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84 Cards in this Set
- Front
- Back
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Opioid analgesics:
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Morphine
Methadone Meperidine Fentanyl Codeine Heroine Dextromethorphan |
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Where do Opioid analgesics act? How?
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At Mu receptors - agonists to modulate synaptic transmission
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What is the agonist of
-Mu opioid receptors -Delta opioid receptors -Kappa opioid receptors |
Mu = morphine/endorphins
Delta = Enkephalin Kappa = dynorphin |
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What is Dextromethorphan used for?
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Cough suppression
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What are Loperamide and Diphenoxylate used for?
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Anti-diarrhea
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What is Methadone used for?
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Methadone maintainance for opioid addicts
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What are 2 other uses of Opioid analgesics?
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-Pain
-Acute pulmonary edema |
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Major risk of opioid analgesics:
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Addiction
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4 signs of opioid toxicity:
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-Constipation
-Miosis - pupil constriction -Respiratory depression - additive with other CNS depressents |
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To what 2 side effects does tolerance NOT develop with opioid analgesics?
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Constipation
Miosis |
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Treatment for Opioid toxicity:
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-Naloxone
-Naltrexone |
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What is CONTRAINDICATED in morphine overdose? Why?
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Oxygen therapy - may lead to MORE respiratory failure
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Pathway that makes Leukotrienes:
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Lipoxygenase
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LTB4
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Chemotactic for neutrophils
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LTC4/D4/E4
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-Bronchoconstriction
-Vasoconstriction -Sm muscle contraction -Increased vasc permeability |
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How do Corticosteroids affect arachidonic acid metabolism?
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-Inhibit PLA2 from releasing AA from the membrane
-Inhibit Cox2 synthesis |
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5-lipoxygenase inhibitor
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Zileuton
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Leukotriene receptor antagonists:
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Zafirlukast/Montelukast
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What Leukotriene receptors do Zafirlukast and Montelukast specifically inhibit and what is the effect?
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Receptors for LTC4/D4/E4 - inhibits bronchoconstriction
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How do corticosteroids inhibit Cyclooxygenase?
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By inhibiting the PROTEIN SYNTHESIS of COX2
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What are 3 agents that inhibit the COX enzymes by direct binding?
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-NSAIDS
-Acetominophen -COX2 inhibitors |
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4 main NSAIDS to know:
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-Naproxen
-Indomethacin -Ketorolac -Ibuprofen |
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How do the NSAIDS affect cyclooxygenases?
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Reversibly inhibit both Cox1/2
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What is the effect of inhibiting the COX enzymes?
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No Prostaglandin synthesis
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What does Aspirin do?
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Irreversibly inhibits both enzymes
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What are the uses of NSAIDS? 3 effects:
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-Anti-pyrretic
-Anti-inflammatory -Analgesic |
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What is Indomethacin's specific use?
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Close a PDA
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4 toxic side effects of NSAIDS:
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-Renal damage
-Aplastic anemia -GI distress -Ulcers |
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Cox-2 inhibitors:
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Celecoxib
Valdecoxib |
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Mechanism of Cox2 inhibitors:
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Reversible inhibition of Cox-2 specifically
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What is the rationale for only inhibiting Cox2?
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Cox2 is what is responsible for inflammation and pain in inflammatory cells; Cox1 keeps cytoprotective effects on the gastric mucosa - no ulcers!
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2 clinical uses of the cox2 selective inhibitors (celecoxib and valdecoxib)
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Rheumatoid arthritis
Osteoarthritis |
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What is an increased risk of the Cox2 inhibitors?
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THROMBOSIS - overactive Cox1 in platelets produces too much txa2
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Mechanism of Acetominophen:
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Reversible inhibition of Cox in the CNS
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Why doesn't Acetominophen do much in the periphery?
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Its inactivated in the periphery
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How do the effects of Acetaminophen compare to the NSAIDS?
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-Antipyrretic
-Analgesic But not anti-inflammatory |
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What does Acetaminophen overdose cause? Why?
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HEPATOTOXICITITY - overwhelms Cyp2E1 and GSH availability - overproduction of NAP1Q
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Antidote for Acetaminophen toxicity; how does it work?
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N-acetylcysteine - regenerates GSH
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What are the 4 gout drugs?
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-NSAIDS
-Colchicine -Allopurinol -Probenacid |
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Which drugs are used for acute vs chronic gout?
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Acute = Colchicine
Chronic = Allopurinol/Probenecid |
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Mechanism of Colchicine:
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Depolymerizes Microtubules - impairs leukocyte chemotaxis and degranulation; thus less inflammatory response to the
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What is an adverse side effect of Colchicine?
