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Antimicrobials Flashcards

1
Q

penicillin G, V

A

penicillin G (IV and IM form), penicillin V (oral); prototype B-lactam antibiotics

MOA: D-Ala-D-Ala structural analog => binds penicillin-binding proteins (PBPs, transpeptidases) => block transpeptidase cross-linking of peptidoglycan in cell wall => activate autolytic enzymes (bactericidal)

use: gram positive organisms (S. pneumoniae, S. pyogenes, Actinomyces), gram negative cocci (N. meningitidis), and spirochetes (T. pallidum)

AE: hypersensitivity reactions, direct Coombs positive hemolytic anemia, drug-induced interstitial nephritis

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2
Q

amoxicillin, ampicillin, aminopenicillins

A

penicillinase-sensitive penicillins

MOA: same as penicillin (D-Ala-D-Ala analog => prevents cross-linking of peptidoglycan in cell wall); can combine with clavulanic acid to protect against destruction by B-lactamase

use: H. influenzae, H. pylori, E. coli, Enterococci, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella (“HHEELPSS kill enterococci”)

AE: hypersensitivity reactions, rash, pseudomembranous colitis

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3
Q

dicloxacillin, nafcillin, oxacillin

A

penicillinase-resistant penicillins

MOA: same as penicillin (D-Ala-D-Ala analog => prevents cross-linking of peptidoglycan in cell wall); bulky R group blocks access of B-lactamase to B-lactam ring

use: S. aureus (except MRSA)

AE: hypersensitivity reactions, interstitial nephritis

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4
Q

piperacillin

A

antipseudomonal penicillin

MOA: same as penicillin (D-Ala-D-Ala analog => prevents cross-linking of peptidoglycan in cell wall); penicillinase sensitive (use with B-lactamase inhibitors)

use: Pseudomonas species and gram negative rods

AE: hypersensitivity reactions

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5
Q

cefazolin, cephalexin

A

first generation cephalosporins

MOA: B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal

use: gram positive cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae; cefazolin used prior to surgery to prevent S. aureus wound infections (“positive PEcK”)

AE: hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency

DDI: increase nephrotoxicity of aminoglycosides

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6
Q

cefaclor, cefoxitin, cefuroxime, cefotetan

A

second generation cephalosporins (“2nd graders wear fake fox fur to tea parties”)

MOA: B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal

use: gram positive cocci, H. influenzae, Enterobacter aerogenes, Neisseria species, Serratia marcescens, Proteus mirabilis, E. coli, Klebsiella pneumoniae (“positive HENS PEcK”)

AE: hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency

DDI: increase nephrotoxicity of aminoglycosides

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7
Q

ceftriaxone, cefotaxime, cefpodoxime, ceftazidime, cefixime

A

third generation cephalosporins

MOA: B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal; can cross BBB

use: serious gram negative infections resistant to other B-lactams; ceftriaxone = meningitis, gonorrhea, disseminated Lyme disease; ceftazidime = Pseudomonas

AE: hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency

DDI: increase nephrotoxicity of aminoglycosides

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8
Q

cefepime

A

fourth generation cephalosporin (“four vowels”)

MOA: B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal

use: gram negative organisms, increased activity against Pseudomonas and gram positive orgamisms

AE: hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency

DDI: increase nephrotoxicity of aminoglycosides

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9
Q

ceftaroline

A

fifth generation cephalosporin

MOA: B-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases; bactericidal

use: broad gram positive and gram negative organism coverage; UNLIKE 1st-4th generation, 5th generation covers MRSA and Enterococcus faecalis but DOES NOT cover Pseudomonas

AE: hypersensitivity reactions, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency

DDI: increase nephrotoxicity of aminoglycosides

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10
Q

clavulanic acid, avibactam, sulbactam, tazobactam

A

B-lactamase inhibitors

MOA: added to penicillin antibiotics to protect the antibiotic from destruction by B-lactamase

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11
Q

doripenem, imipenem, meropenem, ertapenem

A

carbapenems (“Pens cost a DIME”)

MOA: B-lactamase-resistant; binds PBPs => inhibition of cell wall synthesis => cell death; always administered with cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules

use: gram positive cocci, gram negative rods, anaerobes; use limited to life-threatening infections or when other drugs have failed

AE: GI distress, rash, CNS toxicity (seizures)

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12
Q

aztreonam

A

monobactam antibiotic

MOA: less susceptible to B-lactamases; prevents peptidoglycan cross-linking by binding to PBP3; synergistic with aminoglycosides; no cross-allergenicity with penicillins

use: gram negative rods ONLY; for penicillin-allergic patients and those with renal insufficiency who cannot tolerate aminoglycosides

