Type 1 Diabetes Mellitus Medication

Updated: Dec 13, 2023
  • Author: Romesh Khardori, MD, PhD, FACP; Chief Editor: George T Griffing, MD  more...
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Medication

Medication Summary

Insulin injected subcutaneously is the first-line treatment of type 1 diabetes mellitus (DM). The different types of insulin vary with respect to onset and duration of action. Short-, intermediate-, and long-acting insulins are available. Short-acting and rapid-acting insulins are the only types that can be administered intravenously (IV). Human insulin currently is the only species of insulin available in the United States; it is less antigenic than the previously used animal-derived varieties. 

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Antidiabetics, Insulins

Class Summary

Rapid-acting insulins are used whenever a rapid onset and short duration are appropriate (eg, before meals or when the blood glucose level exceeds target and a correction dose is needed). Rapid-acting insulins are associated with less hypoglycemia than regular insulin.

Currently, short-acting insulins are less commonly used than the rapid-acting insulins in patients with type 1 DM. They are used when a slightly slower onset of action or a greater duration of action is desired.

Intermediate-acting insulins have a relatively slow onset of action and a relatively long duration of action. They are usually combined with faster-acting insulins to maximize the benefits of a single injection.

Long-acting and ultralong-acting insulins have a very long duration of action and, when combined with faster-acting insulins, provide better glucose control for some patients. In patients with type 1 DM, they must be used in conjunction with a rapid-acting or short-acting insulin given before meals.

Premixed insulins contain a fixed ratio of rapid-acting insulins with longer-acting insulin, which can restrict their use. Premixed insulin is usually not recommended in type 1 DM patients, because of their need for frequent adjustments of premeal insulin doses.

Insulin aspart (NovoLog, Fiasp)

Insulin aspart has a rapid onset of action, 5-15 minutes. The peak effect occurs within 30-90 minutes, and the usual duration of action is 2-4 hours. Insulin aspart is approved by the US Food and Drug Administration (FDA) for use in insulin pumps.

Fiasp also has a rapid onset of action, with its first measurable effect occurring within 16-20 minutes. The peak effect occurs within 91-133 minutes, and the usual duration of action is 5-7 hours.

Insulin glulisine (Apidra)

Insulin glulisine has a rapid onset of action, 5-15 minutes. The peak effect occurs within 30-90 minutes, and the usual duration of action is 2-4 hours. Insulin glulisine is FDA-approved for use in insulin pumps.

Insulin lispro (Humalog, Admelog, insulin lispro-aabc, Lyumjev)

Insulin lispro has a rapid onset of action, 5-15 minutes. The peak effect occurs within 30-90 minutes, and the usual duration of action is 2-4 hours.

Insulin inhaled (Afrezza)

Orally inhaled rapid-acting insulin in powder form. When 8 units were administered, maximum serum insulin concentration was reached by 12-15 minutes and declined to baseline by about 180 minutes.

Regular insulin (Humulin R, Novolin R, Myxredlin)

Regular insulin has a short onset of action, 0.5 hour. Its peak effect occurs within 2-4 hours, and its usual duration of action is 5-8 hours. Preparations that contain a mixture of 70% neutral protamine Hagedorn (NPH) insulin and 30% regular human insulin (eg, Novolin 70/30 and Humulin 70/30) are available, but the fixed ratios of intermediate-acting to rapid-acting insulin may restrict their use.

Insulin detemir (Levemir)

Insulin detemir is indicated for once-daily or twice-daily subcutaneous administration in individuals with type 1 DM who require long-acting basal insulin for hyperglycemia control. Its duration of action ranges from 5.7 hours (low dose) to 23.2 hours (high dose). The prolonged action results from slow systemic absorption of detemir molecules from the injection site. Its primary activity is regulation of glucose metabolism.

Insulin detemir binds to insulin receptors and lowers blood glucose levels by facilitating cellular uptake of glucose into skeletal muscle and fat; it also inhibits glucose output from the liver. The drug inhibits lipolysis in adipocytes, inhibits proteolysis, and enhances protein synthesis.

Insulin degludec (Tresiba)

Ultralong-acting basal insulin indicated to improve glycemic control in adults with diabetes mellitus who require basal insulin. It is highly protein bound, and following SC, the protein-binding provides a depot effect. The elimination half-life is 25 h and its duration of action is beyond 42 h.

