Exam 3 Flashcards
Term? An unpleasant sensory and emotional experience associated with actual or potential damage
pain
three causes of acute pain?
disease, injury, or inflammation
onset of acute pain?
comes on suddenly
what two things often accompany acute pain?
anxiety or emotional distress
what is chronic pain believed to represent?
disease itself
what two types of factors greatly worsen chronic pain?
environmental and psychological factors
term? Persists over a long period of time and is resistant to most medical treatments
chronic pain
examples of acute pain?
MVA; broken bone
what is one of the most prevalent public health epidemics?
death involving prescription drug abuse
what type of opioids are most problematic re: death?
synthetic opioids
lack of knowledge among prescribers (re: opioids) involve what three topics?
addiction, dependence, and misuse
current pain management guidelines, risk management practices, research in pain management- these are what?
contributing factors to opioid misuse/issues
non-low back, musculoskeletal injuries- start with what?
topical NSAIDs with or without menthol gel
non-low back, musculoskeletal injuries- second recommendation?
oral NSAIDs +/- acetaminophen
non-low back, musculoskeletal injuries- third recommendation?
opioids including tramadol
whether or not to prescribe opioids for pain- which guidelines?
CDC
selecting opioids and determining dosages- which guidelines?
CDC
deciding duration of initial opioid prescription and determining follow up- which guidelines?
CDC
assessing risk and addressing potential harms of opioid use- which guidelines?
CDC
what methodology do CDC guidelines use?
GRADES framework
what is the most common source of chronic pain?
lower extremity pain
what is the second most common source of chronic pain?
back pain
2023 opioid guidelines- what are the four 1st line recommended classes of agents?
NSAIDs, anticonvulsants, acetaminophen, muscle relaxants
what are the three 1st line opioids for mild pain?
tramadol, codeine, hydrocodone
opioids used for mild to moderate pain?
hydrocodone or oxycodone
three opioids used for mild pain? 1st line
tramadol, codeine, hydrocodone
three opioids used for severe pain?
hydrocodone, oxycodone, morphine
three fundamental tenets of responsible opioid prescribing?
1- patient eval and selection 2- period review and monitoring 3- treatment plans
1- patient eval and selection 2- periodic review and monitoring 3- treatment plans (what are these?
fundamental tenets of responsible opioid prescribing
what are the seven components of comprehensive pain assessment?
1- pain condition; 2-general medical history; 3-previous treatments; 4- psychosocial history and eval; 5- substance use history and addiction screening; 6-sleep patterns; 7- functional assessment
two examples of opioid prescribing risk stratification tools?
opioid risk tool; SOAPP Version 1.0-14Q
a self-report screening tool designed for adult patients in primary care settings to assess risk for opioid abuse among pts with chronic pain
opioid risk tool
a tool for clinicians designed to determine how much monitoring a patient on long-term opioid therapy might need
SOAPP
urine drug testing- component of what?
responsible opioid prescribing
pain management agreement- component of what?
responsible opioid prescribing
establishing treatment goals- component of what?
responsible opioid prescribing
setting realistic treatment goals- component of what?
responsible opioid prescribing
WHAT is needed to prescribe opioids for chronic pain?
informed consent
what are the three types of opioids?
natural, semisynthetic, or synthetic
absence of pain?
analgesia
what do opioid analgesics provide?
absence of pain without resulting in loss of consciousness/sleep
what are the two natural opioids?
morphine and codeine
what are the three semisynthetic opioid derivatives?
oxycodone, hydromorphone, and oxymorphone
what are the two categories of synthetic opioids?
phenylpiperidines and pseudopiperidine
what are the two phenylpiperidines?
meperidine and fentanyl
what is the example of the pseudopiperidine?
methadone
methadone- drug class?
pseudopiperidine (synthetic)
fentanyl- drug class?
phenylpiperidines (synthetic)
meperidine- drug class?
phenylpiperidines (synthetic)
oxycodone- type of opioid?
semisynthetic derivative
hydromorphone- type of opioid?
semisynthetic derivative
oxymorphone- type of opioid?
semisynthetic derivative
morphine- type of opioid?
natural
codeine- type of opioid?
natural
what are the three categories of opioid receptors?
mu, kappa, delta
what is the most important opioid receptor?
mu receptor
what receptor is responsible for most of the action of the opioids?
mu receptor
where is the mu 1 receptor located?
outside of the spinal cord
what receptor is responsible for central interpretation of pain?
mu 1
what is mu 1 receptor responsible for?
central interpretation of pain
where is the mu 2 receptor located?
throughout the CNS
what four things is mu 2 responsible for?
respiratory depression, spinal analgesia, physical dependence, euphoria
what receptor? Respiratory depression, spinal analgesia, physical dependence, euphoria
mu 2
what receptor is responsible for some of the side effects of opioid analgesia?
mu 2
which opioid receptors give modest analgesia?
kappa receptors
do kappa receptors affect respiratory depression? Yes/no
no
do kappa receptors pose risk of dependence? Yes/no
no
which opioid receptor causes dysphoric effects?
kappa receptors
term- sense of unease, anxiety
dysphoria
delta receptor agonists, show poor WHAT?
analgesia
do delta receptor agonists have addictive potential?
little addictive potential
delta agonists are used to minimize what?
some of the mu2 side effects
what drugs are used to minimize some of the mu 2 side effects?
delta agonists
morphine- drug class?
pure opioid agonist
codeine- drug class?
pure opioid agonist
buprenorphine- drug class?
mixed opioid agonist (mu)
nalaxone- drug class?
pure opioid antagonist
butorphanol- drug class?
mixed opioid agonist (kappa)
pentazocine- drug class?
mixed opioid agonist (kappa)
what opioid receptors decrease GI motility?
mu and kappa
by what three routes are opioid analgesics generally well-absorbed?
cutaneous, IM, and mucosal surfaces
where are the highest concentrations of opioid analgesics?
in the tissues
first pass effect of oral opioid analgesics?
fairly significant
highly lipophilic opioids concentrate where?
adipose tissue
what type of opioids are concentrated in adipose tissue?
highly lipophilic
what is a large reservoir of opioid analgesics?
skeletal muscle
what are two examples of highly lipophilic opioid analgesics?
fentanyl and codeine
what can cause prolonged analgesia in patients with compromised renal function?
morphine metabolites
renal excretion of opioid analgesics?
renally excreted unchanged
other than renal, route of excretion of opioid analgesics?
bile- minor amounts in enterohepatic circulation
what is another name for the descending aminergic pathways?
antinociceptive pathway
what class? Enhance activity in descending aminergic pathways that exert inhibitory effects on the processing of nociceptive information in the spinal cord
opioid analgesics
what pathway is affected with opioid analgesics?
descending aminergic pathways
what mechanism is closed with opioid analgesics?
close N-type voltage operated calcium channels
what type of channels are closed with opioid analgesics?
