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which IBD type is increased Th1 (cell mediated/T-cell)?
crohn’s disease
which IBD type is increased Th2 (humoral)?
ulcerative colitis
what part of the GI does crohn’s affect?
any part (mostly ileum)
transmucosal
T/F: crohn’s is the continuous one
false - ulcerative colitis
can lifestyle changes (how you eat) help IBD?
yes
sulfasalazine (azulfidine) counseling
bone marrow suppression
needs folic acid
what is the active drug of sulfasalazine?
gut bacteria converts it mesalamine (5-ASA)
sulfasalazine MOA
decreased PG synthesis
decreased inflammatory cytokine production
T/F: purine analogs are the true anti-inflammatories
false - it’s aminosalicylates; the rest are immunosuppressants
purine analog drugs
azathioprine (imura)
6-mercaptopurine (purinethol)
how do purine analogs work?
decrease DNA synthesis → decrease T/B cell function
what happens with slow metabolizers that are taking a purine analog?
myelosuppression (absent TPMT → increased TG)
T/F: purine analogs are useful as anti-inflammatory
false - NO
purine analog DDI
allopurinol → reduce AZA-/6-MP dose to 1/4 to 1/3
what is the active component when describing purine analogs?
6 TG
T/F: 6-TU and 6-MMP are active
false - inactive
infliximab brand
remicade
adalimumab brand
humira
golimumab brand
simponi
certolizumab pegol brand
cimzia - PEG
T/F: ustekinumab (stelara) is not an anti-TNF
true
which monoclonal antibody has lower efficacy?
infliximab due to immunogenicity because it is chimeric (about 30% mouse derived)
can trigger anti-drug antibodies that increase drug clearance and reduce efficacy
mAb ADRs
injection-site/infusion (give benadryl or steroid)
reactivation of latent TB
increased risk of infection
cancer/lymphoma
which drug causes PML?
natalizumab
T/F: an ADR of anti-TNF is peripheral neuropathy
false - it’s an ADR of cyclosporine
T/F: cyclosporine has an ADR of HTN
true
what are the corticosteroids in IBD?
responsive (taper)
dependent (daily low dose → give prednisone)
non-responsive (switch to other drugs)
prednisone ADRs
HTN
osteoporosis
iatrogenic cushing syndrome
hypokalemia
infection
T/F: corticosteroids have ADRs of hypotension and hyperkalemia
false - HTN and hypokalemia
what does ustekinumab (stelara) act as?
IL 12/23 antagonist
what is stelara used for?
IBD
psoriatic arthritis
plaque psoriasis
what is stelara NOT used for?
RA
what do RA interleukins cover?
IL-17
IL-6
IL-1
what is long term effect of stelara?
cancer
what are the integrin receptor antagonists?
natalizumab (tysabri)
vedolizumab (entyvio)
how do integrin receptor antagonists work?
block lymphocytes from migrating into tissue
cyclosporine class
immunosuppressant
calcineurin inhibitor
cyclosporine MOA
binds cyclophilin → complex with calcineurin → NFAT not formed → decreased IL2 → decreased T/B cells
methotrexate low dose indication
IBD
how is methotrexate administered?
once weekly, PO
methotrexate MOA
inhibits AICAR transformylase (and TYMS) → increased adenosine → decreased IL2 → decreased inflammation
what is DHFR inhibition high dose used for?
cancer
JAK inhibitor
tofacitinib (xeljanz)
drug with -tinib acts as what?
kinase inhibitor
how is tofacitinib administered?
PO
what is tofacitinib used for?
RA
IBD
what are drugs that increase prolactin?
DA antagonists (antipsychotics, metoclopramide, prochlorperazine)
T/F: DA agonists do not raise PRL
true
what are the DA agonists?
bromocriptine
cabergoline
what is the effect of DA agonist?
decrease PRL release
decrease GH in acromegaly
what is the cheapest option but not most effect?
DA agonists
DA agonist ADR
orthostatic hypotension
who cannot benefit from bromocriptine?
patients with psychosis
cabergoline advantages over bromocriptine
more effective at decrease PRL and tumor size
restores gonadal function
long half life
high selectivity
better tolerated
dosed 1-2 per week
an except question, choose one thats not on the list
which DA is preferred in pregnancy?
bromocriptine, NOT cabergoline
acromegaly drug classes
GH antagonist (pegvisomant)
somatostatin analogs
DA agonists
somatostatin analog agents
octreotide
lanreotide
how do somatostatin analogs work?
inhibitory
decrease GH/IGF
decrease insulin/glucagon
SSA ADRs
diarrhea/GI discomfort
blood glucose - hyperglycemia in type 2 while hypoglycemia in type 1 (DM)
what are GH related agents?
somatropin (rhGH)
somatomedin (IGF)
T/F: somatostatin is not a GH related agent
true
somatropin ADRs
intracranial ADRs
insulin resistance/hyperglycemia
which growth hormone receptor antagonist used to treat acromegaly can cause hepatotoxicity?
pegvisomant
spironolactone class
aldosterone (mineralocorticoid receptor) antagonists
spironolactone indication
cushing syndrome
aldosteronism
hirsutism in women
HF
what does spironolactone NOT treat?
addison’s disease
aldosteronism treatment
spironolactone
eplerenone
amiloride
what drug is not used to treat with aldosteronism?
fludrocortisone - used for addison’s
which hormones are decreased in addison’s disease?
glucocorticoids
mineralocorticoids
sex steroids
signs of addison’s disease
fatigue
hyperpigmentation (high ACTH/MSH)
salt craving
hyperkalemia
low sodium
hypotension
dehydration
treatment for addison’s disease
glucocorticoid (hydrocortisone)
mineralocorticoid (fludrocortisone)
DHEA in women
what are some cholesterol derivatives?
glucocorticoids
mineralocorticoids
sex steroids (progesterone, estrogen, testosterone)
glucocorticoids ADRs
adrenal/growth suppression
HTN
hypokalemia
T/F: glucocorticoids can cause hyperkalemia
false - NO
what should be given as supplement when taking glucocorticoids?
potassium
calcium
vit d/c/b6
protein
cushing syndrome treatment
steroidogenesis inhibitors - metyrapone (metopirone), mitotane (lysodren), mifepristone (korlym)
ketoconazole/levoketoconazole (recorlev)
osilodrostat (isturisa)
which cushing syndrome treatment is only given in the hospital?
mitotane (lysodren)
mitotane class
adrenolytic
mitotane (lysodren) MOA
cellular destruction of adrenal cortex → adrenal cortex atrophy and decreased cortisol production
how is metyrapone classified?
steroidogenesis inhibitor, not adrenolytic
which neuromodulator works by decreasing ACTH in cushing syndrome?
cyproheptadine (periactin)
mifepristone (korlym) classification
antiprogesterone
glucocorticoid receptor antagonist
NOT steroidogenesis inhibitor
diseases/disorders related to pituitary
hyperprolactinemia
acromegaly
short stature
hypogonadism
diseases/disorders related to adrenal
cushing syndrome
aldosteronism
addison’s
CAH
how does CAH differ from addison’s?
androgens are high (decreased cortisol/aldosterone, increased androgens)
when is CAH diagnosed?
newborns
CAH treatment
glucocorticoid ± mineralocorticoid PRN
crinecerfont (crenessity) - for androgen control
how does crinecerfont work?
CRF-1 receptor antagonist → decreases androgens