Biphasic Insulin Aspart for Diabetes Mellitus: Dosage, Effectiveness, Considerations, and Side Effects

Overview:

For people with diabetes, Insulin is a useful medication for glucose control and averting complications. Newer Insulin formulations, such as Biphasic insulins, have been developed to increase patient acceptance of Insulin treatment. In a single injection, Biphasic insulins conveniently supply baseline and prandial insulin. Long-acting insulin and fast-acting insulin are the two forms of insulin that are combined to create it.

The FDA (Food and Drug Administration) authorized Insulin aspart on September 25, 2020, to treat type 1 and type 2 diabetes mellitus and enhance glycemic control in adults and children. Diabetic ketoacidosis (when the body creates excessive amounts of ketones) can also be treated with Insulin aspart, although this is not an FDA-approved use case.

Drug Group:

The drug group of biphasic insulin analogs includes Biphasic insulin aspart. This indicates that a single premixed injection contains two different kinds of Insulin:

• Rapid-acting Insulin aspart (70 percent or 50 percent).

• Long-acting Insulin aspart (30 percent or 50 percent).

Available Doses and Dosage Forms:

Prefilled cartridges and vials containing Biphasic insulin aspart are available for injection using an insulin pen or syringe. Depending on the particular brand and formulation, several rapid-acting to long-acting Insulin dosages and ratios are available:

• 70 by 30- Thirty percent of Insulin aspart is long-acting, while seventy percent is rapid-acting. Cartridges with dosages of three milliliters, nine milliliters, and ten milliliters are available.

• 50 by 50- Fifty percent long-acting Insulin aspart and fifty percent rapid-acting Insulin aspart. Cartridges with three-milliliter and ten-milliliter dosages are available.

For Patients:

What Is Diabetes Mellitus?

Diabetes mellitus, which is sometimes abbreviated as diabetes, is a long-term metabolic illness marked by hyperglycemia (increased blood sugar). This occurs when the body either produces insufficient insulin, a hormone that aids in the absorption of glucose by cells for energy, or the cells develop an immunity to its effects. Diabetes can take many different forms, the most prevalent of which are:

• Type 1 Diabetes: An insulin shortage that is caused by the immune system attacking and destroying insulin-producing cells in the pancreas.

• Type 2 Diabetes: To overcome insulin resistance, the body either stops producing enough insulin or becomes resistant to it. This is the most prevalent kind, frequently associated with lifestyle choices, including inactivity and obesity.

• Gestational Diabetes: Due to hormonal changes during pregnancy, gestational diabetes develops and affects the blood sugar levels of both the mother and the unborn child.

How Does Biphasic Insulin Aspart Work?

A premixed injection with two different forms of Insulin is called Biphasic insulin aspart.

• Rapid-Acting Insulin Aspart (70 Percent or 50 Percent): This kind of Insulin regulates blood sugar after meals by starting to operate within minutes after injection and peaking in one to four hours.

• Long-Acting Insulin Aspart (30 Percent or 50 Percent): This type of Insulin starts slowly and releases Insulin steadily for up to 24 hours, helping to control blood sugar levels both during and after meals.

This combination provides both rapid and long-term blood sugar management by imitating the body's normal rhythm of insulin release.

What Is the Dosage of Biphasic Insulin Aspart?

Determining the appropriate dosage of Biphasic insulin aspart requires careful consideration of several factors, including:

• Type and severity of diabetes.

• Individual blood sugar control goals.

• Weight and age.

• Diet and activity level.

• Other medications are being used.

Common dosages are:

• 70 by 30 Formulation: A biphasic insulin analog is usually given in two doses per day to cover meals and snacks. The patient's demands should determine the specific dosage, which should be applied subcutaneously in different areas.

• 50 by 50 Formulation: Up to three times a day, with dosage determined by glycemic management objectives and individual metabolic requirements. Changes in renal or hepatic function, physical activity, eating habits, or switching from one Insulin regimen to another may all require adjustments.

How Effective Is Biphasic Insulin Aspart?

