Pharmacology Flashcards
Corticosteroids belong to what class of medications?
Interleukin 1 inhibitors
Which medications are calcineurin inhibitors?
2 items
- tacro
- cyclosporine
Which medications are antiproliferative agents?
2 items
- azathioprine
- mycophenolate mofetil
Which medications are mTOR inhibitors?
2 items
- sirolimus
- everolimus
Which medications are antibodies?
6 items
- Atgam
- thymoglobulin
- basilixamab
- rituximab
- alemtuzumab
- IVIG
Is ATG monoclonal or polyclonal?
polyclonal
What are the advantages of polyclonal induction agents?
2 items
- stronger
- can be used to treat rejection
What are disadvantages of polyclonal induction agents?
3 items
- common acute side effects
- higher infection (CMV) and malignancy rates
- potential to develop antibodies
Is basiliximab monoclonal or polyclonal?
monoclonal
What are advantages of monoclonal induction agents?
* 2 items
- no acute side effects
- not associated with infection and malignancy
What are disadvantages of monoclonal induction agents?
2 items
- weaker
- cannot be used for rejection
Why would a polyclonal antibody (ATG) be used intraoperatively?
to reduce delayed graft function
Why would a polyclonal antibody (ATG) be used for induction?
to prevent acute rejection
Why would a polyclonal antibody (ATG) be used for rescue?
to treat rejection
What are polyclonal antibodies mechanism of action?
2 items
- t-cell depletion
- cytotoxic activities
What side effects (related to lab values) can be attributed to polyclonal antibodies?
2 items
- leukopenia
- thrombocytopenia
What is the mechanism of action for CNIs?
inhibition of t-cell activiation
This leads to reduced circulating t-cell activators.
The adverse effect of nephrotoxicity for cyclosporine and tacrolimus is…
1. worse for tacro
2. the same
3. worse for cyclosporine
2
The adverse effects of neurotoxicity for cyclosporine and tacrolimus is…
1. worse for tacro
2. the same
3. worse for cyclosporine
1
Side effects include tremors, HA, parasthesias, PRES
The adverse effects of hematological changes for cyclosporine and tacrolimus is…
1. worse for tacro
2. the same
3. worse for cyclosporine
2
CNIs can cause what hematological adverse effects?
3 items
- HUS
- Thrombocytopenic Purpura
- Thrombocytopenia
The adverse effect of hyperlipidemia for cyclosporine and tacrolimus is…
1. worse for tacro
2. the same
3. worse for cyclosporine
3
The adverse effect of hyperglycemia for cyclosporine and tacrolimus is…
1. worse for tacro
2. the same
3. worse for cyclosporine
1
What is the most common side effect of CNIs?
HTN
What is the dermatological side effect of tacrolimus?
hair loss
What are the dermatological side effects of cyclosporine?
2 items
- hair growth
gingival hyperplasia
The gastrointestinal adverse effects for cyclosporine and tacrolimus are…
1. worse for tacro
2. the same
3. worse for cyclosporine
1
What GI adverse effects associated with cyclosporine?
5 items
- nausea
- vomiting
- anorexia
- bloating
- bad smell
Drugs/foods that increase tacro/cyclosporine levels include…
7 items
- antifungals (‘azole meds)
- metoclopramide
- grapefruit/pomegranate juice
- simepravir
- ‘mycin meds
- diltizame, verapamil
- amiodarone
Drugs/foods that decrease tacro/cyclosporine levels include…
10 items
- cholestyramine
- kayexalate
- ocreatide
- probucol
- Mg and Al antacids
- rifampin
- herbs
- nafcillin
- phenytoin
- phenobarbitol
mTOR inhibitors are structurally similar to what medication?
tacrolimus
What is the mechanism of action for mTOR inhibitors?
inhibiting t-cell activation and proliferation
When is sirolimus used?
3 items
- adjunct to prevent chronic rejection
- if intolerant of CNIs
- used for steroid-free protocols
When CNIs and sirolimus are used syngergistically, what does it allow for?
1. higher levels of CNIs and lower levels of sirolimus
2. lower levels of both CNIs and sirolimus
3. lower levels of CNIs and higher levels of siolimus
2
What is the loading dose, maintenance dose, and target trough level for sirolimus?
