Pharmacology: MSK Drugs Flashcards
What is the mechanism of action of most NSAIDs?
Act as nonselective inhibitors of the cyclooxygenase (COX) enzymes
What is the mechanism of action of toclizumab?
Inhibits IL-6
What is the mechanism of action of oral bisphonates?
Analogues of pyrophosphate that absorb onto bone within the matrix; ingested by osteoclasts leading to cell death thereby inhibiting bone resorption
Prevent bone loss at all sites vunerable to osteoporosis
What is the mechanism of action of teriparatide?
Recombinant parathyroid hormone; stimulates bone growth rather than reduces bone loss (anabolic)
Why is certolizumab safe throughout pregnancy/breastfeeding?
Unable to cross the placental barrier due to its pergolated component
Weight gain, skin atrophy and osteoporosis are side affects of which medication used in the management of vasculitis?
Corticosteriods
What is the mechanism of action of zoledronic acid?
IV bisphosphate - analogues of pyrophosphate that absorb onto bone within the matrix; ingested by osteoclasts leading to cell death thereby inhibiting bone resorption
What is the mechainsm of action of febuxostat?
Xanthine oxidase inhibitor
What is the mechanism of action of methotrexate?
Folate antagonist, mode of action unknown
Name a contraindication of NSAIDs
Peptic ulcer disease
What are the main indications for oral bisphonates?
First line in majority of patients with osteoporosis
- Consider treatment with when T score = -2.5
- If ongoing steroid requirement >/= 7.5mg prednisolone for 3 months or more or if there is a prevalent vertebral fracture, consider treatment with T score < 1.5
Paget’s disease of bone
May have some benefit in patients with osteogenesis imperfecta in teenage years
What is the main contraindication for romosozumab?
Previous MI/CVA
Why must leflunomide be stopped in females at least 3 months before conception?
It is teratogenic
What is the mechanism of action of romosozumab?
Monoclonal antibody that binds to and inhibits sclerostin (sclerostin inhibits bone formation) to increase bone formation and reduce bone resorption
What is the main indication of febuxostat?
Gout prophylaxis when allopurinol not tolerated/contraindicated
What is the main indication for zoledronic acid?
Second line for majority of patients with osteoporosis e.g. patients with side effects with oral bisphonates
What is the main indication for desonumab?
Another second line alternative to oral bisphonates in patients with osteoporosis
Why must methotrexate be stopped in females at least 3 months before conception?
It is teratogenic
When would anti-TNF therapy be indicated in RA, psoriatic arthritis and ankylosing spondylitis?
After a failure of 2 DMARDs or in ankylosing spondylitis 2 NSAIDs
What is leflunomide?
Second line DMARD with a similar efficacy to methotrexate
What is the main indication of teriparatide?
Recommended over oral bisphosphate in postmenopausal women with at least 2 moderate or 1 severe low trauma vertebral fracture to prevent vertebral fracture
Name three side effects of desonumab
Hypocalcaemia
Eczema
Cellulitis
NSAIDs are indicated in the management of which type of arthritis?
Inflammatory arthritis
What is the first line DMARD for use in RA, psoriatic arthritis, connective tissue disease, and vasculitis?
Methotrexate
Name a common cutaneous side effect of allopurinol and febuxostat
Rash (vasculitis)
What is the mechanism of action of desonumab?
Monoclonal antibody which reduces osteoclast activity
Binding to RANKL (receptor activator of nuclear factor-kB ligand) prevents the activation of RANK which inhibits development and activity of osteoclasts, decreasing bone resorption and increasing bone density
What is the mechanism of action of allopurinol?
Xanthine oxidase inhibitor
What is the mechanism of action of tofacitinib/baricitinib?
Janus kinase inhibitors
Why should FBC + LFTs be monitored in a patient taking methotrexate/leflunomide/sulfasalazine?
Can cause leukopenia, thrombocytopenia, hepatitis and cirrhosis
What is the mechanism of action of rituximab?
Monoclonal antibody against B (CD20) lymphocytes
What are the main indications for hydroxycholoroquine?
Used in connective tissue diseases - SLE, Sjogren’s syndrome
Can decrease malaise and myalgia in patients with inflammatory arthritis when taken alongside methotrexate (but no effect on joint damage)
Name a contraindication of allopurinol
Renal impairment
Anti-TNF therapy and other biologics increase the risk of infection (especially ___) and may increase risk of malignancy (especially ____ _____)
Anti-TNF therapy increases the risk of infection (especially TB) and may increase risk of malignancy (especially skin cancer)
Why should a prophylactic NSAID or colchicine be prescribed for at least 6 months after starting a xanthine oxidase inhibitor for gout prophylaxis?
Rapid reduction in uric acid level may result in further exacerbation of gout
What is the main indication of allopurinol?
Gout prophylaxis (first line)
What is the mechanism of action of abatacept?
CTLA-4 Ig - biologic which blocks full activation of T lymphocytes
Why do patients on hydroxychloroquine require annual optometry checkups?
Risk of retinopathy
What is the mechanism of action of secukinimab?
Inhibits IL-17
Name a contraindication of febuxostat
Ischaemic heart disease
What is the main indication of romosozumab?
Recommended for postmenopausal women with severe osteoporosis who have had a fragility fracture and are at imminent risk of further fracture (24 months)
What can be prescribed with methotrexate to reduce some of its adverse affects?
Folic acid
Name a side effect of zoledronic acid which occurs in 1/3 patients
1/3 acute phase reaction with first infusion - manage with paracetamol
What is sulfasalazine?
DMARD often used in combination with methotrexate in early inflammatory arthritis
Why are oral bisphonates only prescribed for 5-10 years?
To reduce risk of (rare) long-term side effects associated with duration of use: osteonecrosis of the jaw, oesophageal carcinoma, atypical fractures
Name the only anti-TNF licensed in pregnancy/breastfeeding
Certolizumab
Name an affect sulfasalazine can have on fertility
(Reversible) oligozoospermia
