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179 Cards in this Set
- Front
- Back
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- Nitrogen Mustard Alkylating Agent (N7 of G), CSNS
- IV, rapid, NOT EXCRETED S/E: bone marrow depression Tx: Hodgkin's disease (MOPP) |
Mechlorethamine
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- Nitrogen Mustard Alkylating Agent (N7 of G), CSNS
- Oral, IV, IM, etc - PRODRUG activated by liver S/E: hemorrhagic cystitis (2nd to product ARCOLEIN, give MESNA to neutralize) TX: Burkitt's, ALL |
Cyclophosphamide
Ifosfamide (analog) |
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- Nitrogen Mustard Alkylating Agent (N7 of G), CSNS
-least toxic of nitrogen mustards TX: CLL, but not used much anymore |
Chlorambucil
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-Nitrogen mustard+estradiol
-Oral Tx: pallative prostate CA |
Estramustine phosphate
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-Alkylating agent, but not NM
S/E= PULMONARY FIBROSIS, hyperpigmentation Tx: CML (remission, but no cure) |
Busulfan
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-Nitrosoureas, are prodrugs that become alkylators in vivo
-Lipophilic so +CNS S/E: CNS effects, pulmonary fibrosis, nephrotoxic Tx: BRAIN TUMORS, PANCREATIC CA (streptozotocin) |
Carmustine
Lomustine Semustine Streptozotocin |
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- Metabolites are reactive species & alkylating compound; inhibit DNA, RNA, protein synth CCNS
SE: Avoid use with MAOIs TX: Hodkin's, MOPP regimin |
Procarbazine
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-Methylates DNA & RNA; CCNS
TX: Hodkin's ABVD regimin, Melanoma |
Dacarbazine
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- binds G in DNA/RNA, fragments DNA; CCNS
SE: nephrotoxic, ototoxic, peripheral neuropathies (nephro reduced with forced diuresis), hyperuricemia TX: TESTICULAR CA, OVARIAN CA *with 5-FU and leucovorin for colon cancer |
Carboplatin
Cisplatin *Oxaliplatin |
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-Anthracycline binds b/w bps in DNA, prevents transcription, ss breaks, inhibits DNA repair, free radical formation
- CCNS SE: CARDIOTOXIC, may be irreversible (the red death!) (prevent with DEXRAZONE when EKG changes appear) TX: Hodgkin's ABVD, various carcinomas |
Doxorubicin
Daunorubicin |
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-Anthracycline; bins DNA leading to DNA breakage (no free radicals)
S/E: lower incidence of cardiotoxicity |
Mitoxantrone
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-Anthracyclines, better side effect profiles
*related to doxorub, Tx for bladder CA, not as cardiotoxic |
Idarubicin
Epirubicin *Valrubicin |
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- acts on Topo II to cleave DNA, inhibits repair, CCNS (G2 and S)
TX: TESTICULAR TUMORS (can get cures!), Small cell of lung |
Etoposide
Teniposide |
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- inhibits Topo I
- PRODRUG activated by CARBOXYESTERASES |
Irinotecan
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- bind reduced iron, DNA scission and ihbits repair
- some ABX properties - CSS for G2 phase S/E: PULMONARY FIBROSIS and PNEUMONITIS, CUTANEOUS RXNS, minial BM depression TX: Advanced Testicular CA (combo with VB,Cisplat), lymphomas |
Bleomycin
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- interacts with dsDNA through peptide loops to inhibit DNA-dep RNA-synth at dG-dC, prevents trasncription
- CCNS, MOST POTENT ANTI-TUMOR AGENT KNOWN S/E: oral ulcerations, stomatitis TX: MTX-resistant CHORIOCARCINOMA, WILM'S, RHABDOMYOSARCOMA |
Dactinomycin
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- reduced under ANAEROIC conditions, binds to N2 of G, crosslinks and free radicals, ssDNA breaks
Tx: Solid tumors |
Mitomycin
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- inhibits DHFR to block thymidylate and purine synth
- CCS at S phase S/E: oral/GI ulceration, hepatotoxic, pulmonary toxic Tx: CHORIOCARCINOMA, ALL, low doses for autoimmune disorders *LEUCOVORIN rescue for normal cells after high dose |
Methotrexate
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- inhibits thymidylate synthetase, incorporated into DNA/RNA
- CCNS S/E: Oral, GI ulceration Tx: Solid tumors |
Fluorouracil (5-FU
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- inhibits DNA polymerase alpha
- CCS for S phase S/E: oral ulceration Tx: Acute leukemias |
Cytarabine
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- inhibits DNA synth via many mechanisms after form of active metabolite
- CCNS TX: several carcinomas, syngery with platinum and rads |
Gemcitabine
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- inhibits synth of purines by blocking iosinate conversion
- CCS at S phase - INHIBITED BY ALLOPURINOL S/E: oral and GI ulcers Tx: Acute leukemias |
Mercaptopurine (6-MP)
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- inhibits synthesis of purines
- CCS at S phase Tx: acute leukemias |
Thioguanine (6-TG)
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- inhibits adenosine deaminase, decrease DNA synth
Tx: HAIRY CELL LEUKEMIA DOC* |
Pentostatin
Cladribine* Fludarabine |
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- bind soluable tubulin, block polymerization and arrest mitosis
