Appendix 1
Common Disease Modifying Anti-Rheumatic Drugs used in treating autoimmune diseases (DMARD’s)
DRUG/PK/PD
TOXICITIES /SE TO
MONITOR
BASELINE MONITORING
ROS/ EXAM
LABORATORY/MONITORI
NG
Salilcylates, NSAIDs
PK: liver, CYP450:2C9
substrate
PD: Inhibits
cyclooxygenase, reducing
prostaglandin and
thromboxane synthesis
GI ulceration, Kidneys
CVD disease
CBC, Creatinine AST, ALT
Dark/black stool,
dyspepsia, abd. pain,
edema
CBC’s, LFT’s,
Creatinine q 6 months
Hydroxychloroquine
DOSE: 200mg BID
(or less than 6.5mg/kg per
day)
PK: Liver,
CYP450:unknown
Half-life 35-50 days
PD: Concentrates in acidic
cytoplasmic vesicles,
raises pH in lysosomes &B
may interfere with the
processing of autoantigenic peptides
Macular damage
GI upset
Photosensitive rash
Visual changes,
fundoscopy w/field of
vision
CBC, Creatinine
LFT’s, q 6 months with
Q 6 month to yearly
field of vision exam.
Usually take up to 3
months to
demonstrate any
positive effect
Azathioprine
DOSE: 50mg QD up to
2.0-2.5 mg/kg
PK: liver, erythrocytes,
CYP450. Half-life 5hr
PD: inhibits T lymphocytes
Myelosuppression, hepatic
toxicity, lymphoproliferative
disorders
Leucopenia
GI upset
Increases risk for shingles
Increase risk for infection
Hold if active infection
CBC, platelets, creatinine,
AST/ALT
May consider testing ofr
TMPT enzyme activity to
prevent toxicity
GI upset
Leucopenia
Decreased sperm count
CNS SE
CBC, LFT’s
Consider screen for G6PD
deficiency
Sulfasalazine
DOSE: 500mg QD up to
max of 3000mg/day
PK : GI tract, liver, CYP450
1
None, unless pt. is >40y/o
or hx of eye ds
Preg. B, D in 3rd trimester
Preg C
Symptoms of
myelosuppression
CBC, platelets,
creatinine, AST/ALT q
4 months, monitor for
infection
Allopurinol can
increase toxcitiy
Preg D
Rash, GI symptoms of
intolerance
CBC, LFT’s Q 8-12
weeks early on. Then
Appendix 1
Common Disease Modifying Anti-Rheumatic Drugs used in treating autoimmune diseases (DMARD’s)
DRUG/PK/PD
TOXICITIES /SE TO
MONITOR
Half-life 7.5 -14 hrs
PD: block cyclooxygenase
and inhibit prostaglandin
production to produce antiinflammatory effects
Fever, rash and elevated
LFT’s
Hold if active infection
Corticosteroids oral
DOSE: < or = to 10mg 30mg of prednisone or
equivalent QD. Should only
be used for flares and
bridging therapy
PK: liver, CYP450:3A4
substrate
Half-life varies on drug
PD: possibly inhibits
inflammatory cytokines
Hypertension,
hyperglycemia
Increases risk for shingles
Increases risk for infection
Increase risk for
osteoporosis
Increase risk for cataracts
Mood alteration
Weight gain
Adrenal insufficiency
B/P, CMP, DXA
Leflunomide
DOSE 10-20mg per day
PK: liver, GI tract, CYP450
Half life 15 -18 days
PD: inhibits pyimidine
synthesisvia dihydroorotate
dehydrogenase inhibition,
resulting in
immunomodulatory and
antiproliferative activity
Myelosuppression,
Increase risk for infection
Increase risk for shingles
Hold if active infection
Methotrexate
Oral or SQ
DOSE: titrated by
symtpoms and labs. Usual
start dose is 7.5mg to 10
Myelosuppression, hepatic
toxicity and/or fibrosis,
cirrhosis, pulmonary
infiltrates/fibrosis
Increase risk for infection
2
BASELINE MONITORING
ROS/ EXAM
LABORATORY/MONITORI
NG
Q 3 to 4 months
Preg B, trimester
specific
B/P, weight gain, SOB,
polyuria, polydipsia,
edema, visual changes
Urinalysis for glucose
yearly
Screening for Hep B & C
prior to start.
Symptoms of
myelosuppression
CBC, Creatinine, liver
enzymes every 8 to 12
weeks (q 2 months)
Preg X
CBC, Hepatitis B and C
serology, LFT;s albumin,
bilirubin and creatinine.
Chest Xray with in the last
year
Symptoms of
myelosuppression, SOB,
N/V, oral ulcers, hair loss.
CBC and platelet count
LFT’s, Creatinine and
albumin Q 8 weeks.
Monitor for infection
Preg X
Preg B
Appendix 1
Common Disease Modifying Anti-Rheumatic Drugs used in treating autoimmune diseases (DMARD’s)
DRUG/PK/PD
TOXICITIES /SE TO
MONITOR
BASELINE MONITORING
mg once weekly. Max is
25mg once weekly.
PK: liver, intracellular, GI
tract (oral); CYP450
Half life 3 -10 hrs based on
dose
PD: immunosuppressant:
inhibits dihydrofolate
reductase; inhibits
lymphocyte proliferation
(folate antagonist)
Increase risk for shingles
Daily supplement with folic
acid required
Hold if active infection
TB test
3
ROS/ EXAM
LABORATORY/MONITORI
NG
Appendix 1
BIOLOGICS
B and T cell modulators
DRUG/PK/PD
Abatacept
DOSE: IV dose is weight
based, q 4 weeks. SQ is
125mg SQ weekly
PK:CYP450:unknown
Half life: 13.1-14.3 days
PD:selectively
modulates T cell
activation, altering
immune response
Rituximab
DOSE: weight adjusted
PK:CYP450:unknown
Half life: 18-32 days
PD: binds to Blymphocyte CD20
surface antigens
4
TOXICITIES / SE TO
MONITOR
BASELINE
MONITORING
ROS/EXAM
LABORATORY /
MONITORING
S/S of immune
suppression
Hold if active infection
Hep B & C screen, TB
screen, immunization
status.
S/S of infection or
malignancy
CBC
Preg C
S/S of
immunesuppresion
Fatal PML
Serious/fatal infusion rxn
and/or mucocutaneous
rxn.
Hep B reactivation
Caution if malignancy
risk
Hold if active infection
Hep B & C screen, TB
screen, immunization
status
Pregnancy status, and
birth control measures
during tx and 12 months
after
S/S of infection or
malignancy
CBC
Preg C
Appendix 1
BIOLOGICS
TNF alpha Inhibitors
DRUG/PK/PD
Infliximab
Enteracept
Adalimumab
Golimumab
Certolizumab pergol
DOSE: Varies by drug
and route
PK: CYP450:none
PD: inhibits tumor
necrosis factor alpha,
reducing inflammation
and altering immune
response.
5
TOXICITIES / SE TO
MONITOR
S/S of immune
suppression
S/S of melanoma
Worsening CHF
Hold if active infection
BASELINE
MONITORING
Hep B & C screen, TB
screen, immunization
status.
ROS/EXAM
S/S of infection or
malignancy
Increased risk for
lymphoma and
melanoma
CHF
Drug induced lupus
LABORATORY /
MONITORING
CBC
Preg Cat.B