Shared Flashcard Set

Details

Antibiotics
IUSM
40
Pharmacology
Professional
10/06/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
amoxicillin/clavulanic acid
Definition
Class: Anti-biotic, B-lactam, pencillin class

Mechanism: clavulanic acid blocks lactamases and amoxicillin inhibits PBPs, inhibits cell wall synthesis, bactericidal

Clinical use: bacteria with lactamases; H. influenza, P. miribalis, N. gonorrhoeae

Contraindication: previous allergic rxn to any B-lactam

Drug interactions:
Angtagonism - bacteriostatic abx, low pH, destrose solutions, aminoglycosides
Synergism - probenicid (blocks excretion)

Adverse effects: allergic (rash, anaphylaxis), GI distress

Absorption: oral
Distribution: renal high, CNS low (facilitate by inflamed meninges, renal impaired, or long hige dosage)
Elimination - renal 1*, hepatic 2*
Term
piperacillin/tazobactam
Definition
Class: anti-biotic, b-lactam, penicillin group

Mechanism: tazo blocks lactamases, piperacillin inhibits PBP, interferes w/ cell wall synthesis, bactericidal

Clinical use: bacteria with lactamases; H. influenza, P. miribalis, N. gonorrhoeae

Contraindication: previous allergic rxn to b-lactam

Drug interactions:
Antagonism - bacteriostatic abx, acidity, dextrose solutions, aminoglycosides
Synergism - probenicid (blocks excretion)

Adverse effects: allergy (rash, anaphylaxis), [GI distress]

Absorption: parenteral
Distrubtion: renal high, CNS low (facilitate with inflame meninges, renal impair, or long high dosage)
Elimination: 1* kidney, hepatic 2*
Term
penicillin G
Definition
Class: abx, B-lactam, penicillin group

Mechanism: inhibit PBP by mimic D-Ala-D-Ala, compromises cell wall integrity, bactericidal

Clinical use: S. pneumonia, N. meningitides, T. pallidum, B. anthracis

Contraindications: previous allergic rxn to B-lactam

Drug interactions:
Antagonism - bacteriostatic abx, acidity, dextrose solution, aminoglycosides
Synergism - probenicid (blocks excretion)

Adverse effects: allergy (rash, anaphylaxis), [GI distress]

Absorption: parenteral
Distribution: renal high, CNS low (facilitate inflamed meninges, renal impair, long high dosage)
Elminnation - 1* renal, hepatic 2*
Term
penicillin V
Definition
Class: abx, B-lactam, penicillin group

Mechanism: inhibit PBP by mimic D-Ala-D-Ala, compromises cell wall integrity, bactericidal

Clinical use: S. pneumonia, S. pyogenes, B. anthracis

Contraindications: previous allergic rxn to B-lactam

Drug interactions:
Antagonism - bacteriostatic abx, acidity, dextrose solution, aminoglycosides
Synergism - probenicid (blocks excretion)

Adverse effects: allergy (rash, anaphylaxis), [GI distress]

Absorption: oral
Distribution: renal high, CNS low (facilitate inflamed meninges, renal impair, long high dosage)
Elminnation - 1* renal, hepatic 2*
Term
amoxicillin
Definition
Class: abx, b-lactam, penicillin group

Mechanism: inhibit PBP by mimic D-Ala repeat, compromises cell wall integrity, bactericidal

Clinical use: S. pneumonia, H. influenza, E. coli, Salmonella, Listeria, P., miribalis, Enterococci

Contraindication: prvs allergic rx to b-lactam

Drug interaction:
Antagonism - bacterioastatic abx, acidity, dextrose sln, aminoglycoside
Synergism - probenicid (reduces excretion)

Adverse effects: allergy (rash, anaphylaxis), GI distress
**rash may not be allergy

Absorption: oral, better than ampicillin
Distribution: renal high, low CNS (except inflame meninges, renal impair, or long high dosage)
Elimination - renal 1*, hepatic 2*
Term
ampicillin
Definition
Class: abx, b-lactam, penicillin group

Mechanism: inhibit PBP, mimic D-Ala repeat, compromise cell wall, bactericidal

Clinical use: S. pneumonia, H. influenza, E. coli, Salmonella, Listeria, P. miribalis, Enterococci

