Musculoskeletal Pharm 2
Terms
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Opioids-morphine, fentanyl, codeine, heroin,methadone, meperidine
1)MOA
2)Uses
3)Toxicity
4)Overdose trt -
1) Agonist at opioid receptor (mu= morphine, delta=enkephalins, kappa=dynorphin)
2) Pain, Cough Suppression (Dextromethorphan), diarrhea, Acute Pulmonary Edema, Trt of Addicts (methadone)
3) Respiratory Depression, Consitpation, Pinpoint Pupils, CNS depression
No tolerance to constipation and pinpoint pupils
4) Naloxone, Naltexone -
NASAIDs- Ibuprofen, Naproxen, Indomethacin, Ketorolac
1)MOA
2)Uses
3)Toxicity -
1) Reversibly inhibit COX1 & COX2 to prevent prostaglandin synthesis
2) Antipyretic, anaglesic, anti-inflammatory, closes PDA (indomethicin)
3) renal damage, aplastic anemia, GI ulcers -
COX2 Inhibitors (celecoxib, valdecoxib)
1)MOA
2)Uses
3)Toxicity -
1) Selective inhibition of COX2 which is found in inflammatory cells (COX1 is involved in GI mucosa) -->prevents pain, but no risk of ulcers
2) Rheumatoid and Osteoarthritis
3) Similar to NSAIDS but less GI problems -
Acetaminophen
1)MOA
2)Uses
3)Toxicity
4)Antidote -
1) Reversible COX inhibitor, mostly CNS --> inactivated peripherally
2) Antipyretic, Analgesic, no anti-inflammatory
3) Overdose causes hepatic necrosis via depletion of gluathione --> allows free radical damage in liver and in renal medulla (don't combine acetominophen with aspirin)
4) N-acteylcysteine regenerates glutathione -
Colchicine
1)MOA
2)Uses
3)Toxicity -
1) Depolymerizes microtubules to impair leukocyte chemotaxis and degranulation --> blocks pain
2) Pain in acute gout attack
3) GI side effects -
Probenecid
1)MOA
2)Uses
3)Toxicity -
1) Blocks reabsorption of uric acid in the kidney and increases penicillin excretion
2)Chronic Gout -
Allopurinol
1)MOA
2)Uses
3)Toxicity -
1) Blocks Xanthine Oxidase to decrease conversion of xanthine --> Uric Acid.
2)Chronic Gout,and Lymphoma/Leukemia where increased cell turnover leads to uricemia
3) Blocks 6-mercaptopurine excertion --> lower dose -
Etanercept
1)MOA
2)Uses -
1) Recombinant form of TNF that bind TNF-alpha
2) Rheumatoid Arthritis, Psoriasis, Ankylosing Spondylitis -
Infliximab
1)MOA
2)Uses -
1) Antibody to TNF-alpha
2) Crohn's disease, Rheumatoid Arthritis, Ankylosing Spondylitis -
Cyclosporine
1)MOA
2)Uses
3)Toxicity -
1) Binds to cyclophilines to prevent differentiation and activation of T-cells (no IL-2 production)
2) Suppression of organ rejection
3) Predisposed to viral infxn, lymphoma, and it is nephrotoxic -
Tacrolimus
1)MOA
2)Uses
3)Toxicity -
Similar to cyclosporine, it blocks IL-2 and other cytokine release
2) Potent immunosuppressant in transplant
3) Significant nephrotoxicity, peripheral neuropathy, HTN, pleural effusion -
Azathioprine
1)MOA
2)Uses
3)Toxicity -
1) derivative of 6-MP that inferferes with nucleic acid production, so it is toxic to proliferating Lymphocytes
2) Kindney transplants, autoimmune disorders
3) Bone marrow suppression, toxic effects are worsened by Allopurinol