Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
131 Cards in this Set
- Front
- Back
|
therapy duration depends on?
|
pathogen
site of infection host factors |
|
|
what diseases have precise data on duration of therapy?
|
"STaGS"
strep pharyngitis TB gonorrhea syphilis |
|
|
bactericidal drugs?
|
aminoglycosides
metronidazole quinolones quinupristin/dalfopristin polymixin vancomycin rifampin pyrazinamide bacitracin beta-lactams isoniazid |
|
|
what types of drugs are indicated in immunosuppressed pts?
|
bacteriocidal
|
|
|
concentration dependent drugs
1) what are they 2) how do you dose them 3) are they bacteriostatic or bacteriocidal? |
[ ] dependent drugs
1) aminoglycosides - inhibit protein synthesis quinolones - inhibit DNA gyrase/topoisomerase 2) once daily dosing 3) bacteriocidal |
|
|
therapy duration depends on?
|
pathogen
site of infection host factors |
|
|
what diseases have precise data on duration of therapy?
|
"STaGS"
strep pharyngitis TB gonorrhea syphilis |
|
|
bactericidal drugs?
|
aminoglycosides
metronidazole quinolones quinupristin/dalfopristin polymixin vancomycin rifampin pyrazinamide bacitracin beta-lactams isoniazid |
|
|
what types of drugs are indicated in immunosuppressed pts?
|
bacteriocidal
|
|
|
concentration dependent drugs
1) what are they 2) how do you dose them 3) are they bacteriostatic or bacteriocidal? |
[ ] dependent drugs
1) aminoglycosides - inhibit protein synthesis quinolones - inhibit DNA gyrase/topoisomerase 2) once daily dosing 3) bacteriocidal |
|
|
time dependent drugs
1) what are they 2) how do you dose them 3) are they bacteriostatic or bacteriocidal? |
time dependent drugs
1) beta lactams - inhibit cell wall synthesis vancomycin - inhibit cell wall synthesis 2) serum [ ] must remain > MBC 3) bacteriocidal |
|
|
antimicrobials are preferred to be administered how?
|
orally
|
|
|
in what pt populations would you give IV antimicrobials?
|
critically ill
N/V/gastrectomy bacterial meningitis/endocarditis |
|
|
what drug combos would you use to rx enterococcal endocarditis?
|
penicillins/vancomycin + aminoglycosides
combo makes it bactericidal |
|
|
what prophylactic drugs would you use for emergency colorectal surgery/colorectal obstruction/appendectomy?
|
cefoxitin
cefotetan |
|
|
what prophyllactic drugs would you use in elective colorectal surgery?
|
oral erythromycin
neomycin cephalosporin |
|
|
what are the mechanisms of antimicrobial synergism
|
1) block sequential steps in metabolic sequence
2) inhibit enzymatic inactivation 3) enhance antimicrobial agent uptake |
|
|
what is the DOC for surgical prophyllaxis
|
cefazolin
|
|
|
what is the requirement of antimicrobial drugs in surgical prophylaxis?
|
[ ] of agent > MIC @ time of incision
|
|
|
nonsurgical prophyllaxis of suspected exposure of anthrax
|
ciprofloxacin, doxycycline
|
|
|
nonsurgical prophylaxis of close contact w/ cholera
|
tetracycline
|
|
|
nonsurgical prophylaxis of dental procedures in @ risk pt for endocarditis
|
amoxicillin
clindamycin |
|
|
nonsurgical prophylaxis of HIV blood exposure by needle stick
|
zidovudine
lamivudine |
|
|
nonsurgical prophylaxis of recurrent otitis media infection
|
amoxicillin
|
|
|
what antiprotozoal drugs are used for malaria prophylaxis
|
chloroquine
mefloquine pyrazinamide proguanil doxycycline |
|
|
which species is responsible for most disease and death of malaria worldwide
|
Plasmodium falciparum
|
|
|
what anti-protozoal drug rx tissue schizonticides in malaria?
|
primaquine
|
|
|
what anti-protozoal drug rx blood schizonticides in malaria?
|
chloroquine
mefloquine quinine pyrimethanine proguanil antibiotics |
|
|
what anti-protozoal drug rx gametocides in malaria?