- CCS for M phase S/E: Peripheral neuropathy, alopecia Tx: Hodgkins (MOPP)*, Testiculat tumors^, Hodgkins (ABVD)^ |
Vincristine*
Vinblastine^ Vinorelbine |
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- prevents microtubule depolymerization, arrests cells in mitosis
- CCS for M phase S/E: peripheral neuropathy Tx: Advanced Ovarian Cancer, wide use as secondline *newer for mets Breats CA, Non-Small cell CA |
Paclitaxel
Docetaxel* |
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- hydrolyzes asparagine
S/E: liver damage, pancreatitis Tx: ALL |
L-Asparaginase
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- similar to DDT, relatively selective for adrenocortical cells
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Mitotane
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- natural antiviral defense mech, inhibits some tumor and viral growth
- CCNS, has to be IM/SubQ - used as immuno stimulant S/E: ACUTE FLU Like Rxn, myelosup Tx: Kaposi's, hairy cell, non-hodgkins, HepB, Hep C, MS, HPV warts |
Interferon alpha (and others)
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- suppress mitosis in lymphs and is lympholytic, inhibits Tcell proliferation (immunosuppress), affects Tcells more than B
- manage hemolytic anemia and complications of CLL and lymphomas - have antiinflammatory effects Tx: Hodgkins (MOPP), acute leukemia, prevent transplant reject, autoimmune dis |
Prednisone
Prednisolone |
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- hormone
Tx: endometrial carcinoma, renal cell |
Progestin
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- hormone
Tx: Prostate CA, mammary CA |
Estrogens/Androgens
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- "Anti" estrogen but NON steriod, has partial estrogen activity
Tx: ER+ Breast CA |
Tamoxifen
Toremifine |
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- "Anti"androgen
- combined with leuprolide Tx: prostate CA |
Flutamide
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-recombinant AB against HER2
Tx: breast CA |
Trastuzumab
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-monoclonal AB against CD33, with cytotoxic antibiotic
Tx: CD33+ AML in relapse |
Gemtuzumab ozogamicin
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-chimeric AB against CD20 on Bcells
Tx: Non-Hodgkins Lymphoma (yttrium couterpart beta-emitter - $30K!) |
Rituximab
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-antibody given with alkylating agents
Tx: CLL in pts that fail fludarabine |
Alemtuzumab
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-Irreversible Aromatase Inhibitor blocks conversion of adrenal androgen
Tx: Breast CA in postmenopausal women |
Anastrazole
Exemestane Letrozole |
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-estrogen receptor like antagonist, but w/o estrogen activity (similar to tamoxifen)
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Fulvestrant
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-Tyrosine Kinase Inhibitor
Tx: CML after interferon failure |
Imatinib mesylate
Gefitinib Erlotinib |
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- Retinoid X receptor activator, alter gene expression
Tx: Tcell lymphoma, APML with antracyclines |
Bexarotene
Tretinoin |
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MOPP Regimen
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Mechlorethamine
Vincristine (O) Procarbazine Prednisone Hodgkins |
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ABVD Regimen
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Doxorubicin (A)
Bleomycin Vinblastine Dacarbazine Hodgkins |
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- binds to cyclophilin and inhibits CALINEURIN
- decreases production of cytokines, some protooncogenes, and IL2 receptors, - increases TGF-B - Selective for T-cells S/E: nephrotoxic Tx: prevent and treat organ rejection, autoimmune dis |
Cyclosporine
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- binds to cytosolic protein and inhibits CALCINEURIN (same effects as cyclosporin, decreased cytokines, IL2-R and increases TGFB)
-100x more potent than cyclo. S/E: nephrotoxic Tx: prevent and treat organ rejection, autoimmune dis |
Tacrolimus
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- binds to IMMUNOPHILIN FKBP, which inhibits MTOR, and blocks Tcell cycle progression
S/E: elevated lipids, delayed graft function, anemia, NOT directly nephrotoxic TX: prevent and treat organ rejection, autoimmune dis |
Sirolimus
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- cytotoxic, immunosuppressant
- converted to mercaptopurine in vivo - inhibit purine biosynthesis Tx: post trasnplant |
Azathioprine
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- cytotoxic, immunosuppressant
- converted to mycophenolic acid in vivo - inhibits iosine monophosphate dehydrogenase (decreases purines) Tx: post renal txp |
Mycophenolate mofetil
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- ployconal IG from horses immunized with human thymus cells
- immunosuppressant - binds circ T-cells to cause lymphopenia S/E: serum sickness, nephritis, chills, fever Tx: allograft rejection |
Antithymocyte globulin (ATGAM)
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- immunosupresant
- mouse antibody against CD3 of Tcells - binds to Ts and hinders their binding to antigen S/E: cytokine release syndrome |
Muromonab
(daclizumab, basilixmab: human versions anti cd25) |
