Arthritis Drugs Flashcards
Ibuprofen
Non selective cox inhibitor
First choice drug low side effects
Mechanism of action: unknown. It does however inhibit cox and enzyme involved in synthesis of PG at the arachidonic acid pathway.
SE:
Bronchospasm ( asthma)
Nausea, heart burn, headache, dizziness, mild rash.
Aspirin
Non selective cox inhibitor
Suppresses production of PG and thromboxane a2 (platelet agrevation) by irreversible inactivation of cox enzyme.
SE:
Nausea, rash bronchospasm, gi ulcer due to reduced mucous production.
Diclofenac
Reduced leukocyte migration and PG production due to cox inhibition.
Absorbed in the GI tract completely
Meloxicam
Works by reducing PG production.
Don not drink
Do not take aspirin alongside
SE: nausea, diarrhoea, rash, flu symptoms
GI bleeding, swelling, wheezing, heat attack.
Paracetamol
Not an NSAID. Does not reduce inflamAtion.
Overdose can cause fatal damage to liver detectable 24, 48 hours post overdose.
SE:
Nausea, fever.
Dark urine or jaundice get help !!
Prednisolone
Gluco corticoid receptor agonist.
Metabolised in the liver to active form. Crosses cell membrane and binds with high affinity to cytoplasmic receptors.
Inhibition of leukocyte infiltration and humoral response to inflammation.
SE: acne, dizziness, nausea, sleeplessness
Severe: similar to allergic reaction
Dexamethasone
Glucocorticoid agonist
Cross cell membrane and bind with high affinity to receptors.
Inhibit humoral response to inflammation.
SE: nausea, dizziness, rash, sever allergic reaction.
Fludrocortisone
Binds to mineralocorticoid receptor ( aldosterone).
Causes and increase in ion and water transport. Raising extra cellular fluid volume and lowering potassium levels.
SE:
Insomnia, acne, headaches, nausea.
Corticosteroids
Block gene transcription and synthesis of inflammatory proteins.
Immunosuppressant.
Gluco corticoids Naturally produced Metabolic effect Anti inflammatory Immunosuppressive
Mineralocorticoid
Water and electrolyte balance between
Natural steroids
Hydrocortisone/ corticosteroids
Show both MC +GC activities
Aldosterone
Mineralocorticoid only
Steroid duration of action
Short acting :
Cortisone / hydrocortisone
Intermediate acting :
Prednisolone
Long acting :
Dexamethasone
Glucocorticoid action in RA
Anti inflammatory immunosuppressant
Lower transcription of pro inflammatory cytokines (il-2)
Reduces circulating lymphocytes
Beclamethasone
Glucocorticoid used in both asthma and arthritis
Stabilise mast cells
Reduce histamine release
Budesonide
GC for arthritis and asthma
Stabilises mast cells reducing histamine release
Unwanted effects of oral corticosteroids
Buffalo hump
Moon face
Hypertension
thinning of skin
Increased risk of infection
Poor wound healing
Osteoporosis
Can reduce these by reducing plasma concentration and choosing administration route
Sulfasalazine
Disease modifying anti rheumatoid drug
Common 1st choice
Complex of salicylate(nsaid) and sulphonamide (antibiotics)
Scavengers free radicals produced by neutrophils
Causes remission in active RA
Enteric coated tablets
SE: gi upset, headache, skin reaction, leukopenia.
Penicillamine
Disease modifying anti rheumatoid drug
75% respond but effects take weeks Lower il1 generation Lower fibroblast proliferation Lower immune response Given orally SE: rashes, stomatitis, anorexia, taste disturbance, fever NOT TO BE GIVEN WITH GOLD COMPOUNDS
Gold compounds
Disease modifying anti rheumatoid drug
Oral auranofin - inhibits induction of il1 and tif a reducing pain and joint swelling
Sodium auranofin - deep I’m injection, concentrate in synovial cells, liver cells, kidney tubules, adrenal cortex and macrophages
Effects develop 3-4 months
SE: skin rash, flue, mouth ulcers, blood disorders.
Serious SE: encephalopathy, peripheral neuropathy, hepatitis
Anti malarials
Chloroquine, hydroxychloroquine
Raise oh of intracellular vacuoles interfering with presenting antigen.
Induces apoptosis in t lymphocytes
Used when other treatments fail
One month for effects
SE: n+v, dizziness, blurred vision,
Anti cytokine drugs
Engineered recombinant antibodies which bind to specific immune cells, inhibiting immune response
VERY EXPENSIVE
USE restricted to patients who don’t respond well to DMARDS.
Can be given with methotrexate
Given sc or iv injections
SE: may develop latent disease, opportunistic infection, heart failure, hypersensitivity.
Adalimumab
Anti cytokine drug
Targets TNF
Enteracept
Anti cytokine drug
Targets TNF
Infliximab
Anti cytokine drug
Targets TNF
Rituximab
Anti cytokine drug
Targets leukocyte receptor
Abatacept
Anti cytokine Drug
Targets leukocyte receptor
Tocilizumab
Anti cytokine drug
Blocks il6 receptor
Disrupting immune signalling
Immunosuppressants
Rheumatoid arthritis is an autoimmune disorder
Suppressing the immune system will suppress disease
Inhibit DNA synthesis or T cell activation
Increase risk of infection
Increased risk of cancer
NSAIDs
Eg, aspirin, ibuprofen, diclofenac, meloxicam.
Tablets, suspensions, gels, injections,
Antipyretic - inhibit PG on hypothalamus
analgesic- reduce sensitivity of neutrons to bradykinin
Anti inflammatory - reduce Vado dilation and vascular permeability.
May inhibit coz 1 (essential for PG production responsible for cv platelet agrevation, and gi mucous) and cox 2( stomach ulcer, cv events)
Scavenge oxygen radicals reducing tissue damage
Ciclosporin
Immunosuppressant. First discovered in fungus.
Inhibits il2 gene transcription, reduces T cell proliferation.
Poorly absorbed orally
Accumulates in high conc. in tissues
SE: nephrotoxicity, hepatoxicity, hypertension, nausea, gum hyper trophy, GI problems
Azathioprine
Immunosuppressant
Cytotoxic, interferes with dna synthesis
Depresses cell mediated and antibody mediated immune reactions
Targets cells in induction phase of immune response.
SE - suppression of bone marrow.
Methotrexate
Immunosuppressant
Folic acid antagonist- inhibits DNA synthesis
Blocks growth and rapid dividing cells
Inhibits T cell activation
SE: blood abnormalities, liver cirrhosis, folate difficiency
Often prescribed with DMARD
Leflunomide
Immunosuppressant
Specific inhibitor of activated T cells
Well absorbed orally with long t life
SE: diarrhoea, alopecia, high liver enzymes, heptotoxicicty
Cyclophosphamide
Immunosuppressant
Only used when other therapies have failed
Pro drug - administered orally activated in liver to phosphoramide mustard and acrolein
Acrolein can result in haemohaggic cystitis - give win lots of fluids
Osteoarthritis
Primary cause- wear and tear
Secondary cause- trauma, disease, obesity
Pain caused through inflammation
Rheumatoid arthritis
Systemic autoimmune disorder
May affect other tissues
Pain through inflammation
