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Pharmacology > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

amoxicillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, broad spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection, can cause drug induced liver damage
  • Beta-lactamase sensitive
  • Organisms: gram (+) cocci, E.coli, H.influenzae, L.monocytogenes, B.burgdorferi, H.pylori
  • use: URT, pharyngitis, fever w/ neutropenia
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2
Q

amoxicillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, broad spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: gram (+) cocci, E.coli, H.influenzae, L.monocytogenes, B.burgdorferi, H.pylori
  • Use: uncomplicated skin & soft tissue, neonatal meningitis
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3
Q

azlocillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, extended spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: gram (-) rods, antipseudomonal
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4
Q

ticarcillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, extended spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: gram (-) rods, antipseudomonal
  • use: complicated skin & soft tissue, bone/joint, intra-abdominal
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5
Q

piperacillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, extended spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: gram (-) rods, antipseudomonal
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6
Q

methicillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, very-narrow spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase resistant
  • Organisms: staphylococci (not MRSA)
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7
Q

nafcillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, very-narrow spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase resistant
  • Organisms: staphylococci (not MRSA)
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8
Q

oxacillin

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, very-narrow spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase resistant
  • Organisms: staphylococci (not MRSA)
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9
Q

penicillin G

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, narrow spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: streptococci, pneumococci, meningococci, Treponema pallidum
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10
Q

penicillin V

A
  • Cell wall synthesis inhibitor, beta-lactam compound, penicillin, narrow spectrum
  • MOA: bind and inhibit PBP enzymes–>prevent maintenance of peptidoglycan cell wall
  • Adverse effects: hypersensitivity, hemolytic anemia, secondary vaginal candidiasis infection
  • Beta-lactamase sensitive
  • Organisms: streptococci, pneumococci, meningococci, Treponema pallidum
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11
Q

clavulanic acid
sulbactam
tazobactam

A
  • Beta-lactamase inhibitors
  • use: avoid inactivation of cell wall inhibitors by bacterial degradation
  • often prescribed with amoxicillin, ampicillin, and piperacillin
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12
Q

cefazolin

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 1st generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: surgical prophylaxis, uncomplicated skin/soft tissue
  • does NOT enter CNS
  • organisms: gram (+) cocci
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13
Q

cephalexin

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 1st generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: surgical prophylaxis
  • does NOT enter CNS
  • organisms: gram (+) cocci
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14
Q

cefotetan

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 2nd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • does NOT enter CNS
  • organisms: gram (+) cocci, some gram (-)
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15
Q

cefaclor

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 2nd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • does NOT enter CNS
  • organisms: gram (+) cocci, some gram (-)
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16
Q

cefuroxime

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 2nd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • enters CNS
  • organisms: gram (+) cocci, some gram (-)
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17
Q

ceftriaxone

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 3rd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: empirical tx of meningitis and sepsis, osteomyelitis, septic arthritis, hospital acquired/ventilated related pneumonia, endocarditis
  • enter CNS
  • organisms: gram (+) and gram (-) cocci, gram (-) rods
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18
Q

cefotaxime

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 3rd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: empirical tx of meningitis and sepsis
  • enter CNS
  • organisms: gram (+) and gram (-) cocci, gram (-) rods
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19
Q

cefdinir

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 3rd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: empirical tx of meningitis and sepsis
  • enter CNS
  • organisms: gram (+) and gram (-) cocci, gram (-) rods
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20
Q

cefixime

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 3rd generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase sensitive
  • use: empirical tx of meningitis and sepsis
  • enter CNS
  • organisms: gram (+) and gram (-) cocci, gram (-) rods
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21
Q

cefepime

A
  • cell wall synthesis inhibitor, beta-lactam compound
  • 4th generation cephalosporin
  • MOA: bind and inhibit PBPs
  • Adverse effects: hypersensitivity, disulfiram-effect (avoid alcohol), bleeding disorder
  • beta-lactamase resistant
  • use: broadest spectrum, osteomyelitis sepsis
  • enter CNS
  • organisms: gram (+) and gram (-)
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22
Q

