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Pharmacology > Antibacterial Drugs > Flashcards

Antibacterial Drugs Flashcards

1
Q

Penicillin G

A

Action: Block transpeptidase cross-linking of peptidoglycan; prototype beta-lactam.

Uses: Gram-positive organisms (S. pneumoniae, S. pyogenes, Actinomyces); N. meningitidis; T. palliduim.

Toxicity: Hypersensitivity reactions; hemolytic anemia.

Resistance: Penicillinase-sensitive.

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2
Q

Ampicillin

A

Action: Block transpeptidase cross-linking of peptidoglycan; aminopenicillin.

Uses: Extended-spectrum penicillin = H. influenzae, E. coli, L. monocytogenes, P. mirabilis, Salmonella, Shigella, enterococci.

Toxicity: Hypersensitivity reactions; rash; pseudomembranous colitis.

Resistance: Penicillinase-sensitive.

Other drugs in class: Amoxicillin.

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3
Q

Nafcillin

A

Action: Block transpeptidase cross-linking of peptidoglycan; penicillinase-resistant penicillin.

Uses: S. aureus (except MRSA).

Toxicity: Hypersensitivity reactions; interstitial nephritis.

Resistance: MRSA resistance via altered PBPs.

Other drugs in class: Oxacillin; dicloxacillin.

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4
Q

Piperacillin

A

Action: Block transpeptidase cross-linking of peptidoglycan; antipseudomonal.

Uses: Pseudomonas spp. and gram-negative rods.

Toxicity: Hypersensitivity reactions.

Resistance: Penicillinase-sensitive.

Other drugs in class: Ticarcillin.

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5
Q

Clavulanic acid

A

Action: β-lactamase inhibitor.

Uses: Added to penicillin antibiotics to protect the antibiotic from destruction by β-lactamase (penicillinase).

Other drugs in class: Sulbactam; tazobactam.

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6
Q

Cefazolin

A

Action: Block transpeptidase cross-linking of peptidoglycan; 1st generation cephalosporin.

Uses: Gram- positive cocci; Proteus mirabilis; E. coli, Klebsiella pneumoniae; used prior to surgery to prevent S. aureus wound infections.

Toxicity: Hypersensitivity reactions; vitamin K deficiency; increase nephrotoxicity of aminoglycosides.

Resistance: penicillinase-sensitive (better than PCN).

Other drugs in class: cephalexin.

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7
Q

Cefoxitin

A

Action: Block transpeptidase cross-linking of peptidoglycan; 2nd generation cephalosporin.

Uses: Gram-positive cocci; H. influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcescens.

Toxicity: Hypersensitivity reactions; vitamin K deficiency; increase nephrotoxicity of aminoglycosides.

Resistance: penicillinase-sensitive (better than PCN).

Other drugs in class: cefaclor; cefuroxime.

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8
Q

Ceftriaxone

A

Action: Block transpeptidase cross-linking of peptidoglycan; 3rd generation cephalosporin.

Uses: Serious gram-negative infections resistant to other β-lactams.

Toxicity: Hypersensitivity reactions; vitamin K deficiency; increase nephrotoxicity of aminoglycosides.

Resistance: penicillinase-sensitive (better than PCN).

Other drugs in class: cefotaxime; ceftazidime.

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9
Q

Cefepime

A

Action: Block transpeptidase cross-linking of peptidoglycan; 4th generation cephalosporin.

Uses: High activity against Pseudomonas and gram-positive organisms.

Toxicity: Hypersensitivity reactions; vitamin K deficiency; increase nephrotoxicity of aminoglycosides.

Resistance: penicillinase-sensitive (better than PCN).

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10
Q

Ceftaroline

A

Action: Block transpeptidase cross-linking of peptidoglycan; 5th generation cephalosporin.

Uses: Broad gram-positive and gram-negative organism coverage, including MRSA; does not cover Pseudomonas.

Toxicity: Hypersensitivity reactions; vitamin K deficiency; increase nephrotoxicity of aminoglycosides.

Resistance: penicillinase-sensitive (better than PCN).

