Antibacterials Flashcards
Lactulose
MOA: degraded by intestinal flora to lactic acid and other acids
Effect: acids trap the ammonia in the GIT so it cannot enter circulation and exacerbate the encephalopathy
Uses: hepatic encephalopathy, use as osmotic laxative, prebiotic
SE: osmotic diarrhea, flatulence, abd pn
Quinolones Drug Interactions
Theophylline, NSAIDS, corticosteroids = enhanced toxicity of quinolones
3rd and 4th gen = raide serum levels of Warfarin, Caffeine and Cyclosporine
Clindamycin PK and SE
PK: PO or IV, good penetration (gets to abscesses/bones)
SE: C. difficile, GI sx’s, skin rash, neutropenia and impaired liver fxn
2nd Gen Quinolones
Ciprofloxacin
Spectrum: extended G-ve activity, some G+ve, and some atypicals
DOC: anthrax
Use: ETEC, Pseudomonas (CF pt’s), meningitis prophylaxis (alt to Ceftriaxone and Rifampin)
Cefaclor / Cefoxitin / Cefotetan / Cefamandole
2nd generation Cephalosporins
Active against: H.influenzae, Enterobacter, some Neisseria
Use: sinusitis, otitis infections and LTIs
Cefotetan/Cefoxitin use: prophylaxis and therapy of abd/pelvic cavity infections
Sulfonamides PK, SE, CI
PK: PO or topical, acetylated in liver, eliminated via urine
SE: photosensitivity, crystalluria, HS rxn, hematopoietic disturgances (G6PD), kernicterus
CI: newborns/infants < 2 yo
Drug interaction: displace Warfarin, Phenytoin and Methotrexate from albumin
Tetracyclines (names)
Doxycycline / Minocycline / Tetracycline
Concentration-dependent Killing
Bigger the dose the better effect (covalent bonding so it doesnt matter if you keep giving it, the blockade is already in place)
*e.g. - aminoglycosides
Oxacillin
Excretion: renal and biliary
SE: hepatitis
Use: meningitis s/p trauma or surgery (S. aureus)
Aminoglycosides PK and SEs
PK: once daily admin, IV only, well distributed, high levels in renal cortex and inner ear
Excretion: kidney
SE: ototoxicity, nephrotoxicity, NM blockade
CI: MG (bc of NM blockade), pregnancy (unless benefits outweigh risks)
Tetracyclines DOC
Chlamydia, M. pneumoniae, Lyme dz, cholera, anthrax prophylaxis, RMSF, Typhus
Combo therapy for: H. pylori eradication, Malaria prophylaxis/tx, tx plague, Tularemia, Brucellosis
Polymyxin B
Spectrum: G-ve (bactericidal) MOA: acts as detergent, attach to and distrupt the cell membrane, binds and inactivates endotoxin Effect: cell lysis Use: topically for skin infections SE: nephrotoxic if given systemically
Ampicillin / Amoxicillin
‘Extended spectrum penicillins’
MOA: sensitive to β-lactamases, so activity is enhanced w/ β-lactamase inhibitor
PK: Amoxicillin has higher oral bioavailability than other penicillins
Use: children and pregnancy for acute otitis media, GAS pharyngitis, pneumonia, skin infection, UTIs, URIs (H. flu and S. pneumo)
SE: maculopapular rash, C. difficile
Neomycin
Use: bowel surgery, adjunct in hepatic encephalopathy, topical infections
SE: dermatitis
Cephalosporins SE
Pain @ infections ite, thrombophlebitis, superinfections (C. difficile), kernicterus (pregnancy)
Tetracyclines PK and SE
PK: variable PO absorption (decreased by divalent and trivalent cations)
Excretion: kidney
SE: teratogenic (category D), N/V/D, discoloration and hypoplasia of teeth, stunting growth, fetal hepatotoxicity, photosensitization, dizziness
Calvulanic acid / Sulbactam / Tazobactam
MOA: β-lactamas inhibitors
Effect: bind to and inactivate β-lactamases
Use: used in fixed combinations w/ specific penicillins but never used as abx themselves
Quinolones PK, SE, CI
PK: good oral bioavailability, high Vd, divalent cations interfere w/ absorption, adjust dose w/ renal dysfunction pt
SE: connective tissue damage (tendon rupture), peripheral neuropathy, QT prolongation, superinfections
CI: pregnancy/nursing mother, children < 18
Fosfomycin
MOA: inhibition of enolpyruvate transferase
Effect: inhibits CW synthesis
Admin: PO
Use: uncomplicated lower UTI
Aminoglycosides MOA
