Week 7- DM/ Thyroid Flashcards
What drug is in the biguanide class
metformin (glucophage)
what MoA is metformin
Decrease hepatic glucose production by decreasing gluconeogenesis
Causes an increase in peripheral glucose uptake + utilization (sensitivity)
(Reduces glucose uptake in GI tract)
Does not stimulate insulin release
what are the common uses for metformin
first line DM medication, initial monotherapy for adults/kids
black box warning of metformin
BOX WARNING: Rare but life-threatening lactic acidosis, hypothermia, hypotension, bradycardia death (50% fatality)
side effects of metformin
gas, diarrhea, weight loss, DOES NOT DIRECTLY C/ HYPOGLYCEMIA.. but it can still happen
contraindications of metformin
advanced renal disease, metabolic acidosis, monitor renal function
drug interactions of metformin
avoid iodine-based contrast (hold 48 hrs before/after imaging), watch drugs that use renal excretion too
what drugs are in the DPP-4 inhibitor class
linagliptin, saxagliptin, sitagliptin
MoA of gliptans
Acts on incretin system- stimulate insulin secretion from pancreatic beta cells
Slow gastric emptying by prolonging action of GLP-1 hormones
common uses of gliptins
DM-2
OK monotherapy—
Typically adjunct
Overweight & DM-2
side effects of gliptins
Arthralgia
Pancreatitis
Skin autoimmune issues
Rhabdo
Heart failure
drug interactions of gliptins
ACEI, DM drugs, Quinilones, Protease inhibitors: Higher risk hypoglycemia
Dig
GLP-1 receptor agonist drugs
dulaglutitide, exenatide, liraglutide
MoA of GLP-1 “glutides”
Acts on incretin system- stimulate insulin secretion from pancreatic beta cells and decrease glucagon release from alpha cells
(increases insulin secretion, lowers glucose levels, delays gastric emptying, induces weight loss)
GLP-1 Receptor Agonists
Combo w/ other meds for poorly controlled type 2 DM
& Obesity + CVD
NOT FOR DM-1
CI for all GLP 1 Receptor Agonists
GI disease (UC, crohn’s, gastroparesis, pancreatitis
also not recommends for people with renal impairment
side effects of GLP-1 receptor agonists
GI distubrances, pancreatic duct metaplasia, pancreatitis, thyroid tumors
black box warning GLP 1 Receptor
Agonists
thyroid C-Cell tumors and hyperplasia BOX WARNING
which GLP 1 agonists has the most nausea
exenatide
Dulaglutide can increase or decrease CV events
Decrease CV events
DDI of GLP 1
Most drug interactions tied to delayed gastric emptying & dual therapy hypoglycemia
ASA, salicylates, fibrates, MAOIs, sulfonamides, ARBs and ACEIs, beta blockers, contraceptives, Dig
which GLP 1 has the highest propensity for increased INR with warfarin
exenatide
which drugs are SGLT2 inhibitors
canaglifozin, dapagliflozin, empaglifozin “flozins”
what is the mechanism of action of flozins/ SGLT2 inhibitors
Inhibits SGLT2: blocks reabsorption of glucose in the kidneys & promotes excretion of glucose
No effect on natural insulin secretion
monotherapy of flozins
DM-2 (can be monotherapy)
Can be renal protective in pts w/ new dx DM-2
Reduce HF Hospitalizations
side effects of flozins
Hypotension (from volume loss)
Most common: Genital fungal infections, UTIs and increased urination
Increase LDL
side effects of canaglifozin
monitor for new pain, sores, or ulcers in lower limbs (D/C)
flozin contraindications
Contraindicated in renal impairment, ESRD
what drugs are in the sulfonylurea gland
glimepiride, glipizide, glyburdie
sulfonylureas mechanism of action
Stimulate insulin release from panc beta cells, suppression of glucose from liver
Oral Hypoglycemic
(Must have some endogenous insulin secretion)
uses of sulfonylurea
DM-2
Typically combo meds + 2nd line therapy
side effects of sulfonylureas
Hypoglycemia: Avoid old ppl & High risk
Common: GI- N/D heartburn/ epigastric fullness.
Not for pregnancy: neonates born with severe hyperglycemia
Weight gain
SIADH
NeuroL Dizzy, nervous, HA, tremor
black box warning for sulfonylureas
Box Warning: Increased CV mortality (based on 1st gen study from 1970’s but applied to all)
which sulfonylurea has delayed absorption with food
Glipizide
what drug class is pioglitazone
PRODRUG- thiazolidinediones
how does pioglitazone work
Stimulating peroxisome proliferator-activated receptor gamma in cell nucleus
(this increases expression of proteins that improve insulin action)
(improves utilization of insulin on liver and muscle cells)
Depend on insulin for their action (so DM-2 only)
Reduce hepatic glucose production
Improve insulin sensitivity in DM-2
how is pioglitazone used
DM-2
Typically with 2-3 other drugs
(can be monotherapy)
side effects of pioglitazone
Weight gain
Edema
Serious: HF, elevated liver labs.
