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Pharmtest4...

pharm4

QuestionAnswer
penicillin V [oral; BACTERIOCIDAL] bind PBPs (block transpeptidase --> inhibit cell wall synthesis); USE = Gram+, Gram- cocci, spirochetes; AE = allergy, drug-induced hemolytic anemia
penicillin G [IV; BACTERIOCIDAL] bind PBPs (block transpeptidase --> inhibit cell wall synthesis); USE = Gram+, Gram- cocci, spirochetes; AE = allergy, drug-induced hemolytic anemia
methicillin binds PBPs --> blocking peptidoglycan cross-link; USE = S. aureus; AE = interstitial nephritis; OTHER = b-lactamase resistant; SIMILAR DRUGS = nafcillin, oxacillin, dicloxacillin
ampicillin binds PBPs --> blocking peptidoglycan cross-link; USE = (HELPS = H. influenza, E. coli, Listeria, Proteus, Salmonella) & enterococci; AE = skin rash, colitis; SIMILAR DRUGS = amoxicillin (great ORAL bioavailability)
ticarcillin binds PBPs --> blocking peptidoglycan cross-link; USE = Pseudomonas; AE = allergy; SIMILAR DRUGS = piperacillin, carbenicillin (Take Care of Pseudo)
1st-gen cephs [-CIDAL] binds PBPs --> blocking peptidoglycan cross-link; USE = Gram+ cocci, PEcK (Proteus, E.coli, Klebsiella); AE = disulfiram-like, nephrotoxic, allergy, bleeding (block vit K epoxidase); OTHER = b-lactamase resistant; DRUGS = cephalexin, cefazolin
2nd-gen cephs [-CIDAL] binds PBPs --> block peptidoglycan crosslink; USE = Gram+ cocci, HENPEcKS (H.influenza, Klebsiella, Enterobacter, Neiserria, Proteus, E.coli, Serratia); AE = disulfiram-like, nephrotoxic, allergy, bleed; DRUGS = cefotetan, cefoxitin, cefuroxime
3rd-gen cephs [-CIDAL] binds PBPs --> blocking peptidoglycan cross-link; USE = meningitis, Neiserria (ceftriaxone), Pseudomonas (ceftazidime); AE = disulfiram-like, nephrotoxic, allergy, bleeding (block vit K epoxidase); DRUGS = ceftriaxone, cefotaxime, ceftazidime
4th-gen cephs [-CIDAL] binds PBPs --> blocking peptidoglycan cross-link; USE = Haemophilus, Enterobacter, Neiserria, Pseudomonas, Serratia, S. aureus, S. pneumo; AE = disulfiram-like, nephrotoxic, allergy, bleeding (block vit K epoxidase); DRUGS = cefipime
imipenem binds PBPs --> blocking peptidoglycan cross-link; USE = Enterobacter, gram+ cocci, gram- rods, anaerobes; AE = GI upset, seizures; OTHER = always given with cilastatin!
aztreonam monocyclic b-lactam: binds PBPs --> blocking peptidoglycan cross-link; USE = Gram- rods (Pseudomonas, Serratia, Klebsiella); AE = GI upset; OTHER = used in penicillin allergy & renal insufficiency
vancomycin binds D-ala D-ala terminus --> inhibit transglycosylase (weakened cell wall); USE = Gram+ rods (-static)/cocci (-cidal), MRSA, C. difficile; AE = nephrotoxic, ototoxic, thrombocytopenia, rash; OTHER = resistance via D-ala D-lactate;
cilastin inhibits renal dihydropeptidase I (which inactivates imipenem in renal tubules)
clavulanate inactivate B-lactamases (added to amoxicillin or ampicillin to increase spectrum)
Bacteriostatic ECSTaTiC (erythromycin, chloramphenical, SMX, TMP, tetracycline, clindamycin
Bacteriocidal Very Fucking Proficient At Cell Murder (Vanc, Fluroquinolones, Penicillin, Aminoglycosides, Cephalosporins, Metronidazole)
tetracycline [-STATIC] 30S(aa-tRNA binding); USE = VACUuM THe BedRoom (Vibrio, Acne, Chlamydia, Ureaplasma, Mycoplasma, Tularemia, H. pylori, Borrelia, Rickettsia); AE = teratogen, tooth discoloration, dec bone grow, photosensitive; OTHER = iron/milk/antacids inhibit
Is tetracycline useful in patients with renal failure? No but doxycycline is!