|
primaquine
quinine (P.vivax, ovale) |
|
|
what drugs disrupt polymerization of heme -> hemozoan to lyse RBC's and the bug?
|
chloroquine
mefloquine quinine |
|
|
contraindications to chloroquine
|
psoriasis/porphyria
retinal abnormalities kaolin / antacids reduce absorption myopathy SAFE IN PREGNANCY AND CHILDREN |
|
|
against what does quinine eradicate?
|
all 4 species blood schizo
ovale+vivax gametocytes NOT ACTIVE AGAINST LIVER STAGE PARASITES |
|
|
quinine is effective against what species?
how do you administer |
P. falciparum
give with doxycycline to reduce duration of use to 3 days (toxicity) |
|
|
AE of quinine
|
tinnitus
headache nausea deafness dizziness flushing visual disturbances |
|
|
contraindication quinine
|
cardiac abnormalities - QT prolongation
taking with or recently taken mefloquine - cardiac arrest/convulsions |
|
|
what do you give chloroquine resistant strains of P. falciparum
|
mefloquine
|
|
|
what do you give to rx severe infections.. why
|
quinine
rapid activity, less likely resistance |
|
|
AE mefloquine
|
nausea
vomiting dizziness sleep, behavioral disturbances |
|
|
contra mefloquine
|
epilepsy
psychiatric disorders quinine/quinidine cardiac conditions - arrythmias G6PD deficiency (decreased NADPH/GSH levels) |
|
|
primaquine is effective against what species
|
P. ovale, vivax
liver forms gametocides |
|
|
AE primaquine
|
hemolysis in G6PD def
intestinal distress methemoglobinemia |
|
|
contra primaquine
|
pregnancy
myelosuppression |
|
|
pyrimethamine MOA
|
inhibit folate metabolism in parasite (dihydrofolate reductase)
|
|
|
proguanil MOA
|
inhibit folate metabolism in parasite (dihydrofolate reductase)
|
|
|
ab effective against all 4 species of erythrocytic schizonts
|
tetracycline
doxycycline clindamycin azithromycin |
|
|
what ab do you give in chloroquine resistance malaria
|
clindamycin
|
|
|
what antiprotozoal drugs are effective against all 4 species of erythocytic schizonts
|
quinine
pyrimethamine proguanil antibiotics |
|
|
what are the 4 stages of amebiasis
|
asymptomatic intestinal infection
mild to moderate intestinal colitis severe intestinal infection (colitis) liver abcess |
|
|
what drugs to you give to rx asymptomatic intestinal infection of amebiasis
|
luminal amebicide
iodoquinol paromomycin |
|
|
what drugs to you give to rx amoebic colitis of amebiasis
|
metronidazole + luminal amoebocide (iodoquinol, paromomycin)
|
|
|
what drugs to you give to rx extraintestinal infections of amebiasis
|
metronidazole + luminal amoebocide (iodoquinol, paromomycin)
|
|
|
metronidazole is the DOC 4?
|
amebiasis
trichomoniasis giardiasis |
|
|
metronidazole MOA
|
protozoal enzymes reduce the nitro grp to produce toxic, nitro-free radicals that damage DNA and protein
|
|
|
metronidazole caution?
|
H2 blockers (cimetidine)
peptic ulcers toxic b/c block metabolic pathway of liver *need to lower dose* |
|
|
paromomycin contra?
|
renal problem - accumulates with renal insufficiency leading to toxicity
ulcers - increases amt in circulation - *reduce dosage* |
|
|
what drug do you use to rx giardiasis in kids?