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-immunosuppressant
- antibodies used in RA and Chron's dis - anti TNFalpha |
Infliximab
Etanercept |
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-immunosuppressant
-LFA1 inhibitors Tx: prevent transplant rejection, psoriasis |
Efalizumab
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-immune stimulant
- pooled human plasma Tx: immune deficiences, prevention of measels, hepA, AIHA, etc |
Immune Globulin
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- immune stimulant
- viable attenuated mbBovis - stimulates NKcells and Tcells S/E: shock, hypersensitivity Tx: Bladder CA |
Bacillus Callmette - Guerin (BCG) vaccine
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- Immune stimulant
- antihelminic agent that inhibits T-suppressor lymphokine production Tx: colon cancer |
Levamisole
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-immune stimulant
-increased proliferation of T cells, B cells, activated macros, NK cells -natural or recombinant S/E: severe hypotension, cardiovascular toxicity, pulmonary edema Tx: meta melanoma, renal cell, AIDS |
IL-2
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-immune stimulant
-induces bone marrow progenitor cells to mature |
filgrastim (G-CSF)
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-Enhancement of one drug by another
Ex: TMP/SMX Ex: PCN/Aminoglyc |
Synergism
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-Persistent effect even though below MIC
-Fluoroquinolones, Aminoglycosides |
Post Antibiotic Effect (PAE)
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-Kill depends on peak concentration (PAE)
- Fluoroquinolones, aminoglycosides |
Concentration Dependent Kill (CDK)
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-Kill depends on amoutn of time above MIC
-B lactams (PCNs, Cephalos) |
Time Dependent Kill (TDK)
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-inactivating ENZ (Betalactamases)
-alter cell wall/porin -alter binding site/receptor -increased metabolite (sulfonamide resistance due to Increased PABA) -drug efflux pump (FluoroQ resistance: change in enz and efflux) |
Microbial Resistance
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-inhibit bacterial cell wall synth (PBPs)
-bacteriCIDAL, TDK -Resist: betalactamase, fail to penetrate porin, low affinity binding -PenV, Amox, Carben are not descreased by food -Well dist but lipid insoluable -RE except Amp, Nafc, Antipseudomonal -IgE analphy, IgM/IgG maculopapular rash (most common) |
Penicillins General
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-G: Acid labile (IV only) V: acid stable (oral)
Tx: SSE, but mostly just strep (staph and enterococcus largely resistant now), Peptostrepto(Anaer) |
Pen G
Pen VK |
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-Acid Stable (Oral), can take with food
-Amino allows porin entry Tx: SSE (Staph often resist), Whimpy G-, GATE bugs, Anaerobes (with combo) S/E: Diarrhea *AMP DOC for ENTEROCOCCUS) |
Aminopencillins (Ampi, Amoxi)
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-Acid stable (oral)
-can penetrate cell walls Tx: SS only NO E, Whimpy G-, GATE, SPACE**, Anaerobes (with combo) *Carbenicillin for Pseudomonas UTIs S/E: Ticarcillin most effective but INCREASES NA LOAD, hypersensitivies, platelet dysfunction |
Carboxypencillins (Carbenicillin, Ticarcillin)
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-similar to carboxy, but less of NA problem
Tx: SSE, Whimpy G-, GATE, SPACE, Anarobes (with combo) |
Ureidopencillins (Piperacillin)
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IV: Methicillin, Oxacillin, Nafcillin
(Meth off market b/c of kidney damage) (NAF IS HEPATIC ELIM) PO: Cloxacillin, Dicloxacillin ("SS" only - no "E") |
Penicillinase Resistant PCNS
(Antistaph PCNS) |
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-Amoxic/Clavulanic Acid (PO)
-Ampi/Sulbactam (IV) -Ticar/Clavulanic Acid -Piper/Tazobactam |
PCN Combos (PCN+Blact inhib)
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Serratia
Pseudomonas** Actinobacter Citrobacter Enterobacter |
"SPACE" BUGS (hardest to kill)
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Proteus
E.coli Klebsiella "PEK" |
"Gate" bugs (can be hard to kill or easy depending on strain)
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Hemophilus
Moraxella Salmonella Shigella Morganella |
WIMPY G- bugs
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Chlyamidia
Mycoplasma Legionella "CML" |
Atypical Bugs
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Peptostreptococcus
Clostridium Bacteroidies* "PCBs" |
Anaerobes
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Cell wall Inhibit: Piper, Ticar, Ceftrazidine, Cefepime, Imipenem, Meropenem, Aztreonam
30S inhibit: Gent, Tobra, Amikacin DNA gyrase inhibit: Levofloxin, Cipro "Kitchen" Sink: Colistin |
SPACE bug coverage
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Staph
Strept Enterococcus ("SSE") |
Most G+
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-mimic D-ala-D-ala, halt X-bridge of cell wall
-BacteriCIDAL -IV, Xcpt: CEFUROXIME, CEFPODOXIME (prodrugs) -RENAL elim, Xcpt: CEFOPERAZONE, CEFTRIAXONE (HE) -Hypersensitive, Diarrhea, bleeding (MAN the ZONE is TAN), disulfiram effect (MZT), serum sickness in kids (CEFACLOR**) DD: potentiates Warfarin, Probenecid prolongs RE excretion NONE COVER ENTEROCC, CML, MRSA or LISTERIA |
