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Voglibose + Metformin
Indications, Uses, Dosage, Drugs Interactions, Side effects
Voglibose + Metformin
Drug Related WarningVoglibose + Metformin
- VOGLIBOSE + METFORMIN may elevate the risk of cardiovascular diseases and hypoglycemic conditions in patients with renal and liver diseases.
- Combined with other alpha-glucosidase inhibitors, it can lead to pneumatosis intestinalis, characterized by gas-filled cysts on the bowel wall. Thorough monitoring for gastrointestinal side effects is recommended.
- VOGLIBOSE + METFORMIN carries an increased risk of lactic acidosis, a rare but severe metabolic complication related to metformin accumulation. This risk is higher in older individuals with kidney, liver, or heart conditions.
- Limit alcohol consumption, as excessive alcohol intake can exacerbate the risk of lactic acidosis.
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:
Alpha-Glucosidase Inhibitor, Biguanide, Therapy Class:
Antidiabetic Agent, Approved Countries
India, the United States, Canada, the United Kingdom, Japan, France and Australia.
Voglibose+ Metformin is an Anti-diabetic Agent belonging to the pharmacological class of Alpha-Glucosidase inhibitors and biguanides.
Voglibose+ Metformin has been approved to treat type 2 diabetes in adults when diet and exercise alone do not provide adequate glycemic control.
Voglibose is absorbed in the gastrointestinal system, primarily eliminated in the urine, and does not significantly undergo metabolism. In the small intestine, metformin is absorbed, undergoes little metabolic processing, and is eliminated unaltered in the urine. These two drugs increase glucose synthesis and use in the liver while blocking glucose absorption in the gastrointestinal tract.
The common side effects of Voglibose+ Metformin are taste changes, nausea, vomiting, diarrhoea, stomach pain and bloating.
Voglibose+ Metformin is available as a tablet for convenient administration.
Voglibose+ Metformin is available in India, the United States, Canada, the United Kingdom, Japan, France and Australia.
Voglibose+ Metformin is an Anti-diabetic Agent belonging to the pharmacological class of Alpha-Glucosidase inhibitors and biguanides.
Voglibose: A synthetic substance called Voglibose, an alpha-glucosidase inhibitor, has strong and long-lasting therapeutic effects against diseases of the sensory, motor, and autonomic nerve systems brought on by diabetes mellitus. Alpha-glucosidase inhibitors are oral anti-diabetic medications used to treat type 2 diabetes mellitus. They function by stopping the breakdown of complex carbohydrates, such as starch. Usually, simple sugars, or monosaccharides, are formed from complex carbohydrates and can be absorbed by the colon. As a result, alpha-glucosidase inhibitors lessen the effect that complex carbohydrates have on blood glucose.
Metformin: Metformin decreases hepatic glucose production, reduces glucose absorption in the intestine and improves insulin sensitivity (increases peripheral glucose uptake and utilization).
Synergistic Benefits: Metformin and Voglibose combination provide synergistic effects on type 2 diabetes management. Voglibose effectively decreases blood sugar spikes after meals by delaying the gut's processing and absorption of carbohydrates. Inversely, metformin mainly works by improving peripheral tissue insulin sensitivity and reducing the amount of glucose produced in the liver. Together, these medications offer an effective method of managing diabetes and also help with weight management (metformin may provide a little amount of weight loss) and blood sugar control and may even benefit the cardiovascular system by lowering the risk of heart-related problems. The combination also reduces the possibility of hypoglycemia, which can be harmful when using some other antidiabetic drugs.
Data Onset of action of Voglibose+ Metformin typically occurs within 1 to 2 hours after administration.
Data duration of action of Voglibose+ Metformin effects generally within 4 to 6 hours after administration.
The Data of Tmax (time to peak concentration) of Voglibose+ Metformin generally reached within 1-2 hours after oral administration.
The Data of Cmax of Voglibose+ Metformin is achieved within 1-2 hours following administration.
Voglibose+ Metformin is available in 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 before meals or generally with a meal.
To manage type 2 diabetes mellitus, voglibose + metformin should be used. Through improved insulin sensitivity and delayed carbohydrate absorption, it helps improve glycemic control in individuals with diabetes by controlling blood sugar levels.
Voglibose: Voglibose is an alpha-glucosidase inhibitor used for lowering postprandial blood glucose levels in people with diabetes mellitus.
Metformin: Metformin improves glucose tolerance by lowering basal and postprandial plasma glucose. It exerts its effect by decreasing hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis, delaying intestinal glucose absorption, and increasing insulin sensitivity by increasing peripheral glucose uptake and utilization.
