mykw Flashcards
Common mechanisms of Drug resistance?
Spontaneous mutations in target proteins, Natural enzymes that inactivate agent, Spontaneous changes in membrane permaability
Molecular Targets for Antimicrobial drugs
Cell Wall synthesis, DNA gyrase, DNA-Direction RNA polymerase, Protein synthesis, Cell membrane, Folic acid metabolism, Periplasmic space
Gram negative vs Gram positive
Gram negative has small cell wall, gram positive have big cell wall
B-lactam anibiotic classes
Cephalosporins and penicillins
Mechanism of Beta-lactam Action
Bind to Pencillin binding proteins, Inhibits peptidoglycan synthesis, Stimulates Autolysins, results in cell lysis
Beta Lactams are inactivated by?Static or cidal?Most effective against Gram pos or Neg?
B-lactamASES, Gram positive but can have effect on negative
What is the allergen from Pencillins?
Penicillinoic acid
Natural Pencillins, Route, and Target, CNS penetration?
G, V, G (Benzathine), G is iv/im, V is oral, G B is IM long acting. Gram positive. No CNS
What does MRSA really stand for?
Resistant to all Beta lactams
Semisynthetic Pencillins ases resistant, route, used for? CNS penetration?
Nafcillin, Dicloxacillin.. Good CNS with meniges inflammation
Semisynthetic Pencillins (Extended spectrum). Route, Spectrum? Combination of?
Amoxicillin, Ampicillin, Piperacillin Extended to Gram + and some Gram -. Combination of minopencillin + Beta-lactamase inhibitor(Clavulanate, Sulbactam,Tazobactam)
Synthetic Penicillin-Like (Carbapenems), Spectrum? Co-admined with?
Imipenem/Cilastatin. Broadest spectrum Most + and - . Coadministered with Cilastatin. Inhibitor of the degradation renal enzymes
Semi-synthetic monobactams. Spectrum? Not affected by?What patients?
Aztreonam. Inhibits PBP of Gram NEGATIVE ONLY, beta lactamases. Good for B-lactam allergic patients with gram negative
Cephalosporins are used as what in hospital settings?Natural product of?
Prophylaxis, molds
1st Generation Cephalorsporins, Specrum, Used for?
Cephazolin (Ancef), Cephalexin (Keflex), Gram + and Some gram -, Surgical prophylaxis, UTI
2nd Generation Cephalorsporins, Spectrum? Used for?
Cerfuroxime (Zinacef), Cefuroxime axitel (Ceftin), Intermediate Spectrum. Gram + and extended Gram Negative.
Third Generation Cephalorsporins. Spectrum? Used for? Special consideration?
Ceftriaxone (Rocephin), Ceftazidime (Fortaz), Broad spectrum Gram + and Gram Negative. CNS penetration
Fourth Generation cephalosporins. Spectrum? Used for?
Cefepime (Maxiprime). Very broad Gram + and Negative. Aerobic. Used for limited resistants and nosocomial infections
B-Lactam adverse reactions. 3 stages and effects
1st immediate= anaphylaxis <72 hours Milder, maybe rash. 3rd is Late reaction Drug fever
Tetracycline bacteriostatic or bacteriocidal?
Static
Tetracycline mechanism
Blocks tRNA bind=Block protein synthesis 30s
Tetracycle spectrum? UV? Divalent metals?
Very broad spectrum. Forms complexes with Teeth and Bones. Absorbs UV causing inflammatory response
Chloramphenicol block wwhat ribsome?
50s
Chloramphenicol spectrum? Cidal or static? Alternative for?
Extremely broad. Static. Alternative to Beta lactams for CNS
Chloramphenicol side effects bone marrow? Babys?
Grey baby, Bone marrow toxicity
Macrolide/Ketolides block what ribsome?Static or cidal?Spectrum?
50S, static, NO CNS, Gram positive with limited negative
Macrolide and Ketolide Protoypes
Erythromycin, Azithromycin, Clarithrymycin, Telithromycin, Clindamycin
Polumyxin spectrum? Acts on? Static or cidal? ROUTE?
Gram Negative bacteria. Acts on lipid membrane. BacteriCIDAL, TOPICAL only
Bacitracin Route? Spectrum? Mechanism?
Topical only. Limited to Gram positive. Blacks cell wall synthesis
Vancomycin Route? Spectrum? Mechanism?
IV/IM, Limited to Gram positive. Blocks cell wall synthesis
Inhibitors of Cell wall synthesis?
Bactracin and vancomycin
Tigecycline is for? Spectrum? Mechamism?Class?
Resistant strains. Tetracyline. Blocks tRNA binding on 30s ribosome. Broad + and - spectrum
Quinupristin/Dalfopristin (Synercid). Spectrum? Class? Used for? Mechanism?
Blocks protein synthesis on 30s ribosome. Used for ONLY Gram positive. For resistant Vanomycin strains. Macrolide class
Linezolid. Spectrum?Class? Used for? Mechanism?
Oxazolidone class. Blocks protein synthesis at TRNA formation. Broad against Gram positive. For VRSA
Daptomycin. Class?Spectrum?Used for?
Natural derived class. Used for MRSA and VRE. Gram positive
Mercaptopurine mechanism, converted to?
Blocks purine synthesis by being an analog of purine bases hypoxanthine or adenine, T-IMP
Azathioprine is?
prodrug of 6-MP
Methotrexate mechanism, inhibits what enzyme and synthesis
Inhibits dihydrofolate redutase and inhibits synthesis of thymidine and purines
5-Flurouracil mechanism, inhibits what? Inhibits synthesis of what?
Inhibits thymidylate synthase, inhibiting synthesis of thymidine
Hydroxyurea inhibits what?
ribonucleotide reductase
Anti-microtubules are considered to be what phase specific agents?
M phase
Anti dna nucleotide synthesis is for what phase?
G1
Vinca alkaloids mechanism? Vincristine, Vinblastine, Vinorelbine
Binds to tubulin and inhibit tublin polymerization
Taxanes (Paclitaxel, Docetaxel) mechanism
prevent depolymerization
Anthracyclines (doxorubicin, Daunorubicin mechanism
Insert into DNA, inhibits topoisomerase II and induce production of ROS. Deforming DNA
Bleomycin (blenozane, Cipla, Bleocip), anesthesia concerns
Requires metal and oxygen for its activity, causes DNA damage by producing ROS. Causes pulmonary fibrosis
Nitroden mustards:cyclophosphamide
Alklyating agents, crosslinking DNA.
Tamoxifen is?
Selective estrogen receptor modulator for breast cancer
Aromtase inhibitor (Anastrozole)
Blocks estrogen synthesis
Imatinib (Gleevec)
Inhibits Tyrosine kinase inhibitor for Chronic myeloid leukemia
Trastuzumab (Herceptin)
Monoclonal antibody against HER2, for breast cancer, cardiotoxic
Bevacizumab (Avastin)
Monoclomal antibody againsst Angiogensis
FDA Pregnacy rating ABCDX
A, adequate studies show no risk, B Animal studies fail to show risk, no study in human. C-Animals positive, no studies Human. D-Positive in human studies but may be used. X-Animals/Human positive and risks outweight benefits. N-No classification
Thalidomide concerns, which enantomer?
Presciped for pregnacy associated nausea, bilateral limb reduction, kidney eyes ears heart deformities. S enantiomer
Diethylstilbesterol (DES)
Oral synthetic nonsteroidal estrogen analog, Use to prevent miscarriages. Teratogen seen 20-30 years later