aztreonam

A
  • cell wall synthesis inhibitors, beta-lactam compound
  • monobactam compound
  • MOA: bind and inhibits PBPs
  • beta-lactamase resistant
  • enter CNS
  • organisms: gram (-) rods
  • use: serious pneumonia, meningitis, and sepsis
  • adverse effects: hypersensitivity
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23
Q

doripenem
imipenem
ertapenem
meropenem

A
  • cell wall synthesis inhibitors, beta-lactam compound
  • carbapenems compound
  • MOA: bind and inhibits PBPs
  • beta-lactamase resistant but susceptible to carbamenemase
  • imipenem inactivated by kidney–>administered with cilastatin
  • enter CNS
  • organisms: gram (-) and gram (+)
  • use: empirical tx of life-threatening infections
  • adverse effects: vomiting, diarrhea, hypersensitivity, hypotension, confusion, tremors, seizures
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24
Q

vancomycin

A
  • cell wall synthesis inhibitor
  • glycopeptide antibiotic
  • MOA: bind D-ala-D-ala pentapeptide–>prevent elongation of peptidoglycan–>inhibit cell wall synthesis
  • good tissue penetration but NOT CNS
  • organisms: gram (+) and gram (-)
  • Use: uncomplicated skin, MRSA, C.diff, meningitis, sepsis
  • adverse effects: flushing “red man syndrome”, ototoxicity, nephrotoxicity
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25
Q

bacitracin

A
  • cell wall synthesis inhibitor
  • polypeptide
  • MOA: block incorporation of aa and nucleic acids into cell wall
  • topical and ophthalmic ointment
  • use: broad spectrum for gram (+) and gram (-)
  • adverse effects: hypersensitivity is rare
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26
Q

fosfomycin

A
  • cell wall synthesis inhibitor
  • phosphoenolpyruvate
  • MOA: prevents synthesis of UDP-N-acetylmuramic acid–> blocks early step in cell wall synthesis
  • use: broad spectrum for gram (-) and (+), uncomplicated UTI in females
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27
Q

daptomycin

A
  • target cell membrane
  • lipopetide
  • MOA: binds membrane (Ca2+ dependent) –> depolarization of membrane–> bactericidal
  • use: gram (+), complicated tissue and skin, bacteremia, endocarditis, MRSA, enterococcus
  • adverse effects: myopathy
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28
Q

polymyxin B

A
  • target cell membrane
  • detergent
  • MOA: bind phospholipids in cell membrane–> disrupt structure
  • use: topically for skin in combo w/ bacitracin, gram (-)
  • adverse effects: rare
29
Q

streptomycin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-)
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
30
Q

genamicin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-), neonatal jaundice
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
31
Q

kanamycin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-)
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
32
Q

amikacin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-)
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
33
Q

tobramycin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-)
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
34
Q

neomycin

A
  • protein synthesis inhibitor
  • aminoglycoside
  • MOA: bind 30S (maybe 50S) and blocks formation of initiation complex (step 1)
  • use: bactericidal, combo w/ beta-lactams for serious gram (-)
  • adverse effects: nephrotoxicity, ototoxicity, hypersensitivity
35
Q

erythromycin

A
  • protein synthesis inhibitor
  • macrolide
  • MOA: binds 50S and impairs translocation to P site (step 4)
  • bacteriostatic at low conc. and bactericidal at high
  • use: gram (+) and some gram (-), pneumonia, Legionella pneumophila, C. jejuni, H. pylori
  • adverse effects: stomach cramps, nausea, vomiting, diarrhea (motilin receptor agonist), CYP450 inhibition
36
Q

