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Pharm > Exam One Antibiotics: MOA, AE, USE etc > Flashcards

Exam One Antibiotics: MOA, AE, USE etc Flashcards

1
Q

• Therapeutic Use: Bactericidal Antibiotic
• MOA: cell wall synthesis inhibitor by inhibiting transpeptidase
• AE: inactivated by B-lactamases, mutant transpeptidases, down-regulated porins, efflux pump.
• Drug interactions: Not metabolized, excreted by kidney. Do not enter CNS, unless inflammation present.
• Notes: Probenecid decreases excretion of penicillins. Anti-staph penicillins are Isoxazolyls (Dicloxacillin and Oxacillin). Nafcillin and Dicloxicillin are penicillinase resistant penicillins.
o TAAM: Broad spectrum
o DOPP: Narrow spectrum

A

Cell Wall Synthesis Inhibitors
Penicillins

Penicillin G
Penicillin V
Oxacillin
Dicloxacillin
Ampicillin
Amoxicillin
Ticarcillin
Mezlocillin
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2
Q
  • Therapeutic Use: Nosocomial pneumonia, cellulitis, sinusitis, bone & joint infections.
  • MOA: bind irreversibly to and inhibit bacterial -lactamases.
  • AE: Cross the BBB
  • Drug interactions: Widely distributed, even to brain; renally excreted.
  • Notes: Not bacteriostatic or bactericidal (NOT ANTIBIOTICS). Piperacillin increases half-life of tazobactam.
A

ß-Lactamase Inhibitors
Clavulanate (oral)
Sulbactam (IV)
Tazobactam (IV)

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3
Q

• Therapeutic Use: Broad spectrum bactericidal (especially nosocomial pneumonia: pseudomonas aeruginosa, MRSA, Gr-‘s).
• Active: Gr+ cocci, Gr- with G2, G3, G4. Not MRSA or enterococci.
• MOA: Inhibit Cell wall synthesis by blocking transpeptidase.
• AE: if Pt is allergic to penicillin, probably allergic to cephalosporins. GI stress,
• superinfections, increases bleeding, Disulfram-like toxic Reaction w/ alcohol (red-face).
• Resistance: inactivated by -lactamases, mutation, porin down-regulation, efflux pumps
• Drug interactions: Unmetabolized and excreted by kidney.
• Notes: G4s are generally better than penicillins EXCEPT for anaerobes.
o Anti-pseudomonals treated with a G3 or G4 with clindamycin, cipro, imipenem, or meropenem.
o Probenecid (uricosuric agent) decreases excretion of cephalosporins.
o 1st Gen cephalosporin is a good empiric choice (Dr. Latva).
o OMNICEF po is a 3rd gen cephalosporin for ped puncture wound.
o Extra C makes them more resilient to Beta lactamases.

A

Cephalosporins (Beta-lactam antibiotics)

1st Generation
Cefazolin
Cephalexin

2nd Generation
Cefuroxime
Cefoxitin

3rd Generation
Cefixime
Cefoperazone
Cefotaxime
Ceftriaxone

4th Generation
Cefepime
Cefpirome

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4
Q
  • Therapeutic Use: Serious Broad-spectrum infections; Cilastin increases imipenem’s t1/2. Anti-pseudomonal.
  • MOA: Inhibit cell wall synthesis by inhibiting transpeptidase preventing PG crosslinking. Excreted by kidneys.
  • AE: distributes to brain; poor oral absorption. Penicillin allergic pt will have 50% allergy to carbapenems. GI distress
  • Drug interactions: some strains of Pseudomonas are resistant.
  • Notes: Not effective against MRSA, enterococcus, C. dificile, Legionella.
  • Cilastatin inhibits dehydropeptidase preventing imipenem’s degradation by kidney.
A

Carbapenems

Imipenem/Cilastatin

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5
Q
  • Therapeutic Use: Gr- & anaerobes; Serious narrow-spectrum infections, bactericidal and anti-pseudomonal.
  • MOA: Inhibit cell wall synthesis by inhibiting transpeptidase preventing PG crosslinking.
  • AE: GI distress.
  • Drug interactions:
  • Notes: Not effective against MRSA, enterococcus, C. dificile, Legionella. if pt is allergic to penicillin and carbapenem this is good to give.
A

