Drugz Flashcards
Anti-inflamm and pain relief drugs for rheumatoid conditions
- Aspirin for transient MSK pain and pyrexia (fever)
- NSAIDs for inflam cond’s
- Paracetamol 1st line pain relief where NSAIDs not indicated. Codeine if not sufficient
Paracetamol (acetaminophen) mechanism of action
- Inhibits synthesis of prostaglandins in the CNS and peripherally blocks pain impulse generation
- Reduces pyrexia by inhibition of the hypothalamic heat-regulating centre
Paracetamol indications
Mild to moderate pain, pyrexia. NSAIDs are preferred for pain relief in the inflammatory arthritides
Paracetamol SEs
Rare unless in overdose
Paracetamol cautions/contraindications
Dosing interval 6 hours or greater if eGFR
NSAIDs mechanism of action
Inhibition of cyclo-oxygenase (COX), the enzyme which catalyses the synthesis of cyclic endoperoxidases from arachidonic acid to form prostaglandins.
Drawback of NSAID mechanism of action and how can it be avoided
- Inhibition of the COX-1 isoform in the GI tract leads to reduction in protective prostaglandins and predisposes to gastroduodenal damage.
- COX 2 is the form mainly induced in response to pro-inflammatory cytokines.
- The selective inhibitors of COX-2 (‘coxibs’, etoricoxib and celecoxib) have a lower risk of gastroduodenal damage that the non-selective NSAIDs (e.g. ibuprofen, diclofenac)
NSAIDs indications
- Pain and inflammation associated with inflammatory arthritides and severe osteoarthritis
- Crystal synovitis
- Transient MSK pain
- Pain caused by secondary bone tumours
E.gs of NSAIDs and their benefits and drawbacks
Ibuprofen - fewer SEs but anti-inflam weaker
Indometacin - more potent but more SEs
Diclofenac and naproxen in between the two
SE’s NSAIDs
- GI toxicity w highest risk in elderly. Inflammation and ulceration most apparent in stomach and duodenum
- Co-prescribe PPIs w non-selective NSAIDs in high risk pts (>65y, pmhx peptic ulceration, other med that inc GI risk: warfarin, aspirin, corticosteroids)
- Hypersensitivity reactions, blood disorders, fluid retention, AKI, hepatitis, pancreatitis, exacerbation of colitis
Cautions and contraindications NSAIDs
- contraindicated in pts w hx of hypersensitivity to aspirin or any other NSAID.
- contraindicated in severe HF
- Avoid in pts w previous GI ulceration
- In pts w renal, cardiac or hepatic impairment NSAIDs may cause a deterioration in organ function
What drugs affect bone metabolism?
bisphosphonates, calcium, vitamin D
mechanism of action bisphosphonates
adsorbed onto hydroxyapatite crystals in bone and inhibit growth and activity of osteoclasts, thereby reducing the rate of bone turnover
indications bisphosphonates
OSTEOPOROSIS -Prophylaxis and treatment in combination with calcium and vit D supplements if dietary intake inadequate.
PAGET’S DISEASE AND HYPERCALCAEMIA OF MALIGNANCY - treatment
OSTEOLYTIC LESIONS AND BONE PAIN in bone metastases associated with breast cancer or multiple myeloma - treatment
SE’s bisphosphonates
- GI - dyspepsia, nausea, vomiting, abdo pain, diarrhoea, constipation
- Flu like symptoms
- Oesophageal reactions with alendronic acid
- MSK pain
- Biochemical abnormalities (hypophosphataemia, hypocalcaemia, hyper or hypokalaemia, hypernatraemia)
- Anaemia
- Thrombocytopenia
- Lymphocytopenia
- Seizures
- AKI
- Conjunctivitis
- Osteonecrosis of the jaw - greatest risk in pts recieving IV bisphosphonates for cancer indications