clarithromycin

A
  • protein synthesis inhibitor
  • macrolide
  • MOA: binds 50S and impairs translocation to P site (step 4)
  • bacteriostatic at low conc. and bactericidal at high
  • use: gram (+) and some gram (-), pneumonia, Legionella pneumophila, C. jejuni, H. pylori
  • adverse effects: stomach cramps, nausea, vomiting, diarrhea (motilin receptor agonist), CYP450 inhibition
37
Q

azithromycin

A
  • protein synthesis inhibitor
  • macrolide
  • MOA: binds 50S and impairs translocation to P site (step 4)
  • bacteriostatic at low conc. and bactericidal at high
  • use: gram (+) and some gram (-), pneumonia, Legionella pneumophila, C. jejuni, H. pylori
  • adverse effects: stomach cramps, nausea, vomiting, diarrhea (motilin receptor agonist), CYP450 inhibition
38
Q

tetracycline

A
  • protein synthesis inhibitors
  • tetracyclines
  • MOA: binds 30S subunit of ribosome–> prevent binding of new aminoacyl-tRNA to A site (step 1)
  • use:broad spectrum, bacteriostatic, H. pylori, Rickettsia, Borrelia burgdorferi, Brucella, Vibrio
  • adverse effects: nutrient interaction (bind calcium–>growth of calcified tissue, discoloration of teeth, affect growth), disrupt normal flora, photosensitivity, chelator (prevent absorption of cations)
39
Q

minocycline

A
  • protein synthesis inhibitors
  • tetracyclines
  • MOA: binds 30S subunit of ribosome–> prevent binding of new aminoacyl-tRNA to A site (step 1)
  • use:broad spectrum, bacteriostatic, H. pylori, Rickettsia, Borrelia burgdorferi, Brucella, Vibrio
  • adverse effects: nutrient interaction (bind calcium–>growth of calcified tissue, discoloration of teeth, affect growth), disrupt normal flora, photosensitivity, chelator (prevent absorption of cations)
40
Q

doxycycline

A
  • protein synthesis inhibitors
  • tetracyclines
  • MOA: binds 30S subunit of ribosome–> prevent binding of new aminoacyl-tRNA to A site (step 1)
  • use:broad spectrum, bacteriostatic, H. pylori, Rickettsia, Borrelia burgdorferi, Brucella, Vibrio
  • adverse effects: nutrient interaction (bind calcium–>growth of calcified tissue, discoloration of teeth, affect growth), disrupt normal flora, photosensitivity, chelator (prevent absorption of cations)
41
Q

tigecycline

A
  • protein synthesis inhibitors
  • tetracyclines
  • MOA: binds 30S subunit of ribosome–> prevent binding of new aminoacyl-tRNA to A site (step 1)
  • use:broad spectrum, bacteriostatic, H. pylori, Rickettsia, Borrelia burgdorferi, Brucella, Vibrio, multi drug resitant enterococci and gram (-)
  • adverse effects: nutrient interaction (bind calcium–>growth of calcified tissue, discoloration of teeth, affect growth), disrupt normal flora, photosensitivity, chelator (prevent absorption of cations)
42
Q

clindamycin

A
  • protein synthesis inhibitor
  • MOA: binds 50S subunit of ribosome–>prevent formation of initiation complexes and translocation to P site
  • use: narrow spectrum, gram (+) cocci, MRSA, uncomplicated skin/soft tissue
  • adverse effects: nausea, vomiting, diarrhea, C.diff infection
43
Q

chloramphenicol

A
  • protein synthesis inhibitor
  • MOA: binds 50S subunit of ribosome–> prevents transpeptidation or peptidyl bond formation (step 2)
  • use: broad spectrum, bacteriostatic, 2nd line agent, typhus, Rocky Mountain spotted fever, eye infections
  • adverse effects: RBC suppression, Gray Baby Syndrome (infants lack glucuronic acid conjugation–> shock, vomiting, vascular collapse)
44
Q