Cephalosporins (General)
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-1st Generation
Tx: "SS", a few G- *CEFAZOLIN long t1/2, surgical prophy |
Cephalexin (PO)
Cefazolin (IV) |
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-2nd Generation NATURAL
Tx: "SS", whimpy G-, +/- GATE |
Cefuroxime axetil (PO)
Cefuroxime (IV) |
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-2nd Generation SYNTHETIC
Tx: "SS", whimpy G-, GATE, "SE", ANAEROBES (A TAN FOX will bite you) -NMTT side chain!! DM foot infections, abdominal surgeries |
Cefoxitin (IV)
Cefotetan (IV) (cephamycins) |
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-3rd Generation General
Tx: "SS", whimpy G-, GATE, "SACE" (no P!) **CAP DOC, Meningitis, STDs (Neisseria) |
Ceftriaxone (IV)
Cefotaxmine (IV) |
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-3rd Generation Anti-Pseudo
Tx: Very POOR G+, whimpy G-, GATE, SPACE *HAP, Meningitis, neutropenic fevers |
Ceftazidime (IV)
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-4th Generation
Tx: "SS", whimpy G-, GATE, SPACE *HAP, Menigitis |
Cefepime
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-beta lactam agent
-CILASTIN given with to prevent extensive RE by brush border -can cause SEIZURES, have to renal adjust -BacteriCIDAL TX: SSE, G-, SPACE, ANAEROBES expensive so used for serious, nosocomial, multiple organism infxs |
Imipenem/cilastin
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-beta lactam agent
-similar toe Imipenem, but less S/E -BacteriCIDAL TX: SSE, G-, SPACE, ANAEROBES expensive so used for serious, nosocomial, multiple organism infxs, **MENINGITIS [Erta no SPACE coverage) |
Meropenem
Ertapenem |
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-cell wall inhibitor
-Xreactivity with PCN is RARE so can use in PCN allergic pts -NO G+, G- and SPACE, some anaerobes |
Aztreonam
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-CDK, BacteriCIDAL, PAE
-Bind 30S, inhibit mRNA & protein -mostly IV, RENAL excretion (unchanged) TX: mainstay for serious G- infections S/E: NEPHROTOXIC (high trough), OTOTOXIC (high peaks), potentiate NM blocks *once daily dosing for lungs (need high []) *monitor blood levels (3rd dose) |
AMINOGLYCOSIDES (General)
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-Iv/Im Aminoglycoside
-need trough <2 Tx: synergy for G+, GREAT G- coverage (SPACE) **serious G- Infx, BRUCELLOSIS |
Gentamicin
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-Iv/Im aminoglycoside
-need trough <2 Tx: synergy for G+, GREAT G- coverage (SPACE) **serious G- infx, topical/opthalmic solutions |
Tobramycin
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-Iv/Im aminoglycoside
-rarely used b/c hard to get levels (need higher toughs) Tx: synergy for G+, GREAT G- coverage (SPACE) ** serious G- infx |
Amikacin
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-PO aminoglycoside
-NOT absorbed, wipes out gut flora as prep for gut surgery -can help REDUCE UREMIA in hepatic coma -also can reduce cholestrol in hyperlipidemia |
Neomycin
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-Iv/Im aminoglycoide
-reserved for TB use, must be obtained from manufac. (RIPE"S") |
Streptomycin
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-glycopeptide derived from streptomyces, has come back into used b/c of MRSA
-inhibits cell wall by complexing with d-ala-d-ala -BacteriCIDAL, CDK, PAE -IV, or PO for C.diff -RE unchanged -good for pts with PCN allergy S/E: Redman/Redneck syndrome, nephrotoxic, ototoxic (must monitor) TX: G+ (including MRSA, MRSE, Anthrax, Diptheria), NO G- **use guidelines exist (1gm q 12h) |
Vancomycin
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-irreversibly binds 50S inhibiting peptide chain formation
-CIDAL if given together TX: G+ including VRE (not faecalis though), PCN-R Strept, MRSA, some anaerobes, some G- S/E: give through PICC or Central b/c of infusion site reactions |
Quinupristin, Dalfopristin
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-oxazolidinone, binds to 23S of 50S to inhibit protein synth
-PO=IV Tx: VRE, VISA, MRSA S/E: thrombocytopenia, serotonin storm with SSRIs (MAOinhib), yeast superinfxn |
Linezolid
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-topical cream
TX: MRSA eradication in nares (controversial for long terms), impetigo, wound infxs |
Mupirocin
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-structural analogs of PABA, compete for DHPSynthetase, so cell can't make THfolic acid (blocks nucleic acid/protein synth)
-hosts require preformed so are not affected -BACTERIOSTATIC -RE (extent of met varies) S/E: hypersens common, STEVENS-JOHNSON, CRYSTALLURIA (nephrotox), KERNICTERUS, photosens TX: G+, G-, some atypicals, falciparum (NO Pseudo) *resistance via overproduce PABA **Acute Uncomplicated UTI only use for Sulfa alone -- used mostly in combo with TMP (PCP, Toxo, malaria) |
Sulfonamide
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-nonsulfa pyrimadine analog, competes for DHFR, 50000X more active against bacterial ENZ
-CD either CIDAL or STATIC -RE (mostly unchanged) S/E: N/V/D, rash, *use WITH CAUTION IN FOLATE DEF (Alch, preg, kids) TX: G+, G-, PCP **acute UTI, UTI PROPHYLAXIS (spinal cord pts), diarrhea |
Trimethoprim
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-synergistic, reduces resistance devo.
