DM Drugs Flashcards
Metformin
Glycemia? Weight? Other effects?
Euglycemic, weight loss, decreases macrovascular events (stroke, #1 DM killer), decreases TG.
Metformin S/E
Common: GI (diarrhea)
Serious: Lactic acidosis (esp in ESRD, also in hepatic dz, alcoholism, diseases that predispose to hypoxia: CHF, COPD, being super sick in the hospital, etc). Take pts off 2 days before contrast and when in hospital sick.
Metformin–does it have a black box?
Yes, Lactic acidosis
Metformin–when to take off
2 days before getting contrast
If sick in the hospital
If kidneys are failing
If pt can’t tolerate the diarrhea
Which drugs are second line after Metformin?
Incretins:
incretin mimetics {“-tide”, exenatide (Byetta), Liraglutide (Victoza), Dulaglutide (Trulicity)}
DPP-IV inhibitors {“-gliptin”, sitagliptin (Januvia), saxagliptin (Ongyliza), Linagliptin (Tradjenta), Alogliptin (Nesina)}
How is Metformin given?
Orally–
850-1000mg PO bid, start low and move up. Give w meals, stop for contrast
Extended release: 1000-2000 PO qpm
Metformin MOA
Increases insulin sensitivity–> increased glucose uptake.
Decreases hepatic glucose production (gluconeogenesis)
decreases GI glucose absorption
Decreases glucagon production
MOA incretin mimetics
Activate glucagon-like-peptide-1 (GLP1) receptor–> increase insulin secretion, decrease glucagon secretion, delay gastric emptying
MOA DPP-IV inhibitors
Blocks DPP-IV, which degrades incretins, thereby potentiality incretin effects. (Up insulin, dn glucagon, dn gastric emptying)
Name the incretin mimetics
Exenatide (Byetta)
Liraglutide (Victoza)
Dulaglutide (Trulicity)
Name the DPP-IV inhibitors
Sitagliptin (Januvia)
Saxagliptin (Ongyliza)
Linagliptin (Tradjenta)
Alogliptin (Nesina)
How are incretin mimetics administered?
S.C…..either 60 min before 2 main meals, or once a week
How are DPP-IV inhibitors administered?
Orally…once a day (Januvia 100mg)
Adverse effects of Incretin mimetics
Common: GI disturbance. Slows GI emptying, so careful w pts w slow GI dz. careful w renal impairment.
Bad: pancreatitis, pancreatic CA.
Adverse effects of DPP-IV inhibitors
Common: Less than incretin mimetics. Slow GI probs
Bad: pancreatitis, pancreatic CA (less than incretins)
Main difference between incretin mimetics and DPP-IV inhibitors
Incretin mimetics cause weight loss, DPP-IV I are weight neutral.
Do incretin mimetics have a black box?
Yes—Liraglutide (Victoza), for Thyroid CA. Contraindicated in pts w medullary thyroid carcinoma hx or FHx, and in pts w MEN-2
Do DPP-IV inhibitors have a black box?
No
Third line after Metformin and incretins?
SLGT2 Inhibitors, glitizones, alpha-glucosidase inhibitors, welchol/colesevelam
Name the SLGT2 inhibitors
Canagliflozin (Invokana)
Dapagliflozin (Farxiga)
SGLT2 inhibitors MOA
Inhibit SGLT2 transporters in proximal tubule, causing glucose to be peed out
Contraindications/cautions to SGLT2-I
Severe renal impairment/dialysis; prone to UTIs, etc
Adverse effects of SGLT2-I
Genital mycotoxins infections, UTIs etc
Osmotic diuresis (causes ortho hypo, dehydration, so careful in pts w renal impairment.)
Incretins lower glucose when?
Fasting and post prandial
SGLT2-I decrease glucose when?
A1c
MOA alpha-glucosidase inhibitors
Inhibit alpha-glucose fade in small intestine–> decrease in absorption of glucose.
S/E alpha-glucosidase inhibitors
Common: gas (VERY gassy)
AGI caution
Slow GI (ileus, obstruction, IBS, hernia)
Hepatic dz
Renal impairment
AGI decreases glucose when? Other effects?
Decreases post prandial glucose
No effect on weight or fasting glucose
Thiazolindinediones names
-glitazones
Pioglitazone (Actos)
Rosuglitazone (Avandia)
Do AGI have a black box?
No
Do TZDs have a black box?
Yes–Rosiglitazone, for CHF, cause or exacerbate it (edema). MI/angina.
MOA TZDs
Insulin sensitizers. Bind to nuclear PPAR-alpha receptor–> inc glucose transporters.
DO NOT increase insulin secretion
Effects of TZDs
Decrease insulin resistance (can use prophylactically), TG, fasting glucose, A1c. Slight inc HDL.
Adverse s/e, cautions
Appetite stimulant–> weight gain
Edema–> inc risk of HF in CHF
caution in liver dz, CHF (EF
MOA Colesevelam
Bile acid binding resin…unk why it works.
Colesevelam uses
Decrease fasting glucose in combo. Good in HLD but also inc TG.
Name bile acid binding resin
Colesevelam (Welchol)
Do resins have a black box?
No
Adverse effects/cautions of resins
Generally safe/no common s/e
Caution: Slow GI dz, TG>500, GI obstruction /surgery,
Sulfonylureas/Meglitinides
Stimulate beta cells to produce insulin. VERY hypoglycemic. Destroy pancreas quicker. Sulfonylureas=sulfas, contra in sulfa Ax. Also cause weight gain. Meglitinides are short acting, others are long.
Name the Sulfonylureas
First gen: Tolbutamide, Chlorpropamide, Tolazamide
Second gen: Gluburide, Glipizide, Glimepiride
Name the Meglitinides
-glinides
Repaglinide (Prandin)
Nateglinide (Starlix)
What is Metformin used for?
DM2 and PCOS
