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Antimicrobials
| Term | Definition |
|---|---|
| B-lactams | bind to active enzymes |
| Penicillins | Cloxacillin, Ampicillin/amoxicillin, amoxicillin/clav acid, Ticarcillin, piperacillin, piperacillin/tazobactam. TREATS: Gram + cocci. Syphillis, endocarditis, meningitis, pneumonia. |
| Cephalosporins | more stable towards beta-lacatmase, broader spectrum then penicillin, activity depends on side chain, BACTERIACIDAL. |
| Carbapenems | Imipene/Cilastin, Meropenem, Ertapenem, Doripenem |
| Cell wall synthesis inhibitors USES | TREATS: Gram + and Gram – and anaerobes. BROAD SPECTRUM Used for MDR and/or systemic infections. Monobactams |
| Cell wall synthesis inhibitors (B-lactams) | Carbapenems, Cephalosporins, Penicillins, B-lactams |
| Cell wall synthesis inhibitors (Glycopeptides) | Vancomycin, bacitracin |
| Vancomycin | prevents transfer of sugar pentapeptide (inhibits biosynthesis of peptidoglycan) Acts 1 step earlier than penicillin. |
| Vancomycin SIDE FX, DOWNS, Toxicity | USES: Gram + bacteria. Restistance emerging. DOWNS: Poor CNS penetration, Poor oral absorbation, renal excretion Toxicity: red man syndrome, nephrotoxicity. |
| Bacitracin | polypeptide antibiotic, often found in combination with polymixin, neomycin. Topical creams and ointments (polysporin). |
| Protein synthesis inhibitors (aminoglycosides 30S) | Gentamicin, Tobramycin, Amikacin |
| Gentamicin, Tobramycin, Amikacin | CDKR and PAE macrolides, neomycin, streptomycin Spectrum: aerobic gram-negative bacilli -with penicillin for gram + |
| Gentamicin, Tobramycin, Amikacin USES and SIDE FX | MOA: Interferes with protein synthesis =misread genetic code, =wrong amino acid = death. BACTERICIDAL Side effects: acute tubular necrosis, glomerular toxicity, ototoxicity |
| Protein synthesis inhibitors (tetracyclines 30S) | tetracycline, doxycycline, minocycline, tigecyline |
| Azithromycin, clarithromycin, erythromycin | Many gram + and some gram – h. pylori |
| Azithromycin, clarithromycin, erythromycin USE, MOA, SIDE FX | Use: upper respiratory tract, peptic ulcer, Chlamydia MOA: Inhibits peptidyl transferase Side effects: GI discomfort, (nausea heartburn etc..), no serious toxicities Some inhibit CYP3A4 Pneumococcal and staphylococcal usually resistant. |
| Tetracycline, doxycycline, minocycline, tigecyline | BROAD SPECTRUM Gram +ve, Gram -, MRSA etc.. Mycoplasmas, chlamydiae, protozoa |
| Tetracycline, doxycycline, minocycline, tigecyline USES, MOA, SIDE FX | USE: -Lyme disease, Chlamydia, SSTIs (ex: acne) MOA: Block binding of tRNA to 30S subunit. BACTERIOSTATIC Side effects: Nephrotoxicity, hepatoxicity (incr risk in pregnant woman,) teeth discolouration, photosensitivity. Quick development of resistence |
| Protein synthesis inhibitors (macrolides 50S) | Azithromycin, clarithromycin, erythromycin, |
| Clindamycin Fluorquinolones Cyproflaxin | a lincosamide used for gram +ve cocci, anaerobes, MRSA, penicillin resistant strep. Prevents translocation of peptide from A site to P site. NUCLEIC ACID INHIBITORS |
| Linezolid | oxazolidinedione that binds 23S RNA component of 50S ribosome. Used on gram +ve. Bacteriostatic for enterococci and bacteriocidal for streptococci. Use for WRE, MSSA, MRSA pneoumonia, |
| Mupirocin | competes for bining to tRNA. Used on gram +ve bacteria. Use on staphylococci, MRSA, B-hemolytic strep. Side effect: skin infections. Available as a topical cream. |
| RNA polymerase inhibitors | METABOLISM INHIBITORS: Trimethoprim, Sulfamethoxazole and Dapsone |
| Sulfamethoxazole and Dapsone | Inhibits Dihydropteroate Synthetase (first step) |
| Trimethoprim | Inhibits Dihydrofolate Reductase (third step). USES: Gram +, Gram – |
| Trimethoprim COMMON INFECTIONS, TOXICITY | Common infections: UTI, prostatic infections, pulmonary infections. Toxicity: hypersensitivity reactions (Stevens-Johnson syndrome), GI (N/V/D), Blood hemolytic anemia, low platelets, low white count CELL MEMBRANE INHIBITORS Only in USA |
| Fluoroquinolones | inhibit 2 types of bacterial type IIa topoisomerases (DNA gyrase and Type IV topoisomerase). Well tolerated. Can cause seizures, changes in blood glucose, and phototoxicity. |
| Nucleic acid inhibitors | Fluoroquinolones |
| Acyclovir, Famiciclovir, Penciclovir, Valcyclovir | Treat HSV, VZV infections. Prevent CMV infections. |
| Antivirals (Nucleoside Analogs) | Acyclovir, Famiciclovir, Penciclovir, Valcyclovir, Ganciclovir, Valgancilclovir, Cidofovir |
| Ganciclovir, Valgancilclovir, Cidofovir | prevent and treat CMV infection. |
| Antivirals (Neuraminidase Inhibitors) | Oseltamivir, zanamivir |
| Oseltamivir, zanamivir | bind to active site and inhibit neuraminidase enzyme. For Influenze A and B |
| Antivirals (Adamantanes) | Amantadine, Rimantadine |
| Amantadine, Rimantadine | block the M2 proton selective ion channel. For Influenza A only. |
| HIV Drugs (Reverse transcriptase inhibitors) | NRTIs, NNRTIs |
| NRTIs | gets converted to active metabolite in host cell. Compete with nucloside triphosphates for incorporation into viral DNA. Cause DNA chain termination. |
| NNRTIs | directly bind to reverse transcriptase, disrupting active site. |
| Protease inhibitors | Bind to active site of HIV protease. |
| HEPATITIS DRUGS | Ribavirin, Interferons |
| Ribavirin | purine analogue inhibits synthesis of viral nucleic acid. (inhibits inosine monophosphate dehydrogenase) |
| Interferons | increase host cell defenses that lead to viral and infected cell destruction. |
| ADD | Tazobactam, Clav acid, Sulbactam |
Created by:
vbukorovic
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