AE: usually nontoxic; occasional GI upset

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13
Q

vancomycin

A

glycopeptide antibiotic

MOA: inhibits cell wall peptidoglycan formation by binding D-Ala-D-Ala portion of cell wall precursors; bactericidal against most bacteria (bacteriostatic against C. difficile); not susceptible to B-lactamases

use: gram positive bugs ONLY; for serious, multidrug resistant organisms (MRSA, S. epidermidis, sensitive Enterococcus species, and C. difficile)

AE: nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing (vancomycin infusion reaction), DRESS syndrome

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14
Q

gentamicin, neomycin, amikacin, tobramycin, streptomycin

A

aminoglycosides (“mean GNATS cannot kill anaerobes”)

MOA: bind 30S subunit => irreversible inhibition of initiation complex; can cause misreading of mRNA and block translocation; require O2 for uptake - do NOT work against anaerobes

use: severe gram negative rod infections; synergistic with B-lactam antibiotics; neomycin for bowel surgery

AE: nephrotoxicity, neuromuscular blockade, ototoxicity, teratogenicity

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15
Q

tetracycline, doxycycline, minocycline

A

tetracyclines

MOA: bacterioSTATIC; bind to 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetration

use: Borrelia burgdorferi, M. pneumoniae; Rickettsia, Chlamydia; community-acquired MRSA (doxycycline); doxycycline used for patients with renal failure (fecally eliminated)

AE: GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity, teratogenic; do not take tetracyclines with milk, antacids, or iron-containing preparations because divalent cations inhibit drugs’ absorption in the gut

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16
Q

tigecycline

A

tetracycline derivative

MOA: binds to 30S, inhibiting protein synthesis; also bacterioSTATIC

use: broad-spectrum anaerobic, gram negative and gram positive coverage; multidrug-resistant organisms (MRSA, VRE)

AE: nausea, vomiting

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17
Q

chloramphenicol

A

MOA: blocks peptidyltransferase at 50S ribosomal unit; bacterioSTATIC

use: meningitis (H. influenzae, N. meningitidis, S. pneumoniae) and rickettsial diseases (Rocky Mountain spotted fever); limited use due to toxicity

AE: anemia (dose-dependent), aplastic anemia (dose-independent), gray baby syndrome (premature infants lack liver UDP-glucuronosyltransferase)

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18
Q

clindamycin

A

lincomycin antibiotic

MOA: blocks peptide transfer (translocation) at 50S ribosomal subunit; bacterioSTATIC

use: anaerobic infections (Bacteroides species, C. perfringens) in aspiration pneumonia, lung abscesses, and oral infections; treats anaerobic infections ABOVE the diaphragm

AE: pseudomembranous colitis, fever, diarrhea

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19
Q

linezolid

A

oxazolidinone antibiotic

MOA: inhibits protein synthesis by binding to 50S subunit and preventing formation of initiation complex

use: gram positive species including MRS and VRE

AE: myelosuppression (especially thrombocytopenia), peripheral neuropathy, serotonin syndrome (partial MAO inhibition)

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20
Q

azithromycin, clarithromycin, erythromycin

A

macrolides

MOA: inhibit protein synthesis by blocking translocation; bind to 23S rRNA of 50S ribosomal subunit; bacterioSTATIC

use: atypical pneumonias (Mycoplasma, Chlamydia, Legionella), STIs (Chlamydia), gram positive cocci (streptococcal infections in patients allergic to penicillin), B. pertussis

AE: gastrointestinal Motility issues, Arrhythmia caused by prolonged QT interval, acute cholestatic hepatitis, Rash, eOsinophilia (“MACRO”)

DDI: increases serum concentration of theophylline and oral anticoagulants

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21
Q

colistin (polymyxin E), polymyxin B

A

polymyxins

MOA: cation polypeptides that bind to phospholipids on cell membrane of gram negative bacteria; disrupt cell membrane integrity => leakage of cellular components => cell death

use: salvage therapy for multidrug-resistant gram negative bacteria (P. aeruginosa, E. coli, K. pneumoniae); polymyxin B is used in triple antibiotic ointments

AE: nephrotoxicity, neurotoxicity (slurred speech, weakness, paresthesias, respiratory failure

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22
Q

sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine

A

sulfonamides

MOA: inhibit dihydropteroate synthase => inhibits folate synthesis; bacterioSTATIC (bactericidal when combined with trimethoprim)

use: gram positive and negative, Nocardia; TMP-SMX for simple UTI

AE: hypersensitivity reaction, hemolysis of G6PD deficiency, nephrotoxicity (tubulointerstitial nephritis), photosensitivity, Stevens-Johnson syndrome, kernicterus in infants, displaces other drugs from albumin (e.g., warfarin)

