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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 |
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Flucytosine
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- prodrug of 5-fluorouracil
- inhibits DNA synthesis (fungal) - prominant adverse effect is bone marrow suppression |
|
azole mechanism
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inhibiting fungal sterol synthesis
|
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all azoles except which one are inhibitors of P450 system
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fluconazole
|
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fluconazole
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- good CNS penetration and not much interaction with P450 system
|
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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 |
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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 |
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general toxicities of alkylating agents
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- 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
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- 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) - |
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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 |
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busulfan
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- used for chronic myelogenous leukemia
|
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thiotepa
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- used for bladder cancer
- alkylating agent |
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Ifosfamide
|
alkylating agent
|
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Nitrosoureas - (-mustine)
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- very lipophilic so can be used to tx brain tumors
- |
|
streptozocin
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- 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
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- 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) |
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lucovorin
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- rescue from methotrexate toxicity
|
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Mercaptopurine
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- resistance via reduced HGPRT
- metabolized systemically by xanthine oxidase (drug interaction with allopurinol - causes increased levels of mercaptopurine) - toxicities: cholestatic jaundice |
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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 |
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leucovorin
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increases Fluorouracil effect
decreases methotrexate effect |
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cytarabine use
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acute myelocytic leukemia
|
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Doxorubicin
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- intercollate and bind to DNA inhibiting replication and causing damage
- toxicity: cardiotoxicity - (-rubocin) - |
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doxarubicin
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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 - |
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bleomycin
|
***** pulmonary fibrosis
- very effective against testicular cancer - "molecular scissors" chops up DNA |
|
main cuase of pulmonary fibrosis
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bleomycin
|
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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 |
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Etoposide
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used in testicular cancer
|
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Topotecan
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breast and colorectal cancer
|
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asperigenase
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hydrolyses asparagine
used to tx leukemias |
|
interferon alpha 2
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used in hairy cell leukemia and kaposis sarcoma
- |
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Interleukin 2
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- used for advanced malignant melanoma
|
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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 |
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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) |
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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
|
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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 |
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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) - |
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mefloquine
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- 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 |
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Fansidar
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- 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
|
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Malarone
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- Atovaquone + proguanil
- 1st line choice for non complicated malaria (safer than quinine) - non complicated malaria is pretty much if the patient is conscious |
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artemisinin and derivatives
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- used in combo for tx of severe malaria as alternatives
|
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Primaquine
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- only tissue schizonticide available
- cannot use it in pt with Glucose 6 dehydrogenase patient - teratogenic |
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DOC entamoeba histolytica
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Metronidazole plus luminal amebicide
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Giardia lamblia DOC
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Metronidazole
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Trichomonas vaginalis DOC
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Metronidazole
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DOC Toxoplasma gondii
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Pyrimethamine plus Sulfadiazine flus folic acid
|
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Pneumocystis jiroveci
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Trimethoprim plus sulfamethoxazole plus folic acid
|
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DOC tapeworms (cestodes)
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Niclosamide
|
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DOC ascaris lumbricoides
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(roundworm - nematode)
mebendazole or pyrantel pamoate |
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DOC enterobius vermecularis
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(pinworm - nematode)
tx with mebendazole or pyrantel pamoate |
|
DOC necator americanus
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(hookworm - nematode)
tx with mebendazole or pyrantel pamoate |
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DOC trichonella spiralis
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(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
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- activated by viral thymidine kinase
- very similar to acyclovir - converted to pancyclovir |
|
valacyclovir
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prodrug of acyclovir - more orally available but pretty much the same drug
|
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trifluridine
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topically for herpes infections
|
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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 |
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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)
|
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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 |
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amantidine
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- (-mantidine = coating inhibitors)
- not very effective |
|
rimantidine
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(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) |