|
nitazoxanide
|
|
|
what drug do you use to rx giardiasis in adults
|
metronidazole
|
|
|
MOA nitazoxanide
|
active metabolite : tizoxanide
inhibits pyruvate: ferredoxin oxidoreductase pathway (needed in anaerobic energy metab in protozoa) |
|
|
american trypanosomiasis
symptoms and rx |
cardiomyopathy
common in infants transmitted by feces rx: nifurtimox |
|
|
african trypanosomiasis - gambiense
symptoms and rx |
slow to enter CNS
transmitted by tsetse fly causes sleeping sickness rx: suramin (IV), petamidine in early stages |
|
|
african trypanosomiasis - rhodensiense
symptoms and rx |
early invasion CNS
fatal if not rx Rx: eflornithine (less toxic than melarsoprol), melarsoprol |
|
|
melarsoprol MOA
|
react with trypanothione *reducing agent inside parasite* --> makes parasite susceptible to oxidative stress
affect parasite replication |
|
|
why is melarsoprol not given prophylactically
|
contains arsenic -> toxic
readily [ ] in parasite and eliminated rapidly |
|
|
eflornithine MOA
|
selective irreversible inhibitor of ornithine decarboxylase
inhibits replication |
|
|
nifurtimox MOA
|
generates oxygen radicals which are toxic to parasite (lacks catalase)
|
|
|
leishmaniasis
1) transmitted by? 2) 2 forms of infection? 3) geographic area? |
1) sandfly
2) mucosal, visceral 3) seen around mexican border |
|
|
rx leishmaniasis
|
sodium stibogluconate - inhibit glycolysis/FA metab
reduces production ATP/GTP miltefosine - inhibit RNA synthesis |
|
|
AE nifurtimox
|
anorexia
vomiting neuropathy pancytopenia |
|
|
AE sodium stilbogluconate
|
bone marrow suppression
chemical pancreatitis prolonged QT rash |
|
|
AE metronidazole
|
headache,
nausea, metallic taste, neuropathy |
|
|
AE suramin
|
nausea
vomiting shock |
|
|
AE melarsoprol
|
fever
phlebitis neuropathy reactive encephalopathy |
|
|
what is the helminth that accounts for most of the infections of the world's population
|
nematode
MCC=ascaris |
|
|
albendazole
1) DOC 2) MOA |
1)nematodes:
ascariasis, trichuriasis, hookworm, pinworm 2) inhibits beta tubulin microtubule synthesis in worm |
|
|
Diethylcarbamazine
1) rx for? 2) half life longer in acidic/alkaline urine? 3) MOA |
1) filariasis, loiasis, tropical eosinophilia
2) alkaline 3) immobilizes microfilaria, displacing them from tissue so cleared by host defenses *alters arachidonic acid pathway in worm *if knock out INOS/COX2 in human host not protected* |
|
|
Ivermectin
1) rx? 2) MOA? 3) drug has __affinity for worm ___ |
1) strongloidiasis, onchocerciasis, lymphatic filariasis (elephant leg), cutaneous larva migrans
2) activates glutamate-gated Cl channels in worm, enhances GABA signals in peripheral nerves - CAUSE WORM FLACCID PARALYSIS 3) 100x, GABA |
|
|
what is the Mazzotti rxn?
symptoms? DOC?? |
hypersensitivity response from microfilariae (parasitic antigens) targeted by rx drug
fever, pruitis, arthralgia, headache DOC=corticosteroids |
|
|
Mebendazole
1) rx? 2) MOA? 3) contra? |
1) nematode infections
ascariasis, trichuriasis, hookworm, pinworm 2) inhibits microtubule synthesis 3) pregnancy |
|
|
praziquantel
1) rx for? 2) MOA? |
1) schistosome,
TREMATODES (paragonimiasis, clonorchiasis, schistosomiasis) cestodes 2) increases Ca permeability leading to SPASTIC PARALYSIS - dispels worm |
|
|
pyrantel pamoate
1) rx for? 2) active against? 3) MOA? |
1) pinworm, ascaris, hookworm (NO TRICHURIASIS / STRONGYLOIDIASIS)
2) active against luminal organisms 3) neuromuscular blocking agent - produces depolarization of NMJ blockade - SPASTIC PARALYSIS AND EXPULSION - Ach release, cholinesterase inhibition |
|
|
how do you reverse drug resistance?
