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41 Cards in this Set

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  • Back
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
Acute gout. Depolymerizes microtubules, impairing WBC chemotaxis and degranulation. GI side effects. (Note: indomethacin less toxic, more commonly use.)
Chronic gout. Inhibits reabsorption of uric acid (also inhibits secretion of penicillin).
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