Term
| What are characteristics of COX1 and COX2. |
|
Definition
| Cox1 one is constitutive and it is autocrine or paracrine. Cox1 is involves in regulating the synthesis PGs used GI mucus, GI acid secretion, and platelet aggregation. Cox2 is inducable and it used in inflammation. Cox2 is used in synthesizing PGs used in mediation inflammatory response. |
|
|
Term
| How NSAIDs work as an analgesic? |
|
Definition
| PGE2 sensitizes nerver ending to mechanical and chemical stimuli. No tolerance or addiction seen with long term use. |
|
|
Term
|
Definition
| NSAIDs block the fever caused by inflammation, surgery or injury. they reduce the fever but do not reduce the fever induced by exercise. |
|
|
Term
|
Definition
| Block edema, hyperanalgesia, and vasodilation. They don't stop the progression of tissue injury. They are used injuries such as rheumatoid arthritis, sports injury, and osteoarthritis. |
|
|
Term
| how the NSAIDs are used in labor or after |
|
Definition
| NSAIDs inhibit PGE2 which maintains patency of ductus arteriosis which is used for profusion of baby but after birth NSAIDs are used to block the ductur arteriosis and they are used cause it to close for premature births. |
|
|
Term
| List the side effects of NSAIDs |
|
Definition
gastic ulceration caused by inhibition PGI2 and PGE2
Inhibition of TXA2 causes bleeding
Closure of ductus arteriosis by causind decreased levels of PGF2 and PGI2.
Renal complication in patients due to decreases blood flow and decreased GFR can cause the acute renal failure.
Can also cause edema by inhibiting ADH enzyme and chlorine reabsorption. |
|
|
Term
| List the acetylated NSAIDs |
|
Definition
The acetylated NSAID is aspirin and it is most widely used. It irreversibly inhibits cox. examples bufferin and excedrin.
It has antipyretic, analgesic and antiinflammatory properties. |
|
|
Term
| List the non-acetylated NSAIDs and their therapeutic effects and side effects. |
|
Definition
Diflunisal, Salsalate and Na salicylate.
Competitively inhibit COX. More potent than acetylated and antipyretic activity.
Side effects include nausea, vomiting, upset stomach, GI ulceration. Reyes syndroms in people with connective tissue disorder.
Moderate overdosing can cause nausea, vomiting, tinnitis, tainted vision. It can also cause respiratory alkalosis due to increased production of CO2. |
|
|
Term
| What affects toxic overdoses have on people? |
|
Definition
| The toxic overdose increases acidosis due to acidic property of salicylates. Also, it can impair the renal function and causes accumulation of acid. it can alter carbohydrate metabolism resulting in formation of the pyruvic acid in people. |
|
|
Term
| List carbo and heterocyclic acetic acids |
|
Definition
Indomethacin
Sulindac
Ketorolac
diclonfinac
etodolac
tolmetin |
|
|
Term
|
Definition
| Antiinflammatory and analgesic inhibits the polymorphonuclear movement of leukotrienes. Used as a first line of therapy for gout, and primary NSAID used for cardiac failure in children due to patent ductus arteriosis. Used for the delaying uterine contractions during labor. |
|
|
Term
|
Definition
| It is used for osteoarthiritis, ankylosing spondlysis, rheumatoid arthritis, and acute gout. it has less side effects. It doesn't have any affect on renal fuction and specifically used in patients with poor renal function. |
|
|
Term
|
Definition
| Used as an injection, as effective as morphine but without side effects. Highly ulcerogenic when give by injection. |
|
|
Term
|
Definition
| Limited effect for RA, but effective as a postoperative analgesic. |
|
|
Term
|
Definition
| Greater potency than aspirin as an analgesic and it accumulates in synovial joints. Used for RA, OA and ankylosing spondylitis. Postoperative surgery of cateract. Major inhibitor of cox. Inhibits transminase activity in liver so transaminase activity needs to monitored. |
|
|
Term
| List all the propionic acid derived NSAIDs. |
|
Definition
| Ibuprofen, ketoprofen, naproxen, flurbiprofen, oxaprozin, fenoprofen. Used for RA, OA, and ankylosis spondylisis. Also used for sports related injuries such as bursitis or tendonitis. These are more potent than aspirin and overdose can cause renal failure. |
|
|
Term
| List all the fenamates and their uses? |
|
Definition
Mefenamic acid and meclofenamate.
Used for menustral cramping but not common in US. More common in Europe. |
|
|
Term
| Name all the oxicams and their properties. |
|
Definition
Piroxicam: Better than aspirin, inhibits both COX. Longer duration. Needs only one daily dose.
Meloxicam: Cox II inhibitor and used for RA, OA and ankylosing spondylisis. Longer duration than diclofenac, and piroxicam |
|
|
Term
|
Definition
| Nabumetone, used as prodrug and converted to active form in liver. Induces less gastric irritation or platelet activity. Long half life. |
|
|
Term
| Diaryl substituted pyrazole. |
|
Definition
Celecoxib, rofecoxib, valdecoxib, paracoxib, etoricoxib.
Use for RA, OA and AS. Parecoxib is used parenterally. virtually no platelet activity, 4 fold less gastric ulceration, and risk of stroke or heart attack. |
|
|
Term
|
Definition
Inflammatory: Diseased joints contain neutrophils and macrophages. Also, they have IL-1 and TNF-a.
Immune response: Joints are found to have B and T cells.
can see circulating anti-bodies, cirtrulinated polypeptides and collagen. |
|
|
Term
|
Definition
Aurothioglucose, gold sodium thiomalate, auranofin.
The major component is gold attached to sulfur. It can be used for RA. It can not only slow the progression but can also revert the disease too.
Side affects can occur anytime. Skin lessions, GI disturbances, Proteinuria, thrombocytopenia and leukopenia. |
|
|
Term
|
Definition
Most common antineoplastic agent used in US for chemotherapy. It binds to DHFR and decreases its activity as folate is important enzyme used for the nucleic acid synthesis.
Side effects include suppression of immune, chills, fever, headache, and increased sun sensitivity. |
|
|
Term
|
Definition
Pyrimidine synthesis inhibitor by specific inhibition of DHODH. Uses the DHODH is important enzyme for synthesis of pyrimidine, and lymphocytes use this DHODH and it is inhibited.
Side effects include diarrhea, nausea, vomiting, stomach aches. |
|
|
Term
| List the functions of TNF |
|
Definition
Induce cells adhesion molecule.
Activation of macrophages in response to inflammation.
Activation of metalloprotein complex.
Containment of infection, by promoting clotting in capillaries.
TNF develops immune response to prepare lymphoids to supports lymphocytes. |
|
|
Term
|
Definition
Used for inflammation by blocking the cytokine network.
It is used used for RA, Chron's disease and with methotrexate to treat RA.
Side effects include infusion reaction, allergic reaction and lupus like symptoms. |
|
|
Term
|
Definition
| Binds to TNF55a receptor. binds to TNF and blocks its ability to interact with endogenous receptors. Used for OA, Chrone's disease and for RA in combination with methotrexate. |
|
|
Term
| Successes and failures of anti-TNF |
|
Definition
No affect on asthma.
Makes lupus worse
May help MDI but no solid results. |
|
|
Term
|
Definition
Induces fever
hepatic protein product
PGE2 production
Cartilage breakdown
Bone reabsorption
Augmentation of T cell response |
|
|
Term
|
Definition
Anakinra:
Abatacept: Blocks T cells
rutiximab: Blocks B cell activation |
|
|