N-type voltage operated calcium channels
what type of channels are opened with opioid analgesics?
calcium dependent potassium channels
what is the results of changes to channels that happens with opioid analgesics?
hyperpolarization and reduction in neuronal excitability
what are the two components of pain?
affective and sensory
where does analgesia happen?
CNS
what component relates to pain unpleasantness?
affective
what component relates to pain intensity?
sensory
pain unpleasantness- term?
affective pain component
pain intensity- term?
sensory pain component
anxiolytic, pleasant- term?
euphoria
where does euphoria occur?
CNS
individuals not in pain may experience WHAT with opioid analgesics?
dysphoria
when might dysphoria occur in patients taking opioid analgesics?
if they are not in pain
what is a common consequence of opioid administration?
sedation
sedation with opioid use can result in what?
limited amnesia
describe sleep with opioid use?
patient can be easily awakened
describe sleep with opioid + sedative hypnotic?
deep sleep
what two opioids are likely to produce significant sleep?
synthetic morphine, oxycodone (less likely with fentanyl)
what is caused by inhibition of the brainstem respiratory center with opioids?
respiratory depression
what causes respiratory depression in opioids?
inhibition of the brainstem respiratory center
where is the respiratory center located?
brainstem
what are the two factors affecting opioid respiratory depression?
dose-related and influenced by sensory input
what patients can tolerate slight resp depression with opioids?
patients without prior respiratory problems
where is the cough center located?
medulla oblongata
what class of drugs suppresses cough center in medulla oblongata?
opioids
which specific opioid analgesic is the best at producing cough suppression?
codeine
class? Stimulate the brainstem chemoreceptor trigger zone
opioids
where is the chemoreceptor trigger zone?
brainstem
vestibular component may also be present with what?
opioid-related nausea and vomiting
effect of opioid on heart rhythm?
usually just mild bradycardia
what happens to PCO2 with opioid resp depression?
increased
what is the cerebral vascular effect of increased PCO2 with opioids?
cerebral vasodilation and increased blood flow
what effect do opioids have on ICP?
increased ICP
why do opioids have increased ICP?
respiratory depression and increased PCO2
increased or decreased PCO2 with opioids?
increased (resp depression)
what two mechanisms are involved with opioid-related constipation?
local and enteric CNS mechanisms
effects on stomach motility- opioids?
decreased
effect of opioids on stomach tone?
increased
effect of opioids on stomach acid production?
decreased
effect of opioids on tone of small intestine?
increased
effect of opioids on tone of large intestine?
increased
effect of opioids on biliary tract?
biliary smooth muscle contriction
effect of opioids on intestinal peristalsis?
diminished
effect of opioids on renal function?
depressed
effect of opioids on renal blood flow?
decreased
effect of opioids on bladder tone?
increased
effect of opioids on ureteral tone?
increased
where is the thermoregulatory center?
hypothalamus
what drugs alter the equilibrium point of the hypothalamic heat regulatory mechanisms?
opioids
what do opioids do to the hypothalamic heat regulatory mechanisms?
alter the equilibrium point
renal blood flow increased/decreased with opioids?
decreased
renal function increased/decreased with opioids?
decreased
bladder tone increased/decreased with opioids?
increased
ureteral tone increased/decreased with opioids?
increased
chills during opioid withdrawal likely related to what?
altered equilibrium of hypothalamus
effect of opioids on blood pressure?
hypotension
effect of opioids on ability to urinate?
urinary retention
cross tolerance can be seen among what?
different opioid agents
psychological dependence seen with what class?
opioid analgesics
what three situations can lead to opioid toxicity?
clinical overdosage, accidental overdosage in addicts, or suicide attempts
coma, pinpoint pupils, depressed respiratory status suggests what?
opioid toxicity
what three things suggest opioid toxicity?
coma, pinpoint pupils, respiratory depression
pupil appearance in opioid toxicity?
pinpoint
rhinorrhea and lacrimation- seen what withdrawal of what class?
opioids
hyper/hypoventilation seen in opioid withdrawal?
hyperventilation
HR changes in opioid withdrawal?
tachycardia
GI (3) sx seen in opioid withdrawal?
N/V/D
yawning- seen in what condition?
opioid withdrawal
skin appearance in opioid withdrawal?
piloerection
respiratory changes in opioid withdrawal?
hyperventilation
what does federal government have re: controlled substances?
dual imperative
what three things does a governmental system of controls prevent?
abuse, trafficking, diversion
abuse, trafficking, diversion are prevented by what?
government system of control
what are the two components of the federal government’s dual imperative?
establish a system of controls; ensure medical availability
ensuring medical availability of controlled substances is part of the government’s WHAT?
dual imperative
term- first enacted in 1970 to regulate the manufacture, importation, possession, use, and distribution of certain substances
Controlled Substances Act
when was the Controlled Substances Act enacted?
1970
who is responsible for interpreting and enforcing the CSA?
DEA
who has supporting responsibilities for CSA?