Contraindication: previous allergic rxn to b-lactam

Drug interactions:
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress
**rash may not be allergy

Absorption: oral or parenteral
Distribution: renal high, CNS low (except inflamed meninges, renal impairment, high long dosage)
Excretion - renal 1*, hepatic 2*
Term
nafcillin
Definition
Class: abx, b-lactam, pencillin group

Mechanism: inhibit PBP, mimic D-Ala repeate, compromise cell wall, bactericidal

Clinical use: MSSA

Contraindication: prvs allergic rxn to b-lactam

Drug interaction:
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress

Absorption: parenteral
Distribution: renal high, CNS low (except meninges inflamed, renal impaired or long high dosage)
Excretion - HEPATIC 1*
Term
piperacillin
Definition
Class: abx, b-lactam, penicillin group

Mechanism: inhibit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

Clinical use: Pseudomonas spp.

Contraindication: previuos rxn to B-lactam

Drug interactions:
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synegism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress

Absorption: parenteral
Distribution: renal high, CNS low (except inflamed meninges, renal impaired, or long high dosage)
Excretion: renal 1*, hepatic 2*
Term
cefazolin
Definition
Class: abx, B-lactam, cephalosporin, 1st generation

Mechanism: inhibit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

Clinical use: G+ cocci, E. coli, P. mirabilis

Drug interactions:
Increase toxicity - nephrotoxicity
Prevent ceph absorption - antacids, H2 blockers
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress, DIRECT toxicity to kidneys

Distribution: renal high, CSF low
Excretion: renal 1*, hepatic 2*
Term
cephalexin
Definition

Class: abx, b-lactam, cephalosporin, 1st generation

 Mechanism: inhibit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

 Clinical use: G+ cocci, E. coli, P. miribalis

 

Drug interactions:

Increase toxicity - nephrotoxic drugs

Decrease ceph absorption - antacids, H2 blockers

Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides

Synergism - probenicid (reduce excretion)

 

Adverse effects: allergy, GI distress, DIRECT toxicity to kidneys

 Distribution: renal high, CSF low

Excretion: 1* kidney, 2* liver

Term
ceftoxamine
Definition
Class: abx, b-lactam, cephalosporin, 3rd generation

Mechanism: inhibit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

Clinical use: G-, enterobacter, serratia, PSEUDOMONAS

Drug interaction:
Increase toxicity - nephrotoxic drugs
Dec. absorption of ceph - antacids, H2 blockers
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress, DIRECT toxicity to kidney

Distribution: renal high, CSF low
Excretion: 1* renal, 2* hepatic
Term
ceftriaxone
Definition
Class: abx, b-lactam, cephalosporin, 3rd generation

Mechanism: inhibit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

Clinical use: G-, enterobacter, serratia, N. GONORRHOEAE, MENIGITIS

Drug interactions:
Increase toxicity - nephrotoxic drugs
Dec. ceph absorption - antacids, H2 blockers
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress, DIRECT toxicity to kidney, BILIARY SLUDGE form prolonged use (pain, nausea, vomit, 43%)

Distribution: renal high, CSF low
Excretion: HEPATIC 1*
Term
aztreobam
Definition
Class: abx, b-lactam, monobactam

Mechanism: inhibit PBP, mimic D-ala repeat (single B-lactam ring), compromise cell wall, bactericidal

Clinical use: G- AEROBES including aerobic forms of Enterobacter and Pseudomonas; OKAY FOR PPL WITH PENICILLIN ALLERGY

Drug interaction:
Increase toxicity - nephrotoxic drugs
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress, DIRECT toxicity to kidney

Distribution: renal high, CSF low
Excretion: renal 1*, hepatic 2*
Term
imipenem

**need pharmacokinetics
Definition
Class: abx, b-lactam, carbapenem

Mechanism: inhbit PBP, mimic D-ala repeat, compromise cell wall, bactericidal

Clinical use: broad, G+/-, RESERVE TREATMENT, co-administer with Cilastin to prevent degradation by renal enzymes

