Antidiabetes Drugs; Indications, Side Effects, Drug Interactions

Antidiabetes Drugs; Indications, Side Effects, Drug Interactions

Antidiabetes drugs is used in diabetes treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions of insulin, exenatide, liraglutide and pramlintide, all are administered orally and are thus also called oral hypoglycemic agentsor oral antihyperglycemic agents. There are different classes of anti-diabetic drugs, and their selection depends on the nature of the diabetes, age and situation of the person, as well as other factors.

Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in Type I, which must be injected.

Diabetes mellitus type 2 is a disease of insulin resistance by cells. Type 2 diabetes mellitus is the most common type of diabetes. Treatments include (1) agents that increase the amount of insulin secreted by the pancreas, (2) agents that increase the sensitivity of target organs to insulin, and (3) agents that decrease the rate at which glucose is absorbed from the gastrointestinal tract.

List of Medications for Diabetes

  • Insulins
  • Insulin sensitizers (reduce insulin resistance)
    • Biguanides
    • Thiazolidinediones
  • Secretagogues (stimulate insulin release)
    • Sulfonylureas
    • Meglitinides
  • Agents that slow the digestive/absorptive process:
    • Alpha-Glucosidase Inhibitors
  • Glucagon-Like Peptide-1 (GLP-1) Agonists
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
  • Amylin Analogues
  • Sodium-Glucose Transporter-2 (SGLT-2) Inhibitors
  • Combination Products

This comprehensive listing includes antihyperglycemic agents that can be used for glycemic control in diabetes.

New Antihyperglycemics

Class Generic/Brand/Approval year
SGLT-2 inhibitor Canagliflozin (Invokana), 2013
DPP-4 inhibitor Alogliptin (Nesina, Vipidia), 2013
SGLT-2 inhibitor Dapagliflozin (Farxiga), 2014
SGLT-2 inhibitor Empagliflozin (Jardiance), 2014
GLP-1 receptor agonist Albiglutide (Tanzeum), 2014
GLP-1 receptor agonist Dulaglutide (Trulicity), 2014
Inhaled insulin powder Afrezza, 2014

Insulin preparations differ in how quickly they work, when they peak maximal activity, and how long they work. Insulins are available for intravenous, intramuscular, and subcutaneous administration.

Generic Brand Name
Rapid Acting Insulins
Insulin aspart Novolog
Insulin glulisine Apidra
Insulin lispro Humalog
Insulin human Afrezza Inhalation Powder
Short Acting Insulins
Regular insulin Humulin R, Novolin R
Intermediate Acting Insulins
Insulin NPH Hagedorn NPH , Humulin N, Novolin N
Long Acting Insulins
Insulin detemir Levemir
Insulin glargine Lantus
Premixed Insulins
Insulin aspart protamine/
insulin aspart
NovoLog 50/50, NovoLog 70/30
Insulin lispro protamine/
insulin lispro
Humalog 50/50, Humalog 75/25
Combination with Insulins
Insulin glargine /Lixisenatide Soliqua 100/33
Insulin degludec/Liraglutide Xultophy 100/3.6


Sensitizers increase the sensitivity of target organs to insulin.

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Biguanides improve peripheral glucose uptake and utilization.

Generic Brand Name
Metformin Glucophage, Glucophage XR, Glumetza, Riomet, Fortamet

Phenformin and Buformin were withdrawn due to lactic acidosis risk.

Thiazolidinediones (Glitazones)

Thiazolidinediones work through the improvement of insulin sensitivity by acting on adipose, muscle, and liver to increase glucose utilization and decrease glucose production.

Generic Brand Name
Rosiglitazone Avandia
Pioglitazone Actos


Secretagogues increase insulin secretion by the pancreas.


Sulfonylureas stimulate insulin secretion by inhibiting the K(ATP) channel complex of the pancreatic beta cells. Sulfonylureas are used to treat type II diabetes. These agents are not indicated for type I diabetes.

Generic Brand Name
Acetohexamide Dymelor
Chlorpropamide Diabinese
Tolazamide Tolinase
Tolbutamide Orinase
Glipizide Glucotrol, Minidiab, Glibenese
Glyburide (glibenclamide) Diabeta, Micronase, Glynase, Daonil, Euglycon
Glimepiride Amaryl
Gliclazide Uni Diamicron
Glyclopyramide Deamelin-S
Gliquidone Glurenorm


Meglitinide derivatives stimulate insulin secretion from pancreatic cells, lowering blood glucose levels.

Generic Brand Name
Nateglinide Starlix
Repaglinide Prandin, NovoNorm

Alpha-Glucosidase Inhibitors

Alpha-glucosidase inhibitors are not technically glucose lowering agents because they do not have a direct effect on insulin secretion or sensitivity. These medications slow the digestive and absorptive process, preventing postprandial glucose raise.

