notes Flashcards
What endogenous steroid does fludrocortisone mimic?
aldosterone
what kind of activity does fludrocortisone have?
mineralocorticoid that balances water and electrolytes which keeps BP stable
fludrocorticoid is FDA approved for what?
Addison’s disease
what activity do other steroids like prednisone have?
glucocorticoid that is mostly anti-inflammatory
what is cushing’s syndrome?
it is the excess of cortisol production either from the adrenal gland production or high doses of exogenous steroids
what is the suppression of the hypothalamus-pituitary-adrenal axis (HPA)?
high doses of steroid can cause the adrenal gland to stop producing cortisol by feedback inhibition by suppression of the HPA axis
What is Addison’s disease?
when the adrenal gland is not producing enough cortisol
When stopping steroids, they must be tapered off, why?
to give time for adrenal glands to start producing cortisol
list glucocorticoids from least to most potent
cute & hot pharmacists & physicians marry together & deliver babies
cortisone 25 hydrocortisone 20 prednisone 5 prednisolone 5 methylprednisolone 4 triamcinolone 4 dexamethasone 0.75 betamethasone 0.6
dexamethasone brand
DexaPak 6, 10, 13 day
methylprednisolone brand
Medrol Medrol Therapy Pack A-Methapred SOLU-medrol Pack DEPO-medrol
prednisone brand
Prednisone Intensol
Deltasone
prednisolone brand
Millipred
Orapred ODT
Pediapred
Triamcinolone brand
Kenalog
When should steroids be taken to mimic the natural diurnal cortisol release?
between 7-8am
short term SE <1 month of glucocorticoids
mood lability insomnia indigestion bitter taste hyperglycemia hypertension increased appetite/ weight gain fluid retention
long term SE > 1 month
increased intraocular pressure
cushing-like symptoms (moon facies, buffalo hump, muscle wasting, weak bones, striae, acne, GI bleed, esophagitis, hypothyroidism, impaired wound healing, hirsutism, irregular menstruation)
what dose of prednisone constitutes as immunosuppressed?
> =2mg/kg/day or >=20mg/day of prednisone/prednisone equivalent for >2 weeks
How many days taper is the Medrol Therapy Pak?
6 days
What are the common symptoms of autoimmune disease?
fatigue, weakness, pain
strong immunosuppressants can reactivate what diseases?
Tb
hep B & C
What are main differences b/w RA and OA?
RA is bilateral and symmetrical
OA does not cause “prolonged stiffness”
What are some symptoms of RA?
bone deformity
pain
stiffness
joint swelling
which laboratory tests assist in RA diagnosis
anti-citrulinated peptide Ab (ACPA) rheumatoid factor (RF) - less specific
when should pts w/ RA be initiated on a DMARD?
when symptomatic regardless of disease severity
What is the RA txt goal?
disease remission or low disease activity
What is the preferred initial therapy for RA pts?
methotrexate
What is the drug treatment regimen for pts with moderate to high disease activity despite MTX (w/ or w/o steroids) ?
a combination of DMARDs, TNF inhibitor biologic or non-TNF biologic, w/ or w/o MTX
Do not use two biologic DMARDs in combination b/c of fatal risk of infection
What options are there for bridging to wait for DMARDs to take effect in RA?
low dose steroids (<10mg/day)
high dose NSAIDs
methotrexate brands
Trexall
Otrexup
Xatmap
Rasuvo
BW methotrexate
pregnancy
hepatotoxicity
mucositis/stomatitis
myelosuppression
CI methotrexate
pregnancy
SE methotrexate
alopecia photosensitivity N/V/D increasing LFTs stomatitis
When can folate be given when on methotrexate?
5mg PO weekly on the day following MTX
hydroxychloroquine brand
Plaquenil
warning Plaquenil
irreversible retinopathy and loss of vision acuity
caution in pts w/ G6PD deficiency
SE Plaquenil
N/V/D, abdominal pain, vision changes (dose-related), skin & hair color changes (rare), rash, pruritus, HA
What should be monitored in pts on Plaquenil?
eye exams
sulfasalazine brand
Azulfidine
warning sulfasalazine
caution in pts w/ G6PD deficiency
CI sulfasalazine
allergy to sulfa or salicylate
SE sulfasalazine
rash, HA, yellow-orange skin/urine
What should be given in addition to sulfasalazine and why?
folate 1mg/day
decreased folate absorption on sulfasalazine
leflunomide brand
Arava
warnings leflunomide
fetal-embryo toxicity
hepatotoxicity
CI leflunomide
hepatic impairment and pregnancy
What needs to be tested and how before using leflunomide?
must have negative pregnancy test and use 2 forms of birth control while on medication
how long does a pt have to wait to be pregnant after taking leflunomide?
