Acarbose + Metformin

Acarbose+ Metformin is an Anti-diabetic Agent belonging to the pharmacological class of alpha-glucosidase inhibitors and biguanides.

Acarbose+ Metformin has been approved as a treatment for type 2 diabetes mellitus, helping to control blood sugar levels in those individuals with diabetes by improving insulin sensitivity and delaying carbohydrate absorption, ultimately managing high blood sugar.

Acarbose is minimally distributed throughout the body, slowly absorbed from the digestive tract, and primarily metabolized in the intestines. The kidneys eliminate Metformin after being immersed in the intestines without being metabolized.

The common side effects of Acarbose+ Metformin are flatulence, diarrhoea, abdominal pain, fluid retention (oedema), and increased liver enzymes.

Acarbose+ Metformin is available as a tablet for convenient administration.

Acarbose+ Metformin is available in India, the United States, Canada, the United Kingdom, Germany, France and Australia.

Acarbose+ Metformin is an Anti-diabetic Agent belonging to the pharmacological class of alpha-glucosidase inhibitors and biguanides.

Acarbose: Competitive inhibitor of intestinal brush border α-glucosidases and pancreatic α-amylase, which causes a dose-dependent decrease in postprandial serum insulin and glucose peaks; delays the hydrolysis of ingested complex carbohydrates and disaccharides and glucose absorption and prevents sucrose from being metabolized into glucose and fructose.

Metformin: Metformin decreases hepatic glucose production, reduces glucose absorption in the intestine and improves insulin sensitivity (increases peripheral glucose uptake and utilization).

Synergistic Benefits: A combination medication of metformin + Acarbose has synergistic effects on type 2 diabetes management. Metformin enhances insulin sensitivity and lowers the liver's synthesis of glucose; Acarbose slows down the digestion and absorption of carbohydrates. When combined, they efficiently assist in the control of blood sugar levels. This combination may result in a lower risk of hypoglycemia, decreased post-meal spikes in glucose, and improved glycemic control. Regardless of the reduced calorie absorption, it could also promote weight loss.

Data Onset of action of Acarbose+ Metformin typically occurs within 1 to 2 hours after administration.

Data duration of action of Acarbose+ Metformin effects generally up to several hours after administration.

The Data of Tmax (time to peak concentration) of Acarbose+ Metformin generally reached within 1-3 hours after oral administration.

The Data of Cmax of Acarbose+ Metformin is achieved within 1-3 hours following administration.

Acarbose+ 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.

Acarbose+ Metformin can be used in the following health conditions:

Acarbose: In the small intestine, ingested complex carbohydrates and disaccharides are broken down, and glucose absorption is delayed as a result of the competitive and reversible inhibition of pancreatic α-amylase and membrane-bound intestinal α-glucosidases by Acarbose. Because of this action, blood glucose fluctuations are decreased due to a decreased postprandial spike in blood glucose.

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.

Acarbose+ Metformin is used to treat type 2 diabetes, or non-insulin-dependent diabetes (NIDDM). Usually, doctors recommend it when diet and exercise alone are insufficient to control increased blood sugar levels properly. This combination of medication includes an "alpha-glucosidase inhibitor," aspartame inhibits the action of intestinal enzymes that slow down the breakdown of carbohydrates after meals. Whereas the "biguanide" increases intestinal glucose absorption while decreasing glucose tolerance. Collectively, they help in reducing the hazards associated with diabetes, including nephropathy, diabetic retinopathy, neuropathy, foot ulcers, delayed wound healing, and other problems.

Acarbose+ Metformin is approved for use in the following clinical indications:

Orally: Acarbose+ 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; swallow them whole. A healthcare professional should assess glycemic control when metformin extended-release pills are partially dissolved in the stool, as has happened with some of them. The tablet strength determines the precise dosage. Do not double the next dose if missed; take it as soon as possible.

The dosage and duration of treatment should be as per the treating physician's clinical judgment.

Acarbose+ Metformin has various strengths, such as 25mg+500mg, 50mg+500mg

Acarbose+ Metformin is available in the form of Oral tablets.

Initial dose: Start with 500 mg of metformin and 25 mg of acarbose PO TDS.

Dosage adjustments: Oral: The dose should be increased gradually to minimize GI adverse effects.

Acarbose+ Metformin should be used in treating type 2 diabetes mellitus, along with appropriate dietary restrictions.

Acarbose+ Metformin is usually taken with meals to reduce the risk of gastrointestinal side effects and to ensure proper absorption.

Limit alcohol intake as it can potentiate the risk of lactic acidosis associated with Metformin.

Individuals should follow a diet that is low in fat and sugar. This involves substituting carbohydrates with whole grains, fruits, and vegetables, as carbohydrates can be converted into sugars, resulting in elevated blood sugar levels. High glycemic foods like potatoes should be avoided due to their potential to raise blood sugar.

The dietary restriction should be individualized as per patient requirements.

Acarbose+ Metformin may be contraindicated under the following conditions:-

Avoid excessive intake of high-sugar or high-fat foods. Take low fat and a low sugar diet.

The adverse reactions related to Acarbose+ Metformin can be categorized as:-

The clinically relevant drug interactions of Acarbose + metformin are briefly summarized here:

Drug Interactions: Metformin and Acarbose + Metformin shouldn't be taken with other medications for heart problems (digoxin), medicines for lowering cholesterol (cholestyramine), supplements containing digestive enzymes (lipase, pancreatin, amylase), or intestinal absorbents (charcoal).

Drug-Food Interaction: When taken with home sugar, Acarbose + metformin may upset the stomach and produce discomfort in the abdomen. Consequently, it is not advised to have a diet heavy on sugar. When using Acarbose plus metformin, alcohol should also be avoided as it may cause blood sugar levels to drop or rise.