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23
Q

dapsone

A

sulfone antibiotic

MOA: similar to sulfonamides (inhibit folate synthesis), but structurally distinct

use: leprosy (lepromatous and tuberculoid), Pneumocystis jirovecii prophylaxis or treatment (when combined with TMP)

AE: hemolysis in G6PD deficiency, methemoglobinemia, agranulocytosis

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24
Q

trimethoprim

A

MOA: inhibits bacterial dihydrofolate reductase; bacterioSTATIC (bactericidal when combined with SMX - sequential block of folate synthesis)

use: UTIs, Shigella, Salmonella, Pneumocystis jirovecii pneumonia treatment and prophylaxis, toxoplasmosis prophylaxis

AE: hyperkalemia (high doses), megaloblastic anemia, leukopenia, granulocytopenia (avoided with coadministration of leucovorin)

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25
ciprofloxacin, enoxacin, norfloxacin, ofloxacin; gemifloxacin, levofloxacin, moxifloxacin
fluoroquinolones MOA: inhibit prokaryotic enzymes topoisomerase II (DNA gyrase) and topoisomerase IV; bactericidal use: gram negative rods of urinary and GI tracts (including Pseudomonas), some gram positive organisms, otitis externa AE: GI upset, superinfections, skin rashes, headache, dizziness, leg cramps and myalgia; must not be taken with antacids; may cause tendonitis or rupture, possible damage to cartilage - contraindicated in pregnancy and children <18; may prolong QT interval
26
daptomycin
MOA: lipoprotein that disrupts cell membranes of gram positive cocci by creating transmembrane channels use: S. aureus skin infections (especially MRSA), bacteremia, infective endocarditis, VRE; NOT used for pneumonia (avidly binds and is inactivated by surfactant) AE: myopathy, rhabdomyolysis
27
metronidazole
MOA: forms toxic free radical metabolites in the bacterial cell that damage DNA; bactericidal, antiprotozoal use: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (Bacteroides, C. difficile); can be used in place of amoxicillin in H. pylori "triple therapy" if penicillin allergy ("GET GAP on the Metro") AE: disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol, headache, metallic taste
28
treatment and prophylaxis: M. tuberculosis
prophylaxis: rifamycin-based regimen for 3-4 months treatment: Rifampin, Isoniazid, Pyrazinamide, Ethambutol ("RIPE for treatment")
29
treatment and prophylaxis: M. avium-intracellulare
prophylaxis: azithromycin, rifabutin treatment: azithromycin or clarithromycin + ethambutol; can add rifabutin or ciprofoxacin
30
treatment and prophylaxis: M. leprae
no prophylaxis treatment: long-term treatment with dapsone and rifampin for tuberculoid form; add clofazimine for lepromatous form
31
rifampin, rifabutin, rifapentine
rifamycins MOA: inhibit DNA-dependent RNA polymerase use: Mycobacterium tuberculosis; delays resistance to dapsone when used for leprosy; meningococcal prophylaxis and chemoprophylaxis in contacts of children with H. influenzae type b AE: minor hepatotoxicity and drug interactions; orange body fluids "4 Rs of Rifampin = RNA polymerase inhibitor, Ramps up microsomal CYP450, Red/orange body fluids, Rapid resistance if used alone" note: rifabutin does NOT ramp up CYP450
32
isoniazid
MOA: decreased synthesis of mycolic acids; bacterial catalase-peroxidase (encoded by KatG) needed to convert INH to active metabolite use: M. tuberculosis; also as a monotherapy for latent TB AE: hepatotoxicity, cytochrome P450 inhibition, drug-induced SLE, anion gap metabolic acidosis, vitamin B6 deficiency (peripheral neuropathy, sideroblastic anemia), seizures
33
pyrazinamide
MOA: uncertain; works best at acidic pH (e.g., in host phagolysosomes) use: M. tuberculosis AE: hyperuricemia, hepatotoxicity
34
ethambutol
MOA: decreased carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase use: M. tuberculosis AE: optic neuropathy (red-green colorblindness, usually reversible)
35
streptomycin (for TB)
MOA: interferes with 30S component of ribosome use: M. tuberculosis (second line) AE: tinnitus, vertigo, ataxia, nephrotoxicity
36
prophylaxis treatment for: exposure to meningococcal infection
ceftriaxone, ciprofloxacin, or rifampin
37
prophylaxis treatment for: high risk for infective endocarditis and undergoing surgical or dental procedures
amoxicillin
38
prophylaxis treatment for: history of recurrent UTIs
TMP-SMX
39
