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Block 9 - Reproductive and Endocrine Disease > Block 9 Drugs - Antimicrobials > Flashcards

Block 9 Drugs - Antimicrobials Flashcards

1
Q

Sulfonamides

A

Inhibitors of folate synthesis

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2
Q

Sulfamethoxazole

A

MOA: Inhibits incorporation of para-aminobenzoic acid (PABA) into dihydrofolate precursors

USE: acute UTI infections

S/E: Nephrotoxicity due to crystalluria

CI: Steven-Johnson Syndrome

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3
Q

Trimethoprim

A

MOA: Inhibits bacterial dihydrofolate reductase

USE: acute prostatitis, vaginitis, and UTI infections

S/E: Megaloblastic anemia, leukopenia, granulocytopenia

CI: Can lead to folic acid deficiency

UNIQUE: Co-administraton with Folinic acid (not metabolized by bacteria) and reverse side effects

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4
Q

Sulfamethoxazole + Trimethoprim (Cotrimoxazole)

A

MOA: Sequential inhibitors of folate metabolites

Bacterialcidal

USE:

  • chronic prostatitis vaginitis and UTI infections
  • Haemophilus influenza
  • opportunistic pneumonia in HIB patients
  • community acquired MRSA

S/E: -Nephrotoxicity due to crystalluria (sulfamethoxazole) -Megaloblastic anemia, leukopenia, granulocytopenia (trimethoprim)

CI: Stevens-Johnson syndrome (sulfamethoxazole)

UNIQUE: Combination at 5:1 sulfamethoxazole: trimethoprim synergistically superior to either drug alone

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5
Q

Inhibitors of bacterial cell wall biosynthesis

A

Penicillin, Methicillin, Amoxicillin, Cephalosporins, Carbapenems

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6
Q

Penicillin

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Gram + cocci, Gram + bacilli, Gram - cocci

Anaerobes-Clostridium

Spirochetes

S/E: Allergic hypersensitivity

Diarrhea

Nephritis

Neural, hematological and/or cation toxicities at high doses

CI: -

UNIQUE: Very effective for gonorrhea and syphilis

Pneumoccocal pneumonia

Penicillin V. - acid stable

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7
Q

Penicillin G

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis Bactericidal

USE: Gram + cocci, Gram + bacilli, Gram - cocci

Anaerobes-Clostridium

Spirochetes

S/E: Allergic hypersensitivity

Diarrhea

Nephritis

Neural, hematological and/or cation toxicities at high doses

CI: -

UNIQUE: Very effective for gonorrhea and syphilis

Pneumoccocal pneumonia

G:

  • Much more active against Gram+-bacteria.
  • Unstable in acid, susceptible to degradation by penicillinases (ß-lactamases)
    • Penicillinase-resistant derivatives much less susceptible to cleavage
    • Use only when known/strongly suspected that infecting bacteria produces penicillinase
  • Semi-synthetic penicillins derived to overcome these problems
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8
Q

Penicillin V

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis Bactericidal

USE: Gram + cocci, Gram + bacilli, Gram - cocci

Anaerobes-Clostridium

Spirochetes

S/E: Allergic hypersensitivity

Diarrhea

Nephritis

Neural, hematological and/or cation toxicities at high doses

CI: -

UNIQUE: Very effective for gonorrhea and syphilis

Pneumoccocal pneumonia

V:

  • ACID-STABLE: Better absorbed in active form from GI tract (Penicillin VK - K=potassium)
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9
Q

Methicillin

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: S. aureus

S/E: Acute interstital nephritis

CI: No longer used in patients

UP: Used routinely in the clinical laboratory to determine S. aureus sensitivity; MSSA vs. MRSA

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10
Q

Amoxicillin

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE:

Broader spectrum for Gram(-) than penicillin
Similar to penicillin for Gram(+)

S/E: Same as penicillin

Allergic hypersensitivity

Diarrhea

Nephritis

Neural, hematological and/or cation toxicities at high doses

CI: Not useful for intestinal microbe infections due to complete absorption

Unique: Stable in acid (used with clavulanic acid)

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11
Q

Cephalosporins

All have -cef or -ceph

A

MOA: Inhibit transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Generation dependent

S/E: Hypersensitivity reactions (3-4x’s more likely if already allergic to penicillin)

Severe reactions to penicillin preclude use

CI: Hypersensitivity to penicillin risk

nephrotoxic in patients w/ preexisting renal disease

Unique: Affected by same resistance mechanicisms as penicillins

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12
Q

Cephalothin (1st gen)