- 6-12 mg loading
- 2-5 mg maintenance
- trough level 6-12
What 3 hematological lab results may be caused by sirolimus?
- neutropenia
- thrombocytopenia
- leukopenia
The incidence of anemia is increased when sirolimus is used with what other medication?
1. tacro
2. steroids
3. mycophenolate
4. phenytoin
5. phenobarbitol
3
Sirolimus can cause which of the following?
1. hyperlipidemia and hypertriglyceridemia
2. hyperlipidemia and hypotriglyceridemia
3. hypolipidemia and hypertriglyceridemia
4. hypolipidemia and hypotriglyceridemia
1
Sirolimus may cause what in relation to its inhibition of cell and muscle proliferation?
delayed wound healing
How do nausea, vomiting, and diarrhea side effects compare between sirolimus and mycophenolate mofetil?
1. they are the same
2. worse in sirolimus
3. worse in mycophenolate mofetil
3
What side effects of the mouth can be caused by sirolimus?
mouth ulcers
What is the treatment for interstitial pneumonitis while on sirolimus?
discontinuation of drug
How does sirolimus affect a UA?
causes proteinuria
What are the 2 black box warnings for sirolimus?
- hepatic artery thrombosis liver patients
- bronchial anastomotic dehiscence lung transplant patients
What is everolimus used for?
prevention of rejection in low-mod risk renal transpant recipients
What 3 medications can everolimus be used with?
- basiliximab
- low dose cyclosporine
- corticosteroids
Everolimus is given at the same time as what other medication?
cyclosporine
What is the dosing for everolimus?
0.75 mg PO BID
What are the side effects of everolimus?
12 items
- hypercholesterolemia
- hypertriglyceridemia
- leukopenia
- anemia
- mouth ulcers
- acne
- impaired wound healing
- lymphocele
- proteinuria
- nephrotoxicity
- graft thrombosis
- rash
These are very similar to sirolimus
When is azathioprine used?
for those who don’t tolerate mycophenolate
What is the mechanism of action for azathioprine?
inhibits t-cell proliferation
What is the dosing for azathioprine?
1-3 mg/kg/day
What are the side effects of azathioprine?
9 items
- leukopenia
- thrombocytopenia
- nausea/vomiting
- macrocytic anemia
- alopecia
- pancreatitis
- hepatotoxicity
- malignancy
- infection
What drugs does azathioprine have an interaction with?
2 items
- allopurinol
- mycophenolate
Allopurinol: Switch to cellcept. Causes profound pancytopenia.
Mycophenolate: separate stopping and starting by 24 hours
What is the mechanism of action of mycophenolate mofetil?
Inhibits T and B cell proliferation
What delays mycophenolate absorption?
food
What are the side effects of mycophenolate?
7 items
- diarrhea
- nausea/vomiting
- anemia
- thrombocytopenia
- infections
- CMV tissue invasion
- malignancy
What are the mycophenolate drug interactions?
6 items
- ganciclovir, valgan…, acycl…
- cyclosporine
- sirolimus
- aza
- cholestyramine
- aluminum/mag containing antacids
Mycophenolate drug interactions ganciclovir, valganciclovir, acyclovir, and sirolimus may cause what?
increased risk of bone marrow suppression
The drug interaction between mycophenolate and cyclosporine may cause what?
decreased level of MPA
The drug interaction between mycophenolate and aza may cause what?
toxicity
24 hours between stopping one and starting another
The drug interaction between mycophenolate and cholestyramine may cause what?
decrease in mycophenolate levels
The drug interaction between mycophenolate and antacids may cause what?
decreased absorption
What is plasmapheresis?
The removal of circulating antibodies.
Does not affect b cells.
What is IVIG used for?
prevention and treatment of humoral rejection
What is rituximab used for?
2 items
- humoral rejection
- PTLD
What are the treatments for antibody mediated rejection?
6 items
- plasmapheresis
- IVIG
- rituximab
- antithymocyte globulin
- cyclophosphamide
- bortezomib
What medications are used to prevent PCP?
* 4 items
- sulfamethoxazole/trimethoprime
- pentamidine inhalation
- dapsone
- atovaquone
