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Infectious Disease Therapeutics > Macrolides/Tetracyclines/Glycopeptides > Flashcards

Macrolides/Tetracyclines/Glycopeptides Flashcards

1
Q

Macrolide Examples

A

Erythromycin
Clarithromycin
Azithromycin

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2
Q

Macrolide MOA

A

attach to the 23S rRNA on the 50S subunit of bacterial ribosome resulting in

inhibition of protein synthesis

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3
Q

Macrolide Killing??

A

Generally bacteriostatic; time dependent killing

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4
Q

Bacteria resistance to macrolides

A
  • Change to the binding site

methylation of the rRNA receptor
Inactivating enzymes (able to produce some enzyme that can mess with macrolide causing it to be inactive)
Active efflux (drug actively pumped out so cannot attach at the ribosome)

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5
Q

Macrolides spectrum of activity

A

Gram positive – pneumococci, streptococci and corynebacteria (reserved for penicillin allergic patients)
M pneumoniae
Chlamydia trachomatis –> STI
C. pneumophilia
Bordatella pertussis –> Whooping cough (beta-lactams ineffective)
Campylobacter jejuni –> Stomach/gut
Helicobacter pylori –>Stomach/gut

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6
Q

Erythromycin Route of Admin

A

IV or Oral

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7
Q

Adverse Effects of Erythromycin

A

Gi

Increased liver function tests (LFTs)

Cholestatic hepatitis – increased with estolate and pregnancy (dark urine and jaundice)

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8
Q

Drug Interaction Erythromycin

A

QT prolongation/cardiac arrhythmias particularly when combined with CYP 3A inhibitors –> Have to be alert for drug interactions

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9
Q

Clarithromycin and Azithromycin Spectrum of Activity

Just Azithro covers……

A

Active against staph and strep

  • Enhanced against:

L. pneumophilia (pneumonias) , Chlamydia trachomatis (STI), Chlaydiophila pneumoniae, Moraxella catarrhalis, H. influenzae (azithro), Mycobacterium avium complex and other mycobacteria

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10
Q

Clarithromycin and Azithromycin are useful for some…..

A

MRSA

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11
Q

Clarithromycin and Azithromycin have lower rates of….

A

G.I. adverse effects

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12
Q

Azithromycin is unique because….

A

Long half-life leads to long intracellular concentrations

5 days of azithromycin = 10days of therapy

Long periods of sub-inhibitory concentrations may lead to more resistance

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13
Q

Uses of Macrolides include…

A

Upper respiratory tract infections
Sexually transmitted infections
Acne –> effective

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14
Q

Macrolide Drug Interactions. Which one has the least interactions?

A

Significant number of DI especially with erythromycin and clarithromycin

Fewer with azithromycin (if pt is on. A lot of meds)

Erythromycin and clarithromycin are substrates and inhibitors of CYP 3A4

Long list of drugs that are metabolized by CYP 3A4, so E or C may increase the toxicity

Antiarryhthmics, antidepressants, benzodiazepines, anticonvulsants, statins (very common), anticonvuslasants, etc

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15
Q

Clindamycin MOA

A

same as macrolides

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16
Q

Clindamycin Spectrum

A

anaerobes, S. aureus including some MRSA as well as streptococci

17
Q

Clindamycin Use. Is it the drug of choice for any infections? Why?

A

Used in patients with penicillin allergies or with resistant organisms
Not DOC for any infections
Oral or parenteral –> Can be used in serious and minor infections

Associated the most of antibiotic caused diarhhea  worst culprit of Clostridium difficile infection

18
Q

Clindamycin Adverse Effects and Counselling Tip

A

Nausea, vomiting, diarrhea
Rash
Elevated LFTs–> not the same degree of macrolides

Esophageal irritation –> pt. counselling –> always be taken with liquid or water –>sit upright after taking it for awhile

Associated with C. difficile diarrhea

19
Q

Tetracycline Examples

A
  • tetracycline
  • minocycline
  • doxycycline
20
Q

Tetracycline MOA

A

inhibit binding of aminoacyl-tRNA to the 30S unit of ribosome thereby

inhibiting protein synthesis

21
Q

Tetracycline killing

A
  • Bacteriostatic
22
Q

Tetracyclines spectrum of activity

A

active against many gram positive and negative organisms but high rates of resistance (e.g. E. coli, S. pneumoniae)

drugs of choice for rickettsiae, Bartonella, chlamydiae and M. pneumoniae
Nocardia –> less common
P. acnes

23
Q

Adverse Effects of Tetracyclines and Contraindications

A

Gi upset (N, V, D)
Skin rashes
Photosensitivity
Yeast overgrowth –> vaginitis, skin inf (moist places), mouth inf
Deposited in bones and teeth; do not use in children < 8 years old (can cause discolouration of teeth as well as bone deformities)
Hepatitis

24
Q

Tetracycline Drug Interactions + Counselling

A

Some anticonvulsants may reduce tetracycline levels ( phenobarbital, phenytoin, carbamazepine) –> May not get eves high enough to treat the infection
Divalent and trivalent cations reduce absorption ( iron, bismuth, calcium, magnesium, aluminum); separate doses
Counsel pt’s –> do not take with multivitamin
Doxyxycline has less binding to calcium so therefore do not need to counsel on not taking with milk, etc.
Increased INR and bleeding with warfarin –> Increased bleeding

25
Q

Glycylcyclines Example

A

Synthetic analogue of tetracycline – tigecycline

26
Q

Tigecycline Spectrum

A

Active against many gp and gn organisms including MRSA, S. pneumoniae and enterococci, Salmonella, Shigella and Acinetobacter; also anaerobes

27
Q

Tigecycline eliminated through… and are for…

A

Eliminated through biliary tract and feces

Reserved for resistant organisms

28
Q

Glycopeptides Example

A

Vancomycin

29
Q

Glycopeptide MOA

A

– inhibits cell wall peptidoglycan synthesis

  • Bactericidal
30
Q

Glycopeptides resistance

A
  • VRE, S. aureus (VISA)
31
Q

Vancomycin Spectrum

A

gpc in particular enterococci, PRSP (penicillin resistant streptococcus pneumonaie) and MRSA (pt who is very ill with MRSA); active against clostridia, Clostrioides and some bacilli

32
Q

Vancomycin is the DOC for

A

Vancomycin is the drug of choice for C. Diff Infection (any antibiotic can produce C. Diff but the more narrow the less chance of infection

33
Q

Vancomycin Route of Admin

A

IV for serious infections

PO only for C. difficile; not orally absorbed

34
Q

Adverse Effects of Vancomycin

A

Nephrotoxicity – especially in combination with nephrotoxins –> damage to the kidneys
Ototoxicity –> Manifests as hearing impairement; or imbalances (not usually)
Red-man syndrome (red-neck syndrome) –> person turns red, uncomfortable, associated with hypotension, pt fees nauseated, flushed, uncomfortable –> can be reduced by reducing the infusion rate
–> Need to keep in mind of infusion rate –> if to fast, every one will get RMS
- 500 mg infused over an hour –> long infusion rates
Granulocytopenia –> long term use

Infectious Disease Therapeutics (17 decks)

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