2 years OR do an accelerated drug elimination procedure of cholestyramine or activated charcoal x 11 days
tofacitinib brand
Xeljanz
Xeljanz XR
what should Xeljanz not be used with?
do not use in combination w/ other biologic DMARDs
MOA tofacitinib
JAK enzymes inhibitor which stimulates immune cells
pharmacokinetics Xeljanz
avoid 3A4 inhibitors, inducers 2C19 inhibitor (IR only)
dose adjust Xeljanz
dose adjust IR only in moderate renal ior hepatic impairment
which pts should Xeljanz not be initiated?
ANC <1000
lymphocyte count < 500
Hgb < 9
DDI methotrexate
alcohol, increased hepatotoxicity
what is another name for anti-TNF biologics?
TNF-alpha inhibitors
Each anti-tNF inhibitor has its own what type of registry
pregnancy registry b/c of unknown risks to the fetus
which anti-tnf biologic DMARDs are available as IV?
infliximab (Remicade)
golimumab (Simponi Aria)
Which anti-TNF biologic DMARDs are available SC?
adalimumab (Humira)
etanercept (Enbrel)
golimumab (Simponi)
certolizumab pegol (Cinzia)
How often is etanercept administered?
once weekly SC
which anti-TNF inhibitor DMARDs require a filter and why?
infliximab (Remicade)
golimumab (Simponi Aria)
which anti-TNF inhibitor DMARD causes a infusion reaction?
infliximab (Remicade)
which anti-TNF inhibitor DMARD causes delayed hypersensitivity reaction? how far later?
infliximab (Remicade)
3-12 days after infusion
infliximab is compatibile with which solvent only?
NS only
BW for anti-TNF inhibitors?
serious infections, malignancies
CI infliximab
> 5mg/kg dose in mod-sev HF
CI etanecept
sepsis
CI in anti-TNF inhibitors
active systemic infections
warning TNF inhibitors
may cause demyelinating disease, HF, hepatotoxicity, serious infections, hep B reactivation, myelosuppression
how should TNF inhibitors be stored?
refrigerator
Humira and Enbrel can be stored at room temp x 14 days
when can anti-TNF biologics be used as initial therapy?
in severe disease presentation
where can Humira be injected?
SC in thigh, abdomen
where can Enbrel and Simponi be injected?
SC thigh, abdomen, upper arm
how is rituximab administered?
IV
MOA of rituximab
depletes CD20 B cells
warning rituximab
reactivation of hep B and C
infusion-elated reactions (premedicate w/ steroid, acetaminophen , anti-histamine)
anakinra brand
Kinemet
warnings anakinra
serious infection, malignancy, Tb reactivation
when is anakinra used?
reserved for after one or two DMARD failure
abatacept brand
Orencia
warning abatacept
serious infection
malignancy
Tb reactivation
COPD worseninig
what solvent is abatacept stable in?
NS only
tocilizumab brand
Actemra
when should Actemra not be used?
ANC < 2000, AST or ALT >1.5x ULN, platelets < 100,000
when should Kevzara not be used?
ANC < 2000, AST or ALT >1.5x ULN, platelets < 150,000
Kevzara generic
sarilumab
classic symptoms of SLE?
depression, fatigue, anorexia, weight loss, malar rash, muscle pain, photosensitivity
which manifestations of SLE lead to morbidity/mortality?
hematologic, neurologic, renal manifestations
arthritis and cutaneous manifestations are most common
what % of pts develop lupus nephritis?
50%
which drugs are most associated with drug-induce lupus erythematosus?
anti-TNF hydralazine isoniazid methimazole methyldopa minocycline procainamide propylthiouracil quinidine terbinafine
Annie Hall Is Merry Merry Mini Pretty Pie & Quite Tubby
What agents are used to treat SLE?
how long does it take these agents to work?
which one is the only ones FDA approved for SLE
NSAIDS (w/ PPIs), azathioprine, MMF, cyclosporine, cyclophosphamide, hydroxychlooquine, belimumab
6 months to work
belimumab, hydroxychloroquine
belimumab brand
BeLysta
belimumab MOA
IgG1 monoclonal antibody - prevent B lymphocyte survival
interferon beta agents in MS
Avonex Plegridy Betaseron Rebif Extavia Glatiramer acetate (Copaxone, Glatopa)
which interferon beta used in MS is pegylated? What is the difference of pegylation?
Plegridy
pegylated interferon allows for SC dosing q14 days
other agents are parenteral
what MS agents are oral?
teriflunomide (Aubagio)
dimethyl fumarate (Tecfidera)
fingolimod (Gilenya)
what is the dose of glatiramer acetate?
20mg daily SC OR 40mg TIW SC (spaced q48 hours)
SE glatiramer acetate
injection site reactions, pain, flushing, dyspnea, infection, diaphoresis
What is the preferred agent in MS patients who are pregnant?
glatiramer acetate (Copaxone, Glatopa)
MOA glatiramer acetate
immune modulator that suppresses T-lymphocytes
Which agents for MS are interferon beta-1a?
