SLE pharmacology

Topicals

Clinical pearls:
Low potency options should be used on the face in a short-term capacity only

Moderate strength are used on the body long term

Calcineurin inhibitors have no time limit for use on the face

NSAIDs

MOA: inhibit COX 1 and COX 2 enzymes decreasing the production of inflammatory mediators

Use: control mild to moderate symptoms of inflammation depending on patient response

BBW: Cardiovascular thrombolytic events and GI bleeding ulceration or perforation

ADR: Renal impairment, pulmonary hypertension, decreased hematology

Monitoring:

• electrolytes every 6 months

• BP every 12 months

Glucocorticoid’s

MOA: Decreases inflammation by suppression of migration leukocytes and reversal of increased capillary permeability

Use: Used to suppress immune response and therefore inflammatory response

ADR: CNS/behavioral effects, GI effects, Ocular effects

Monitoring: Adrenal insufficiency

Clinical Pearls:

• Lowest possible dose to control symptoms should be used

• For flares methylprednisolone pulse therapy (250-1000mg for 1-3 days) followed by an oral taper

• tapering:

  • If a patient’s disease is controlled but they’re taking more than 5 mg of prednisone per day, the goal is to gradually reduce (taper) the dose to below 5 mg and completely stop prednisone within 6 months.

  • If the patient can’t get off prednisone (down to 0 mg) without their disease flaring, then you should start or increase other immunosuppressive medications so the disease can be controlled without long-term steroid use.

Chloroquine(CQ)

Aralen

MOA: Inhibit Prostaglandin synthesis

Use: modulate the immune system and prevent activation of dendritic cells

Dose: Max dose 2.3mg/kg/day

ADR: Blue-grey skin pigmentation, hypoglycemia, abdominal cramp

Monitoring: CBC with diff at baseline

Azathioprine(AZA)

Imuran

MOA: Blocks purine synthesis

Dose: 2-3mg/kg/day in 2 divided doses
BBW: Malignancies in patients with inflammatory bowel disease

ADR: pancreatitis, liver toxicity, infections

Monitoring:

• CBC with diff

• LFTs

• SCR

Is safest drug for SLE in pregnancy

Methotrexate(MTX)

Trexall, Rheumatrex

MOA: Inhibit purine and thymidylic acid synthesis decreasing immune response

Dose: 20-25mg SubQ or oral once WEEKLY

BBW: embryo-fetal toxicity, bone marrow suppression, serious infections, toxicity(GI toxicity, hepatic toxicity, pulmonary), hypersensitivity, and dermatologic reactions

ADR: dermatological toxicity, diarrhea, increased liver enzymes

Monitoring: 

• CBC with diff

• LFT monthly for 3 months then every 3 months thereafter

Anakinra

Kineret

MOA: Antagonist of the interleukin-1 (IL-1) receptor.

Dose: 100mg SubQ or IV daily

Use: Adjunctive or alternative to immunosuppressants and used to lower steroid need

ADRS: Increase LFTs, hyperkalemia, hypernatremia

Monitoring:

• CBC every month ×3 months, then q3 months ×3 months, then q6 months ongoing

Anifrolumab

Saphnelo

MOA: IgG1-kappa monoclonal antibody that blocks the biologic activity of type 1 interferon receptors

Dose: 300mg IV infusion every 4 weeks

ADR: Antibody development, infection, hypersensitivity reactions

Pearls: Zoster vaccine prior to starting

Belimumab

Benlysta

MOA: IgG1 antibody; Decrease the ability for autoreactive B-cells to mature and cause damage

Dose:

• IV dosing: 10 mg/kg/dose q 2 weeks x 3 doses then q 4 weeks

• SC dosing: 200 mg week

ADR: Diarrhea, Nausea, Infections, PML

Monitor: Hypersensitivity and suicide ideation

Pearls: Takes 2-4 months to see results

Colchicine

Colcrys

MOA: inhibiting β-tubulin polymerization into microtubules;

• this prevents activation, degranulation, and migration of neutrophils

Dose: 0.6-1.2mg daily; decreased with 3A4/PgP inhibitors

ADR: GI effects, Myalgia

Monitor:

• Eye screening baseline then every 4-6 months

• EKG at baseline and as needed

Cyclophosphamide(CYC)

Frindovyx

MOA: prevents cell division by cross-linking
DNA strands and decreasing DNA synthesis.