aminoglycosides [-CIDAL] 30S (interfere w/ initiation complex & misreading of mRNA > premature termination in polysome); USE = Gram- rods; AE = nephrotoxic, ototoxic, teratogen (NOT); OTHER = needs O2 for uptake & synergistic w/ b-lactams
chloramphenicol [-STATIC] bind 50S (prevent aa-tRNA binding); USE = bacterial meningitis (SHiN), Rickettsia; AE = gray-baby syndrome (absence of UDP-glucuronyl transferase), dose-dep anemia, dose-indep aplastic anemia; OTHER = inhibit CYP3A4, reaches CNS
macrolides [-STATIC] bind 23S of 50S (inhibit translocation); USE = Gram+ cocci, URT (mycoplasma/legionella), STDs (neisseria/chlamydia - prophylactic neonate eye drops); AE = GI upset, cholestatic hepatitis, long QT w/ VT
clindamycin [-STATIC] binds 50S (inhibit translocation); USE = anaerobic infection above diaphragm aka aspiration or lung abscess, babesiosis; AE = pseudomembranous colitis
30s inhibitors buy AT 30 (aminoglycosides, tetracycline)
50S inhibitors CCELLS at 50 (clindamycin, chloramphenicol, erythromcyin, linezolide, lincomycin, streptogramins)
How would you treat a patient w/ gonorrhea & chlamydia? tetracycline (chlamydia) & ceftriaxone (gonorrhea)
Sulfonamides [-STATIC] PABA analog (competitive inhibitor of dihydropteroate synthase); USE = Gram+/-, Nocardia, Chlamydia; AE = hemolytic anemia (G6PD-D), agranulocytosis, photosensitive, Stevens Johnson, rash, kernicterus
trimethoprim [-STATIC] inhibits dihydrofolate reductase; USE = recurrent UTI, Shigella, Salmonella, PCP; AE = Megaloblastic anemia, leukopenia, granulocytosis
TMP-SMX [-CIDAL] inhibits folic acid synthesis; USE = enteric bacteria, Nocardia, PCP, UTIs, cyclosporiasis/isosporiasis, toxo (prophylaxis); AE = hemolytic anemia, kernicterus, Steven-Johnsons
fluoroquinolones [-CIDAL] inhibits DNA gyrase (topo II); USE = Gram- (urinary/GI/URT/) & Legionella, Mycoplasma, Neisseria; AE = tendonitis & rupture, muscle cramps, teratogen (damage growing cartilage), colitis; OTHER = don't take with dairy/antacids; DRUGS = -oxacin
metronidazole [-CIDAL] forms toxic metabolites in cell & prevent reoxidation of NADH/NADPH; USE = GET GAP (giardia, Entamoeba, Trichomonas, Gardnerella, anaerobes, H. Pylori) & VRE; AE = leukopenia, disulfuram-like, seizures, metallic taste
TB drugs RIPES (rifampgin, INH, Pyrazinamide, Ethambutol, Streptomycin)
M. avium prophylaxis Azithromycin
TB prophylaxis INH
PCP prophylaxis TMP-SMX
Recurrent UTI prophylaxis TMP-SMX
Prophylaxis for dental procedures w/ endocarditis Penicillin
Treatment of VRE streptogramin & linezolid
enfuvirtide binds viral gp41 --> blocks fusion of HIV virion to lymphocytes; USE = HIV; AE = pneumonia, hypersensitivity
amantadine binds M2 (prevent uncoating) & causes dopamine release from nigra striatum; USE = influenza A (90% resistance) & Parksinson's; AE = ataxia, dizziness, slurred speech
rimantadine binds M2 (prevent uncoating); USE = influenza A; AE = ataxia, dizziness, slurred speech; OTHER = does NOT cross BBB
oseltamivir inhibit neuraminidase (no sialic acid cleavage --> needed for viral replication); USE = influenza A & B
zanamivir inhibit neuraminidase (no sialic acid cleavage --> needed for viral replication); USE = influenza A & B
acyclovir guanosine analog - phosphorylated by thymidine kinase (inhibit viral DNA polymerase); USE = HSV 1/2, VZV, EBV
gancyclovir guanosine analog - phosphorylated by viral kinase (inhibit CMV DNA pol); USE = CMV retinitis; AE = pancytopenia
