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Flashcards in Antibiotics II Deck (31):
1

Penicillin G

B-lactam
Use: Strep and meningococcal infections, syphilis. Penase susceptible
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: Rapid renal elim, frequent dosing
Toxic: Hypersensitivity reactions (5-6%)

2

Penicillin V

B-lactam
Use: Strep and meningococcal infections, syphilis. Penase susceptible
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: Rapid renal elim, frequent dosing
Toxic: Hypersensitivity reactions (5-6%)

3

Nafcillin

B-lactam
Use: Staphylococcal infections, Penase resistant
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: Rapid renal elimination, frequent dosing. Some biliary clearance
Toxic: Hypersensitivity reactions (5-6%)

4

Ampicillin

B-lactam
Use: Greater activity vs gram-negative bacteria
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: rapid renal elimination
Toxicities: Hypersensitivity reactions (5-6%), GI distress, maculopapular rash

5

Amoxicillin

B-lactam
Use: Greater activity vs gram-negative bacteria
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: rapid renal elimination
Toxicities: Hypersensitivity reactions (5-6%)
Combo: Add Clavulanate, a B-lactamase inhibitor (Augmentin)

6

Piperacillin

B-lactam
Use: Greater activity vs gram-negative bacteria
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: rapid renal elimination
Toxicities: Hypersensitivity reactions (5-6%)

7

Ticarcillin

B-lactam
Use: Greater activity vs gram-negative bacteria
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: rapid renal elimination
Toxicities: Hypersensitivity reactions (5-6%)

8

Cephalexin

B-lactam
Use: 1st gen. Skin, soft tissue UT infections
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: Oral for older drugs, IV for newer. Renal elim. Short half life
Toxic: Hypersensitivity (~2%), assume cross reactivity (partial w/ penicillins), GI distress

9

Cefuroxime

B-lactam
Use: 2nd gen. More active vs. S. pneumoniae and H. influenza
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: Oral and IV, renal clearance, short half life
Toxic: Toxic: Hypersensitivity (~2%), assume cross reactivity (partial w/ penicillins), GI distress

10

Ceftriaxone

B-lactam
Use: 3rd gen. Pneumonia, meningitis, pyelonephritis, gonorrhea
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: IV, mixed clearance, longer half life (6 hrs). Good CNS penetration
Toxic: Toxic: Hypersensitivity (~2%), assume cross reactivity (partial w/ penicillins), GI distress

11

Ceftazidime

B-lactam
Use: 3rd gen. good activity vs. Pseudomonas. Poor vs. gram +
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: IV, renal elim, short half life, enters CNS
Toxic: Toxic: Hypersensitivity (~2%), assume cross reactivity (partial w/ penicillins), GI distress

12

Cefepime

B-lactam
Use: 4th gen. Broad activity, beta-lactamase stable
Mech: Prevents bacterial cell wall syn, binds and inhibits transpeptidases
Pharm: IV, renal elim, short half life
Toxic: Toxic: Hypersensitivity (~2%), assume cross reactivity (partial w/ penicillins), GI distress

13

Vancomycin

Glycopeptic
Use: Gram + activity, includes MRSA and PRSP
Mech: binds D-Ala-D-Ala terminal of peptidoglycan – inhibits transglycosylation
Pharm: Parenteral, oral for C. dificile colitis
Toxic: Red-man syndrome, rare nephrotoxicity

14

Tetracycline

Use: Infections of chlamydiae, mycoplasma, rickettsiae, spirochetes, malaria, H pylori, acne (low dose)
Mech: Binds 30S ribosomal subunit, bacteriostatic, broad spectrum
Pharm: Oral, IV. Renal and biliary clearance, half life 8 hrs, dosed every 6 hrs
Toxic: GI upsets, deposition in developing bones/teeth, photosensitivity, superinfection

15

Doxycycline

Tetracycline
Use: CA pneumonia, exacerbations of bronchitis. Infections of chlamydiae, mycoplasma, rickettsiae, spirochetes, malaria, H pylori, acne (low dose)
Mech: Binds 30S ribosomal subunit, bacteriostatic, broad spectrum
Pharm: Oral and IV, longer half life (18 hr). dosed 2x daily. Nonrenal elim.
Toxic: Toxic: GI upsets, deposition in developing bones/teeth, photosensitivity, superinfection

16

Tigecycline

Glycylcycline
Use: Broad spectrum antibiotic, unaffected by common tetracycline resistant mechs
Mech: Tetracycline analog, Binds 30S ribosomal subunit, bacteriostatic, broad spectrum
Pharm: IV only
Toxic: Nausea and vomiting

17

Gentamicin

Aminoglycoside
Use: Aerobic gram-negative bacteria, synergistic activity in endocarditis caused by streptococci, staphylococci, enterococci with B-lactams
Mech: Binds 30S ribosomal subunit, prevents protein synthesis
Pharm: IV, renal clearance, HL 2.5 hrs, once-daily dosingat 5-7 mg/kg = less toxicity
Toxic: Nophrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade

18

Tobramycin

Aminoglycoside
Use: More active than Gentamicin vs. Pseudomonas
Mech: Binds 30S ribosomal subunit, prevents protein synthesis
Pharm: IV, HL 2.5 hrs, renal clearance
Toxic: May have less nephrotoxicity than gentamicin, ototoxicity, neuromuscular blockade

