Pharm 17 Immunopharmacology

Front 1

Antithymocyte Immunoglobulin
1) Drug Class
2) Mechanism of action
3) Uses
4) Adverse reaction

Back 1

1) Polyclonal Induction/Rescue drug
2) Equine or rabit Ig targeting T cell markers--> T cell clearance, modulation of activity, Fc receptor mediated opsonization and lysis
3) Host graft disease, prophylaxis for transplant, transplant rejection treatment, severe aplastic anemia
4) Infection, malignancy, anaphylaxis, CYTOKINE RELEASE SYNDROME!, leukopenia, thrombocytopenia

Front 2

OKT3: Orthoclone
1) Drug Class
2) Mechanism of action
3) Uses
4) Adverse reaction

Back 2

1) Monoclonal Induction/Rescue
2) Murine Ig (nonhuman) to CD3, opsonization and removal of CD3
3) Induction treatment
4) Cytokine release syndrome, anaphylaxis, malignancy, infection

Front 3

Basiliximab: Simulect
1) Drug Class
2) Mechanism of action
3) Uses
4) Adverse reaction
5) Advantages

Back 3

1) Monoclonal Induction/Rescue Agent (chimeric murine/human)
2) Binds and blocks IL-2 receptor
3) Induction
4) Only GI side effects, considered weaker with less side effects, good for Hep C patients
5) longer half life than OKT3

Front 4

Daclizumab: Zenapax
1) Drug Class
2) Mechanism of action
3) Uses
4) Adverse reaction
5) Advantages

Back 4

1) Monoclonal Induction/Rescue agent
2) Anti CD25 Ab binds IL-2 complex and prevents binding
3) Induction
4) GI symptoms, no malignancy/infection
5) 90% human --> less anaphylaxix/cytokine release syndrome, long half life

Front 5

Cyclosprine
1) Drug Class
2) Mechanism of action
3) Uses
4) Disadvantages

Back 5

1) Calcineurin inhibitor
2) Bind cyclophilin which inhibits calcineurin and thus IL-2 expression
3) Rescue, host graft, autoimmune
4) Dose response highly unpredictable--> constant monitoring

Front 6

Cyclosporine
1) Metabolism
2) Excretion
3) DDI
4) Adverse effects

Back 6

1) p450 in liver
2) Mostly bile, 6% renal, 0.1% unprocessed
3) p450 inducers- anticonvulsants
p450 inhibitors - cimetidine, grapefruit juice, antifungals, calcium channel blockers, sirolimus
4) Nephrotoxicity, infection, hypertension, TREMOR, seizures, hirsutism, gingival hyperplasia, nausea, vomiting, diarrhea

Front 7

Sandimmune
1) Drug class
2) Preparation
3) Digestions
4) Disadvantages

Back 7

1) calcineurin inhibitor, cyclosporine
2) in olive oil --> unpredictable F
3) Digestion dependent on bile emulsification
4) Monitoring necessary for same reasons as cyclosporine

Front 8

Neoral
1) Drug class
2) Preparation
3) Digestion
4) Advantages

Back 8

1) Calcineurin inhibitor, cyclosporine
2) Microemulsion
3) Not bile dependent, but forms micelles
4) F increased as well as predictability, Cmax, AUC and Tmax is decreased

Front 9

Tacrolimus: Prograf, FK
1) Drug class
2) Mechanism
3) Uses
4) Advantages over classmate
5) Metabolism
6) Side effects differing from classmate

Back 9

1) Anti calcineurin
2) Binds FKBPs--> calcineurin inhibition
3) Alternative to cyclosporine, induction, rescue, autoimmune
4) same survival rate, lower rejection rate
5) p4503A4
6) has rash, itching (pruritis) but no hirsutism, or gingival hyperplasia, still hyperglycemia, nephrotoxicity, GI tremors

Front 10

Anti calcineurin administrations
1) IV
2) Oral
a) cyclosporine, b) tacrolimus

Back 10

1. only indicated in those that can't tolerate oral b/c highly nephrotoxic (30% oral dose)
2. a) cyclosporine monitoring with sandimmune, not so much neoral
b) tacrolimus, highly variable, must monitor blood levels

Front 11

Axathioprine: Imuran
1) Drug class
2) Mechanism
3) Uses
4) Disadvantages

Back 11

1) Antimetabolite
2) nonspecific competitive inhibitor of de novo synthesis of guanosine nucleotides, targets T and B cells dependent on de novo synthesis
3) RENAL transplant prophylaxis, USED WITH CYCLOPORINE AND CORTICOSTEROID
4) Myelotoxic

Front 12

MMF: Myophenolate mofetil (CellCept)
1) Drug class
2) Mechanism
3) Uses
4) Advantages

Back 12

1) Antimetabolite
2) Blocks de novo purine synthesis via noncompetitive reversible binding
3) RENAL TRANSPLANT induction with cyclosporine and corticosteroids
4) not myelotoxic nor nephrotoxic

Front 13

MMF: CellCept
5) Adverse effects
6) Metabolism
7) DDI

Back 13

5) Diarrhea, gastrointestinal hemmorrhage, neutropenia plus the normal
6) Converted to active MPA in blood, then to inactive MPAG in liver and then stored in bile, has enterohepatic cycling with peak at 6-12 hrs after administration
7) Tubular secretion inhibitors

Front 14

Mycophenolic Acid: Myfortic
1) Drug class
2) Advantages?

Back 14

1) Antimetabolite in enteric coating
2) supposedly reduced GI side effects but active ingredient is still in tact so actually no advantage over MMF

Front 15

Sirolimus: Rappamune
1) Drug class
2) Mechanism
3) Uses
4) Metabolism and DDI
5) Adverse effects

Back 15

1) mTor inhibitor
2) Binds FKBP which inhibits mTor (regulatory kinase) which inhibits cytokine T cell proliferation (G1-->S)
3) RENAL transplant induction with cyclosporine and corticosteroids.
4) p450
5) Usual + DECREASED WOUND HEALING, THROMBOCYTOPENIA, hypercholesterolemia, hyperlipidemia

Front 16

Corticosteroids
1) Mechanism
2) Uses
3) Metabolism
4) Adverse effects
5) Dosing

Back 16

1) Inhibit IL-1 secretion
2) Induction/rescue
3) Prodrug, converted rapidly to prednisolone
4) STEROID PSYCHOSIS, hyperglycemia, PEPTIC ULCER
5) Differing doses for induction (highest), rejection (less), TREATMENT OF CYT RELEASE SYNDROME (lowest) (given 1hr prior to Ab therapy)