B12 Immune Drugs: DMARDs And NSAIDs Flashcards
What is a DMARD?
Disease modifying anti-rheumatic drugs which are used to prevent the progression of rheumatoid arthritis and are typically anti-inflammatory or immunosuppressive agents. They are grouped into synthetic DMARDs and biologic DMARDs
What are the main DMARDS?
Chloroquinine
Azathriopine
Methotrexate
Sulphasalazine
How does chloroquine work?
It is a synthetic DMARD which inhibits the intracellular toll-like receptor 9, for recognition of foreign nuclei acids and self-nucleic acids.
NB: Cannot be given for acute porphyria. Side effects are rare but they include cardiomyopathy.
How does azathriopine work?
It is a DMARD which inhibits the purine synthesis of B and T cells, leading to bone marrow suppression and increased infection risk. Azathriopine can lead to acute pancreatitis.
How does Cyclophosphamide work?
It is a DMARD which at low doses, can cause apoptosis of regulatory T cells through alkylation during the cell cycle, creating DNA cross links. It also promotes the release of the anti-inflammatory cytokines IL-4 and IL-10.
How does Ciclosporin work?
It is a synthetic DMARD which inhibits calcineurin for the activation of NF-AT which upregulates T cell activation.
After administration, it causes transient hypertension and it can promote tumour growth.
How does Aurothiomalate work?
It is a synthetic DMAD, with an Intramuscular injection of liquid gold which inhibits prostaglandin synthesis. It increases the sensitivity of skin to sunlight.
How does sulphasalazine work?
It is a synthetic DMARD which inhibits cyclo-oxygenase and lipo-oxygenase enzymes to prevent production of inflammatory mediators. It can cause GI discomfort, diarrhoea and fever.
How does Prednisolone work?
It is a synthetic DMARD which is a glucocorticoid to reduce the transcription of pro-inflammatory mediators at low doses, and at higher doses, is immunosuppressive.
NB: Due to the structural simialrity to Cortisol, it can cause Cushing’s syndrome and fluid retention.
What is methotrexate?
A synthetic DMARD which inhibits adenosine deaminase to increase the availability of adenosine to act on adenosine receptors for anti-inflammatory effect.
NB: Should be avoided with ascites or effusion, because it indicates liver damage which affects drug elimination.
Which DMARD is given for mild Rheumatoid arthritis?
Chloroquinine
Which DMARD is given for moderate to severe Rheumatoid arthritis?
Methotrexate.
How does diclofenac work?
It is an NSAID which is a non-selective COX-inhibitor to reduce inflammatory mediator production, like prostaglandin and thromboxane.
What are important considerations for diclofenac use?
It should be avoided in cerebrovascular event because DIclofenac inhibits thromboxane for platelet aggregation. Avoid in asthma because prostaglandins cause diclofenac blocks prostaglandin, a transient bronchodilator.
Diclofenac causes peptic ulcers because it reduces prostaglandin production, which promotes gastric mucosa production. Low prostaglandins cause oedema because of reduced renal blood flow with less vasodilation of afferent arteriole.
What is Celecoxib?
Selective inhibitor of **COX-2 enzyme for downregulation of prostaglandins associated with inflammation. **
Should be avoided with GI bleeding or cerebrovascular event. Celecoxib can cause angina due to reduced vasodilation of blood vessels and it causes GI ulcers.