TX: G+, G-, PCP NO PSEUDO *UTIs, RTIs, PCP, GI, many others **Potentiates WARFARIN **Displaces METHOTREXATE, increases [] |
TMP/SMX combo
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-unclear MOA
S/E: pulmonary rxns, can mimic pneumo Tx:100% use for UTIs (very high urine []) ONLY CYS, NOT PYLEO (MRSA, VRE UTI TX!) *rate of ex linear w/CrCl, don't use if less than 50 |
Nitrofuran
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-No MOA alone, at acidic pH, hydrolyzed to formaldehyde, kills bacteria
S/E: hypersensitivity, has ammonia byproduct (avoid Hepatic!) Tx: UTI Prophy for virtually all ** frequent VOIDs will decrease effects |
Methenamine
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-structurally related to Nalidixic acid, inhibits DNA gyrase (Topo IV), BacteriCIDAL
-ORAL=IV, PAE, can switch to oral! S/E: arthropathy ESP IN KIDS (exc for CF kids) DDR: Antacids reduces absorption |
Quinolones (General)
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Tx: fair for G+, G-, SPACE, DOC FOR PSEUDO
DD: can double Theophylline levels (dec metab), potentiates Warfarin *huge range of indications, SWITCH to ORAL when available |
Ciprofloxacin
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Tx: Good G+ coverage, pretty good for G-, SPACE, atypicals
-less side effects than Cipro |
Levofloxacin
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Tx: G+, G-, ANAEROBES
No UTIs - only anaerobes |
Moxifloxacin
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TX: Bad G+, Good G-/SPACE
-cipro is 4x more potent |
Ofloxacin
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TX: Good G+, esp Enterococcus, Good G-/SPACE, Aytpicals, ANAEROBES
|
Trovafloxacin
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-inhibits Mycolic acid synth (is txp into Bact)
-kills active and dormant bact -met by acetylation, rate depend on race (eqypt slow, esk/jap fast) S/E: heptatoxic, NEUROTOXIC (PERIPHERAL) Tx: TB Mainstay (R"I"PES) *COADMIN PYRIDOXINE to prevent neuro probs DOC for PPD+ |
Isoniazid
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-inhibits DNAdep-RNApoly, inhibits RNA synth
-BACTERICIDAL against many, but reserved S/E: ORANGE DISCOLORATION of BODY FLUIDS, Hepatotoxic esp with INH, *AUTOINDUCTION, revs up Liver, so have to change hepatic drugs (Induces Theopy, Warfarin, Steroids, narcotics, oral hypogly) Tx: TB ("R"IPES), 2nd for PPD+ |
Rifampin
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-MOA not well understood, bactericidal against dormant in macros (acidic environs)
-HE, competes with uric acid S/E: will complicate GOUT, hepatotoxic, hyperuricemia, rash Tx: TB (RI"P"ES) |
Pyrazinamide
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-bacterioSTATIC
S/E: OPTIC NEURITIS, use with caution in KIDS (unreliable vision test) Tx: TB (RIP"E"S) |
Ethambutol
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-Aminoglycosides
-Iv or IM S/E: OTOTOXIC (VERTIGO), more ADRs than E Tx: TB (RIPE"S") |
STREPTOMYCIN
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-like rifampin
S/E: NEUTROPENIA, HEPATOTOXIC TX: MAC/MAI |
Rifabutin
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Tx: AntiLeprosy agent
S/E: numerous, DISCOLORS SKIN AND EYES |
Clofazamine
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-if more than 4% resistance: 4 drugs for 2 months, then 2 drugs for 4 months
(RIPE or RIPS then RI) -macrolides and fluoroQs used adjunctively |
TB TX
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-competitive inhibitor of folic acid synth, sulfa
-BacterioSTATIC S/E: anemia, sulfone syndrome (jaundice, dermatitis) TX: Leprosy (also clofazamine, rifampin) |
Dapsone
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-reversibly binds 50S, inhibits protein synth
-bacterioSTATIC, higher tissue [] vs serum -HE -complete absorb while fasting S/E: DIRECT GASTRIC IRRITANT (MOTILIN RELEASE) *used to tx gastroparesis, CHOLESTATIC HEPATITIS (*AVOID ESTOLATE in preg) DD: decreases THEOP,WARFA, CARBAMA, STATIN metabolism (p450) Tx: SS, ATYPICALS, PCN allergic |
Erythromycin
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-reversibly binds 50S, inhibits protein synth