Insulin aspart protamine/insulin aspart (NovoLog 70/30)

The combination of insulin aspart protamine with insulin aspart includes 30% rapid-onset insulin (ie, insulin aspart) and 70% intermediate-acting insulin (ie, insulin aspart protamine). Insulin aspart is absorbed more rapidly than regular human insulin, and insulin aspart protamine has a prolonged absorption profile after injection.

Insulin lispro protamine/insulin lispro (Humalog 75/25)

The combination of insulin lispro protamine with insulin lispro includes 75% insulin lispro protamine, which has a prolonged duration of action, and 25% insulin lispro, which is a rapid-onset insulin.

Insulin degludec/insulin aspart (Ryzodeg)

Combines the ultralong-acting basal insulin (degludec 70 units) and a rapid-acting insulin (aspart 30 units). It is indicated to improve glycemic control in adults with diabetes mellitus.

Insulin glargine (Lantus, Lantus SoloStar, Toujeo, Toujeo Max, Basaglar)

Insulin glargine stimulates proper utilization of glucose by the cells and reduces blood sugar levels. It has no pronounced peaks of action, because a small amount of insulin is gradually released at a constant rate over 24 hours. The amount of insulin in Toujeo and Toujeo Max SoloStar is three times greater (300 Units/mL) than in Lantus or Basaglar (100 Units/mL).

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Antidiabetics, Amylinomimetics

Class Summary

These amylinomimetic agents elicit endogenous amylin effects by delaying gastric emptying, decreasing postprandial glucagon release, and modulating appetite.

Pramlintide acetate (Symlin)

Pramlintide acetate is a synthetic analogue of human amylin, a naturally occurring hormone made in pancreatic beta cells that is deficient in people with type 1 DM. It slows gastric emptying, suppresses postprandial glucagon secretion, and regulates food intake through centrally mediated appetite modulation.

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Hypoglycemia Antidotes

Class Summary

Pancreatic alpha cells of the islets of Langerhans produce glucagon, a polypeptide hormone. Glucagon increases blood glucose levels by promoting hepatic glycogenolysis and gluconeogenesis.

Glucagon (GlucaGen, Gvoke)

Glucagon elevates blood glucose levels by inhibiting glycogen synthesis and enhancing the formation of glucose from noncarbohydrate sources such as proteins and fats (gluconeogenesis). It increases hydrolysis of glycogen to glucose in the liver and accelerates hepatic glycogenolysis and lipolysis in adipose tissue. Glucagon also increases the force of contraction in the heart and has a relaxant effect on the gastrointestinal tract. It is available in a reconstitutable powder form. Glucagon is also available as a ready-to-use subcutaneous (SC) solution in prefilled syringes or an autoinjector.

Glucagon intranasal (Baqsimi)

This agent activates hepatic glucagon receptors, which stimulate cyclic adenosine monophosphate (cAMP) synthesis. Hepatic glycogenolysis and gluconeogenesis are thus accelerated, with blood glucose levels consequently increasing. Glucagon requires preexisting hepatic glycogen stores to effectively treat hypoglycemia. Glucagon intranasal is indicated for severe hypoglycemic reactions in adults and children (aged 4 years or older) with diabetes.

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Monoclonal Antibodies

Class Summary

Teplizumab is a humanized monoclonal antibody (mAb) that targets the CD3 antigen, which is coexpressed with the T-cell receptor on the surface of T lymphocytes.

Teplizumab (Tzield)

Indicated to delay onset of stage 3 type 1 DM in adults and in children aged 8 years or older.

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Allogeneic Islet Cells

Class Summary

Pancreatic islets regulate blood glucose levels through highly regulated, pulsatile secretion of multiple hormones in response to fluctuations in blood glucose. Insulin, glucagon, somatostatin, pancreatic peptide, and ghrelin are released by endocrine cells within pancreatic islets. It is believed that insulin secretion by infused (transplanted) beta cells is donislecel’s primary mechanism of action.

Donislecel (Lantidra)

Indicated for adults with type 1 diabetes who, owing to current, repeated episodes of severe hypoglycemia, have been unable to approach target HbA1c, even with intensive diabetes management and education. It is meant for concomitant use with immunosuppression.

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