Pales diabetic meds Flashcards
Sulfonylurea-I
Second generation: Glyburide (Micronase, Diabeta), Glipizide (Glucotrol) regular and XL, Glimepride (Amaryl)
Main mechanism: increase an insulin secretion by blocking K channels of b-cells of pancreas
The effect decreases with prolong use, 50% failure in 5 years
Contraindications: pregnancy/lactation, significant liver or renal insufficiency, sulfa allergy (?)
Sulfonylurea side effects
GI upset Urticaria Jaundice (due to biliary stasis) SIADH (decreased Na, increased BP) * Weight gain
* Hypoglycemia Over age of 60 Impaired renal function Poor nutrition Multidrug therapy
Sulfonylurea comparison
Glipizide/Glimepride have dual (renal/liver) elimination routes, Glyburide is solely renally eliminated. So with CRF use Glipizide/Glimepride.
Avoid using sulfonyluria with unstable renal failure/irregular meals pattern/older patients with frequent hypoglycemic episodes.
Use regular rather XL forms in these patients if you absolutely need to.
Meglitinides
Repaglinide (Prandin)
Nateglinide (Starlix)
Act by closing ATP-dependent K channels of b-cells.
Short acting (about 2-4 hours)
monotherapy or with other diabetic drugs excluding sulfonyluria
Should be taken with meals and if patient skips a meal, he should skip a dose as well
Greater effect on postprandial rises
Good drug to switch to in patients on sulfonyluria at risk for hypoglycemia
Adverse effects:
hypoglycemia, weight gain
Incretins
Injectable/GLP 1
Exenatide (Byetta, Bydureon)
Liraglutide (Victoza)
Oral (DPP-IV inhibitors) Sitagliptine (Januvia) Saxagliptine (Oglyza) Vildagliptin (Galvus) Linagliptin (Trajenta) Alogliptin (Nesina)
DPP-IV inhibitors
the -gliptins
Modest HbA1c reduction (about 0.7) May be used with renal failure, but dose is to be adjusted Doesn’t cause hypoglycemia No weight change May cause pancreatitis (???)
GLP-1 analogs
Exenatide, liraglutide, albiglutide, dulaglutide
SQ injections
Average of 7-12 lbs weight loss
Great in obese diabetics
Major side-effects: nausea(common), pancreatitis (rare)
No hypoglycemia when used alone or with Metformin
Biguanides
Metformin(Glucophage)
Mechanism:, decreases glucose production by liver(primary), increases sensitivity of insulin receptors
decreases LDL, TC, and TG
* Promotes weight loss
* Doesn’t cause hypoglycemia
Side effects:GI upset, * lactic acidosis, decreases B12 and Folate intestinal absorption
biguanide contraindications
Renal and liver insufficiency (Cr.>1.5) Chronic hypoxia past Hx of lactic acidosis alcoholism Withhold if Pt. getting iodinated contrast
Thiazolidinediones
Rosiglitazone (Avandia ) and Pioglitazone (Actos)
Mechanism: increases sensitivity to insulin (primary), decreases hepatic gluconeogenesis
May be combined with SU, or MF
Caution when combining it with insulin
May cause significant weight gain
May take few weeks to work
May cause water retention. Should not be used with significant history of CHF or poor E.F.
May cause liver damage. Not to be used for patients with liver problems(ALT >2.5N)
Rosiglitazone may increase risk of MI, almost was pulled out of market
a-Glycosidase Inhibitors
Acarbose (Precose) and Miglitol (Glyset)
Mechanism: decreases absorption of CH by decreasing brash-border alpha-Glycosidase blunting postprandial. hyperglycemia
No hypoglycemia, lactic acidosis, weight gain
monotherapy or with other
most useful for severe postprandial gluc. rise
From UKPDS 0.5% decrease in HbA1c Only 39% remained on the drug after 3 years Terrible Flatulence-30% Diarrhea: 16% Contraindications: Major GI disorders
GlucosuricsSGLT-2 Inhibitors
Canagliflozin
Dapagliflozin
Block the re-uptake of glucose in the renal tubules --> promote loss of glucose in the urine. Mild weight loss and NO hypoglycemia. Side effects Urinary tract infections Dehydration Yeast infections
Pramlintide
Analogue of Island Amyloid Polypeptide (secreted by B-cells in equal amounts with insulin).
Suppresses glucagon secretion, delays gastric emptying, and decreases appetite.
Rarely used
mechanism unknown diabetes drugs
Bile Acid Sequestrants
Colesevelam (Welchol)
Primarily used for LDL reduction
No effect on CV events
Bromocriptine
dopamine 2 receptor agonist,
Causes nausea, vomiting, dizziness, and headache.
Insulin preparations
Regular insulin at high dose acts like intermediate-acting. It’s rarely used now.
All insulin preparations tend to last longer with renal insufficiency
Intermediate-acting insulins and long acting insulins can be given once or a twice a day in different patients depending on circumstances.
Intermediate-acting insulins should be combined with short-acting insulins in Type I and in more severe Type II patients