Immunosupressants Flashcards
Azathioprine
- Class
- MoA
- Side effects
- Interactions
- Monitoring
Class:
Anti-proliferative agents
MoA:
Anti-metabolite - broken down to 6 mercaptopurine by liver which blocks purine synthesis. Preferential inhibition of T cells over B cells.
Side effects:
Bone marrow suppression, hepatotoxicity, pancreatitis, increase of non-melanoma skin cancer risk
Interactions:
Allopurinol
Monitoring:
Must have TPMT checked prior to initiation.
Ciclosporin
Class:
Calcineurin inhibitor
MoA:
Prevents T cell proliferation via reduced IL-2 expression
Side effects:
Nephrotoxic, hepatotoxic, fluid retention, hypertension, neurotoxic, dysmorphism, gingival hypertrophy, hypertension, hyperkalemia, hypertrichosis, tremor, impaired glucose tolerance, hyperlipidemia
Extra info:
‘Virtually non-myelotoxic’. Cannabidiol may increase concentration.
Tacrolimus
- Class
- MoA
- Side effects
Class:
Calcineurin inhibitor
MoA:
Prevents T cell proliferation via reduced IL-2 expression
Side effects:
Nephrotoxic, neurotoxic, hypertension, diabetogenic, hypelipidemia
Methotrexate
- Class
- MoA
- Contraindications
- Side effects
Class:
Anti-proliferative
MoA:
Anti-folate which inhibits dihydrofolate reductase to decrease DNA synthesis.
Side effects:
Bone marrow suppression, infections, malignancy, teratogenic, pneumonitis, pulmonary fibrosis, liver fibrosis, folate deficiency, mucositis
Interactions:
Trimethoprim/co-trimoxazole, high dose aspirin
Extra info:
Both mother and father should be off methotrexate for 6 months prior to conception
Prednisolone
- Class
- MoA
- Side effects
- Extra info
Class:
Corticosteroid with predominantly gluocorticoid actions
MoA:
Inhibits phospholipase A2 (no breakdown of phospholipids to arachidonic acid means blocked prostaglandin synthesis)
Side effects:
Endocrine: impaired glucose regulation, increased appetite/weight gain, hirsutism, hyperlipidaemia, Cushing’s syndrome
Musculoskeletal: Osteoporosis, proximal myopathy, avascular necrosis of femoral head
Immunosuppressive
Psychiatric: Insomnia, mania, depression, psychosis
Gastrointestinal: Peptic ulceration, pancreatitis
Opthalmic: Glaucoma, cataracts
Suppression of growth
Intracranial hypertension
Neutrophilia
Extra info:
Patient cannot have live vaccines. Long-term patients hould double dose when sick.
Cyclophosphamide
Class:
Anti-proliferative
MoA:
Alkylates guanine causing cross linking and preventing cell replication. Affects B cells more than T cells.
Side effects:
Bone marrow suppression, hair loss, sterility, haemorrhagic cystitis, malignancy, pneumocystitis jiroveci, transitional cell carcinoma
Mycophenolate
- Class
- MoA
- Side effects
Class:
Anti-proliferative
MoA:
Anti-metabolite which inhibits IM PDH and prevents guanine synthesis. Affects T cells more than B cells.
Side effects:
Bone marrow suppression, ?progressive multifocal leukoencephalopathy (JC virus)
Rituximab
- Class
- MoA
- Side effects
- Extra info
Class: Monoclonal antibody
MoA: Anti-CD20 so leads to depletion of mature B cells
Side effects: Infusion reactions, exacerbation of cardiovascular disease
Extra info:
Screen for hepatitis B prior to use
Infliximab/adalimumab/etanercept
- Class
- MoA
- Side-effects
- Extra information
Class:
Monoclonal antibody
MoA:
Anti-TNF alpha
Side effects: Infusion reaction, infection, lupus-like conditions, demyelination, malignancy
Extra information:
Screen for TB prior to use
Denosumab
- Class
- MoA
- Contraindications
- Side effects
Class:
Monoclonal antibody
MoA:
Anti-RANK ligand - inhibits osteoclast differentiation and function
Contraindications: Hypocalcemia
Side effects: Injection site reaction, infection, avascular necrosis of jaw
Imantinib
- Class
- MoA
Class:
Monoclonal antibody
MoA:
Tyrosine kinase inhibitor
Trastuzumab
- Class
- MoA
Class:
Monoclonal antibody
MoA:
HER receptor
Bevacizumab
- Class
- MoA
Class:
Monoclonal antibody
MoA:
Anti VEGF