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Microbiology
FA complete review part 6 Antimicrobials (antibiotics, antivirals, antifungals)
| Question | Answer |
|---|---|
| What are the most common Sulfonamides? | Sulfamethoxazole (SMX), Sulfisoxazole, and Sulfadiazine |
| Trimethoprim is: | Folic acid synthesis and reduction (DNA methylation) |
| What two categories of antibiotics disrupt the cell wall? | 1. Peptidoglycan synthesis 2. Peptidoglycan cross-linking |
| What two common Glycopeptides? | Vancomycin and Bacitracin |
| Common Penicillinase-sensitive penicillins: | Penicillin G, V Ampicillin Amoxicillin |
| Which are some Penicillinase-resistant penicillins? | Oxacillin Nafcillin Dicloxacillin |
| Common Antipseudomonas? | Ticarcillin and Piperacillin |
| What is the most common Monobactam? | Aztreonam |
| What are common Carbapenems? | Imipenem, Meropenem, Ertapenem, and Doripenem |
| The 30S subunit ribosomes is attacked by: | Aminoglycosides, Glycylcycline, and Tetracyclines |
| What are the most common aminoglycosides? | Gentamicin Neomycin Amikacin Tobramycin Streptomycin |
| Three tetracyclines | Tetracycline, Minocycline, and Doxycycline |
| Which ribosomal subunit do Tetracyclines attack? | 30S |
| Which antibiotic categories act by inhibiting protein synthesis through inactivation of the 50S ribosomal subunit? | Chloramphenicol, Clindamycin, Linezolid, Macrolides, and Streptogramins |
| What are the MC streptogramins? | Quinupristin and Dalfopristin |
| Common macrolides? | Azithromycin, Clarithromycin, and Erythromycin |
| Common antibiotic that disrupts DNA integrity via free radicals? | Metronidazole |
| Rifampin works by: | Inhibition of mRNA synthesis by the use of an RNA polymerase |
| Which are the two types of Gyrase antibiotic categories? | Fluoroquinolones and Quinolones |
| Common Fluoroquinolones | Ciprofloxacin, Levofloxacin |
| Nalidixic acid is an _________________ | Quinolone |
| Daptomycin works by inhibiting the ______________ _____________. | Membrane integrity |
| The 50S ribosomal subunit is attacked by: | Chloramphenicol, Clindamycin, Linezolid, Macrolides, and Streptogramins |
| What medication prevents the formation of THF? | TMP |
| Which antibiotics are known to inhibit PABA? | Sulfonamides |
| DNA gyrase is inhibited by _____________________. | Fluoroquinolones |
| Which antibiotics work on the Cell Wall? | Penicillins and Glycopeptides (vancomycin andbacitrancin) |
| What forms is Penicillin G found? | IV and IM forms |
| Penicillin V is only found in the ____________ form. | Oral |
| Which penicillin, G or V, is administered orally only? | Penicillin V |
| What are the prototype B-lactam antibiotics? | Penicillin G, V |
| What is the mode of action of Penicillin G and Penicillin V? | Binds penicillin-binding proteins --> blocks transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes |
| What are the clinical uses for Penicillin G, V? | 1. Mostly gram (+) organisms (S. pneumoniae, S. pyogenes, Actinomyces) 2. Gram (-) cocci (mainly N. meningitidis) 3. Spirochetes (T. pallidum) |
| Penicillin G, V, is bactericidal or bacteriostatic? | Bactericidal |
| What are the adverse effects associated with Penicillin G, V? | 1. Hypersensitive reactions 2. Direct Coombs (+) hemolytic anemia 3. Drug-induced interstitial nephritis |
| Mode of resistance of Penicillin G, V? | B-lactamase cleaves the B-lactam ring. ---> MUTATIONS in PBP |
| Another name for Penicillin-binding proteins? | Transpeptidases |
| The MOA is same as Penicillin. Wider spectrum; penicillinase sensitive; combine with clavulanic acid to protect against destruction by B-lactamase. | Penicillinase-sensitive penicillins |
| Which hver wider spectrum of action, Penicillin G, V or Penicillinase-sensitive penicillins? | Penicillinase-sensitive penicillins |
| What are the clinical uses of Penicillinase-sensitive penicillins? | H. influenzae, H. pylori, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, and enterococci. |
| What mnemonic is used to remember the coverage of Penicillinase-sensitive penicillins? | HHELPSS |
| HHELPSS stands for: | H. influenzae H. pylori E. coli Listeria monocytogenes Proteus mirabilis Salmonella Shigella Enterococci |
| What are common adverse effects of Penicillinase - sensitive penicillins? | Hypersensitive reactions, rash, and Pseudomembranous colitis |
| Amoxicillin is an | Penicillinase-sensitive penicillin |
| What is the mode of acquired resistance of Amoxicillin and ampicillin? | Penicillinase (a type of B-lactamase) cleaves B-lactam ring. |
| Which type of penicillins are of narrow spectrum? | Penicillinase-resistant penicillins |
| What makes Penicillinase-resistant penicillins "resistant"? | The bulky R group blocks access of B-lactamase to B-lactam ring. |
| What is the use for Penicillinase-resistant penicillins? | S. aureus only |
| Why is MRSA not treated with Dicloxacillin? | It is resistant to Penicillinase-resistant penicillins due to altered PBP. |
| What are the main adverse effects of Nafcillin, Oxacillin, and Dicloxacillin? | Hypersensitivity reactions and Interstitial nephritis |
| What nephrotic disorder is seen as adverse effect of Penicillinase-resistant penicillins? | Interstitial nephritis |
| Which type of penicillins may have interstitial nephritis as an adverse effect? | Penicillin G, V and Penicillinase-resistant penicillins |
| Spectrum type of each: 1. Penicillinase-sensitive penicillins 2. Penicillinase-resistant penicillins 3. Antipseudomonal penicillins | 1. Broad 2. Narrow 3. Extended |
| Antipseudomonal are penicillinase __________________. | Sensitive |
| What is often added to anti pseudomonal to protect them from B-lactamase destruction? | B-lactamase inhibitors |
| What are the clinical uses (infections) treated with Antipseudomonal penicillins? | Pseudomonas spp. and gram (-) rods |
| What are the most (4) B-lactamase inhibitors? | Clavulanic acid, Avibactam, Sulbactam, and Tazobactam |
