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145 Cards in this Set

  • Front
  • Back
amphotericin B
- interacts with ergosterol - depolarizes membrane so autotransport mechanisms are gone and cells die (fungus - tears a holes in fungal membrane)
- DOC for all systemic fungal infection except - cryptococcal infection and aspergillosus (caspofungin)
- deadly nephrotoxic!!
- liver toxicity
Flucytosine
- prodrug of 5-fluorouracil
- inhibits DNA synthesis (fungal)
- prominant adverse effect is bone marrow suppression
azole mechanism
inhibiting fungal sterol synthesis
all azoles except which one are inhibitors of P450 system
fluconazole
fluconazole
- good CNS penetration and not much interaction with P450 system
caspofungin (other - fungins)
- used only when there is resistance against other agents
- usually used against aspergillosis
- inhibits cell wall synthesis by inhibiting synthesis of B glycan
griseofulvin
- inhibits microtubule assembly
- prominant adverse effect of disulfiram like effect
nystatin
same mech as amphoteracin B (binds ergosterol --> membrane pores)
- too toxic orally - hepatotoxicity
- for tx of topical infection
general toxicities of alkylating agents
- myelosuppression (bone marrow suppression), N/V (both from chemoagent and from affecting rapidly dividing cells in the gut), hair follicles, sterility (effects on rapidly dividing cells in gonads), terratogenic,


- cyclophosphamide
- mechlorethamine
- carmustine
- cisplatin
- Busulfan
mechlorethamine
- used for tx of hodgkins disease
- can cause hyperuricemia when used for leukemia (large tumor burdon being destroyed)
- treat hyperuricemia with adequate hydration and allopurinol (xanthane oxidase inhibitor)
-
cyclophosphamide
- prodrug activated in the liver
- can be used orally
- in addition to all the classic side effects of alkylating agents it can also cause hemorrhagic cystitis - due to accumulation of acalyne in the bladder - tx with hydration and MENSA
- can cause inappropriate secretion of ADH
busulfan
- used for chronic myelogenous leukemia
thiotepa
- used for bladder cancer
- alkylating agent
Ifosfamide
alkylating agent
Nitrosoureas - (-mustine)
- very lipophilic so can be used to tx brain tumors
-
streptozocin
- tx of pancreatic cancer
- nitrosourease
Cisplatin
- acts like an alkylating agent (crosslinks DNA and proteins causing damage) - but does not have the myelosuppression that the alkylating agents have
- renal toxicities
- acoustic nerve damage !!!!!!
- causes anaphylaxis
methotrexate
- antimetabolite
- dihydrofolate reductase inhibitor
- use lucovorin to rescue from methotrexate toxicity
- widely used for many cancers and used as immunosuppresive agent
- precipitates in kidneys and causes nephrotoxicities
- liver toxicities
- pulmonary fibrosis (not as bad as gliomyocin though)
lucovorin
- rescue from methotrexate toxicity
Mercaptopurine
- resistance via reduced HGPRT
- metabolized systemically by xanthine oxidase (drug interaction with allopurinol - causes increased levels of mercaptopurine)
- toxicities: cholestatic jaundice
Fluorouracil (5-Fluorouracil)
- mech: inhibits thymidolate synthase
- augmented by use of leucovorin (increased effect)
- used for a ton of things particularly colorectal cancer and topically for tx of basil cell carcinoma
- tox: bone marrow suppression
leucovorin
increases Fluorouracil effect
decreases methotrexate effect
cytarabine use
acute myelocytic leukemia
Doxorubicin
- intercollate and bind to DNA inhibiting replication and causing damage
- toxicity: cardiotoxicity
- (-rubocin)
-
doxarubicin
intercalate into DNA causing suppression of DNA replication and causing DNA damage
- cardiotoxicity
- breast cancer and ovarian cancer
- resistance via P glycoprotein pumping drugs out and decreased uptake
- (daumorubicin similar)
- decrease cardiotoxicity with iron chelator
-
bleomycin
***** pulmonary fibrosis
- very effective against testicular cancer