|
verapamil inhibits Ca channel transporter
|
|
|
alkylating agents
1) MOA 2) drug resistance |
1) transfer alkyl grp to N7 position of guanine within DNA
2) increased DNA repair decreased permeability to drug increased glutathione production |
|
|
Cyclophosphamide
1) MOA 2) contra |
1) must be converted to active metabolite by liver P450
in non-hepatic tissue, nonenzymatic conversion to other cytotoxic forms 2) liver problems |
|
|
carmustine
1) MOA 2) DOC for? 3) unique pharmacokinetics |
1) requires nonenzymatic conversion to active form
2) glioma 3) highly soluble, crosses BBB |
|
|
procarbazine
1) MOA 2) doc for? |
1) inhibit DNA, RNA, protein synthesis via alkylation - generates azoprocarbazine and H2O2--> cause strand breaks
2) hodgkin's dz |
|
|
Cisplatin
1) MOA 2) AE 3) rx for? |
1) crosslinks DNA @ N7 guanine
2) nephrotoxicity (need aggressive IV hydration/diuretics) and severe nausea 3) rx testicular, ovarian, bladder cancer |
|
|
name 6 antimetabolites
|
MERCAP CLAD METH in a FLUORO-CYTA CAPE
mercaptopurine cladribine methotrexate fluorouracil cytarabine capecitabine |
|
|
Methotrexate
1) MOA 2) AE 3) drug resistance mech |
bind to dihydrofolate reductase catalytic site
interferes with DNA, RNA, protein synthesis polyglutamates of methotrexate are [ ] inside the tumor cells 2) toxic to normal and abnormal cells - requires leucovorin rescue 3) decrease drug transport mutation/change formation polyglutamate overexpress DHFR reduced affinity of MTX DHFR |
|
|
what is leucovorin rescue
|
give folinic acid to bypass the inhibited dihydrofolate reductase so cell can recover from methotrexate
|
|
|
what are 2 purine antagonists
|
mercaptopurine
cladribine |
|
|
mercaptopurine (6-MP)
1) MOA 2) drug resistance 3) caution when given with allopurinol? |
1) decrease purine synthesis by being converted to HGPRT
2) drug resistance - decreased HGPRT activity 3) need to reduce dose by 75% when given with allopurinol |
|
|
Cladribine
1) MOA |
prodrug converted to CDAMP which is resistant to adenosine deaminase - toxic [ ] buildup in cell -> interfere with elongation of strand - strand breaks.
|
|
|
Fluorouracil
1) MOA 2) AE 3) where metabolized 4) indicated for? |
1) FdUMP - forms complex with thymidylate synthase... thymidylate is not synthesized... inhibits DNA synthesis
FUTP - incorporated to RNA - interfere with RNA processing and prevent mRNA translation FdUTP - incorporated into DNA - inhibits DNA synthesis 2) severe oral/GI ulceration, bone marrow suppression, anorexia 3) liver, lung, kidney 4) colorectal cancer, solid tumors |
|
|
Capecitabine
1) MOA 2) AE 3) where metabolized? 4) indicated for? 5) contraindications? 6) caution? |
1) prodrug for 5-FU
thymidine phosphorylase convert to 5-FU 2) GI distress 3) liver 4) metastatic breast cancer resistant to 1st line therapy and other solid tumors 5) pregnant, lactating mothers, 5-FU hypersensitivity 6) hepatic/renal |
|
|
Cytarabine
1) MOA? 2) indicated for? 3) admin? 4) AE? |
1) metabolized to Ara-CTP... S-phase specific.... competitively inhibits DNAP... incorporates into DNA/RNA and interfere with chain elongation
2) AML 3) IV 4) severe myuelosuppression, hepatic dysfxn |
|
|
Vinblastine
1) MOA 2) indicated for 3) AE |
1) depolymerizes microtuble - binds tubulin and terminates microtubule assembly
MITOTIC ARREST IN METAPHASE 2) Hodgkins, non-Hodgkins, breast cancer 3) myelosuppression |
|
|
Vincristine
1) MOA 2) indicated for 3) AE |
1) depolymerizes microtubules - binds to tubulin and terminates assembly
2) ALL, hematologic malignancies (Hodgkins, non-Hodgkins), pediatric tumors (Ewing's and Wilm's) 3) peripheral neuropathy, constipation, inappropriate secretion ADH |
|
|
Etoposide
1) MOA 2) indicated for? 3) caution? when should dose be reduced? |
1) block cell division in late S-G2 phase.... inhibits topoisomerase II - breaks DNA strand
2) germ cell cancer, lung cancer, hematologic malignancies, gastric cancer 3) renal dysfxn - dose needs to be reduced |
|
|
Topotecan
1) MOA 2) indicated for? 3) caution? dose needs to be reduced with? |