Monobactams

Aztreonam

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6
Q
  • Therapeutic Use: IV, Non-beta-lactam cell wall inhibitor. MRSA!!!
  • MOA: binds D-ala D-ala moiety of pentapeptide of outer membrane preventing transpeptidase.
  • AE: poor oral absorption, wide distribution (not to brain), excreted unchanged by kidney. Thrombophlebitis, red man syndrome; Ototoxicity and nephrotoxicity (if combined with aminoglycoside).
  • Resistance: enterococci
  • Notes: for serious infections by Gr-, especially MRSA. Drug of last resort. VancoR enterococci get synercid (quinupristin / dalfopristin) or linezolid.
A

Vancomycin

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7
Q
  • Therapeutic Use: Topical, Non-beta-lactam cell wall inhibitor. Gr+.
  • MOA: inhibits de-P of C55 isoprenyl pyrophosphate carrier. Blocks addition of UDP from getting to membrane.
  • AE: wide distribution, kidney excreted. Severe nephrotoxicity so only used topically!
  • Resistance: None
  • Notes:
A

Bacitracin

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8
Q
  • Therapeutic Use: Narrow Spectrum (MRSA, vanco resistant Enterococcus, strep.)
  • MOA: Streptogramin; Protein synthesis inhibitor by binding 23S RNA of 50S subunit. Inhibits peptidyl transferase blocking elongation.
  • AE: thrombophlebitis, athralgia, myalgia. Poor oral absorption.
  • Resistance: lil known
  • Drug interactions: Increases effects of warfarin, diazepam, NNRTIs, and cyclosporines.
  • Notes: used in combination as Synercid. Dalfo is early phase and Quinu is late phase. Bacteriostatic, -cidal when used with lenezolid. Metabolized in liver and excreted in feces.
A

Protein Synthesis Inhibitors
Streptogramins
Quinupristin/dalfopristin

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9
Q
  • Therapeutic Use: VRE, MRSA, penicillin res Strep. Anti-TB
  • MOA: Oxazolidinone, protein synthesis inhibitor. Binds 23S RNA of 50S subunit inhibiting formation and initiation. Good oral absorption or IV
  • AE: Not good against Gr-. GI distress.
  • Drug Interactions: augments action of antidepressants and serotonin.
  • Resistance: some enterococcal strains.
  • Notes: bactericidal when used with Synercid.
A 
Oxazolidinones
Linezolid (Zyvox)
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10
Q
  • Therapeutic Use: Bacteriostatic, but –cidal at high doses. Chlamydia, mycoplasma, mycobacterium, Legionnaire’s, MAC
  • MOA: Bind 50S subunit and block formation of translation complex
  • AE: GI distress, Cholestatic hepatitis (failure of bile flow).
  • Resistance:
  • Notes: Good for pt allergic to penicillin. Lots of other drug interactions. Erythromycin used for topical acne treatment.
A

Macrolides ACE
Azithromycin
Clarithromycin
Erythromycin

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11
Q
  • Therapeutic Use: Ketolide (semi-synthetic macrolide), respiratory tract infection where macrolides don’t work.
  • MOA: Inhibits CYP3A4 system.
  • AE:
  • Resistance:
  • Notes: Taken orally. Back-up to macrolides.
A

Ketolides

Telithromycin

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12
Q
  • Therapeutic Use: Lincosamide; penicillin res. Gr+, anaerobes, Chlamydia, strep, staph, pneumococci.
  • MOA: binds 23S RNA of 50S inhibiting translation and formation of initiation complex.
  • AE: GI distress, respiratory paralysis (baclofen, diazepam, atracurium)
  • Resistance: Not for Gr-. Do not give with a muscle relaxant!!!
  • Notes: Bacteriostatic, good for pt allergic to penicillin. For nosocomial pneumonia use with G3 or G4 cephalosporin. Used for acne treatment.
A

Lincosamides

Clindamycin

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13
Q
  • Therapeutic Use: Gr-, Gr+, Pseudomonas, endocarditis, septicemia, nosocomial pneumonia, UTI. Anti-TB
  • MOA: Bind 16S RNA subunit of 30S ribosomal subunit and inhibits protein synthesis.
  • AE: Ototoxicity, Nephrotoxicity (w/ vanco or cyclosporine), NM blockade, respiratory distress.
  • Resistance: Anaerobes
  • Notes: Bactericidal. Poor oral absorption. Unmetabolized and eliminated by kidneys.
  • SGT-KA
A

