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Questions and Answers
Describe the mechanism for Class 1 antibiotics.
Describe the mechanism for Class 1 antibiotics.
Antibiotics which block specific metabolic steps that are essential to the microorganism (Trimethoprim, Sulfonamides). Agents that affect the nucleic acid metabolism (rifampin and quinolones).
Describe the mechanism for Class 2 antibiotics.
Describe the mechanism for Class 2 antibiotics.
Agents that inhibit synthesis of microbial cell walls. Includes Penicillins and Cephalosporins which are structurally similar (Beta-lactams).
Describe the mechanism for Class 3 antibiotics.
Describe the mechanism for Class 3 antibiotics.
Bacteriocidal agents that bind to the 30 S ribosomal subunit and alter protein synthesis, which eventually leads to cell death. Includes aminoglycosides.
Describe the mechanism for Class 4 antibiotics.
Describe the mechanism for Class 4 antibiotics.
Give examples of Class 1 antibiotics.
Give examples of Class 1 antibiotics.
Give examples of Class 2 antibiotics.
Give examples of Class 2 antibiotics.
Give examples of Class 3 antibiotics.
Give examples of Class 3 antibiotics.
Give examples of Class 4 antibiotics.
Give examples of Class 4 antibiotics.
Give examples of Class 5 antibiotics.
Give examples of Class 5 antibiotics.
Describe the purpose of Class 5 antibiotics.
Describe the purpose of Class 5 antibiotics.
What is the structure and function of Sulfonamides?
What is the structure and function of Sulfonamides?
What is the inhibitory mechanism of Sulfonamides?
What is the inhibitory mechanism of Sulfonamides?
What works synergistically with Sulfonamides?
What works synergistically with Sulfonamides?
What range of antimicrobial activity do Sulfonamides possess?
What range of antimicrobial activity do Sulfonamides possess?
What antimicrobial(s) is/are used in Nocardiosis (Nocardia spp.)?
What antimicrobial(s) is/are used in Nocardiosis (Nocardia spp.)?
What antimicrobial(s) are/is used in Toxoplasmosis?
What antimicrobial(s) are/is used in Toxoplasmosis?
What is co-trimoxazole and what is it commonly used to treat?
What is co-trimoxazole and what is it commonly used to treat?
What are some of the adverse reactions associated with Sulfonamides?
What are some of the adverse reactions associated with Sulfonamides?
What specific drug interactions are associated with Sulfonamides?
What specific drug interactions are associated with Sulfonamides?
What is the structure and function of fluoroquinolones?
What is the structure and function of fluoroquinolones?
Describe the mechanism of action of fluoroquinolones.
Describe the mechanism of action of fluoroquinolones.
What is the significance of inhibition of gyrase?
What is the significance of inhibition of gyrase?
What is the significance of topoisomerase IV inhibition?
What is the significance of topoisomerase IV inhibition?
Describe and list the newer fluoroquinolones and their bacterial spectrum.
Describe and list the newer fluoroquinolones and their bacterial spectrum.
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Study Notes
Class 1 Antibiotics
- Block specific metabolic steps essential to microorganisms.
- Include Trimethoprim, Sulfonamides, Rifampin, and Quinolones.
- Affect nucleic acid metabolism.
Class 2 Antibiotics
- Inhibit synthesis of microbial cell walls.
- Include Penicillins and Cephalosporins (structurally similar Beta-lactams).
Class 3 Antibiotics
- Bactericidal agents targeting the 30S ribosomal subunit.
- Alter protein synthesis leading to cell death.
- Include Aminoglycosides.
Class 4 Antibiotics
- Bacteriostatic agents affecting the 30S or 50S ribosomal subunit.
- Cause reversible inhibition of protein synthesis.
- Include Chloramphenicol, Tetracyclines, Macrolides, and Clindamycin.
Class 5 Antibiotics
- Target Mycobacterial diseases such as tuberculosis and leprosy.
- Include Isoniazid, Rifampin, Ethambutol, Streptomycin, Pyrazinamide, Dapsone, and Clofazimine.
Sulfonamides
- Bacteriostatic and structurally similar to PABA (p-aminobenzoic acid).
- Inhibit dihydropteroate synthesis, blocking folic acid production.
- Wide antimicrobial activity against gram-positive and gram-negative bacteria.
Synergistic Agents for Sulfonamides
- Trimethoprim works synergistically with Sulfonamides to enhance efficacy.
Clinical Uses of Sulfonamides
- Effective against Nocardiosis (Nocardia spp.).
- Used in combination with pyrethamine and sulfadiazine for Toxoplasmosis.
Co-trimoxazole
- Combination of sulfamethoxazole and trimethoprim.
- Commonly used to treat urinary tract infections and GI infections.
Adverse Reactions of Sulfonamides
- Urinary tract disturbances, acute hemolytic anemia, granulocytosis, aplastic anemia.
- Sulfa allergies and gastrointestinal issues such as nausea and vomiting.
Drug Interactions for Sulfonamides
- Interact with oral anticoagulants, sulfonylureas, hypoglycemic drugs, and hydantoin anticonvulsants.
Fluoroquinolones
- Synthetic fluoroquinolones are DNA gyrase inhibitors.
- Broad antimicrobial activity with minimal side effects.
Mechanism of Action of Fluoroquinolones
- Block bacterial DNA synthesis by inhibiting topoisomerase II (gyrase) primarily and topoisomerase IV secondarily.
Importance of Inhibition of Gyrase
- Prevents relaxation of supercoiled DNA necessary for transcription and replication.
Significance of Topoisomerase IV Inhibition
- Interferes with separation of replicated DNA during cell division.
Newer Fluoroquinolones
- Include Ciprofloxacin, Enoxacin, Lomefloxacin, Levofloxacin, Ofloxacin, and Pefloxacin.
- Exhibit broad-spectrum activity particularly against gram-negative bacteria.
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