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Antimicrobial Drugs
Kaplan
| Question | Answer |
|---|---|
| What are some Antimicrobial agents that “inhibit cell wall synthesis” ? | Penicillins, Cephalosporins, Vancomycin, Imipenem, Meropenem, Aztreonam |
| Antimicrobial agents that inhibit bacterial protein synthesis? (4) | Aminoglycosides (only work on aerobic organisms), Macrolides, Tetracyclines, Chloramphenicol |
| Antimicrobial agents that inhibits Nucleic acid synthesis? (2) | Fluoroquinolones, Rifampin |
| Antimicrobial agents that inhibits folic acid synthesis? (3) | Sulfonamides, Trimethoprim, Pyrimethamine |
| What are the two main ways that Antimicrobial chemotherapy work? | 1. Bactericidal (kill the organism) 2. Bacteriostatic (stop the growth) - hoping that the patient immune system is going to take over and kill the rest of the bacteria, that is why not given to immunocompromised patients. |
| What are a side effect of aminoglyc(O2)sides (2)? | 1. Nephrotoxic 2. Ototoxic 2 ears and kidneys |
| What is a known combination of Antimicrobial agents that cause syngergism? | PENICILLINS and AMINOGLYCOSIDES |
| The cell wall synthesis inhibitors are divided into 2 categories which are… | 1. B- lactic drugs 2. Non- B lactase drugs (Vancomycin) |
| What are the 2 building blocks of bacterial cell wall? | 1. NAM (N-Acetyl Muramic acid) 2. NAG (N-Acetyl Glucosamine) |
| Which enzyme plays a role in peptidoglycan elongation (laying the bricks NAM and NAG) down? | Transglycosylase |
| Which enzyme plays a role in cross links of the peptidoglycan layer? | Transpeptidase |
| Which drug affects the EARLY STAGES of bacterial cell wall formation? | VANCOMYCIN (by inhibiting transglycosylase) |
| Which group of drugs inhibits (irreversibly) the cross linking of peptidoglycan cell layer? | B- lactam rings also known as PBP’s (Penicillin binding protein) |
| What are the (3) mechanism of RESISTANCE of penicillins? | 1. Penicillinases (b-lactamase) break lactam ring 2. Structural change in PBPs (seen in MRSA) 3. Change in porin structure (Pseudomonas) |
| What are the (4) types of Penicillins? | 1. Antistaph penicillins 2. Natural penicillins 3. Amino penicillins 4. Antipseudomonal penicillins (As you go down more gram negatives are covered) |
| What are the Antistaph penicillins (3)? | 1. Nafcillin 2. Oxacillin 3. Methicillin B- lactamase resistance |
| What are the Natural penicillins? (2) | 1. Penicillin G 2. Penicillin V B- lactamase sesitive |
| What are the Aminopenicillins? (2) | 1. Amoxicillin 2. Ampicillin B-lactamase sensitive |
| What are the Antipsedomonal penicillins (1) ? | 1. Pipercillin ( B-lactase sensitive) 2. Ticacillin |
| What are the beta-lactamase inhibitors that enhance the MOA of Penicillins? (2) | 1. Clavulanic acid 2. Sulbactam |
| Which Penicillin is used for treatment of Listeria? | Ampicillin (aminopenicillins) |
| Which Penicillin is used in treatment of Syphilis? | Benzathine penicillin G (a natural penicillin) |
| What are the side effects of penicillins? (2) | 1. Hypersensitivity 2. Jarisch- Herxheimer reaction in treatment of syphilis. This is a fever like reaction that occurs dt sudden release of the bacteria’s endotoxins. |
| Penicillins active tubular secretion can be blocked by which drug? | Probenecid (Treatment for chronic gout) |
| What are the 2 penicillinase inhibitors that are suicide inhibitors? | 1. Clavulanic acid 2. Sulbactam Suicide inhibitor: The enzyme "commits suicide" by activating the inhibitor that ends up permanently disabling it. Thinking the “enzyme is a normal substrate. |
| What is the mechanism of action of Cephalosporins? | INHIBITS TRANSPEPTIDASE (same as Penicillins) |
| How many generations of Cephalosporins are there? | 5 |
| What are the 1st generation Cephlosporins (2) and their coverage spectrum? | 1. Cefazolin 2. Cephalexin Narrow spectrum (grampositives- strep and MSSA) Does NOT cross the CNS For gram+ and skin |
| What are the 2nd generation Cephalosporins (4) And their coverage spectrum? | 1. Cefotetan 2. Cefaclor 3. Cefuroxime (enters CNS) 4. Cefoxitin (NOT REALLY TESTABLE) Broad pspectrum (kills gram negatives as well as gram positives) Does NOT enter CNS, except for one |
| What are the 3rd generation Cephalosporins (4) | 1. Ceftriaxone 2. Cefotaxime 3. Cefdinir 4. Cefixime MOST enters CNS For meningitis + serious infection |