| What mnemonic is used to summarize the B-lactamase inhibitors? | CAST Clavulanic acid, Avibactam Sulbactam Tazobactam |
| What is the function of B-lactamase inhibitors? | Added to penicillin antibiotics to protect the antibiotic from destruction by B-lactamase |
| What is another name for B-lactamase? | Penicillinase |
| What is prevented by adding Clavulanic acid to Piperacillin? | Destruction of Piperacillin with B-lactamase |
| Cephalosporins are _________________. | Bactericidal |
| Mechanism of action of Cephalosporins | B-lactam drugs that inhibit cell wall synthesis but ar less susceptible to penicillinases. |
| Which are more susceptible to penicillinases, penicillins or cephalosporins? | Penicillins |
| Which organisms are NOT covered with generations 1st-4th Cephalosporins? | LAME Listeria Atypicals (Chlamydia, Mycoplasma) MRSA Enterococci |
| What mnemonic is used to remember the organisms not covered by generations 1-4 of cephalosporins? | LAME |
| What are the two main 1st generation cephalosporins? | Cefazolin and Cephalexin |
| Cefazolin is a _______ generation cephalosporin. | 1st |
| What cephalosporin is generation is Cephalexin? | 1st |
| Cefazolin and Cephalexin are both _______ generation cephalosporins? | 1st |
| What organisms are covered by 1st generation cephalosporins? | PEcK Proteus mirabilis E. coli Klebsiella pneumoniae |
| What is the common use for Cefazolin? | Used prior to surgery to prevent S. aureus wound infections |
| HENS PEcK | Mnemonic used for organisms covered by 2nd Gen cephalosporins |
| What are the most common 2nd Generation Cephalosporins? | Cefaclor, Cefoxitin, Cefuroxime, and Cefotetan |
| Cefaclor is ______ gen cephalosporin. | 2nd |
| Cefoxitin and Cefuroxime are both _____ generation cephalosporins. | 2nd |
| What generation of cephalosporins are Cefaclor, Cefoxitin, Cefuroxime, and Cefotetan? | 2nd |
| What mnemonic is used to summarize the organisms covered by 2nd generation cephalosporins? | HENS PEcK |
| What organisms are covered by 2nd Generation cephalosporins? | 1. Gram (+) cocci 2. H. influenzae 3. Enterobacter aerogenes 4. Neisseria spp 5. Serratia marcescens 6. Proteus mirabilis 7. E. coli 8 . Klebsiella pneumoniae |
| Which cephalosporins can cross the BBB? | 3rd generation cephalosporins |
| What are the 3rd generation cephalosporins? | Ceftriaxone, Cefotaxime, Cefpodoxime, and Ceftazidime |
| What is the main use for 3rd generation cephalosporins? | Serious gram (-) infections resistant to other B-lactams |
| What re the most common uses for Ceftriaxone? | Meningitis, gonorrhea, disseminated Lyme disease |
| Which cephalosporin is often used to treat disseminated Lyme disease? | Ceftriaxone |
| What generation of cephalosporin is Ceftriaxone? | 3rd generation |
| Which 3rd gen Cephalosporin is used to treat Pseudomonas? | Ceftazidime |
| Ceftazidime is a _____ generation cephalosporin | 3rd |
| What type or generation of cephalosporins are used in seriums gram (-) infections? | 3rd |
| Cefotaxime is a ______ generation cephalosporin | 3rd |
| What is the MC 4th generation cephalosporin? | Cefepime |
| What are the clinical uses of Cefepime? | Gram (-) organisms, with increased activity against Pseudomonas and gram (+) organisms |
| Besides gram negative activity, what other infections can be treated with 4th generation cephalosporins? | Pseudomonas and gram (+) organisms |
| What is the most commonly referred 5th generation Cephalosporin? | Ceftaroline |
| What is the coverage of 5th generation cephalosporins? | Broad gram (+) and gram (-) organism |
| Unlike generations 1st --- 4th, the ______ generation of cephalosporins cover: | 5th; Listeria, Atypicals (Chlamydia and Mycoplasma), MRSA, and Enterococci |
| MRSA is covered by ______ generation cephalosporins | 5th |
| What is covered by the 4th generation cephalosporins, but NOT by the 5th generation? | Pseudomonas |
| List of adverse effects seen with Cephalosporins: | 1. Hypersensitivity reactions 2. Autoimmune hemolytic anemia 3. Disulfiram-like reaction 4. Vitamin K deficiency 5. Low rate of cross-reactivity even in penicillin-allergic patients 6. Increase nephrotoxicity with aminoglycosides |
| What kind of anemia may be seen with Cephalosporin therapy? | Autoimmune hemolytic anemia |
| What common Vitamin deficiency is a possible adverse effect of prolonged use of Cephalosporins? | Vitamin K |
| A disulfiram-like reaction is seen with all generations of __________________. | Cephalosporins |
| What other type of antibiotics increase the risk of nephrotoxicity seen in Cephalosporin therapy? | Aminoglycosides |
| What kind of antibiotics should be avoided in patients on Cephalosporin? | Aminoglycosides |
| What is always coadministered with Imipenem? | Cilastatin |
| What is the MOA of Cilastatin? | Inhibition of renal dehidropeptidasa I |
| Inhibitor of renal dehydropeptidase I | Cilastatin |
| Which are the newer Carbapenems? | Ertapenem and Doripenem |
| What is the purpose of using Cilastatin with Imipenem? | Decrease inactivation of drugs in renal tubules |
| What are the main uses for Carbapenems? | 1. Gram (+) cocci 2. Gram (-) rods 3. Anaerobes |
| What is the safest carbapenem? | Meropenem |
| What enzyme is inactivated in renal tubules by the use of Carbapenems? | Dehydropeptidase I |
| What are the adverse effects of carbapenems? | GI distress, rash, and CNS toxicity (seizures) at high plasma levels |
| What is the most significant side effect seen with Carbapenems? | CNS toxicity ---> seizures |
| Aztreonam is an ________________________. | Monobactam |
| Monobactam are less susceptible to ___________________. | B-lactamases |
| How does Aztreonam prevent peptidoglycan cross-linking? | Binding to Penicillin-Binding protein 3 |
| What kind of antibiotics act by binding to PBP-3? | Monobactam |
| Monobactams are synergistically with ____________________. | Aminoglycosides |