DHHS
DEA does what re: CSA?
interpreting and enforcing the CSA
what schedule- no currently acceptable medical use, high potential for abuse?
schedule 1
schedule 1 description?
no currently acceptable medical use, high potential for abuse
what schedule- high potential for abuse?
schedule 2
schedule 2- description?
high potential for abuse
what schedule- less abuse potential than schedule 2?
schedule 3
schedule 3- description?
less abuse potential than schedule 2
schedule 4 description?
less abuse potential relative to schedule 3
schedule 5 description?
low abuse potential relative to schedule 4
cocaine- schedule?
schedule 1
heroin- schedule?
schedule 1
two examples of schedule 1 drugs?
cocaine and heroin
when is cocaine used medically?
intractable epistaxis
pseudoephedrine- schedule in some states?
schedule 5
what label does not change medical value of medications?
“controlled substance”
efforts to prevent abuse must not interfere with what two things?
medical practice and patient care
healthcare providers must comply with what two types of regulations?
federal and state
which rule applies when federal and state regulations differ?
the more stringent rule applies
where do you find the federal regulations?
the Controlled Substances Act
where do you find the state regulations?
the state/licensing board/governing board
class? Biguanides
antidiabetic drugs
class? Sulfonylureas
antidiabetic drugs
class? Thiazolidinediones
antidiabetic drugs
class? Meglitinides
antidiabetic drugs
class? Selective sodium glucose cotransporter 2 inhibitors
antidiabetic drugs
class? Amylin agonists
antidiabetic drugs
class? Dipeptidyl peptidase-4 inhibitors
antidiabetic drugs
class? Glucagon-like peptide 1 receptor agonists
antidiabetic drugs
class? Dual-acting GLP1 and glucose-dependent insulinotropic polypeptide receptor agonists
antidiabetic drugs
biguanide drug?
metformin
specific class? Metformin
biguanide
other uses for metformin/biguanides?
metabolic-syndrome type disorders like PCOS
drugs used in PCOS?
metformin (biguanides)
does metformin address major patho processes of diabetes?
yes
effect of metformin on insulin sensitivity?
improved
effect of metformin on hepatic gluconeogenesis?
decreased
effect of metformin on absorption of glucose by intestines?
decreased
effect of metformin on weight?
weight-neutral or weight loss
effect of metformin on platelets?
inhibition of platelet aggregation
effect of metformin on triglycerides?
decreased
effect of metformin on HDL?
increased
effect of metformin on LDL?
decreased
what generally improves triglyceride levels in DM?
better glycemic control
when is metformin primarily used?
first line for DM
what are most prominent side effects with metformin?
GI
examples of GI side effects with Metformin?
bloating, nausea, and diarrhea
how should metformin be dosed?
start low and titrate slow
how to reduce side effects with metformin?
start low and titrate slow
deficiency of what can be caused by metformin?
vitamin B12
patients on metformin should be monitored for deficiency of what?
vitamin B12
rare but serious side effect with metformin?
lactic acidosis
what increases the risk for lactic acidosis with metformin?
comorbid conditions (renal dysfunction)
hypoglycemia with metformin?
rare (not an insulin secretagogue)
side effect of metformin re: liver?
hepatitis (Rare)
effect of metformin on TSH?
decreased TSH levels
when is thyroid function most likely to be altered with metformin?
first 6 months
what patients are at risk for decreased TSH with metformin?
those with abnormal thyroid function
possible life threatening side effect of metformin?
lactic acidosis
does metformin cause more insulin to be released from the pancreatic beta cells?
no
strategy to avoid adverse effects of metformin?
start low and titrate slow
why should metformin be used cautiously in older adult population?
liver and kidney dysfunction due to aging
why is severe renal dysfunction a contraindication for metformin?
increased risk for lactic acidosis
acute or chronic metabolic acidosis is a contraindication for what drug?
metformin (biguanides)
hypoperfusion of the kidneys increases risk of what with metformin?
lactic acidosis
patients with hypoxia are at increased risk for what with metformin?
lactic acidosis
alcoholics with severe liver dysfunction are at increased risk for what with metformin?
lactic acidosis
patients with liver dysfunction are at risk for what with metformin?
lactic acidosis
what may happen when IV contrast given with metformin?
renal dysfunction
can you give metformin if DKA?
no
two example drugs of sulfonylureas?
glyburide and glipizide
glyburide and glipizide drug class?
sulfonylurea
glyburide drug class?
sulfonylurea
glipizide drug class?
sulfonylurea
are sulfonylureas insulin secretagogues?
yes
can hypoglycemia occur with sulfonylureas?
yes
when is hypoglycemia most likely to occur with sulfonylureas?
especially with older generation drugs
hypoglycemia can be WHAT with sulfonylureas?
life-threatening
weight gain with sulfonylureas?
yes
how to minimize GI upset with sulfonylureas?
divide up the dose
what drug class may produce disulfram-like reaction with alcohol?
sulfonylureas
what causes disulfram like reaction with sulfonylureas?
alcohol
what is increased in disulfram reaction with sulfonylureas?
increased serum acetaldehyde
signs of disulfram reaction?
sweating, palpitations, flushing, N/V, vertigo, hypotension, tachycardia
signs of what? Sweating, palpitations, flusing, N/V, vertigo, hypotension, tachycardia
disulfram-like reaction (sulfonylureas + alcohol)
blood cell dyscrasias- what antidiabetic class?
sulfonylureas
what are signs of blood cell dyscrasias?
evidence of infections (WBCs), easy bruising/bleeding (platelets), fatigue/pallor (RBCs)
sulfonylureas- antidiuretic effects?
yes
why should patients report edema, weight gain, SOB with sulfonylureas?
antidiruetic effects
what is the exception to antidiuretic effects with sulfonylureas?
glyburide
glyburide does what to fluid balance?
mild diuresis
are sulfonylureas usually first line drugs?
no
what is an insulin secretagogue?
increases amount of insulin being released from the pancreas
why should we use newer generation sulfonylureas?
less risk of hypoglycemia
how should we divide doses of sulfonylureas?
divide into two doses
use of sulfonylureas with what may mask hypoglycemia?