ribavirin guanosine analog - competitively inhibits IMP DH (no guanine nucleotides); USE = RSV, HCV (w/ IFN-a); AE = teratogen, hemolytic anemia
entecavir guanosine analog - inhibits HBV DNA polymerase & reverse transcriptase; USE = HBV
telbivudine thymidine analog - inhibits HBV DNA polymerase & reverse transcriptase; USE = HBV
foscarnet inhibits viral DNA pol (no viral kinase activation); USE = CMV retinitis (2nd line), acyclovir-resistant HSV/VZV; AE = nephrotoxic
zidovudine [NUCLEOSIDE-NRTI] thymidine analog (competes w/ dTTP for binding on HIV-RT); USE = HIV; AE = megaloblastic anemia, neutropenia, lactic acidosis, nausea, insomnia
lamivudine [NUCLEOSIDE-NRTI] inhibit HIV-RT (no DNA synthesis by competing w/ dNTPs); USE = HIV, HBV; AE = GI upset, neutropenia, insomnia, fatigue
abacavir [NUCLEOSIDE-NRTI] inhibit HIV-RT (no DNA synthesis by competing w/ dNTPs); USE = HIV; AE = hepatomegaly, hypersensitivity, lactic acidosis
nevirapine [NNRTI] binds/blocks HIV-RT; USE = HIV; AE = Steven-Johnson, fulminant hepatitis
efavirenz [NNRTI] binds/blocks HIV-RT; USE = HIV; AE = nightmares & CNS disturbances
Protease inhibitors [-NAVIR] inhibit HIV protease (responsible for cleaving precursor into mature -> no replication); USE = HIV; AE = lipodystophies (w/ buffalo hump or central obesity), hyperglycemia, GI disturbances, elevated bili & ARF (both indinavir)
raltegravir HIV integrase strand transfer inhibitor; USE = multi-drug therapy for HIV
Nucleoside-RTIs zidovudine, didanosine, stavudine, abacavir, lamivudine
NNRTIs nevirapine, efavirenz, delavirdine (Never Ever Deliver)
amphotericin B binds ergosterol (forms membrane pores for leakage); USE = Cryptococcus, Blastomyces, Coccidioides, Aspergillus, Histoplasma, Candida, Mucor, Sporothrix; AE = fevers, chills, nephrotoxic, phlebitis, anemia
nystatin [NOT ON LIST] binds ergosterol (forms membrane pores); USE = oral & cutaneous candidiasis; AE = far more toxic than amphotericin B
itraconazole inhibit 14-a-demethylase (no ergosterol made); USE = dermatophytoses (skin) & onychomycosis (nails); AE = CHF, fever, chills, gynecomastia, hepatotoxic
fluconazole inhibit 14-a-demethylase (no ergosterol made); USE = cryptococcal meningitis, Candida esophagitis; AE = fever, chills, gynecomastia, hepatotoxic
terbinafine inhibits squalene epoxidase; USE = topical (tinea cruris/pedis/corporis), oral (tinea capitis & cutaneous candida); AE = local burning, pruritis, contact dermatitis, alopecia, fatigue
caspofungin inhibit B(1,3)-D-glucan synthase (disrupt fungal cell wall); USE = candidiasis & invasive aspergillosis; AE = GI upset
flucytosine cytosine analog --> inhibit thymidylate synthetase (no fungal DNA/RNA); USE = cryptococcus & candida (w/ amphotericin B); AE = bone marrow suppression, hepatotoxic
griseofulvin interfere with microtubule formation; USE = nail/skin/hair infections by Epidermophyton, Micosporum, Trichophyton; AE = teratogenic, carcinogenic, headache, confusion
IFN-B USE = MS
IFN-gamma USE = CGD, osteopetrosis
IFN-a USE = HCV, HBV, Kaposi sarcoma, CML, hairy cell leukemia
INH [BACTERIOSTATIC/-CIDAL] inhibits mycolic acid synthesis; USE = TB; AE = neurotoxic, hepatotoxic, allergies; OTHER = activated via CATALASE PEROXIDASE
Rifampin [BACTERICIDAL] inhibits DNA-dep RNA-pol; USE = TB, meningococcal (H. influenza), leprosy (w/ dapsone); AE = orange body fluids, hepatotoxic, nephritis, thrombocytopenia
Ethambutol [BACTERIOSTATIC] inhibits arabinogalactan synthesis; USE = TB; AE = optic neuritis (red-green blindness)