Studies have shown it to be:

• More efficient than basal and other Biphasic insulins at preventing blood sugar elevations after meals.

• Comparable to basal Insulins and other Biphasic insulins in terms of reducing long-term blood sugar management.

• Generally well accepted, with a simple dosage regimen of once or twice daily.

Individual reactions to medicine might differ, though. One must speak with the physician to ascertain whether Biphasic insulin aspart is the best course of action and to track its efficacy in treating the particular illness.

What Are the Things to Inform the Doctor Before Taking the Drug?

Before beginning Biphasic insulin aspart, it is important to let the doctor know about medications that are being used.

• Every medical condition, such as liver or kidney issues, heart conditions, thyroid conditions, and allergies of any kind, particularly to insulin or its ingredients.

• All of the drugs and prescription medications used.

• Medications used without a prescription, like vitamins and herbal supplements.

• Unplanned or planned pregnancy, nursing.

• Drinking alcohol.

• Any recent dietary or weight changes.

The doctor uses this information to evaluate the risks, interactions, and acceptability of Biphasic insulin aspart for specific circumstances.

How Is Biphasic Insulin Aspart Administered?

Before administering Insulin, always read the label. Subcutaneous injections should be made in a variety of locations, such as the upper arm, buttocks, thigh, or abdomen, before or after meals. To avoid lipodystrophy (fat tissue changes at the injection site), injection sites should be rotated.

• Type 1 Diabetes: Take the medication 15 minutes before starting a meal.

• Type 2 Diabetes: Take the medication 15 minutes before or after starting a meal.

Avoid giving intravenously. Avoid using insulin delivery systems. Before usage, it needs to be promptly reconstituted.

What Are the Side Effects of Biphasic Insulin Aspart?

Biphasic insulin aspart can have adverse effects, just like any other medicine, although not everyone will experience them. Typical adverse effects include the following:

• Low Blood Sugar (Hypoglycemia): The most frequent adverse effect is low blood sugar, or hypoglycemia, which can happen if the dosage is too high, meals are missed or taken later than usual, or there is more physical activity. Sweating, lightheadedness, shakiness, and hunger are some of the symptoms.

• Reactions at the Injection Site: These may include discomfort, swelling, redness, or itching.

• Weight Increase: Insulin may encourage the accumulation of fat, which might result in weight gain.

• Lipodystrophy: This is an uncommon adverse effect that causes thickening or atrophy of the fat tissue where the injection was made.

• Rash and Pruritis: Rash and pruritis (itching) may be caused by some people.

Dietary Considerations:

Although Biphasic insulin aspart aids in blood sugar regulation, a balanced diet is still essential for the overall management of diabetes. These are important things to keep in mind:

• Consistent carbohydrate intake. To help in anticipating how the blood sugar will react to insulin, try to consume the same quantities of carbs every day.

• Emphasize whole, unprocessed foods. Pick lean protein sources, whole grains, fruits, and veggies.

• Refined carbs and sugary beverages should be avoided, as they can quickly raise blood sugar levels.

• Consult a licensed dietitian, as they can design a customized food plan that fits the tastes and objectives of managing diabetes.

• Remember that Biphasic insulin aspart does not replace the necessity of a balanced diet.

Missed Dose:

If a Biphasic insulin aspart dosage is missed:

• Never take two doses to make up for one that is missed.

• Verify the blood sugar concentration.

• Unless the doctor instructs otherwise, take the next dosage on time.

Overdose:

• Hypoglycemia and hypokalemia (low potassium) can result from administering too much Insulin. Oral glucose is often useful in treating mild hypoglycemia episodes. Changes may be required to the way medication is taken.

• For more severe episodes, including coma, seizures (aberrant electrical activities in the brain), or neurologic impairment, concentrated intravenous glucose or intramuscular or subcutaneous glucagon may be used as a treatment.

• Because hypoglycemia can reoccur even after a seemingly complete clinical recovery, continued carbohydrate ingestion and monitoring may be required.

