LOCO2 Drugs Flashcards
Which drug can be used to determine how mineralised bone is? [1]
Tetracycline can be used to see how mineralised bone is. Tetracycline gets taken up on the calcium ions, and becomes deposited here and auto-fluoresces
A 36-year-old woman presents to her GP with pain in both hands. It is worse in the morning and occurs for more than 30 minutes.
A diagnosis of rheumatoid arthritis is suspected and blood tests are organised before the patient is referred to secondary care for a rheumatology opinion. The rheumatologist confirms the diagnosis and prescribes a first-line disease-modifying anti-rheumatic drug: methotrexate.
What medication should be co-prescribed for this patient?
Fluorouracil
Folic acid
Furosemide
Nicotinic acid
Vitamin B12
Folic acid
A 76-year-old woman presents to her physician with non-healing mucosal ulcers and loose teeth. She has a past medical history of recurrent falls, bilateral hip replacement, diabetes and asthma.
Examination findings show periodontal disease.
Radiology reports show sclerotic lesions in the mandible and maxilla consistent with osteonecrosis.
Which one of the following drugs may be the cause of her presentation?
Insulin
Denosumab
Vitamin D supplements
Calcium supplements
Alendronate
Alendronate
Bisphosphonates can cause osteonecrosis of the jaw
You are a junior doctor working in orthopaedic surgery and have been asked to see a 44-year-old woman who is booked in for surgery tomorrow for repair of an open radial fracture sustained after falling from her bike. She has a past medical history of severe psoriasis, gastro-oesophageal reflux disease, polycystic ovary syndrome and depression. You order some routine bloods prior to surgery, and are surprised by the following results:
Bilirubin 17 µmol/L (3 - 17)
ALP 89 u/L (30 - 100)
ALT 354 u/L (3 - 40)
γGT 61 u/L (8 - 60)
Albumin 34 g/L (35 - 50)
Which of her medications is most likely to be responsible for this derangement?
Combined oral contraceptive pill
Fluoxetine
Methotrexate
Morphine
Omeprazole
Methotrexate: cause hepatotoxicity
A 77-year-old woman is reviewed on the orthogeriatrics ward round 5 days following a hemiarthroplasty for a fractured neck of femur. The consultant decides to start her on a RANK ligand inhibitor for secondary prevention of osteoporosis.
Which of the following medications will you commence?
Alendronic acid
Denosumab
Letrozole
Raloxifene
Teriparatide
Denosumab
A 42-year-old woman complains to her General Practitioner of general fatigue during the last two months. She says the joints in both her hands and wrists are increasingly painful and stiff, especially in the morning and she finds it difficult to write. Her X-ray is diagnostic of rheumatoid arthritis and she is started on methotrexate and sulfasalazine. Which enzyme does methotrexate inhibit?
Dihydroorotate dehydrogenase
Cyclooxygenase 2
Dihydrofolate reductase
Matrix metalloproteinase 1
Serine hydroxymethyltransferase
Dihydrofolate reductase
A 27-year-old woman is referred to a rheumatology clinic as she has developed pain and stiffness in the small joints of her hands. She is diagnosed with rheumatoid arthritis and is started on methotrexate.
Given her diagnosis and management, the risk of which side effect is reduced by giving a folate supplement?
Infection
Hepatitis
Myelosuppression
Pneumonitis
Teratogenesis
Myelosuppression
A 65-year-old retired firefighter presents to the general practice surgery with recurrent burning central chest pain. He finds the pain is worse after eating a take-away and drinking alcohol and he feels that he is belching more than usual.
Past medical history is significant for high cholesterol, type two diabetes and osteoarthritis. His medications are atorvastatin, metformin, gliclazide, naproxen and omeprazole which he often forgets to take.
Which of his medication is the most likely cause of his symptoms?
Atorvastatin
Gliclazide
Metformin
Naproxen
Omeprazole
Naproxen: Peptic ulcers are a side effect of NSAIDs
A 59-year-old female presents to the rheumatology clinic, she has a diagnosis of rheumatoid arthritis and has been started on a new medication to help prevent disease progression and joint destruction. However, with this she needs to take daily folic acid and have frequent blood tests. Which medication is she likely to be on?
Sulfasalazine
Prednisolone
Methotrexate
Rituximab
Etanercept
Methotrexate
A 46-year-old female with poorly controlled rheumatoid arthritis and a history of significant large bowel resection. She has just had sulfasalazine, a prodrug, added to her medications, however the consultant is worried that she will be unable to convert the prodrug into its active form with her shortened colon.
Which therapeutically active compound is her medication converted to in the colon?
