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Which transplant medications are 3A4 substrates ? (3)
- 1. Tacrolimus (Prograf)
- 2. Cyclosporine (Sandimmune, Neoral, Gengraf)
- 3. Rapamycin (Rapamune)
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What are the 3 dosage formulations of Tacrolimus?
- IV (Prograf)
- PO (0.5, 1, 5mg caps)
- Topical (Protopic) - atopic dermatitis
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What should be monitored in usage of tacrolimus? (7)
- CMP -->
- 1. SCr (increase)
- 2. BG (increase)
- 3. K (increase)
- 4. CBC (increase WBC's, risk of infx)
- 5. BP (increase)
- 6. Lipids (inc'd chol)
- 7. TROUGH (5-20ng/ml)
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Counseling points with tacrolimus? (4)
- -With or w/o food (empty stomach for decreased variability)
- -May have stomachache and diarrhea
- -Fine hand tremor (will go away over time)
- -Hair loss, will resolve in ~6 months
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Conversion ratio of tacrolimus from IV to PO?
IV/PO - 1:3
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Dosage formulations of Mycophenolate (CellCept)? (3)
- IV
- 250, 500mg caps
- Oral susp (mixed, stable for 60d)
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Monitoring parameters for Mycophenolate? (7)
- 1. CBC (inc WBC) - weekly x1month, 2x/month xmonth 2-3, then monthly for 1st year
- 2. BP (inc)
- 3. Electrolytes (HypoMg, K, Ca; HyperK)
- 4. BG (inc)
- 5. Lipids (inc chol)
- 6. SCr and BUN (inc)
- 7. Pregnancy test (BBW)
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What are the rules for usage of mycophenolate in women of childbearing age? (3)
- -Must have negative pregnancy test
- -2 forms of contraception starting 4 weeks prior to tx
- -Contraceptives used during and for 6 weeks after d/cing med
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Counseling points for CellCept? (4)
- -Separate Ca supplements by 2 hours
- -Take on empty stomach
- -May have stomach upset and diarrhea
- -For women, must be on 2 contraceptives
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What are the dosage formulations of Cyclosporine (brand names)? (3)
- 1. IV (SandImmune only)
- 2. Caps (25, 50, 100mg) - all brands
- 3. Oral soln (100mg/ml) 50ml- all brands
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Stability of cyclosporine formulations?
- 1. IV - RT, ampules protected from light, stable for 6hr in PVC or 24hr in glass (POUR in glass)
- 2. Caps - RT
- 3. Soln - RT, use within 2 months and mixed in GLASS
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Monitoring parameters of cyclosporine? (4)
- 1. BP
- 2. SCr (inc)
- 3. Lipids (inc TG's)
- 4. Trough
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Counseling points of cyclosporine? (5)
- -With or w/o fd
- -May grow hair (hirsutism)
- -Gum hyperplasia
- -HA
- -N/D
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Bioavailability of cyclosporine products?
Neoral = Gengraf (MODIFIED = microemulsion) have increased bio availability
Sandimmune is non-modified. Not interchangeable with above
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