Type 2 diabetes is treated with metformin + Voglibose. Voglibose and metformin are combined in it. Voglibose prevents intestinal enzymes from breaking down complex sugars into simple sugars like glucose. It postpones the absorption of glucose. The spike in blood glucose levels that occurs right after meals is stopped by this treatment.In contrast, metformin exhibits the non-pancreatic action to lower blood sugar levels without boosting insulin production. Its ability to enhance the effects of insulin has given it the name "insulin sensitizer." Because it doesn't lower blood sugar, it is regarded as a particular anti-diabetic medication. In most circumstances, metformin is not associated with weight gain.
Voglibose +Metformin is approved for use in the following clinical indications:
- For the management of type 2 diabetes mellitus.
- To control blood glucose levels.
- To improve glycemic control and manage diabetes in individuals with type 2 diabetes mellitus.
Orally: Voglibose+ Metformin is available as a tablet that can be taken orally.It is advised to progressively raise the metformin dose at the beginning of treatment to reduce gastrointestinal adverse effects. Take the drug along with food. Avoid breaking, crushing, dissolving, or chewing extended-release pills; instead, swallow them whole. When metformin extended-release pills are partially dissolved in the stool, as has happened with some of them, a healthcare professional should assess glycemic control. The tablet strength determines the precise dosage. Do not double the next dose if missed; instead, take it as soon as possible.
The dosage and duration of treatment should be as per the treating physician's clinical judgment.
Voglibose+ Metformin has various strengths, such as 0.3mg+500mg or 0.2mg+500mg.
Voglibose+ Metformin is available in the form of Oral tablets.
Dosage Adjustment for Adult Patients
Type 2 Diabetes Mellitus
A single tablet, given two or three times a day, during or after meals, is the typical starting dose for the fixed-dose combination of Voglibose 0.2/0.3 mg and metformin hydrochloride 500 mg. Blood glucose levels should be used to modify the dosage after ten to fifteen days. The gastrointestinal tolerance of a dosage increase could be improved gradually. Metformin's highest suggested dosage is 3 g daily, administered in three separate doses. Limit the daily dosage of metformin to 2500 mg and Voglibose to 0.9 mg.
If switching from another oral antidiabetic is the strategy, stop taking the other medication and start taking metformin at the previously mentioned dosage.
Voglibose+ Metformin should be used in treating type 2 diabetes mellitus, along with appropriate dietary restrictions.
Voglibose+ Metformin is usually taken with meals to reduce the risk of gastrointestinal side effects. Excessive alcohol consumption should be avoided as it can potentiate the risk of lactic acidosis, a rare but severe side effect associated with Metformin.
While taking this combination, it is advised to stay hydrated, consume a rich-balanced diet low in saturated fats and cholesterol—and drink plenty of vegetables, whole grains, fruits, and lean proteins in meals.
The dietary restriction should be individualized as per patient requirements.
Voglibose+ Metformin may be contraindicated in the following conditions:-
- Dialysis, end-stage renal disease, or moderate-to-severe renal disease (eGFR <45 mL/min/1.73 m2)
- Metabolic acidosis, either acute or chronic, including diabetic ketoacidosis (ketoacidosis is treated with insulin)
- History of severe hypersensitivity response to metformin or Voglibose.
- This medication must only be administered to patients undergoing lifestyle adjustments (diet and/or exercise) when the 2-hour postprandial blood glucose levels are equal to or more than 200 mg/dL.
- Patients with a history of ileus or laparotomies; those with chronic intestinal diseases associated with complications with digestion and absorption; those whose symptoms worsen as a result of increased intestinal gas production (such as those with severe hernias, stenosis and ulcers of the large intestine, and Roemheld syndrome); and those with severe hepatic or renal disorders should be cautious when using Voglibose tablets.
- Patients must adhere to their diet plan, consistently dividing their daily carbohydrate intake. Patients who are overweight should keep eating a low-energy diet.
- Regular execution of the standard laboratory tests is necessary for diabetes monitoring. Hypoglycemia is rarely brought on by metformin alone. However, using it with insulin and sulfonylureas should be done with caution. Patients should be trained to identify and comprehend hypoglycemia symptoms and how to treat them.
- A temporary loss of control of blood sugar may happen in diabetic individuals who experience unexpected stressors such as fever, trauma, illness, or surgery. Insulin therapy may be required during these periods for a while.
Alcohol Warning
It is unsafe to consume Voglibose+ Metformin with alcohol.
Breast Feeding Warning
There is insufficient scientific evidence regarding the use and safety of Voglibose+ Metformin in breastfeeding.
Pregnancy Warning
Safe to use during pregnancy only if the possible benefit outweighs the potential risk to the foetus.
