4.1.1 Pharmaceuticals for Musculoskeletal Pain Flashcards
What is the immune response?
Immunologically competent cells are activated in response to foreign organisms.
May be beneficial or deleterious
Numerous molecular mediators
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What is the general strategy in pain management?
Relief of pain
Delay or arrest of disease process
Arachadonic acids is a precursor molecule for?
Prostaglandins
Thromboxane
Prostacyclin
Where in the arachidonic acid pathway do the COX enzymes work?
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What is the difference between COX1 and COX2
COX1 - Constitutively active, provides protection in the gut, protective function
COX2 - Inducible, inflammatory response
How does acetaminophen differ from other drugs?
Acetaminophen works on the CNS as well
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What are the anti-inflammatory effects of asprin?
Nonselective inhibitor or COX isoforms
Irreversibly inhibits COX and platelet aggregation
What are the analgesic effects of asprin?
Most effective in reducing pain of mild to moderate intensity through reducing inflammation
What are the antipyretic effects of asprin?
Antipyretic effects probably mediated by both COX inhibition in the CNS and inhibition of IL-1
What are some of the adverse effects of asprin?
Gastric Upset
How is ibuprofen different that asprin?
Often prescribed in lower doses with analgesic, but not anti-inflammatory efficacy
NSAIDS
What is a good use for indomethacin?
Particularily popular for gout and ankylosing spondylitis
NSAID
Mainly used for severe inflammation
What are the characteristics of COX-2 selective inhibitors?
Inhibit prostaglandin synthesis by COX-2 induced at sites of inflammation.
Lower liability for GI upset
No impact on platelet aggregation though
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What are some of the COX-2 selective inhibitors?
Celecoxib
Etoricoxib
Meloxicam
What are the characteristics of acetaminophen?
Weak inhibitor of COX enzymes
Central direct analgesic effects
Not an anti-inflammatory at typical doses
Antipyretic
Describe the dietary manipulation of inflammation,
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What are the characteristics of the Disease-Modifying Anti-Rheumatic Drugs (DMARDs)?
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What are the characteristics of methotrexate?
Inhibition of AICAR tranformylase leading to secondary effects on chemotaxis
What are the characteristics of cyclophosphamide
Cross-linking DNA to prevent cell replication
What are the characteristics of cyclosporine?
Inhibits IL-1 and IL-2
What are the characteristics of Azathioprine?
Suppresses B and T cell function Ig production and IL-2 secretion
What are the characteristics of sulfasalazine?
IgA and IgM rheumatoid factor production are decreased
What are the two meanings for biologic therapies?
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What are the anti-TNF agents?
Etanercept - cytokine receptor fusion protein
Infliximab - anti-TNF chimeric monoclonal antibody
Adalimumab - anti-TNF monoclanal antibody
What is the action of rituximab?
B-cell depleting agents
What is the action of abatacept?
T-cell co stimulation inhibitor
What are the actions of leflunomide?
Cell growth arrestors - G1 phase
What is the action of anakinra?
IL-1 inhibition
What is the action of Secukinumab (Costenyx)?
IL-17A inhibitors
What is the action of Ixekizumab (Taltz)?
IL-17A used in plaque psoriasis
What are the characteristics of steroidal anti-inflammatory therapy?
Inhibition of NF-kB and AP-1 transcription
Net result is decreased lymphocytes, monocytes, eosinophils and basophils
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What are the different steroid medication and what are their durations? Why do physicians do not what to keep patients on for extended periods?
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What is gout?
Metabolic disease characterized by recurrent episode of acute arthritis due to depositions of monosodium urate in joints and cartilage
What are the therapeutic goals for gout?
Providing control of pain and inflammation
What are the characteristics of Colchicine?
Inhibits microtubule aggregation which disrupts leukocyte chemotaxis and phagocytosis
Inhibition of crystal-induced production of chemotatic factors
Producesdiarrhea and other GI side effects
What treatments have replaced colchicine?
NSAIDs
Indomethacin - inhibits urate crystal phagocytosis
What are the drugs that are used in the prophylaxis of gout?
Xanthine Oxidase inhibitors
Allopurinol - blocks conversion of xanthine to uric acid
Febuxostat - New class of xanthine oxidase inhibitor, more selective
What are the characteristics of the Uricosuric drugs?
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What are the characterisitcs of Opoid analgesics? Not super specific
Morphine is derived from opium
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