- "molecular scissors" chops up DNA
main cuase of pulmonary fibrosis
bleomycin
Dactinomycin
- suppressed RNA synthesis interfering with cellular proliferation
- used in lab to suppress RNA replication
- radiation recall - appearance of burns during chemotherapy that were previously treated with radiation
Vincristine
- microtubule affecting drugs
- much more neurotoxic (crisps the nerves)
- used for hodgkins disease
-
Vinblastine
- microtubule affecting drug
- much more myelosuppressive (gets the blast cells)
- some neurotoxicity (not as much as vincristine)

-
Paclitaxel
- microtubule affecting drugs
- used in a lot of advanced cancers (breast, ovarian, lung)
- very very toxic - muscle pain, bone pain, severe GI, N/V, bone marrow depression
Etoposide
used in testicular cancer
Topotecan
breast and colorectal cancer
asperigenase
hydrolyses asparagine
used to tx leukemias
interferon alpha 2
used in hairy cell leukemia and kaposis sarcoma
-
Interleukin 2
- used for advanced malignant melanoma
prednisone
- used in a lot of leukemias and lymphomas in combo with other drugs because it suppresses the immune system
- also used to control swelling and inflammation with other cancer drugs and chemotherapy
tamoxifen
- estrogen response modifier
- adjunct in chemotherapy for estrogen positive tumors
- prophylactic agent for women with history of breast cancer
- prophylactic for people with family hx of breast cancer
traztuzumab
- monoclonal antibody based drugs
- targets HER2 receptor
- reaction with doxorubicin --> increased cardiotoxicity
Flutamide
- testosterone receptor antagonist
- suppress the flair of prostate cancer growth when starting tx with Gonadotropin release hormone analogues (Leuprolide, goserelin)
Imatinib
- protein tyrosine kinase inhibitor
- inhibits BCRable fusion kinase that drives chronic myelogenous leukemia (Philadelphia chromosome)
-
if patient is going to southeast asia which malaria meds do you give
malarone (atovaquone + proguanil) or doxycycline
chlorquine
- malarial DOC if its going to work
- very long half life so it can be used once a week for prophylaxis
- rare toxicities at standart theraputic dose
- toxicities: dizziness, ringing in the ears but usually just with higher doses
quinine
- more toxic than chloroquine
- DOC for severe parasitemia often combined with doxycycline
- side effects: similar to asparine OD (ringing in ears, dizzyness, N/V)
- class I antiarrythmic - arrythmogenic (quinidine)
-
mefloquine
- only prophylactic tx in areas where chloroquine resistance is high
- only available orally
- cannot use in pt with previous hx of seizures or mental disorders
Fansidar
- pyrimethamin and sulfadoxine - - good antimalarial if your giong to be away from medical treatment - if you have sx looking like malaria take fansidar until you reach medical help
Malarone
- Atovaquone + proguanil
- 1st line choice for non complicated malaria (safer than quinine)
- non complicated malaria is pretty much if the patient is conscious
artemisinin and derivatives
- used in combo for tx of severe malaria as alternatives
Primaquine
- only tissue schizonticide available
- cannot use it in pt with Glucose 6 dehydrogenase patient
- teratogenic
DOC entamoeba histolytica
Metronidazole plus luminal amebicide
Giardia lamblia DOC
Metronidazole
Trichomonas vaginalis DOC
Metronidazole
DOC Toxoplasma gondii
Pyrimethamine plus Sulfadiazine flus folic acid
Pneumocystis jiroveci
Trimethoprim plus sulfamethoxazole plus folic acid
DOC tapeworms (cestodes)
Niclosamide
DOC ascaris lumbricoides
(roundworm - nematode)
mebendazole or pyrantel pamoate
DOC enterobius vermecularis
(pinworm - nematode)
tx with mebendazole or pyrantel pamoate
DOC necator americanus
(hookworm - nematode)
tx with mebendazole or pyrantel pamoate
DOC trichonella spiralis
(nematode)
- mebendazole
DOC cysticercosis
praziquantel
Flukes (trematodes) - shistosoma ....