prophylaxis treatment for: malaria prophylaxis for travelers
atovaquone-proguanil, mefloquine, doxycycline, primaquine, or chloroquine
40
prophylaxis treatment for: pregnant patients carrying group B strep
intrapartum penicillin G or ampicillin
41
prophylaxis treatment for: prevention of gonococcal conjunctivitis in newborn
erythromycin ointment on eyes
42
prophylaxis treatment for: prevention of postsurgical infection due to S. aureus
cefazolin; vancomycin if positive for MRSA
43
prophylaxis treatment for: prophylaxis of strep pharyngitis in child with prior rheumatic fever
benzathine penicillin G or oral penicillin V
44
[?] is used as prophylaxis against Pneumocystis pneumonia and toxoplasmosis in patients with HIV
TMP-SMX
45
amphotericin B
antifungal MOA: binds ergosterol; forms membrane pores that allow leakage of electrolytes use: serious, systemic mycoses; Cryptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucor AE: fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis supplement K+ and Mg+ because of altered renal tubule permeability; hydration decreases nephrotoxicity
46
nystatin
antifungal MOA: same as amphotericin B (binds ergosterol and forms membrane pores) use: "swish and swallow" for oral candidiasis (thrush), topical for diaper rash or vaginal candidiasis
47
flucytosine
antifungal MOA: inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase use: systemic fungal infections (especially meningitis caused by Cryptococcus) in combination with amphotericin B AE: myelosuppression
48
clotrimazole, fluconazole, isavuconazole, itraconazole, ketoconazole, miconazole, voriconazole
azoles MOA: inhibit fungal sterol synthesis by inhibiting cytochrome P450 enzyme that converts lanosterol to ergosterol use: local and less serious systemic mycoses -fluconazole: chronic suppression of cryptococcal meningitis in people living with HIV and candidal infections of all types -itraconazole: Blastomyces, Coccidioides, Histoplasma, Sporothrix schenckii -clotrimazole, miconazole: topical fungal infections -voriconazole: Aspergillus and some Candida -isavuconazole: serious Aspergillus and Mucor infections AE: testosterone synthesis inhibition (gynecomastia, especially ketoconazole), liver dysfunction (inhibits cytochrome P450), QT interval prolongation
49
terbinafine
MOA: inhibits fungal enzyme squalene epoxidase use: dermatophytosis (especially onychomycosis - fungal infections of finger or toe nails) AE: GI upset, hepatotoxicity, taste disturbance
50
anidulafungin, caspofungin, micafungin
echinocandins MOA: inhibit cell wall synthesis by inhibiting synthesis of B-glucan use: invasive aspergillosis, Candida AE: GI upset, flushing (by histamine release)
51
griseofulvin
MOA: interferes with microtubule function, disrupts mitosis; deposits in keratin-containing tissues use: oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm) AE: teratogenic, carcinogenic, confusion, headaches, disulfiram-like reaction, increased P450 and warfarin metabolism
52
antiprotozoal therapy: -toxoplasmosis = ? -T. brucei = ? -T. cruzi = ? -leishmaniasis = ?
toxoplasmosis = pyrimethamine T. brucei = suramin and melarsoprol T. cruzi = nifurtimox leishmaniasis = sodium stibogluconate
53
permethrin, malathion, ivermectin
used to treat scabies and lice
54
chloroquine
MOA: blocks detoxification of heme into hemozoin; heme accumulates and is toxic to plasmodia use: plasmodial species other than P. falciparum (resistance due to membrane pump that decreases intracellular concentration of drug) AE: retinopathy (cumulative dose-dependent), pruritis
55
P. falciparum infections treated with [?]
artemether/lumefantrine or atovaquone/proguanil
56
antihelminthic therapy
pyrantel pamoate, ivermectin, mebendazole, praziquantel, diethylcarbamazine
57
oseltamivir, zanamivir
antiviral MOA: inhibit influenza neuraminidase => decrease release of progeny virus use: influenza A and B
58
baloxavir
antiviral MOA: inhibits "cap snatching" (transfer of 5' cap from cell RNA onto viral RNA) endonuclease activity of influenza virus RNA polymerase => decreased viral replication use: influenza
59
remdesivir
antiviral MOA: prodrug of an ATP analog; active metabolite inhibits viral RNA-dependent RNA polymerase and evades proofreading by viral exoribonuclease (ExoN) => decreased viral RNA production use: COVID-19
60
acyclovir, famciclovir, valacyclovir