• Corrective action must be taken for hypokalemia.

Storage:

Biphasic insulin aspart should be stored as directed by the manufacturer, usually:

• Refrigerate unopened at two to eight degrees Celsius (36 degrees Fahrenheit to 46 degrees Fahrenheit).

• Once opened, keep it at room temperature for up to 28 days (up to 25 degrees Celsius or 77 degrees Fahrenheit).

• Avoid freezing, being in direct sunlight, or excessive heat.

• Never use Insulin that has expired.

For Doctors:

Indication:

The prescription drug known as Biphasic insulin aspart is recommended for:

• Enhancing glycemic management in people with type 1 diabetes mellitus, both adults and children.

• Enhancing glycemic control in individuals with type 2 diabetes mellitus that is not well managed with food, exercise, or oral drugs.

Dose:

Among the variables affecting dose are:

• Diabetes type and severity.

• Personal blood sugar goals for management.

• Age and weight.

• Diet and degree of exercise.

• Utilizing other drugs.

Suspendable injectables are available in 100 units per milliliter (U-100) as:

• Three milliliter (ml) cartridges for a single patient.

• Vials containing 10 ml.

Dosing Considerations:

Factors influencing dosing include:

• Initial Dosage Determination: Individual circumstances guide the physician in setting the initial dosage.

• Dosage Adjustments: Based on blood sugar monitoring and the overall response to treatment, dosage changes may be necessary.

• Injection Technique: Proper injection technique, including site rotation, is vital for optimal drug absorption and minimizing adverse effects, with guidance provided by the healthcare provider.

• Monitoring: Regular blood sugar monitoring is necessary to assess drug effectiveness and detect hypoglycemia episodes.

• Dietary Management: A balanced diet is essential, along with Biphasic insulin aspart to support effective diabetes management.

What Are the Pharmacological Aspects of Biphasic Insulin Aspart?

• Pharmacodynamics

It encourages the absorption of glucose from the circulation into the cells of the liver, muscle, and fat, which lowers the concentration of blood sugar. It works to further regulate blood sugar by inhibiting the liver's capacity to generate glucose.

• Mechanism

Biphasic insulin aspart functions by imitating the actions of both of its constituent parts:

1. Rapid-Acting Insulin Aspart: Inhibits the hepatic synthesis of glucose while increasing absorption of glucose via binding to insulin receptors on muscle, fat, and liver cells. After eating, this causes the blood sugar levels to drop quickly.

2. Long-Acting Insulin Aspart: After injection, it crystallizes and releases Insulin gradually over a long time. This maintains blood sugar management throughout the night and in between meals.

Reduces Blood Sugar: Biphasic insulin aspart helps diabetics manage hyperglycemia, or high blood sugar, by encouraging glucose absorption and preventing synthesis.

• Pharmacokinetics

1. Absorption: Rapid-acting Insulin aspart is rapidly absorbed from the injection site and peaks in one to four hours. Long-acting Insulin aspart provides a continuous release for up to 24 hours; it is absorbed slowly because of crystal formation.

2. Distribution: Both substances circulate throughout the body, arriving at specific tissues such as the fat, muscle, and liver.

3. Metabolism: Enzymes in the body break down both components.

4. Excretion: Biphasic insulin aspart breakdown products are mostly eliminated via the kidneys and urine.

Toxicity:

• Like other drugs, Biphasic insulin aspart can have side effects, although severe toxicity is rare. Hypoglycemia, or low blood sugar, is the most frequent adverse effect that might happen with an excessively high dosage, missing or skipping meals, or engaging in greater physical activity. Hypoglycemia manifests as hunger, shakiness, sweating, and dizziness.

• Additional possible adverse outcomes include reactions at the injection site (pain, redness, swelling, and itching), gaining weight, and lipodystrophy. See a doctor if having any unsettling side effects after taking Biphasic insulin aspart.

