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Other Protein Synthesis Inhibitor

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Presentation on theme: "Other Protein Synthesis Inhibitor"— Presentation transcript:

1 Other Protein Synthesis Inhibitor
Course Coordinator Jamaluddin Shaikh, Ph.D. School of Pharmacy, University of Nizwa Lecture 6 October 03, 2011

2 Other Protein Synthesis Inhibitor
Chloramphenicol Macrolids Erythromycin Clarithromycin Azithromycin Clindamycin 2

3 Chloramphenicol Active against a wide range of gram-positive and gram-negative organisms Because of its toxicity, its use is restricted However, it was previously used to life-threatening infections for which no alternatives exist

4 Chloramphenicol: Mechanism of Action
Binds to the bacterial 50S ribosomal subunit and inhibits protein synthesis by preventing peptide elongation

5 Chloramphenicol: Antibacterial Spectrum
Have a broad range of antibacterial activity Also effective against organisms other than bacteria, e.g., Rickettsia Rickettsia is a genus of non-motile, Gram-negative, non-sporeforming, highly pleomorphic bacteria that can present as cocci (0.1 μm in diameter), rods (1–4 μm long) or thread-like (10 μm long).

6 Chloramphenicol: Pharmacokinetics
Well absorbed orally Can also be given by intramuscular and intravenous routes Widely distributed and CSF penetration is excelent Mainly undergoes hepatic glucuronidation Half-life is 6 hours. In neonates this is prolonged due to the immaturity of the glucuronidation enzymes

7 Cholramphenicol: Adverse Effects
Hematologic Dose-related erythroid suppression is common, but in addition aplastic anemia occurs Gray baby syndrome The gray color is due to shock (hypotension and tissue hypoperfusion). Chloramphenicol accumulates in neonates (especially if premature) due to reduced glucuronidation in the immature liver Other effects Chloramphenicol can also cause sore mouth, diarrhea, encephalopathy and optic neuritis Erythroid: red-blood cell; Aplastic anemia: a condition where bone marrow does not produce sufficient new cells to replenish blood cells. Anemia refers to low red blood cell counts, but aplastic anemia patients have lower counts of all three blood cell types. Encephalopathy: disorder or disease of the brain. Optic neuritis: inflammation of the optic nerve

8 Chloramphenicol: Drug Interactions
Inhibits metabolism of alcohol, warfarin, phenytoin and theophylline. This can cause clinically important toxicity if effects and/or plasma concentrations of these drugs are not monitored closely and their dose modified accordingly

9 Chloramphenicol: Mechanisms of Resistance
Confered by R factor, which codes for an acetyl coenzyme A transferase that inactivates chloramphenicol Also due to the inability of chloramphenicol to penetrate the organism R-factor is an old name for a plasmid that codes for antibiotic resistance. Often, R-factors code for more than one antibiotic resistance factor: genes that encode resistance to unrelated antibiotics may be carried on a single R-factor

10 Other Protein Synthesis Inhibitor
Chloramphenicol Macrolids Erythromycin Clarithromycin Azithromycin Clindamycin 10

11 Erythromycin Uses include respiratory infections, whooping cough, Campylobacter enteritis, and non-specific urethritis A useful alternative to penicillin in penicillin-allergic patients Useful for skin infections such as low-grade cellulitis and infected acne, and is an acceptable drug for patients with an infective exacerbation of chronic bronchitis Urethritis is inflammation of the urethra; Cellulitis is a common skin infection caused by bacteria 11

12 Erythromycin: Mechanism of Action
Bind to a site on the bacterial 50S ribosomes, inhibiting the ribosomal translocation step of protein synthesis. 12

13 Erythromycin: Pharmacokinetics
Well absorbed orally Food delays its absorption but may reduce GI side effects Distributed adequately to most sites except the brain and CSF Inactivated by hepatic N-demethylation, less than 15% being eliminated unchanged in the urine 13

14 Erythromycin: Adverse Effects
Erythromycin is a remarkably safe antibiotic, and may be used in pregnancy and children Nausea, vomiting, diarrhea and abdominal cramps are the most common adverse effects reported Cholestatic jaundice has been reported following prolonged use cholestasis is a condition where bile cannot flow from the liver to the duodenum 14

15 Erythromycin: Drug Interactions
Erythromycin inhibits cytochrome P450 and causes accumulation of theophylline, warfarin and terfenadine. This can result in clinically important adverse effects 15

16 Comparison of Microlids
Erythromycin Azitromycin Clarithromycin T1/2 1-1.5 h 40-60 h 5 h (approx.) Intravenous preparation available Yes No Gastrointestinal adverse effects Common Less common Tissue penetration Reasonable Extremely high High 16

17 Clindamycin Same mechanism of action as macrolides
Useful against anaerobes, such as Bacteroides fragilis Mechanism of resistance is also the same as microlids Well absorbed by the oral route Distributes well into all body fluids except the CSF Undergoes extensive oxidative metabolism to inactive products Excreted into the bile or urine by glomerular filtration Side effects are skin rash and psudomembranous colitis 17

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