antivirals MOA: guanosine analogs; monophosphorylated by HSV/VZV thymidine kinase => preferentially inhibit viral DNA polymerase by chain termination use: HSV-induced mucocutaneous and genital lesions and encephalitis; prophylaxis for immunocompromised patients or those with recurrent infection NO effect on CMV because CMV lacks thymidine kinase necessary to activate guanosine analogs; no effect on latent forms of HSV, VZV AE: obstructive crystalline nephropathy and acute kidney injury if not properly hydrated
61
ganciclovir
antiviral MOA: guanosine analog; 5'-monophosphate formed by CMV viral kinase => preferentially inhibits viral DNA polymerase use: CMV, especially in immunocompromised AE: myelosuppression, renal toxicity
62
foscarnet
antiviral MOA: viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor; binds to pyrophosphate-binding site of enzyme, does not require kinase activation use: CMV retinitis in immunocompromised (if ganciclovir fails), acyclovir-resistant HSV AE: nephrotoxicity, multiple electrolyte abnormalities that can lead to seizures
63
cidofovir
antiviral MOA: preferentially inhibits viral DNA polymerase; does not require phosphorylation by viral kinase use: CMV retinitis in immunocompromised (if ganciclovir fails), acyclovir-resistant HSV AE: nephrotoxicity (co-administer with probenecid and IV saline to decrease toxicity)
64
abacavir, emtricitabine, lamivudine, tenofovir, zidovudine
nucleotide reverse transcriptase inhibitors (NRTIs) MOA: competitively inhibit nucleotide binding to reverse transcriptase and terminate DNA chain; tenofovir is a nucleotide, the others are nucleosides use: HIV therapy (2 NRTIs and 1 integrase inhibitor); zidovudine can be used for general prophylaxis and during pregnancy to reduce the risk of transmission AE: myelosuppression (reversed with G-CSF), nephrotoxicity abacavir contraindicated in patients with HLA-B*5701 mutation (increased risk of hypersensitivity)
65
[?] is contraindicated in patients with HLA-B*5701 mutation
abacavir - increased risk of hypersensitivity
66
efavirenz, nevirapine
non-nucleotide reverse transcriptase inhibitors (NNRTIs) MOA: bind to reverse transcriptase at site different from NRTIs; do not require phosphorylation to be active or compete with nucleotides use: HIV AE: rash and hepatotoxicity; vivid dreams and CNS symptoms (efavirenz)
67
bictegravir, dolutegravir, elvitegravir, raltegravir
integrase inhibitors MOA: inhibit HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase use: HIV therapy (2 NRTIs and 1 integrase inhibitor) AE: increased creatine kinase, weight gain
68
atazanavir, darunavir, lopinavir, ritonavir
protease inhibitors MOA: inhibits HIV protease - assembly of virions depends on HIV-1 protease (pol gene), which cleaves the polypeptide products of HIV mRNA into their functional parts AE: hyperglycemia, GI intolerance DDI: rifampin decreases protease inhibitor concentrations (use ribabutin instead); ritonavir (CYP450 inhibitor) increases other drug concentrations
69
enfuvirtide, maraviroc
entry inhibitors MOA: -enfuvirtide: binds gp41, inhibiting entry/fusion -maraviroc: binds CCR-5 on T cells/monocytes, inhibits interaction with gp120 (inhibits attachment) AE: skin reaction at injection site
70
ledipasvir, ombitasvir, velpatasvir
NS5A inhibitors MOA: inhibits NS5A (viral phosphoprotein involved in RNA replication) use: hepatitis C AE: headache, diarrhea
71
sofosbuvir, dasabuvir
NS5B inhibitors MOA: inhibits NS5B (RNA-dependent RNA polymerase), acting as chain terminator; prevents viral RNA replication use: hepatitis C AE: fatigue, headache
72
grazoprevir, simeprevir
NS3/4A inhibits MOA: inhibit NS3/4A (viral protease), preventing viral replication use: hepatitis C AE: headache, fatigue (grazoprevir); photosensitivity reactions, rash (simepravir)
73
ribavirin
MOA: inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase use: adjunct in hepatitis C cases refractory to newer medications AE: hemolytic anemia, severe teratogen
74
antimicrobials to avoid in pregnancy
"SAFe Children Take Really Good Care" sulfonamides (kernicterus), aminoglycosides (ototoxicity), fluroquinolones (cartilage damage), clarithromycin (embryotoxic), tetracyclines (discolored teeth, inhibition of bone growth), ribavirin (teratogenic), griseofulvin (teratogenic), chloramphenicol (gray baby syndrome)

Step 1 - Quick Decks (18 decks)

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