Generic Brand Name
Acarbose Precose, Glucobay
Miglitol Glyset
Voglibose Basen

Glucagon-Like Peptide 1 (GLP-1) Agonists

GLP-1 analogs normalize fasting and postprandial blood glucose levels without causing hypoglycemia . Also, GLP-1 analogs reduce food intake and promote modest weight loss.

Generic Brand Name
Short-acting GLP-1 analogs
Exenatide Byetta
Lixisenatide Lyxumia, Adlyxin
Long-acting GLP-1 analogs
Liraglutide Victoza
Prolonged-acting GLP-1 analogs
Albiglutide Tanzeum
Dulaglutide Trulicity
Exenatide once weekly Bydureon
Under development
Taspoglutide Phase III clinical trials

Dipeptidyl Peptidase-4 Inhibitors (Gliptins)

Dipeptidyl peptidase-4 (DPP-4) inhibitors inhibit DPP-4, the enzyme that inactivates incretin hormones GLP-1 and GIP.

Generic Brand Name
Alogliptin Nesina, Vipidia
Anagliptin Suiny
Linagliptin Trajenta
Saxagliptin Onglyza
Sitagliptin Januvia
Teneligliptin Tenelia
DPP-4 inhibitors under development

Amylin Analogues

Pramlintide is a synthetic form of amylin, a pancreatic peptide produced by β-cells. Amylin and pramlintide lower postprandial glucose by lowering postprandial glucagon and delaying gastric emptying. Pramlintide is indicated for Type 1 and Type 2 diabetics who use insulin.

Generic Brand Name
Pramlintide Symlin

Sodium-Glucose Cotransporter 2 (SGLT-2) inhibitors

SGLT-2 inhibitors are a new class of drugs for Type 2 diabetes with novel mechanism of action. SGLT-2 inhibitors block reabsorption of glucose in the kidneys, leading to excretion of glucose in urine. These glucose lowering medications work independently of insulin.

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Generic Brand Name
Canagliflozin Invokana
Dapagliflozin Forxiga, Farxiga
Empagliflozin Jardiance
SGLT-2 inhibitors under development
Remogliflozin etabonate

Other Anti-diabetic Drugs

Generic Brand Name
Dopamine agonist
Bromocriptine Parlodel, Cycloset
Bile acid sequestrant
Colesevelam Welchol, Cholestagel, Lodalis


Generic Brand Name
Alogliptin + Metformin Kazano
Dapagliflozin + Metformin Xigduo XR
Glipizide + Metformin Metaglip
Glyburide + Metformin Glucovance
Linagliptin + Metformin Jentadueto
Pioglitazone + Metformin Actoplus Met, Actoplus Met XR
Repaglinide + Metformin Prandimet
Rosiglitazone + Metformin Avandamet
Saxagliptin + Metformin Kombiglyze XR
Sitagliptin + Metformin Janumet
Rosiglitazone + Glimepiride Avandaryl
Pioglitazone + Glimepiride Duetact
Alogliptin + Pioglitazone Oseni
Simvastatin + Sitagliptin Juvisync
Empagliflozin + Metformin Synjardy

Mechanism of Action of antidiabetes drugs

Antidiabetes drugs mechanisms of action differ from other classes of oral antihyperglycemic agents. Antidiabetes drugs decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by  antidiabetes drugs of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats. Activation of AMPK is required for antidiabetes drugs inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. Antidiabetes drugs administration also increases AMPK activity in skeletal muscle. AMPK is known to cause GLUT4 deployment to the plasma membrane, resulting in insulin-independent glucose uptake. The rare side effect, lactic acidosis, is thought to be caused by decreased liver uptake of serum lactate, one of the substrates of gluconeogenesis. In those with healthy renal function, the slight excess is simply cleared. However, those with severe renal impairment may accumulate clinically significant serum lactic acid levels. Other conditions that may precipitate lactic acidosis include severe hepatic disease and acute/decompensated heart failure.

Indications antidiabetes drugs

  • Diabetes, Type 2
  • Polycystic Ovary Syndrome
  • Diabetes, Type 3c
  • Insulin Resistance Syndrome
  • Female Infertility
  • For use as an adjunct to diet and exercise in adult patients (18 years and older) with NIDDM. May also be used for the management of metabolic and reproductive abnormalities associated with polycystic ovary syndrome (PCOS). Jentadueto is for the treatment of patients when both linagliptin and metformin is appropriate.
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Side Effects of Antidiabetes Drugs

Most common

More common

Less common

  • Abnormal stools
  • bad, unusual, or unpleasant (after) taste
  • change in taste
  • difficulty with moving
  • discoloration of the fingernails or toenails
  • flu-like symptoms
  • joint pain
  • rash
  • runny nose
  • sneezing
  • stuffy nose
  • swollen joints

Drug Interactions of Antidiabetes Drugs

Antidiabetes drugs may interact with following drugs ,suppliments & may decrease the efficacy of drug


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