*note: there’s a whole lot more drugs in the lecture for each generation than the table. I’ll wait until the actual lecture and then if they’re things I’ll add them (yes I know they’ll probably be things. I’ll add them)

A

MOA: Inhibit transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: alternate to penicillin; prophylaxis during and after surgery

S/E: hypersensitivity reaction

Severe reactions to penicillin preclude use

CI: hypersensitivity to penicillin risk (guys I think there’s a trend here)

Unique: Affected by same resistance mechanisms to penicillins

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13
Q

Cefamandole (2nd gen)

A

MOA: Inhibit transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Greater activity against some Gram(-); weaker for Gram(+)

S/E: hypersensitivity reaction

Severe reactions to penicillin preclude use

CI: hypersensitivity to penicillin risk (guys I think there’s a trend here)

Unique: Affected by same resistance mechanisms to penicillins

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14
Q

Cefotaxime (3rd gen)

A

MOA: Inhibit transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Enhanced activity against Gram(-) bacilli and enterics (drugs of choice for meningitis)

S/E: hypersensitivity reaction

Severe reactions to penicillin preclude use

CI: hypersensitivity to penicillin risk (guys I think there’s a trend here)

Unique: Affected by same resistance mechanisms to penicillins

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15
Q

Cefepime (4th gen)

A

MOA: Inhibit transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Broad spectrum: staphylocci and streptococci; P. aeruginosa

S/E: hypersensitivity reaction

Severe reactions to penicillin preclude use

CI: hypersensitivity to penicillin risk (guys I think there’s a trend here)

Unique: Affected by same resistance mechanisms to penicillins

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16
Q

Imipenem (Carbapenems)

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Active against ß-lactamase producing Gram(+) and Gram(-); anaerobes; P. aeruginosa

S/E: Nausea, vomiting, diarrhea; Seizures possible at high conc.

CI: MRSA still resistant

Unique: Resistant to most ß-lactamases except metalloclass

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17
Q

Aztreonam (Carbapenems)

A

MOA: Inhibit the transpeptidase responsible for peptidoglycan synthesis

Bactericidal

USE: Gram(-) rods; usually for Enterobacter sp.; P. aeruginosa

S/E: Minor; phlebitis, skin rash, abnormal liver enzymes

CI: No activity for Gram (+) or anaerobes

Unique: Can be used in patients with penicillin and/or cephalosporin hypersensitivity

Resistant to ß-lactamases

Good at maintaining population of gut gram (+) and anaerobes

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18
Q

Vancomycin (Carbapenems)

A

MOA: Inhibits bacterial cell wall lipid biosynthesis and polymerization of peptidoglycan

Bactericidal

USE: Gram (=) microbes especially MRSA and enterococcal sp.

Can act synergistically with aminoglycosides

S/E: Fever and chills

Infusion associated histamine shock

Nephrotoxicities

CI: Intravenous - toxic if given too rapidly (red-man syndrome)

Oral tablets used for severe C. difficile infection

Unique: Effective for drug resistant S. aureus and enterococci

Clinical decision to use for severe C. difficile treatments vs. risk of emerging hospital resistant strains

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19
Q

Bacitracin (Carbapenems)

A

MOA: Binds to bacterial cell wall isoprenyl-pyriphosphate sterols in wall membrane

USE:

S/E: Nephritis (if used internally)

CI: Primarily for topical use

Unique: Effective for topical application of minor skin wounds, but not for punctures or larger wounds

20
Q

Clavulanic acid (Beta-lactamase Inhibitor)

A

MOA: Active site inhibitor of ß-lactamase; likely causes irreversible denaturation of target enzyme

No bacteriostatic or bactericidal activity

USE: Any microbe being targeted with ß-lactam antibiotics (usually a penicillin class)

S/E: May enhance penicillin class side-effects when used in combination

Mild GI symptoms

CI: Use only when target microbe is susceptible to ß-lactam inhibitors; usually amoxicillin

Unique: Used to inhibit the ß-lactamases of the target microbe, allowing ß-lactam antibiotics to remain active

DOES NOT inhibit cephalosporinase

21
Q

Sublactam (Beta-lactamase inhibitor)

A

MOA: Inhibit ß-lactamase

No bacteriostatic or bactericidal activity

USE: Same as Clavulanic acid - Any microbe being targeted with ß-lactam antibiotics (usually a penicillin class)

S/E: Same as Clavulanic acid - May enhance penicillin class side-effects when used in combination

Mild GI symptoms

CI: Use only when target microbe is susceptible to ß-lactam inhibitors; usually ampicillin

Unique: Same as Clavulanic acid - Used to inhibit the ß-lactamases of the target microbe, allowing ß-lactam antibiotics to remain active