Drug interactions:
Increase toxicity - nephrotoxic drugs
Dec. absorption - antacids, H2 blockers
Antagonism - bacteriostatic abx, acidity, dextrose sln, aminoglycosides
Synergism - probenicid (reduces excretion)

Adverse effects: allergy, GI distress
Term
ciprofloxacin
Definition
Class: abx, quinolones, 2nd generation

Mechanism: target topoisomerases, interferes with uncoil/coil of DNA, bactericidal; G+ - topoisomerase IV that unlinks daughter chromosomes; G- topoisomerase II/DNA gyrase that negative supercoils

Clinical use: UTI and GI tract infections of G- rods; B. anthracis inf or exposure; Resp infections by G- aerobes; CA pneumonia alternative of Legionella or M pneumonia

Contraidications: children, pregnant/nursing (damage to growing cartilage), use in CF kids (benefit>risk)

Drug interactions:
Antagonism - metal chelate the cipro
Pharm - slows theophylline metabolism (nausea, vomit, tremors agitation)
Additive - drugs that prolong QT

Adverse effects: peripheral neuropathy, QT interval prolonged, tendinitis (damage, pain, rupture)

Absorption: oral (40-99%)
Distribution: excellent, SPUTUM AND LUNG TISSUE, CNS 10%
Elimination: RENAL
Term
levofloxacin
Definition
Class: abx, quinolones, 3rd generation

Mechanism: target topoisomerase, interfere with coil/uncoil of DNA, bactericidal; G+ topoisomerase IV which decatenates daughter chromosomes; G- topoisomerase II/DNA gyrase which relaxes supercoils

Clinical use: UTI and GI tract infections by G- rods, CA pneumonia alternative for Legionella or M. pneumonia; S. pneumonia with high penicillinase activity

Contraindiation: children, pregnant/nursing (damage growing cartilage)

Drug interactions:
Metals chelate quinolones block absorption
Increase QT prolonging drug effects

Adverse effects: peripheral neuropathy, prolonged QT interval, tendinitis (damage, pain, rupture)

Absorption: oral (40-99%)
Distribution: excellent, SPUTUM AND LUNG TISSUE
Elimination: Renal
Term
sulfamethoxazole
Definition
Class: abx, anti-folate, sulfonamide

Mechanism: resemble PABA and reversibly inhibit DHPS in folate metabolism to THF for DNA/RNA synthesis

Clinical use: UTIs

Contraindications: pregnant near term or nursing, and infants (risk of bilirubin displacement, jaundice)

Drug interactions: potentiates toxic drugs, anticoagulants, and hemolytic drugs

Adverse effects: allergy (rash, fever, photosensitivity; esp. HIV and G6PD deficient); may precipitate in urine

Absorption: oral
Half-life 6-12 hours
Term
trimethoprim/sulfamethoxazole
Definition
Class: abx and anti-fungal, anti-folate

Mechanism: inhibits two sequential steps in folate metabolism to THF for DNA/RNA synthesis, synergistic, minimizes resistance; inhibits DHPS and DHFR

Clinical use: RECURRENT UTIs, acute exacerbations of CHRONIC BRONCHITIS, GI tract infections, b-lactam resistant ear infections, opportunistic infections of AIDS; PNEUMOCYSTIS JIROVECI PNEUMONIA

Drug interactions: other antifolates - has potent additive effect in human cells

Adverse effects: more pronounced due to combo effect; ALLERGY (rash, fever, photosensitivity), may precipitate in urine, MEGALOBLASTIC ANEMIA, LEUKOPENIA, GRANULOCYTOPENIA (offset with supplemental folinic acid), nephrotoxicity

Absorption: oral, can give IV
Distribution: good, including CSF and sputum
Excretion - renal
Term
erythromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+ bacteria, Legionella pneumonia, mycoplasma pneumonia

Contraindication: hepatic impairment, esp. pregnant women

Drug interactions: potent inhibitor of CYP450s, interferes with metabolism of other drugs
Impaired by: chloramphenicol and clindamycin antagnozie, antihistamines or fluoroquinolones increase risk of arrhythmias;
theophylline and anticoagulants increase serum conc.
digoxin increases serum conc.