linezolid

A
  • protein synthesis inhibitor
  • oxazolidinone
  • MOA: bind P site of 50S ribosome–> inhibit formation of ribosomal-fMET-tRNA complex (Step 1)
  • use: MRSA, multi-drug resistant enterococci
  • adverse effects: myelosuppression
45
Q

sulfadiazine

A
  • DNA synthesis inhibitor, antifolate drug
  • sulfonamide
  • MOA: compete with PABA for enzyme dihydropteroate synthase–>block dihydrofolic acid synthesis–> block DNA synthesis
  • broad spectrum
  • in combo w/ other drugs for gram (+/-)
  • adverse effects: hypersensitivity, photosensitivity, Steven-Johnson syndrome (serious/fatal skin and mucous membrane eruption)
46
Q

sulfamethoxazole

A
  • DNA synthesis inhibitor, antifolate drug
  • sulfonamide
  • MOA: compete with PABA for enzyme dihydropteroate synthase–>block dihydrofolic acid synthesis–> block DNA synthesis
  • broad spectrum
  • in combo w/ other drugs for gram (+/-), UTIs, prostatitis
  • adverse effects: hypersensitivity, photosensitivity, Steven-Johnson syndrome (serious/fatal skin and mucous membrane eruption)
47
Q

sulfamethizole

A
  • DNA synthesis inhibitor, antifolate drug
  • sulfonamide
  • MOA: compete with PABA for enzyme dihydropteroate synthase–>block dihydrofolic acid synthesis–> block DNA synthesis
  • broad spectrum
  • in combo w/ other drugs for gram (+/-)
  • adverse effects: hypersensitivity, photosensitivity, Steven-Johnson syndrome (serious/fatal skin and mucous membrane eruption)
48
Q

trimethoprim

A
  • DNA synthesis inhibitors, antifolate drug
  • trimethoprim
  • MOA: inhibits bacterial dihydrofolate reductase–> impaired DNA synthesis
  • use: gram (-), UTIs, prostatitis
  • adverse effects: bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia
49
Q

pyrimethamine

A
  • DNA synthesis inhibitors, antifolate drug
  • trimethoprim
  • MOA: inhibits bacterial dihydrofolate reductase–> impaired DNA synthesis
  • use: gram (-)
  • adverse effects: bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia
50
Q

trimethoprim-sulfamethoxazole (TMP-SMX)

A
  • DNA synthesis inhibitors, antifolate
  • MOA: synergistic activity
  • use: UTI and prostatitis
51
Q

norfloxacin

A
  • DNA synthesis inhibitor
  • group 1
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • least effective but broad spectrum against gram (+/-)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
52
Q

ciprofloxacin

A
  • DNA synthesis inhibitor
  • group 2
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (-) but some gram (+)
  • use: urinary, GI, respiratory, STI, anthrax, fever w/ neutropenia
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
53
Q

levofloxacin

A
  • DNA synthesis inhibitor
  • group 2
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (-) but some gram (+)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
54
Q

oxfloxacin

A
  • DNA synthesis inhibitor
  • group 2
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (-) but some gram (+)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
55
Q

gatifloxacin

A
  • DNA synthesis inhibitor
  • group 3
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (+) but some gram (-)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
56
Q

gemifloxacin

A
  • DNA synthesis inhibitor
  • group 3
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (+) but some gram (-)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
57
Q

moxifloxacin

A
  • DNA synthesis inhibitor
  • group 3
  • fluoroquinolones
  • MOA: disrupt winding of DNA/ separation of strands during transcription and translation (topoisomerase II and IV)
  • broad spectrum best against gram (+) but some gram (-)
  • use: urinary, GI, respiratory, STI, anthrax
  • adverse effects: nausea, vomiting, diarrhea, bind divalent cations, prevent absorption, QT prolongation
58
Q

metronidazole

A
  • DNA damage
  • MOA: prodrug–>organism activates–> reaction metabolites bind DNA–> disrupt function/ cause damage
  • use: anaerobic bacteria, abdomina, vaginitis, C. diff, brain abscess
  • adverse effects: nausea, vomiting, diarrhea, disulfiram-effect (avoid alcohol)
59
Q