Amikacin / Gentamicin / Tobramycin / Streptomycin / Neomycin
Bactericidal, assoc. w/ serious toxicities so used mostly in combo w/ other Rx
MOA: passively diffuse across membrane of G-ve, then actively transported (O2 dependent) across cytoplasmic membrane then bind irreversibly (covalently) to 30S subunit of ribosome
Effect: prevent complex formation = prevent transcription = death of organism
Penicillin V
Administration: PO
Use: URIs, skin infections d/t strep
DOC: GAS pharyngitis
SE: +ve Coomb’s Test
β-lactamase inhibitors
Protect penicillins (β-lactams) from inactivation
Vancomycin
MOA: binds D-Ala-D-Ala pentapeptide terminus of PG, inhibits transglycosylation
Effect: inhibits CW synthesis and prevents elongation/polymerization of PG
Spectrum: G+ve only (MRSA, enterococci, PRSP)
Resistance G-ve (intrinsic), plasmid-mediated changes in drug permeability, modification of attachment site (adding D-lactate to terminus)
Minimal Bactericidal Concentration (MBC)
Lowest concentration of abx that results in a 99.9% decline in colony count after overnight incubation
*MBC of truly bactericidal agent is = to or slightly above the MIC
Respiratory Quinolones
Levofloxacin / Moxifloxacin / Gemifloxcin (3rd and 4th gen)
Target: S. pneumoniae, H. influenzae, M. catarrhalis
Use: when 1st line agents have failed, in presence of comorbidities, inpt management
Tetracyclines
MOA: entry via passive diffusion and energy-dependent transport, then bind the 30S subunit of ribosome to prevent attachment of animoacyl tRNA
Effect: protein synthesis halted = bacteriostatic
Spectrum: aerobic and anaerobic G+ve and G-ve
Resistance: impaired influx or increased efflux (plasmid-encoded), enzymatic inactivation, proteins that interfere w/ binding
Use: severe acne, rosacea, syphilis (pt’s w/ penicillin allergy)
Nafcillin
Excretion: primarily in bile
PK: not good for PO administration
Penicillins SEs
HS rxn, diarrhea, interstitial nephritis, hepatitis
Linezolid PK and SE
PK: PO, weak inhibitor of MAO, high Vd
SE: BM suppression, neuropathy, lactic acidosis
CI: caution when coadministration of drugs to increase adrenergic and serotonergic neurotransmitter levels
Penicillins resistance
Inactivation by β-lactamase, modification of target PBP, impaired penetration, increased efflux by pumps
*MRSA: altered target PBPs (low affinity for β-lactam abs)
Bacitracin
MOA: interferes w/ CW synthesis Active against: G+ve organisms Admin: topical use mainly Use: skin infections etc SE: nephrotoxic
Macrolides
Erythromycin / Clarithromycin / Azithromycin / Telithromycin
Bacteriostatic (bactericidal @ high concentration)
MOA: reversibly bind 23S rRNA of 50S subunit (same binding site as Clindamycin and Chloramphenicol)
Effect: blocks translocation halting transcription
Amoxicillin DOC
For endocarditis prophylaxis during dental or respiratory tract procedures (S. viridans)
*Amoxicillin + clavulanic acid is prophylactic for bites
Aminoglycosides DOC
Used in combo - septicemia, nosocomial RTIs, complicated UTIs, endocarditis
*once organism is identified these abx are usually d/c’d
Ampicillin Use/SE
Used in combo w/ Aminoglycosides to tx Enterococcus and Listeria (meningitis)
SE: pseudomembranous colitis
Chloramphenicol Uses
Serious infections resistant to less toxic drugs, or if it can reach the site of infection better it can be used, infections w/ VRE, topical tx of eye infections
Penicillins G Procaine
Developed to prolong duration of Penicilling G
Administration: given IM, seldom used (increases resistance)
PK: t1/2 = 12-24h
Co-trimoxazole (TMP-SMX)
Trimethoprim + Sulfamethoxazole = bactericidal
MOA: synergistic inhibition of sequential steps in folic acid synthesis
PK: PO, high Vd
DOC: uncomplicated UTIs, PCP, Nocardiosis
Use: toxoplasmosis (alt drug), URI d/t H. inflluenzae, M. catarrhalis
SE: dermatologic, GI, hematolytic anemia, high incidence of SE in AIDS pt
CI: pregnancy