Oral Antidiabetic / Hypoglycemic agents
Introduction:
Bullet point (Hard words):
Hypoglycemia
Oral hypoglycemic agents.
Diabetes
Type 1 diabetes
Type 2 diabetes
Insulin
Hypoglycemia is a condition in which your blood sugar (glucose) level
is lower than normal.
Synthetic organic compounds which lowers the blood glucose level are
known as oral hypoglycemic agents.
Diabetes is a disease which involves high blood sugar (glucose) level.
Type 1 diabetes, once known as juvenile diabetes or insulin-dependent
diabetes, is a chronic condition in which the pancreas produces little or
no insulin.
Oral hypoglycemic drugs are used only in the treatment of type 2
diabetes or non-insulin-dependent diabetes
Insulin is a hormon secreated by β-cell of pancreas when blood glucose
level is rises. Insulin Regulate blood glucose level.
,Classification of Oral Antidiabetic / Hypoglycemic
agents:
Chemical and mechanistic Classification:
1] Chemical Class: Biguanides (Mechanistic Class: Insuline
sensitizer via activation of AMPK): e.g. Metformin
Metformin is derivative of biguanide.
2] Chemical Class: Sulfonylurea (Mechanistic Class: ATP-sensitive
potassium channel blocker [Enhances insulin secretion]): e.g.
Tolbutamide, Chlorpropamide, Glipizide, and glimepiride
Tolbutamide, Chlorpropamide, Glipizide, and glimepiride are
sulfonylurea derivatives.
These sulfonylurea / ATP-sensitive potassium channel blocker are
classified as follows
a) 1st Generation like Tolbutamide, and Chlorpropamide.
b) 2nd Generation: e.g. Glipizide, and glimepiride.
,3] Chemical Class: Meglitinide (Mechanistic Class: ATP-sensitive
potassium channel blocker [Enhances insulin secretion]): e.g.
Repaglinide, Nateglinide.
4] Chemical Class: Thiazolidinedione (Mechanistic Class: Insuline
sensitizer via stimulation of Peroxisome Proliferator Activated
Receptor [PPAR]): e.g. Rosiglitazone and Pioglitazone.
Fully saturated analogue of thiazole is known as thiazolidine
Rosiglitazone and Pioglitazone are derivatives of
thiazolidine-2,4-dione.
5] Mechanistic Class: α- Glucosidase inhibitors (Chemical Class:
Miscellaneous): e.g. Acarbose, and Voglibose.
6] Mechanistic Class: Dipeptidyl Peptidase IV (DPP IV) Inhibitors
(Chemical Class: Miscellaneous):
7] Mechanistic Class: GLP-1 agonists (Chemical Class:
Miscellaneous):
Sulfonylurea
Chemistry:
Generic name, Structure and IUPAC name of Sulfonylureas
A] 1st Generation sulfonyl urea
Scaffold structure / general structure
, Phenylsulfonylurea
Sulfonylureas are urea derivatives with an para substituted
phenylsulfonyl group at 1st position and bulky aliphatic substituent
at 3rd position.
Generic name: Chloropropamide
Structural information obtained from generic name.
-propa word in generic name indicates that bulky aliphatic substituent
on urea nitrogen atom is n-propyl.
-Chloro word in generic name indicates that at para position of phnyl
ring (R1) contains chloro group.
Structure:
Introduction:
Bullet point (Hard words):
Hypoglycemia
Oral hypoglycemic agents.
Diabetes
Type 1 diabetes
Type 2 diabetes
Insulin
Hypoglycemia is a condition in which your blood sugar (glucose) level
is lower than normal.
Synthetic organic compounds which lowers the blood glucose level are
known as oral hypoglycemic agents.
Diabetes is a disease which involves high blood sugar (glucose) level.
Type 1 diabetes, once known as juvenile diabetes or insulin-dependent
diabetes, is a chronic condition in which the pancreas produces little or
no insulin.
Oral hypoglycemic drugs are used only in the treatment of type 2
diabetes or non-insulin-dependent diabetes
Insulin is a hormon secreated by β-cell of pancreas when blood glucose
level is rises. Insulin Regulate blood glucose level.
,Classification of Oral Antidiabetic / Hypoglycemic
agents:
Chemical and mechanistic Classification:
1] Chemical Class: Biguanides (Mechanistic Class: Insuline
sensitizer via activation of AMPK): e.g. Metformin
Metformin is derivative of biguanide.
2] Chemical Class: Sulfonylurea (Mechanistic Class: ATP-sensitive
potassium channel blocker [Enhances insulin secretion]): e.g.
Tolbutamide, Chlorpropamide, Glipizide, and glimepiride
Tolbutamide, Chlorpropamide, Glipizide, and glimepiride are
sulfonylurea derivatives.
These sulfonylurea / ATP-sensitive potassium channel blocker are
classified as follows
a) 1st Generation like Tolbutamide, and Chlorpropamide.
b) 2nd Generation: e.g. Glipizide, and glimepiride.
,3] Chemical Class: Meglitinide (Mechanistic Class: ATP-sensitive
potassium channel blocker [Enhances insulin secretion]): e.g.
Repaglinide, Nateglinide.
4] Chemical Class: Thiazolidinedione (Mechanistic Class: Insuline
sensitizer via stimulation of Peroxisome Proliferator Activated
Receptor [PPAR]): e.g. Rosiglitazone and Pioglitazone.
Fully saturated analogue of thiazole is known as thiazolidine
Rosiglitazone and Pioglitazone are derivatives of
thiazolidine-2,4-dione.
5] Mechanistic Class: α- Glucosidase inhibitors (Chemical Class:
Miscellaneous): e.g. Acarbose, and Voglibose.
6] Mechanistic Class: Dipeptidyl Peptidase IV (DPP IV) Inhibitors
(Chemical Class: Miscellaneous):
7] Mechanistic Class: GLP-1 agonists (Chemical Class:
Miscellaneous):
Sulfonylurea
Chemistry:
Generic name, Structure and IUPAC name of Sulfonylureas
A] 1st Generation sulfonyl urea
Scaffold structure / general structure
, Phenylsulfonylurea
Sulfonylureas are urea derivatives with an para substituted
phenylsulfonyl group at 1st position and bulky aliphatic substituent
at 3rd position.
Generic name: Chloropropamide
Structural information obtained from generic name.
-propa word in generic name indicates that bulky aliphatic substituent
on urea nitrogen atom is n-propyl.
-Chloro word in generic name indicates that at para position of phnyl
ring (R1) contains chloro group.
Structure:
