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Pharm > Antibacterials - Protein Synthesis Inhibitors > Flashcards

Antibacterials - Protein Synthesis Inhibitors Flashcards

1
Q

List the types of protein synthesis inhibitors?

A
  1. Tetracyclines
  2. Glycylcyclines
  3. Aminoglycosides
  4. Macrolides
  5. Chloramphenicol
  6. Clindamycin
  7. Streptogramins
  8. Linezolid
  9. Mupirocin
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2
Q

What is the MOA of protein synthesis inhibitors?

A

MOA: bind to and interfere with ribosome since bacterial ribosomes (70S: 30S+50S) differ from mammalian ribosomes (80S); mostly bacteriostatic

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3
Q

What are the 3 Tetracyclines, their MOA, and 3 mechanisms of widspread resistance (plasma meadiated)?

A

Doxyxycline, Minocycline, Tetracycline

MOA: passive diffusion & energy-dependent transport to bind reversibly to 30S subunit of ribosome

  1. Impaired influx or increased efflux
  2. Production of proteins that interfere with bindind to ribosomes
  3. Enzymatic inactivation
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4
Q

What are the clinical applicatrions of tetracyclines?

A
  • severe acne/rosacea,
  • Empiric therapy of community-acquired PNA,
  • Infections of (respiratory tract, sinuses, middle ear, urinary tract, intestines), atypical PNAs (Mycoplasma, Chlamydia, Legionella)
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5
Q

What are the pharmacokinetics of tetracylcines?

A
  • Variable oral absoprtion because of divalent & trivalent cations
  • Doxycycline is lipid soluble (STDs and prostatitis)
  • Excreted by urine except doxycycline in bile
  • Teratogenic - cross placenta and excreted in breast milk
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6
Q

What are the adverse effect of Tetracyclines?

A
  • Discoloration & hyperplasia of teeth, stunting of growth
  • Photosensitization
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7
Q

What is the Glycylcycline drug and what differentiate it from the other protein inhibitors and what is its clinical applications?

A

Tigecycline

  • Broad-spectrum against multidrug-resistant gram postive/negative & anaerobic organisms
  • Little resistance
  • CA: treatment of complicated skin, soft tissue, and intra-abdominal infections (black box warning of increased mortaility)
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8
Q

What are the PK/AE of glycylcyclines?

A
  • IV only with primarily bile/fecal elimination
  • Well tolerated with AE similar to tetracyclines
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9
Q

What are the Aminoglycosides and what differentiates them?

A

Amikacin, Gentamicin, Tobramycin, Streptomycin, Neomycin

  • Bactericidal
  • Serious toxicites
  • Largely replaced by safer antibiotics
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10
Q

What is the MOA and specturm of aminoglycosides?

A

MOA: covalently bind to 30S ribosomal subunit; passively diffuse across membranes of gram negative or active O2 dependent transport

  • Mostly aerobic Gram-negative bactera
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11
Q

What are the 3 principal mechamisns of aminoglycosides resistance?

A
  1. Plasmid-associated synthesis of enzymes that modify/inactivate drug by acetylation, phosphorylation, and adenylation
  2. Decreased accumulation of drug
  3. Receptor protein on 30S ribosomal subinit maybe deleted or altered due to mutation
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12
Q

What are the clinical application of aminoglycosides?

A
  • Used mostly in combination
  • Emperic therapy of serious infection (septicemia, nocosomial RTIs, complicated UTIs, endocarditis with vancomycin)
  • Neomycin for bowel surgery, hepatic enchephalophathy, and topically
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13
Q

What are the pharmacokinetic factors of aminoglycosides?

A
  • Paraenteral administration only
  • Once daily administration
  • High levels in renal cortex and inner ear
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14
Q

What are the adverse effects of amioglycosides?

A
  • Both time and concentration dependent
  • Ototoxicity
  • Nephrotoxicity
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15
Q

What is oral Neomycin comonly used for?

A

Adjunct or alternative treatment for hepatic encephalopathy

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16
Q

What is the MOA and AE of Lactulose?

A

MOA: degreded by intestinal bacteria > lactic acid + other organic acids > acidfication of gut lumen > formation of NH4+ > reduced plamsa ammonia concentration

AE: osmotic diarrhea, flatulence, abdominal cramping

17
Q

What are the Macrolides, their MOA, and specturm?

A

Erythromycin, Clarithromycin, Azithromycin, Telithromycin

MOA: reversibly bind to 23S rRNA of the 50S subunit

Spectrum: mostly gram positive

18
Q

What are the clinical application of macrolides?

A
  • Empiric therapy of community-acquired PNA
  • Treating atypical PNAs (mycopalsma, chlamydia, legionella)
  • Treating URIs and soft tissue infections
  • Common substitue for pts with penicillin allergy
19
Q

What are the PK and contraindication of macrolides?

A
  • CYP P450 inhibition (excepot azithromycin)
  • Dont use statins because of CYP P450 inhibition
  • Telithromycin has more severe symptoms so only for major illnesses
20
Q

What is the MOA, specturm, and AE of chloramphenicol?

A

MOA: binds reversibly to 50S ribosome subunit and can inhibit protein synthesis in mitochondrial ribosomes leading to bone marrow toxicity

Spectrum: very broad spectrum, never given systemically for minor infections because of AE

AE: bone marrow depression, Gray baby syndrome (cyanosis)

21
Q

What are the clinical applications and PK of chloramphenicol?

A
  • Serious infeciont resistant to less toxic drugs
  • Superior penetrability
  • VRE
  • Topical eye infections

PK: inhibits hepatic oxidases (3A4 & 2C9)

22
Q

What is the MOA and AE of Clindamycin?

A

MOA: binds to 50S subunit of ribosomes

AE: potentially fatal pseudomembranous colitis (superinfection of C. difficile)

23
Q

What are the clinical applications of Clindamycin?

A
  • Anaerobic infections
  • Skin and soft tissue infections
  • Alternative for prophylaxis in penicillin-allergic pts

Pharm (14 decks)

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