Adverse effects: GI distress; ESP. INCREASE GI MOTILITY; PROLONG QT INTERVAL

Absorption:1* oral, food decrease absorption, IV form available
Distribution: conc. in macrophages and most tissues, lung good, CNS too low for therapy
Elimination: hepatic, CYP3A4, biliary, some renal
Term
clarithromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+ bacteria, Legionella pneumonia, bronchitis

Contraindications: hepatic impairment, esp. pregnant women

Drug interactions: potent inhibitor of CYP450s, interferes with metabolism of other drugs
Impaired by: chloramphenicol and clindamycin [antagnozie], rifamycins lower serum level, theophylline and anticoagulants increase serum conc.

Adverse effects: GI distress, cardiac arrhythmias

Absorption: 1* oral
Distribution: conc. in macrophages and most tissue, good to lung, CNS to low for therapy
Elimination: hepatic CYP3A4, biliary, 30% by renal
Term
azithromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+/- bacteria, Legionella, H. influenze pneumonia, Chlamydia, Neissera, bronchitis, mycobacterium avium (AIDS), mycoplasma pneumonia

Contraindications: hepatic impairment, esp. pregnant women

Drug interactions: antacids with Mg or Al dec. serum conc.; chloramphenicol and clindamycin antagonize; antihistamines and fluoroquinolones increase risk of arrhythmias

Adverse effects: GI distress, CARDIAC ARRHYTHMIAS, PROLONG QT INTERVAL

Absorption: 1* oral, food dec. absorption, first dose is double, IV form available
Distribution: conc. in macrophages and most tissues, lung tissue good, CNS too low for therapy
Elimination: hepatic, biliary, some renal
Term
fidaxomicin
Definition
Class: abx, macrolides

Mechanism: targets RNA polymerase, accumulates in G+ and macrophages

Clinical use: G+ bacteria, CLOSTRIDIUM DIFFICILE SUPERINFECTIONS

Contraindication: hepatic impairment, esp. pregnant women

Drug interactions: chloramphenicol and clindamycin antagonize

Adverse effects: cardiac arrhythmias

Absorption: 1* oral
Distribution: conc in macrophages and most tissue, good to lung, CNS too low for therapy
Elimination: hepatic, biliary, some renal
Term
doxycylcine
Definition
Class: abx, tetracycline

Mechanism: bind to 30S, blocks binding of aminoacyl RNA, pumped into bacteria, high differential conc.

Clinical use: broad, G+/-; Proprionibacterium (acne), Rickettsia, Vibrio cholera, spirochetes (Lyme disease, syphilius)

Contraindications: children under 8y/o, pregnant/lactating, hepatic impairment

Drug interactions: antacids, sodium bicarbonate and iron salts prevent absorption to therapeutic level

Adverse effects: GI distress, GERD, PHOTOSENSTIVITY, SKELETAL - binds to bone and teeth

Absorption: highly lipophilic, near complete oral
Elimination: hepatic or other non-renal

**spontaneous cnversion to toxic form over time - DONT USE AFTER EXPIRATION
Term
chloramphenicol
Definition
Class: abx, protein synthesis inhibitor

Mechanism: bind 50S, blocks peptide bond formation

Clinical use: Brain abscesses (B. fragilis, Streptococci), Meningitis (H. influenza, N. meningititis), Rickettsia, Salmonella typhi, Bacterial conjunctivitis ("no" adverse effects)

Contraindication: pregnancy (except topical), moderate inf. for which safer drugs can be used

Drug interactions:
Inhibits CYP450s - blocks metabolism of other drugs
Potentiate bone marrow suppressants
Antagonize erythromycin and clindamycin, similar binding site on 50S

Adverse effects: Bone marrow suppression, Gray-Baby syndrome, Peripheral neuritis or optic neuritis

Absorption: generally good
Distribution: CSF conc. 9x serum, CNS infection if other tx fails
Metabolism: liver, UDP-glucuronyl transferase
Elimination: glomerular filtration
Term
erythromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+ bacteria, Legionella pneumonia, mycoplasma pneumonia

Contraindication: hepatic impairment, esp. pregnant women

Drug interactions: potent inhibitor of CYP450s, interferes with metabolism of other drugs
Impaired by: chloramphenicol and clindamycin antagnozie, antihistamines or fluoroquinolones increase risk of arrhythmias;
theophylline and anticoagulants increase serum conc.
digoxin increases serum conc.