DOES NOT inhibit cephalosporinase

22
Q

Chloramphenicol (Beta-lactamase inhibitor)

A

MOA: Binds to peptidyl transferase center of the 50s ribosome subunit, preventing the attachment of the incoming AA-tRNA

Bateriostatic

USE: Broad spectrum

No longer used except for life threating organism when there are no other drug options available

S/E: Aplastic anemia

Gray baby syndrome: can accumulate in neonates due to inability to metabolize drug; can lead to cyanosis

Leukopenia

CI: May have toxicity toward mitochondria eukaryotic ribosomes

Unique: Resistance due to

  1. inactivation by bacterial acetyl-transferases
  2. poor penetration/uptake
23
Q

Azithromycin (Macrolides-Erythromycin 1st in class)

A

MOA: Binds irreversibly to the peptidyl transferase center of the 50s ribosome subunit, preventing any translocation and elongation

Bacteriostatic but -cidal at high concentrations

USE: L. pneumophilia, M. pneumonia, C. jejuni, Chlamydia

Mycobacteria-avium intracellulare (AIDS patients)

Penicillin-resistant microbes

Diptheria carrier state

Bordetella pertussis

S/E: GI distress

Hepatotoxicity, jaundice

Ototoxicity

CI: Avoid in patients with underlying liver disease, as macrolides can accumulate in the liver

Unique: Resistance due to:

  1. decreased uptake
  2. methylation of the ribosomal target protein
  3. esterase modification of the drug

[Erythromycin rarely used now as other macrolides are less toxic and more effective]

24
Q

Clindamycin (lincosamide)

A

MOA: Binds irreversibly to peptidyl transferase center of the 50s ribosome subunit, preventing any translocation and elongation

Bacteriostatic but -cidal at high concentration

USE: anaerobes, esp. B. fragilis

Some MRSA

S/E: Same as macrolides

GI distress

Hepatotoxicity, jaundice

Ototoxicity

CI: Avoid in pts with underlying liver or kidney disease

Unique: Resistance due to:

  1. decreased uptake
  2. methylation of the ribosomal target protein
  3. esterase modification of the drug
25
Q

Tetracyclines

A

Inhibitors of Protein Synthesis

Interference with tRNA binding

26
Q

Tetracycline

A

MOA: Bind to the 30S ribosoomal subunit and prevent assocation of the [AA-tRNA] complex with tthe A site on 70S ribosome

USE: Rickettsia (Rocky Mountain spotted fever)

Cholera

Chlamydia

  • Mycoplasma pneumonia*
  • B. burgdorferi* (Lyme disease)

brucellosis

anthrax

S/E: Photosensitivity (sunburn)

GI distress

Hepatotoxicity

Deposition in bones and teeth (dicoloration); limited use in pediatric patients

Hypersensitivity

CI: Cross resistance common across each tetracycline (excpet tigecycline)

Risk to fetus during pregnancy

Unique: Resistance due to:

  1. decreased accumulation of the drug-efflux
  2. enzymatic inactivation
  3. decreased access of the drug to the ribosome

Each drug in the class has similar resistance mechanisms

27
Q

Doxycycline

A

MOA: Bind to the 30S ribosoomal subunit and prevent assocation of the [AA-tRNA] complex with tthe A site on 70S ribosome

USE: Rickettsia (Rocky Mountain spotted fever)

Cholera

Chlamydia

Mycoplasma pneumonia

B. burgdorferi (Lyme disease)

brucellosis

anthrax

S/E: Photosensitivity (sunburn)

GI distress

Hepatotoxicity

Deposition in bones and teeth (dicoloration); limited use in pediatric patients

Hypersensitivity

CI: Cross resistance common across each tetracycline (except tigecycline)

Risk to fetus during pregnancy

Unique: **Most commonly used tetracycline class drug**

Resistance due to:

decreased accumulation of the drug-efflux

enzymatic inactivation

decreased access of the drug to the ribosome

Each drug in the class has similar resistance mechanisms

28
Q

Minocycline

A

MOA: Bind to the 30S ribosoomal subunit and prevent assocation of the [AA-tRNA] complex with tthe A site on 70S ribosome

USE: Rickettsia (Rocky Mountain spotted fever)

Cholera

Chlamydia

Mycoplasma pneumonia

B. burgdorferi (Lyme disease)

brucellosis

anthrax

S/E: Photosensitivity (sunburn)

GI distress

Hepatotoxicity

Deposition in bones and teeth (dicoloration); limited use in pediatric patients

Hypersensitivity

Concentrates in the endolymph of the ear: dizziness, vertigo, tinnitus

CI: Cross resistance common across each tetracycline (except tigecycline)