praziquantel
acyclovir*** very important for all other antivirals
- mech: phophorylated by thymidine kinase - causes it to get concentrated in the cell
- competes with dGTP
- very non toxic - get sleeping and dizzy when taken with zidovudine (AZT)
- oral, topically, IV
- DOC herpes
- valacyclovir is prodrug - more orally active
- safe with pregnancy
Famcyclovir
- activated by viral thymidine kinase
- very similar to acyclovir
- converted to pancyclovir
valacyclovir
prodrug of acyclovir - more orally available but pretty much the same drug
trifluridine
topically for herpes infections
docosanol
- drug for cold sores
- prevents virus from fusing to the cell
- OTC topical
DOC herpes
acyclovir or valacyclovir
gancyclovir
- same mech as acyclovir when tx of herpes (phosphorylated by thymidine kinase - competes with dGTP)
- in tx of CMV activated by viral protein kinase posphotransferase then competes with GTP
- better CMV coverage than acyclovir (DOC)
- used for prophylaxis against CMV and herpes together
- can cause neutropenia (rare) (when combined with zidovudine)
- prodrug is valgancyclovir
foscarnet
- direct acting drug used in resistant infections
- toxic to kidney
cidofovir
know the name an antiviral (wont be the right answer)
- toxic to kidney
fomivircen
eye infection with CMV (not bolded)
oseltamivir
- Neuraminidase inhibitor selective for influenza A and B
- inhibits release of virus
- oral
- SE: N/V
(-amivir)
zanamivir
(-amivir - like oseltamivir but intranasal) - focus on oseltamivir
- Neuraminidase inhibitor selective for influenza A and B
- inhibits release of virus
- S/E: bronchospasm
amantidine
- (-mantidine = coating inhibitors)
- not very effective
rimantidine
(uncoating - -mantidine)
- not used very often
Ribaviron
- uses: hep C and Respiratory synsitial virus
- active against RNA viruses
- given by inhilation for RSV
- category X terratogen**** - must use 2 forms of contraceptives to use
- people who are pregnant cant administer drug
- orally for hep C
- trouble breathing is big side effect
- other big side effect is anemia - very common especially since people with hep C are commonly treated with other drugs that cause anemia
palivizumab
antibody used against RSV
Lamivudine
- tx for HIV and Hep B coinfection
- used in people with chronic Hep B
- very low toxicity and very effective
- prototype for hep B
- inhibits hepatitis B DNA polymerase
adefovir
-2nd line hep B (behind Lamivudine)
- competatively inhibits hep B DNA polymerase (same as Lamivudine)
Entecavir
-2nd line hep B (behind Lamivudine)
- competatively inhibits hep B DNA polymerase (same as Lamivudine)
Telbivudine
-2nd line hep B (behind Lamivudine)
- competatively inhibits hep B DNA polymerase (same as Lamivudine)
interferon alpha 2b
- initial tx in hep C types 2 and 3 with ribaviron
- used with polyethylene glycol to decrease side effects
- S/E: people feel like they have fever, chills, aches, pain, N/V depression, suicide, neutropenia, anemia (common), thrombocytopenia (not as common), hypotension
tx of hep C strand 1
- interpheron alpha 2b with protease inhibitors (very infectieve - one of there side effects is anemia)
interferon alpha 2a
- used in pts who have not succeeded with alpha 2b with hep C
- used with polyethylene glycol to decrease side effects
-
pts treated with Hep C will def get what (or usually)
ANEMIA (and feel crummy)
how many reverse transcriptase inhibitors do you use together
two
reverse transcriptase inhibitor drugs
- Zidovudine
- Lamivudine (have you dined (-vudine) with my nuclear family)
- Tenofovir
- Emtricitabine
- Didanosine
HIV combination drug therapy
- 2 nucleoside reverse transcriptase inhibitors
- 1 non nucleoside RTI
- 1 or 2 protease inhibitors
reverse transcriptase inhibitors (drugs)
- zidovudine
- Lamivudine
- Tenofovir
- Emtricitabine
- Didanosine
non nucleoside reverse transcriptase inhibitors (drugs)
- Nevirapine
- Efavirenz**
protease inhibitors
- saquinavir
- Ritonavir
- Atazanavir
(NAVIR hit a protease)
most commonly used non nucleoside reverse transcriptase inhibitor
Efavirenz
toxicity of all reverse transcriptase inhibitors
- lactic acidosis with hepatotoxicity****
zidovudine
- nucleotide (deoxythymidine) analogue
- get into cell get phosphorylated
- incorperated into DNA and stop the chain from making a double chain
- combined because with monotherapy resistance happens fast
- often combined with lamivudine
- pretty well tolerated
- metabolized by liver
- excreted by kidneys