1) inhibit topoisomerase I
2) advanced ovarian cancer (when 1st line CISPLATIN, CARBOPLATIN, OXALIPLATIN doesn't work) 3) renal insufficiency - dose needs to be reduced |
|
|
Paclitaxel
1) MOA 2) indication 3) AE? 4) need to know before give drug? |
1) bind microtubule, enhance and stabilize tubulin polymerization - render it nonfxnal
2) solid tumors - ovarian/breast 3) neutropenia, transient asymptomatic bradycardia 4) premedicate - dexamethasone/diphenhydramine and H2 blocker to prevent serious hypersensitivity rxn |
|
|
Doxorubicin
1) MOA 2) indicated for? 3) AE? |
1) inhibit topoisomerase II - affect S and G2
DNA binding and inhibit DNA synmthesis bind cell membrane and alter fluidity and ion transport generate Reactive Oxygen Species (tumor and heart cells low in superoxide dismutase) 2) BROAD SPECTRUM hematologic malignancies, solid tumors, sarcomas 3) irreversible dose dependent heart toxicity, increase skin pigment, bone marrow suppression |
|
|
Daunorubicin
1) MOA 2) indicated for? 3) AE? |
1) inhibit topo II
DNA binding and inhibit DNA synthesis bind cell membrane and alter fluidity and ion transport generate ROS 2) AML 3) irreversible dose dependent heart toxicity, increased skin pigment, bone marrow suppression |
|
|
Dactinomycin
1) MOA 2) indicated for |
1) bind btw G-C pair of DNA - interferes with DNA dependent RNAP.. inhibits RNA synthesis
2) pediatric tumors |
|
|
Dactinomycin
1) MOA 2) indicated for? 3) AE? |
1) binds DNA btw G-C base pairs... interfere with DNA dependent RNAP... inhibit RNA synthesis
2) Ped tumor - Wilms, etc 3) bone marrow suppression, sensitizes to radiation - inflamm @ radiation sites |
|
|
Mitomycin
1) MOA 2) indication? |
1) metabolized to alkylating agent that cross-links DNA
2) hypoxic tumor cells of solid tumors that are usu resistant to alot of chemo drugs |
|
|
Bleomycin
1) MOA 2) indication 3) attack where in cell cycle? 4) caution? 5) AE? |
1) peptide with DNA binding region + Fe binding domain... when bind DNA, Fe oxidizes and chromosome abnormailities form
2) broad spectrum - testicular tumors 3) G2 4) dose needs to be reduced in renal insufficiency 5) pulmonary toxicity, myelosuppression |
|
|
Tamoxifen
1) MOA 2) indicated for? |
1) binds estrogen receptor of estrogen dependent tumors - endogenous estrogen must be ablated
2) breast cancer |
|
|
Flutamide
1) MOA 2) indicated for? 3) AE |
1) competitively binds and blocks androgen receptor with testosterone - androgen antagonist
2) prostate cancer 3) liver failure, gynecogmastia, GI distress |
|
|
Leuprolide
1) MOA 2) indicated for |
1) analog of GnRH... initial binding leads to a increase in FSH/LH ->desensitization and reduced FSH/LH + decreased testosterone synthesis
2) androgen-receptor positive tumors (prostate cancer) |
|
|
Anastrolzole
1) MOA 2) indicated for |
1) nonsteroidal aromatase inhibitor
2) postmenopausal metastatic breast cancer |
|
|
Exemestane
1) MOA 2) indicated for 3) metabolism? |
1) irreversible steroidal aromatase inhibitor
2) postmenopausal metastatic breast cancer 3) CYP3A4 but no cross resistance |
|
|
Imatinib
1) MOA 2) indicated for |
1) inhibits oncoprotein tyrosine kinases (inhibit cell proliferation, promote abn proliferation and anti-apoptotic pathways)
2) Bcr-Abl (CML) c-kit (GI stromal tumors) |
|
|
Asparaginase
1) MOA 2)indicated for |
1) deprive tumor of asparagine (tumor cells lack asparagine synthetase).. prevents protein synthesis
2) ALL |
|
|
Sorafenib
1) MOA 2) indicated for |
1) inhibits many kinases involved in angiogenesis and intraceullar signalling - inhibits tumor growth
2) renal cell carcinoma |
|
|
Nelarabine
1) MOA 2) indicated for |
1) LIKE CYTABINE
prodrug of ara-G.... ara-GTP disrupts DNA synthesis and induces apoptosis 2) lymphoblastic leukemia |
|
|
Lenalidomide
1) MOA 2) indicated for |
1) thalidomide analog... anti-angiogenic, anti-inflamm axns and enhances anti-cancer activity of T cells and NK cells
2) myelodysplastic syndromes, skin disorders |
|
|
immunosuppressive agents?
