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41 Cards in this Set

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Some examples of Opioid analgesics are: (7)
Morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
Mechanism of Opioid analgesics:
Act as agonists at opioid receptors to modulate synaptic transmission (mu = morphine, delta = enkephalin, kappa = dynorphin)
Clinical use of Opioid Analgesics:
Pain, cough suppression (dextromethorphan), diarrhea (loperamide and diphenoxylate), acute pulmonary edema, maintenance for addicts (methadone)
Toxicities of Opioid analgesics:
Addiction, *respiratory depression, constipation, miosis (pinpoint pupils), additive CNS depression with other drugs
How do you Tx Opioid toxicity?
Naltrexone, naloxone (opioid receptor antagonists) - oxygen is contraindicated if morphine overdose, might worsen respiratory failure
Some examples of NSAIDs are: (4)
Ibuprofen, naproxen, indomethacin, ketorolac
Mechanism of NSAIDs:
Reversible inhibition of COX1 & COX2. Block PG synthesis.
Clinical use of NSAIDs:
Antipyretic, analgesic, anti-inflammatory. Indomethacin used to close PDA (recall: prostaglandins needed to maintain a PDA).
Toxicities of NSAIDs:
Renal damage (acute interstitial nephritis), aplastic anemia, GI distress, ulcers
COX2 inhibitors, celecoxib and valdecoxib, are clinically used for:
Rheumatoid arthritis, osteoarthritis
Mechanism of acetaminophen:
Reversibly inhibits COX, mostly in CNS. Inactivated peripherally.
Clinical use of acetaminophen:
Antipyretic, analgesic.
Toxicity of acetaminophen; antidote:
Overdose --> hepatic necrosis, depletes glutathione and forms toxins in liver; N-acetylcysteine --> regenerates glutathione
Colchicine:
Acute gout. Depolymerizes microtubules, impairing WBC chemotaxis and degranulation. GI side effects. (Note: indomethacin less toxic, more commonly use.)
Probenecid:
Chronic gout. Inhibits reabsorption of uric acid (also inhibits secretion of penicillin).
Allopurinol:
Chronic gout. Inhibits xanthine oxidase, dec. conversion of xanthine to uric acid. Also used in lymphoma and leukemia to prevent tumor lysis-associated urate nephropathy.
Etanercept mechanism:
Recombinant human TNF receptor that binds TNF-a
Etanercept clinical use:
RA, psoriasis, ankylosing spondylitis
Infliximab mechanism:
TNF-a antibody
Infliximab clinical use:
Crohn's, ulcerative colitis, RA, ankylosing spondylitis
Cyclosporine mechanism:
Bind to cyclophilins. Complex blocks differentiation and activation of T-cells by inhibiting calcineurin, preventing production of IL-2 and its receptor
Cyclosporine clinical use:
Supress organ rejection after transplant; select autoimmune disorders
Cyclosporine toxicity:
Predispose to viral infections and lymphoma; nephrotoxic (preventable with mannitol diuresis)
Tacolimus (FK506) mechanism:
Binds to FK-binding protein, inhibiting IL-2 secretion and other cytokines.
Tacrolimus clinical use:
Potent immunosuppressive used in organ transplant recipients
Tacrolimus toxicity:
Nephrotoxicity, peripheral neuropathy, HTN, pleural effusion, hyperglycemia
Azathioprine mechanism:
Antimetabolite derivative of 6-MP that interferes with metabolism and synthesis of nucleic acids. Toxic to proliferating lymphocytes.
Azathioprine clinical use:
Kidney transplant, autoimmune disorders (glomerulonephritis and hemolytic anemia)
Azathioprine toxicity:
Marrow suppression. Active metabolite mercaptopurine is metabolized by xanthine oxidase; this, toxic effect may be inc. by allopurinol.
Aldesleukin =
IL-2 (usef for renal cell CA and metastatic melanoma)
Erythropoietin =
for anemias, esp. in renal failure
Filgrastim =
G-CSF (recovery of bone marrow)
Sargramostim =
GM-CSF (recovery of bone marrow)
a-IFN =
Hepatitis B & C, Kaposi's sarcoma, malignant melanoma, leukemia
b-IFN =
multiple sclerosis
gamma-IFN =
chronic granulomatous disease
Oprelvekin =
IL-11 (thrombocytopenia)
Thrombopoietin =
for thrombocytopenia
Rh3 (D) immune globulin is an immunosuppressive that acts:
at the antigen recognition stage (B and T-cells)
Antilymphocytic globulin and monoclonal anti-T-cell antibodies are immunosuppressives acting at:
antigen recognition, lymphocyte proliferation, and differentiation & synthesis stages
Dactinomycin =
[see First Aid p309]
- intercalates in DNA
- for Wilm's, Ewing's, rhabdomyosarcoma
- myelosuppression toxicity