-bacterioSTATIC, tissue [] stay high (5 DAY THERAPY) -HE (bilary) T1/2=68 HOURS! S/E: METALLIC TASTE, some N/V/D DD: does not affect p450 Tx: SS, Hflu/Mcat CAP**, MAC/MAI, ATYPICALS *Chlamydia 1dose |
Azithromycin
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-reversibly binds 50S, inhibits protein synth
-bacterioSTATIC, higher tissue [] vs serum -HE S/E: METALLIC TASTE, some N/V/D DD: decreases THEOP,WARFA, CARBAMA, STATIN metabolism (p450) Tx: SS, Hflu/Mcat CAP, MAC/MAI, H PYLORI* (Prevpak with Amox, PPI), ATYPICALS |
Clarithromycin
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-derived from lincomycin, NOT a macrolide
-binds 50S, inhibits protein synth -Oral=IV, HE S/E: C.DIFF* PMC, hepatotoxic Tx: SS (some MRSA), ANAEROBES*, Toxo, PCN allergies |
Clindamycin
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-reversibly binds 50s of 70S, inhibits protein synth
-Oral BETTER than IV (hyrdolysis in GUT required) -HE, widely varies in kids, monitor! -EXCELLENT CSF[] S/E: APLASTIC ANEMIA, BM Dep, GRAY BABY SYNDROME Tx: G+, G-, ANAEROBES, ATYPICALS, RICKETTSIA, *meningitis (NOT used in USA) |
Chlorampenicol
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-reversibly binds 30S
-bacterioSTATIC -RENAL Excretion, FOOD affects S/E: PHOTOSENSE, DISCOLORS DEVO TEETH (<8 yo), FRANCONI-LIKE SYN (with outdated citric acid drug; N/V, acidosis) DD: potentiates Warfarin, ANTAGONIZES CIDAL AGENTS, CHELATED by cation (foods, antacids) Tx: G+, whimpy G-, ATYPICALS, RICKETTSIA, *ACNE, SIADH (Deme) |
Tetracycline
Oxytetracycline Demeclocycline |
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-reversibly binds 30S
-bacterioSTATIC -HE Excretion, ORAL=IV S/E: DISCOLORS DEVO TEETH (<8 yo), Vestibular syx (Minoc) DD: potentiates Warfarin, ANTAGONIZES CIDAL AGENTS, CHELATED by cation (foods, antacids) Tx: G+, whimpy G-, ATYPICALS, RICKETTSIA, *ACNE, Lyme Dis |
Doxycycline
Minocycline |
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-Req's VIRAL thymidine kinase, inhibits viral DNA pol
-RE (needs adjustment!), IV/PO S/E: cyrstalline nephropathy, dose dep N/V/D, CNS Syx, Hepatitis Tx: HSV infections (*IV DOC for HSV ENCEP), unknown for HZV, NOT for CMV |
Acyclovir
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-PRODRUG of acyclovir (PO only)
-converted by HE, good F S/E: CNS Syx at high dose Tx: HZV, HSV in HIV/Immunocom (less freq dose than acyclo) |
Valacylovir
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-req's VIRAL thymidine kinase, inhibits viral DNA pol
-LOW bioavailability S/E: BM Supp, CNS Sx, GI Tx: CMV, EBV infxs, some HSV, HZV |
Ganciclovir
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-PRODRUG of Ganciclovir
-MUCH better F -RE, requires adj S/E: BM Supp, CNS Sx, GI Tx: CMV prophy, retinitis |
Valganciclovir
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-ONLY available as TOPICAL CREAM in US
-req's VIRAL thymadine kinase, inhibits HSV polymerase (DNA/rep) S/E: site irriation TX: HSV cold sores |
Penciclovir
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-PRODRUG of Penciclovir
-req's VIRAL thymadine kinase, inhibits HSV polymerase (DNA/rep), good F -RE, dose adjust S/E: CNS/HA,GI Tx: HZV (w.i 72hrs), HSV esp in HIV/AIDS to avoid nephropathy |
Famciclovir
|
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-MOA unclear but NOT VIRAL thymadine kinase
S/E: HIGHLY Nephrotoxic, Neutropenia, acidosis (**MUST BE given w/saline and Probenecid) Tx: RESERVED for CMV retinitis in HIV/AIDS that fail Ganciclovir/foscarnet |
Cidofovir
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-competes for VIRAL pyrophosphate site (iorganic phosphate)
S/E: NEPHROTOXIC, LYTES DISTURBANCES, GI, CARDIO/EKG Changes Tx: CMV Retinitis (2nd line b/c of S/Es), HSV in HIV/AIDS |
Foscarnet
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-originally retroviral, met to ddATP, incorp into VIRAL DNA, chain term
-RE, dose adj, GOOD F S/E: LACTIC ACIDOSIS, SEVERE HEPATOMEGALY *black box, Peripheral Neuropathy Tx: HEP B, HIV |
Lamivudine
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-MOA UNKNOWN
-Food INCREASES Abs, T1/2 100-200 hrs! -RE, dose adj S/E: Anemia (esp if w/interferon) Tx: RSV, Hep C (*DOC with interf) |
Ribavirin
