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
- Insulin sensitizers (reduce insulin resistance)
- Secretagogues (stimulate insulin release)
- 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.
|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.
|Rapid Acting Insulins|
|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 aspart protamine/
|NovoLog 50/50, NovoLog 70/30|
|Insulin lispro protamine/
|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.
Biguanides improve peripheral glucose uptake and utilization.
|Metformin||Glucophage, Glucophage XR, Glumetza, Riomet, Fortamet|
Phenformin and Buformin were withdrawn due to lactic acidosis risk.
Thiazolidinediones work through the improvement of insulin sensitivity by acting on adipose, muscle, and liver to increase glucose utilization and decrease glucose production.
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.
|Glipizide||Glucotrol, Minidiab, Glibenese|
|Glyburide (glibenclamide)||Diabeta, Micronase, Glynase, Daonil, Euglycon|
Meglitinide derivatives stimulate insulin secretion from pancreatic cells, lowering blood glucose levels.
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.
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.
|Short-acting GLP-1 analogs|
|Long-acting GLP-1 analogs|
|Prolonged-acting GLP-1 analogs|
|Exenatide once weekly||Bydureon|
|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.
|DPP-4 inhibitors under development|
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.
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.
|SGLT-2 inhibitors under development|
Other Anti-diabetic Drugs
|Bile acid sequestrant|
|Colesevelam||Welchol, Cholestagel, Lodalis|
|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.
Side Effects of Antidiabetes Drugs
- physical weakness (asthenia)
- gas (flatulence)
- symptoms of weakness, muscle pain (myalgia)
- upper respiratory tract infection
- low blood sugar (hypoglycemia)
- abdominal pain (GI complaints), lactic acidosis (rare)
- low blood levels of vitamin B-12
- chest discomfort
- chills, dizziness
- bloating/abdominal distention
- Abdominal or stomach discomfort
- cough or hoarseness
- decreased appetite
- fast or shallow breathing
- fever or chills
- general feeling of discomfort
- lower back or side pain
- muscle pain or cramping
- painful or difficult urination
- 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
- runny nose
- stuffy nose
- swollen joints
Drug Interactions of Antidiabetes Drugs
Antidiabetes drugs may interact with following drugs ,suppliments & may decrease the efficacy of drug
- angiotensin converting enzyme inhibitors (ACEIs; captopril, enalapril, ramipril)
- antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine,
- birth control pills
- corticosteroids (e.g., dexamethasone, prednisone)
- diabetic drugs (e.g., glyburide, insulin, repaglinide, sitagliptin)
- diuretics (e.g., furosemide, hydrochlorothiazide)
- HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
- quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
- selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, sertraline paroxetine,