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71 Cards in this Set
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first generation sulfonylureas
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tolbutamide, chlorpropamide; block K+ channels of β cells --> depolarization --> ↑Ca+ --> release of insulin
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second generation sulfonylureas
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glipizide, glyburide, glimepiride; block K+ channels of β cells --> depolarization --> ↑Ca+ --> release of insulin
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side effects of sulfonylureas
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hypoglycemia, weight gain, sulfa allergy, hypoglycemia with cimetidine (fisrt generation), disulfram-like (first generation)
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hypoglycemia
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paresthesia, lethargy, confusion, sweats, tremors, tachychardia, coma, seizures
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metformin
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↓ gluconeogenesis; can be used in patients with no islet function; side effect: lactic acidosis
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glitazones
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↑ target cell sensitivity to glucose via PPARs; side effects: weight gain, edema, hepatotoxicity, CV toxicity
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α-glucosidase inhibitors
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acarbose, miglitol; no hypoglycemia; inhibit brush border α-glucosidase; side effects: GI disturbance
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xenatide
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GLP-1 receptor full agonist --> augments insulin secretion; hypoglycemia when used with sulfonylureas
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orlistat
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inhibits pancreatic lipases; used in obesity; side effects: steatorrhea, fat malabsorption
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sibutramine
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serotonin/norepinephrine reuptake inhibitor; obesity management; side effects: ebesity, tachychardia
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propylthiouracil/methimazole
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inhibits organification and coupling; side effects: agranulocytosis, aplastic anemia, skin rash
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anastrozole
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aromatase inhibitor --> ↓ estrogen synthesis; use: estrogen-dependant postmenopausal breast cancer
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clomiphene
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↓ feedback inhibition --> ↑FHS/LH --> ↑ovulation; fertility drugs; adverse effects: multiple births
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tamoxifen/raloxifene
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estrogen receptor agonist in bone; estrogen receptor antagonist in breast; partial agonist in endometrium
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progestins/estrogens/oral contraceptives
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medroxyprogesterone, norethindrone, desogestrel, estrogens; ↑progesterone --> ↓LH/FSH; side effects: ↑LDL ↓HDL, glucose intolerance, androgenic, antiestrogenic
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mifepristone
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progesterone antagonist --> abortifacient
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methyltestosterone
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ilicit in athletics, used in male hypogonadism; side effects: premature closure of epiphysis, jaundice, aggression
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flutamide
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androgen receptor blocker; used in prostate cancer
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leuprolide
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GnRH analog; prostate cancer
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finasteride
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5-α-reductase inhibitor --> ↓dihydrotestosterone; BPH, baldness; teratogenic
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biphosphonates
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use in Paget, osteoporosis; alendronate, etidronate, pamidronate
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energy source of RBC
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anaerobic glycolysis --> lactate (90%) and HMP shunt (10%)
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antithrombin III
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activated by heparin; inactivates thrombin, Ixa, Xa, Xia
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tPA
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tissue plasminogen activator; fibrinolytic; generates plasmin from plasminogen; ↑PT and ↑PTT
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protein C
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inactivates factors Va and VIIIa --> anticoagulation
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factor V leiden
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mutation causes resistance to activated protein C --> hypercoagulable state
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warm agglutinin
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IgG; AIHA seen in SLE, CLL and methyldopa; "Warm weather is GGGreat, Cold ice cream MMM"
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cold agglutinin
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IgM; AIHA seen in mycoplasma or infectious mononucleosis infections; "Warm weather is GGGreat, Cold ice cream MMM"
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heparin
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activates antithrombin III; measure PTT; use: PE, DVT, AMI, DIC; side effects: bleeding, heparin-induced thrombocytopenia, hypersensitivity
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protamine sulfate
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rapid reversal of heparinization; binds negatively-charged heparin
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antithrombin III
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serine protease inhibitor binds to activated clotting factors to inactivate them
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warfarin antidote
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vitamin K
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warfarin
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epoxide reductase inhibitor decreases vitamin K-dependant factors; slow onset; check PT; SE: skin necrosis; metabolized by P450
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warfarin-induced skin necrosis
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protein C and VIIa have the shortest half-lives --> transient inactivation of protein C and extrinsic pathway while intrinsic path is stil active due to longer half-lives of factors --> hypercoagulable state --> thrombosis
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platelet activators
