Diabetes drugs Flashcards
metformin (Glucophage)
Class: Biguanides
MoA: - Inhibits glucose production by liver
- Sensitizes insulin receptors in fat and muscle tissues.
- Slight decrease in glucose absorption in the gut
- Does not actively drive blood glucose levels down resulting in ↓risk for hypoglycemia when used by itself.
Uses: First line drug for Type 2 diabetes (T2DM). May be used in combination with other drugs or insulin. May prevent T2DM in younger high-risk patients that were overweight.
Admin: PO BID or XR
Considerations: Generally stopped at hospital admission and substituted for insulin to prevent lactic acidosis from stress. Unbound to plasma proteins, not metabolized in liver, excreted unchanged in urine, potentially resulting in accumulation w/ renal impairment: check creatinine and GFR. Hold for 48 h after dye injections. Alcohol, cimetidine, stress may increase r/f lactic acidosis. Contraindicated in severe infections, trauma, major surgery or acidosis.
AEs: Decreased appetite, nausea, diarrhea, dizziness, malabsorption of amino acids, lactic acidosis (rare but can be fatal), decreased absorption of folic acid and vit B12 which may cause peripheral neuropathy and anemia.
glyburide (Glynase)
Class: Sulfonylureas
MoA: Stimulate the release of insulin from the beta cells in the pancreatic islets resulting in lowering blood glucose levels. May also increase tissue responsiveness to insulin.
Uses: Used in conjunction with life-style changes (diet and activity) for DM2. Generally added to drug regimen if metformin alone is not working.
Admin: PO 1-2 x daily, XR available
Considerations: NSAIDS, ETOH can increase drug effect. Beta blockers may mask symptoms of hypoglycemia and they also suppress insulin release resulting in decreased effectiveness of sulfonylureas. Incr. r/f hypoglycemia in pts w/ renal or hepatic failure. Use w caution in pregnancy or lactation, stop 2 weeks before delivery date.
AEs: hypoglycemia, weight gain
sitagliptin (Januvia)
Class: DPP-4 inhibitors (Gliptins)
MoA: Boosts incretin action by blocking DPP-4 to prevent breakdown of incretin hormones, stimulating the release of insulin. Also decreases release of glucagon causing decrease in gluconeogenesis in the liver.
Uses: Second-line therapy for DM2 in adjunct to Metformin or glitazones.
Admin: PO.
Considerations: No significant interactions. Contraindicated in lactation and use only if absolutely necessary in pregnancy.
AEs: Upper resp infections, headache, inflammation of nasal passages and throat, pancreatitis and hypersensitivity reactions (rare).
exenatide (Byetta)
Class: Glucagon-like GLP-1 receptor agonists
MoA: Activates GLP-1 receptors which results in slower gastric emptying, stimulation of insulin release, inhibiting release of glucagon, suppressing appetite.
Uses: Treat DM2 when other oral drugs and lifestyle changes have not worked to achieve target Hgb A1C
Admin: SubQ injector pens BID w largest meals at least 6h apart. Do not administer drug if skipping a meal. Stored in fridge.
Considerations: R/f hypoglycemia when used w/ sulfonylurea. May delay absorption of PO drugs d/t delayed gastric emptying, PO drugs must be taken 1h before injection of this med. Contraindicated in pts w/ liver disease or elevated LFTs who are taking a statin. Contraindicated in pregnancy and pts w severe renal impairment (excreted unchanged in urine).
AEs: N/V/D, hypoglycemia, injection site irritation, pancreatitis, hypersensitivity, renal impairment.
repaglinide (Prandin)
Class: Meglitinides (glinides)
MoA: Stimulate the release of insulin from the beta cells in the pancreatic islets -> Lowers blood glucose levels.
Uses: Treat DM2 in combination w/ metformin or insulin.
Admin: PO taken w/ each meal. Eat w/in 30 minutes of taking drug. Shorter acting than sulfonylurea.
Considerations: Gemfibrozil (Lopid) and ETOH may increase drug levels and r/f hypoglycemia. Rapid absorption and elimination by hepatic metabolism and biliary excretion: metabolism may be slower in pts w hepatic dysfunction -> incr. r/f hypoglycemia.
