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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 .

DECREASE HEPATIC RELEASE OF GLUCOSE 3.SULFONYLUREAS • MOA :1. STIMULATE BETA CELLS TO RELEASE INSULIN (BY BINDING AND BLOCKING ATP SENSITIVE K+ CHANNELS) 2. 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 .

15 MG) GLIBENCLAMIDE (GLUBURIDE) (2.LASSIFICATION • FIRST GENERATION TOLBUTAMIDE CHLORPROPAMIDE (NOT USED NOW BECAUSE OF HYPOGLYCEMIA) • SECOND GENERATION GLICLAZIDE GLIPIZIDE (5 MG .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. PATIENTS ON ASPIRIN . PATIENTS WITH ACTIVE INFECTIONS. ALCOHOLICS.

LASSIFICATION • METFORMIN 500/800 MG * BD/TDS 500/1000 MG SR * OD/BD • PHENFORMIN WITHDRAWN IN 1970s DUE TO LACTIC ACIDOSIS SIDE EFFECTS • LACTIC ACIDOSIS (MAIN BUT RARE) • NAUSEA. ANOREXIA • METALLIC TASTE . VOMITING.

• 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 .

2-0.ALPHA-GLUCOSIDASE INHIBITORS • MOA :INHIBITS DISACCHARIDASES IN THE GUT AND DELAY CARBOHYDRATE ABSORPTION DRUGS • ACARBOSE : 50 MG * TDS (WITH EACH MEAL) • VOGLIBOSE : 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 .

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 .5.MEGLITINIDES • MOA :SAME AS SULFONYLUREAS DRUGS • REPAGLINIDE : 0.

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

• 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 .

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 .IV INHIBITORS (GLIPTINS) • DIPEPTIDYL PEPTIDASE IV INHIBITORS • POTENTIATE ACTION OF INCRETINS AS GLP-1 IS RAPIDLY PROTEOLYSED BY DPP.DPP.

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? .