alcohol
what type of risk is posed with long-term use of sulfonylureas?
cardiovascular risk
what drug should not be used in older patients as may mask hypoglycemia?
glyburide
what happens when sulfonylureas used in pregnancy?
risk for severe neonatal hypoglycemia
sulfonylureas in lactation?
no
sulfonylureas in pediatrics?
cautious use
sulfonylureas in type 1 DM?
no
oral drugs in DKA?
no
sulfonyulreas in severe hepatic dysfunction?
no
sulfonylureas in severe renal dysfunction?
no
sulfonyulreas in uncontrolled infection, burns, trauma?
no
sulfonylureas in patients that are unstable?
no- increased risk for hypoglycemia
what antidiabetic agent is preferred in pregnancy?
insulin
when are thiazolidinediones used?
type 2 diabetes
can TZDs be used alone?
yes
specific class? Pioglitzaone
thiazolidinediones
specific class? Rosiglitazone
thiazolidinediones
what effect do TZDs have in insulin resistance?
decreased
does insulin have to be present to decrease insulin resistance?
yes
how to TZDs decrease insulin resistance?
activation of the peroxisome proliferator-activated receptor gamma
peroxisome proliferator-activated receptor gamma- involved in what class?
thiazolidinediones
gene transcription is regulated so that proteins are produced in the cell that help insulin to act in the cell- what class?
thiazolidinediones
what is regulated in TZDs to help proteins be produced to allow insulin to act in the cell?
gene transcription
weight gain with TZDs?
yes
edema with TZDs?
yes (fluid volume expansion)
fluid volume expansion can be significant and progress to what with TZDs?
heart failure
why is there edema and potential HF with TZDs?
decreased urinary excretion of sodium and water
fluid volume expansion can be significant and progress to what with TZDs?
heart failure
why is there edema and potential HF with TZDs?
decreased urinary excretion of sodium and water
what causes plasma volume expansion with TZDs?
decreased urinary excretion of sodium and water
what happens to vascular permeability with TZDs?
increased vascular permeability
what does increased vascular permeability cause with TZDs?
edema
heart failure exacerbation- possible with what antidiabetic class?
thiazolidinediones
hypertension can be caused by what antidiabetic class?
thiazolidinediones
cholestatic hepatitis- adverse effect of what antidiabetic class?
thiazolidinediones
cholestatic hepatitis in TZDs- prevalence?
rare
hepatotoxicity in TZDs- prevalence?
rare
macular edema- what antidiabetic class?
thiazolidinediones
what causes decrease in hemoglobin with TZDs?
increase in plasma volume
what is a marker for increased plasma volume with TZDs?
decreased hemoglobin
decreased hemoglobin- what antidiabetic class?
thiazolidinediones
effect of TZDs on liver function?
elevated LFTs; hepatotoxicity possible but is rare
patients taking what antidiabetics should monitor for edema and weight gain?
thiazolidinediones
what antidiabetic agent should be used cautiously in HIV?
thiazolidinediones
what can happen if TZD taken on HAART?
increased cholesterol and triglyceride levels
increased cholesterol and triglyceride levels increase the risk for what? (antidiabetic context)
pancreatitis
macular edema is also a contraindication for what class?
thiazolidinediones
what antidiabetic class can cause ovulation?
thiazolidinediones
TZDs in pregnancy?
only if benefits clearly outweigh risks
TZDs in lactation?
avoid
NYHA class III or class IV- contraindication for what antidiabetic class?
thiazolidinediones
any volume overload situation- contraindication for what antidiabetic class?
thiazolidinediones
what antidiabetic class is contraindicated during an acute coronary event?
thiazolidinediones
what is the rule for ALT contraindications in TZDs?
ALT > 2.5x upper limit of normal
development of jaundice signals what?
hepatic injury
active bladder cancer or risk for bladder neoplasm- contraindication for what drug?
pioglitazone
class? Acarbose
alpha-glucosidase inhibitors
class? Miglitol
alpha-glucosidase inhibitors
two example drugs of alpha-glucosidase inhibitors?
acarbose and miglitol
acarbose and miglitol- class?
alpha-glucosidase inhibitors
where do alpha-glucosidase inhibitors act?
small bowel
what do AGIs compete with in the small bowel?
complex carbohydrates
class? Act in small bowel to compete with complex carbohydrates for digestion?
alpha-glucosidase inhibitors
where does induction of digestive enzyme occur with AGIs?
large intestine
what may patient experience over weeks to months when starting AGIs?
excessive flatus and abdominal bloating
when do AGIs lower blood glucose relative to meals?
postprandial lowering of blood glucose
effect of AGIs on A1c?
reduction over time
are AGIs insulin secretagogues?
no
what benefit can AGIs have if given with sulfonylureas?
mitigate the weight gain that tends to happen with sulfonylureas
what antidiabetic class can worsen underlying bowel disease?
alpha-glucosidase inhibitors
Chron disease or ulcerative colitis can be worsened by what antidiabetic class?
alpha-glucosidase inhibitors
why do patients often discontinue AGIs?
Gi side effects (diarrhea, abdominal pain, excessive gas, bloating)
what can minimize adverse effects of AGIs?
slow titration
when can hypoglycemia occur with AGIs?
if combined with other medications that cause hypoglycemia
are AGIs used for monotherapy?
no
when may adverse effects dissipate with AGIs?
first two weeks at same dose
when can adverse effects return with AGIs?
when a dose is increased
AGIs in pregnancy?
safety not established- avoid use
AGIs in lactation?
no
AGIs in children?
safety not established
AGIs in severe renal impairment?
no
what should be monitored with AGIs? (acarbose)
AST, ALT, renal function
AGIs in bowel disorders?
no
what antidiabetic class is contraindicated with use of any intestinal absorbents?
alpha-glucosidase inhibitors
what antidiabetic class is contraindicated with use of prescribed digestive enzymes?
alpha-glucosidase inhibitors
when should AGIs be taken?
first bite of a meal
what antidiabetic class should be taken with the first bite of a meal?
alpha-glucosidase inhibitors
what antidiabetic class is contraindicated with charcoal?
alpha-glucosidase inhibitors
intestinal adsorbents are contraindicated with what antidiabetic class?
alpha-glucosidase inhibitors
are meglitinides monotherapy?
usually not
indication for meglitinides?
type 2 diabetes
nateglinide- class?
meglitinides
repaglinide- class?
meglitinides
are meglitinides insulin secretagogues?
yes
can meglitinides cause hypoglycemia?
yes
meglitinides effect on postprandial glucose?
decrease
describe meglitinides effect on postprandial glucose?
proportional to the level of postprandial hyperglycemia
two examples of meglitinides?
nateglinide, repaglinide
nateglinide and repaglinide- class?
meglitinides
when should repaglinide be given?