Dose: 750mg-1000mg/m2 IV monthly for 6 months

ADR: Bone Marrow suppression, hepatotoxicity, pulmonary toxicity

Monitor:

• CBC and SCr qweek for 1 month then monthly

• Urine pregnancy test prior to each infusion

• Urinalysis every 6 months following course

Pearls:Can cause permeant infertility

Cyclosporine(CNI)

Gengraf, Neoral, Sandimmune

MOA: MOA: Inhibition of production and release of interleukin II

Dose: 3-5mg/kg/day by mouth in 2 divided doses

BBW: Hypertension, Nephrotoxicity, Immunosuppression

ADR: infections, diabetes, neurotoxicity

Monitor: 

• CBC & LFT monthly for 3 months then every 3 months.

• SCr, Potassium, Magnesium every 2 weeks for 3 months then monthly

• Lipid every 6 months.

Dapsone

Aczone

MOA: Inhibit neutrophil movement and the lack of the ability to initiate inflammatory processes

Use: refractory skin disease

Dose: 50mg daily (max 150mg) in 2 divided doses

ADR: Hypersensitivity reactions, hepatic effects, blood dyscrasias

Monitor: 

• CBC, LFT q week for 4 weeks—> 4 weeks for 3 months—>every 3 months. 

• G6PD testing before starting

Hydroxychloroquine(HCQ)

Plaquenil

MOA: Inhibits locomotion of neutrophils and chemotaxis of eosinophils; impairs complement-dependent antigen-antibody reactions.

Dose: 200-400mg /day in 2 divided dose start at 5mg/kg

ADR: QT prolongation, hypoglycemia, retinal toxicity

Monitor: 

• CBC, LFT, SCr at baseline and then as needed. 

• Eye screening at baseline then annually no later than 5 years after. 

• EKG at baseline then as needed

Pearls:  Typically first line for SLE

• Takes 2-4 months to see results

• Continue therapy even if remission is reached

IVIG

Use: used for patient with low platelet or RBC counts

Dose: 2g/kg given over 2-5 days consecutively monthly

BBW: Thrombosis and acute renal failure

ADR: Abdominal pain, chest pains, hypertension
Monitor: 

• CBC at baseline then monthly before infusion. 

• LFTs and chemistry panel prior to infusion

Lenalidomide

Revlimind

MOA: TNFa inhibitor

Dose: 5 mg every day PO

BBW: Embryo fetal toxicity, hematological, and VTEs

ADRs: hypokalemia, edema, rash

Monitoring:

• CBC, LFT, SCr, TSH at baseline then every month for 3 months

• Urine pregnancy test 2 weeks prior and before infusion adminstration, every week *4 weeks, then every 2-4 weeks, then 4 weeks after d/c treatment

Not really used due to risk; often for refractory cases

Leflunomide

Arava

MOA: inhibits pyrimidine synthesis

Dose: 10-20mg every day 

BBW: embryo-fetal toxicity, hepatotoxicity

ADR: Diarrhea, Infection, interstitial lung disease

Monitor:

•  CBC with diff, LFTs, SCr monthly for 3 months then every 3 months

Mycophenolate mofetil(MMF or MPAA)

Cellcept

MOA: T-cells become less responsive and therefore decrease immune response

Dose: 2-3g by mouth daily in 2 divided doses

BBW: Infections, embryo-fetal toxicity, malignancies

ADR: Edema, GI effects, hypertension

Monitor: 

• CBC every 2 weeks after each dose change then once stable once yearly.

• Urine Pregnancy screening 8-10 days after baseline and at subsequent visits

Obinutuzumab(anti-CD20)

Gazyva

MOA: Anti-CD20 medications that specifically cause cell death to B-cells that would be autoreactive

Dose: 1 gram IV on Day 1 and at weeks 2, 24, 26 and 52

BBW: Hepatitis reactivation, PML

ADR: Skin rash, hyperkalemia, hypernatremia

Monitor: 

• CBC with Diff at 3 months then every 6 months

• IgG levels assessed every 6 months

Rituximab(anti-CD20)

Rituxan

MOA: Anti-CD20 medications that specifically cause cell death to B-cells that would be autoreactive

Dose: 1 gram IV on Days 1 and 15

BBW: Infusion reactions, hepatitis b reactivation, PML, Mucocutaneous reactions

Monitor: 

• CBC with Diff at 3 months then every 6 months

• IgG levels assessed every 6 months

Tacrolimus(CNI)

Prograf

MOA: suppresses cellular immunity

BBW: Mortality in liver transplants, malignancies and serious infections

ADR: Diabetes, nephrotoxicity, neurotoxicity

Monitor: 

• CBC with Diff, LFT monthly for 3 months then every 3 months.

• Creatine potassium and magnesium every 2 weeks for 3months then monthly