cyclosporine binds to cyclophilin --> inhibit calcineurin --> block IL-2 expression; USE = organ transplants (GvHD), autoimmune; AE = nephrotoxic, neurotoxic, HTN, hirsuitism, gingival hyperplasia
tacrolimus binds to FKBP --> inhibit calcineurin --> block IL-2 expression; USE = kidney/liver transplant; AE = nephrotoxic, neurotoxic, HTN, inhibit pancreatic B-cell
sirolimus binds to FKBP --> inhibit PI-kinase relates protein kinase mTOR --> lack of IL-2 Tcell response; USE = acute rejection after kidney transplant, restenosis; AE = anemia, thrombocytopenia, hyperlipidemia
mycophenolate mofetil inhibit IMP-DH (no purine synthesis --> no lymphs); USE = renal/heart transplant; AE = diarrhea, leukopenia
leflunomide inhibits dihydroorotate DH (pyrimidine synthesis); USE = active RA; AE =diarrhea, nausea, hepatotoxic;
daclizumab chimeric Ab against IL-2R a-chain (CD25) --> inhibits IL-2 T-cell activation; USE = kidney/cardiac transplants; AE = hypersensitivity
infliximab chimeric Ab against TNF-a; USE = Crohns, UC, RA, psoriasis, ankylosing spondylitis; AE = increased infection
etanercept chimeric Ab (p75-TNF & IgG Fc region) --> takes up free TNF; USE = RA, ankylosing spondylitis, psoriasis; AE = URI, malignancy
Adalimumab binds TNF-a receptor; USE = RA, psoriasis, ankylosing spondylitis
muromonab mouse monoclonal Ab against T-cell CD3 e-chain --> blocks TCR engagement; USE = reversal of organ rejection
azathioprine purine analog metabolized to 6-MP --> inhibits purine synthesis; USE = RA, kidney transplant; AE = GI upset, leukopenia; OTHER = xanthine oxidase metabolizes
anakinra IL-1R antagonist analog; USE = RA; AE = bacterial infections
cyclophosphamide alkylating agent(N-7 of guanine) --> nitrogen mustard; USE = NHL, breast & ovary cancer; AE = pulm fibrosis, cystitic, water retention, alopecia, immunosuppression
lomustine alkylating agent --> nitrosourea; USE = malignant glioma; AE = hematopoietic depression, pulm fibrosis, renal insufficiency, alopecia
carmustine alkylating agent --> nitrosourea; USE = malignant glioma; AE = hematopoietic depression, pulm fibrosis, renal insufficiency, alopecia
busulfan alkylating agent; USE = CML; AE = hyperpigmentation, pulm fibrosis
cisplatin platinum complex --> alkylating agent (form cross-links); USE = genital & head/neck cancer; AE = myelosuppresion, nephrotoxic, ototoxic
procarbazine alkylating agent; USE = Hodgkin dz [MOPP]; AE = MAO inhibitor, carcinogen, myelosuppression
vincristine vinca alkaloids --> binds tubulin (depolymerization of mitotic spindle); USE = ALL, Wilms, Ewings, HL [MOPP]; AE = neuropathy, myelosuppression, stimulate ADH; OTHER = M-phase
vinblastine vinca alkaloids --> binds tubulin (depolymerization of mitotic spindle); USE = testicular/breast cancer, lymphomas; AE = BM suppression; OTHER = M-phase
paclitaxel taxane --> binds tubulin (promote polymerization of mitotic spindle = halts mitosis); USE = breast/ovarian cancer, restenosis; AE = BM suppression, arrhythmias, neutropenia
etoposide inhibit topoisomerase II; USE = small-cell lung cancer, Hodgkins dz; AE = BM suppression, pancytopenia, alopecia
teniposide inhibit topoisomerase II; USE = small-cell lung cancer, Hodgkins dz; AE = BM suppression, pancytopenia, alopecia
doxorubicin DNA intercalation & introduction of ssDNA breaks, also produce oxygen radicals; USE = solid malignancies, HL [ABVD]; AE = cardiac toxicity, BM suppression