Clinical Studies:

Biphasic insulin aspart 70/30 (70 by 30) or Biphasic insulin aspart 50/50 were administered to individuals with type 1 or type 2 diabetes and a BMI (body mass index) of more than 30 kg/m2 (kilogram per square meter) during a 16-week experiment. The suppertime dose of Biphasic insulin aspart 50/50 was changed to Biphasic insulin aspart 70/30 for those whose prebreakfast blood glucose level was greater than 144 mg/dL (milligrams per deciliter). In comparison to Biphasic insulin aspart 70/30, the results demonstrated considerably reduced HbA1c levels in type 2 diabetic patients on three daily Biphasic insulin aspart 50/50. In a different trial, individuals with type 2 diabetes who received three daily injections of Biphasic insulin aspart formulations showed non-inferior glycemic control compared to those who received a basal-bolus therapy with Insulin aspart plus NPH.

These investigations have shown:

• Efficacy in reducing blood sugar levels, especially surges that occur after meals.

• Research has demonstrated that in terms of long-term blood sugar management (HbA1c), Basal insulins and other Biphasic insulins are not more efficient than Biphasic insulin aspart.

• The most prevalent adverse effect of Biphasic insulin aspart is hypoglycemia; however, the overall side effect profile is seen to be good.

What Are the Contraindications of Biphasic Insulin Aspart?

• Do not use in individuals who are allergic to Biphasic insulin aspart or any of its excipients.

• Do not use in hypoglycemic episodes.

Warnings and Precautions:

• Hypoglycemia: Sweating, lightheadedness, shakiness, and hunger are some of the symptoms. Know the warning signs and symptoms and have a strategy in place for dealing with hypoglycemia, which should include easy access to glucose supplies.

• Dosage Modifications: Blood sugar levels can be impacted by dietary, activity, and medication changes, which may require modifying the amount of Biphasic insulin aspart. Do not change the dosage without first talking to the physician.

• Problems With the Kidneys and Liver: These illnesses can alter how insulin is metabolized, so close observation and possible dose modifications may be required.

• Allergies: Although they are uncommon, Biphasic insulin aspart might cause allergic responses. If one gets symptoms like intense itching, rash, wheezing, or trouble breathing, get medical help right away.

• Operating and Directing Machinery: Hypoglycemia can cause problems with judgment and coordination, making it dangerous to drive or operate machinery. Exercise caution and keep an eye on the blood sugar levels before doing such things.

What Are the Drug Interactions of Biphasic Insulin Aspart?

• The blood glucose-lowering effect and susceptibility to hypoglycemia may be increased by several factors, including oral antidiabetic medications, Pramlintide, ACE inhibitors (Angiotensin-converting enzyme), Disopyramide, Fibrates, Fluoxetine, monoamine oxidase (MAO) inhibitors, Propoxyphene, salicylates, somatostatin analogs (for example., Octreotide), and sulfonamide antibiotics.

• Conversely, corticosteroids, Niacin, Danazol, diuretics, sympathomimetic agents (for example., Spinephrine, Salbutamol, Terbutaline), Isoniazid, phenothiazine derivatives, Somatropin, thyroid hormones, estrogens, progestogens (for example., in oral contraceptives), and atypical antipsychotics may diminish the blood-glucose-lowering effect.

• Beta-blockers, Clonidine, Lithium salts, and alcohol may either enhance or weaken insulin's blood-glucose-lowering effect.

• Pentamidine can induce hypoglycemia, followed by hyperglycemia. Patients taking sympatholytic medications such as beta-blockers, Clonidine, Guanethidine, and Reserpine may experience reduced or absent signs of hypoglycemia.

Specific Considerations:

• Pregnancy and Nursing: One can take Biphasic insulin aspart during pregnancy and nursing, but the doctor must closely monitor.

• Drinking Alcohol: Drinking alcohol increases the risk of hypoglycemia and can interact with Biphasic insulin aspart. Use caution and talk to the doctor about alcohol use.

• Sick Days: The body's reaction to Insulin may alter while one is sick. For advice on how to manage diabetes when unwell, speak with the doctor and keep a closer eye on the blood sugar levels.