Adverse effects: GI distress; ESP. INCREASE GI MOTILITY; PROLONG QT INTERVAL

Absorption:1* oral, food decrease absorption, IV form available
Distribution: conc. in macrophages and most tissues, lung good, CNS too low for therapy
Elimination: hepatic, CYP3A4, biliary, some renal
Term
clarithromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+ bacteria, Legionella pneumonia, bronchitis

Contraindications: hepatic impairment, esp. pregnant women

Drug interactions: potent inhibitor of CYP450s, interferes with metabolism of other drugs
Impaired by: chloramphenicol and clindamycin [antagnozie], rifamycins lower serum level, theophylline and anticoagulants increase serum conc.

Adverse effects: GI distress, cardiac arrhythmias

Absorption: 1* oral
Distribution: conc. in macrophages and most tissue, good to lung, CNS to low for therapy
Elimination: hepatic CYP3A4, biliary, 30% by renal
Term
azithromycin
Definition
Class: abx, macrolides

Mechanism: bind to 50S, inhibit translocation, accumulates in G+ and macrophages

Clinical use: G+/- bacteria, Legionella, H. influenze pneumonia, Chlamydia, Neissera, bronchitis, mycobacterium avium (AIDS), mycoplasma pneumonia

Contraindications: hepatic impairment, esp. pregnant women

Drug interactions: antacids with Mg or Al dec. serum conc.; chloramphenicol and clindamycin antagonize; antihistamines and fluoroquinolones increase risk of arrhythmias

Adverse effects: GI distress, CARDIAC ARRHYTHMIAS, PROLONG QT INTERVAL

Absorption: 1* oral, food dec. absorption, first dose is double, IV form available
Distribution: conc. in macrophages and most tissues, lung tissue good, CNS too low for therapy
Elimination: hepatic, biliary, some renal
Term
fidaxomicin
Definition
Class: abx, macrolides

Mechanism: targets RNA polymerase, accumulates in G+ and macrophages

Clinical use: G+ bacteria, CLOSTRIDIUM DIFFICILE SUPERINFECTIONS

Contraindication: hepatic impairment, esp. pregnant women

Drug interactions: chloramphenicol and clindamycin antagonize

Adverse effects: cardiac arrhythmias

Absorption: 1* oral
Distribution: conc in macrophages and most tissue, good to lung, CNS too low for therapy
Elimination: hepatic, biliary, some renal
Term
doxycylcine
Definition
Class: abx, tetracycline

Mechanism: bind to 30S, blocks binding of aminoacyl RNA, pumped into bacteria, high differential conc.

Clinical use: broad, G+/-; Proprionibacterium (acne), Rickettsia, Vibrio cholera, spirochetes (Lyme disease, syphilius)

Contraindications: children under 8y/o, pregnant/lactating, hepatic impairment

Drug interactions: antacids, sodium bicarbonate and iron salts prevent absorption to therapeutic level

Adverse effects: GI distress, GERD, PHOTOSENSTIVITY, SKELETAL - binds to bone and teeth

Absorption: highly lipophilic, near complete oral
Elimination: hepatic or other non-renal

**spontaneous cnversion to toxic form over time - DONT USE AFTER EXPIRATION
Term
chloramphenicol
Definition
Class: abx, protein synthesis inhibitor

Mechanism: bind 50S, blocks peptide bond formation

Clinical use: Brain abscesses (B. fragilis, Streptococci), Meningitis (H. influenza, N. meningititis), Rickettsia, Salmonella typhi, Bacterial conjunctivitis ("no" adverse effects)

Contraindication: pregnancy (except topical), moderate inf. for which safer drugs can be used

Drug interactions:
Inhibits CYP450s - blocks metabolism of other drugs
Potentiate bone marrow suppressants
Antagonize erythromycin and clindamycin, similar binding site on 50S