30 minutes before meals
when should nateglinide be given?
1-30 minutes before meals
do insulin secretagogues work with minimal beta cell function?
no
severe hepatic impairment with meglitinides?
cautious use and adjustment
severe renal impairment with meglitinides?
cause use and adjustment
repaglinide should not be combined with what drug?
gemfibrozil
gemfibrozil should not be combined with what antidiabetic drug?
repaglinide
meglitinides- pregnancy?
safety not established- avoid use
meglitinides- lactation?
safety not established- avoid use
meglitinides- pediatrics?
safety not established- avoid use
combination of what two antidiabetic drugs has caused myocardial ischemia?
repaglinide and NPH insulin
SGLT2 inhibitors- stands for what?
selective sodium glucose co-transporter 2 inhibitors
SGLT2 inhibitors- indications?
type 2 diabetes as monotherapy or combination therapy
can SGLT2 inhibitors be used as monotherapy?
yes
canagliflozin- class?
selective sodium glucose co-transporter 2 inhibitors
empagliflozin- class?
selective sodium glucose co-transporter 2 inhibitors
dapagliflozin- class?
selective sodium glucose co-transporter 2 inhibitors
ertugliflozin- class?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class inhibits reabsorption of glucose in kidney proximal tubule?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class causes increased excretion of glucose in the urine?
selective sodium glucose co-transporter 2 inhibitors
where to SGLT2s work?
renal proximal tubule
how to SGLT2s lower blood glucose?
increased glucose excretion in the urine
what antidiabetic class can cause hypovolemia?
selective sodium glucose co-transporter 2 inhibitors
what causes hypovolemia with SGLT2 inhibitors?
osmotic diuresis
what antidiabetic class can cause genital fungal infections?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class can cause UTI?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class can cause intravascular volume depletion?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class can cause increased LDL cholesterol?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class can cause increased hemoglobin?
selective sodium glucose co-transporter 2 inhibitors
what is SGLT2 effect on hemoglobin?
increased
why can SLGT2 inhibitors increase hemoglobin?
intravascular volume contraction
what antidiabetic class poses a risk for DKA?
selective sodium glucose co-transporter 2 inhibitors
what two conditions may experience DKA with SGLT2 inhibitors?
type 1 and type 2 DM
what antidiabetic class can cause bone loss and fracture?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class can cause lower extremity infection?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class is associated with risk for amputation?
selective sodium glucose co-transporter 2 inhibitors
when can hypoglycemia happen with SGLT2 inhibitors?
when combined with insulin or insulin secretagogues
what class of drugs is used in HFrEF and diabetes?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic class should be used cautiously with osteoporosis?
selective sodium glucose co-transporter 2 inhibitors
what antidiabetic drug has a black box warning for risk for amputation?
canagliflozin
what antidiabetic drug should not be used with a history of amputation?
canagliflozin
SGLT2s- use in severe renal dysfunction?
contraindication
can SGLT2 inhibitors be used in DKA or type 1?
no
can SGLT2 inhibitors be used in DKA?
NO
can SGLT2 inhibitors be used in T1DM?
no
what are the risks with intravascular volume depletion in SGLT2 inhibitors?
syncope and falls
what should be monitored with SGLT2 inhibitors?
renal function, electrolytes, volume status
what antidiabetic drug is associated with increased risk for fractures?
canagliflozin
what electrolyte imbalance may occur with SGLT2 inhibitors?
hyperkalemia
what antidiabetic class may cause hyperkalemia?
selective sodium glucose co-transporter 2 inhibitors
antidiuretics and antihypertensives may worsen intravascular volume depletion with what drug class? (antidiabetics)
selective sodium glucose co-transporter 2 inhibitors
peripheral vascular disease is a contraindication for what antidiabetic drug?
canagliflozin
neuropathy is a contraindication for what antidiabetic drug?
canagliflozin
history of leg ulcers is a contraindication for what antidiabetic drug?
canagliflozin
history of leg infection is a contraindication for what antidiabetic drug?
canagliflozin
current leg ulcer or infection are contraindications for what antidiabetic drug?
canagliflozin
amylin agonists use in type 2 dm?
yes
amylin agonists use in type 1 dm?
yes
are amylin agonists first line therapy?
no
pramlintide- class?
amylin agonists
example drug of amylin agonists?
pramlintide
what effect does pramlintide have on gastric emptying?
delayed
how do amylin agonists affect weight?
possible weight loss
what does weight loss in DM accomplish?
improve insulin sensitivity
what is the black box warning with pramlintide?
severe hypoglycemia (esp in type 1 dm)
what effect do amylin agonists have on glucagon?
decreased glucagon secretion
what effect do amylin agonists have on appetite?
central inhibition of appetite
who is most at risk for severe hypoglycemia with amylin agonists?
type 1 diabetics
what are the GI adverse effects of amylin agonists?
nausea, vomiting, abdominal pain, decreased appetite
how to minimize GI adverse effects with amylin agonists?
gradually titrate to desired dosing
amylin synthetic analogue that acts like endogenous amylin- class?
amylin agonists
what antidiabetic class is contraindicated with gastroparesis?
amylin agonists
why are amylin agonists contraindicated with gastroparesis?
