Pharmacology of MOS Flashcards
What are the doses of low, medium and high dose Glucocorticoids
Low: 5-10 mg/d
Medium: 20-40 mg/d
High: 60 mg/d
MOA for Glucocorticoids
Regulation of transcription of certain genes; suppress macrophage activation, WBC trafficking and cytokine production
Side Effects of Glucocorticoids
Insomnia/Psychosis/Irritability Weight gain Hyperglycemia Cushing's Syndrome HTN Infection Osteoporosis Cataracts
What MUST you consider before placing a patient on Glucocorticoids
PPD testing
Review/Update immunizations
Calcium/Vitamin D supplementation
Antimalarial agent that can also be used as an anti-inflammatory; Inhibits TLR signaling, and thus cytokine production and WBC activity; used for SLE, RA and Sjogren syndrome; CONTRAINDICATED with retinopathy and G6PD deficiency
Hydroxychloroquine
Indications for Hydroxychloroquine
Malaria prophylaxis
SLE
RA
Sjogren Syndrome
Contraindications for Hydroxychloroquine
G6PD deficiency
Retinopathy
How does Hydroxychloroquine have anti-inflammatory effects?
Inhibit TLR signaling–> dec. cytokines and WBC activity
Dihydrofolate Reductase inhibitor used for inflammatory and autoimmune diseases; CONTRAINDICATED in Pregnancy or with Sulfamethoxazole
Methotrexate
MOA of Methotrexate
Dihydrofolate Reductase inhibitor -> interferes with DNA synthesis
Contraindications for Methotrexate
PREGNANCY
Sulfamethoxazole
____________ ___________ is administered prophylactically along with Methotrexate to prevent megaloblastic anemia and glossitis
Folic Acid
Side Effects of Methotrexate
Fatigue/Nausea Mucosal ulcerations Hepatotoxicity Bone Marrow toxicity Pneumonitis
*note that most involve rapidly dividing cells
Dihydroorate Dehydrogenase Inhibitor (no Orotate–> no de novo pyrimidine synthesis); used for arthritis and SLE; TERATOGEN
Leflunomide
MOA of Leflunomide
Dihydroorate Dehydrogenase inhibitor (no Orotate–> no de novo pyrimidine synthesis)
Side Effects of Leflunomide
Rash Alopecia Diarrhea Liver toxicity Bone marrow toxicity
*note most have rapidly dividing cells
Contraindications for Leflunomide
PREGNANCY
Immunosuppressant precursor of 6-mercaptopurine (inhibits Purine synthesis); used for SLE, Systemic Vasculitis and Inflammatory Myopathy; SAFE in pregnancy
Azathioprine
MOA of Azathioprine
Precursor to 6-mercaptopurine, which prevents conversion of PRPP to IMP/AMP/GMP
Side Effects of Azathioprine
Fever Rash Anaphylaxis Infection Bone marrow toxicity Hepatotoxicity Malignancy
Azathioprine is (safe/dangerous) in pregnancy
Pregnancy
Immunosuppressant that inhibits the conversion of IMP to GMP (Purine synthesis); indicated for SLE, Scleroderma, Vasculitis and Inflammatory Myopathy
Mycophenolate
MOA of Mycophenolate
Inhibit conversion of IMP to GMP (Purine synthesis)
Side Effects of Mycophenolate
Dyspepsia Diarrhea Abdominal pain Rash Infection Bone Marrow suppression Malignancy
Alkylating agent used for immunosuppression; used for Organ THREATENING complications, like SLE, Vasculitis, Lung Sclerosis, etc; can cause infection, bone marrow toxicity, infertility, hemorrhagic cystitis and bladder malignancy
Cyclophosphamide
Indications for Cyclophosphamide
ORGAN THREATENING complications (SLE, Vasculitis, Lung Sclerosis, etc.)
Side Effects of Cyclophosphamide
Infection Bone marrow toxicity Infertility Hemorrhagic cystitis Bladder malignancy
Examples of TNF-a inhibitors (5 total)
Etanercept Infliximab Adalimumab Certolizumab Golimumab
Indications for TNF-a inhibitors (Etanercept, Adalimumab, Infliximab, etc.)
RA
Psoriasis
IBD
TNF-a inhibitors can be used for SLE (True or False)
False; associated with worsening disease
Side Effects of TNF-a inhibitors (Etanercept, Adalimumab, Infliximab, etc.)
TB and Hepatitis B reactivation
NO LIVE VACCINES
_______ is involved with the inflammatory response and granuloma formation around Tuberculosis
TNF-a
Monoclonal antibody against B-cell CD20; causes B-cell depletion; indicated for RA, ANCA vasculitis (GPA and MPA) and other autoimmune diseases
Rituximab
MOA of Rituximab
Antibody against CD20–> depletes B cells
Side Effects of Rituximab
Infusion reactions HTN Arthralgias Serum Sickness PML Hepatitis B reactivation
Anti-IL-6 receptor antibody; indicated for Giant Cell (Temporal) Arteritis and RA
Tocilizumab
MOA for Tocilizumab
IL-6 receptor antibody
Side Effects of Tocilizumab
Infusion reaction
Cytopenias
Dyslipidemia
Antibody that blocks the activation of B cells (via B Lymphocyte Stimulator); used for SLE refractory to treatment
Belimumab
Purpose of Intravenous Ig for treating autoimmune diseases
Occupies and blocks Fc receptors, preventing immune-mediated phagocytosis and production of cytokines
Indications for IVIg
Kawasaki’s disease
ITP
SLE