| Which (2) 3rd generation Cephalosporins are used in the treatment of meningitis? | 1. CeftriAXone 2. CefotAXime AXE to the head |
| What is the 4th generation Cephalosporins (1) ? | 1. Cefepime (IV) Enters CNS For Pseudomonas |
| What is the 5th generation Cephalosporins? (1) | 1. Ceftaroline (for MRSA, kill more gram positives than negatives) |
| Which drug is used for neonatal meningitis? | CefotAXime (NOT ceftriAXone bc it is eliminated by bile and neonates has a decreased metabolism and smudging of the bile) |
| If patient develop rash on Penicillin which drug is used instead? | Cephalosporins (dt same mechanism, diff side effects) |
| If patient develop anaphylaxis on Penicillin, which drug group must be avoided? | AVOID B-Lactams |
| What are the 2 “-penem” drugs (cell wall synthesis inhibitors) and their MOA? | 1. Imipenem 2. Meropenem MOA; Inhibits Transpeptidase (same as Penicillins and Cephalosporins) Resistance to B-lactamase |
| Which cell wall synthesis Antimicrobial is given as empirical treatment in severe life threatening infections? | “-penems” (Imipenem or Meropenem) VERY VERY broad spectrum |
| Imipenem is given with which OTHER drug and what is the reason? | Given with CILASTATIN (“silly”statin because it is not a -statin drug) INHIBITS Imipenem metabolism to a nephrotoxic metabolite. ( its a renal dehydropeptidase inhibitor) |
| What is a side effect is Imipenem? | SEIZURE (occurs in overdose or renal dysfunction- bc it undergoes renal elimination) |
| MOA of Aztreonam? | Same MOA as Penicillins and Cephalosporins w/o cross- allergenicity w penicillins and cephalosporins because it lacks 2nd ring (b-lactam) |
| what is the MOA of Vancomycin? | Inhibits TRANSGLYCOSYLASE (by binding to the D-ala D-ala of NAM) |
| What is the coverage spectrum of Vancomycin? | Severe Gram positives (MRSA, Enterococci, Clostridium difficile) |
| In enterococcal resistance the D-ala on NAG gets substituted for what? | D- lactate |
| What is a side effect of Vancomycin and WHY? | RED MAN SYNDROME (dt Histamine release) this occurs when the drug is administered too rapidly causes flushing/redness of the skin dt histamine release. |
| What are the B-lactams and NON B-lactams Antimicrobial agents? | B- lactams: Pen, Cephalopod, -penem, Aztreonam (only has 1 ring) NON B-lactams: Vancomycin |
| What are the 2 groups of drugs that work at/inhibit the 30s? | 1. Aminoglycosides 2. Tetracyclins |
| What are the 2 groups of drugs that work at/ inhibits 50s? | 1. Macrolides 2. Singles |
| What are the (4) mechanism of protein synthesis inhibition? | 1. Formation of initiation complex 2. Amino-acid incorporation 3. Formation of peptide bond 4. Translocation (acceptor to donor site) |
| MOA of Tetracycline? | Blocks the attachment of aminoacyl tRNA to acceptor site (amino acid incorporation) |
| MOA of Chloramphenicol? | Blocks formation of peptide bond. (Inhibits the activity of peptidyltransferase) |
| MOA of Macrolides and Clindamycin? | Blocks translocation (inhibits translocation of peptidyl tRNA from acceptor to donor site) |
| What are the Aminoglycosides and their MOA? (4) | 1. Gentamycin 2. Tobramycin 3. Amikacin 4. Streptomycin MOA: block initiation, translocation and misreading Accumulate in AEROBIC GRAM NEGATIVES and is bactericidal |
| What are the 3 side effects of Aminoglycosides? | 1. Nephrotoxicity 2. Ototoxicity 3. Blocks Ach release by blockiade of presynaptic calcium channels —> muscle weakness |
| Where is Streptomycin used and its the DOC for what? | Used in Tuberculosis DOC in: bubonic plague and tularemia (It is a Aminoglycosides) |
| What are the Tertracylins? (2) and MOA | 1. Doxycycline 2. Minocycline MOA: block docking at tRNA Tets for Ticks (Rocky mountain fever, Lyme disease) |
| What are the Antibiotics that are SAFE in PREGNANCY? (3) | 1. Penicillins 2. Cephalosporins 3. Macrolides |
| What are the 3 organisms that Tetracycline is good for? | 1. Chlamydia 2. Rickettsia 3. Borrelia burgdorferi |
| What are the contraindications of Tetracyclins? | Chelators! Bind divalent cations (Ca, Mg, Al)which decrease their absorption (also avoid dairy products) Chelator : A substance that binds to metal ions in the body, facilitating their excretion. |
| What are the side effects of Tetracyclins? (2) | 1. Phototoxicity 2. Tooth enamel dysplasia and decrease bone growth in children dt CALCIUM |
| What is the MOA of Chloramphenicol? | Blocks peptidyltransferase (works at 50s) |