| What is the use of Aztreonam? | Gram (-) rods only |
| Which patients are the ones usually treated with Monobactams? | Penicillin-allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides |
| Inhibits cell wall peptidoglycan formation by binding D-Ala-D-Ala portion of cell wall precursors. | Vancomycin |
| Vancomycin is not susceptible to ______________________. | B-lactamases |
| What bugs are treated with Vancomycin? | Gram (+) bugs |
| Examples of gram (+) bugs treated with Vancomycin? | Serious, multi resistant organisms, including MRSA, S. epidermidis, sensitive Enterococcus species, and C. difficile |
| Vancomycin is bactericidal except for: | C. difficile |
| What is the main syndrome due adverse reaction to Vancomycin? | Red man syndrome |
| What is the cause of Red man syndrome? | Adverse effect to Vancomycin |
| What is the Red man syndrome? | Diffuse flushing due to vancomycin toxicity |
| What are the most common adverse effects of Vancomycin? | Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing (red man syndrome), drug reaction with eosinophilia and systemic symptoms (DRESS syndrome) |
| DRESS syndrome and Red man syndrome are commonly associated with: | Vancomycin toxicity |
| What is the amino acid modification that causes Vancomycin resistance? | D-Ala-D-Ala ----> D-Ala-D-Lac |
| D-Ala-D-Lac | Amino acid change causing Vancomycin resistance |
| How is Red man syndrome prevented? | 1. Pretreatment with antihistamines 2. Slow rate of infusion of Vancomycin |
| What are the bacterial ribosomes targeted by protein inhibitors? | 30S and 50S |
| 30S +50S = | 70S bacterial ribosome |
| All protein inhibitors are _______________________, except for: | Bacteriostatic; Aminoglycosides (bactericidal) LInezolid (variable) |
| Which kind of protein inhibitors are the only bactericidal? | Aminoglycosides |
| Linezolid is bactericidal or bacteriostatic? | Variable (both) |
| Aminoglycosides and Tetracyclines target the _______ ribosomal subunit. | 30S |
| What are the main protein inhibitors that target bacterial 50S ribosomal subunit? | Chloramphenicol, Clindamycin, Erythromycin (macrolides) Linezolid |
| What protein inhibitors directly affect Translocation? | Macrolides and Clindamycin |
| What is the mechanism of action of Aminoglycosides? | 1. Irreversible inhibition of initiation complex through binding of the 30S subunit 2. Cause misreading of mRNA 3. Block translocation |
| Why are aminoglycosides ineffective against anaerobes? | They require Oxygen to work |
| What is the result of aminoglycosides inhibition of the initiation complex by binding to the 30S subunit? | Misreading of mRNA |
| What is the main use of aminoglycosides? | Severe gram (-) rod infections |
| What aminoglycoside is used for bowel surgery? | Neomycin |
| Aminoglycosides work synergistic with? | B-lactam antibiotics |
| What are the most common adverse effects of aminoglycosides? | Nephrotoxicity Neuromuscular blockade Ototoxicity Teratogen |
| Ototoxicity by Aminoglycosides is increased if used with: | Loop diuretics |
| What kind of antibiotic should be avoided in case a patient is on Furosemide? | Aminoglycosides |
| What is the mechanism of resistance presented by aminoglycosides? | Bacterial transferase enzymes inactivate the drug by acetylation, phosphorylation, or adenylation. |
| Which protein inhibitor drug class targets/inhibits the A-site tRNA binding? | Tetracyclines |
| Peptidyl transferase is inhibited by _____________________. | Chloramphenicol |
| Linezolid inhibition of 50S subunit prevents _____________ to integrate. | Initiator tRNA |
| Bind to 30S and prevent attachment of aminoacyl-tRNA. | Tetracyclines |
| Tetracyclines have limited ______ penetration. | CNS |
| How is Doxycycline eliminated from the body? | Fecally |
| Why is doxycycline used in renal failure patients? | It is fecally excreted |
| Which products, meds or preparations must be avoided when taking tetracyclines? | 1. Milk (Ca2+) 2. Antacids (Ca2+ and Mg2+) 3.. Iron-containing preparations |
| What kind of cations can inhibit tetracycline absorption in the gut? | Divalent (2+) |
| A person with severe GERD is taking OTC antacids, which protein inhibitor antibiotic should be avoided? | Tetracyclines |
| What are the clinical uses for Tetracyclines? | 1. Borrelia burgdorferi 2. M. pneumoniae 3. RIckettsia and Chlamydia 4. Acne 5. Doxycycline is effective against MRSA |
| Which tetracycline is used for MRSA infection? | Doxycycline |
| Why are tetracyclines especially against Rickettsia and Chlamydia? | Drug's' ability to accumulate intracellularly |
| What are common adverse effects of Tetracyclines? | 1. GI distress 2. Discoloration of teeth and inhibition of bone growth in children 3. Photosensitivity 4. Contraindicated in pregnancy |
| Discolored teeth due a medication. | Tetracycline toxicity |
| What is the mechanism of resistance? | Decrease uptake or increase effeflux out of bacterial cells by plasmid-encoded transport pumps |
| Tigecycline is a _____________________. | Glycylcyclines |
| What are a type of tetracycline derivatives? | Glycylcycline |
| What are the clinical uses of Glycylcyclines? | 1. Broad-spectrum anaerobic, gram (-), and gram (+) coverage 2. MRSA and VRE 3, Infection requireing deep tissue penetration |
| What is the mechanism of action of Chloramphenicol? | Blocks peptidyltransferase at 50S ribosomal subunit. Bacteriostatic |
| What are the MC uses of Chloramphenicol? | 1. Meningitis (H. influenzae, N. meningitidis, Strep pneumoniae) 2. Rickettsial diseases (Rocky Mountain spotted fever) |
| What are the adverse effects of Chloramphenicol? | 1. Anemia (dose dependent) 2. Aplastic anemia (dose independent) 3. Gray baby syndrome |
| Why do infants develop gray baby syndrome in Chloramphenicol? | They lack liver UDP-glucuronosyltransferase |
| What is the mode of resistance of Chloramphenicol? | Plasmid-encoded acetyltransferase inactivates the drug |