TNF-alpha
6-mercaptopurine
Methotrexate
Sulfamethoxazole
5-ASA (5-aminosalicylates)
5-ASA (5-aminosalicylates)
A 74-year-old woman attends her GP following a diagnosis of osteoporosis after sustaining a radial fracture during a fall. The doctor explains that they would like to prescribe alendronic acid, a bisphosphonate, to help prevent further fractures.
What is the mechanism of action of this drug?
Increased cholecalciferol synthesis
Increased serum calcium levels
Osteoblast inhibition
Osteoclast inhibition
Osteoclast stimulation
Osteoclast inhibition
A 48-year-old male discusses his secondary prophylaxis medications after suffering from a myocardial infarction last week. Aspirin is included in the several drugs but he is hesitant due to suffering from multiple bouts of acid reflux despite gastric protection. Celecoxib another COX (cyclooxygenase) inhibitor is prescribed instead.
What best describes the mechanism of action of this drug?
Reversible COX-1 inhibitor
Reversible COX-2 inhibitor
Non-reversible COX-1 inhibitor
Non-reversible COX-2 inhibitor
Non-reversible COX-1 and 2 inhibitor
Reversible COX-2 inhibitor
A 63-year-old woman has been referred by her GP to the osteoporosis clinic for alternate bone-sparing treatment. She has recently had a bone density scan following a low impact distal radial fracture. Her T-score in her hip and spine has returned as -2.6 and -2.2 respectively. She was subsequently commenced on bone-sparing treatments but she developed significant gastrointestinal side effects despite the trial of different preparations of bisphosphate including alendronate and risedronate. A decision has been made at the clinic to commence patient on a receptor activator of nuclear factor kappa-Β ligand (RANKL) inhibitor.
Which of the following is this treatment referring to?
Denosumab
Strontium ranelate
Teriparatide
Zoledronic acid
Raloxifene
Denosumab
An 81-year-old woman is admitted following a fall. Upon subsequent examination and imaging, she is diagnosed with a wrist fracture. This is deemed to be a fragility fracture given the low impact mechanism of injury.
Two weeks later, she is discharged on a new medication to increase bone density as per the National Institute for Health and Care Excellence (NICE) guidance.
What is the mechanism of the drug she has been prescribed?
Increases calcium availability to bone
Inhibits osteoblasts
Inhibits osteoclasts
Promotes osteoblasts
Promotes osteoclasts
Inhibits osteoclasts
A 68-year-old woman with breast cancer is started on a chemotherapy regimen including methotrexate.
Which enzyme is inhibited by this drug?
Thymidylate synthase
Methionine synthase
Dihydrofolate reductase
Methylenetetrahydrofolate reductase
Folylpolyglutamate synthase
Dihydrofolate reductase
RA
Methotrexate and Rituximab would be
First line treatment
Second line treatment
Third line treatment
Fourth line treatment
Third line treatment
RA
Methotrexate and a 2nd line DMARD would be
First line treatment
Second line treatment
Third line treatment
Fourth line treatment
First line treatment
RA
Methotrexate & a TNF-inhibitor would be
First line treatment
Second line treatment
Third line treatment
Fourth line treatment
Second line treatment
Methotrexate inhibits which enzyme? [1]
dihydrofolate reductase
RA
Sulfasalazine is a prodrug for [1]
5-ASA
Hydroxychloroquine blocks:
TLR7
TLR8
TLR9
TLR10
TLR11
TLR9
RA
Leflunomide inhibits which enzyme? [1]
What is the effect of this? [2]
Dihydroorotate dehydrogenase (DHODH): stops pyrimidine synthesis & therefore reduces pro-inflammatory cytokines: IL-1, TNF-A and IL-6; Blocks T cell proliferation
Which is the staple treatment for RA?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which is the staple treatment for RA?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which treatment for RA inhibits dihydrofolate reductase?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which treatment for RA inhibits dihydrofolate reductase?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which treatment for RA reduces purine synthesis?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Methotrexate
Which treatment for RA reduces pyrimidine synthesis?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Leflunomide
Which treatment for RA is safe for pregnant people?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Sulfasalazine
Which treatment for RA is prodrug that operates in large intestine?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which treatment for RA is prodrug that operates in large intestine?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Which treatment for RA that targets TLR-9?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Hydroxychloroquine
Which treatment for RA that reduces dendritic cell activation?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Hydroxychloroquine
Which is a treatment for RA that inhibits dihydro-orotate dehydrogenase?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Hydroxychloroquine
Which treatment for RA requires folate to be given alongside?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Methotrexate
Which treatment for RA is a tumor necrosis factor-alpha (TNF-alpha) inhibitor?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Infliximab
Which treatment for RA is a monoclonal antibody?