might worsen it due to delayed gastric emptying effects
what antidiabetic class is contraindicated in hx of severe hypoglycemia?
amylin agonists
what antidiabetic class should be avoided in noncompliance?
amylin agonists
why should amylin agonists be used cautiously in older adults?
may not be aware of hypoglycemia
amylin agonists- pregnancy?
safety not established- avoid use
amylin agonists- lactation?
safety not established- avoid use
what does DPP4 stand for?
dipeptidyl peptidase-4 inhibitors
another name for DPP4 inhibitors?
gliptins
when are DPP4 inhibitors used?
type 2 diabetes
sitagliptin- class?
dipeptidyl peptidase-4 inhibitors
saxagliptin- class?
dipeptidyl peptidase-4 inhibitors
linagliptin- class?
dipeptidyl peptidase-4 inhibitors
alogliptin- class?
dipeptidyl peptidase-4 inhibitors
what antidiabetic class slows the breakdown of GLP-1?
dipeptidyl peptidase-4 inhibitors
how do DPP4 inhibitors work?
slow the breakdown of GLP1
what is the benefit of slowing the breakdown of GLP1 with DPP4 inhibitors?
allow it to exert its effects longer
what does GLP1 do to gastric emptying?
slows
what does GLP1 do to glucagon secretion?
suppress
what does GLP1 do to beta cell mass?
increases
what does GLP1 do to insulin synthesis?
increases
what does GLP1 do to appetite?
decreased
joint pain- adverse effect of what antidiabetic class?
dipeptidyl peptidase-4 inhibitors
hypoglycemia with DPP4 inhibitors?
yes
urinary and respiratory tract infection- what antidiabetic class?
dipeptidyl peptidase-4 inhibitors
can you see weight loss with DPP4 inhibitors?
yes
can renal dysfunction occur with DPP4 inhibitors?
yes
what antidiabetic class can cause bulbous phemphgoid?
dipeptidyl peptidase-4 inhibitors
what antidiabetic class can cause SJS?
dipeptidyl peptidase-4 inhibitors
what antidiabetic class can cause heart failure?
dipeptidyl peptidase-4 inhibitors
what antidiabetic class can cause rhabdomyolysis?
dipeptidyl peptidase-4 inhibitors
lab monitoring with DPP4 inhibitors?
renal function, electrolytes, volume status
teach patients to monitor for signs of what with DPP4 inhibitors?
heart failure
DPP4 inhibitors- pregnancy?
safety not established- avoid use
DPP4 inhibitors- lactation?
safety not established- avoid use
DPP4 inhibitors- pediatrics?
safety not established- avoid use
can GLP1 agonists be used in type 1?
no
can GLP1 agonists be monotherapy?
yes
can GLP1 agonists be combination therapy?
yes
exenatide- class?
GLP1 receptor agonist
liraglutide- class?
GLP1 receptor agonist
lixisenatide- class?
GLP1 receptor agonist
dulaglutide- class?
GLP1 receptor agonist
semaglutide- class?
GLP1 receptor agonist
what class acts like endogenous GLP1?
GLP1 receptor agonist
effect of GLP1 agonists on insulin synthesis?
increased
effect of GLP1 agonists on beta cell mass?
increased
effect of GLP1 agonists on gastric emptying?
slowed
effect of GLP1 agonists on appetite?
decreased
effect of GLP1 agonists on triglycerides?
decreased
effect of GLP1 agonists on systolic blood pressure?
decreased
which antidiabetic class can reduce SBP?
GLP1 receptor agonist
effect of GLP1 agonists on glucagon secretion?
suppressed
GI adverse effects of GLP1 agonists?
nausea vomiting
GI adverse effects of GLP1 agonists? Improve or not
tend to resolve over time
diarrhea or constipation with GLP1 agonists?
diarrhea
gallbladder disease associated with which antidiabetic class?
GLP1 receptor agonist
biliary disease associated with which antidiabetic class?
GLP1 receptor agonist
pancreatic duct metaplasia associated with which antidiabetic class?
GLP1 receptor agonist
potential thyroid dysfunction and nodules- which antidiabetic class?
GLP1 receptor agonist
pancreatitis associated with which antidiabetic class?
GLP1 receptor agonist
elevated calcitonin levels associated with which antidiabetic class?
GLP1 receptor agonist
which antidiabetic class associated with acute kidney dysfunction/failure/injury?
GLP1 receptor agonist
immune thrombocytopenia associated with which antidiabetic drug?
exenatide
risk for hypoglycemia with GLP1 agonists?
small when used alone but only when combined with other drugs that cause hypoglycemia
exenatide has been associated with what?
immune thrombocytopenia
what antidiabetic class has been associated with thyroid cancer?
GLP1 receptor agonist
GLP1 agonist- route?
injection
how often to give GLP1 agonists?
once weekly
when might GLP1 agonists not be effective?
if not adequate GLP1 receptors in the gut (lost in DM)
when should GLP1 agonists be used?
in severe forms of GI disease- chrons or UC
history of pancreatitis is a contraindication for what antidiabetic drug class?
GLP1 receptor agonist
endocrine neoplasia is a contraindication for what antidiabetic drug class?
GLP1 receptor agonist
what antidiabetic class is associated with neuroendocrine tumor precautions?
GLP1 receptor agonist
lab monitoring with GLP1 agonists?
GLP1 receptor agonist
GLP1 agonist- pregnancy?
safety not established- avoid use
GLP1 agonist- lactation?
safety not established- avoid use
GLP1 agonists should not be used alongside what other antidiabetic drug class?
dipeptidyl peptidase-4 inhibitors
medullary thyroid dysfunction- contraindication for what antidiabetic drug class?
