anti DM tables Flashcards
Biguanides
metformin
Biguanides Moa
Liver (primary) – decreases glucose production
Muscle/adipose tissue - decreases insulin resistance
metoformin moa
Metformin comments
risk hypoglycemia?
Weight ?
first line??
role with insulin?
Beneficial in the treatment of?
vitamin deficiency risk?
ADRs common in what system
metabolic adr? rare in?
Low risk of hypoglycemia when used as monotherapy
Weight neutral
One of the first line drug therapy options added to diet and exercise
Ameliorates insulin- associated weight gain
Beneficial in the treatment of prediabetes
B12 deficiency risk
GI ADRs (e.g., diarrhea, nausea, cramping)
Lactic acidosis (rare) in patients with cardiovascular, renal, or hepatic dysfunction
Glucagon-like peptide-receptor agonists (GLP1-RA)
dulaglutide
exenatide
liraglutide
lixisenatide
semaglutide
Glucagon-like peptide-receptor agonists (GLP1-RA) moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying
dulaglutide moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
exenatide moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
liraglutide moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
lixisenatide moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
semaglutide moa
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
Glucagon-like peptide-receptor agonists (GLP1- RA)
risk of hypoglycemia
nausea?
Weight?
CV/ renal? agents?
Injection site?
Pancreatitis (rare)
May be associated with dx of what GI organ?
Risk of tumors where?
Low risk of hypoglycemia when used as monotherapy
Nausea
Weight loss
CV benefit (albiglutide, dulaglutide, liraglutide, semaglutide) and renal
benefit (liraglutide, semaglutide)
Injection site reactions
Pancreatitis (rare)
May be associated with gallbladder disease
Risk of Thyroid-C cell tumors
Glucagon-like, peptide-1 (GLP-1) agonist and glucose- dependent insulinotropic polypeptide (GIP) agonist (a “twincretin”):
tirzepatide
Glucagon-like, peptide-1 (GLP-1) agonist and glucose- dependent insulinotropic polypeptide (GIP) agonist moa
increases insulin secretion in response to elevated glucose, decreases glucagon
secretion, slows gastric emptying
tirzepatide moa
increases insulin secretion in response to elevated glucose, decreases glucagon
secretion, slows gastric emptying
tirzepatide
risk of hypoglycemia?
weight?
A1c reduction?
CV/renal?
May delay absorption of?
Low risk of hypoglycemia
More weight loss than GLP-1 agonists
More A1c reduction than most GLP-1 agonists.
No CV or kidney outcomes data yet.
May delay oral contraceptive absorption
Sodium glucose cotransporter-2 inhibitors (SGLT-2
bexagliflozin
canagliflozin
dapagliflozin
empagliflozin
ertugliflozin
Sodium glucose cotransporter-2 inhibitors (SGLT-2) moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
bexagliflozin moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
canagliflozin moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
dapagliflozin moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
empagliflozin moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
ertugliflozin moa
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
Sodium glucose cotransporter-2 inhibitors (SGLT-2)
risk of hypoglycemia?
Weight?
CV and renal? agents?
Genital side effects?
BP?
lipid profile?
urine?
pancreas?
May be associated with rare? agent?
bones?
Increased risk of what gangrene?
Low risk of hypoglycemia
Weight loss
CV and renal benefit (canagliflozin, dapagliflozin, empagliflozin)
Genital fungal (yeast) infections (male/female)
UTI
Dizziness, hypotension,
Increased LDL
Increased urination
Acute pancreatitis (rare)
May be associated with rare amputations (canagliflozin
Increases fracture risk (rare)
Increased risk of Fournier’s gangrene - infection in the scrotum (which includes the testicles), penis, or perineum (rare)
Dipeptidyl-
Peptidase-4
Inhibitors (DPP-4
alogliptin
linagliptin
saxagliptin
sitagliptin
Dipeptidyl- Peptidase-4 Inhibitors (DPP-4 )moa
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
alogliptin moa
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
linagliptin moa
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
saxagliptin moa
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
sitagliptin moa
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
DPP-4 inhibitors
risk of hypoglycemia?
Weight?
May be associated with?
CV?
joints?
Low risk of hypoglycemia when used as monotherapy
Weight neutral
May be associated with pancreatitis
New or worsening heart failure
May cause severe joint pain
Thiazolidinedione
(TZD)
pioglitazone
rosiglitazone
TZD moa
Muscle and adipose – peroxisome proliferator- activated receptor γ(gamma) - (PPARγ) agonist, makes tissues more sensitive to endogenous insulin and enhances glucose uptake into the tissues. Does not increase pancreatic insulin secretion
rosiglitazone moa
Muscle and adipose – peroxisome proliferator- activated receptor γ(gamma) - (PPARγ) agonist, makes tissues more sensitive to endogenous insulin and enhances glucose uptake into the tissues. Does not increase pancreatic insulin secretion
pioglitazone moa
Muscle and adipose – peroxisome proliferator- activated receptor γ(gamma) - (PPARγ) agonist, makes tissues more sensitive to endogenous insulin and enhances glucose uptake into the tissues. Does not increase pancreatic insulin secretion
Thiazolidinedione
risk of hypoglycemia?
peripheral tissues?
Weight ?
CV?
bones?
Low risk of hypoglycemia when used as monotherapy
Edema
Weight gain
Heart failure. Avoid in patient with symptomatic heart failure
Increased fracture risk
Sulfonylureas (SU)
Note: 1st generation not included since not commonly used in practice
glimepiride (2nd Gen)
glipizide (2nd Gen)
glyburide(2nd Gen)
Start with ”g” and end in “ide” - glipizide, glyburide, glimepiride
Sulfonylureas (SU) moa
Secretagogue
Pancreas - Stimulates beta cells causing insulin secretion
glimepiride moa
Secretagogue
Pancreas - Stimulates beta cells causing insulin secretion
glipizide moa
Secretagogue
Pancreas - Stimulates beta cells causing insulin secretion
glyburide moa
Secretagogue
Pancreas - Stimulates beta cells causing insulin secretion
Sulfonylureas (SU)
Hypoglycemia?