daunorubicin DNA intercalation & introduction of ssDNA breaks, also produce oxygen radicals; USE = acute leukemia, neuroblastoma, HL [ABVD]; AE = cardiac toxicity, BM suppression
dactinomycin DNA intercalation; USE = Wilms, Ewings, rhabdomyosarcoma; AE = myelosuppresion
bleomycin binds DNA --> triggers oxygen radical formation; USE = testicular tumors, Hodgkins dz [ABVD], squamous cell carcinomas (non-lung); AE = pulm fibrosis, skin lesions
methotrexate inhibits dihydrofolate reductase; USE = abortifacient, RA, Crohns, ALL, breast cancer, head/neck cancer, osteosarcoma, choriocarcinoma; AE = BM suppression, teratogen, pulm toxicity, hepatotoxic, nephrotoxic
leucovorin supplies reduced folate to bypass inhibited reductase in MTX; USE = reduces BM suppression in MTX administration
5-FU metabolized to 5-FdUMP --> inhibit thymidylate synthase; USE = adenocarcinoma, basal cell carcinoma; AE = BM suppression; OTHER = S-phase specific
cytosine arabinoside metabolized to araCTP --> inhibitor of DNA pol; USE = ALL, AML; AE = BM suppression; OTHER = S-phase specific
6-MP converted to thio-IMP via HGPRT --> inhibit purine synthesis; USE = ALL, AML; AE = BM suppression, hepatotoxic; OTHER = metabolized via S-methylation (TPMT) & oxidation (xanthine oxidase)
6-TG converted to nucleoside monophosphate via HGPRT --> inhibit purine synthesis; USE = ALL; AE = myelosuppression, hepatotoxic; OTHER = metabolized via S-methylation
asparaginase inhibits protein synthesis; AE = lack of secreted proteins
imatinib mesylate inhibit tyrosine kinase enzymes; USE = CML & Ph+ ALL (bcr-abl), GIST (c-kit, PDGF); AE = CHF, myelosuppression
trastuzumab monoclonal Ab against erb-B2 receptor; USE = HER-2+ breast cancer; AE = cardiotoxic
ATRA USE = APML
hydroxyurea inhibits ribonucleotide reductase (no DNA synthesis); USE = myeloproliferative (CML, polycythemia); AE = BM suppression; OTHER = S-phase specific
tamoxifen ER agonist (endometrial), antagonist (breast); USE = postmenopausal ER+ breast cancer; AE = hot flashes, vaginal bleeding, dermatitis, endometrial cancer, thromboemboli
raloxifene ER agonist (bone), antagonist (breast); USE = postmenopausal ER+ breast cance, osteoporosis; AE = hot flashes, vaginal bleeding, dermatitis, thromboemboli
anastrozole aromatase inhibitor; USE = postmenopausal breast cancer
letrozole aromatase inhibitor; USE = postmenopausal breast cancer
exemestane aromatase inhibitor; USE = postmenopausal breast cancer
leuprolide GnRH analog (agonist = pulsatile, antagonist = continuous); USE = infertility (pulsatile), metastatic breast & prostate cancer (continuous)
goserelin GnRH analog (agonist = pulsatile, antagonist = continuous); USE = infertility (pulsatile), metastatic breast & prostate cancer (continuous)
abarelix GnRH antagonist (no LH/FSH); USE = prostate cancer
flutamide androgen antagonist; USE = prostate cancer
bicalutamide androgen receptor antagonist; USE = prostate cancer
Pyrazinamide inhibits mycobacterial FA synthase I gene; USE = TB (short-term); AE = hepatotoxic; OTHER = activated by PYRAZINAMIDASE
Dapsone inhibits folate synthesis; USE = leprosy; AE = hemolysis, GI upset, erythema nodosum leprae
abatacept chimeric Ab (CTLA-4 & IgG Fc region) --> block CD80/86 bindind to CD28 for T-cell; USE = RA
streptogramins [-CIDAL] A (binds & induces 50S conformation change) & B (binds 50S --> inhibit translocation); USE = gram+ cocci; AE = phlebitis, arthralgias, myalgias
Created by: lamsonma