Updated: 10/1/2018

Immunosuppressive Drugs

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Snapshot
  • A 36-year-old woman presents to the emergency department with worsening weakness and decreased visual acuity of the right eye. She reports that her symptoms progressively worsened over the course of a week and after developing an upper respiratory infection. Medical history is significant for multiple sclerosis (MS) treated with rituximab. Physical examination is significant for 2/5 strength in the lower extremities and an afferent pupillary defect appreciated in the right eye. Magnetic resonance imaging of the brain and spine shows new enhancing lesions when compared to prior imaging. After further evaluation, it was determined she had an MS exacerbation. She is started on intravenous methylprednisolone.
Immunosuppressants
 
Immunosuppressants
Medication
Clinical Use
Mechanism of Action Adverse Effects
Cyclosporine
  • Rheumatoid arthritis
  • Psoriasis
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor which
    • impairs IL-2 production and release
    • impairs IL-2-induced T-cell activation
  • Nephrotoxicity 
  • Neurotoxicity
  • Hirsutism
  • Gingival hyperplasia
  • Hypertension
  • Hyperlipidemia
Tacrolimus (FK506) 
  • Transplant rejection prophylaxis
  • Calcineurin inhibitor via binding with intracellular FKBP-12 protein which
    • impairs IL-2 production and release
    • impairs IL-2-induced T-cell activation
  • Nephrotoxicity
  • Neurotoxicity
  • ↑ risk of diabetes
Sirolimus (Rapamycin)
  • Lymphangioleiomyomatosis
  • Renal transplantation prophylaxis
  • mTOR inhibitor via binding with intracellular FKBP-12 protein which
    • ↓ cytokine-induced T-cell proliferation
  • Pancytopenia
  • Hyperlipidemia
  • Edema
  • Insulin resistance
Basiliximab
  • Renal transplantation prophylaxis
  • Targets the α-chain of the IL-2 receptor complex which
    • is expressed on activated T-cells
  • Edema
  • Tremor
  • Hypertension
Azathioprine
  • Rheumatoid arthritis
  • Renal transplantation
  • Inflammatory bowel disease
  • A precursor of 6-mecaptopurine which
    • incorporates itself into the cell's DNA and
      • halts replication
  • Pancytopenia
Mycophenolate mofetil
  • Organ transplantation
  • Lupus nephritis
  • Inosine monophosphate dehydrogenase (IMPDH) inhibitor which 
    • impairs guanosine nucleotide synthesis
  • Gastrointestinal upset
  • Pancytopenia
  • Hypertension
Corticosteroids
  • A number of autoimmune and inflammatory disorders
  • NF-κB inhibitor
  • Induces T-cell apoptosis
  • Hyperglycemia
  • Osteoporosis
  • Cushing syndrome
  • Adrenocortical atrophy
  • Peptic ulcers
  • Cataracts
  • Avascular necrosis
  • Psychosis
 
 