Adverse effects: Bone marrow suppression, Gray-Baby syndrome, Peripheral neuritis or optic neuritis

Absorption: generally good
Distribution: CSF conc. 9x serum, CNS infection if other tx fails
Metabolism: liver, UDP-glucuronyl transferase
Elimination: glomerular filtration
Term
clindamycin
Definition
Class: abx, protein syn. inhibitors

Mechanism: bind 50S, inhibits translocation, passively enters bacteria, conc. in macrophages

Clinical use: ANAEROBIC G- bacilli, septicemia, respiratory ailments, AEROBIC G+ cocci alternative if penicillin resistant or allergy

Contraindications: C. diff colitis (natural resistance), severe hepatic impairment

Drug interactions: pontentiates neuromuscular blockers, blocks absorption of anti-diarrheal, prolong colitis, antagonist of chloramphenicol and macrolides

Adverse effects: diarrhea (10-30%), ANTIBIOTIC RESISTANT COLITIS

Absorption: oral, unaffected by food
Distribution: therapeutic con. in many fluid/tissue/bone, not in CNS
Elimination: hepatic metabolism
2-3hrs half-life
Term
gentamycin
Definition
Class: abx, aminoglycoside, highly polar cation, 3 amino sugars

Mechanism: binds to ribosomal protein, blocks translation, causes miscoding, block translocation; requires porin that uses oxygen and energy to get into bacteria; aerobic only, bactericidal

Clinical use:
G-: enterbacter, klebsiella, proteus, pseudomonas
G+: w/ B-lactam, S. viridans, S. alagactiae, enterococcus
EMPERIC THERAPY

Contraindications: mild/moderate infections

Drug interactions:
Potentiates - b-lactams in vivo
Increase risk - ototoxic drugs, nephrotoxic drugs, neuromuscular blockade

Adverse effects: ototoxicity (esp. pregnant for fetus), renal toxicity, neuromuscular blockade

Absorption: IV or IM or topical
Distribution: low lipid solubility, pumps conc. in renal tubules and inner ear hair cells
Metabolism: minimal
Excretion: ~exclusively renal, highly variable (slow: neonates, elderly; fast: CF, burn)
Term
streptomycin
Definition
Class: abx, aminoglycoside, highly polar cation, 3 amino sugars

Mechanism: binds ribosomal proteins, blocks transcription/translocation, causes miscoding; requires porin, oxygen and energy for entry; aerobic only, bactericidal

Clinical use:
G+: w/ b-lactam, S. viridians, S. alagactiae, enterococcus
M. tuberculosis, N. gonorrhoeae if pen/quinolone allergy/resistant
EMPERIC THERAPY

Contraindications: mild/moderate infections

Drug interactions:
Potentiates: B-lactam in vivo
Increase risk: ototoxic/nephrotoxic drugs, neuromuscular blockade

Adverse effects: ototoxicity (esp. pregnancy for fetus), renal toxicity, neuromuscular blockade

Absorption: IV, IM, or topical
Distribution: low lipid solubility, pumps conc. in renal tubule and inner ear hair cells
Metabolism: minimal
Excretion: renal, rate is variable (slow: neonates, elderly; fast: CF, burn)
Term
neomycin
Definition
Class: abx, aminoglycoside, highly polar cation, 3 amino sugars

Mechanism: binds ribosomal protein, blocks transcription/translocation, causes miscoding; requires porin, oxygen, energy for entry; aerobic only, bactericidal

Clinical use:
G+: w/ b-lactam, S. viridians, S. alagactiae, enterococcus
EMPERIC THERAPY

Contraindications: mild/moderate inf.

Drug interactions:
Potentiates: b-lactam in vivo
Increase risk: ototoxic/nephrotoxic drugs, neuromuscular blockade

Adverse effects: ototoxicity (esp. pregnancy for fetus), renal toxicity, neuromuscular blockade

Absorption: IV, IM, topical
Distribution: low lipid solubility, pumps conc. in renal tubules and inner ear hair cells
Metabolism: minimal
Excretion: renal, rates vary (slow: neonates, elderly; fast: CF, burn)
Term
tobramycin
Definition
Class: abx, aminoglycoside, highly polar cation, 3 amino sugars

Mechanism: binds ribosomal protein, blocks transcription/translocation, causes miscoding; requires porin, oxygen and energy for entry; aerobic only, bactericidal

Clinical use:
G-: proteus, klebsiella, enterobacter, pseudomonas
G+: w/ b-lactam, S. viridians, S. alagactiae, enterococcus
EMPERIC THERAPY

Contraindications: mild/moderate inf.

