Diabetes Pharm Flashcards
Drugs with little/no risk of HYPOGLYCEMIA (5)
Metformin
GLP-1 RA
SGLT2-I
DPP4-I
TZD
Drugs with HIGH risk of HYPOGLYCEMIA
Sulfonuryea
Insulin
Drugs causing weight gain?
Sulfunayrea
Insulin
TZD
Drugs causing weight loss
Metformin i
GLP-1 RA
SGLT2-I
DPP4-I
Metformin (glucophage)
MOA
Limits haptic production of glucophage
Metformin (Glucophage)
Indications + off label
Treatment of T2DM
Off-label: Pre diabetes prevention, PCOS
Metformin (Glucophage)
Effectiveness/Advantages
reduces A1C by 1.5-2%
Modest weight loss or weight stabilization
Low risk of hypoglycemia
Metformin (Glucophage)
S.E.
GI most common (allergies)
Diarrhea, N/V
Metallic taste
Minimized by gradual dose titration or XR formulations
Also can be done used in IV contrast (hold 48hrs before to 48hrs later)
Metformin
BBW
Elevated lactate and anion acidosis
Increased risk in renal impairment
Hypoperfusion
Hypoxia
Glucophage CI
Metformin
CKD Heart Failure ALcohol use Surgery Significant chronic liver disease
Can cause b12 deficiency
Sulfonylureas
MOA
Stimulate pancreatic beta cells to secrete more insulin REGARDLESS of glucose levels
Sulfonylureas
Drug list
glyburide (Micronase, Diabeta)
Glipizide (Glucotrol)
Glimepiride (Amaryl)
Sulfonylureas
SE/Adverse outcomes
Can cause weight gain
Can cause hypoglycemia
Increase in all cause mortality (may even increase CVD)
Sulfonylurea
Effectiveness
Reduces A1c by 1-2%
Effectiveness decreases over time as b-cell mass declines
Sulfonylurea
C/i
Sulfa allergic patients (avoid in those with SJS/TEN rxns)
G6PD def.
Sulfonylurea indications
Used often 2nd line therapy for T2DM
Falling out of favor
GLP-1 analogs
MOA + possible benefit
Stimulating glucose dependent insulin release from pancreatic islets
Slows gastric emptying, inhibits inappropriate post meal glucagon release and reduce food intake
MAY Also stimulate beta cell recovery
Drug list
GLP-1 analogs
Exenetide (Byetta, Bydureon) - daily, weekly
Liraglutide (Victoza) - daily
Albiglutide (Tanzeum) - weekly
Dulaglutide (Trulicity) -weekly
GLP-1 RA
Indications
Used 1st Lin in pts with T2DM
GLP-1 Analogs
Effectiveness
Lower A1c by 1%
GLP-1 Analogs
ADRs
GI effects (cause nausea, v/d)
pancreatitis
Injection site reactions
Thyroid C cell tumors
CI of GLP-1 Analogs
Stage V CKD
Also use caution in CKD stage IV
DPP-IV inhibitors
MOA
Inhibits the breakdown and prolongs action of endogenous incretin hormones
Drug list DPP-IV inhibitors
Stigalipitin (Januvia)
Sazeglipitin (Onglyza)
Linagliptin (Tradjenta)
Alogliptin (Nesina)
Linagliptin
Special note
Tradjenta
No need to dose adjust for liver or kidney disease
DPP-IV inhibitors
Benefits
Weight neutral
DPP-IV inhibitors
ADRs/
Less effective than GLP -1
Pancreatitis
Alterations in immunity
HA, dizziness
Hepatic inflammation
Skin lesions
MSK
Increase HF
DPP-IV inhibitors
Place in therapy
Can be first line, or more often used as add on
Lower A1c by 0.6-0.8%
SGLT2 - Inhibitors
MOA
Blocks reabsorption of glucose in the kidney and causes glucose removal in the urine
Limited by amnt of glucose filtered and osmotic diuresis
SGLT2 - Inhibitors
Benefits
Should not cause hypoglycemia
Promotes weight loss and lower blood pressure
SGLT2 - Inhibitors
Effectiveness
First line monotherapy
Lowers A1c by 0.5-0.7% (moderately effective)
SGLT2 - Inhibitors
Drug list
Canagliflozin (Invokana)
Dapagliflozin (Farxiga)
Empaglifozin (Jardiance)
SGLT2 - Inhibitors
ADRs
Increased risk of infection + delays recognition of DKA (this is a problem bc infxn can cause DKA)
Can contribute to orthostatic hypotension + bone loss (will fall often, and break a hip)
May cause AKI, has to be dose adjusted in CKD
Increased risk of lower extremity amputation (canagliflozin)
SGLT2 - Inhibitors
Special benefit of Empagliflozin
Lowers CV mortality !!
TZD/Glitazones
Drug choices
Pioglitazone (Actos)
Rosiglitazone (Avandia)
TZD/Glitazones
Effectiveness
Lower A1C by 0.5-1.4%
TZD/Glitazones
SE (many!)
Believed to be causing MI at one time (associated with higher risk of HF)
Lipid effects (Ros- increase LDL)
Piog- increased risk of HF
causes weight gain
Can cause bladder cancer
Increase risk of osteoporosis
TZD/Glitazones C/I
Patients w/NYHA class III or IV heart failure
Drugs in Meglitinides class
Repaglinide (Prandin)
Nateglinide (Starlix)
Meglitinides
Place in therapy
Diabetic patients who have allergies to sulfonylureas
Considerably more expensive with no real added benefit so really not used
Meglitinides
SE
May lead to CV events
Caution in liver dz
Risk of weight gain
CI in CKD
Alpha-glucosidase Inhibitors
MOA
Inhibits upper GI enzymes, so ingested polysaccharides are not converted to monosaccharides so decreased absorption in small intestine
Limits postprandial glucose excursions
Alpha-glucosidase Inhibitors
Drug lists
Acarbose (Precose)
Miglitol (Glyset)
Why are Alpha-glucosidase Inhibitors not used often
Can cause flatulence and diarrhea
Reduced efficacy (0.5-0.9%), high expense, and poor tolerance
Rapid acting insulin
Absorbed more quickly than regular following injection
Onset of action is 5-10 min, peak 45-75 min, duration 2-4 hrs
Carbs should be ingested first, take 20 min before meal
Types of rapid acting insulin
brand + generic
Insulin lispro (Humalog)
Insulin aspart (Novolog)
Insulin glulisine (Apidra)
Regular insulin - short acting
Pharmacokinetics
Onset of 30 minutes
Peaks at 2.5-5 hrs
Duration is 4-12 hrs
Regular insulin - short acting
Therapy use
Can be given as basal bonus for mealtime coverage (being replaced)
Main use is IV tx of DKA