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-topical Tx for HPV warts
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Imiquimod
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-prevents viral entry into cells
-RE (adj Am) S/E: CNS Tx: Prophy/Tx for FLU A (w/i 48 hrs), Ama for Parkinson's |
Amantadine
Rimantidine |
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-inhibits VIRAL NEURAM req'd for viral release, reduces spread
S/E: N/V/D (Oral O), bronchospasm (inhaled Z) Tx: Treat/prophy FLU A & B |
Osteltamivir
Zanamivir |
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-structural analogs of nucleic acids
-block RT by competition -RE TX: HIV -generally no DDRxns Zidovudine, lamivudine, Stavudine, Zalacitabine, didanosine, abacavir, tenofovir, Emtricibaine |
NRTIs
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-NRTI for HIV
S/E: BONE MARROW Supp |
Zidovudine
|
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-NRTI for HIV
-LEAST toxic |
Lamivudine
Emtricitabine |
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-NRTI for HIV
-NEUROPATHY, LACTIC ACIDOSIS, HEPATIC STEATOSIS |
Stavudine
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-NRTI for HIV
-PERIPHERAL NEUROPATHY, PANCREATITIS |
Didanosine
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-NRTI for HIV
-SEVERE PERIPHERAL NEUROPATHY |
Zalcitabine
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-bind directly to RT are not incorporated or +PO4
-MOST Susceptible to Resistance if MONOTHERAPY, HAVE to have COMPLIANCE S/E: RASHES Nevirapine, Efavirenz, Delvaridine |
NNRTIs
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-NNRTI
-RASH, elevates LFTS |
Nevirapine
|
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-NNRTI
-RASH, STEVEN's JOHNSON SYNDROME -inhibits CYP3A |
Efavirenz
|
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-NNRTI
-RASH, CNS Syx (can be severe) |
Delvaridine
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-inhibit HIV protease-1, so viral chains are not cleaved
-HE, DD Rxns S/E: Lipid abnormalities, glucose abnormalities, GI Syx AmprenAVIR, Fosamprenavir, Atazanavir, Indinavir, Nelfinavir, Ritonavir**, Saquinavir, Tipranavir |
Protease Inhibitors (PIs)
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-PI
-used as a "Booster" with other PIs, allowing for lower pill burden |
Ritonavir
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-Viral Fusion Inhibitor
-Blocks HIV1 entry into cells -SUBQ S/E: INJECTION SITE IRRIT, NODULES, expensive, inconvenient TX: for pts that fail other regimens! |
Enfuvirtide
|
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Atazanavir+Indinavir= hyperbiliruinemia
Didanosine+Zalcitabine= severe peripheral neuropathy Stavudine+Zalcitabine= severe peripheral neuropathy |
Anti HIV drug combos to AVOID
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- ONE NNRTI + TWO NRTIs
- COMBO PI + TWO NNRTIS |
HIV TX
|
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-Post HIV Exposure Prohphy, start w/i 2 hours for 28 days
(no Etoh) |
Combivir
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-binds to ergosterol, alters mem perm so K, etc leak out, lysis
-Static or Cidal [] dep -POOR CSF, has to be intrathecal S/E: 80% NEPHROTOXIC, direct vascoconstrictive, usually rev, Anemia, Lyte changes, Infusion related (premed with NSAIDs) Tx: virtually ALL fungal infections GOLD STANDARD |
Amphotericin B
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-same as Amphi B, but less nephrotoxic, under study
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Amphotercinin B Lipid (Liposomal)
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-penetrates fungal cell walls, met to 5-FU, antimetabolite (like in CA TX)
-good CSF penetration S/E: BM hypoplas, N/V/D Tx: Serious Crypto and Candida (syngerism with Amphi B) |
5-Flucytosine
|
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-Triazole, interferes more selectively with fungal p450
-Oral=IV, not affected by pH or food -Good CSF penetration -RE S/E: N/V/D, elevated LFTs DD: potentiates warfarin, cyclosporin Tx: Crypto, Coccoi, Candida |
Fluconazole (IV, PO)
|