Weight?
“Durability”
Hypoglycemia, especially with renal dysfunction (usually discontinue with use of insulin)
Weight gain
“Durability” declines over time
metformin
Biguanides
Liver (primary) – decreases glucose production
Muscle/adipose tissue - decreases insulin resistance
Biguanides Moa
dulaglutide
exenatide
liraglutide
lixisenatide
semaglutide
Glucagon-like peptide-receptor agonists (GLP1-RA)
incretin mimetic – Glucagon-like peptide 1 (GLP-1) receptor agonist that enhances glucose- dependent insulin secretion by the pancreatic beta-cell, suppresses
inappropriately elevated glucagon secretion, and slows gastric emptying
Glucagon-like peptide-receptor agonists (GLP1-RA) moa
tirzepatide
Glucagon-like, peptide-1 (GLP-1) agonist and glucose- dependent insulinotropic polypeptide (GIP) agonist (a “twincretin”):
increases insulin secretion in response to elevated glucose, decreases glucagon
secretion, slows gastric emptying
Glucagon-like, peptide-1 (GLP-1) agonist and glucose- dependent insulinotropic polypeptide (GIP) agonist moa
bexagliflozin
canagliflozin
dapagliflozin
empagliflozin
ertugliflozin
Sodium glucose cotransporter-2 inhibitors (SGLT-2
Inhibition the protein, Sodium glucose cotransporter-2 in the proximal tubules, blocks
the reabsorption of glucose in the kidney, increases glucose excretion, and lowers
blood glucose levels
Sodium glucose cotransporter-2 inhibitors (SGLT-2) moa
alogliptin
linagliptin
saxagliptin
sitagliptin
Dipeptidyl-
Peptidase-4
Inhibitors (DPP-4
Inhibits the action of DPP- 4, an enzyme which destroys incretin hormones (Glucagon-like
peptide 1 (GLP-1 and Gastric inhibitory polypeptide GIP) The inhibition causes decreased glucagon release which results in increased insulin secretion, decreased gastric emptying and decreased blood glucose levels
Dipeptidyl- Peptidase-4 Inhibitors (DPP-4 )moa
pioglitazone
rosiglitazone
Thiazolidinedione
(TZD)
Muscle and adipose – peroxisome proliferator- activated receptor γ(gamma) - (PPARγ) agonist, makes tissues more sensitive to endogenous insulin and enhances glucose uptake into the tissues. Does not increase pancreatic insulin secretion
TZD moa
glimepiride
glipizide
glyburide
Sulfonylureas (SU)
Note: 1st generation not included since not commonly used in practice
Secretagogue
Pancreas - Stimulates beta cells causing insulin secretion
Sulfonylureas (SU) moa
rapid acting insulins
Humalog,
Amelog,
Lyumjev (insulin lispro)
NovoLog,
Fiasp* (insulin aspart)
Apidra (insulin glulisine)
use of rapid acting insulins
Bolus dosing(meals) and insulin
pumps (administration ranges 5-15
minutes before meals –see specific
product information)
short acting insulins
Humulin R or Novolin R - Regular
insulin -
use of short acting insulins
Bolus dosing(meals)
(administration ranges 15-30
minutes before meals –see specific
product information)
intermeadiate acting insulins
Humulin N or Novolin N - NPH
intermeadiate acting insulins use
~ “Basal-like” (administration Q
day to BID)
long acting insulins
Lantus, Basaglar* Rezvoglar,
Semglee, (insulin glargine) – 100
units/mL
Toujeo (insulin glargine) – 300
unitls/mL
Levemir (insulin detemir) – to be
discontinued in 2024
long acting insulin uses
Basal (administration Q day)
ultra long acting insulins
Tresiba (insulin degludec)
ultra long acting insulins use
Basal (administration Q day,
anytime of day)
Humalog,
Amelog,
Lyumjev (insulin lispro)
NovoLog,
Fiasp* (insulin aspart)
Apidra (insulin glulisine)
rapid acting insulins
Bolus dosing(meals) and insulin
pumps (administration ranges 5-15
minutes before meals –see specific
product information)
use of rapid acting insulins
Humulin R or Novolin R - Regular
insulin -
short acting insulins
Bolus dosing(meals)
(administration ranges 15-30
minutes before meals –see specific
product information)
use of short acting insulins
Humulin N or Novolin N - NPH
intermeadiate acting insulins
~ “Basal-like” (administration Q
day to BID)
intermeadiate acting insulins use
Lantus, Basaglar* Rezvoglar,
Semglee, (insulin glargine) – 100
units/mL
Toujeo (insulin glargine) – 300
unitls/mL
Levemir (insulin detemir) – to be
discontinued in 2024
long acting insulins
Basal (administration Q day)
long acting insulin uses
Tresiba (insulin degludec)
ultra long acting insulins
Basal (administration Q day,
anytime of day)
ultra long acting insulins use
ultra long lasting insulin
which DM rx have CV benefits
GLP-RA and SGLT-2 inhib
which DM rx have renal benefits
SGLT-2 inhib
which DM rx have risk of hypoglycemia
SU and insulins
which DM Rx cause weight gain
SU and TZD
which DM Rx cause weight loss
SGLT2 inhib
trizepatide
GLP1RA
which DM rx can cause new/worse HF
DPP4 inhib and TZD