Aminoglycosides

Streptomycin
Gentamicin
Tobramycin
Kanamycin
Amikacin
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14
Q
  • Therapeutic Use: Gr+, Gr-, anaerobes, Chlamydia, mycoplasmas, protozoa.
  • MOA: Bind 16S to the 30S ribosomal subunit and block docking of tRNA on ribosome.
  • AE:
  • Resistance:
  • Notes: Bacteriostatic. Use DOXYCYCLINE unless otherwise noted.
A

Tetracyclines
Tetracycline
Doxycycline
Minocycline

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15
Q
  • Therapeutic Use: New IV broad spectrum Abx against many drug resistant organisms (MRSA) for skin infections.
  • MOA: Glycycycline. Bind 16S to the 30S ribosomal subunit and block docking of tRNA on ribosome. Metabolized in liver, excreted by kidneys
  • AE: Incorporates into teeth and bones, phototoxicity, GI distress, oto-, hepato-, nephrotoxicity. Superinfections.
  • Resistance: Pseudomonas
  • Notes: Tetracycline derivative, don’t give to kids (goes into teeth!), pregnant, renal/liver implant.
A

Glycycyclines

Tigecycline (Tiger striped teeth)

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16
Q
  • Therapeutic Use: Gr- strep, pneumococci, meningococci, gonococci, bacilli. Chlamydia, protozoa.
  • MOA: Folic acid metabolism inhibitors by suppressing dehydropteroate synthase. Inhibits THF synthesis
  • AE: Overproduction of PABA and many renal, derm, and GI problems.
  • Resistance: only if M.O. imports folic acid.
  • Notes: structurally related to PABA. Stimulate Rickettsiae. Will cross BBB. Don’t give if pregnant (Kernicterus and jaundice to baby)
A

Folate Metabolism Inhibitors
Sulfonamides

Sulfamethoxazole
Sulfasalazine
Sulfadiazine

17
Q
  • Therapeutic Use: Broad spectrum, UTI, URTI, bronchitis.
  • MOA: Folic acid metabolism inhibitor by inhibiting dihydrofolate reductase.
  • AE: rash, neutropenia, hematologic toxicity in AIDS pt.
  • Resistance: mutations, if MO imports folic acid.
  • Notes: given with Sulfamethoxazole as Bactrim-DS. Don’t give in pt with liver impairment!!!
A

Trimethoprim

Folate Metabolism Inhibitors

18
Q

• Therapeutic Use: Broad spectrum, limited against anaerobes. Good for pseudomonas (cipro), Chlamydia, mycoplasma (anti-TB), conjunctivitis.
• MOA: block DNA synthesis by gyrase and topo IV.
• AE: GI distress N/C/V. Damages growing cartilage (bad for kids)
• Resistance:
• Notes: fluoride derivative of nalidixic acid. Cipro can treat anthrax! Don’t give to kids under 18 or if pregnant.
Ciprofloxacin
Levofloxacin

A

DNA Replication, Transcription and Metabolism Inhibitors

Fluoroquinolones

19
Q
  • Therapeutic Use: vaginitis, and other infections, acne.
  • MOA: inhibits DNA synthesis
  • AE:
  • Resistance:
  • Notes: Anti-protozoal drug
A

Urinary Tract Antiseptics

Metronidazole

20
Q
  • Therapeutic Use: acute and chronic UTI (E. coli, enterococci)
  • MOA: reduces nitrofuritonin damaging bacterial DNA
  • AE: GI, anorexia, hemolytic anemia, neuropathy, renal failure.
  • Resistance: rare.
  • Notes: bacteriostatic
A

Urinary Tract Antiseptics

Nitrofurantoin

21
Q
  • Therapeutic Use: UTI prophylaxis
  • MOA: bactericidal due to formaldehyde
  • AE: GI, polyuria, albuminuria, produces ammonia.
  • Resistance: Proteus
  • Notes: affects nearly all bacteria
A

Urinary Tract Antiseptics

Methenamine

22
Q
  • Therapeutic Use: topical staph causing impetigo; Gr+; Gr-.
  • MOA: inhibits bacterial enzymes for protein and RNA synthesis.
  • AE:
  • Resistance:
  • Notes: Broader spectrum than OTC products.
A

Urinary Tract Antiseptics

Mupirocin

23
Q
  • Therapeutic Use: Topical Gr- infection.
  • MOA:
  • AE:
  • Resistance:
  • Notes: only given topical because of toxicity
A

Urinary Tract Antiseptics

Polymyxins

Pharm (19 decks)

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