| MOA of Clindamycin: | Blocks peptide transfer (translocation) at 50S ribosomal subunit. Bacteriostatic |
| What are common uses of Clindamycin? | - Anaerobic infections in aspiration pneumonia, lung abscess, and oral infections. - Also effective against invasive group A streptococcal infetion |
| What are adverse effects associated with Clindamycin? | Pseudomembranous colitis (C. difficile overgrowth), fever and diarrhea. |
| Clindamycin treats infections _________________________ diaphragm. | Above |
| What is the most common Oxazolidinones? | Linezolid |
| What type of antibiotic is Linezolid? | Oxazolidinones |
| What is the mode of action of Linezolid? | Inhibit protein synthesis by binding to 50S subunit and preventing formation of the initiation complex. |
| What organisms are commonly treated with Linezolid? | Gram (+) species including MRSA and VRE |
| What are most important adverse effects of Linezolid? | 1. Bone marrow suppression (especially thrombocytopenia) 2. Peripheral neuropathy 3. Serotonin syndrome |
| What syndrome is adversely seen in the use of Linezolid? | Serotonin syndrome |
| How can Linezolid acquire resistance? | Point mutation of ribosomal RNA |
| What are the MC macrolides? | Azithromycin, clarithromycin, and erythromycin |
| What cell process is inhibited by Macrolides? | Translocation |
| What is the mechanism of action of Macrolides? | Inhibit protein synthesis by blocking translocation; bind to the 23S rRNA of the 50S ribosomal subunit |
| Where do macrolides bind to prevent protein synthesis? | 23S of the 50S ribosomal subunit |
| What are the MC clinical uses of Macrolides? | 1. Atypical pneumonias (Mycoplasma, Chlamydia, Legionella) 2. STIs (Chlamydia) 3. Gram (+) cocci (streptococcal infections in patients allergic to penicillin), 4. B. pertussis |
| What antibiotics can be used to treat atypical pneumonias? | Macrolides |
| Mnemonic of adverse effects seen in macrolides | MACRO |
| What are the most common adverse effects of Macrolides? | 1. Gastrointestinal Motility issues 2. Arrhythmia caused by prolonged QT interval 3. acute Cholestatic hepatitis 4. Rash 5. eOsinophilia |
| What macrolides inhibit cytochrome P-450? | Clarithromycin and Erythromycin |
| Methylation of 23S rRNA-binding site prevents binding of drug. | Mechanism of resistance of macrolides |
| What are the most common Polymyxins? | Colistin (polymyxin E), polymixin B |
| MOA of Polymyxins | Cation polypeptides that bind to phospholipids on cell membrane of gram (-) bacteria. |
| What is the clinical use for Polymyxins? | Salvage therapy for multidrug-resistant gram (-) bacteria (P. aeruginosa, E. coli, Klebsiella pneumoniae). |
| What is a common use for Polymyxin B? | Component of a triple antibiotic ointment used for superficial skin infections |
| What are the most significant adverse effects seen with Polymyxins? | Nephrotoxicity, Neurotoxicity (slurred speech, weakness, paresthesias), and respiratory failure. |
| What enzyme is primarily blocked or inhibited by Sulfonamides? | Dihydropteroate synthase |
| What is the end result of inhibition of dihydropteroate synthase by sulfonamides? | Inhibition of folate synthesis |
| When are sulfonamides bactericidal? | When combined with TMP |
| Sulfonamides are bacteriostatic or bactericidal, when used alone? | Bacteriostatic |
| What are the most significant clinical uses of Sulfonamides? | Gram (+), gram (-), Nocardia |
| TMP-SMX is used in treating? | Simple UTI |
| What is a problems seen in a G6PD deficiency patient on Sulfonamides? | Hemolysis |
| What are some adverse effects seen with Sulfonamides? | - Hypersensitivity reactions - Hemolysis (in G6PD deficiency) - Nephrotoxicity (Tubulointerstitial nephritis) - Photosensitivity -Stevens-Johnson syndrome - Kernicterus in infants - Displacement of other drugs form albumin |
| What is the teratogenic adverse effect of Sulfonamides? | Kernicterus |
| Which patients are at higher risk of hemolysis by using sulfonamides? | G6PD deficient |
| What is the way of resistance of Sulfonamides? | Altered enzyme (bacterial dihydropteroate synthase), decrease uptake, or increase PABA synthesis |
| What acid is prevented from forming by the use of Sulfonamide and/or Dapsone? | Dihydropteroic acid |
| What is the MC use for Dapsone? | 1. Leprosy, 2. Pneumocystis jirovecii prophylaxis |
| Two serious adverse effects of Dapsone therapy? | 1. Hemolysis of G6PD deficient 2. Methemoglobinemia |
| What does TMP stand for? | Trimethoprim |
| What is the mechanism of action of TMP? | Inhibits bacterial dihydrofolate reductase; Bacteriostatic |
| What antibiotic combination cause a sequential block of folate synthesis? | TMP-SMX |
| What infections are treated with TMP in combination with Sulfonamides? | UTIs, Shigella, Salmonella, Pneumocystis jirovecii pneumonia, and toxoplasmosis prophylaxis |
| What is a common treatment for Toxoplasmosis prophylaxis? | TMP-SMX |
| List of TMP adverse effects: | 1. Megaloblastic anemia 2. Leukopenia 3. Granulocytopenia |
| How can granulocytopenia seen with TMP can be avoided? | Coadministration of folinic acid |
| What is the common suffix seen fluoroquinolone nomenclature? | -floxacin |
| Mechanism of action of fluoroquinolones | Inhibit prokaryotic enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. |
| What should never be taken with fluoroquinolones? | Antacids |
| Antacids should be avoided when also taking: | Fluoroquinolones and Tetracyclines |
| Clinical uses of Fluoroquinolones: | 1. Gram (-) rods of urinary and GI tracts 2. Some gram (+) organisms 3. Otitis externa |
| Why pregnant women cannot take fluoroquinolones? | May cause cartilage damage |
| What populations are at risk of cartilage damage by Fluoroquinolone use? | Pregnant women, nursing mothers, and children < 18 years old. |
| What is a possible ECG adverse effect of fluoroquinolones? | QT prolongation |