- safe in prego
- toxicities: anemia, neutropenia (tx with erythropeotin (epogen) and neupogen)
- CNS, GI toxicities - interactions with acyclovir, gancyclovir or acetominophen - increased likelyhood of neutropenia
-
other main reverse transcriptase inhibitor group (other than your vudines)
- tenofovir
- emtricitabine
didanosine
- nucleotide reverse transcriptase inhibitor
- not used much any more because they can cause peripheral neuropathy
Efavirenz
- DOC non nucleoside reverse transcriptase inhibitor
- teratogenic (so are all NNRTI)
protease inhibitors
- clips off the proteins as virus is getting ready assemble
- NAVIR (navir tease a protease)
- poor bioavailability
- use subtheraputic dose of rotanavir to inhibit CYP3A to increase absorption of protease inhibitor
- st. johns wart can cause there metabolism to be reduced (or anything that inhibits cyp4503A4)
- side effects: look like corticosteroids except at the face
-
ritonavir
protease inhibitor
- not used at theraputic levels but used to increase the bioavailability of the others
atazenavir
- least side effects of all the protease inhibitors (but there pretty much all the same)
Enfuvirtide
fusion inhibitor
- can cause infusion reaction
- prevents virus from binding
cortisteroids (prednisone)
- very broad immunosuppressants
- used a lot early after transplants
- used to decrease rejection episodes
- inhibit many aspects of the immune system
- side effects know them
- cause T lymphocytes to be lysed (used with cancers)
cyclosporin
- inhibit calcinurin --> decreases the ability to increase IL-2 (used for T cell activation)
- used to prevent transplant rejection
- very selective for T cells so dont cause bone marrow suppression
- S/E: HTN, kidney toxicity, hyperglycemia (especially when combined with corticosteroids),
- unique toxicity (from tacrolimus) = gingival hyperplasia
tacrolimus
- inhibit calcinurin --> decreases the ability to increase IL-2 (used for T cell activation)
- used to prevent transplant rejection
- very selective for T cells so dont cause bone marrow suppression
- S/E: HTN, kidney toxicity, hyperglycemia (especially when combined with corticosteroids),
- S/E that is unique from cyclosporin = insomnia
Sirolimus
- blocks response of T cells to IL-2
- causes bone marrow suppression (but not kidney toxicity so good in kidney transplants)
-
mycophenolate mofetil
inhibits monophosphate dehydragenase --> inhibiting T and B cells from making purines (other cells in the body dont need this) so pretty selective
- used as antirejection drug
- S/E = RASH - must stop
- terratogenic
cyclophosphamide (in immunosuppression)
it can inhibit an already established immune reaction
- destroys T cells that have already been activated
- can be used for organ transplant rescue
Leflunomide
- tx of rheumatoid arthritis
- terratogenic
Thalidomide
- ONE OF THE MOST TERRATOGENIC AGENTS
- used for multiple myeloma and graft vs. host, AML, leprosy and all sorts of things
Lymphocyte immune Globulin
- from horses and rabbits
- people respond to them as foreign substances so administer with corticosteroids
- used to rescue acute rejection episodes
Antithymocyte Globulin
- from horses and rabbits
- people respond to them as foreign substances so administer with corticosteroids
- used to rescue acute rejection episodes
Muromonab
- monoclonal antibody to the CD3 (T3) receptor but is not huminized so you can get a cytokine release syndrome so pretreat with corticosteroids
- pretreat with corticosteroids
- similar to the globins
Daclizumab
huminized proteins
- very long duration of actions because antibodies bind and stay there
- used to induce immunosuppression prior to kidney transplants
other main reverse transcriptase inhibitor group (other than your vudines)
- tenofovir
- emtricitabine
didanosine
- nucleotide reverse transcriptase inhibitor
- not used much any more because they can cause peripheral neuropathy
Efavirenz
- DOC non nucleoside reverse transcriptase inhibitor
- teratogenic (so are all NNRTI)
protease inhibitors
- clips off the proteins as virus is getting ready assemble
- NAVIR (navir tease a protease)
- poor bioavailability
- use subtheraputic dose of rotanavir to inhibit CYP3A to increase absorption of protease inhibitor
- st. johns wart can cause there metabolism to be reduced (or anything that inhibits cyp4503A4)
- side effects: look like corticosteroids except at the face
-
ritonavir
protease inhibitor