Food Warning
Avoid excessive intake of high-sugar or high-fat foods.
The adverse reactions related to Voglibose+ Metformin can be categorized as:-
- Common Adverse Effects: Gastrointestinal disturbances, such as diarrhoea, flatulence, abdominal pain, nausea and loss of appetite.
- Less Common Adverse Effects: Hypoglycemia, increased liver enzyme levels, skin reactions such as rash or itching
- Rare Adverse Effects: Pneumatosis intestinalis (gas-filled cysts on the bowel wall), lactic acidosis
The clinically relevant drug interactions of Voglibose and metformin are briefly summarized here:
- Sulfonylureas: Co-administration with sulfonylureas (e.g., glimepiride) may increase the risk of hypoglycemia, so dose adjustments and close blood glucose monitoring are necessary.
- Diuretics: Concurrent use with diuretics, particularly thiazides, may potentiate the risk of dehydration and increase the likelihood of lactic acidosis, so caution is advised.
- Beta-2 agonists: Combining Voglibose+ Metformin with beta-2 agonists (e.g., albuterol) may increase the risk of hypoglycemia, requiring dose adjustments.
- Steroids: Using corticosteroids (e.g., prednisone) may reduce the blood glucose-lowering effects of Voglibose+ Metformin, necessitating careful monitoring and possible dose adjustments.
- ACE Inhibitors: ACE inhibitors (e.g., lisinopril) may increase the risk of hypoglycemia when used alongside Voglibose+ Metformin, so close monitoring of blood glucose levels is essential, and dosage adjustments may be needed.
The most common side effects of Voglibose+ Metformin include:
Abdomen ache
Breathing difficulties
Nausea
Vomiting
Stomach pain
Rash on the skin
Bloating
Changes in taste
Diarrhoea
Dizziness
Flatulence (intestinal wind/gas)
Voglibose+ Metformin should be prudent in the following group of special populations.
- Pregnancy
Pregnancy Category C: Use with caution if the benefits outweigh the risks.
There are currently no relevant epidemiological data available. Because there are no reported adverse effects of the medication on pregnancy, fetal or embryonic development, parturition, or postnatal development, it should only be administered to pregnant or potentially pregnant women when the potential benefits outweigh the risks. This is supported by research on animals. To reduce the risk of fetal abnormalities linked to abnormal blood glucose levels, insulin should be used to keep blood glucose levels as close to normal as possible when the patient wishes to get pregnant and throughout the pregnancy. Metformin should not be used to treat diabetes.
- Nursing Mothers
Lactating rats excrete metformin into their milk. Since there is a lack of comparable data for humans, the benefits of continuing the compound in the mother should be considered when deciding whether to stop nursing or stop taking metformin.
Research conducted on rats has indicated that Voglibose has a suppressive effect on the increase in body weight of newborns. This effect is likely attributed to the suppression of milk production in mother animals, which results from the suppression of carbohydrate absorption. As such, it is preferable to avoid giving women Voglibose when they are nursing. Nursing should be avoided when administration cannot be avoided.
- Pediatric Use
As per FDA, safety and effectiveness in the pediatric population have yet to be established.
- Geriatric Use
Given that older individuals typically exhibit a physiological hypofunction, it is preferable to proceed with caution and begin the administration of the medication at low doses (e.g., 0.1 mg at a time). In addition, for the disease, this medication should be closely monitored and carefully provided. The initial onset of gastrointestinal symptoms and blood sugar levels should also be closely monitored.
Dose Adjustment in Kidney Impairment Patients:
Kidney Impairment (Mild to Severe): Not recommended; Regular assessment of renal function is necessary.
Dose Adjustment in Hepatic Impairment Patients:
Mild-to-moderate: No dosage modification is required.
Severe: This has not been researched and is not advised.
Signs and Symptoms
The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Voglibose+ Metformin.
Overconsumption of Voglibose+ Metformin could lead to
severe hypoglycemia (very low blood sugar), gastrointestinal disturbances, and lactic acidosis, with manifestations like nausea, vomiting, and abdominal pain.
Management
There is no specific antidote for Voglibose+ Metformin overdose, emphasizing the need for immediate medical attention. Suspected overdose warrants discontinuation of the medications. In recent overdose cases, gastric lavage or activated charcoal can limit further absorption. Supportive care addresses symptoms through fluids, electrolyte correction, and antiemetics for nausea and vomiting. Severe hypoglycemia necessitates close monitoring until stabilization.
In cases of severe metformin-induced lactic acidosis, hemodialysis may be an option to remove excess metformin and correct acidosis. Timely intervention and medical supervision are imperative to manage Voglibose+ Metformin overdose effectively and mitigate potential complications.
