Antidiabetes Drugs; Indications, Side Effects, Drug Interactions

Antidiabetes drugs
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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

ClassGeneric/Brand/Approval year
SGLT-2 inhibitorCanagliflozin (Invokana), 2013
DPP-4 inhibitorAlogliptin (Nesina, Vipidia), 2013
SGLT-2 inhibitorDapagliflozin (Farxiga), 2014
SGLT-2 inhibitorEmpagliflozin (Jardiance), 2014
GLP-1 receptor agonistAlbiglutide (Tanzeum), 2014
GLP-1 receptor agonistDulaglutide (Trulicity), 2014
Inhaled insulin powderAfrezza, 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.

GenericBrand Name
Rapid Acting Insulins
Insulin aspartNovolog
Insulin glulisineApidra
Insulin lisproHumalog
Insulin humanAfrezza Inhalation Powder
Short Acting Insulins
Regular insulinHumulin R, Novolin R
Intermediate Acting Insulins
Insulin NPHHagedorn NPH , Humulin N, Novolin N
Long Acting Insulins
Insulin detemirLevemir
Insulin glargineLantus
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 /LixisenatideSoliqua 100/33
Insulin degludec/LiraglutideXultophy 100/3.6

Sensitizers

Sensitizers increase the sensitivity of target organs to insulin.

Biguanides

Biguanides improve peripheral glucose uptake and utilization.

GenericBrand Name
MetforminGlucophage, 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.

GenericBrand Name
RosiglitazoneAvandia
PioglitazoneActos

Secretagogues

Secretagogues increase insulin secretion by the pancreas.

Sulfonylureas

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.

GenericBrand Name
First-generation
AcetohexamideDymelor
ChlorpropamideDiabinese
TolazamideTolinase
TolbutamideOrinase
Second-generation
GlipizideGlucotrol, Minidiab, Glibenese
Glyburide (glibenclamide)Diabeta, Micronase, Glynase, Daonil, Euglycon
GlimepirideAmaryl
GliclazideUni Diamicron
GlyclopyramideDeamelin-S
GliquidoneGlurenorm

Meglitinides

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

GenericBrand Name
NateglinideStarlix
RepaglinidePrandin, 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.

GenericBrand Name
AcarbosePrecose, Glucobay
MiglitolGlyset
VogliboseBasen

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.

GenericBrand Name
Short-acting GLP-1 analogs
ExenatideByetta
LixisenatideLyxumia, Adlyxin
Long-acting GLP-1 analogs
LiraglutideVictoza
Prolonged-acting GLP-1 analogs
AlbiglutideTanzeum
DulaglutideTrulicity
Exenatide once weeklyBydureon
Under development
TaspoglutidePhase 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.

GenericBrand Name
AlogliptinNesina, Vipidia
AnagliptinSuiny
LinagliptinTrajenta
SaxagliptinOnglyza
SitagliptinJanuvia
TeneligliptinTenelia
DPP-4 inhibitors under development
Dutogliptin
Gemigliptin

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.

GenericBrand Name
PramlintideSymlin

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.

GenericBrand Name
CanagliflozinInvokana
DapagliflozinForxiga, Farxiga
EmpagliflozinJardiance
SGLT-2 inhibitors under development
Ertugliflozin
Ipragliflozin
Remogliflozin etabonate
Tofogliflozin

Other Anti-diabetic Drugs

GenericBrand Name
Dopamine agonist
BromocriptineParlodel, Cycloset
Bile acid sequestrant
ColesevelamWelchol, Cholestagel, Lodalis

Combinations

GenericBrand Name
Alogliptin + MetforminKazano
Dapagliflozin + MetforminXigduo XR
Glipizide + MetforminMetaglip
Glyburide + MetforminGlucovance
Linagliptin + MetforminJentadueto
Pioglitazone + MetforminActoplus Met, Actoplus Met XR
Repaglinide + MetforminPrandimet
Rosiglitazone + MetforminAvandamet
Saxagliptin + MetforminKombiglyze XR
Sitagliptin + MetforminJanumet
Rosiglitazone + GlimepirideAvandaryl
Pioglitazone + GlimepirideDuetact
Alogliptin + PioglitazoneOseni
Simvastatin + SitagliptinJuvisync
Empagliflozin + MetforminSynjardy

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

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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