- not used at theraputic levels but used to increase the bioavailability of the others
atazenavir
- least side effects of all the protease inhibitors (but there pretty much all the same)
Enfuvirtide
fusion inhibitor
- can cause infusion reaction
- prevents virus from binding
cortisteroids (prednisone)
- very broad immunosuppressants
- used a lot early after transplants
- used to decrease rejection episodes
- inhibit many aspects of the immune system
- side effects know them
- cause T lymphocytes to be lysed (used with cancers)
cyclosporin
- inhibit calcinurin --> decreases the ability to increase IL-2 (used for T cell activation)
- used to prevent transplant rejection
- very selective for T cells so dont cause bone marrow suppression
- S/E: HTN, kidney toxicity, hyperglycemia (especially when combined with corticosteroids),
- unique toxicity (from tacrolimus) = gingival hyperplasia
tacrolimus
- inhibit calcinurin --> decreases the ability to increase IL-2 (used for T cell activation)
- used to prevent transplant rejection
- very selective for T cells so dont cause bone marrow suppression
- S/E: HTN, kidney toxicity, hyperglycemia (especially when combined with corticosteroids),
- S/E that is unique from cyclosporin = insomnia
Sirolimus
- blocks response of T cells to IL-2
- causes bone marrow suppression (but not kidney toxicity so good in kidney transplants)
-
mycophenolate mofetil
inhibits monophosphate dehydragenase --> inhibiting T and B cells from making purines (other cells in the body dont need this) so pretty selective
- used as antirejection drug
- S/E = RASH - must stop
- terratogenic
cyclophosphamide (in immunosuppression)
it can inhibit an already established immune reaction
- destroys T cells that have already been activated
- can be used for organ transplant rescue
Leflunomide
- tx of rheumatoid arthritis
- terratogenic
Thalidomide
- ONE OF THE MOST TERRATOGENIC AGENTS
- used for multiple myeloma and graft vs. host, AML, leprosy and all sorts of things
Lymphocyte immune Globulin
- from horses and rabbits
- people respond to them as foreign substances so administer with corticosteroids
- used to rescue acute rejection episodes
Antithymocyte Globulin
- from horses and rabbits
- people respond to them as foreign substances so administer with corticosteroids
- used to rescue acute rejection episodes
Muromonab
- monoclonal antibody to the CD3 (T3) receptor but is not huminized so you can get a cytokine release syndrome so pretreat with corticosteroids
- pretreat with corticosteroids
- similar to the globins
Daclizumab
huminized proteins
- very long duration of actions because antibodies bind and stay there
- used to induce immunosuppression prior to kidney transplants
Basilizimab
- huminized proteins
- very long duration of actions because antibodies bind and stay there
- used to induce immunosuppression prior to kidney transplants
- same as Daclizumab
Interleukin 2
- used for metastatic renal cell carcinoma and malignant melanoma
- severe toxicities many times patients have to be hospitalized
- activates the immune system
oprelvekin
- for thrombocytopenia
- improves that for people on chemotherapy
- toxicity: fluid retention
Granulocyte stimulating factor; Filgrastim
- tx of neutropenia induced by chemo or other drugs
- given subcutaneous
- toxicity: bone pain
Epoetin
- recombinant of erythropoetin
- used to treat anemia
- causes HTN and blood clots
interferon beta-1B
tx of multiple sclerosis
Category A pregnancy drugs mean what
- controlled studies showed no risk
category B pregnancy drugs mean what
- no evidence of risk in humans
- well controlled studies in humans showed no harm but studies in animals did find adverse effects
category C pregnancy drugs mean what
- No adequate human studies but studies in animals have shown harm
- possibility of fetal harm so prescribe only if potential benifits to justify perscription
category D prego drugs meaning
studies in humans have shown fetal risk
only use in life threatening circumstances
must have warning label
category X prego drugs mean what
risk outweighs potential benefits
contraindicated in women with prego
antibiotics to avoid in prego
Clarithromycin
Sulfonamides
Aminoglycoside
Fluoroqunolones
Metronidazole
Tetracyclines
Ribavirin
Griseofulvin
Chloramphenicol

Countless SAFe Moms Take Really Good Care
when do terratogens exert there effects during pregnancy
- at any time not all first trimester
- effects are not always seen immediately (diethylbesterol - DES)