| What is a risk of fluoroquinolone therapy in persons over 60 years old or those using prednisone? | May cause Tendonitis or tendon rupture |
| Which two organs or tissues are at risk of damage in Fluoroquinolone therapy? | Cartilage and tendos |
| What effect does ciprofloxacin have on the CYP450 system? | Inhibits |
| How do fluoroquinolones acquired resistance? | Chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps |
| What is the mode of action of Dapsone? | Lipopeptide that disrupts cell membranes of gram (+) cocci by creating transmembrane channels |
| What drug is known to destroy cell membrane by creating transmembrane channels? | Daptomycin |
| What are the most common uses for Daptomycin? | 1. S. aureus skin infections (especially MRSA) 2. Bacteriemia 3. Endocarditis 4. VRE |
| VRE and MRSA can be treated with ________________, by disrupting the cell membrane. | Daptomycin |
| Why is Daptomycin not used in pneumonias? | It tends to avidly bind to and is inactivated by surfactant |
| What medication is known to bind to surfactant and also by inactivated by surfactant as well? | Daptomycin |
| Adverse effects seen in Daptomycin? | Myopathy and rhabdomyolysis |
| What is the mechanism of action of Metronidazole? | Forms toxic free radicals metabolites in the bacterial cell that damage DNA |
| Metronidazole is ______________ and _______________. | Bactericidal and antiprotozoal |
| GET GAP | Mnemonic used to summarize organisms trated with Metronidazole |
| What does GET GAP stand for: | G- Giardia E- Entamoeba T- Trichomonas G- Gardnerella vaginalis A- Anaerobios (Bacteroides, C. diff) P. H. Pylori |
| What medication can substitute Amoxicillin in triple therapy for H. pylori infection? | Metronidazole |
| Metronidazole treat ANAEROBIC infections _________ the diaphragm. | Below |
| Clindamycin treats anaerobic infections ______________ the diaphragm. | Above |
| What adverse effect is seen with Metronidazole + ETOH? | Disulfiram-like reaction |
| What is disulfiram-like reaction presented? | Severe flushing, tachycardia, and hypotension |
| What are the lesser adverse effects of Metronidazole? | Headache and metallic taste |
| What DNA damaging antibiotic may provoke a disulfiram -like reaction if combined with alcohol? | Metronidazole. |
| What is used for prophylaxis is use for M. tuberculosis? | Isoniazid |
| What is the common treatment for M. tuberculosis? | Rifampin, Isoniazid, Pyrazinamide, and Ethambutol |
| RIPE | Mnemonic for M. tuberculosis treatment |
| What drugs are use for prophylaxis for M. avium-intracellulare? | Azithromycin, rifabutin |
| What is the empiric treatment for M. avium-intracellulare? | Azithromycin or clarithromycin + ethambutol. Can add rifabutin or ciprofloxacin |
| What is the long-term treatment of Tuberculoid M. leprae? | Dapsone and rifampin |
| What drug is added to leprae treatment in the Lepromatous form? | Clofazimine |
| What are the two most common Rifamycins? | Rifampin and Rifabutin |
| What is the mechanism of action of Rifamycin? | Inhibit DNA-dependent RNA polymerase |
| What are some clinical uses for Rifamycins? | 1. Mycobacterium tuberculosis 2. Delay resistance to dapsone when used for leprosy 3. Meningococcal meningitidis prophylaxis 4. Chemoprophylaxis in contacts of children with H. influenzae type b. |
| Why is are rifamycins used with Dapsone in treating Leprosy? | It helps delay the resistance to Dapsone |
| What drug causes orange body fluids? | Rifampin |
| Which rifamycin is favored in HIV? | Rifabutin |
| Why is rifabutin used in HIV patients and not Rifampin? | RIfabutin has less cytochrome P-450 stimulation |
| What are the adverse effects seen with Rifamycins? | 1. Minor hepatotoxicity 2. Induction of CYP450 system 3. Orange body fluids |
| What is the mode of resistance of Rifamycins? | Mutations reduce drug binding to RNA polymerase |
| What is a risk of rifampin monotherapy? | Rapid development of resistance to medication |
| What is the mode of action of Isoniazid? | Decreased synthesis of mycolic acids |
| Enzyme required to convert Isoniazid into active metabolite | Bacterial catalase-peroxidase |
| What is encoded by KatG? | Bacterial catalase-peroxidase |
| A deficiency or mutation to KatG gene can result in: | Defective function of INH due to inactivation |
| What is the main infection treated with Isoniazid? | M. tuberculosis |
| Which is the only agent (RIPE), that can be used in monotherapy prophylaxis of TB? | Isoniazid |
| Monotherapy for latent TB? | Isoniazid |
| What defines INH half-lives? | Fast vs Slow acetylators |
| Fast and slow acetylators. Association? | Represent possible Isoniazid half-lives |
| List of Isoniazid adverse effects: | 1. Hepatotoxicity 2. P-450 inhibition 3. Drug-induced SLE 4. Vitamin B6 deficiency --->Neuropathy and Sideroblastic anemia |
| What vitamin may be depleted by use of Isoniazid? | Vitamin B6 |
| What are clinical manifestations of Vitamin B6 deficiency due to INH toxicity? | Peripheral Neuropathy and Sideroblastic anemia |
| What anemia may be seen as side effect of INH toxicity? | Sideroblastic anemia |
| What is co administered with Isoniazid in order to prevent Vitamin B6 deficiency? | Pyridoxine |
| Mutations leading to underexpression of KatG | Mechanism of resistance of Isoniazid |
| What two cell types are most affected by Isoniazid? | Neurons and Hepatocytes |
| What does RIPE stand for? | Rifampin Isoniazid Pyrazinamide Ethambutol |
| What is the clinical use for Pyrazinamide? | M. tuberculosis |
| Which are the two associated adverse effects of Pyrazinamide? | Hyperuricemia and hepatotoxiciy |
| What is the best pH level for Pyrazinamide to function properly? | Acidic |
| What is the mechanism of action of Ethambutol? | Decreased carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase |
| What is the associated adverse effects of Ethambutol? | Optic neuropathy |