GLP1 receptor agonist
when should we monitor liver function with GLP1 agonists?
history of gallbladder or liver disease
can GLP1 agonists be used with metformin?
yes- consider clinical siguation
can you use GLP1 agonists with basal insulin?
yes- depending on clinical situation
tirzepatide- class?
dual acting GLP1 and glucose-dependent insulinotropic polypeptide receptor agonists
tirzepatide indications? 2
diabetes type 2 and weight management
tirzepatide, actions?
same as the GLP1 agonists alone
what must be present for GLP1 agonists and GIP dual agonists to work?
glucose
another name for HMG CoA reductase inhibitors?
statins
class- HMG CoA reductase inhibitors?
antilipidemics
class- cholesterol absorption inhibitors?
antilipidemics
class- bile acid sequestrants?
antilipidemics
class- fibric acid derivatives?
antilipidemics
class- niacin?
antilipidemics
class- proprotein convertase subtilisin/kexin type 9?
antilipidemics
class- bempedoic acid?
antilipidemics
what does PCSK9 stand for?
proprotein convertase subtilisin/kexin type 9
rosuvastatin- class?
statin
atorvastatin- class?
statin
two examples of statins?
rosuvastatin and atorvastatin
class? Competitively block HMG CoA reductase
statins
what is HMG CoA reductase?
an enzyme required in cholesterol synthesis in the liver
clinical uses of statins?
to decreases LDL and treat hyperlipidemia; includig hypertriglyceridemia
what three levels do statins lower?
total cholesterol, LDL, apo B lipoprotein
what other use do statins have?
prevention of atherosclerosis
what is the FDA warning with statins?
concerns re: statins causing DM and cognitive dysfunction (memory and concentration)
what are the manifestations of cognitive dysfunction caused by statins?
memory and concentration
GI side effects of statins?
nausea, vomiting, pain/dyspepsis, constipation/diarrhea, flatulence
what is the common muscular side effect of statins?
myalgia
what are the three muscular side effects of statins?
myalgia (common), myositis, rhabdomyolysis
what is the potentially life-threatening side effect of statins?
rhabdomyolysis (can injure the kidneys and be life-threatening)
characterize the risk of liver dysfunction with statins?
small- routine LFT testing not advised
fatigue and flu-like symptoms seen with which antilipidemics?
statins
statins in active liver disease?
contraindication
statins with heavy alcohol intake?
caution
statins with history of liver disease?
caution
statins in pregnancy?
most cases- absolutely contraindicated
statins in women planning to become pregnant?
do not prescribe
statins in lactation?
do not prescribe
ezetimibe- specific class?
cholesterol absorption inhibitor
can ezetimibe be used as monotherapy?
yes (for patients intolerant to statins)
can ezetimibe be used as an adjunct to statins?
yes
what cholesterol metrics does ezetimibe affect?
LDL (reduction)
what drug- inhibits the absorption of cholesterol at the brush border of the small intestine?
ezetimibe (cholesterol absorption inhibitor)
what sources of cholesterol are inhibited by ezetimibe?
dietary and biliary sources
where does ezetimibe inhibit cholesterol absorption?
brush border of the small intestine
what drug? Decreased delivery of intestinal cholesterol to the liver?
ezetimibe (cholesterol absorption inhibitor)
two significant adverse effects with ezetimibe?
acute liver injury; muscular- myalga, myopathy, rhabdomyolysis
ezetimibe in active liver disease?
contraindication
colestipol- specific class?
bile acid sequestrants
cholestyramine- specific class?
bile acid sequestrants
colestipol- broad class?
antilipidemics
cholestyramine- broad class?
antilipidemics
effect of bile acid sequestrants on LDL?
reduction
effect of bile acid sequestrants on HDL?
some increase
class? Chloride ions are exchanged with bile acids (negatively charged)
bile acid sequestrants
what effect do bile acid sequestrants have on bile acid?
more bile acid is excreted
class? Liver converts more cholesterol to bile acids along with an upregulation of LDL recptors on cell membranes
bile acid sequestrants
constipation that can lead to impaction- antilipidemic class?
bile acid sequestrants
folate deficiency seen in which antilipidemic class?
bile acid sequestrants
(rare) urine has an odor of something being burned? Antilipidemic class?
bile acid sequestrants
down or upregulation of LDL receptors on cell membranes with bile acid sequestrants?
upregulation
gemfibrozil- specific class?
fibric acid derivatives
fenofibrate- specific class?
fibric acid derivatives
gemfibrozil- general class?
antilipidemics
fenofibrate- general class?
antilipidemics
class? Act by causing an increase in lipolysis of triglycerides by using lipoprotein lipases
fibric acid derivatives
class? Decreases VLDL synthesis by the liver
fibric acid derivatives
what antilipidemic class is linked to gallstones?
fibric acid derivatives
what antilipidemic class is linked to decreased hemoglobin, HCT, WBC?
fibric acid derivatives
fibric acid derivatives- pregnancy?
avoid
class? Reduce hypertriglyceridemia with indirect elevation of HDL cholesterol d/t lowering of triglyceride levels
fibric acid derivatives
class? Assists to avoid pancreatitis in hypertriglyceridemia?
fibric acid derivatives
what antilipidemic drug is not longer favored?
niacin
what antilipidemic drug has been removed from guidelines for therapy?
niacin
what antilipidemic drug? No efficacy in decreasing cardiovascular endpoints and all-cause mortality
niacin
why has niacin been removed from guidelines?
no efficacy in decreasing cardiovascular endpoints and all-cause mortality
monoclonal antibodies- specific class?
PCSK9 inhibitors
monoclonal antibodies- broad class?