contraindications of pioglitazone
Contraindications: Heart failure
Monitor liver function
DDI with pioglitazones
CYP 450 inhibition
Do not use with contraceptives
Antiretrovirals: HLD
which insulin is rapid acting
lispro, aspart, glulisine
how does insulin work
binds to insulin receptors
how quick is insulin (rapid acting)
effect within 15 minutes
how is it usually given (rapid acting insulin)
premeal- immediate correction of hyperglycemia
what is regular/short acting insulin called
humulin
how is humulin usually given
Bolus to correct high
Meals
Effect within 30 min
DKA + HHS: infusion
Other: Hyperkalemia
Safe in pregnancy
IV/SC
how is NPH intermediate
Delayed onset by combining insulin with protamine
what are the timings of NPH
onset : 1-2 hrs
Duration 14-24 hrs
which insulins are long acting
glargine, detemir, insulin degludec
how do long acting insulins work differently than other insulins
Substituting glycine and arginine for other amino acids in human insulin
timing of long acting insulins
24 hrs– no true peak, DM 1 and DM 2
positive effects of long acting insulin
improved glycemic control w/ less variability
side effects of insulin
Both up and down life threatening
Too Much insulin or exercise or not enough food: Hypoglycemia
Too Little insulin: DKA
Other: Lipodystrophy from not rotating sites can lead to infection/ abcess
are different brands the same for insulin
no- not all brands are bioequivalent
DDIs of insulin
ETOH.. honestly many drug interactions– making them too high or too low
what drug class are synthyroid and levoxyl
levothyroxine
difference between the two meds
these drugs are basically the same, but have dif inactive ingredients
how does levothyroxine work
Synthetic hormone: providing your body with a man-made version of thyroxine (T4), a type of thyroid hormone
Most effects are exerted through control of DNA transcription and protein synthesis
common uses for levothyroxine
hypothyroidism
side effects of levothyroxine
Increased HR, decreased bone density, diarrhea, sweating, irritability, headache, SoB, heat intolerance
(Essentially mimic hyperthyroid symptoms)
contraindications of levothyroxine
CAD may worsen when thyroid hormones, people with recent MI should avoid
DDI of levothyroxine
Beta blockers, cholestyramine, digoxin, estrogens, glucocorticoids, iodides (like CONTRAST for scans!), DM medications, SSRIs, tricyclics and warfarin
cytomel class
Liothyronine T3
mechanism of action of cytomel
Triiodothyronine (T3) and L-thyroxine (T4) diffuse into the cell nucleus and bind to thyroid receptor proteins attached to DNA.
This hormone nuclear receptor complex activates gene transcription and synthesis of messenger RNA and cytoplasmic proteins
(Mimics normal physiology)
what are cytomel common uses
Mild hypothyroidism, congenital hypothyroidism, simple nontoxic goiter, myxedema
-Second line tx when synthroid/ Levoxyl doesn’t work
side effects of cytomel
Increased HR, decreased bone density Diarrhea, sweating, irritability, headache, SoB, heat intolerance
Teach patient how to measure pulse rate, and signs of OD, may experience hair loss
Cardiotoxicity risk: higher than synthroid
risk for older adults and cytomel
Older adults have higher risk of developing A. Fib w/ this medication
how are thyroid medications adjusted
Levels are monitored every 2-3 weeks throughout therapy, more often w/ adjustments and when starting… 2-4 weeks for adults, 4-8 weeks for older adults & CV risk ~low and slow~
signs of hyperthyroidism (med OD)
increased HR, cardiac arrhythmias, chest pain, tremors, nervousness, insomnia, irritability, diarrhea, vomiting, weight loss, menstrual irregularities, heat intolerance
what drugs are antithyroid agents
methimazole and propylthiouracil
mechanism of action of antithryoid agents
inhibit synthesis of thyroid hormones,
Partially inhibits conversion of T4 to T3
Don’t inactivate existing thyroxine Triiodothyronine
common uses for antithryoid agents
Adults & kids
Hyperthyroidism
(aka: Thyrotoxicosis)
Graves
Toxic goiter
side effects of anti-thyroid agents
Agranulocytosis (watch for sore throat, bleeding, bruising) , aplastic anemia
Drug-induced hepatitis, abnormal hair loss, drowsiness, nausea, skin rash, drug induced hepatitis
antithyroid agents notes/considerations
NO PREGNANT LADIES, levels are monitored every 2-3 weeks throughout therapy, more often w/ adjustments and when starting.. Also check WBC count
administration of anti-thyroid meds
Administration: taken every 8 hrs, dose missed? Take as soon as remembered
DDI for methimazole and PTU
Any bone marrow depression drugs, phenothiazines, potassium iodide, amiodarone, OTC cold meds that have iodine