isoniazid

A
  • first line anti-tuberculosis drug
  • bactericidal for actively growing bacilli
  • penetrates macrophages
  • structurally similar to pyridoxine (vit. B6)
  • MOA: activated by mycobacterial catalase-peroxidase enzyme (Kat G)–> impedes proteins synthesizing mycolic acid
  • use: prophylactic, active, and latent regimens
  • resistance: mutation in Kat G, over expression of Inh A protein (mycolic acid synthesis)
  • 2 drugs MUST be used for active TB
  • adverse effects: hepatitis (age and alcoholics increased risk), peripheral neuropathy (slowly metabolized)
60
Q

rifampin

A

-first line anti-tuberculosis drugs
-gram (+/-) and chlamydia sensitive
-MOA: bind DNA-dependent RNA polymerase–> inhibit transcription
-bactericidal, penetrate tissue and phagocytic cells
-use: 1st line active TB, alternative to INH in latent TB
-resistance: point mutation in RNA polymerase gene
adverse effects: nausea vomiting, headache, dizziness, hepititis, red-orange urine feces sweat tears and saliva (harmless)
-inducer of cytochrome P450–>eliminate many drugs–> contraindicated in HIV patients taking antiretrovirals

61
Q

pyrazinamide

A
  • first-line anti-tuberculosis drugs
  • analogue of nicotinamide use in combo therapy
  • MOA: bacterial pyrazinamidase enzyme activates–> inhibit mycolic acid synthesis?
  • dependent on acidic environment
  • use: part of active TB regimen
  • resistance: mutation in pyrazinamidase enzyme
  • enter macrophages
  • adverse effects: hepatotoxicity, hyperuricemia–> acute gouty arthritis
62
Q

ethambutol

A
  • first-line anti-tuberculosis drug
  • MOA: inhibits arabinosyl transferase–>inhibit cell wall synthesis
  • use: active TB, M. avium complex (MAC)
  • resistance: point mutation in arabinosyl transferase
  • use in combo
  • adverse effects: retrobulbar neuritis (impaired vision, red-green color blindness), hyperuricemia
63
Q

streptomycin

A
  • first-line anti-tuberculosis drug
  • aminoglycoside antibiotic
  • MOA: interfere with bacterial protein synthesis
  • use: M. tuberculosis, M. avium complex, TB of strains resistant to other drugs
  • injected, penetrates cells poorly
  • resistance: point mutations in ribosomal proteins
  • adverse effects: ototoxic, nephrotic
64
Q

rifabutin

A
  • second line anti-tuberculosis drug
  • MOA: inhibits RNA polymerase
  • use: active M. tuberculosis and M. avium complex (greater against MAC)
  • less potent induce of cytochrome P450–> use for HIV pts instead of rifampin
65
Q

M. avium complex (MAC) tx

A
  • pulmonary infection: macrolide (clarithromycin or azithromycin), rifampin, ethambutol, streptomycin
  • disseminated: macrolide, rifampin, ethambutol
  • prophylaxis in HIV pts: clarithromycin or azithromycin
66
Q

Active TB regimen

A
  • initial: INH, RIF, PZA, and EMB daily (8 wks)

- continuation phase: INH, RIF daily (18 wks)

67
Q

Leprosy regimen

A
  • dapsone, clofazimine, rifampin
  • tuberculoid: 1-2 yrs
  • lepromatous: 5 yrs
68
Q

dapsone

A
  • leprosy treatment
  • MOA: competitive inhibitor of folic acid synthesis
  • high conc in skin, muscle, kidney
  • adverse effects: non-hemolytic anemias, hemolytic anemia in pts with G6PD
69
Q

clofazimine

A
  • leprosy treatment
  • MOA: bactericidal dye, DNA binding?
  • highly lipophilic
  • skin discoloration–> red-brown to black

Pharmacology (34 decks)

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