AEs: Hypoglycemia, resp. congestion, GI upset
canagliflozin (Invokana)
Class: Sodium-Glucose Co-transporter (SGLT-2) inhibitor (Gliflozins)
MoA: Blocks reabsorption and increases excretion of glucose in the urine by inhibiting renal SGLT-2. Provides renal protection by decrease in protein loss and damage caused by hyperfiltration. Associated with calorie loss and weight loss. Also shown to improve CV and renal outcomes in pts w/ CVD.
Uses: Treat DM2. Being studied for treating DM1.
Admin: PO, Q24h before first meal.
Considerations: Contraindicated in pts w/ significant renal impairment (GFR <30). Cautious use w/ loop & thiazide diuretics d/t added r/f dehydration and orthostatic hypotension. K+ sparing diuretics and ACEI can increase r/f hyperkalemia. Rifampin, phenytoin or phenobarbital can decrease efficacy.
AEs: Incr r/f UTIs & female genital yeast infections d/t glucose in urine. Increased urination from osmotic diuresis can lead to orthostatic hypotension and dehydration w/ associated dizziness. Renal impairment may cause hyperkalemia, hypermagnesemia, and hyperphosphatemia, reduction in GFR and incr. creatinine.
rosiglitazone maleate (Avandia)
Class: TZDs / glitazones
MoA: Activates insulin-responsive genes that stimulate receptors on tissue cells to restore effectiveness of insulin by decreasing insulin resistance, promoting glucose uptake by muscle and fat cells, and decreasing gluconeogenesis by the liver.
Uses: Treat DM2 usually alongside metformin, sulfonylurea, insulin or GLP-1 receptor agonist.
Admin: PO 1-2 x day w/ or w/out food.
Considerations: Increased risk for hypoglycemia when combined with insulin
Greater risk of fluid retention if rosiglitazone is used in combo with insulin. Can cause increased symptoms of acute heart failure in patients with HF diagnosis.
AEs: Upper respiratory tract infection, headache sinusitis and myalgia.
Fluid retention if used w/ insulin.
Risk for fractures in women.
May cause ovulation.
Hepatic failure (rare) monitor liver function test (ALT) every 6 mos.
Metabolized by liver. Eliminated mainly in feces and urine.
Contraindicated in patients w/ active liver disease, pregnancy or lactation.
acarbose (Precose)
Class: Alpha-glucosidase inhibitors
MoA: Alpha-glucosidase enzymes (sucrase, maltase and amylase) are in the brush border cells of the intestinal lining that breaks down complex carbohydrates to monosaccharides (glucose and other simple sugars). Acarbose inhibits the enzyme slowing the breakdown of the carbohydrates, delaying absorption of carbs, resulting in decreased rise in BG after a meal.
Uses: Treat DM2, works well with sulfonylurea.
Admin: PO TID w/ meals.
Considerations: Only 2% of drug is absorbed from GI tract causing v few systemic effects, thus all AEs relate to GI tract. Decreases digoxin levels. Corticosteroids decrease drug effect. Contraindicated in DKA, cirrhosis, inflammatory or malabsorptive bowel disorders, and severe renal impairment. Liver function tests needed regularly to monitor liver function. If hypoglycemic do not use fructose or sucrose as enzyme to break them down is blocked.
AEs: Flatulence, cramps, abdominal distention, diarrhea, borborygmi, anemia d/t decreased iron absorption.
Dextrose 50%
MoA: Raises blood glucose levels immediately
Uses: Drug of choice to treat severe hypoglycemia in pt w/ altered LOC
Admin: IV push when CBG <50
Considerations: Give oral tablets when LOC and ability to swallow are restored to maintain BG WNL.
AEs: n/a
glucagon
MoA: raises BG by promoting breakdown of glycogen into glucose and reducing creation of glycogen.
Uses: Only if IV dextrose not available. Can be given IM or subQ in home setting.
Admin: IM subQ or IV. BG will rise enough to restore LOC in approx. 20 min
Considerations: Give oral carbs when LOC and ability to swallow are restored.
AEs: n/a
Short duration & rapid acting insulin
- Lispro (Humalog)
- Aspart (Novolog)
- Glulisine (Apidra)
Afrezza - INHALED Bolus only
Regular - short duration & slower acting
- Humulin R
Novolin R
NPH - Intermediate duration & slow acting
- Humulin N
- Novolin N
Long duration & slowest acting
Glargine
Detemir
Short & rapid onset/peak/duration
- Onset 5-30min
- Peak 1-3h
Duration 4-8h
- Peak 1-3h
