Antiinfectives (1 & 2) Enhancement Reviewer PDF
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NCM 106
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Summary
This document provides an overview of antibacterial drugs, including their mechanisms of action, types, and resistance. It details various classes of antibiotics, such as penicillins, macrolides, and cephalosporins, along with their specific mechanisms, examples, and adverse effects.
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PROPERTY BY: NCM 106 PHARMACOLOGY TEAM Overview of Microorganisms Types of Pathogens: Bacteria, Viruses, Protozoa, and Fungi. Their pathogenicity depends on their virulence. Bacteria: Prokaryotes (lack a true nucleus and nuclear membrane). ○ Shapes: Bacillus (rod-shap...
PROPERTY BY: NCM 106 PHARMACOLOGY TEAM Overview of Microorganisms Types of Pathogens: Bacteria, Viruses, Protozoa, and Fungi. Their pathogenicity depends on their virulence. Bacteria: Prokaryotes (lack a true nucleus and nuclear membrane). ○ Shapes: Bacillus (rod-shaped), Cocci (spherical); may form clusters (staphylococci) or chains (streptococci). ○ Classification by Staining: Gram-positive: Retain purple stain. Gram-negative: Do not retain stain; often more resistant to drugs. ○ Toxin Production: Some bacteria produce toxins, such as beta-lactamase, which promotes cell lysis. Mechanisms of Antibacterial Action Cell Wall Synthesis Inhibition: Disrupts cell structure, leading to cell death. Membrane Permeability Alteration: Compromises cell integrity. Protein Synthesis Inhibition: Prevents the formation of essential proteins. RNA and DNA Synthesis Inhibition: Disrupts genetic material, halting reproduction. Metabolism Interference: Alters cellular processes critical for survival. Types of Antibacterial Drugs Narrow-spectrum: Target specific pathogens. Broad-spectrum: Effective against a wide range of Gram-positive and Gram-negative bacteria. Drug Resistance NCM 106 TEAM Inherent Resistance: Natural immunity to certain drugs. Acquired Resistance: Developed through exposure to antibiotics. Hospital-acquired Infections: Often involve drug-resistant bacteria. Cross-resistance: Resistance to drugs with similar mechanisms. Antibiotic Combinations: ○ Additive: Combined effect equals the sum of individual effects. ○ Potentiative: One drug enhances the effect of the other. ○ Antagonistic: Drugs work against each other. Classes of Antibacterial Drugs and Key Agents Penicillins ○ Mechanism: Interfere with cell wall synthesis, bacteriostatic or bactericidal. ○ Common Types: Penicillin G: First penicillin, painful injectionG, short-acting. Penicillin V: Effective for mild infections. Broad-spectrum: Amoxicillin and Ampicillin, active against various Gram-negative organisms. Penicillinase-resistant: Dicloxacillin, Nafcillin, Oxacillin; effective against penicillinase-producing S. aureus. ○ Extended-Spectrum Penicillins: Effective against Pseudomonas aeruginosa and Gram-negative bacteria. ○ Adverse Effects: Allergic reactions, superinfections, organ toxicity. Beta-Lactamase Inhibitors ○ Action: Combine with penicillins (e.g., Amoxicillin-Clavulanic Acid) to inhibit bacterial enzymes, extending the antibacterial effect. ○ Examples: Clavulanic acid, Sulbactam, Tazobactam. PROPERTY BY: NCM 106 PHARMACOLOGY TEAM Cephalosporins (e.g., Ceftriaxone) ○ Mechanism: Cell wall synthesis inhibition, bactericidal. ○ Generations: Expanded activity across different Gram-negative bacteria as the generations progress. ○ Side Effects: GI disturbances, rash, headache; serious reactions include anaphylaxis, nephrotoxicity. Macrolides ○ Mechanism: Bind to ribosomes, inhibiting protein synthesis; bacteriostatic or bactericidal. ○ Examples: Erythromycin: Used for respiratory infections. Azithromycin: Broad use in respiratory and skin infections. ○ Adverse Reactions: GI disturbances, photosensitivity, hepatotoxicity; potential drug interactions with theophylline, carbamazepine, and warfarin. Extended Macrolide Group ○ Mechanism: they also inhibit protein synthesis, have a longer half-life and are administered once a day. ○ Example: clarithromycin Lincosamides (e.g., Clindamycin) ○ Action: Inhibits protein synthesis; effective against Gram-positive bacteria. ○ Adverse Reactions: GI disturbances, colitis, anaphylaxis. Glycopeptides (e.g., Vancomycin) ○ Mechanism: Inhibits cell wall synthesis; effective against drug-resistant Gram-positive bacteria. ○ Uses: MRSA infections, surgical prophylaxis for penicillin-allergic patients. ○ Adverse Reactions: Nephrotoxicity, ototoxicity, “red man syndrome” with rapid IV administration. NCM 106 TEAM Oxazolidinones ○ Mechanism: inhibit protein synthesis on the 50S ribosomal subunit of bacteria. This action prevents formation of 70s initiation complex, which is necessary for bacterial reproduction. ○ Example: Linezolid for Nosocomial pneumonia ○ tedizolid Ketolides (e.g., Telithromycin) ○ Use: Treats community-acquired pneumonia. ○ Adverse Reactions: Visual disturbances, liver failure, exacerbation of Myasthenia Gravis. Lipopeptides (e.g., Daptomycin) ○ Mechanism: Causes bacterial cell death; used for complex skin infections and septicemia. ○ Adverse Reactions: Increased bleeding risk, rhabdomyolysis. Tetracyclines (e.g., doxycycline) ○ Mechanism: Inhibits protein synthesis, broad-spectrum. ○ Uses: Respiratory infections, acne, STIs; avoid in pregnant women. ○ Side Effects: Photosensitivity, GI disturbances, tooth discoloration in children. Aminoglycosides (e.g., Gentamicin) ○ Mechanism: Protein synthesis inhibition; bactericidal, effective for serious infections. ○ Uses: Sepsis, meningitis, endocarditis. ○ Adverse Reactions: Ototoxicity, nephrotoxicity; careful monitoring of blood levels needed. Fluoroquinolones (e.g., Ciprofloxacin, Levofloxacin) ○ Mechanism: Inhibits DNA synthesis, effective against Gram-negative organisms. ○ Uses: UTIs, respiratory, skin infections. ○ Cautions: May cause CNS effects if given with NSAIDS, avoid antacids since it decreases absorption. Sulfonamides ○ Mechanism: Inhibits folic acid synthesis; bacteriostatic. ○ Uses: UTIs, ulcerative colitis ○ Adverse Reactions: Allergic reactions, photosensitivity, GI disturbances. Nitroimidazoles (e.g., Metronidazole) ○ Mechanism: Disrupts DNA synthesis in anaerobic bacteria and protozoa. ○ Uses: Anaerobic infections, C. difficile colitis, surgical prophylaxis. ○ Side Effects: Nausea, dizziness, metallic taste; disulfiram-like reaction with alcohol. PROPERTY BY: NCM 106 PHARMACOLOGY TEAM Patient Education and Nursing Considerations Compliance: Emphasize the importance of completing the entire course of antibiotics to prevent resistance. Fluid Intake: Advise increased fluids to prevent crystalluria (especially with sulfonamides and fluoroquinolones). Photosensitivity: Use sunscreen and avoid direct sunlight, especially with tetracyclines and sulfonamides. Drug Interactions: ○ Avoid combining with antacids (tetracyclines, fluoroquinolones). ○ Be cautious with oral contraceptives (reduced effectiveness with certain antibiotics). ○ Avoid alcohol with metronidazole (disulfiram reaction). Monitor for Side Effects: Report signs of superinfection (e.g., mouth ulcers), allergic reactions, and adverse effects (e.g., hearing loss with aminoglycosides). Administration Tips: ○ Take with food if GI upset occurs (unless contraindicated). ○ Chewable forms must be chewed thoroughly. ○ Store medications out of reach of children. NCM 106 TEAM