Unit 5-Diabetes Flashcards
Metformin
Drug class
Biguanide
Metformin
Mechanism
Activates AMP-kinase and inhibits mitochondrial isoform of glycerophosphate dehydrogenase => decreases hepatic glucose production
Metformin
Uses
First-line therapy in diabetes due to no weight gain or hypoglycemia, reduction in cardiovascular events and mortality
Metformin
Side effects
Lactic acidosis (rare)
GI (diarrhea, abdominal discomfort, N & V), B12 deficiency
Contraindicated in renal impairment; low cost
Glipizide
Drug class
Sulfonylurea
Glipizide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glipizide
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Generally well-tolerated; low cost
Glyburide
Drug class
Sulfonylurea
Glyburide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glyburide
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Long-acting (in general, avoid)
Glimepiride
Drug class
Sulfonylurea
Glimepiride
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glimepiride
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Generally well-tolerated; low cost
Repaglinide
Drug class
Meglitinide
Repaglinide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Repaglinide
Uses
Short-acting; dose with meals
Generic repaglinide available
Repaglinide
Side effects
Weight gain; hypoglycemia (less than sulfonylureas)
Nateglinide
Drug class
Meglitinide
Nateglinide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Nateglinide
Uses
Short-acting; dose with meals
Nateglinide
Side effects
Weight gain; hypoglycemia (less than sulfonylureas)
Pioglitazone
Drug class
Thiazolidinedione
Pioglitazone
Mechanism
Binds PPAR-γ, a nuclear transcription factor; increases peripheral insulin sensitivity
Pioglitazone
Uses
No hypoglycemia; increases HDL cholesterol, decreases triglycerides
Pioglitazone
Side effects
Weight gain; edema; heart failure; bone fractures; macular edema
Increased risk of bladder cancer; possible reduction in myocardial infarctions
Generic available
Rosiglitazone
Drug class
Thiazolidinedione
Rosiglitazone
Mechanism
Binds PPAR-γ, a nuclear transcription factor; increases peripheral insulin sensitivity
Rosigitazone
Uses
No hypoglycemia
Rosiglitazone
Side effects
Weight gain; edema; heart failure; bone fractures; possible increase in cardiovascular events
Increased LDL cholesterol
Expensive; contraindicated in heart disease
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Drug class
GLP-1 receptor agonist
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Mechanism
Activates GLP-1 receptor in β-cells in the pancreas and brain; increases insulin secretion and decreases glucagon secretion in a glucose-dependent fashion; slows gastric emptying, increases satiety; can cause weight loss
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Uses
SubQ injection only (exenatide twice daily, extended release once weekly,liraglutide once daily, others once weekly
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Side effects
GI (nausea, vomiting, diarrhea); acute panceatitis
Hypoglycemia (less than sulfonylureas; caution with renal insufficiency; C cell hyperplasia/medullary thyroid tumors in rodents
expensive
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Drug class
DPP-4 inhibitor
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Mechanism
Inhibition of GLP-1 metabolism; increases insulin and decreases glucagon secretion
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Uses
No hypoglycemia, weight neutral
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Side effects
Well tolerated; rarely urticaria/angioedema & pancreatitis; arthralgias
Expensive
Canagliflozin (Invokana); Dapaglifloxin (Farxiga); Empaglifloxin (Jardiance)
Drug class
SGLT2 inhibitor
Canagliflozin (Invokana); Dapaglifloxin (Farxiga); Empaglifloxin (Jardiance)
Mechanism
Reduces glucose resorption in the kidney; increases urinary glucose excretion; alpha cell agonist (increases glucagon)
Canagliflozin (Invokana); Dapaglifloxin (Farxiga); Empaglifloxin (Jardiance)
Uses
No hypoglycemia; weight loss possible
