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17 Cards in this Set

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MOA of lincoamides:
- 50S subunit ribosomal subunit
- inhibit bacterial protein synthesis
Drug - Drug Interaction:
- Macrolides and chloramphenicol
- Binding of one of the antibiotics to the ribosome may inhibit the interaction of the others.
- May potentiate effects of neuromuscular blockers.
Clindamycin: (PO) no worry about food.
Palmitate vs. Phosphate:
Clindamycin Palmitate: inactive prodrug
Where can lincosamides accumulate:

NOT IN CNS
1. polymorph leukocytes
2. alveolar macrophages
3. abscesses
Resistance occurs with lincoamides from:
- alteration of binding site on the 50S ribosomal unit (methylation).
Adverse Effect of lincoamides:
1. Diarrhea
2. Pseudomembranous enterocollitis
3. Rashes
How does chloramphenicol work?
- Works by inhibiting PEPTIDYLTRANSFERASE (of mammalian NOT cytoplasmic)
with binding of new a.a. to nascent polypeptide chain.
Chloramphenicol where does it bind?
50S ribosomal subunit -- inhibiting bacterial protein synthess.
- BACTERIOSTATIC (increase cidal at higher dose: N. meningitis, H. influenza, S. pneumoniae
Chloramphenicol can inhibit:
mammalian mitochondrial > cytoplasmic ribo because they resemble bacterial ribo.
Resistance to chloramphenicol:
CAT inactivates the drug --> acetylated derivative fails to bind to bacterial ribosomes.
Chloramphenicol Succinate:
- parenteral adm. --> water soluble prodrug.
- distibuted everywhere
How is this chloramphenicol excreted?
- hepatic metabolism --> inactive drug
- tubular secretion and glomerular filtration.
Chloramphenicol adverse reactions:
- hypersentivity:
1. Jarish-Herxheimer
2. Macular or Vesicular skin rashes
Gray Baby Syndrome:
1. flaccidity
2. cynaosis
3. shock
4. CV collapse
Chloramphenicol MOA for gray baby syndrome:
- decreased glucuronide formation
- decreased excretion of unconjugated drug.
More A.E. of chloramphenicol
- dose - related bone marrow depression: anemia, leukopenia, thrombocytopenia
(REVERSIBLE)
Chloramphenicol:
- inhibits microsomal cytochrome p450 .
Aplastic anemia leading to fatal pancytopenia
--- due to prolonged therapy, exposure to drug more than once, genetic predisposition.
Lincoamides we want to reduce dosage in
hepatic and renal
b. fragilis can treat.