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11
Q

Aztreonam

A

Action: Block transpeptidase cross-linking of peptidoglycan; monobactam.

Uses: Gram-negative rods only.

Toxicity: Well tolerated; GI upset.

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12
Q

Meropenem

A

Action: Block transpeptidase cross-linking of peptidoglycan; carbapenem; penicillinase-resistant.

Uses: Wide spectrum; gram-positive cocci; gram-negative rods; anaerobes.

Toxicity: GI distress; skin rash; CNS toxicity (seizures) at high plasma levels.

Other: Always administered with cilastatin (inhibitor of renal dehydropeptidase I) to increase inactivation of drug in renal tubules.

Other drugs in class: Imipenem; ertapenem; doripenem.

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13
Q

Vancomycin

A

Action: Inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors.

Uses: Gram positive only; serious, multidrug-resistant organisms, including MRSA, enterococci, and Clostridium difficile (oral dose for pseudomembranous colitis).

Toxicity: Well tolerated in general; nephrotoxicity, ototoxicity, thrombophlebitis; diffuse flushing (red man syndrome).

Resistance: Amino acid modification.

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14
Q

Daptomycin

A

Action: Rapid depolarization of the cell membrane.

Uses: Multi-resistant gram positives, notably VRE, MRSA, and corynebacteria.

Toxicity: Less serious and common (diarrhea, N/V, sore throat); more serious and uncommon (rhabdomyolysis, renal failure, asthmatic pulmonary eosinophilia).

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15
Q

Gentamicin

A

Action: Aminoglycoside protein synthesis inhibitor; binds 30S (inhibits initiation and translocation); mRNA misreading; bactericidal.

Uses: Severe gram-negative rod infections; synergistic with beta-lactams; neomycin for bowel surgery.

Toxicity: Nephrotoxicity; neuromuscular blockade; ototoxicity; teratogen.

Resistance: Inactivation by bacterial transferase enzymes.

Other: requires oxygen for uptake; no action against anaerobes.

Other drugs in class: Neomycin; amikacin; tobramycin; streptomycin.

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16
Q

Doxycycline

A

Action: Tetracycline protein synthesis inhibitor; binds 30S (prevent attachment of aminoacyl-tRNA); bacteriostatic.

Uses: B. burgdorferi; M. pneumoniae; Rickettsia; Chlamydia; used to treat acne.

Toxicity: GI distress; discoloration of teeth and inhibition of bone growth in children; photosensitivity; contraindicated in pregnancy.

Resistance: Plasmid-encoded transport pumps decrease uptake and increase efflux.

Other: Doxycycline eliminated fecally (use in renal failure); divalent cations inhibit gut absorption.

Other drugs in class: Tetracycline; minocycline.

17
Q

Azithromycin

A

Action: Macrolid protein synthesis inhibitor; binds the 23S rRNA of 50S (blocks translocation); bacteriostatic.

Uses: Atypical pneumonias (Mycoplasma, Chlamydia, Legionella); STDs (for Chlamydia); gram- positive cocci (streptococcal infections in patients allergic to penicillin).

Toxicity: Gastrointestinal motility issues, arrhythmia caused by prolonged QT, acute cholestatic hepatitis, rash, eosinophilia.

Resistance: Methylation of 23S rRNA-binding site.

Other drugs in class: Clarithromycin; erythromycin.

18
Q

Chloramphenicol

A

Action: Protein synthesis inhibitor; binds 50S (blocks peptidyltransferase); bacteriostatic.

Uses: Meningitis (H. influenzae, N. meningitidis, S. pneumoniae); rocky mountain spotted fever (Rickettsia rickettsii).

Toxicity: Anemia (dose dependent); aplastic anemia (dose independent); gray baby syndrome.

Resistance: Plasmid-encoded acetyltransferase inactivates drug.

19
Q

Clindamycin

A

Action: Lincosamide protein synthesis inhibitor; binds 50S (blocks translocation); bacteriostatic.

Uses: Anaerobic infections (e.g., Bacteroides spp., C. perfringens) above the diaphragm; GAS infections.

