ORAL

HYPOGLYCEM
IC DRUGS
Dr Mohit Bansal

Classification

SULFONYLUREAS
BIGUANIDES
ALPHA-GLUCOSIDASE INHIBITORS
THIOZOLIDINEDIONES
MEGLITINIDES
INCRETINS
DPP- IV INHIBITORS (GLIPTINS)
OTHERS

 INSULIN SECRETAGOGUES
1) SULFONYLUREAS
2) NON- SULPHONYLUREAS
a) MEGLITINIDES
b) GLP- 1 AGONISTS
c) DPP- IV INHIBITORS

SULFONYLUREAS
MOA :1. STIMULATE BETA CELLS TO
RELEASE INSULIN
(BY BINDING AND BLOCKING ATP SENSITIVE
K+ CHANNELS)

2. DECREASE HEPATIC RELEASE OF

GLUCOSE
3. INCREASE PERIPHERAL UPTAKE OF
GLUCOSE

 PRESENCE IN GUT DECREASES

ABSORPTION OF GLUCOSE
SHORT HALF LIFE
GIVEN WITHIN HALF HOUR BEFORE
FOOD OR WITH FOOD.
METABOLISED IN LIVER
EXCRETED BY KIDNEY
USED WITH CAUTION IN PATIENTS WITH
RENAL AND HEPATIC DISORDERS
NOT PREFERRED IN OBESE PATIENTS
AS THEY CAUSE WEIGHT GAIN
INTERACTS WITH ASPIRIN AND
ALCOHOL

LASSIFICATION
FIRST GENERATION
TOLBUTAMIDE
CHLORPROPAMIDE
(NOT USED NOW BECAUSE OF HYPOGLYCEMIA)

SECOND GENERATION
GLICLAZIDE
GLIPIZIDE (5 MG ; 15 MG)
GLIBENCLAMIDE (GLUBURIDE)
(2.5/ 5 MG)
GLIMEPERIDE (1/ 2 MG)

IDE EFFECTS
HYPOGLYCEMIA (MORE COMMON
WITH FIRST GENERATION)
CHOLESTASIS
DILUTIONAL HYPONATREMIA
WEIGHT GAIN
HYPERINSULINEMIA
AGRANULOCYTOSIS
APLASTIC AND HEMOLYTIC
ANAEMIA
PRIMARY AND SECONDARY FAILURE (USUALLY
SEEN IN WESTERN POPULATION)

BIGUANIDES
MOA :1) INCREASE PERIPHERAL UPTAKE OF
GLUCOSE
2) IMPAIRS GLUCOSE ABSORPTION FROM GUT
3) INHIBITS GLUCONEOGENESIS IN LIVER
) GIVEN AFTER FOOD INTAKE
) C/I IN HEPATIC AND RENAL FAILURE
PATIENTS; ALCOHOLICS; PATIENTS WITH
ACTIVE INFECTIONS; PATIENTS ON ASPIRIN

LASSIFICATION
METFORMIN
500/800 MG * BD/TDS
500/1000 MG SR * OD/BD
PHENFORMIN
WITHDRAWN IN 1970s DUE TO
LACTIC ACIDOSIS

SIDE EFFECTS
LACTIC ACIDOSIS (MAIN BUT RARE)
NAUSEA, VOMITING, ANOREXIA
METALLIC TASTE

 HELPS IN REDUCTION OF HbA1c BY

2% AND TGs BY 15-20 %
MACROVASCULAR COMPLICATIONS
ARE DECREASED BY METFORMIN
OTHER USES
PCOD
OBESITY
NON ALCOHOLIC HEPATITIS

ALPHA-GLUCOSIDASE
INHIBITORS
MOA :INHIBITS DISACCHARIDASES IN THE GUT
AND DELAY CARBOHYDRATE ABSORPTION
DRUGS
ACARBOSE : 50 MG * TDS (WITH EACH
MEAL)
VOGLIBOSE : 0.2-0.3 MG * TDS
MAGLITOL : 50 MG (JUST BEFORE MEALS)

 CAN ALSO BE USED IN IDDM

SIDE EFFECTS
FLATULENCE
DIARRHOEA
ABDOMINAL BLOATING
CONTRA- INDICATIONS
GASTROPARESIS
INFLAMMATORY BOWEL SYNDROME
CREATININE > 2 MG/ DL

THIOZOLIDINEDIONES
MOA :INCREASES INSULIN SENSITIVITY ON
PERIPHERAL TISSUES ESPECIALLY FAT
* INCREASES LDL AND HDL
* DECREASES TGs
DRUGS
PIOGLITAZONE : 15/30 MG * OD
ROSIGLITAZONE BANNED DUE TO
CARDIOVASCULAR ADVERSE EFFECTS