PCSK9 inhibitors
class? Reduction in LDL cholesterol usually in those with atherosclerotic cardiovascular disease or familial hypercholesterolemia
PCSK9 inhibitors
class? Alteration of an LDL transporter protein so that it transports more LDL to the liver to be used again
PCSK9 inhibitors
what is the overall effect of PCSK9 inhibitors?
more LDL removed from circulation
what do PCSK9 inhibitors do in the liver?
upregulation of LDL receptors in the liver
PCSK9 inhibitors- adverse effects?
usually well-tolerated
class? Mild injection site reactions- erythema, redness, mild swelling
PCSK9 inhibitors
reduction in LDL cholesterol in those with ASCVD (secondary prevention)?
bempedoic acid
class? Those with heterozygous familial hypercholesterolemia
bempedoic acid
class? An adenosine triphosphate-citrate lyase inhibitor that inhibits cholesterol production by the liver
bempedoic acid
adenosine triphosphate citrate lyase is involved in synthesis of what?
cholesterol
where does bempedoic acid work relative to statins?
before the HMG CoA reductase step that the statins inhibit
why does bempedoic acid lower LDL cholesterol?
because more LDL receptors are expressed
what antilipidemic class? Hyperuricemia and gout can occur
bempedoic acid
what antilipidemic class? Tendon rupture
bempedoic acid
is bempedoic acid first line therapy?
no
contraindications for bempedoic acid?
no known contraindications except precautions re: using in the setting of hyperuricemia and/or gout
what is preferred over natural pork-derived thyroid hormone?
synthetic levothyroxine
synthetic levothyroxine is preferred over what?
pork-derived thyroid hormone
synthetic levothyroxine acts like what?
body’s endogenous thyroid hormone
what results in increased metabolic rate in all tissues with concomitent increased O2 consumption?
thyroid hormone
effect of thyroid hormone on protein metabolism?
increased
effect of thyroid hormone on enzyme activity?
increased
effect of thyroid hormone on fat metabolism?
increased
effect of thyroid hormone on temperature?
increased
effect of thyroid hormone on HR?
increased
effect of thyroid hormone on respiratory rate?
increased
effective of thyroid hormone on growth, differentiation, and tissue maturation?
promotes
what is the cause of adverse effects with thyroid hormone therapy?
those of hyperthyroidism
HR with hyperthyroidism?
increased
respiratory rate with hyperthyroidism?
increased
gastrointestinal motility with hyperthyroidism?
increased
weight with hyperthyroidism?
weight loss
heat tolerance with hyperthyroidism?
heat intolerance
cardiac effects with hyperthyroidism?
chest pain, acute coronary syndromes, cardiac dysrhythmias
menstrual effects with hyperthyroidism?
menstrual alterations
what are the symptoms associated with increased GI motility with hyperthyroidism?
diarrhea and vomiting
what should patients be cautioned about with thyroid hormone?
signs and symptoms of both hypo/hyper thyroidism
what should patients be taught to monitor with thyroid hormone?
heart rate
what thyroid dysfunction is very important to treat in pregnancy?
hypothyroidism
what state may require higher doses of thyroid hormone?
pregnancy
why might there be an increased dosage need for thyroid hormone in pregnancy?
higher metabolic demand in pregnancy
thyroid hormone may exacerbate symptoms of what two conditions?
diabetes insipidus and adrenal insufficiency
what medication may precipitate adrenal crisis? (endocrine med)
thyroid hormone
how is adrenal crisis treated?
adrenocorticosteroids
what is the TSH goal for patients with osteoporosis?
upper limits of normal
what may happen to bone density with thyroid hormone therapy?
may decrease
what usually causes the bone density decrease with thyroid hormone therapy?
use of levothyroxine that causes subclinical hyperthyroidism
cautious use of thyroid hormone in what disease process?
cardiovascular disease, especially older adults
thyroid hormone should be avoided in acute WHAT?
acute coronary syndromes if possible
use of levothyroxine to treat what three things is inappropriate in absence of a diagnosis?
obesity, infertility, and depression
what effect does lithium have on the thyroid?
antithyroid
what two things can lithium do re: thyroid?
may cause a goiter and hypothyroidism
thyroid hormone replacement alongside what med may cause a goiter?
lithium
concern for hypo/hyperthyroidism with lithium + thyroid hormone?
hypothyroidism
in what three conditions may we try to suppress TSH?
thyroid cancer, nodules, euthyroid goiter
dosing of thyroid hormone for thyroid suppression therapy?
2.5 mcg/kg daily for 7 to 10 days
start at a lower/higher dose of levothyroxine than you would for hypothyroidism replacement?
higher
another name for for thionamides?
antithyroid drugs
when are thionamides used?
hyperthyroidism
two examples of antithyroid drugs?
propylthiouracil (PTU) and methimazole
what type of drugs are propylthiouracil and methimazole?
thionamides
what do thionamides do?
prevent the synthesis of thyroid hormones
what two drugs are used to prevent the synthesis of thyroid hormone?
propylthiouracil (PTU) and methimazole
effect of thionamides on preexisting thyroxine or triiodothyronine stored in thyroid gland?
not affected
effect of thionamides on exogenously administered levothyroxine levels?
not affected
how does propylthiouracil affect peripheral conversion of T4 to T3?
partial inhibition
agranulocytosis and possible aplastic anemia- can occur with what endocrine drugs?
thionamides
agranulocytosis and aplastic anemia with thionamides should prompt what?
discontinuation of the drug
liver abnormality possible with thionamides?
hepatitis
effect of thionamides on hair growth?
abnormal hair loss
does abnormal hair loss from thionamides resolve with d/c of the drug?
yes
what is the black box warning for propylthiouracil?
liver failure
what should I consult if pregnant patient requires thionamide?
nationally-recognized guidelines
what thionamide is preferrred in children?
methimazole
what three thyroid levels should be monitored with thionamides?
T4, T3, and TSH
why should we monitor a CBC after initiating a thionamide?
to monitor for agranulocytosis
under what circumstances should we monitor LFTs after starting a thionamide?
after initiation of therapy if there is evidence of s/s of liver disease and in those with hx of liver dysfunction
what type of foods should be avoided with thionamides?
iodine-containing foods
class? Replacement of pancreatic enzymes
exocrine pancreatic enzyme replacement therapy
what drugs act like the body’s endogenous pancreatic exocrine enzymes?
exocrine pancreatic enzyme replacement therapy
what is the purpose of exocrine pancreatic enzyme replacement therapy?
assistance with digestion of nutrients to maintain health
cystic fibrosis can result in what?
pancreatic exocrine enzyme deficiency
pancreatitis can result in deficiency of what?
exocrine pancreatic enzymes
