- Inhibit synthesis of prostaglandins from arachidonic acid by inhibiting cyclooxygenase (COX - COX-1 stimulates prostaglandin synthesis essential to preserve gastric mucosa, maintain renal perfusion (by dilating afferent glomerular arterioles) and inhibit thrombus formation at the vascular endothelium - COX-2 expressed in response to inflammatory stimuli stimulates production of prostaglandins that cause inflammation and pain - Therapeutic benefits of NSAIDs are principally COX-2 inhibition and adverse effects by COX-1 inhibition - Selective COX-2 inhibitors (e.g. etoricoxib) developed to reduce the adverse effects

BASIC - MSK Flashcards by Guy Dunbavand

Names of NSAIDs?

Ibuprofen, diclofenac, etoricoxib

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Indications of NSAIDs?

PRN for mild-to-moderate pain

- Regular treatment of pain related inflammation

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Mechanism of NSAIDs?

Inhibit synthesis of prostaglandins from arachidonic acid by inhibiting cyclooxygenase (COX
COX-1 stimulates prostaglandin synthesis essential to preserve gastric mucosa, maintain renal perfusion (by dilating afferent glomerular arterioles) and inhibit thrombus formation at the vascular endothelium
COX-2 expressed in response to inflammatory stimuli stimulates production of prostaglandins that cause inflammation and pain
Therapeutic benefits of NSAIDs are principally COX-2 inhibition and adverse effects by COX-1 inhibition
Selective COX-2 inhibitors (e.g. etoricoxib) developed to reduce the adverse effects

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Side effects of NSAIDs?

GI ulcers/gastritis
Renal impairment
Increased risk of MI/CVA
Fluid retention

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Interactions of NSAIDs?

-	GI Ulceration
o	Aspirin, corticosteroid
-	GI bleeding
o	Anticoagulants, SSRIs, venlafaxine
-	Renal Impairments
o	ACEi, diuretics

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Contraindications of NSAIDs?

o Severe renal impairment
o Heart Failure
o Liver failure

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Cautions of NSAIDs?

o Peptic ulcer disease
o GI bleeds
o CVD

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Prescription of NSAIDs?

Available as tablets, suspensions, gels, suppositories, injectable
Acute pain treatment should be stopped when resolved
Taken with food to minimise GI upset
Can use gastroprotection for patients at increased risk

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Names of oral glucocorticoids?

Prednisolone, hydrocortisone, dexamethasone

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Indications of oral glucocorticoids?

Allergic or inflammatory disorders (anaphylaxis, eczema, asthma, COPD)
Severe croup
Autoimmune disease (IBD, ITP, inflammatory arthritis)
Cancer treatment
Myasthenia Gravis, Polymyalgia rheumatica, GCA, Lupus
Proctitis
Joint injections
Adrenal insufficiency/Hypopituitarism

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Mechanism of oral glucocorticoids?

Bind to cytosolic glucocorticoid receptors which upregulate anti-inflammatory genes and downregulate pro-inflammatory genes (cytokines, TNFa)
Suppression of circulating monocytes and eosinophils
Metabolic effects
o Increased gluconeogenesis
o Increased catabolism
Mineralocorticoid effects
o Stimulate Na and water retention and K excretion

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Side effects of oral glucocorticoids?

Immunosuppression
Diabetes mellitus
Insomnia, psychosis and suicidal ideas
Osteoporosis
Metabolic
o Proximal muscle weakness, skin thinning with easy bruising and gastritis
Mineralocorticoid
o Hypertension, hypokalaemia and oedema
Prolonged
o Adrenal atrophy leading to Addisonian crisis if withdrawn suddenly

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Cautions of oral glucocorticoids?

Infection
Children (suppress growth)
Hepatic or Renal impairment

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Interactions of oral glucocorticoids?

Risk of peptic ulceration – NSAIDs
Hypokalaemia – B2-agonists, theophylline, loop and thiazide diuretics
Affected by CYP450 enzymes

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Prescription of oral glucocorticoids?

o Can be given orally, IM, IV
o OD, taken in the morning to mimic natural circadian rhythm
o Consider use of bisphosphonates and PPIs if long-term and risk

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Monitoring of oral glucocorticoids?

o For children – height and weight monitored annually – refer to paediatrician if slow
o Prolonged treatment – HbA1c or DEXA scan

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Cessation of oral glucocorticoids?

o Abrupt withdrawal can lead to adrenal insufficiency

o Gradual withdrawal used if treatment >3 weeks, received >40mg, repeated evening doses

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Communication of oral glucocorticoids?

o Should feel better in 1-2 days
o Do not stop immediately
o Steroid card to carry round at all times

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Indications of methotrexate?

Rheumatoid arthritis
Crohn’s disease
Chemotherapy – e.g. leukaemia, lymphoma and some solid tumours
Severe psoriasis

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Mechanism of methotrexate?

Inhibits dihydrofolate reductase, which converts dietary folic acid to tetrahydrofolate (FH4)
o FH4 needed for DNA and protein synthesis, so lack of it prevents cellular replication
o Actively dividing cells particularly sensitive so good for cancer
Anti-inflammatory and immunosuppressive effects
o Inhibition of IL-6, IL-8 and TNF alpha

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Side Effects of methotrexate?

Sore mouth, GI upset (diarrhoea, nausea, vomiting)
Neutropenia, leukopenia, thrombocytopenia (Agranulocytosis)
Hepatitis, pneumonitis
Long term use – hepatic cirrhosis, pulmonary fibrosis

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Contraindications of methotrexate?

