Oral Hypoglcaemic Drugs

Question 1

Oral antifiabetic agent

Answer 1

1. Sulfonylurea
2. Meglitinide analogs
3. Biguanide
4. Thiazolidinediones
5. Alpha glucosidase inhibitor
6. Incretin based therapy
7. DPP4 inhibitor
8. SGLT2 inhibitors

Question 2

MOA sulfonylurea

Answer 2

MOA sulfonylurea
-stimulate insulin release
-bind to the sulfonylurea receptor, inhibit the efflux of potassium ions, result in depolarization
-depolarization opens a voltage-gated calcium channel, results calcium influx and release of insulin
-increase binding of insulin to receptor & target tissue
-reduce serum glucagon levels

Exp: Tobutamine, Glyburide, Glypizide, Glimepride

Question 3

Side effect of sulfonylurea

Answer 3

Weight gain, hypoglycemia, disulfiram like reaction with alcohol

Contraindicated: pregnancy - cross placenta

Question 4

MOA meglitinide

Answer 4

Exp: Repaglinide, Nateglinide
MOA
-bind to sulfonylurea receptor of ATP sensitive K+ channels and cause release of insulin

Question 5

MOA biguanide (insulin sensitizers)

Answer 5

Exp: metformin
MOA
-inhibit glucose output by liver
-retard the intestinal absorption of sugar
-reduce plasma glucagon levels
-reduce LDL, VLDL, and increase HDL

Adr: anorexia, nausea, Vomitting, diarrhea, absorption vitamin b12 reduced

Clinical use: first line for type II diabetes mellitus, restore fertility in polycystic ovarian disease

Question 6

Thiazolidinediones MOA

Answer 6

Exp: Piiglitazone, rosiglitazone
MOA: peroxime proliferator-activated receptor (PPAR) gamma regulates genes involved in lipid and glucose metabolism

Adr: fluid retention, edema, risk of cardiac failure

Question 7

Alpha glucosidase inhibitors

Answer 7

Exp: Acarbose, miglitol
MOA: Reversibly inhibit alpha glucosidase in the intestine, slow absorption of carbohydrate

Adr: flatulence, diarrhea, abdominal pain

Question 8

Incretin mimetic

Answer 8

Exp: exenatide, liraglutide
MOA
-improve insulin release
-slows gastric emptying and produce a feeling of satiety
-slowing down absorption of glucose by the guts
-promote beta cell proliferation

Adr:Nausea, Vomitting, pancreatitis

Question 9

DPP4 inhibitor

Answer 9

Exp: sitagliptine, linagliptine
MOA
-inhibit DPP4 which inactivate incretin hormone like GLP-1
-increase insulin release

Adr:nas pharyngitis, headache, pancreatitis

Question 10

SGLT inhibitor
Sodium-glucose cotransporter inhibitor 2

Answer 10

MOA: inhibit SGLT2, inhibit reabsorption of glucose in the kidneys and increase urinary glucose excretion

Adr: vulvovaginal candidiasis, urinary tract infection, urinary frequency