Drug-Disease Interaction: Before using Acarbose + Metformin, people with ulcerative colitis or Crohn's disease (diseases that cause bowel swelling, severe kidney or liver disorders, diarrhoea, bowel pain, vomiting, and weight loss) and large hernias (bulging of a tissue or organ through an unusual opening) in the intestine should consult with a physician.

The most common side effects of Acarbose+ Metformin include:

Flatulence

Edema (swelling)

Increased liver enzymes

Diarrhea

Abdominal pain

Acarbose+ Metformin should be prudent in the following group of special populations.

Acarbose: Pregnancy Category B; Could be acceptable. Either no danger has been shown by animal research, but human studies have not been conducted, or some risk has been shown by animal studies but not by human studies.

It has not been determined whether Acarbose is safe for pregnant women. There is no proof that Acarbose impairs fertility or harms the fetus, according to studies on reproduction conducted in rats at dosages up to 480 mg/kg (nine times the exposure in people, based on drug blood levels). A modest rise in the frequency of embryonic losses in rabbits may have been caused by lower maternal body weight growth, likely caused by the pharmacologic activity of high doses of Acarbose in the intestines. Nevertheless, rabbits administered Acarbose at 32 times the human dose (based on body surface area), or 160 mg/kg, did not exhibit teratogenicity or embryotoxicity. This is equivalent to 10 times the human dose. Acarbose in pregnant women has not, however, been the subject of sufficient or carefully monitored research. Pregnancy should not be treated with this medication unless necessary, as research on animal reproduction is not necessarily indicative of human response. For this reason, most experts advise using insulin to keep the blood glucose levels as close to normal as possible during pregnancy. Available data strongly suggests that abnormal blood glucose levels during pregnancy are linked to an increased incidence of congenital anomalies as well as increased neonatal morbidity and mortality.

Metformin: Pregnancy Category B; Could be acceptable. Either no danger has been shown by animal research, but human studies have not been conducted, or some risk has been shown by animal studies but not by human studies.

According to recent data, there may be a link between elevated blood glucose levels during pregnancy and a higher risk of congenital disabilities. Most medical professionals advise using insulin to keep blood glucose levels as near to normal as feasible when pregnant. If metformin HCl is unnecessary, it is not advisable to use it during pregnancy because research on animal reproduction does not necessarily indicate human response.

Acarbose: When radiolabeled Acarbose is administered to nursing rats, a small amount of radioactivity has been detected in their milk. The medication's ability to be eliminated in human milk is unknown. A nursing woman should not be given Acarbose because it is excreted in human milk and many other medicines.

Metformin: Metformin is excreted into milk and reaches levels similar to those in plasma, according to studies done on nursing rats. No research akin to this has been done on breastfeeding mothers. Given the possibility of hypoglycemia in nursing infants, the mother's importance for the medication should be considered while deciding whether to stop breastfeeding or to stop the medication altogether. Insulin therapy should be regarded as if Metformin HCl is discontinued and diet alone is insufficient to control blood glucose.

As per FDA, safety and effectiveness in the pediatric population have yet to be established.

Acarbose: Acarbose clinical trials in the US involved 65 years of age or older (27%), and 4% were 75 or older. These individuals and younger subjects did not vary regarding overall safety or efficacy. Nevertheless, these differences were not statistically significant. In senior individuals, the maximal concentrations of Acarbose and the mean steady-state area under the curve (AUC) were approximately 1.5 times larger than in young participants.

Metformin: There were not enough elderly volunteers in clinical trials utilizing Metformin HCl to determine whether their reactions differed from those of younger patients. Age-related differences in responsiveness have not been demonstrated, but aging-related reductions in renal function may occur in the elderly. Metformin should be administered carefully in elderly persons since the kidneys are the organs that essentially eliminate it. Elderly patients shouldn't typically be raised to the maximum Metformin HCl dose; dosage decisions should be made carefully while monitoring renal function.

There is no FDA guidance on using Acarbose+ Metformin in patients with renal impairment.

There is no FDA guidance on the use of Acarbose+ Metformin in patients with hepatic impairment.

The physician should be vigilant about the knowledge pertaining to the identification and treatment of overdosage of Acarbose+ Metformin.

Overconsumption of Acarbose+ Metformin could lead to

severe hypoglycemia (very low blood sugar), gastrointestinal disturbances, such as nausea, vomiting, and diarrhoea, and a risk of lactic acidosis.

There is no specific antidote or treatment for excessive intake of Acarbose + Metformin. However, immediate medical attention is essential. Acarbose + Metformin should be terminated immediately when an overdose is suspected or if any unusual symptoms occur after intake.

For hypoglycemia (low blood sugar), consume a source of rapidly absorbed carbohydrates such as glucose tablets, sugar, or honey. Monitor blood glucose levels and repeat treatment if necessary. Intravenous glucose administration may be required to correct the low blood sugar levels rapidly.

Activated charcoal may help absorb any remaining medication in the stomach and reduce further absorption.

Hemodialysis may be considered in severe cases to remove the drugs from the bloodstream. Patients should be closely observed for any signs of lactic acidosis, a rare but potentially life-threatening complication, and treated accordingly.

Acarbose: Acarbose is an agonist for PPARγ, the peroxisome proliferator-activated receptor. Tissues crucial for insulin action, including skeletal muscle, the liver, and adipose tissue, contain PPAR receptors. The transcription of several insulin-responsive genes involved in the glucose regulation and lipid metabolism is modulated by the activation of PPARγ nuclear receptors.

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.

Acarbose: <2% (as active drug) and approx 35% (as metabolites) are absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 1 hour (active drug).

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])

Acarbose: Minimal distribution

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)

Acarbose: 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.

Acarbose: 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.