Immunosuppression

Question 1

Tacrolimus

Answer 1

1. Calcineurin inhibitor, pgp inhibitor
2. Prev and tx of transplant rejection.
3. Dosage depends on type of transplant and immunosuppressive regimen. Adjust dose according to patient response and whole blood concentration.

Adult/child= initially 75-300microg/kg daily in 2 doses.

CR capsules
Adult/child= initially 75-300microg/kg OD mane.

Dose equivalence
The IV dose is approximately one-third of the oral dose.

4. TDM
   Nephrotoxicity= WATCH OUT tx w/other nephrotoxic agents (NSAIDs, aminoglycosides, iodinated contrast media)- additive nephrotoxicity; avoid combo.
   Neurotoxicity
   Drug interactions= before starting or stopping any medication
   Monitor any △ to the regimen carefully, with clinical assessment and TDM.
   Renal fn
   Liver fn
   BP
   Blood glucose conc
   Lipids
   Electrolytes (particularly K+)= WATCH OUT ACEI ↑K+
   Complete blood count
   regularly
   ECG= QT, cardiomyopathy, torsades de pointes.
5. • Take it consistently with regard to food. Best absorbed on an empty stomach, compliance may be improved if it is taken with a meal.
     - Take capsules at the same time each day and in the same way (always with food or always on an empty stomach).
     - Regular blood tests and blood pressure checks while taking this medicine.
     LABELS: 8, 18 12, 18, 21, A
     - Tell all HCPs you are taking this medicine and before starting any new medicines.

Diarrhoea, tremor, alopecia, hyperglycaemia and diabetes.
Neurotoxicity= Tremor and headache are most frequent; other effects include paraesthesia, confusion, seizures, coma, psychosis.

Question 2

Ciclosporin

Answer 2

1. Calcineurin inhibitor
2. Prev and tx of transplant rejection.
   Nephrotic syndrome.
   Severe RA unresponsive to other antirheumatics.
   Atopic dermatitis, severe refractory
   Psoriasis, severe refractory
3. Prev and tx of transplant rejection.
   Dosage depends on the type of transplant and immunosuppressive regimen.
   Adjust dose according to response and whole blood concentration.

Adult/child= initially 4-7.5mg/kg BD.

Dose equivalence
The IV dose is approximately one-third of the oral dose.

4. TDM= Conc monitoring is recommended in transplant patients. Look for signs of toxicity or tx failure.
   Monitor serum Cr and BP as it may be necessary to reduce the dose if they increase.
   Nephrotoxicity= WATCH OUT tx w/other nephrotoxic agents (NSAIDs, aminoglycosides, iodinated contrast media)- additive nephrotoxicity; avoid combo.
   Neurotoxicity
   Drug interactions= before starting or stopping any medication
   Monitor any △ to the regimen carefully, with clinical assessment and TDM.
   Renal fn
   Liver fn
   BP
   Blood glucose conc
   Lipids
   Electrolytes (particularly K+)= WATCH OUT ACEI ↑K+
   Complete blood count
   regularly

C/I= malignancy and uncontrolled hypertension for non-transplant indications.

5. • Regular blood tests and blood pressure checks while taking this medicine.
     LABELS: Capsule: 5, 8, 9, 18, 21, A; eye drop: 13; oral solution: 5, 7b (60 days), 8, 9, 18, 21
     - Tell all HCPs you are taking this medicine and before starting any new medicines.
     - Take capsules 12 hours apart at the same times each day.
     - Clean your teeth and gums regularly.

hypertension, dyslipidaemia, hirsutism and gingival hyperplasia.
Neurotoxicity= Tremor and headache are most frequent; other effects include paraesthesia, confusion, seizures, coma, psychosis.

leave capsule in foil- dont put in webster pack or use within 7 days.
never plastic container for liquid, only glass.

Question 3

Mycophenolate

Answer 3

1. Immunosuppressant
2. Prev and tx of organ and kidney transplant rejection >2y/o (mycophenolate mofetil).
   Prev of kidney transplant rejection in adults (mycophenolate sodium).
   Induction and maintenance of remission in lupus nephritis (mycophenolate sodium).
3. Dosage depends on type of transplant and immunosuppressive regimen. Adjust dose according to patient response and whole blood concentration.
   Mycophenolate mofetil: organ transplantation
   Oral/IV, 1-1.5g BD.
   Child >1 month= Max 1g BD.
   Kidney transplant, w/tacrolimus= 400mg/m2 BD.
   Kidney transplant, w/ciclosporin= 600mg/m2 BD.
   Liver transplant, w/tacrolimus/ciclosporin= initially 10mg/kg BD, ↑ to 20mg/kg BD.

Mycophenolate sodium: organ transplantation
Tabs contain mycophenolate sodium but the dose is expressed as mycophenolic acid.
720mg BD.

Dose equivalence= 720mg of mycophenolic acid is equivalent to 1g of mycophenolate mofetil.

4. TDM
   Complete blood count (including absolute neutrophil count= neutropenia) each week for 1 month, then twice each month for 2 months, then every 1–3 months.
   GI adverse effects: GI ulceration
5. give w/food, 2. give it 3-4 times daily, 3. switch from mycophenolate mofetil to mycophenolate sodium (may have some benefit), 4. ↓ dose (however, this may increase the risk of acute rejection and graft loss).
   Tx w/PPI=may ↓ absorption of mycophenolate mofetil.
   △ the brand a transplant pt is stabilised= monitor for signs of toxicity or tx failure and consider the possibility of an effect on any interacting drugs.
   Oral Abx= may interfere w/enterohepatic recirculation of mycophenolate potentially ↓ its conc and efficacy= monitor conc, particularly w/long course of abx.
   hazardous- not 1dt trimester preg
6. LABELS: A, 4a- AND PHOSPHATE BINDERS, 8
   Mycophenolate sodium= Always take tablets in the same way, either always with food or always without food.

• Tell dr if you get diarrhoea, signs of infection, or unusual bruising or bleeding.
• Take them 12 hours apart at the same times each day.
• Take with food if you need to prevent stomach upset.

Do not take antacids within two hours of this medicine as they may interfere with its absorption.

diarrhoea, nausea, vomiting, abdominal pain, abnormal liver function tests, infections, fatigue, headache, cough, leucopenia, neutropenia, anaemia, thrombocytopenia, pancytopenia.

Question 4

Azathioprine

Answer 4

1. Immunosuppressant= Purine antimetabolite.
2. Prev of organ transplant rejection.
   Immunosuppressant in:
   Severe RA
   IBD
   Autoimmune hepatitis
   SLE
   Pemphigus

3.
4.
5.