Risk to fetus during pregnancy

Unique: **Effective in getting into cerebrospinal fluid (CSF)**

Resistance due to:

decreased accumulation of the drug-efflux

enzymatic inactivation

decreased access of the drug to the ribosome

Each drug in the class has similar resistance mechanisms

29
Q

Tigecycline

A

MOA: Bind to the 30S ribosoomal subunit and prevent assocation of the [AA-tRNA] complex with tthe A site on 70S ribosome

USE: Vancomycin resistant MRSA

S/E: Significant nausea & vomiting

Acute pancreatis

other SE similar to tetracycline (Photosensitivity, Gi distress, hepatotoxicity, etc.)

CI: Not cross-resistant with other tetracyclines

Risk to fetus during pregnancy

Unique: Glycyl cyclic derivative of monocycline

30
Q

Mupirocin

A

MOA: Inhibits bacterial protein synthesis by binding specifically to isoleucyl-tRNA synthetase

Inhibitors of protein synthesis, inhibitor of tRNA synthetases

USE: Topical (nasal) MRSA infections

ONLY used topically - rapidly inactivated upon absorption

31
Q

Aminoglycosides

A

Inhibitors of Protein Synthesis

Alteration of mRNA translation and chain initiation

32
Q

Streptomycin (aminoglycoside)

A

MOA: Interacts specifically with 30s subunit of ribosome, blocks the initiation process

Bactericidal

USE: Enterococci (+ ß-lactam)

Y. pestis (+ ß-lactam)

S/E: Ototoxicity*

Nephrotoxicity*

*Elderly particularly sensitive to both

Neuromuscular paralysis if pushed rapidly IV

CI: Plasma levels of drug should be monitored

Unique: Usually used in combination with other antibiotics

Resistance due to:

  1. Acetly-, nucleotidyl and phospho- transferase modifcations to drug
  2. Decreased uptake
  3. Mutation of S12 protein
33
Q

Tobramycin (aminoglycosides)

A

MOA: Interacts specifically with 30s subunit of ribosome, blocks the initiation process

Bactericidal

USE: P. aeruginosa (+ ß-lactam)

S/E: Ototoxicity*

Nephrotoxicity*

*Elderly particularly sensitive to both

Neuromuscular paralysis if pushed rapidly IV

CI: Plasma levels of drug should be monitored

Unique: Usually used in combination with other antibiotics

Resistance due to:

Acetly-, nucleotidyl and phospho- transferase modifcations to drug

Decreased uptake

Mutation of S12 protein

34
Q

Gentamicin (aminoglycosides)

A

MOA: Interacts specifically with 30s subunit of ribosome, blocks the initiation process

Bactericidal

USE: Francisella tularemia

  • Brucella sp* (+ doxycycline)
  • Klebsiella sp* (+ ß-lactam)

S/E: Ototoxicity*

Nephrotoxicity*

*Elderly particularly sensitive to both

Neuromuscular paralysis if pushed rapidly IV

CI: Plasma levels of drug should be monitored

Unique: Usually used in combination with other antibiotics

Resistance due to:

Acetly-, nucleotidyl and phospho- transferase modifcations to drug

Decreased uptake

Mutation of S12 protein

35
Q

Amikacin (aminoglycosides)

A

MOA: Interacts specifically with 30s subunit of ribosome, blocks the initiation process

Bactericidal

USE: P. aeruginosa

  • Acinetobacter sp.*
  • Enterobacter*
  • S. marcescens*

2nd line mycobacteria TB

S/E: Ototoxicity*

Nephrotoxicity*

*Elderly particularly sensitive to both

Neuromuscular paralysis if pushed rapidly IV

CI: Plasma levels of drug should be monitored

Unique: Uniquely resistant to drug modifying enzymes

Usually used in combination with other antibiotics

Resistance due to:

Acetly-, nucleotidyl and phospho- transferase modifcations to drug

Decreased uptake

Mutation of S12 protein

36
Q

Linezolid (Oxazolidinones)

A

MOA: Binds to the 23S rRNA in the 50s ribosomal subunit and interferes with the formation of the initiation complex

Bacteriostatic

(Oxazolidinones - alteration of mRNA translation and chain initiation)

USE: treatement of vancomycin-resistant S. aureus (VRSA) and vancomycin-resistant Enterococcus (VRE)

S/E: GI; nausea, diarrhea

Thrombocytopenia, anemia, neutropenia

CI: Weak MAOI activity; careful with other serotonergic meds (e.g. SSRIs)

Unique: Primarily used for drug resistant gram (+) microbes

37
Q

Ciprofloxacin (Fluoroquinolones)

A

MOA: Inhibit bacterial DNA gyrase (topoisomerase II) and DNA topoisomerase IV

Forms a complex with DNA and gyrase, results in DNA cleavage

USE: Urinary tract infections

Anthrax

Enterobacter sp.