Pharmacodynamics
Voglibose: Alpha-glucosidase inhibitors are saccharides that function as competitive inhibitors of the alpha-glucosidase enzymes in the small intestine's brush border, which are necessary for digesting carbohydrates. In the small intestine, oligosaccharides, trisaccharides, and disaccharides are hydrolyzed to glucose and other monosaccharides by the membrane-bound intestinal alpha-glucosidases. Acarbose inhibits membrane-bound alpha-glucosidases and also suppresses pancreatic alpha-amylase. In the small intestine lumen, complex starches are hydrolyzed to oligosaccharides by pancreatic alpha-amylase. Compromising these enzyme systems slows down the rate at which complex carbohydrates are metabolized. Because the carbs are not converted into glucose molecules, less glucose is absorbed. The short-term impact of these medication regimens on diabetes patients is a decline in blood glucose levels; the long-term effect is a slight decrease in haemoglobin A1c levels.
Metformin: Metformin is an antihyperglycemic medication that lowers basal and postprandial plasma glucose levels in people with type 2 diabetes, improving their glucose tolerance. Its pharmacologic modes of action are distinct from those of other oral antihyperglycemic medication groups. Metformin increases peripheral glucose uptake and utilization, which lowers intestinal glucose absorption, reduces hepatic glucose synthesis, and enhances insulin sensitivity. Metformin, unlike sulfonylureas, does not result in hyperinsulinemia or hypoglycemia in either type 2 diabetes patients or healthy persons. Metformin medication does not alter insulin secretion, although it may reduce the plasma insulin response throughout the day and insulin levels while fasting.
Pharmacokinetics
Absorption
Voglibose: <2% (as active drug) and approx 35% (as metabolites) are absorbed from the gastrointestinal tract.
Metformin: Slowly and incompletely absorbed from the gastrointestinal tract. Food slightly delays and decreases the extent of absorption. Absolute bioavailability: 50-60%. Time to peak plasma concentration: 2-3 hours (immediate-release); 7 hours, range: 4-8 hours (extended-release).
Bioavailability: 50-60% (Metformin [fasted])
Distribution
Voglibose: Time to peak plasma concentration: Approx 1 hour (active drug).
Metformin: Concentrates in the liver, kidney and gastrointestinal tract. It crosses the placenta and then enters breast milk (small amounts). Volume of distribution: 654 ± 358 L.
Protein-bound: Negligible (Metformin)
Metabolism
Voglibose: Exclusively metabolized in the gastrointestinal tract mainly by intestinal bacteria and digestive enzymes into at least 13 metabolites, including sulfate, methyl, and glucuronide conjugates as the primary metabolites.
Metformin: Excreted unchanged in the urine and did not undergo specific hepatic metabolism (no metabolites have been found in humans) or biliary excretion.
Elimination
Voglibose: Via urine (approx 34% as inactive metabolites; <2% as unchanged drug and active metabolites); faeces (approx 51% as unabsorbed drug). Elimination half-life: Approx 2 hours.
Metformin: With a plasma elimination half-life of roughly 6.2 hours, 90% of the absorbed medication is excreted via the renal pathway during the first 24 hours following oral administration. The elimination half-life of blood is roughly 17.6 hours, indicating that the erythrocyte bulk could constitute a distribution compartment.
Therapeutic benefits of a combination of Voglibose and metformin
Blood Sugar Control: Metformin and Voglibose are combined to control blood sugar levels effectively. Voglibose reduces post-meal glucose increases by inhibiting the digestion of complex carbohydrates in the intestines, which delays absorption. Metformin improves insulin sensitivity and reduces the synthesis of glucose in the liver, which enhances overall glycemic management.
Weight management: Patients with diabetes who may experience weight gain while taking other drugs will benefit most from this combination's neutral or even weight-reducing effects.
Decreased Hypoglycemia Risk: Compared to certain other diabetic drugs, Voglibose and metformin are less likely to induce hypoglycemia, thereby rendering them safer for a large number of people, especially those who are prone to hypoglycemia episodes.
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- Choi HK, Oh M, Kim EJ, Song GS, Ghim JL, Shon JH, Kim HS, Shin JG. Pharmacokinetic study of metformin to compare voglibose/metformin fixed-dose combination with coadministered Voglibose and metformin. Int J Clin Pharmacol Ther. 2015 Feb;53(2):147-53. doi: 10.5414/CP202197. PMID: 25546164; PMCID: PMC4558629.
- https://biocon.com/docs/prescribing_information/diabetology/metadozev_pi.pdf
- https://www.myupchar.com/en/medicine/metformin-voglibose-p37142624#contraindications
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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: 7 Nov 2023 6:51 AM GMT