|
SITAGAC
sirolimus interferons tacrolimus azathioprine glucocorticoids antibodies cyclosporine |
|
|
glucocorticoids
1) MOA 2) ex? 3) caution? 4) when want to terminate - what should you do? |
1) inhibit leukocyte migration... interfere with cell cycle of activated lymphoid cells.... inhibit production of proinflammatory mediators (LT, PG, histamine, bradykinin)
2) prednisone 3) adrenal suppression if > 7 days... body reduced amt corticosteroids produced 4) reduce dosage gradually |
|
|
Cyclosporine
1) MOA 2) indication? |
1) bind to cyclophilin, block NF-AT
2) prevent tissue rejection following transplant |
|
|
Tacrolimus
1) MOA 2) indication? |
1) complex with FK-Binding protein... inhibit calcineurin - block IL-2
2) organ transplants |
|
|
Sirolimus
1) MOA 2) indication |
1) bind FK-BP..inhibits mTOR - inhibits cell cycle progression from G1->S phase... inhibits lymphocyte proliferation
|
|
|
Interferon alpha
1) MOA 2) indication |
1) inhibit cell proliferation and activate NK cells to kill tumor
2) melanoma, renal cell carcinoma, CML.... ANTIVIRAL TO RX HEP C |
|
|
Interferon beta
1)MOA 2)indication |
1) inhibit cell proliferation and activate NK cells to kill tumor cells
2) melanoma, renal cell carcinoma, CML.........MULTIPLE SCLEROSIS |
|
|
Azathioprine
1) MOA 2) AE |
1) antimetabolite that inhibits de novo purine synthesis -> lymphoid cell proliferation.... DERIVATIVE OF MERCAPTOPURINE
2) myeloid suppression |
|
|
Mycophenolate mofetil
1) MOA 2) indication 2) what is it replacing? |
1) reversible inhibitor of inosine monophosphate dehydrogenase - blocks de novo formation of guanosine phosphate....rapidly hydrolyzed in GI tract to mycophenolic acid... DEPRIVES RAPIDLY PROLIFERATING LYMPHOCYTES KEY COMPONENTS OF NUCLEIC ACIDS....
2) graft survival 3) azathioprine b/c more safe and efficacious in graft survival |
|
|
Rh ab
1) MOA 2) indication |
1) deliver w/in 72hr after delivery
2) Rh - mom |
|
|
Trastuzumab
1) MOA 2) indication |
1) bind and downregulate epidermal growth factor receptor HER-2/neu
2) breast cancer |
|
|
Rituximab
1) MOA 2) indication? |
1) bind CD20 on normal and malignant B cells, activates antibody dependent cell cytotoxicity + complement-mediated lysis
2) follicular B cell non-Hodgkin's lymphoma |
|
|
Daclizumab
1) MOA 2) indication? 3) what other mAb has a higher affinity |
1) IL-2 antagonist - bind CD25 - suppress lymphocyte activation
2) organ transplant - give with glucocorticoids and cyclosporine 3) basiliximab |
|
|
Palivizumab
1) MOA 2) who give to? |
1) binds fusion protein of RSV - prevents infection of cell
2) neonates @ risk |
|
|
Abatacept
1) MOA 2) indication? |
1) bind CD80 and CD86 on APC - blocks interaction with CD 28 on T cell - prevent autoimmune T cell activation
2) rheumatoid arthritis |