Toxicity: Pseudomembranous colitis (C. difficile overgrowth); fever; diarrhea.

20
Q

Sulfamethoxazole (SMX)

A

Action: Sulfonamide inhibitor of folate synthesis; competitive antagonist of dihydropteroate synthase (DHPS); bacteriostatic.

Uses: Gram-positive; gram-negative; Nocardia; Chlamydia; UTI.

Toxicity: Hypersensitivity reactions; hemolysis if G6PD deficient; nephrotoxicity (tubulointerstitial nephritis); photosensitivity; kernicterus in infants.

Resistance: altered DHPS; decreased uptake; increase PABA production.

Other drugs in class: Sulfisoxazole; sulfadiazine.

21
Q

Trimethoprim

A

Action: Inhibitor of folate synthesis; inhibits dihydrofolate reductase (DHFR); bacteriostatic.

Uses: Combination with sulfonamides (trimethoprim-sulfamethoxazole [TMP- SMX]), causing sequential block of folate synthesis; combination used for UTIs, Shigella, Salmonella, Pneumocystis jirovecii pneumonia treatment and prophylaxis, and toxoplasmosis prophylaxis.

Toxicity: Megaloblastic anemia; leukopenia; granulocytopenia.

22
Q

Ciprofloxacin

A

Action: Fluoroquinolone inhibitor of DNA gyrase (topoisomerase II) and topoisomerase IV; bactericidal.

Uses: Gram-negative rods of urinary and GI tracts (including Pseudomonas); Neisseria; some gram-positive organisms.

Toxicity: GI upset; superinfections; skin rashes; headache; dizziness; tendonitis; tendon rupture; leg cramps; myalgias.

Resistance: Mutation in DNA gyrase; plasmid-mediated resistance; efflux pumps.

Other drugs in class: Norfloxacin; levofloxacin; ofloxacin, sparfloxacin; moxifloxacin; gemifloxacin; enoxacin; nalidixic acid (quinolone).

23
Q

Metronidazole

A

Action: Damage bacterial DNA via free radical production; bactericidal; antiprotozoal.

Uses: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, anaerobes (Bacteroides, C. difficile); used with a proton pump inhibitor and clarithromycin for “triple therapy” against H. Pylori.

Toxicity: Disulfiram-like reaction (severe flushing, tachycardia, hypotension) with alcohol; headache; metallic taste.

24
Q

Quinupristin/Dalfopristin

A

Action: Streptogramin protein synthesis inhibitor; binds 50S; bacteriostatic.

Uses: E. faecium; MSSA and MRSA.

Toxicity: Venous inflammation; arthralgia.

25
Q

Rifampin

A

Action: Inhibits DNA-dependent RNA polymerase; rifamycins.

Uses: Mycobacterium tuberculosis; delays resistance to dapsone when used for leprosy; meningococcal prophylaxis and chemoprophylaxis for H. influenzae type B.

Toxicity: Minor hepatotoxicity and drug interactions (induces P-450); orange body fluids (nonhazardous side effect).

Other drugs in class: Rifabutin.

26
Q

Isoniazid

A

Action: Decreased synthesis of mycolic acid.

Uses: Mycobacterium tuberculosis; only agent used as solo prophylaxis against TB.

Toxicity: Neurotoxicity; hepatotoxicity; pyridoxine (vitamin B6) can prevent neurotoxicity and lupus.

Other: prodrug must be activated by bacterial catalase-peroxidase.

27
Q

Pyrazinamide

A

Action: Uncertain; thought to acidify intracellular environment.

Uses: Mycobacterium tuberculosis.

Toxicity: Hyperuricemia; hepatotoxicity; polyarthralgia.

28
Q

Ethambutol

A

Action: Decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase.

Uses: Mycobacterium tuberculosis.

Toxicity: Optic neuropathy (red-green color blindness).

29
Q

Linezolid

A

Action: Protein synthesis inhibitor; binds 50S; bacteriostatic.

Uses: Serious gram positives like VRE and MRSA.

Toxicity: Thrombocytopenia.

Pharmacology (17 decks)

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