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FA complete review part 6 Antimicrobials (antibiotics, antivirals, antifungals)

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
Created by: rakomi
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