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Questions (5)
Lab Values
Blood, Plasma, Serum Reference Range
ALT 8-20 U/L
Amylase, serum 25-125 U/L
AST 8-20 U/L
Bilirubin, serum (adult) Total // Direct 0.1-1.0 mg/dL // 0.0-0.3 mg/dL
Calcium, serum (Ca2+) 8.4-10.2 mg/dL
Cholesterol, serum Rec: < 200 mg/dL
Cortisol, serum 0800 h: 5-23 μg/dL //1600 h:
3-15 μg/dL
2000 h: ≤ 50% of 0800 h
Creatine kinase, serum Male: 25-90 U/L
Female: 10-70 U/L
Creatinine, serum 0.6-1.2 mg/dL
Electrolytes, serum  
Sodium (Na+) 136-145 mEq/L
Chloride (Cl-) 95-105 mEq/L
Potassium (K+) 3.5-5.0 mEq/L
Bicarbonate (HCO3-) 22-28 mEq/L
Magnesium (Mg2+) 1.5-2.0 mEq/L
Estriol, total, serum (in pregnancy)  
24-28 wks // 32-36 wks 30-170 ng/mL // 60-280 ng/mL
28-32 wk // 36-40 wks 40-220 ng/mL // 80-350 ng/mL
Ferritin, serum Male: 15-200 ng/mL
Female: 12-150 ng/mL
Follicle-stimulating hormone, serum/plasma Male: 4-25 mIU/mL
Female: premenopause: 4-30 mIU/mL
midcycle peak: 10-90 mIU/mL
postmenopause: 40-250
pH 7.35-7.45
PCO2 33-45 mmHg
PO2 75-105 mmHg
Glucose, serum Fasting: 70-110 mg/dL
2-h postprandial:<120 mg/dL
Growth hormone - arginine stimulation Fasting: <5 ng/mL
Provocative stimuli: > 7ng/mL
Immunoglobulins, serum  
IgA 76-390 mg/dL
IgE 0-380 IU/mL
IgG 650-1500 mg/dL
IgM 40-345 mg/dL
Iron 50-170 μg/dL
Lactate dehydrogenase, serum 45-90 U/L
Luteinizing hormone, serum/plasma Male: 6-23 mIU/mL
Female: follicular phase: 5-30 mIU/mL
midcycle: 75-150 mIU/mL
postmenopause 30-200 mIU/mL
Osmolality, serum 275-295 mOsmol/kd H2O
Parathyroid hormone, serume, N-terminal 230-630 pg/mL
Phosphatase (alkaline), serum (p-NPP at 30° C) 20-70 U/L
Phosphorus (inorganic), serum 3.0-4.5 mg/dL
Prolactin, serum (hPRL) < 20 ng/mL
Proteins, serum  
Total (recumbent) 6.0-7.8 g/dL
Albumin 3.5-5.5 g/dL
Globulin 2.3-3.5 g/dL
Thyroid-stimulating hormone, serum or plasma .5-5.0 μU/mL
Thyroidal iodine (123I) uptake 8%-30% of administered dose/24h
Thyroxine (T4), serum 5-12 μg/dL
Triglycerides, serum 35-160 mg/dL
Triiodothyronine (T3), serum (RIA) 115-190 ng/dL
Triiodothyronine (T3) resin uptake 25%-35%
Urea nitrogen, serum 7-18 mg/dL
Uric acid, serum 3.0-8.2 mg/dL
Hematologic Reference Range
Bleeding time 2-7 minutes
Erythrocyte count Male: 4.3-5.9 million/mm3
Female: 3.5-5.5 million mm3
Erythrocyte sedimentation rate (Westergren) Male: 0-15 mm/h
Female: 0-20 mm/h
Hematocrit Male: 41%-53%
Female: 36%-46%
Hemoglobin A1c ≤ 6 %
Hemoglobin, blood Male: 13.5-17.5 g/dL
Female: 12.0-16.0 g/dL
Hemoglobin, plasma 1-4 mg/dL
Leukocyte count and differential  
Leukocyte count 4,500-11,000/mm3
Segmented neutrophils 54%-62%
Bands 3%-5%
Eosinophils 1%-3%
Basophils 0%-0.75%
Lymphocytes 25%-33%
Monocytes 3%-7%
Mean corpuscular hemoglobin 25.4-34.6 pg/cell
Mean corpuscular hemoglobin concentration 31%-36% Hb/cell
Mean corpuscular volume 80-100 μm3
Partial thromboplastin time (activated) 25-40 seconds
Platelet count 150,000-400,000/mm3
Prothrombin time 11-15 seconds
Reticulocyte count 0.5%-1.5% of red cells
Thrombin time < 2 seconds deviation from control
Volume  
Plasma Male: 25-43 mL/kg
Female: 28-45 mL/kg
Red cell Male: 20-36 mL/kg
Female: 19-31 mL/kg
Cerebrospinal Fluid Reference Range
Cell count 0-5/mm3
Chloride 118-132 mEq/L
Gamma globulin 3%-12% total proteins
Glucose 40-70 mg/dL
Pressure 70-180 mm H2O
Proteins, total < 40 mg/dL
Sweat Reference Range
Chloride 0-35 mmol/L
Urine  
Calcium 100-300 mg/24 h
Chloride Varies with intake
Creatinine clearance Male: 97-137 mL/min
Female: 88-128 mL/min
Estriol, total (in pregnancy)  
30 wks 6-18 mg/24 h
35 wks 9-28 mg/24 h
40 wks 13-42 mg/24 h
17-Hydroxycorticosteroids Male: 3.0-10.0 mg/24 h
Female: 2.0-8.0 mg/24 h
17-Ketosteroids, total Male: 8-20 mg/24 h
Female: 6-15 mg/24 h
Osmolality 50-1400 mOsmol/kg H2O
Oxalate 8-40 μg/mL
Potassium Varies with diet
Proteins, total < 150 mg/24 h
Sodium Varies with diet
Uric acid Varies with diet
Body Mass Index (BMI) Adult: 19-25 kg/m2
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(M1.IM.59) A 31-year-old female receives a kidney transplant for autosomal dominant polycystic kidney disease (ADPKD). Three weeks later, the patient experiences acute, T-cell mediated rejection of the allograft and is given sirolimus. Which of the following are side effects of this medication? Review Topic

QID: 101013
1

Nephrotoxicity, hypertension

12%

(32/257)

2

Pancreatitis

7%

(18/257)

3

Hyperlipidemia, thrombocytopenia

55%

(141/257)

4

Cytokine release syndrome, hypersensitivity reaction

9%

(24/257)

5

Nephrotoxicity, gingival hyperplasia

13%

(33/257)

M1

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