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GI toxicity - esp if given orally - severe diarrhea
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So what is generally used more often than Colchicine for anti-inflammation in Gout?
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Indomethacin
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How does Probenecid treat chronic gout?
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Inhibits reabsorption of uric acid from the kidney tubule by competing for OAT
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What dose Probenecid inhibit SECRETION of at the nephron?
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Penicillin
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What else inhibits reabsorption of uric acid from the kidney tubule?
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High dose salicylates
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What exacerbates Gout by inhibiting tubular SECRETION of uric acid?
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Thiazide diuretics
Low dose salicylates |
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So when are Salicylates good/bad for Gout?
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Good: in HIGH doses
Bad: in LOW doses |
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What is the mechanism of Allopurinol?
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Inhibits Xanthine oxidase which inhibits hypoxanthine/xanthine conversion to uric acid
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In what other conditions is Allopurinol used to prevent Urate nephropathy?
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Lymphoma and Leukemia
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What is Etanercept?
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Recombinant TNF-a receptor - acts as a sink for TNF
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What 3 conditions are treated with Etanercept?
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-Psoriasis
-Rheumatoid arthritis -Ankylosing spondylitis |
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What is Infliximab?
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TNF-a antibody
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What are 3 clinical uses of Infliximab?
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-Crohn's disease
-Rheumatoid arthritis -Ankylosing spondylitis |
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How can you remember the uses of Etanercept/Infliximab?
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RAPE IRAC
RA/Anky spond/Psoriasis - Etan RA/Anky spond/Crohn's - Inflix |
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What are 2 ways that Prednisone is an immunosuppressant?
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1. Inhibits cytokine production via Lipocortin/PLA2 inhibition
2. Sequesters cells - prevents chemotaxis and tissue injury |
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How does Cyclosporine inhibit immune reactions?
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-Binds cyclophilin; complex inhibits Calcineurin which decreases IL2 and IL2 receptor production; no Tcell differentn and activation.
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What are the 2 main clinical uses of Cyclosporine?
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-Prevents Transplant rejection
-Some autoimmune diseases |
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What are 3 TOXIC effects of Cyclosporine?
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-Increased Viral infections
-Risk of LYMPHOMA -Nephrotoxicity |
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How is Cyclosporine NEPHROTOXICITY avoided?
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By mannitol diuresis
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What is the mechanism by which TACROLIMUS is immunosuppressive?
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Binds FK-binding protein; inhibits IL2 and other cytokine secretions
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What is the clinical use of Tacrolimus?
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Potent immunosuppressive to prevent TRANSPLANT rejection
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What are the significant toxic side effects of Tacrolimus?
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-Nephrotoxicity
-Peripheral neuropathy -Hypertension -Pleural effusions -Hyperglycemia |
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How can you remember the toxic side effects of Tacrolimus?
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NPH Prevents Hyperglycemia
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What is Azathioprine?
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An Antimetabolite derivative of 6-mercaptopurine
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What is the mechanism of Azathioprine in immunosuppression?
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Prevents Metabolism/synthesis of nucleic acids and thus toxic to proliferating lymphocytes
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What are the 2 main uses of Azathioprine clinically?
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-Prevent kidney graft rejection
-Autoimmune diseases - HA and glomerulonephritis |
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What is the toxic side effect Azathioprine can have?
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BONE MARROW SUPPRESSION (this is not an effect of cyclosporine or tacrolimus)
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What enzyme metabolizes the active metabolite of Azathioprine?
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Xanthine oxidase
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So what can cause toxicity of Azathioprine by preventing metabolism of its metabolite?
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Allopurinol
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Aldesleukin:
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Recombinant Il-2
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2 uses of Aldesleukin:
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-Renal cell carcinoma
-Metastatic melanoma |
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Erythropoietin
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Recombinant EPO - Epoetin
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Use of Epoetin
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Anemias - esp in renal failure
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Filgrastim
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Recombinant Granulocyte CSF
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Filgrastim is used for:
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Bone marrow recovery after cancer therapy
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Sargramostim:
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Recombinant Granulocyte-Macrophage CSF
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Sargromastim is used for:
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Bone marrow recovery
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alpha-Interferon 4 uses:
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Hep B/C
Kaposi's sarcoma Leukemias Malignant melanoma |
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B-Interferon's use:
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Multiple sclerosis
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gamma-Interferon's use:
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CGD - Chronic granulomatous disease
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Oprelvekin is:
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Recombinant IL-11
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Oprelvekin is used for:
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Thrombocytopenia
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Thrombopoeitin is used for:
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Thrombocytopenia too
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