Drug interactions:
Potentiates: b-lactam in vivo
Increase risk: ototoxic/nephrotoxic drugs, neuromuscular blockade

Adverse effects: ototoxicity (esp. pregnancy for fetus), renal toxicity, neuromuscular blockade

Absorption: IV, IM, topical
Distribution: low lipid solubility, pumps conc. in renal tubules and inner ear hair cells
Metabolism: minimal
Excretion: renal, rate varies (slow: neonates, elderly; fast: CF, burn)
Term
dapsone
Definition
Class: abx, reserve treatment for MDR bugs

Mechanism: antifolate, inhibit DHPS, similar to sulfonamides

Clinical use: daily therapy for leprosy for 1yr, w/ rifampin

Contraindication: pregnancy near term and infants (bilirubin displacement, jaundice)

Drug interactions: potentiates - toxic drugs, anticoagulants and hemolytic drugs

Adverse effects: allergy (fever, rash, photosensitivy; HIV and G6PD deficiency commonly), may precipitate in urine (drink alkaline water)

Absorption: oral
Half-life: 6-12 hrs
Term
isoniazid
Definition
Class: abx, reserve treatment for MDR bugs

Mechanism: inhibits mycolic acid synthesis, disrupts cell wall of mycobacteria, bacteriostatic for resting forms, bactericidal for growing forms

Clinical use: alone for TB prophylaxis, in combo for TB tx

Adverse effects: hepatotoxicity, peripheral neuritis (offset with Vit B6), rash, hemolysis in G6PD deficiency, convulsions in pts prone to seizure

Absorption: readily orally or parenterally
Distribution: enters cells/tissues/fluids, including CSF
Metabolism: liver, acetylases (fast and slow metabolizing genetic polymorphisms)
Excretion: glomerular filtration
Term
metronidazole
Definition
Class: abx, reserve tx for MDR bacteria

Mechanism: metabolized by anaerobes into free radicals that damage DNA and proteins

Clinical use: ANAEROBIC, Bacterioides spp., Helicobacter spp., CLOSTRIDIUM DIFFICILE COLITIS, protozoa

Drug interactions: w/ alcohol -> flushing, headache, GI distress

Absorption: well orally
Distribution: good, even to CNS
Elimination: renal
Half-life: 8hr
Term
polymyxin B & E
Definition
Class: abx, reserve tx for MDR bugs

MechanismL cyclic peptide w/long hydrophic tail (detergent), interacts and disrupts cell membrane, bactericidal

Clinical use: drug-resistant G- bacteria
B-ear, eye, topical use
E-ear topical, IV/oral available only as last resort, "the nuke bomb" for Acinetobacter and Pseudomonas

Adverse effects: generally well tolerated, minor hepatotoxicity

Absorption: oral, topical; IV alt. only
Distribution: well to tissues, including CNS [orange-red bodily fluids may result]
Metabolism: activated by CYP450 metabolism, induces CYP450s
Excretion: biliary and renal routes
Term
vancomycin
Definition
Class: abx, reserve tx for MDR bugs

Mechanism: inhibits cell wall synthesis, binds D-Ala repeat prevent cross-linking, bactericidal in growing bacteria

Clinical use: only G+ that are resistant to other tx, MRSA, MSSE, penicillin-R S. pneumonia, non VRE enterococcus

Drug interactions: additive toxicity to ototoxic and nephrotoxic drugs

Adverse effects: Red Man Syndrome with rapid infusion, allergy (rash, anaphylaxis, 1%)

Absoroption: IV or oral (contra IM, painful)
Distribution: wide, CNS if meninges inflamed
Elimination: renal
Half-life: 6hrs
Supporting users have an ad free experience!