SLE Flashcards
Hydroxychloroquine
(Plaquenil)
MOA: Suppression of T-lymphocyte responses, Decreased leukocyte chemotaxis, Stabilization of lysosomal enzymes , Oxygen radical trapping
Dose: 200mg by mouth once - twice daily
Side effects/Counseling: Monitor vision (long term use)- regular eye exams; Blurry, difficulty focusing , changes in peripheral or night vision
Headache , dizziness, GI upset, dry skin
May take a few weeks-months (up to 3 month) to see effects!!
Pregnancy:
Safest option if therapy is needed
Mycophenolate mofetil/sodium
(CellCept ; Myfortic) Used for more moderate to severe decease
MOA: Inhibition of IMP dehydrogenase —> Decreased T-lymphocyte and B-lymphocyte proliferation
Dosing: 250mg to 2-3g per day in divided doses
Titration of dose is necessary to avoid intolerance (diarrhea=rate limiting step)
Take one hour before or two hours after food with a full glass of water
Side Effects: N/V/D, increased risk of infection, HA, elevated LFTs, peripheral edema, leukopenia, thrombocytopenia
Monitoring: CBC, serum electrolytes, liver enzymes, kidney function
Drug Interactions: PPIs!
Pregnancy: Risk Category D
Negative pregnancy test w/in 1 week of beginning therapy
Two forms of contraception 4 weeks before therapy, during therapy, and 6 weeks after cessation of therapy
Azathioprine
(Imuran)
MOA: blocking the synthesis of purine –> hinders DNA synthesis
*methyl-thioinosine monophosphate (MeTIMP) blocks amidophosphoribosyltransferase
*Thioguanosine triphosphate (TGTP) is incorporated into RNA.
*thiodeoxyguanosine triphosphate (TdGTP) is built into DNA.
Dosing: 1-2mg/kg daily
Drug Interactions!!!
Xanthine oxidase inhibitors (allopurinol/febuxostat), mesalamine, warfarin
Thiopurine methyltransferase (TPMT) deficiency
Side Effects/Counseling:
N/V/D, myalgia, leukopenia, thrombocytopenia (dose dependent), risk of infection, elevated hepatic enzymes and/or elevation of serum alkaline phosphatase and bilirubin
Signs of bleeding, sx of jaundice, change in color of stool
Pregnancy:
Avoid pregnancy, use contraception; **Can be used in pregnancy if SEVERE dx flare during pregnancy
cyclophosphamide
(Cytoxan)
Indications in SLE:
Lupus nephritis, pulmonary HTN
For very severe organ threatening decease – very toxic
MOA: Nitrogen mustard —> Suppresses T-cell and B-cell function
Dose:
Oral: 1-3mg/kg po daily (based on hematologic toxicity) in combo w/corticosteroids
IV: 0.5-1g/m2 monthly w/ dosage adjust. for hematologic toxicity & renal function
Give in combination with mesna to prevent interstitial cystitis
Side Effects:
Hair loss, nausea/vomiting, decreased appetite, stomatitis, amenorrhea, myalgias, nail discoloration, bladder toxicity (interstitial cystitis), infertility, oligospermia or azoospermia, Stevens-Johnson syndrome, increased risk of bladder cancer
Monitoring:
CBC, urinalysis (monthly if on IV therapy)
Pregnancy: Risk Category D
Teratogenic
Two forms of birth control are necessary (whether you are a men or a woman) during therapy, and 6 months after cessation
Counseling Points:
To avoid bladder toxicity, drink plenty of water (~1.5L/day) and empty bladder regularly and before bed. Avoid taking this medication at night
Watch for infections, increased bleeding or bruising, blood in the urine, a blistering skin rash, SOB
Rituximab
(Rituxan)
Reserved for patients resistant to other therapies
CD20 (B-cells, B-cell lymphomas)
Ab dependent cellular toxicity, complement dependent toxicity
Resistance - ↓ complement activation
↓ Ab dependent cellular toxicity
Toxicity - Infusion reactions
fever
neutropenia
Belimumab
(Benlysta)
Monoclonal antibody that binds to the B-lymphocyte stimulator (BLyS) inhibitor
1st drug approved for SLE in 50 years!
Approved March 8th, 2011
Indications in SLE:
Seropositive SLE in combination with “standard of care”
Dosing:
10mg/kg q 2weeks X 3 doses, then q 4weeks
Efficacy:
Based on data, patients with mild musculoskeletal and general malaise/fatigue may be best candidates for therapy
Safety:
Rates of serious infections not statistically significant
Leukopenia
Caution in patients with depression!