ROA and frequency?
Avonex IM weekly
Rebif SC TIW
which agents for MS are interferon beta-1b?
ROA and frequency?
Extavia SC every other day
Betaseron SC every other day
which agent for MS is peginterferon beta-1a?
ROA and frequency?
Plegridy SC q14 days
MOA of interferon beta products
enhances immune function by altering surface antigens
warnings interferon beta priducts
psychiatric disorders, increasing LFTs, injection site necrosis, thyroid disorders (hypo, hyper)
SE interferon beta products
flu-like symptoms (may premedicate)
which interferon beta products can be left at room temperature?
Betaseron
Extavia
which interferon beta products should not be shaken?
Avonex, Betaseron, Extavia
If refrigerated, what should you do with interferon beta products before injection?
bring to room temperature and DO NOT take out air bubbles b/c will lead to loss of medication
which oral immune modulator is contraindicated in pregnancy and severe hepatic impairment?
teriflunomide (Gilenya)
which oral immune modulator causes bradycardia?
How should the pt be monitored?
fingolimod (Aubagio)
monitor for 6 hours after initial administration
ECG baseline and after monitoring period
which immune modulator is contraindicated in pts w/ hx of CVD or stroke?
fingolimod (Aubagio)
which immune modulator should not be crushed, chewed, etc?
dimethyl fumarate (Tecfidera)
SE Aubagio
macular edema, hepatotoxicity, myelosuppression
which immune modulator should be cautious of in pts on HR lowering meds?
fingolimod (Aubagio)
which agent is a potassium channel blocker used in MS? What is it for?
dalfampiridine (Ampyra)
increase nerve conduction for walking
Ampyra contrauindication
hx of seizures
How long does it take for Ampyra to work?
6 weeks, most pts do not respond
What is the mAb that binds to the alpha-4 subunit of integrins on surface of leukocytes used in MS?
natalizumab (Tysabri)
which agent is a CD52 directed cytolytic mAb?
alemtuzumab (Letrada)
which agent targets CD20+ B cells?
ocrelizumab (Ocrevus)
which agent is an IL-2 antagonist?
daclizumab (Zinbryta)
which recombinant humanized mAb used in MS are IV?
Ocrevus and Letrada
CI Lemtrada
HIV pts because prolonged decrease in CD4 count
CI Zinbryta
hepatic disease
CI Ocrevus
active HepB disease
which recombinant humanized mAb used in MS require a REMs program? why?
Lemtrada, Zinbryta
serious, fatal autoimmune conditions, infections, malignancies
Zinbryta can cause autoimmune hepatitis
how do you monitor patients on daclizumab
LFTs at baseline, monthly for 6 months after last dose
When are recombinant humanized mAb indicated in MS?
after failure with 2 or more MS agents
what is the presentation of Raynaud’s phenomenon?
the fingertips turn white ten blue. Once it warms, it becomes red and swollen
What is the preferred agent used in Raynaud’s?
CCB - nifedipine
What is celiac disease?
It is an immune response to gluten found in wheat, barley and rye
What are the common symptoms of celiac disease?
abdominal pain, diarrhea, bloating, weight loss
constipation more in children
how can pharmacists check to see if excipients are gluten-free?
package insert to see if it says it contains starch and if it specified whether or not if its corn, wheat, tapioca or potato. May need to call manufacturer.
What can be used to treat dry eye in Sjogren’s syndrome?
OTC artificial tears. If they dont work then
cyclosporine (Restasis) or lifitegrast (Xiidra).
What is the SE of Restasis
burning
what is the SE of Xiidra
unusual taste
dry mouth treatment agents
OTC salivary stimulation (xylitol, sugar free gum), antimicrobial mouthwashes, salivary substitutes. If these dont work then muscarinic agonistslike pilocarpine (Salagen) or cevimeline (Evoxac).
CI Salagen and Evoxac and why?
contraindicated in pts w/ uncontrolled asthma or narrow angle glaucoma b/c of cholinergic effects
what kind of agent is glycopyrrolate
anticholinergic agent used for excess salivation - check to see if there is inappropriate use causing dry mouth
What are the topical agents used to treat psoriasis?
tazarotene, anthralin, coal tar, steroids, calcipotriene
what is the biggest con of coal tar products?
very messy and stains clothes, bedding, etc
what are the systemic agents for psoriasis txt?
acitetin (Soriatane)
apremilast (Otezla)
when is acitretin (Soriatane) used?
in severe cases of psoriasis
SE of apremilast (Otezla)
diarrhea, weight loss
what are the IL-RA used in psoriasis txt?
ustekinumab (Stelara)
guselkumab (Tremfya)
brodalumab (Siliq)
which agents that are used to treat RA, must be given with methotrexate?
infliximab (Remicade)
golimumab (Simponi, Simponi Aria)
rituximab (Rituxan)