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TxA2, ADP, 5HT --> ↑expression of GpIIb/IIIa receptors
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platelet deactivators
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prostacyclin, cAMP, clopidogrel gpIIb/IIIa blockers
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clopidogrel
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blocks platelet ADP receptors --> ↓platelet activation; SE neutropenia
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abciximab
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gpIIb/IIIa antagonist --> ↓platelet aggregation
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methotrexate
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inhibits dihydrofolate reductase --> ↓dTMP --> ↓DNA synthesis; uses: leukemias, lymphomas, abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis
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5-FU MOA
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inhibits thymidylate synthase --> ↓dTMP --> ↓DNA synthesis; uses: colon cancer and solid tumors, basal cell carcinoma
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6-MP
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activated by HGPRTase --> blocks purine synthesis; uses: leukemias, lymphomas (except CLL or Hodgkin); metabolized by xanthine oxidase (↑toxicity with allopurinol); hepatotoxic
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cytarabine (ara-C)
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DNA polymerase inhibitor; use: AML
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cyclophosphamide
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alkylating agent ---> attacks guanine N7 --> denatures DNA; uses: non-Hodgkin lymphoma, ovarian and breast cancer, neuroblastoma
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cisplatin
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alkylating agent cross-links DNA strands; uses testicular, bladder, ovary and lung carcinomas; nephrotoxic
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doxorubicin
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intercalates DNA inhibits topoisomerase II; uses: Hodgkin's, myelomas, solid tumors; dilated cardiomyopathy
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actinomycin D (dactinomycin)
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intercalates DNA inhibits topoisomerase; uses: Wilm's tumor, Ewing's sarcoma. Rhabdomyosarcoma
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bleomycin
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formation of free radicals cause breaks in DNA strands; uses: testicular cancer, lymphomas; pulmonary fibrosis
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hydroxyurea
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inhibits ribonucleotidde reductase --> decreases DNA synthesis; uses: melanoma, CML, sickle cell disease
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tamoxifen
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estrogen receptor antagonist in breast, agonist in bone; use: breast cancer
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vincristine
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bind tubulin during M phase blocking polymerization of microtubules and formation of mitotic spindle; uses: lymphoma, Wilm's tumor, choriocarcinoma; neurotoxic
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cyclosporine
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binds cyclophillin --> ↓calcineurin --> ↓IL-2, IL-3, IFN-gamma; use in organ transplants
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tacrolimus
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inhibits calcineurin --> ↓IL-2, IL-3, IFN-gamma; use in organ transplants
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infliximab
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monoclonal Ig against TNF; use in rheumatoid arthritis and Crohn's
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trastuzumab
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erb-B2 antagonist; use in breast cancer
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dacliximab
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blocks IL-2 receptors; use in kidney transplants
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etanercept
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Recombinant TNF receptor binds TNF; uses: rheumatoid arthritis, psoriasis, ankylosing spondylitis
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first generation H1 blockers
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reversible; diphenhydramine, chlorpheniramine; uses: allergy, motion sickness, sleep aid; SE: sedation, antimuscarinic and anti-alpha adrenergic effect
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2nd generation H1 blockers
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loratadine, fexofenadine, desloratadine, cetirizine; use: allergy; less sedation
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salmeterol
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beta2 agonist; long-acting; tremor and arrhythmias
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albuterol
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beta2 agonist; use in acute attack
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theophylline
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inhibits phosphodiesterase and increases cAMP --> bronchodilation; cardiotoxic, neurotoxic, narrow therapeutic index; metabolized by P450
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ipratropium
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antimuscarinic used in asthma and COPD
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cromolyn
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not effective in acute attack; prophylaxis
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zileuton
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5-lipoxygenase inhibitor --> decreases leukotrienes
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lukasts
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leukotriene receptor antagonists; aspirin-induced asthma
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guainfenesin
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expectorantt; doesn’t suppress cough reflex
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colchicine
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use in acute gout; depolymerizes tubulin microtubules, prevents leukocyte chemotaxis and degranulation; SE: GI disturbances
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probenecid
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use in chronic gout; inhibits reabsorption of uric acid in PCT
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allopurinol
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use in chronic gout and leukemia; inhibits xanthine oxidase and decreases uric acid.
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imatimab
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inhibitor of BCR/Abl tyrosine kinase of CML without apoptosis
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rituximab
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monoclonal Ab against CD20 used in B-cell lymphomas
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