Pharmacology Flashcards
function and examples of NSAIDS
anti-inflammatory + Analegesic
e.g. Ibuprofen, Naproxen, Diclofenac
mode of action of NSAIDs
target cyclooxygenase-2, an enzyme responsible for inflammation and pain
how can the risk of peptic ulcers in NSAIDs be reduced
Targeting COX-2 selectively
side effects of NSAIDS
Dyspepsia Oesophagitis Gastritis Peptic Ulcer Small/large bowel ulceration Renal impairment Increased cardiovascular events (Cox 2 inhibitors + others) Fluid retention Wheeze Rash
function of DMARDs
anti-inflammatory with no direct analgesic effect
improve standard lab tests of inflammation e.g. ESR CRP
Reduce rate of joint damage
slow acting - weeks to months
what is the first choice DMARD in most patients
Methotrexate
what drug is a folate antagonist
Methotrexate
side effects of methotrexate
Leucopenia / thrombocytopenia Hepatitis / cirrhosis (alcohol intake must be limited) Pneumonitis Rash / mouth ulcers Nausea / diarrhoea
what needs monitored in methotrexate
FBC
LFTs
can methotrexate be given in pregnancy
no
it is teratogenic
must be stopped in male and females at least 3 months before conception
what are side effects of sulfasalazine
Nausea Rash / mouth ulcers Neutropenia Hepatitis Reversible oligozoospermia
what needs to be monitored in sulfasalazine
FBC
LFTs
Hydroxychloroquine can be used to prevent joint damage - true or false
false
has no effect on joint damage
used in CTDs e.g. SLE, Sjogren’s syndrome, RA
side effects of Hydroxychloroquine
retinopathy
what are other less common DMARDS and their side effects
Sodium aurothiomalate (gold) given IM. Adverse effects – bone marrow suppression, glomerulonephritis, rash , mouth ulcers. Monitor FBC plus urine for proteinuria.
Penicillamine oral, adverse effects as for IM gold
what are anti-TNF drugs
Etanercept
Adalimumab
Certolizumab
Infliximab
what is the comparison of anti-TNF to DMARDs
About 1.5 times as effective as standard DMARDs
More effective in combination with DMARDs
~£10,000 per annum
Majority given by sub-cutaneous injection
what can anti-tnf be used in
RA
Psoriatic arthritis
AS
adverse effects of Anti-TNF
Major risk of infection (esp TB)
Question over risk of malignancy (esp skin cancer)
Contraindicated in certain situations e.g. pulmonary fibrosis, heart failure
criteria for anti-TNF treatment
high disease activity score
use of previous standard DMARDs
examples of other biologics (not anti-TNF)
Rituximab - monoclonal antibody against B (CD20) lymphocytes
Tocilizumab – inhibits Interleukin 6
Abatacept - CTLA-4 Ig -blocks full activation of T lymphocytes
Ustekinumab – Inhibits IL12 and IL23
what is the treatment of acute episode of gout
Colchicine (can cause diarrhoea and vomiting)
NSAIDs
Steroids
gout prophylaxis treatment
Urate lowering:
- allopurinol
- febuxostat
- uricosurics
what is the process of making uric acid in the body
Purine >>>> Xanthine >>>> Xanthine oxidase Uric acid
what does allopurinol and febuxostat target
xanthine oxidase
why is allopurinol not commenced during acute episodes
Rapid reduction in uric acid level may result in exacerbation of gout
side effects of allopurinol
Rash (vasculitis) commoner in elderly and in renal impairment, therefore use lower doses
who gets febuxostat
those who cannot tolerate allopurinol i.e. those with renal impairment
examples of uricosurics
Probenecid
Sulphinpyrazone
Azapropazone
Benzbromarone
what rheumatogical diseases are steroids used in
CTD
PMR/GCA
Vasculitis
RA
metabolic effects of steroids
Salt and water retention
Increased gluconeogenesis
Increased hepatic glycogen deposition
Increased protein breakdown
side effects of steroids
Weight gain - centripetal obesity Muscle wasting Skin atrophy Osteoporosis Diabetes Hypertension Cataract Glaucoma Fluid retention Adrenal Suppression Immunosuppression Avascular necrosis of the femoral head
how can corticosteroids toxicity be reduced
Use lowest possible dose for as short a time as possible
Consider steroid sparing agents
Osteoporosis prophylaxis
Watch cardiovascular risk factors