Methotrexate
Sulfasalazine
Hydroxychloroquine
Leflunomide
Infliximab
Infliximab
Which treatment for RA is an anti-CD20 monoclonal antibody?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Rituximab
Which treatment for RA causes B cell depletion?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Rituximab
Which treatment for RA leads to decreased T-cell proliferation and cytokine production?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Abatacept
Which treatment for RA is an IL-1 antagonist?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Anakinra
Which treatment for RA targets IL-6?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Tolizumab
Which treatment for RA targets upregulates CTLA-4, which switches T cell off?
Etanercept
Adalimumab
Anakinra
Rituximab
Abatacept
Tolizumab
Tolizumab
OA - fill in about colexcicb
State the treatment pyramid for RA:
Pain management: [2]
First line disease treament (Mild RA): [2]
Second line disease treatment (moderate RA) [2]
Second line disease management: (severe RA) [2]
Pain management: NSAID & Opioids
First line: Methotrexate & 2nd line DMARD
Second line disease treatment (moderate RA) Methotrexate & TNF-inhibitor
Second line disease management: (severe RA) Methotrexate & Rituximab
If have a flair of RA which drug might be used as adjunct therapy? [1]
Oral corticosteroid pulse (e.g. prednisilone)
How may you start DMARD treatment if have severe RA? [2]
Start with high dose and taper down once under control
OR
Add prednisilone
State 3 reasons why may not prescribe methotrexate [3]
Liver damage (methotrexate metabolised in liver)
Pregnant
Co-morbidities
State two factors that DMARDs improve [2]
What does DMARD not improve? [1]
Improves:
* early improves number of swollen
* improves radiographic progression
No effect:
* the patients fatigue severity
Explain MoA of methotrexate [4]
How is it administered? [1]
Oral dose (can change to subcut. or IM)
MoA:
* Folic acid antagonist which will limits DNA and RNA synthesis by inhibiting dihydrofolate reductase and thymidylate synthetase
* Causes a reduction in purine synthesis
* Induce ROS
* Causes activation of apoptosis
* Inhibits pro-inflam cytokines IL-1 & NF-kB
State three side effects of methotrexate [2]
Can cause liver problems
Can affect blood count
Hair
Describe MoA of Sulfasalazine [5]
Mode of action in RA not well understood:
* Metabolised in the colon by gut bacteria to 5-ASA
* 5-ASA stays in large intestine lamina propria and has local anti-inflammatory actions
* Supresses generation of superoxide radicals and cytokine production by inflammatory cells
* IL8 decreased in synovial fluid and decreased production of IgM and IgG, and decreased angiogenesis
* Inhibits IL-1 and TNF-a
Describe the MoA of Hydroxychloroquine [2]
- Accumulates in lysosomes increasing the pH decreasing protein modifications
- Blocks Toll-like receptor 9 which recognises DNA containing immune complexes decreases activation of dendritic cells: less autoantobodies produced
Describe MoA of Leflunomide [3]
Pro-drug: gets metabolised in liver
Inhibits dihydroorotate dehydrogenase (DHODH) and therefore stops pyrimidine biosynthesis
Reduces pro-inflammatory cytokines: IL-1, TNF-A and IL-6
Blocks T cell proliferation
Name two TNF-a blockers for RA [2]
Etanercept
Infliximab
Explain MoA of Etanercept:
What is etanercept a fusion protein for? [1]
What is etanercept Fc for? [1]
When TNF-a is released: finds receptors on cells, activates and causes signal transduction
Etanercept is a fusion protein human TNF receptor 2 and Fc human IgG.
Etanercept binds to TNF-a before TNF-a can get to cell and cause inflammatory, signalling
Describe MoA of Infliximab [1]
Monoclonal antibody against TNFα
Infliximab often prescribed alongside which drug? [1]
Infliximab and methotrexate
Name another TNF-inhibitor used in RA [1]
Adalimumab
Name a Human recombinant IL-1 receptor antagonist to treat RA
Anakinra
Name drug A used to treat osteoporosis [1]
Denosumab
Name drug A used to treat osteoporosis [1]
Teriparatide
What is first line treatment for osteoporosis? [1]
Describe MoA [3]
Bisphosphonates:
- inhibits osteoclast activity
- promotes osteoclast apoptosis
- Decreases RANKL expression (so osteoblasts don’t turn into osteoclasts [?])
Describe complications of bisphosphonates
Kills off osteoclasts: don’t remove old bone: thickened bone
Get giant osteoclasts: poisoned osteoclasts
Osteonecrosis occurs
Colchicine - inhibits microtubule polymerization by binding to tubulin, interfering with mitosis. Also inhibits neutrophil motility and activity
Name and describe how two therapeutic drugs cause myopathy [2]
Corticosteroids; cause dose dependent type 2 atrophy
Hydroxychloroquine: not dose dependent atrophy; lysosomes damaged
Hydroxychloroquine causing lysosome damage
Which antibiotics would you give for chronic osteomyelitis [1]
Vancomycin cement beads