| Description of the Optic Neuropathy due to Ethambutol use? | Red-green color blindness |
| Which RIPE drug works by blocking arabinosyltransferase? | Ethambutol |
| Inhibition of mycolic acids in Mycobacterium tuberculosis is done with ___________________. | Isoniazid |
| Decrease the carbohydrate polymerization of mycobacterium cell wall. | Ethambutol |
| What is a second line drug for the treatment of M. tuberculosis? | Streptomycin |
| Which ribosome component is interfered by Streptomycin? | 30S |
| What are associated side effects of Streptomycin? | Tinnitus, vertigo, ataxia, and nephrotoxicity. |
| Agent used as prophylaxis in cases of high risk for endocarditis and undergoing surgical or dental procedures? | Amoxicillin |
| Prophylaxis in cases of exposure to gonorrhea? | Ceftriaxone |
| What agent is used in prophylaxis o recurrent UTIs? | TMP-SMX |
| Ceftriaxone, Ciprofloxacin, or rifampin, are used as prophylaxis in: | Cases of exposure to meningococcal infection |
| What is the prophylaxis for pregnant women (+) group B strep? | Intrapartum penicillin G or ampicillin |
| Erythromycin ointment on eyes. Prophylaxis? | Prevention of gonococcal conjunctivitis in newborn |
| Which cases is Cefazolin used as prophylaxis measure? | Prevention of postsurgical infection due to S. aureus |
| Benzathine penicillin G is used a prophylaxis of: | Syphilis |
| What can be used as prophylaxis measures for strep pharyngitis in child with prior rheumatic fever? | Benzathine penicillin G or oral penicillin V |
| What is the most most common infection in HIV patient with CD4+ count < 50, and what is the prophylaxis drug? | Mycobacterium avium complex (MAC); Azithromycin or clarithromycin |
| TMP-SMX is used as prophylaxis in HIV patients with which possible infections? | Pneumocystis pneumonia and toxoplasmosis |
| Medications for MRSA? | Vancomycin, daptomycin, linezolid, tigecycline, ceftaroline, and doxycycline |
| What medications can be used to treat VRE? | Linezolid and streptogramins |
| What is the most common medication used for Multi-drug resistant P. aeruginosa? | Polymyxins B and E (colistin) |
| What enzyme is inhibited by Terbinafine? | Squalene epoxidase |
| What enzyme is inhibited by Azoles? | 14-a-demethylase |
| Which antifungals interfere in Ergosterol synthesis? | Azoles |
| Antifungals that disrupt cell wall synthesis | Ehinocandins |
| What are some importnat echinocandins? | Anidulafungin, Caspofungin, and Micanfungin |
| What is the common ending in nomenclature azoles? | -azole |
| What antifungal disrupts nucleic acid synthesis? | Flucytosine |
| What are common Polyenes? | Amphotericin B and Nystatin |
| What kind of antifungals inhibited cell membrane integrity? | Polyenes |
| What is the MOA of Amphotericin B? | Binds ergosterol; forms membrane pores that allow leakage of electrolytes |
| What cell structure is unique to fungi? | Ergosterol |
| Forms membrane pores that allow leakage of electrolytes. MOA of? | Amphotericin B |
| What important antifungal is used in serious, systemic mycoses? | Amphotericin B |
| What are some organism treated with Amphotericin B? | Cryptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucor. |
| What electrolytes should be supplemented in a patient on Amphotericin B? | K+ and Mg2+ |
| Why is K+ and Mg2+ supplemented in a patient on Amphotericin B? | Due to altered renal tubule permeability |
| What are adverse effects of Amphotericin B? | Fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis |
| IV phlebitis is associated with: | Amphotericin B |
| What are the most important adverse effects of Amphotericin B? | Nephrotoxicity, arrhythmias, andmia and phleblitis. |
| Which antifungal is used topically and not as toxic as Amphotericin B, and with the same mechanism action of Amphotericin B? | Nystatin |
| What is the clinical use of Nystatin? | "Swish and swallow" for oral candidiasis (thrush); topical for diaper rash or vaginal candidiasis. |
| What is a common medication for diaper rash or vaginal candidiasis? | Nystatin |
| What are 3 common Azoles? | Ketoconazole, Itraconazole, fluconazole |
| Inibito fungal sterol (ergosterol) synthesis by inhibiting that CYP450 enzyme that converts lanosterol to ergosterol | Azole mechanism of action |
| Associated adverse effects of Azoles | 1. Testosterone synthesis inhibition 2. Liver dysfunction |
| Which azole is the most likely to cause Gynecomastia? | Ketoconazole |
| Which antifungals are used for local and less serious systemic mycoses? | Azoles |
| What is the MOA of Terbinafine? | Inhibits the fungal enzyme squalene epoxidase |
| What is the most common use for Terbinafine? | Dermatophytosis |
| What is the most common dermatophytose treated with Terbinafine? | Onychomycosis |
| What is Onychomycosis? | Fungal infection of finger or toe nails |
| What are some adverse effects associated with Terbinafine? | GI upset, headaches, hepatotoxicity, and taste disturbance. |
| What is the MOA of Echinocandins? | Inhibit cell wall synthesis by inhibiting synthesis of B-glucan |
| Decrease synthesis is B-glucan is achieved by which kind of antifungals? | Echinocandins |
| What are the most common uses for Echinocandins? | 1. Invasive aspergillosis 2. Candida |
| Why is there flushing in the use of Caspofungin? | Echinocandins release histamine --> flushing |
| What process of the cell cycle is disrupted by Griseofulvin? | Mitosis |
| What is the MOA of Griseofulvin? | Interferes with microtubule function; disrupts mitosis. |
| Where is Griseofulvin commonly deposited? | Keratin-containing tissues (nails) |
| What kind of infection is often treated with Griseofulvin? | Dermatophytes (tinea, ringworm) |
| What is the most significant adverse effect of Griseofulvin therapy? | Disulfiram-like reaction |
| What are the effects on CYP450 and Warfarin, by the use of Griseofulvin? | Increase the metabolism of both |