 ALSO USED FOR INDUCTION OF

OVULATION IN PCOS
SIDE EFFECTS
PEDAL EDEMA
WEIGHT GAIN
BONE #
CHF
CONTRA- INDICATIONS
PREGNANCY
LIVER DISEASE
CARDIAC FAILURE

MEGLITINIDES
MOA :SAME AS SULFONYLUREAS
DRUGS
REPAGLINIDE : 0.5- 1 MG * TDS
NATEGLINIDE
GIVEN MULTIPLE TIMES BECAUSE OF
SHORT HALF LIFE AND SHOULD BE TAKEN
WITH MEALS
SIMILAR SIDE-EFFECTS AS THAT OF SU
BUT HYPOGLYCEMIA IS RARE
REGULATE POST PRANDIAL SUGARS WELL

INCRETINS
(GLP-1)
NEW CLASS OF DRUGS
ORAL GLUCOSE CAUSES RELEASE
OF GUT HORMONES, MAINLY
GLUCAGON LIKE PEPTIDE-1 AND
GLUCOSE INSULINOTROPHIC
POLYPEPTIDE-1, THAT AMPLIFY
THE GLUCOSE INDUCED INSULIN
RELEASE
GLP-1 SUPRESSES GLUCAGON
SECRETION
ALSO, IMPROVES PANCREATIC

 INCRETIN EFFECT IS REDUCED IN TYPE-2

DM AS THERE ARE NO RECEPTORS FOR
INSULIN
GLP-1 IS RAPIDLY PROTEOLYSED BY DPP-IV
DRUGS
EXENTIDE * CONTINOUS I/V INFUSION
LIRAGLUTIDE * S/C
SIDE- EFFECTS
NAUSEA/ VOMITING/ DIARRHOEA
PANCREATITIS
HYPOGLYCEMIA

DPP- IV INHIBITORS
(GLIPTINS)
DIPEPTIDYL PEPTIDASE IV INHIBITORS
POTENTIATE ACTION OF INCRETINS AS GLP-1
IS RAPIDLY PROTEOLYSED BY DPP- IV
PROMOTES INSULIN RELEASE IN PRESENCE OF
GLUCOSE AND INHIBITS WEIGHT GAIN AND
HYPERGLYCEMIA
INHIBITS RISE IN POST-PRANDIAL BLOOD
SUGAR
DRUGS
SITAGLIPTIN : 100 MG * ORAL * OD
VILDAGLIPTIN
SEXAGLIPTIN
GIVEN IN COMBINATION WITH METFORMIN

PRAMLINITIDE
SYNTHETIC ANALOGUE OF ISLET
AMYLOID POLYPEPTIDE (IAPP) OR
AMYLIN
DELAYS GASTRIC EMPTYING AND
DECREASES APETITE
SUPRESSES GLUCAGON
SECRETION
USED IN BOTH T-1 AND T-2 DM
S/C * 15 MCG WITH EACH MEAL

DAPAGLIFLOZIN
SGLT-2 INHIBITORS (INHIBITS GLUCOSE
REABSORPTION IN PROXIMAL
CONVULATED TUBULES OF KIDNEY)
SO, PROMOTES GLYCOSURIA
SIDE-EFFECTS
ELECTROLYTE IMBALANCE
GENITAL INFECTIONS
INCREASE IN FREQUENCY OF
MICTURITION

DRUGS ON BASIS OF SITE OF

ACTION
METFORMIN
THIAZOLIDINEDIONES
DECREASE GLUCOSE OUTPUT

ALPHA-GLUCOSIDASE
INHIBITORS
DELAYS GLUCOSE
ABSORPTION

SULFONYLUREAS
MEGLITINIDES
AMINO ACID
DERIVATIVES
(GLP-1 AGONISTS)
INCREASE INSULIN
SECRETION
METFORMIN
INCREASE PERIPHERAL
GLUCOSE UPTAKE

THIAZOLIDINEDIONES
INCREASE INSULIN
SENSITIVITY

INSULIN IS USED FOR

GESTATIONAL
DIABETES
METFORMIN?

COMBINATIONS
SINGLE OHA : METFORMIN
COMBINATIONS :
SU + METFORMIN
SU+ PIOGLITAZONE
SU + METFORMIN +
PIOGLITAZONE
INSULIN CAN BE ADDED TO ANY
OF THE ABOVE COMBINATIONS

QUERIES/ QUESTIONS
PREFERRED DRUG TO START
TREATMENT?
HOW TO MONITOR EFFECT ?
HOW FREQUENT TO INVESTIGATE
FOR SUGAR LEVELS?
DOSES AND DRUG FREQUENCY?