. However, immediate medical attention is essential. Mitiglinide should be terminated immediately when an overdose is suspected or if any unusual symptoms occur after intake.
Pharmacodynamics
Suppressing action of blood glucose elevation: A single-dose trial employing the double-blind crossover approach was conducted on twenty individuals with Type 2 diabetes mellitus. To stop the rise in blood glucose, 10 mg of this medication was administered, encouraging more insulin to be secreted early after meals. Given orally, mitiglinide calcium hydrate suppressed increased blood glucose after loading the liquid meal orally. It decreased the post-loading plasma glucose area under the concentration-time curve value in streptozotocin-induced diabetes mellitus model rats due to its rapid-acting insulin secretion-promoting activity (in vivo).
Pharmacokinetics:
- Absorption and Distribution: When healthy adult men were given a single oral dose of 5, 10, and 20 mg of mitiglinide right before meals, the half-life (t½) was roughly 1.2 hours, and the maximum plasma concentration (Cmax) was attained 0.23-0.28 hours after administration.
- Metabolism and excretion: In healthy adult males, a single oral dose of 5, 10, and 20 mg of mitiglinide given right before meals resulted in 54–74% of the dose being eliminated in the urine within 24 hours, most of it as glucuronide conjugate metabolites. Less than 1% was accounted for by mitiglinide.
- Phillippe HM, Wargo KA. Mitiglinide: a novel agent for treatment of type 2 diabetes mellitus. Ann Pharmacother. 2010 Oct;44(10):1615-23. doi: 10.1345/aph.1P136. Epub 2010 Sep 14. PMID: 20841518.
- Ojima K, Kiyono Y, Kojima M. [Pharmacological and clinical profile of mitiglinide calcium hydrate (Glufast), a new insulinotropic agent with rapid onset]. Nihon Yakurigaku Zasshi. 2004 Oct;124(4):245-55. Japanese. doi: 10.1254/fpj.124.245. PMID: 15467258.
- Abe M, Okada K, Maruyama T, Maruyama N, Matsumoto K. Efficacy and safety of mitiglinide in the diabetic patients on the maintenance hemodialysis. Endocr J. 2010;57(7):579-86. doi: 10.1507/endocrj.k09e-318. Epub 2010 May 13. PMID: 20467165.
- Sunaga Y, et al. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. doi: 10.1016/s0014-2999(01)01412-1. PMID: 11716850.
- https://pubmed.ncbi.nlm.nih.gov/20841518/
- htthttps://bmcpharmacoltoxicol.biomedcentral.com/
- https://www.mims.com/thailand/drug/info/glufast/dosage
- https://newdrugapprovals.org/tag/mitiglinide/
Dr. Chumbeni E Lotha has completed her Bachelor of Pharmacy from RIPANS, Mizoram and Doctor of Pharmacy from SGRRU,Dehradun. She can be reached at editorial@medicaldialogues.in
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
Published on: 9 Nov 2023 5:53 AM GMT