Beta-lactam MOA
Form covalent bonds with PBP transpeptidase inhibiting activity
Vancomycin MOA
Binds end of polypeptide chain to prevent elongation
Daptomycin MOA
Cyclic lipopetide: binds to cell membrane resulting in depolarization and loss of membrane potential and cell death
Fosfomycin MOA
Blocks first step of peptidoglycan synthesis
Bacitracin MOA
Inhibits lipid carrier bringing peptidoglycan out to the cell
Antibiotic
Natural compound produced by bacteria or fungi
Antimicrobial
Synthetic compound that inhibits bacteria
Gram Negative
Outer lipopolysaccharide covering Thin cell wall
Stains Pink
Gram Positive
Peptidoglycan
Thick Cell Wall
Lack Outer Membrane
Stains Purple
Cell Wall
Peptidoglycan
Transpeptidase
cross-link adjacent strands to give lattice structure for wall
Penicillin Binding Protein
(Enzymes) Responsible for assembly, maintenance, and regulation of peptidoglycan cell wall
Penicillinase Resistant Penicillins
Dicloxacillin
Nafcillin (parenteral)
Oxacillin
Broad Spectrum Penicillins
Ampicillin (+ Sulbactam)
Amoxicillin (+ Clavulanic acid)
Antipseudomonal Penicillins
Piperacillin (+ Tazobactam)
Ticarcillin (+ Clavulanic acid)
Penicillin elimination
Eliminated through active tubular secretion.
Aminoglycoside MOA
Prevents initiation of meth-tRNA from binding to 30s and 50s
Tetracycline MOA
Binds 30s subunit to prevent tRNA from binding to A site and prevents elongation of the peptide.
Microlides and Ketolides MOA
Binds 50s subunit and interferes with initiation complex - Interferes with transfer of peptide tRNA complex from site A to P site - prevents elongation
Lincosamides MOA
Binds to 50s subunit and interferes with the initiation complex - prevents elongation
Cloramphenicol MOA
Binds to 50s subunit - inhibits bond formation between peptide and new amino acid
Dalfopristin MOA
Binds 50s subunit - prevents peptide bond formation
Quinupristin MOA
inhibits tRNA synthesis
Oxazolidinones (Linezolid) MOA
Binds specific 23s ribosomal DNA on 50s subunit preventing fromation of functional 70s ribosomal unit
Mupirocin MOA
Inhibits isoleucyl-tRNA synthase
Sulfonamides MOA
inhibits folate production and incorporation into purines and prevents DNA synthesis
Trimethoprim MOA
Inhibits dihydrofolate reductase - prevents tetrahydrofolate formation
Fluroquinolones MOA
Inhibits DNA gyrase in gram (-)
Inhibits topoisomerase type IV in gram (+)
Methenamine MOA
acidification of urine promotes formation
Nitrofurantoin MOA
Reduced form damages bacterial DNA - reduced in bacteria
Polymyxin B MOA
cationic detergent, hydropobic and hydrophilic regions disrupts membrane in gram (-) bacteria
Isoniazid MOA
Inhibits mycolic acid production - inhibits the waxy coat
Rifampin MOA
Inhibits DNA dependent RNA polymerase - forms complex with enzyme
Ethambutol MOA
Mechanism unknown - inhibits mycolic acid incorporation into membranes, no effect on other bacteria
Pyrazinamide MOA
lowers pH so bacteria can't grow - enters macrophages
Dapson MOA
Inhibits mycobacteria folic acid synthesis
Clofazimine MOA
MOA unknown - binds to DNA
Amphotericin B MOA
forms channels in membrane to allow K and Mg to leak out of the cell - oxidative damage to the membrane
Flucytosine MOA
Inhibits thymidylate synthesis - inhibits DNA synthesis
Azoles MOA
Inhibit lanosterol demethylase - decreased ergosterol
Echinocandins MOA
Inhibit 1, 3-B-D-glucans in cell wall formation
Griseofulvin MOA
Inhibit microtubules - inhibit cell division in Dermatophytes
Allylamines MOA
Inhibit aqualene epoxidase - decreased ergosterol
Metronidazole MOA
Protozal enzyme mediates formation of free nitroradicals which attack DNA
Pyrimethamine MOA
Inhibits protozoal dihydrofolate reductase - prevents growth in RBC
Chloroquine MOA
Clears protozoa from the blood (72h)
Atovaquone MOA
Inhibits mitochondrial function - inhibits liver stage of malaria
Trifluridine, Idoxuradine MOA
Thymidine analog - added into viral DNA by plymerase - can't add next base pair
Acyclovir, Valacyclovir MOA
Guanine analog - selectively phosphorylated by viral thymidine kinase added to viral DNA
Foscarnet MOA
Pyrophosphate derivative - inhibits viral DNA polymerase
Amantadine, Rimantidine MOA
Blocks uncoating of influenza A, but not B
Oseltamivir, Zanamivir MOA
Selective inhibitors of viral neuraminidase
Ribavirin
Modified purine base with d-ribosoe sugar - mechanism unknown - inhibits messenger RNA synthesis
Interferon Alfa MOA
antiproliferative and immune modulating actions, increase phagocytes
Lamivudine MOA
Inhibits DNA polymerase/reverse transcription in HBV
Adenfovir MOA
Adenosine analog prodrug inhibits viral DNA polymerase and reverse transcriptase
Maraviroc MOA
prevents the virus from binding to the chemokine co-receptors 5 receptors - inhibits the virus from entering the cell
Enfuvirtide MOA
36 amino acid peptide that blocks the entry into the cell by binding to the pg41 subunit, thus preventing the conformational change
NRTI and NNRTI MOA
competitively bind to the virus' reverse transcriptase enzyme (converts RNA to DNA) to block further nucleoside addition to the new replicating viral particle.
Abacavir
Hepatic elimination - good if renal problems
Didanosine
Weight based dosing, pancreatitis, neuropathy, portal hypertension
Emtricitabine
treats Hepatitis B, well tolerated
Lamivudine
Treats Hepatitis B, Increased resistance in HIV and HBV
Tenofovir
Proximal tubule toxicity, bone abnormalities, long half life
Stavudine
Very Very bad - do not use, lipodystrophy, mitochondrial toxic, peripheral neuropathy
Zidovudine
Bone marrow suppression, first agent in pregnancy
Efavirenz
Pregnancy category D, CNS 52%, preferred agent
Nevirapine
inducer of 3A4 (dose for autoinduction), rash, worst hepatotoxicity
Etravirine
BID, food required
Integrase Inhibitors (Raltegravir) MOA
Binds integrase preventing the integration of the HIV DNA into the host genome
Protein Cleavage Inhibitors MOA
prevents cleavage of the new post-translational HIV polyproteins into active viral components. Results in immature noninfectious particles
Atazanavir
requires food, increased bilirubin, PR prolongation, renal stones, preferred agent
Darunavir
Preferred agent, inhibits 3A4, sulfa moiety
Indinavir
Hydrate nephrolithiasis, biliary increase
Lopinavir + Rotinavir
Kaletra, Bad GI, Lipids
Nelfinavir
Requires food, causes diarrhea, not recommended
Ritonavir
potent 3A4 and 2D6 inhibitor, BAD GI, hepatitis
Tipranavir
BID, Food, Intracranial hemorrhages, hepatits, not first line agent due to adverse effects
Epzicom
Abacavir/Lamivudine
Truvada
Tenofovir/Emtricitabine
Combivir
Zidovudine/Lamivudine
Trizivir
Zidovudine/Lamivudine/Abacavir