Canagliflozin (Invokana); Dapaglifloxin (Farxiga); Empaglifloxin (Jardiance)
Side effects
UTIs; genital mycotic infections; volume depletion; hyperkalemia; hypersensitivity; reduced bone density; ketoacidosis
Avoid in renal insufficiency
Expensive
Colesevelam
Drug class
Bile acid sequestrant
Colesevelam
Mechanism
Binds bile acids/cholesterol
Colesevelam
Uses
Modest reduction in A1c; no hypoglycemia; decreased LDL cholesterol
Colesevelam
Side effects
Increase in triglycerides
Constipation; may interfere with absorption of other medications
Expensive
Bromocriptine
Drug class
Dopamine-2 agonist
Bromocriptine
Mechanism
Alters hypothalamic regulation of metabolism; increases insulin sensitivity
Bromocriptine
Uses
Modest reduction in A1c; no hypoglycemia
Bromocriptine
Side effects
Dizziness/syncope
Rhinitis, nausea, fatigue
Rarely used
Pramlintide
Drug class
amylin analog
Pramlintide
Mechanism
Mimics amylin: slows gastric emptying, suppresses postprandial glucagon secretion, may reduce appetite
Pramlintide
Uses
SubQ injection only; used with short or rapidly acting insulin with meals; reduces post-prandial glucose levels; may promote weight loss
Pramlintide
Side effects
Hypoglycemia (significant risk)
GI side effects (especially nausea)
Lispro
Drug class
Rapid-acting insulin
Lispro
Mechanism
OoA: 5-30 min; PA: 0.5-3 hrs; DoA: 3-5 hrs
Lispro
Uses
Bolus insulin; subQ injection
Lispro
Side effects
Hypoglycemia, weight gain
Lipohypertrophy, rare allergic reaction
Expensive; U-200 available
Aspart
Drug class
Rapid-acting insulin
Aspart
Mechanism
OoA: 5-30 min; PA: 0.5-3 hrs; DoA: 3-5 hrs
Aspart
Uses
Bolus insulin; subQ injection
Aspart
Side effects
Hypoglycemia, weight gain
Lipohypertrophy, rare allergic reaction
Expensive
Glulisine
Drug class
Rapid-acting insulin
Glulisine
Mechanism
OoA: 5-30 min; PA: 0.5-3 hrs; DoA: 3-5 hrs
Glulisine
Uses
Bolus insulin; subQ injection
Glulisine
Side effects
Hypoglycemia, weight gain
Lipohypertrophy, rare allergic reaction
Expensive
Oral inhaled Afrezza
Drug class
Rapid-acting insulin
Oral inhaled Afrezza
Mechanism
OoA 15 minutes; PA 50-60 minutes; DoA 2-3 hours
Oral inhaled Afrezza
Uses
Bolus insulin; oral/inhaled; requires periodic pulmonary function tests; doses 4-8 unit increments
ORal inhaled Afrezza
Side effects
Decreases FEV; do not use with chronic lung disease.
Regular insulin
Drug class
Short-acting insulin
Regular insulin
Mechanism
OoA: 30-60 min; PA: 1-5 hrs; DoA: 6-8 hrs
Regular insulin
Uses
Bolus insulin; subQ injection or iv
Regular insulin
Side effects
Hypoglycemia, weight gain
Lipohypertrophy; rare allergic reaction
U-500 available; longer DoA
NPH
Drug class
Intermediate insulin
NPH
Mechanism
OoA: 1-4 hrs; PA: 4-10 hrs; DoA: 14-24 hrs
NPH
Uses
SubQ injection; can mix with regular
NPH
Side effects
Hypoglycemia, weight gain
Lipohypertrophy; rare allergic reaction
NPL
Drug class
Intermediate insulin
NPL
Mechanism
OoA: 1-4 hrs; PA: 4-10 hrs; DoA: 14-24 hrs
NPL
Uses
SubQ injection; available premixed with lispro
NPL
Side effects
NPA
Drug class
Intermediate insulin
NPA
Mechanism
OoA: 1-4 hrs; PA: 4-10 hrs; DoA: 14-24 hrs
NPA
Uses
SubQ injection; available premixed with aspart
NPA
Side effects
Hypoglycemia, weight gain
Lipohypertrophy; rare allergic reaction
Detemir
Drug class
Intermediate insulin
Detemir
Mechanism
OoA: 3-4 hrs; PA: 4-8 hrs; DoA: 6-24 hrs
Detemir
Uses
Basal insulin; at higher doses, longer DoA
Detemir
Side effects
Hypoglycemia, weight gain
Lipohypertrophy; rare allergic reaction
Expensive; should not be mixed
Glargine
Drug class
Long-acting insulin
Glargine
Mechanism
OoA: 2-3 hrs; PA: none; DoA: 24-30 hrs
Glargine
Uses
Basal insulin
Glargine
Side effects
Hypoglycemia, weight gain
Lipohypertrophy; rare allergic reaction
Expensive; should not be mixed; U-300 available (longer DoA)
Degludec
Drug class
Ultra long-acting
Degludec
Mechanism
DoA up to 42 hrs +; half life 25 hrs
Degludec
Uses
Basal insulin
Degludec
Side effects
Hypoglycemia, weight gain
Rare lipohypertrophy; rare allergic reaction
Expensive; U-200 available