Diabetes & Weight Loss Drugs

insulin, biguanides, GLP-1 agonists, DPP4 inhibitors, TZDs, SGLT2 inhibitors, secretagogues, GLP-1/GIP agonists

list the categories of diabetes/blood sugar lowering drugs

metformin

list the biguanide drugs

exenatide, dulaglutide, liraglutide, semaglutide

list the GLP-1 agonists

sitagliptin, linagliptin, saxagliptin, alogliptin

list the DPP4 inhibitors

rosiglitazone, pioglitazone

list the TZDs

bexagliflozin, canagliflozin, dapagliflozin, empagliflozin

list the SGLT2 inhibitors

glyburide, glipizide, glimepiride, chlorpropamide, tolbutamide

list the sulfonylurea secretagogues

repaglinide

list the non-sulfonylurea secretagogues

tirzepatide

list the GLP-1/GIP agonists

insulin

formed by pancreatic beta cells, lowers blood sugar

glucagon

formed by pancreatic alpha cells, raises blood sugar

somatostatin

formed by pancreatic delta cells, balances insulin & glucagon levels

amylin

formed by pancreatic beta cells, inhibits glucagon secretion & lowers blood sugar levels, delays gastric emptying after a meal, & increases brain satiety

GLP-1 & GIP

incretin hormones; stimulate insulin secretion & suppress glucagon secretion; slow gastric emptying & increase satiety after a meal

DDP-4

naturally occurring enzyme that breaks down GLP-1 & GIP

insulin

• indication: type 1 diabetes, sometimes type 2 diabetes, gestational diabetes

• MoA: binds insulin receptors on liver, skeletal muscle, & fat which activates tyrosine kinase, promoting uptake, usage, & storage of glucose in skeletal muscle & fat, thus lowering blood glucose

• adverse effects: hypoglycemia, weight gain

• contraindications: cautioned w/ beta blockers

rapid acting

• insulin type

• onset: 15min

• peak: 1-2hr

• duration: 2-4hr

• insulin aspart, insulin glulisine, insulin lispor

regular/short-acting

• insulin type

• onset: 30min

• peak: 2-3hr

• duration: 3-6hr

• human regular

intermediate-acting

• insulin type

• onset: 2-4hr

• peak: 4-12hr

• duration: 12-18hr

• NPH

long acting

• insulin type

• onset: several hours

• duration: 24hr

• degludec, detemire, glargine

ultra long acting

• insulin type

• onset: 6hr

• peak: does not peak

• duration: 36hr

• glargine U-300

inhaled insulin

• insulin type

• onset: 12-15min

• peak: 30min

• duration: 180min

• technosphere insulin-inhalation system

metformin

• type: biguanide

• indication: type 2 diabetes

• MoA: decreases hepatic glucose production, increases insulin-mediated glucose utilization in peripheral tissues

• adverse effects: B12 deficiency, diarrhea, flatulence

• contraindications: renal disease

• does not cause hypoglycemia

• most effective

• inexpensive

• very well tolerated

bexagliflozin, canagliflozin, dapagliflozin, empagliflozin

• type: SGLT2 inhibitors

• indication: type 2 diabetes

• MoA: inhibits SGLT2 in proximal tubule, increasing urinary glucose excretion

• adverse effects: weight loss, reduced BP, dehydration, acute kidney injury, genito-urinary fungal/yeast infections

dulaglutide, exenatide, semaglutide, liraglutide

• type: GLP-1 receptor agonists

• indication: type 2 diabetes, some can be used for weight loss

• MoA: stimulates glucose dependent insulin release from pancreas, mimic GLP-1

• adverse effects: weight loss, pancreatitis, increased risk of medullary thyroid cancer (animal models)

tirzepatide

• type: GLP-1/GIP agonists

• indication: type 2 diabetes, weight loss

• MoA: mimic GLP-1 & GIP, stimulate insulin secretion, suppress glucagon secretion, slow gastric emptying, increase satiety after a meal

• adverse effects: weight loss, pancreatitis, gall bladder issues, increased risk of medullary thyroid cancer & multiple endocrine neoplasia syndrome type 2

sitagliptin, linagliptin, saxagliptin, alogliptin

• type: DPP4 inhibitors

• indication: type 2 diabetes

• MoA: inhibits DPP4, ultimately stimulates glucose dependent insulin release from pancreas

• adverse effects: pancreas, joint pain, myalgias, bullous pemphigoid, heart failure, hepatotoxicity

glyburide, glipizide, glimepiride, chlorpropamide, tolbutamide, repaglinide

• type: sulfonylurea & non-sulfonylurea secretagogues

• indication: type 2 diabetes

• MoA: increase insulin secretion from pancreas by binding to & inhibiting potassium channels on pancreas beta cells

• adverse effects: hypoglycemia, weight gain

• contraindications: cautioned with beta blockers, interactions with NSAIDs, wafrafin, sulfonamide drugs, alcohol, cimetidine, chloramphenicol, diuretics, & corticosteroids

rosiglitazone, pioglitazone

• type: TZDs

• indication: type 2 diabetes

• MoA: activate PPAR which increases transcription/translation of genes involved in production of insulin related proteins in tissues, increases insulin sensitivity; reduces glucose production in liver

• adverse effects: may cause or worsen macular edema, increased Na/H2O retention, edema, weight gain

• contraindications: heart failure

semaglutide, liraglutide

list the GLP-1 agonists that can be used in weight loss tx

naltrexone-bupropion

list the opioid antagonist-antidepressants

phentermine, phentermine-topiramate

list the sympathomimetic amines

setmelanotide

list the melanocortin-4 agonists

orlistat

list the lipase inhibitors

GLP-1 agonists, GLP-1/GIP agonists, opioid antagonist-antidepressants, sympathomimetic amines, melanocortin-4 agonists, lipase inhibitor

list the weight loss drug categories

phentermine

• type: sympathomimetic amines

• indication: weight loss tx

• MoA: stimulant/appetite suppressant

• adverse effects: increased HR, increased BP, insomnia, constipation, nervousness

phentermine-topiramate

• type: sympathomimetic amines

• indication: weight loss tx

• MoA: decrease appetite & craving

• adverse effects: abnormal sensations, dizziness, altered taste, insomnia, constipation, dry mouth, acute myopia & secondary angle closure glaucoma

• contraindications: pregnant, uncontrolled HTN, coronary artery disease, hyperthyroidism, glaucoma, MAOIs, sensitivity to stimulants

naltrexone-bupropion

• type: opioid antagonist-antidepressants

• indication: weight loss tx

• MoA: combines opioid receptor antagonist with antidepressant to affect the pleasure-reward areas of the brain & thereby decrease cravings & appetite

• adverse effects: nausea, constipation, HA, vomiting, dizziness, insomnia, dry mouth, diarrhea, can raise BP

setmelanotide

• type: melanocortin-4 agonists

• indication: weight loss tx for those 6yo+ with a rare inherited condition:

  • pro-opiomelanocortin deficiency

  • proprotein subtilisin-kexin type 1 deficiency

  • leptin receptor deficiency

• MoA: lessens appetite & makes pt feel fuller; helps burn calories when body is at rest

orlistat

• type: lipase inhibitor

• indication: weight loss tx

• MoA: blocks lipase enzyme that breaks down fats consumed through food; inhibits absorption of dietary fats

• adverse effects: oily discharge from rectum, flatus w/ discharge, increased defecation, fecal incontinence