| Suramin and melarsoprol are used to treat: | Trypanosoma brucei |
| T. cruzi is treated with: | Nifurtimox |
| Nifurtimox is a antiprotozoal agent used to treat _____________. | T. cruzi infection |
| Pyrimethamine is used in treating ___________________. | Toxoplasmosis |
| What is a common treatment option for Leishmaniasis? | Sodium Stibogluconate |
| List of common anti-mite/louse drugs: | 1. Permethrin 2. Malathion 3. Oral Ivermectin |
| What is the use for Permethrin? | Scabies and lice infection |
| Mode of action of Permethrin? | Inhibits Na+ channel deactivation --> neuronal membrane depolarization |
| MOA of Malathion | Acetylcholinesterase inhibitor |
| What is the mode of action of Chloroquine? | Blocks detoxification of heme into hemozoin |
| The accumulation of heme due to Chloroquine, is toxic to which organism spp? | Plasmodia |
| What is a common drug used to treat plasmodial species other than P. falciparum? | Chloroquine |
| Why is Chloroquine not used in treating P. falciparum? | Frequency of resistance is too high |
| What are some common adverse effects seen with Chloroquine? | Retinopathy; pruritus |
| List of anti-helminthic therapy drugs | Pyrantel pamoate Ivermectin Mebendazole Praziquantel Diethylcarbamazine |
| Which is a antihelminthic medication that works as an microtubule inhibitor? | Mebendazole |
| What is the mode of action of Praziquantel? | Increased Ca2+ permeability and increased vacuolization |
| HIV Reverse transcriptase include: | NRTIs and NNRITs |
| Common NRTIs | Abacavir (ABC), Didanosine (ddI), Emtricitabine (FTC), Lamivudine (3TC), Stavudine (d4T), Tenofovir (TDF), Zidovudine (ZDV) |
| Commn NNRTIs include: | Delavirdine, Efavirenz, and Nevirapine |
| ABC | Abacavir |
| ddI | Didanosine |
| Emtricitabine | FTC |
| 3TC | Lamivudine |
| Lamivudine | 3TC |
| d4T | Stavudine |
| Stavudine | d4T |
| TDF | Tenofovir |
| Tenofovir is a common HIV ___________________. | NRTI |
| Tenofovir is abbreviated as _______. | TDF |
| Zidovudine | ZDV |
| Which to HIV antivirals prevent the entry of the virus? | Maraviroc and Enfuvirtide |
| What action does Maraviroc prevent that does not allow for entry of HIV to host cell? | Attachment |
| Maraviroc prevents ______________ of HIV to the cell. | Attachment |
| Penetration of HIV to host cell is prevented with ___________. | Enfuvirtide |
| What HIV antiviral prevents entry of HIV by blocking its penetration? | Enfurvitide |
| List of HIV integrase inhibitors | Dolutegravir Elvitegravir Raltegravir Bictegravir |
| What suffix is shared by all HIV integrase inhibitors? | -- tegravir |
| --tegravir | Integrase inhibitor |
| -tegravir is _______________ inhibitor, and --navir is _____________ inhibitor. | Integrase; Protease |
| Raltegravir is a very common ______________________. | HIV integrase inhibitor |
| What process in HIV replication/infection process is disrupted by Integrase inhibitors? | DNA integration |
| DNA integration occurs right after______________________ and before _____________. | Reverse transcription ; Transcription |
| What are 3 common protease inhibitors used in HIV therapy? | Indinavir, Saquinavir, and Lopinavir |
| -- navir | Protease inhibitor |
| What common suffix identifies all or most of HIV Protease inhibitors? | - navir |
| What process in HIV replication in the CD4+ cell is disrupted by Protease inhibitors? | Proteolytic processing |
| HIV proteolytic processing is inhibited with _____________ inhibitors. | Protease |
| Which are categories of antivirals (non-HIV), that disrupt Nucleic Acid synthesis? | 1. Guanosine analogs 2. Viral DNA polymerase inhibitors 3. Guanine nucleotide synthesis |
| Name two common Guanosine analogs (antivirals): | Acyclovir and Ganciclovir |
| Acyclovir is a _____________________________ | Guanosine analog |
| What action is disrupted by Acyclovir? | Nucleic acid synthesis |
| Cidofovir and Foscarnet both are ________________________. | Viral DNA polymerase inhibitors |
| What are common viral infections treated with Foscarnet and Cidofovir? | HSV and CMV |
| What type of nucleic acid synthesis inhibitor is Ribavirin? | Guanine nucleotide synthesis inhibitor |
| Which are the two most common Neuraminidase inhibitors? | Oseltamivir and Zanamivir |
| What are common antivirals used to treat Influenza A and B? | Oseltamivir and Zanamivir |
| Oseltamivir and Zanamivir are: | Neuraminidase inhibitors |
| What is prevented by the use of Neuraminidase inhibitors? | Release of progeny virus |
| Inhibit influenza neuraminidase | Mechanism of action of Oseltamivir and Zanamivir |
| What are the main uses for Acyclovir and other Guanosine analogs? | HSV and VZV |
| Which Guanosine analog has the best oral bioavailability? | Valacyclovir |
| What are the most significant adverse effects of Acyclovir and other Guanosine analogs? | 1. Obstructive crystalline nephropathy 2. Acute renal failure if not adequately hydrated |
| What is the mechanism of resistance? | Mutated viral thymidine kinase |
| What conditions are most commonly treated with acyclovir? | HSV-induced mucocutaneous and genital lesions as well as for encephalitis. |
| Prodrug of acyclovir? | Valacyclovir |
| Why is there few adverse effects with acyclovir and its derivatives? | It monophosphorylated HSV/VZV infected cells by thymidine kinase |
| What is the mechanism of action of Ganciclovir? | 5'- monophosphate formed by a CMV viral kinase |
| What is the most common use for Ganciclovir? | CMV, especially in immunocompromised patients |
| What is the prodrug of Ganciclovir? | Valganciclovir |
| Adverse effects of Ganciclovir | 1. Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia) 2. Renal toxicity |
| What is the MOA of Foscarnet? | Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor. |
| Where does the Foscarnet binds? | Pyrophosphate-binding site of enzyme |
| Which antiviral does not require any kinase activation | Foscarnet |
