T18 drugs used in diabetes & obesity

basal insulin

constant and low amount from beta cell to control fasting glucose

bolus / meal insulin

large amount released in response to ingestion of meal

human insulin - produced from

recombinant DNA technology

human insulin - adverse effects

hypoglycemia, lipodystrophy, weight gain, hungry, sweat, palpitations, headache

lipodystrophy

loose fat at injection site

rapid-acting insulin analogs

lispo, aspart, glulisine

long-acting insulin analogs

glargine, detemir

biguanides - drug names

metformin

biguanides - mechanism

activate AMP kinase → reduce hepatic glucose production

increase insulin sensitivity → stimulate insulin receptor tyrosine kinase & GLUT4

biguanides - uses

1st line drug in type 2 DM

biguanides - advanatage

reduce risk of major adverse cardiovascular events

biguanides - contraindications

renal failure patients

biguanides - adverse effects

lactic acidosis, B12 deficiency, nausea, vomit, diarrhea

biguanides - application

start low, go slow

sulfonylureas - drug names

glibenclamide, glipizide, gliclazide, glimepiride

sulfonylureas - mechanism

close ATP-K+ channels → insulin release

sulfonylureas - advantage

effective A1C decrease

sulfonylureas - application

1-2 doses / day (long acting)

sulfonylureas - contraindications

not for type 1 DM patients

sulfonylureas - adverse effects

hypoglycemia, weight gain

glinides - drug names

nateglinide, repaglinide

glinides - mechanism

close ATP-K+ channels → insulin release

glinides - application

take before meals (short acting!!)

glinides - adverse effects

less hypoglycemia, weight gain

thiazolidinediones / glitazones - drug names

pioglitazone

thiazolidinediones / glitazones - mechanism

activate PPAR-gamma → increase insulin sensitivity

PPAR-gamma - location

fat, muscle, liver

thiazolidinediones / glitazones - adverse effects

fluid retention

thiazolidinediones / glitazones - contraindications

heart failure patients

alpha glucosidase inhibitors - drug names

acarbose

alpha glucosidase inhibitors - mechansim

inhibit intestinal alpha glucosidase → decrease carb absorption of monosaccharides

alpha glucosidase

digest disaccharide & starch

alpha glucosidase inhibitors - advantage

decrease postprandial glucose

alpha glucosidase inhibitors - disadvantage

can also decrease premeal glucose

alpha glucosidase inhibitors - application

take with first bite of meal

alpha glucosidase inhibitors - adverse effects

diarrhea, bloating, nausea, vomit

DPP-4 inhibitors - drug names

sitagliptin, vildagliptin

DPP-4 inhibitors - mechanism

inhibits DPP-4 → increase GLP-1 & GIP → increase insulin → decrease glucagon

DPP-4 inhibitors - adverse effects

moderate A1C decrease, renal dosing for renal impairment patients

GLP-1 receptor agonists - drug names

liraglutide, semaglutide, dulaglutide

GLP-1 receptor agonists - mechanism

increase insulin, decrease glucagon, decrease gastric emptying

decrease gastric emptying

feel full easily → don’t want to eat

GLP-1 receptor agonists - advantage

good for DM patients with atherosclerotic vascular disease or chronic kidney disease

GLP-1 receptor agonists - application

injectable or oral → start low, go slow

GLP-1 receptor agonists - adverse effects

nausea, hypoglycemia

dual GIP & GLP-1 agonist - drug names

tirzepatide

dual GIP & GLP-1 agonist - advantage

strong weight loss, well-tolerated

dual GIP & GLP-1 agonist - adverse effects

expensive, moderate A1C effect, renal dosing for renal impairment patients

SGLT2 inhibitors - drug names

empagliflozin, dapagliflozin, canagliflozin

SGLT2 inhibitors - mechanism

inhibits SGLT2 in kidneys → increase urinary glucose excretion

SGLT2 inhibitors - adverse effects

UTI, genital infections, euglycemic DKA, frequent urination, hypotension in elderly

SGLT2 inhibitors - uses

first line for heart failure, chronic kidney disease, atherosclerotic vascular disease patients

obesity - drug treatment

pancreatic lipase inhibitor

pancreatic lipase inhibitor - drug name

orlistat

pancreatic lipase inhibitor - mechanism

prevent fat digestion → triglycerides cannot be absorbed → increase fat excretion in stool

pancreatic lipase

break down dietary triglycerides in intestine

pancreatic lipase inhibitor - adverse effects

oily stools, fecal incontinence, bloating, flatulence, fat-soluble vitamin deficiencies, hypoglycemia in DM patients

pancreatic lipase inhibitor - application

take with first bit of meal containing fats

pancreatic lipase inhibitor - most effective when

used with fatty meal