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71 Cards in this Set

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