P. aeruginosa in cystic fibrosis patients

Effective for intracellular microbes

S/E: nausea, vomiting, diarrhea

May damage growing cartilage - arthropathy; avoid in patients < 18 y/o

Tendonitis, tendon rupture

Can prolong QT interval

CI: Not effective for MRSA, enterococci and pneumococci

Avoid in pregnancy or during lactation due to arthropathy concers

Unique: Enter bacteria via porins in the outer membrane

Resistance due to mutations in gyrase and topoisomerase

Increased efflux and decreased porins

38
Q

Daptomycin

A

MOA: Cyclic lipopeptide binds to bacterial cytoplasmic membrane causing rapid deploarization

Disrupts all membrane and functional activities

Bactericidal

USE: Gram(+) cocci, including VRE, MRSA, and MSSA

Gram (+) bacilli

S/E: Nausea, Dizziness, Headache

CI: Should not be used for pneumonias due to inactivation by pulmonary surfactants

Unique: Different mechanism of action than other antibiotics

*Alternative to Vancomycin

Increased MIC can occur with prolonged use

39
Q

Metronidazole

A

MOA: Reduction of the drug by enzymes that perform the phosphoroclastic reaction produce a reactive drug product that interferes with DNA replication

Bactericidal

USE: anaerobic microorganisms which carryout the phosphoroclastic reaction

S/E: GI upset; nausea, diarrhea

Rash

CI: Avoid in pregnancy

Avoid alcohol; disulfram reaction w/ alcohol

Unique: Selectivity based on mammalian cells not performing the phosphoroclastic reaction

40
Q

Nitrofurans

A

MOA: reduced to toxic, hihgly reactive intermediates by bacterial enzymes; binds covalently to DNA

USE: UTI

S/E: Nausea

Pulmonary fibrosis risk in long-term use

Unique: Selectivity; drug reduced more rapidly by bacterial enzymes than mammalian

41
Q

Isoniazid

A

MOA: Antitubercular agent

Prodrug activated by mycobacterial catalase-peroxidase that inhibits synthesis of long chain mycolic acids unique to mycobacterial cell walls

USE: M. tuberculosis

S/E: Peripheral neuritis

Hepatitis and idiosyncratic hepatotoxicity

CI: MAOI activity; avoid serotonergic meds (e.g. SSRIs)

Unique: Bacteriostatic for non-dividing mycobacteria; bactericidal for dividing cells

Resistance due to chromosomal mutations in the catalase-peroxidase gene

42
Q

Rifampin

A

MOA: Antitubercular agents

Blocks transcription by inhibiting the beta subunit of mycobacterial DNA dependent RNA polymerase

Bactericidal

USE: Active for both intracellular and extracellular mycobacteria

S/E: Mild, nausea, vomiting, rash

Hepatotoxicity, jaundice; check LFTs (liver enzyme tests)

CI: Never given as a single agent due to rapid drug resistance

Inducer of P450s; may affect other drugs

Unique: Most active anti-leprosy drug

Not active agaianst the beta subunit of the human enzyme

43
Q

Rifabutin

A

MOA: Antitubercular Agent

Similar to Rifampin - blocks transcription by inhibiting the beta subunit of mycobacterial DNA dependent RNA polymerase

Bactericidal

USE: TB in HIV patients

Also from Mycobacteria avium complex

S/E: Similar to Rifampin - Mild, nausea, vomiting, rash

Hepatotoxicity, jaundice, check LFTs

Unique: Used for treating TB in HIV patients; not potent inducer of P450s

44
Q

Pyrazinamide

A

MOA: Antitubercular Agent

Mechanism unknown 🤷🏻‍♀️

mycolic acid synthese affected

Bactericidal

USE: Active against tubercle bacilli in lysosomes and macrophages

S/E: Possible liver dysfunction in combination treatments

Hyperuricemia/Gout

Unique: Used only in combination with isoniazid, rifampin, & ethambutol

45
Q

Ethambutol

A

MOA: Antitubercular Agents

Inhibits arabinosyl-transferase involved in arabinogalactan cell wall biosynthesis

USE: M. tuberculosis and M. kansasii

S/E: Optic neuritis with blurred vision

Unique: Unique drug target; Drug resistance is low when used in drug combinations

Block 9 - Reproductive and Endocrine Disease (22 decks)

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