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-Imidazole, interferes with Fungal P450 (ergosterol)
-ph depend F (needs acidic) S/E: dose dependent hormone depression*, N/V/D, elevated LFTs DD: decreased absopt with PPIs, H2s, Anatacids, potentiate warfarin, cyclosporin Tx: histo, blasto, cocco, candida, tinea (miconazole) |
Ketoconazole (PO, Top)
(Miconazole, IV, Top) |
|
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-Triazole, interferes more selectively with fungal p450
-Oral only, not affected by pH or food -POOR CSF penetration -RE S/E: N/V/D, elevated LFTs DD: potentiates warfarin, cyclosporin Tx: ASPERGILLOSIS, histo/blasto with less S/E than amphi B, crypto, coccio, topical for tinea |
Itraconazole (PO)
|
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-disrupts mitotic spindle, arrests cells in metaphase
-ORAL S/E: H/A, Dizzy DD: induces P450, adj warfarin Tx: dermatophytosis when topicals fail |
Griseofulvin
|
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-inhibits SQUALENE Epoxidase, so sterol synth is halted)
S/E: RASH can be severe, HAs DD: rifampin increases Cl by 100%, cimetidine decreases Cl, cyclosporin Cl increased Tx: Onychomycosis but expensive |
Terbinafine (Lamasil)
|
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N:Oral suspension for candida (thrush), not absorbed from GI tract
C: OTC troches for thrush/topical for ath. foot |
Nystatin
Clotrimazole |
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-ANTImalarial
-prevents parasites from protecting themselves from ferriprotoporphyrin IX (via heme polymerase) -effective against asexual/erythrocyte forms -T1/2=4 days (prophy) S/E: CNS, DO NOT use with Psoriasis, liver dis Tx: prevent, tx malaria |
Chloroquine
|
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-ANTImalarial
-interfers with MTC function -ONLY agent avail for tx exoerythrocytic hyonozoites of VIVAX and OVALE in LIVER S/E: HEMOLYSIS with G6PD def Tx: Radical cure for vivax, ovale; used after Chloroquine in tx |
Primaquine
|
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-ANTImalarial
-Unknown MOA (thought similar to chloro) -Used in Chloroquine resistance S/E: CINCHONISM, Bad TI TX: DOC for parental FALCIPARUM (but Unavail in US) |
Quinine
|
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-ANTImalarial
-Unknown MOA (thought similar to chloro) -Used in Chloroquine resistance S/E: EKG changes, hypotension TX: DOC for parental FALCIPARUM in chlor reist (IS avail in US) |
Quinidine
|
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-ANTImalarial
-Quinine derivative -only effective against shizonts Tx: Prophy against CHLORO resist FALCIPARUM (resistance to mef now problem as well) |
Mefloquine
|
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-ANTImalarial
-Related to TMP, inhibits DHFR, used in combo with sulfa and quinine in chloro resistance S/E: N/V/D, Anemia, *must give LEUCOVORIN replacement Tx: malaria, TOXOPLASMOSIS (with sufla and leuco) |
Pyrimethamine
|
|
|
-AntiGIARDIAL/AntiAMEBIC agent
-serves as e acceptor forms cytotoxic agent, free radicals S/E: METALLIC TASTE, DISULFRAM effect Tx: ANAEROBIC BACT, AMEBAS,GIARDIA, TRICH, Blastocysts (has systemic and luminal activity) |
Metronidazole
|
|
|
-AntiGIARDIAL
-available in suspension, so good for peds pts. |
Furazolidine
|
|
|
-luminal AntiAMEBA
-DOC for asymptomatic cyst passage |
Idoquinol
|
|
|
-luminal AntiAMEBA
-poorly absorbed aminoglycoside, alt to idoquinol |
Paromycin
|
|
|
-DOC for Leishmainia (antimonal)
-only available from CDC/manufact |
Sodium Stibogluconate
|
|
|
-DOC for Chagas (SA Trypanosomes)
-Only available from CDC/manu |
Nitrofurtimox
|
|
|
DOC for African SS (Trypanosomes)
-Also can use pentamidine |
Eflornithine
|
|
|
-AntiHELMINT
-Selectively binds helmin TUBULIN and blocks assembly, inhibits glucose uptake tx: DOC for Ascariasis (round), Trichuriasis (whip) Hookworm |
Mebendazole
|
|
|
-AntiHELMINTH
-GABA receptor agonist, which causes paralysis Tx: DOC for Stronylosidiasis |
Ivermectin
|
|
|
-AntiHELMINTH
-Depolarizing NM BLOCKER -DOC for Enterobiasis (pin), alter in other worms |
Pyrantel Pamoate
|
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DOC in Filarisis
|
Diethylcarbamazine
|