| Chloramphenicol is metabolized by what? | Hepatic glucoronidation |
| What is a major side effect of Chloramphenicol and WHY? | GRAY BABY SYNDROME because neonates have a low glucuronyltransferase so the drug accumulates causing a gray discoloration |
| What are the Macrolides (3) and their MOA? | 1. Erythromycin 2. Azithromycin 3. Clarithromycin MOA: Blocks TRANSLOCATION They inhibit cytochrome P450 (Clarithromycin) |
| What are the 2 major organisms that Macrolides work good against? | 1. Mycoplasma 2. MAC (mycobacterium avium intracellular) MAC (and cheese) is Mmm-mm m & m mycoplasma, MAC m&m motilin, methylation of binding site |
| What is the side effects of Macrolides? | GI DISTRESS (bcit stimulate the motility receptors) ud in diabetic gastroparesis to stimulate motility, that’s why diabetic patients feels full early when eating. |
| Clindamycin MOA and side effect? | MOA: Blocks translocation (same as Macrolides) Side effect: most common cause of PSEUDOMEMBRANOUS COLITIS (by c. Diff) |
| Linezoid MOA, Uses, and S/E | MOA: Blocks initiation complex Uses: VRSA, VRE (used when Vancomycin fails) S/E: serotonin syndrome bs MAO-A and B inhibitor |
| What are the STREPTOGRAMINS? (2) and their MOA | 1. Quinupristin 2. Dalfopristin MOA: Blocks the attachment of tRNA to acceptor site ( at 50s subunit)- inhibit amino acid incorporation |
| Streptogramins are used for which organisms? | E. Faecium (also VRE faecium) but NOT E. Faecalis Linezoid is for both type of enterococci |
| What are the inhibitors of Folic acid synthesis? (3) | 1. Sulfonamides 2. Trimethoprim 3. Pyrimethamine |
| What enzyme does Sulfonamides inhibit? | Dihydropteroate synthetase (enzyme that allows Pteridine+ PABA —> Dihydropteroic acid) ONLY FOUND IN BACTERIA |
| Which enzyme does Trimethoprim and Pyrimethamine inhibits? | Dihydrofolate reductase Found in BACTERIA and HUMANS Trimethoprim + Sulfonamides —> synergy |
| Sulfasalazine is used for what (2 conditions) and what it its COMPOSITION? | Used in: ULCERATIVE COLITIS and RHEUMATOID ARTHRITIS Composed of: 5-ASA and SP 5-ASA = 5- aminosalicylic acid (for ulcerative colitis) SP= sulfapyridine (for rheumatoid arthritis) |
| TMP- SMX is used for what? (3) | 1. UTIs 2 .Pneumocystis jiroveci (fungus) 3. Toxoplasma gondii (protozoa) |
| What are the side effects of Sulfonamides? (3) | 1. Hypersensitivity (Steven’s—Johnson syndrome- hemorrhagic crust of lips/oral mucosa) 2. Hemolysis in G6PD deficiency 3. Phototoxicity |
| What are the “Quinolones” that inhibits Nucleic acid synthesis? | “-floxacins” Ciprofloxacin and Levofloxacin |
| What are the MOA of Quinolones? | Inhibit TOPOISOMERASE 2 (DNA gyrase) and 4 (separation o replicated DNA during cell division) |
| Which divalent inhibits Quinolones absorption? (2) | Iron, Calcium |
| What are the side effects of Quinolones? (2) | 1. Tendonitis, Tendon rupture , Nerve damage 2. Phototoxicity |
| What are the 3 drug groups that cause “Phototoxicity” | 1. Fluoroquinolones 2. Tetracyclins 3. Sulfonamides FoToS |
| MOA of Metronidazole? | Converts to FREE RADICALS (by ferredoxin) and binds to DNA —> bactericidal |
| Which organisms does METRONIDAZOLE work on? (6) (GET BaC on the METRO G) | 1. Giardia 2. Entamoeba 3. Trichomonas 4. Bacterioides species 5. Clostridium 6. Gardnerella |
| What is the side effects of Metronidazole? (2) | 1. Disulfiram- like effect (vomiting, headache) 2. Metallic taste |
| What are the Antitubercular drugs? (4/5) | RIPE or RESPIre 1. Rifampin 2. Ethambutol (eyethambutol) 3. Streptomycin (backup drug) 4. Pyrazinamide 5. Isoniazid (INH) |
| How are antitubercular drugs used? | As COMBINATION DRUG THERAPY to prevent or delay resistance |
| MOA of Rifampin? and S/E | Inhibits DNA-dependent RNA polymerase S/E: Red-orange secretions (urine/sweat/tears), Induce P450, Hepatitis |
| MOA of Ethambutol? And S/E? | MOA: Inhibits synthesis of arabinogalactan S/E: decrease visual acuity and red-green discrimination |
| S/E of Pyrazinamide | Hyperuricemia (bc METABOLITE is a weak acid) |
| MOA of Isoniazid? And S/E? | MOA: Inhibits mycolic acid synthesis S/E: Sideroblastic anemia and Peripheral neuritis (Fix w vitamin B6) |
| What is the PROPHYLAXIS for MAC (Mycobacterium avium complex) ? | Azithromycin or Clarithromycin |
| What is the treatment of MAC (3 combination)? | Clarithromycin + Ethambutol + Rifabutin |
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DVD27