Active infection
Pregnancy – teratogenic (both men and women taking drug need effective contraception during and for 3 months after stopping treatment
Severe renal impairment
Hepatic impairment in non-malignant conditions

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Cautions of methotrexate?

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Abnormal liver function

Interactions of methotrexate?

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Methotrexate toxicity more likely with:
o NSAIDs, penicillins
Risk of haematological abnormalities in trimethoprim and phenytoin
Risk of neutropenia increased in clozapine

Prescription of methotrexate?

- Oral dose, once weekly 7.5-20mg, adjusted according to response - Folic acid prescribed to be taken on the other 6 days when methotrexate isn’t taken - For cancer – given IV/IM/intrathecal

Important communication to patient of methotrexate?

- Report symptoms of sore throat, fever, bruising, bleeding, nausea, abdominal pain, dark urine, breathlessness - Need contraception - Give folic acid to reduce side effects

Monitoring of methotrexate?

- Before treatment – FBC, LFT, U&E and a pregnancy test - 1-2 weekly until established - 2-3 monthly thereafter

Indications of allopurinol?

- Prophylaxis of gout and uric acid/calcium oxalate renal stones - Prophylaxis of hyperuricaemia in cancer

Mechanism of allopurinol?

- Xanthine oxidase inhibitor | - Reduces xanthine to uric acid – lowers concentrations of uric acid

Side effects of allopurinol?

- Skin rash – mild to severe SJS or TENs - Drug hypersensitivity syndrome o Fever, eosinophilia, lymphadenopathy - Acute gout triggered

Contraindications of allopurinol?

- Acute gout | - Recurrent skin reaction

Cautions of allopurinol?

- Ensure adequate fluid intake (2-3 litres/day) | - Start allopurinol before cancer treatment

Dose changes in renal/hepatic impairment of allopurinol?

- Dose reduction

Interactions of allopurinol?

- Allopurinol and amoxicillin risk of rash | - Allopurinol and ACEi/thiazides – risk of hypersensitivity reactions

Prescription of allopurinol?

- Oral start at low dose and titrate according to uric acid levels to maintenance dose - Typical 100mg initial and then up to 200-600mg - Take after food - NSAID or colchicine prescribed for 1 month after serum uric levels normalise to avoid acute attack

Communication of allopurinol?

- Take after meals - Seek advice if rash develops - Do not stop allopurinol in acute attack

Monitoring required of allopurinol?

- Uric acid levels checked 4 weeks after start/dose change | - Aim for uric acid <300 and titrate dose

Names of calcium salts?

Calcium carbonate, calcium gluconate

Names of vitamin D analogue?

Colecalciferol

Indications of calcium salts and vitamin D?

- Osteoporosis - Chronic kidney disease - Severe hyperkalaemia (calcium gluconate) - Hypocalcaemia if symptomatic or severe (<1.9) - Vitamin D used in prevention and treatment of Vitamin D deficiency, including rickets (children) and osteomalacia (adults)

Mechanism of action in calcium and vitamin D?

- Calcium needed for muscles, nerves, bone and clotting - Homeostasis controlled by PTH and vitamin D, which increase serum Ca and calcitonin which reduces Ca level - Restoring positive Ca balance reduces rate of bone loss, restores Ca level in CKD - In hyperkalaemia, calcium gluconate raises myocardial threshold potential, reducing excitability

Side effects of calcium salts?

- Dyspepsia - Constipation - Nausea

Interaction of oral calcium?

- Oral calcium reduces absorption of: | o Iron, bisphosphonates, tetracyclines and levothyroxine

Prescription of calcium salts & vitamin D?

- Adcal D3 BDS contains calcium and vitamin D (cholecalciferol) - Chew then swallow tablets - Separate doses by 4 hours to medicines that interact

Monitoring in calcium salts?

- Check calcium levels regularly

Names of bisphosphonates?

Alendronic acid, disodium pamidronate, zoledronic acid

Indications of bisphosphonates?

- Alendronic acid – patients at risk of osteoprotic fragility fractures - Pamidronate/Zoledronic acid – severe hypercalcaemia of malignancy, myeloma, breast cancer with bone mets - Paget’s Disease

Mechanism of bisphosphonates?

- Reduce bone turnover by inhibiting action of osteoclasts, cells responsible for bone resorption - Reduction in bone loss and improvement in bone mass

Side effects of bisphosphonates?

- Oesophagitis - Hypophosphatemia - Osteonecrosis of jaw - Osteonecrosis of external auditory canal - Atypical femoral fractures

Contraindications of bisphosphonates?

- Severe renal impairment (<35) - Hypocalcaemia - Upper GI disorders

Cautions of bisphosphonates?

- Smokers | - Dental disease

Interactions of bisphosphonates?

- Absorption reduced if taken with calcium salts (including milk), antacids and iron salts

Prescription of bisphosphonates?

- For osteoporosis – alendronic acid oral 70mg once weekly | - For severe hypercalcaemia – slow IV infusions

Communication to patient of bisphosphonates?

- Alendronic acid – swallowed whole >30 mins before breakfast or other medications with plenty of water, patient remain upright for 30 minutes afterwards to reduce oesophageal irritation

Monitoring of bisphosphonates?

- Osteoporosis – check Ca and Vit D before and during treatment, DEXA every 1-2 years - Hypercalcaemia – Ca levels

BASIC - MSK Flashcards

(55 cards)