| Pyrophosphate analog | Foscarnet |
| 1. Viral DNA/RNA polymerase inhibitor 2. HIV reverse transcriptase inhibitor | Mechanisms of action of Foscarnet |
| What are the two most common uses for Foscarnet? | 1. CMV retinitis in immunocompromised patients when Ganciclovir fails 2. Acyclovir-resistant HSV |
| List of adverse effects Foscarnet: | 1. Nephrotoxicity 2. Electrolyte abnormalities ----> seizures |
| What are the common electrolyte abnormalities of Foscarnet? | Hypo-or-Hypercalcemia, hypo/hyperphosphatemia, hypokalemia, and hypomagnesemia |
| What is severe consequence seen in Foscarnet-induced electrolyte abnormalities? | Seizures |
| What is the mode of resistance of Foscarnet? | Mutated DNA polymerase |
| Mechanism of action of Cidofovir? | Inhibits viral DNA polymerase |
| What is the main adverse effect seen with Cidofovir? | Nephrotoxicity |
| What does HAART stand for? | Highly active antiretroviral therapy |
| What are the strongest indications for HAART? | 1. AIDS-defining illness 2. Low CD4+ cell counts (<500 cells/mm), 3. High viral load |
| What is the regimen that composes HAART? | A total of 3 drugs; 2 NRTIs + 1 Integrase inhibitor |
| What is the mechanism of action of NRTIs? | Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain |
| All NRTIs are nucleosides, except for ___________________. | Tenofovir (nucleoTide) |
| What are some unique ZDV clinical uses? | 1. General prophylaxis 2. During pregnancy to decrease risk of fetal transmission |
| What are the associated adverse effects of NRTIs? | 1. Bone marrow suppression 2. Peripheral neuropathy 3. Lactic acidosis 4. Anemia 5. Pancreatitis |
| What NRTI is contraindicated in a patient with HLA-B*5701 mutation? | Abacavir |
| How is bone marrow suppression due to NRTI toxicity reversed? | Co-administer granulocyte colony-stimulating factor [G-CSF] and erythropoietin |
| What is an associated adverse effect of ZDV? | Anemia |
| What is the associated adverse effect of Didanosine? | Pancreatitis |
| What adverse effect is seen with all nucleoside NRTIs? | Lactic acidosis |
| Efavirenz is a _____________. | NNRTI |
| Nevirapine and Delavirdine are both, _____________. | NNRTIs |
| What is the mechanism of action of NNRTIs? | Bind to reverse transcriptase at site different from NRTIs. |
| What are some differences of in mechanism of action between NRTIs and NNRTIs? | 1. Bind different site in the reverse transcriptase 2. NNRTIs do NOT require phosphorylation |
| What are all the common to all NNRTIs adverse effects? | Rash and hepatotoxicity |
| What are adverse effects seen with Efavirenz? | Vivid dreams and CNS symptoms |
| Which NNRTIs are contraindicated in pregnancy? | Delavirdine and Efavirenz |
| What is the mechanism of action of Protease inhibitors? | Assembly of virions depends on HIV-1 protease, which cleaves the polypeptide products of HIV mRNA into their functional parts. |
| Which HIV antivirals prevent the maturation of new viruses? | Protease inhibitors |
| Which Protease inhibitor "boost" other drug concentrations by inhibiting CYP450 system? | Ritonavir |
| Which rifamycin is can be use with Protease inhibitors? | Rifabutin |
| What are shared adverse effects of Protease inhibitors? | Hyperglycemia, GI intolerance, lipodystrophy (Cushing-like syndrome) |
| What are associated side effects of Indinavir? | Nephropathy, hematuria, thrombocytopenia |
| What is the result of Protease inhibitors and Rifampin? | Reducts protease inhibitors concentrations, since Rifampin is potent CYP/UGT inducer. |
| Integrase inhibitor mechanism of action | Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase |
| Adverse effect of Integrase inhibitors | Increased creatine kinase |
| What HIV antiviral is associated with increased levels creatine kinase? | Integrase inhibitors |
| What is the mechanism of action Enfuvirtide? | Binds gp41, inhibiting viral entry. |
| Binds CCR-5 on surface of T cells/monocytes, inhibiting interaction with gp120. | Mechanism of action Maraviroc |
| What is the associated adverse effect of Enfuvirtide? | Skin reaction at injection sites |
| _____________ inhibits fusion. | Enfuvirtide |
| _____________ inhibits docking. | Maraviroc |
| What is the mechanism of action interferons? | Glycoproteins normally synthesized by virus-infected cells, exhibiting a wide range of antiviral and antitumoral properties. |
| Adverse effects associated Interferons? | Flu-like symptoms, depression, neutropenia, and myopathy. |
| List of clinical uses for interferon therapy. | 1. Chronic HBV and HCV 2. Kaposi sarcoma 3. Hairy cell leukemia 4. Condyloma acuminatum 5. RCC 6. Malignant melanoma 7. Multiple sclerosis 8. Chronic granulomatous disease |
| What drug is used with Hepatitis C virus and RSV? | Ribavirin |
| What drugs are commonly used HCV infection? | Ledipasvir, Ribavirin, Simeprevir, and Sofosbuvir. |
| What is MOA of Ledipasvir? | Viral phosphoprotein (NS5A) inhibitor |
| Ribavirin mechanism of action | Inhibitors synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase |
| What are adverse effects of Ribavirin? | Hemolytic anemia and severe teratogen |
| What is the mechanism of action Simeprevir? | HCV protease (NS3/4A); prevents viral replication |
| Adverse effects of Simeprevir? | Photosensitivity reactions |
| Which HCV antiviral works by inhibiting HCV RNA-dependent RNA polymerase (NS5B) acting as a chain terminator? | Sofosbuvir |
| What is the teratogenic effect of Sulfonamides? | Kernicterus |
| Teratogenic effect of Aminoglycosides? | Ototoxicity |
| Cartilage damage is teratogenic effect of: | Fluoroquinolones |
| Associated teratogenic effect of Tetracyclines | Discolored teeth, inhibition of bone growth |
| Gray baby syndrome is the teratogenic result of ______________ in pregnant women. | Chloramphenicol |
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rakomi
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