19

Amikacin

Aminoglycoside
Use: Aerobic gram-negative bacteria, synergistic activity in endocarditis caused by streptococci, staphylococci, enterococci with B-lactams, resistant to enzymes that inactivate gentamicin and tobramycin
Mech: Binds 30S ribosomal subunit, prevents protein synthesis
Pharm: IV, renal clearance, HL 2.5 hrs, higher doses and target peaks and troughs than gentamicin
Toxic: Nophrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade

20

Erythromycin

Macrolide
Use: CA pneumonia, pertussis, corynebacteria, chlamydial infections
Mech: Binds 50S ribosomal subunit, prevents protein synthesis, bacteriostatic
Pharm: Oral and IV, Hepatic clearance, HL 1.5 hrs
Toxic: GI upsets, hepatotoxicity, QTc prolongation, CYP450 inhibition

21

Clarithromycin

Macrolide
Use: CA pneumonia, pertussis, corynebacteria, chlamydial infections. ADDED activity versus M avium complex, toxoplasma, and M leprae
Mech: Binds 50S ribosomal subunit, prevents protein synthesis, bacteriostatic
Pharm: Oral, longer half life (4 hrs), dosed 2x daily
Toxic: GI upsets, hepatotoxicity, QTc prolongation, CYP450 inhibition

22

Linezolid

Use: MRSA, PRSP, and VRE strains
Mech: Binds 23S RNA of 50S subunit, bacteriostatic
Pharm: Oral, IV, hepatic clearance, HL 6 hr
Toxicity: Dose-related anemia, neuropathy, optic neuritis, serotonin syndrome with SSRI’s

23

Ciprofloaxin

Fluoroquinolone
Use: UTI’s, gastroenteritis, osteomyelitis, anthrax
Mech: inhibits DNA replication, binds DNA gyrase and topoisomerase IV. Bactericidal
Pharm: Oral and IV, mostly renal clearance, HL 4 hr, dosed every 12 hrs.
Toxic: GI upsets, CNS effects (dizziness, headaches), tendinitis in cartilage, contraindicated in young children and pregnancy

24

Moxifloaxin

Fluoroquinolone
Use: “respiratory” fluoroquinolone, gram + cocci and atypicals (chlamydia, mycoplasma), also M tuberculosis
Mech: inhibits DNA replication, binds DNA gyrase and topoisomerase IV. Bactericidal
Pharm: Oral and IV, hepatic clearance (don’t use in UTI’s), long half lives = once daily dosing
Toxic: GI upsets, CNS effects (dizziness, headaches), QTc prolongation – caution with use of antiarrhythmics

25

Levofloaxin

Fluoroquinolone
Use: “respiratory” fluoroquinolone w/ improved activity vs. Pneumococcus
Mech: inhibits DNA replication, binds DNA gyrase and topoisomerase IV. Bactericidal
Pharm: Oral and IV, renal clearance, once-daily dosing
Toxic: GI upsets, CNS effects (dizziness, headaches), QTc prolongation – caution with use of antiarrhythmics

26

Metronidazole

Use: Anaerobic bacterial infections and C. dificile colitis, vaginitis
Mech: Disrupts electron transport chain, bactericidal
Pharm: oral and IV, hepatic clearance, HL 8 hrs
Toxic: GI upset, neuropathy, avoid alcohol (disulfram-like effect)

27

Sulfamethoxazole + trimethoprim

Anti-metabolite
Use: UTI’s, respiratory, ear, and sinus infections. P jiroveci pneumonia, toxoplasmosis, nocardiosis
Mech: folate antagonists, block purine and nucleic acid synthesis
Pharm: Oral and IV, renal clearance, HL 8 hrs
Toxicity: Rash, fever, bone marrow suppression, hyperkalemia, highly adverse effects in AIDS

28

Isoniazid

Use: First-line TB agent, treatment of latent TB, less active against other mycobacteria
Mech: inhibits mycolic acid synthesis, essential component of mycobacterial cell walls. Bactericidal
Pharm: Oral and IV, hepatic clearance, HL 1 hr, inhibits metabolism of carbamazepine, phenytoin, and warfarin
Toxic: Hepatotoxicity, peripheral neuropathy (use pyridoxine), hemolysis in G6PDH deficiency

29

Rifampin

Use: primary drug in combo to treat active TB, optional drug for LTBI
Mech: inhibits DNA-dependent RNA polymerase
Pharm: oral and IV, hepatic clearance, HL 3.5 hrs., induces CYP450, body fluids turn orange color
Toxicity: Rash, nephritis, thrombocytopenia, cholestasis, flu-like syndrome with intermittent dosing

30

Pyrazinamide

Use: component of TB treatment regimen
Mech: unknown, but requires bioactivation to pyrazoic acid. Bacteriostatic
Pharm: Oral, hepatic and renal clearance, dose 3x weekly, (may need to adjust dosages based on creatine levels in urine)
Toxicity: Hepatotoxic, hyperuricemia, polyarthralgia (40%), maculopapular rash, porphyria, photosensitivity. Avoid in PREGNANCY

31

Ethambutol

Use: Component of TB treatment regimen, given in initial 4-drug therapy, used in atypical mycobacterial infections
Mech: inhibits mycobacterial arabinosyl transferases (arabinoglycan = cell wall part)
Pharm: Oral, mostly renal clearance, HL 4 hrs, dose reduced in renal failure
Toxicity: Retrobulbar neuritis, visual disturbances (reversible), headache, confusion hyperuricemia.