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Antidiabetic
N/A
17
Pharmacology
Undergraduate 4
11/07/2016

Additional Pharmacology Flashcards

 


 

Cards

Term
insulin lispro/humalog
Definition
rapid acting insulin
15-20 min onset
40-90 peak
3-5 hour duration
2-4 hour low
Term
regular insulin
Definition
regular acting - identical to endogenous
30-60 onset
80-120 peak
4-6 hour duration
3-7 hour low
Term
Neutral Protamine Hagedorn (NPH)
Definition
Intermediate acting insulin
2-4 hour onset
6-12 hour peak
14-16 hour duration
6-14 hour low
Term
insulin glargine
Definition
glargine was modified to have a higher iso-electric point vs human insulin- forms precipitant
2-3 hour onset
peakless
18-24 hour duration
3-4 hour low
Term
insulin detemir
Definition
detemir's B chain was modified to allow for binding to albumin, a depot like effect
1-2 hour onset
8-10 hour peak
14-24 hour duration
8-10 hour low
Term
U-500 insulin
Definition
Severe insulin resistance. Require large amounts of insulin. This is a VERY HIGH RISK DRUG. Don't recommend converting between 500 and 100 units/ml.
Term
metformin
Definition
biguanide
MOA - 1)inhibits glucose production in the liver
2)sensitizes insulin receptors in skeletal muscle (and fat)
3) minimally reduces glucose absorption in the gut
4) has minimal reduction in lipids (LDL/TGs)
Pharmacokinetics - renal elimination!
Indications - 1st line therapy/ drug of choice for DM2 and pre-diabetic patients "The Gold Standard"; gestational diabetes; PCOS
AE - Commonly associated with GI issues- N/D
Counter-act by taking with meals
Can also slowly titrate up to max dose (2550mg/day)
5% patients stop therapy due to this
BOXED WARNING: Lactic Acidosis- can accumulate in renal impairment, rare...but can be deadly!
Weight Neutral! NO HYPOGLYCEMIA
Dermatologic- Rash, Photosensitivity
Decreased B12 and folic acid absorption
DRUG-DRUG INTERACTIONS
Alcohol- both drugs prevent break down of lactic acid
IV radiocontrast - avoid metformin 48 hours after
Contraindications:
Heart Failure
renal impairment
Package insert: SCr>1.5 men, SCr>1.4 mg/dL women
New research has CrCl restrictions
What to monitor:
LFTs, SCr
HgbA1C, BG
Term
Lactic acidosis
Definition
Acidic state in the body, low pH
lactate > 5mmol/L
pH< 7.35
Medical Conditions:
Drugs that can cause this:
metformin (phenformin)
NRTI's
Ethanol (EtOH)
Term
glipizide
Definition
Sulfonylureas (2nd gen - 1st gen no longer used)
MOA - in pancreatic ß cells they inhibit potassium-ATP channels (retain K+)-> depolarizes cell->
Ca2+ influx-> stimulate insulin release
Pharmacokinetics - hepatic metabolism; renal excretion
Indications - Only for DM2; Take with Food!
AE - hypoglycemia- Take with Food!; weight gain; GI- N/V; teratogenic in animals; can cause hypoglycemia in infants; manufacturer recommends to stop 1 month prior to due date
Drug/Drug - Alcohol- disulfiram like reaction; Hypoglycemic Drugs; ß- blockers- mask s/s of hypo
Term
repaglinide
Definition
Meglitinide
MOA - same MOA as sulfonylureas, stimulate insulin release from pancreatic ß cells, but faster acting and shorter duration
Pharmacokinetics - rapid acting; short 1/2 life (1 hour)
Indications - DM2
AE - hypoglycemia- Take with Food!
miss a meal, miss a dose; weight gain; Upper respiratory infections/ Flu like symptoms (11%)
Term
pioglitazone
Definition
Thiazolidinediones (TZDs)
MOA - activates peroxisome proliferator activated receptor gamma (PPAR gamma)- changes gene expression in cells
1) decreased insulin resistance (sensitizing), resulting in increased glucose uptake- skeletal and adipose
2) increases LDL, HDL and lowers TG
Indications - only for DM2
AE -BOXED WARNING: Not for symptomatic heart failure (NYHA Class III and IV); hepatic failure/damage- elevated LFTs; fluid retention/edema (20+%); Ovulation- risk for unintended pregnancy in anovulating women; Bladder Cancer; Increased risk for bone fractures
Term
TZD history
Definition
Troglitazone- first one out on the market
high incidence of liver damage- some fatal
Rosiglitazone-
2007 NEJM meta-analysis found link to MI's
Senate hearing found drug company hid trial
Drug was put on restricted access
FDA restrictions now lifted as of 2013
Europe still has rosiglitazone off the market
Term
acarbose
Definition
alpha glucosidase Inhibitors
MOA - inhibits alpha glucosidase, an enzyme that breaks down complex carbohydrates (sucrose, lactose, maltose)
Pharm - short onset
Indications - DM2
AE - Diarrhea (30% of patients); Flatulence (74% of patients); Abdominal pain (19%); All the GI symptoms will reduce over time
Term
sitagliptin
Definition
Dipeptidyl peptidase-4 Inhibitors (DPP-IV)
MOA - Inhibit DPP-IV, delaying the breakdown of glucagon inhibitory peptide (GIP) and glucagon-like peptide (GLP) (incretin hormones)
Pharm - renal elimination
Indications - DM2
AE - FDA SPECIAL ALERT Aug 2015: This class of medications can cause joint pain that can be severe and disabling
post marketing reports of hypersensitivity reactions (SJS) pancreatitis
Term
canagliflozin
Definition
Sodium-Glucose Co-Transport 2 (SGLT-2) Inhibitors
MOA - Bind to SGLT-2 receptors in the kidney and prevents glucose reabsorption (increasing urinary glucose excretion)
pharm - renally eliminated
Indications - DM2
AE - FDA SPECIAL ALERT June 2015: This class of medications may lead to increased risk for
Diabetic Keto-Acidosis (DKA); Foot and Leg Amputations; Serious Urinary Tract infections (bacterial/fungal); Acute Kidney Injury; increased urine output, nocturia; hypotension
Term
Empagliflozin Trial
Definition
EMPA-REG OUTCOME trial- vs placebo, prevents CV death in 1 in 45 type 2 diabetics over 3 years and overall mortality in 1 in 39 patients
NO DIFFERENCE in MI or stroke
Causes genital yeast infections
1 in 14 women, 1 in 29 men
Linked to UTIs, hypotension and rarely ketoacidosis
Being hailed as the next metformin
“Class effect”?
Next trial results in 2017….
Term
Hyperkalemia
Definition
Drugs to use:
1) Regular Insulin
2) Kayexalate (sodium polysterene sulfonate)
3) New drug 10/21/15- Veltassa®(patiromer)
4) albuterol
5) sodium bicarbonate
6) furosemide
7) calcium
Advantages/Disadvantages to each?
Side Note: always check Magnesium level too
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